Alpha4 beta7 integrin modulators and their use
A novel compound targeting alpha 4 β 7 integrin with selective inhibition properties addresses the limitations of current IBD treatments by providing an orally administrable option with reduced side effects, effectively managing IBD symptoms.
Patent Information
- Application Number
- JP2024566739
- Authority / Receiving Office
- JP · JP
- Patent Type
- Applications
- Current Assignee / Owner
- Priority Date
- 2023-04-21
- Filing Date
- 2023-05-12
- Publication Date
- 2025-06-03
AI Technical Summary
Current treatments for inflammatory bowel disease (IBD), such as ENTYVIO (vedolizumab), require parenteral administration and are associated with significant side effects due to their long half-life, necessitating the development of an orally administrable, highly active, and selective alpha 4 β 7 small-molecule inhibitor with reduced side effects.
A compound with the structure of formula (I) or its pharmaceutically acceptable salt/solvate, where A is selected from specific nitrogen and carbon-containing groups, and R groups are defined to include various substituents, is provided. This compound is designed to selectively inhibit alpha 4 β 7 integrin, offering oral administration and reduced side effects.
The compound effectively modulates alpha 4 β 7 integrin, providing significant anti-inflammatory effects and symptom reduction for IBD patients while minimizing side effects and offering the convenience of oral administration.
Smart Images

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Abstract
Description
Technical Field
[0001] (Cross - Reference to Related Applications) This application claims priority to U.S. Provisional Patent Application No. 63 / 341,993, filed May 13, 2022, and U.S. Provisional Patent Application No. 63 / 497,634, filed Apr. 21, 2023, each of which is hereby incorporated by reference in its entirety.
Background Art
[0002] Alpha 4 beta 7 integrin (α 4 β 7 ) is also known as lymphocyte Peyer's patch adhesion molecule (LPAM) and is a potent signaling molecule embedded in the cell membrane of immune cells. Alpha 4 β 7 binds to mucosal vascular addressin cell adhesion molecule (MAdCAM) located on high endothelial venules of mucosal lymphoid organs, thereby mediating T - cell homing to gut - associated lymphoid tissue. Alpha 4 β 7 has been demonstrated to be involved in several immune system disorders such as inflammatory bowel disease (IBD) (including Crohn's disease (CD) and ulcerative colitis (UC)) and graft - versus - host disease (GVHD).
[0003] Alpha 4 β 7 is a clinically proven target for IBD, and the injectable anti - alpha 4 β 7 mAb, ENTYVIO (vedolizumab), is approved for the treatment of UC and CD. However, the convenience of ENTYVIO is limited by the need for parenteral administration. Furthermore, ENTYVIO causes a range of side effects (including nausea, vomiting, severe diarrhea, abdominal cramps, weight loss, and pain), and due to the long half - life of ENTYVIO, management can be difficult. Therefore, there is a need for an orally administrable, highly active and / or selective alpha 4 β 7 small - molecule inhibitor with reduced side effects.
SUMMARY OF THE INVENTION
[0004] In one aspect, provided herein is a compound having the structure of formula (I), or a pharmaceutically acceptable salt or solvate thereof,
[0005]
CHEM.
[0006]
CHEM.
[0007]
NUM.
[0008] In certain embodiments, the present disclosure provides a pharmaceutical composition comprising a compound or salt of formula (I), (I-a), (II), or (III) and a pharmaceutically acceptable excipient.
[0009] In certain embodiments, the present disclosure provides a method thereof in a subject in need of modulation of alpha4beta7 integrin, comprising administering to the subject a compound or salt of formula (I), (I-a), (II), or (III), or a pharmaceutical composition thereof.
[0010] In certain embodiments, the present disclosure provides a method for a subject in need of treatment of an inflammatory disease or condition, comprising administering to the subject a compound or salt of formula (I), (I-a), (II), or (III), or a pharmaceutical composition thereof. In some embodiments, the inflammatory disease or condition is selected from inflammatory bowel disease, ulcerative colitis, Crohn's disease, graft-versus-host disease, type 1 diabetes, immune-mediated colitis, checkpoint inhibitor-induced colitis, and primary sclerosing cholangitis.
[0011] Incorporation by reference All publications, patents, and patent applications mentioned in this specification are hereby incorporated by reference to the same extent as if each individual publication, patent, or patent application was specifically and individually indicated to be incorporated by reference.
[0012] The novel features of the invention are set forth with particularity in the appended claims. A further understanding of the features and advantages of the invention will be obtained from the following detailed description which illustrates exemplary embodiments of the invention, and from the accompanying drawings.
DETAILED DESCRIPTION OF THE INVENTION
[0013] Integrin alpha4beta7 is an adhesion receptor of the integrin family that shares subunits with alpha4beta1 (VLA4) and alphaEbeta7, which is an E-cadherin receptor. Alpha 4 Beta 7 is important for directing immune cells to the intestinal mucosa and is induced during T cell activation in Peyer's patches or mesenteric lymph nodes. Alpha 4 Beta 7 is a clinically proven target for IBD, and selective alpha 4 Beta 7 inhibition results in significant anti-inflammatory effects and symptom reduction. However, off-target binding to alpha 4 Beta 1 can result in side effects that significantly limit the dose. For example, TYSABRI (natalizumab) is an alpha 4 Beta 7 and alpha4 β 1 is bound to both, and α 4 β 1 binding is associated with progressive multifocal leukoencephalopathy, and as a result, the FDA has restricted the use of TYSABRI in IBD.
[0014] In some embodiments, the present disclosure provides an orally available α 4 β 1 integrin antagonist designed in a manner that mimics its high selectivity for α 4 β 7 over α 4 β 7 For example, in some embodiments, the present disclosure provides a compound having a selectivity greater than 100-fold for α 4 β 1 over α 4 β 7 In some embodiments, the present disclosure provides a compound having a selectivity greater than 1,000-fold for α 4 β 1 over α 4 β 7 over α
[0015] Ulcerative colitis disease UC is a form of IBD characterized by inflammation and ulcers in the large intestine. The clinical symptoms of UC are diarrhea and bloody stools. Its clinical course is characterized by exacerbations and remissions, which can occur spontaneously or in response to changes in diet, changes in treatment regimen, other diseases, or stress.
[0016] UC can be debilitating and sometimes lead to life-threatening complications. Frequent diarrhea and bloody stools can result in weight loss, dehydration, and anemia. Persistent UC is associated with an increased risk of developing colon cancer. The Centers for Disease Control estimates that 3,000,000 people in the United States have IBD, and approximately half of them have UC. In Europe, a similar number of people are estimated to have UC.
[0017] UC is typically treated with anti-inflammatory drugs, starting with relatively mild-acting and locally delivered drugs and progressing to systemic immunosuppressants in patients with refractory disease. The first-line therapy for patients with mild disease consists of 5-aminosalicylic acids such as mesalamine and sulfasalazine. Patients with more severe disease are treated with systemic corticosteroids, with the aim of inducing remission and transitioning the patient to more tolerable drugs such as 5-aminosalicylic acid for maintenance. Some patients may be treated with systemic immunomodulatory drugs such as azathioprine, cyclosporine, and XELJANZ (tofacitinib). Anti-inflammatory biologics such as REMICADE (infliximab), HUMIRA (adalimumab), and SIMPONI (golimumab), which are TNFα antagonists, and STELARA (ustekinumab), which is an IL-12 / IL-23 antagonist, are effective in inducing remission in patients with moderate to severe UC.
[0018] ENTYVIO (vedolizumab) is a monoclonal antibody that selectively targets 4 α 7 β and was first approved by the FDA for the treatment of UC and CD in 2014. In clinical trials, approximately 30% of patients administered ENTYVIO achieved remission at the end of 1 year of treatment. ENTYVIO is administered as a 30-minute intravenous infusion at weeks 0, 2, and 6, followed by administration every 8 weeks. Long-term treatment is generally well tolerated in patients, although frequent dose adjustments have been reported to be necessary to maintain efficacy.
[0019] Background of Crohn's disease CD is a chronic inflammatory disease that most commonly affects the end of the small intestine and the beginning of the large intestine, but can involve any part of the gastrointestinal tract. Both CD and UC are types of IBD, and many of the symptoms and patient populations overlap. In addition to the possibility of CD developing in other parts of the intestine, CD differs from UC, in which the inflammation is continuous, in that normal healthy tissue can exist between patches of affected tissue in CD. CD also differs from UC, which is limited to the innermost layer, in that it can occur in all layers of the intestinal wall. It is estimated that 1.5 million people in the United States and 1.1 million people in Europe are affected by CD.
[0020] The treatment paradigm for CD is very similar to that for UC with currently approved therapies that focus on anti-inflammatory agents. Almost 60% of CD patients will require surgery within 20 years of diagnosis to treat complications such as fistulas (i.e., abnormal connections between body parts), life-threatening bleeding, and intestinal obstruction.
[0021] Although many therapeutic agents are approved for UC and CD, important unmet medical needs remain for patients and clinicians to effectively and conveniently manage these chronic diseases, which could be facilitated by effective oral therapies.
[0022] In some aspects, the compounds of the present disclosure are used for the treatment and / or prevention of IBD. In some aspects of the present disclosure, the compounds provided herein are used for the treatment and / or prevention of UC. In some aspects of the present disclosure, the compounds provided herein are used for the treatment and / or prevention of CD.
[0023] Definitions Unless otherwise defined, all technical and scientific terms used herein have the same meaning as commonly understood by one of ordinary skill in the art to which this invention belongs. All patents and publications cited herein are incorporated by reference.
[0024] As used in this specification and the appended claims, the singular forms "a", "an", and "the" include plural referents unless the context clearly dictates otherwise.
[0025] "Alkyl" refers to a monovalent radical of a straight-chain or branched-chain hydrocarbon chain consisting only of carbon and hydrogen atoms, containing no unsaturation, and preferably having from 1 to 12 carbon atoms (i.e., C 1 ~C 12 alkyl). The alkyl is bonded to the remainder of the molecule through a single bond. In certain embodiments, the alkyl contains from 1 to 12 carbon atoms (i.e., C 1 ~C 12 alkyl). In certain embodiments, the alkyl contains from 1 to 8 carbon atoms (i.e., C 1 ~C 8 alkyl). In other embodiments, the alkyl contains from 1 to 5 carbon atoms (i.e., C 1 ~C 5 alkyl). In other embodiments, the alkyl contains from 1 to 4 carbon atoms (i.e., C 1 ~C 4 alkyl). In other embodiments, the alkyl contains from 1 to 3 carbon atoms (i.e., C 1 ~C 3 alkyl). In other embodiments, the alkyl contains from 1 to 2 carbon atoms (i.e., C 1 ~C 2 alkyl). In other embodiments, the alkyl contains 1 carbon atom (i.e., C 1 alkyl). In other embodiments, the alkyl contains from 5 to 15 carbon atoms (i.e., C 5 ~C 15 alkyl). In other embodiments, the alkyl contains from 5 to 8 carbon atoms (i.e., C 5 ~C 8 alkyl). In other embodiments, the alkyl contains from 2 to 5 carbon atoms (i.e., C 2 ~C 5 alkyl). In other embodiments, the alkyl contains from 3 to 5 carbon atoms (i.e., C 3 ~C 5(alkyl). For example, the alkyl group can be bonded to the rest of the molecule by a single bond and can be, for example, methyl, ethyl, 1-propyl (n-propyl), 1-methylethyl (iso-propyl), 1-butyl (n-butyl), 1-methylpropyl (sec-butyl), 2-methylpropyl (iso-butyl), 1,1-dimethylethyl (tert-butyl), 1-pentyl (n-pentyl), and the like.
[0026] "Alkenyl" consists of only carbon atoms and hydrogen atoms, contains at least one carbon-carbon double bond, and preferably refers to a straight-chain or branched-chain hydrocarbon chain radical group having 2 to 12 carbon atoms (i.e., C 2 ~C 12 alkenyl). In certain embodiments, alkenyl contains 2 to 8 carbon atoms (i.e., C 2 ~C 8 alkenyl). In certain embodiments, alkenyl contains 2 to 6 carbon atoms (i.e., C 2 ~C 6 alkenyl). In other embodiments, alkenyl contains 2 to 4 carbon atoms (i.e., C 2 ~C 4 alkenyl). Alkenyl is bonded to the rest of the molecule by a single bond and can be, for example, ethenyl (i.e., vinyl), prop-1-enyl (i.e., allyl), but-1-enyl, pent-1-enyl, pent-1,4-dienyl, and the like.
[0027] "Alkynyl" consists of only carbon and hydrogen atoms, contains at least one carbon-carbon triple bond, and preferably refers to a straight-chain or branched-chain hydrocarbon chain radical group having 2 to 12 carbon atoms (i.e., C 2 ~C 12 alkynyl). In certain embodiments, alkynyl contains 2 to 8 carbon atoms (i.e., C 2 ~C 8 alkynyl). In other embodiments, alkynyl contains 2 to 6 carbon atoms (i.e., C 2 ~C 6 alkynyl). In other embodiments, alkynyl contains 2 to 4 carbon atoms (i.e., C2 ~C 4 (alkynyl). The alkynyl is bonded to the rest of the molecule by a single bond and is, for example, ethynyl, propynyl, butynyl, pentynyl, hexynyl, etc.
[0028] "Alkylene" refers to a straight-chain divalent hydrocarbon chain consisting of only carbon and hydrogen, containing no unsaturation, connecting the rest of the molecule to a radical group, and preferably having 1 to 12 carbon atoms. Examples include methylene, ethylene, propylene, butylene, etc. The alkylene chain is bonded to the rest of the molecule via a single bond and to the radical group via a single bond. The bonding points of the alkylene chain to the rest of the molecule and to the radical group are each through a terminal carbon. The alkylene chain can be optionally substituted by one or more substituents such as those described herein. In certain embodiments, alkylene contains 1 to 10 carbon atoms (i.e., C 1 ~C 10 alkylene). In certain embodiments, alkylene contains 1 to 8 carbon atoms (i.e., C 1 ~C 8 alkylene). In other embodiments, alkylene contains 1 to 5 carbon atoms (i.e., C 1 ~C 5 alkylene). In other embodiments, alkylene contains 1 to 4 carbon atoms (i.e., C 1 ~C 4 alkylene). In other embodiments, alkylene contains 1 to 3 carbon atoms (i.e., C 1 ~C 3 alkylene). In other embodiments, alkylene contains 1 to 2 carbon atoms (i.e., C 1 ~C 2 alkylene). In other embodiments, alkylene contains 1 carbon atom (i.e., C 1 alkylene). In other embodiments, alkylene contains 5 to 8 carbon atoms (i.e., C 5 ~C 8 alkylene). In other embodiments, alkylene contains 2 to 5 carbon atoms (i.e., C 2 ~C 5(alkylene). In other embodiments, the alkylene contains 3 to 5 carbon atoms (i.e., C 3 ~C 5 alkylene).
[0029] "Alkenylene" refers to a straight-chain divalent hydrocarbon chain consisting of only carbon and hydrogen, containing at least one carbon-carbon double bond, preferably having 2 to 12 carbon atoms, and connecting the rest of the molecule to a radical group. The alkenylene chain is bonded to the rest of the molecule via a single bond and to the radical group via a single bond. The bonding points of the alkenylene chain to the rest of the molecule and the radical group are via terminal carbons respectively. The alkenylene chain may be optionally substituted by one or more substituents such as those described herein. In certain embodiments, the alkenylene contains 2 to 10 carbon atoms (i.e., C 2 ~C 10 alkenylene). In certain embodiments, the alkenylene contains 2 to 8 carbon atoms (i.e., C 2 ~C 8 alkenylene). In other embodiments, the alkenylene contains 2 to 5 carbon atoms (i.e., C 2 ~C 5 alkenylene). In other embodiments, the alkenylene contains 2 to 4 carbon atoms (i.e., C 2 ~C 4 alkenylene). In other embodiments, the alkenylene contains 2 to 3 carbon atoms (i.e., C 2 ~C 3 alkenylene). In other embodiments, the alkenylene contains 2 carbon atoms (i.e., C 2 alkenylene). In other embodiments, the alkenylene contains 5 to 8 carbon atoms (i.e., C 5 ~C 8 alkenylene). In other embodiments, the alkenylene contains 3 to 5 carbon atoms (i.e., C 3 ~C 5 alkenylene).
[0030] "Alkenylene" refers to a straight-chain divalent hydrocarbon chain consisting only of carbon and hydrogen, containing at least one carbon-carbon triple bond, preferably having 2 to 12 carbon atoms, and connecting the rest of the molecule to a radical group. The alkynylene chain is bonded to the rest of the molecule through a single bond and to the radical group through a single bond. The bonding points of the alkynylene chain to the rest of the molecule and to the radical group are through terminal carbons respectively. The alkynylene chain may be optionally substituted by one or more substituents such as those described herein. In certain embodiments, alkynylene contains 2 to 10 carbon atoms (i.e., C 2 ~C 10 alkynylene). In certain embodiments, alkynylene contains 2 to 8 carbon atoms (i.e., C 2 ~C 8 alkynylene). In other embodiments, alkynylene contains 2 to 5 carbon atoms (i.e., C 2 ~C 5 alkynylene). In other embodiments, alkynylene contains 2 to 4 carbon atoms (i.e., C 2 ~C 4 alkynylene). In other embodiments, alkynylene contains 2 to 3 carbon atoms (i.e., C 2 ~C 3 alkynylene). In other embodiments, alkynylene contains 2 carbon atoms (i.e., C 2 alkynylene). In other embodiments, alkynylene contains 5 to 8 carbon atoms (i.e., C 5 ~C 8 alkynylene). In other embodiments, alkynylene contains 3 to 5 carbon atoms (i.e., C 3 ~C 5 alkynylene).
[0031] The term "C x~y ", when used in combination with a chemical moiety such as alkyl, alkenyl, or alkynyl, means including a group containing x to y carbons in the chain. For example, the term "C 1~6 alkyl" refers to a substituted or unsubstituted saturated hydrocarbon group including straight-chain alkyl and branched-chain alkyl groups containing 1 to 6 carbons. -Cx~y The term "alkylene" refers to a substituted or unsubstituted alkylene chain having x to y carbons in the alkylene chain. For example, -C 1~6 alkylene- can be selected from methylene, ethylene, propylene, butylene, pentylene, and hexylene, any of which is optionally substituted.
[0032] "C x~y alkenyl" and "C x~y alkynyl" refer to unsaturated aliphatic groups having a length and possible substitutions similar to the above alkyl, but each containing at least one double bond or triple bond. -C x~y The term "alkenylene-" refers to a substituted or unsubstituted alkenylene chain having x to y carbons in the alkenylene chain. For example, -C 2~6 alkenylene- can be selected from ethenylene, propenylene, butenylene, pentenylene, and hexenylene, any of which is optionally substituted. The alkenylene chain can have one double bond or two or more double bonds in the alkenylene chain. -C x~y The term "alkynylene-" refers to a substituted or unsubstituted alkynylene chain having x to y carbons in the alkynylene chain. For example, -C 2~6 alkynylene- can be selected from ethynylene, propynylene, butynylene, pentynylene, and hexynylene, any of which is optionally substituted. The alkynylene chain can have one triple bond or two or more triple bonds in the alkynylene chain.
[0033] As used herein, the term "carbocyclic ring" refers to a saturated, unsaturated, or aromatic ring in which each atom of the ring is carbon. Carbocyclic rings include 3- to 10-membered monocyclic rings and 6- to 12-membered bicyclic rings. Each ring of the bicyclic carbocyclic ring can be selected from saturated, unsaturated, and aromatic rings. The bicyclic carbocyclic ring can be a fused, bridged, or spiro ring system. In some embodiments, the carbocyclic ring is aryl. In some embodiments, the carbocyclic ring is cycloalkyl. In some embodiments, the carbocyclic ring is cycloalkenyl. In an exemplary embodiment, an aromatic ring, such as phenyl, can be fused to a saturated or unsaturated ring, such as cyclohexane, cyclopentane, or cyclohexene. Any combination of saturated, unsaturated, and aromatic bicyclic rings is included in the definition of carbocyclic ring as long as the valency permits. Exemplary carbocyclic rings include cyclopentyl, cyclohexyl, cyclohexenyl, adamantyl, phenyl, indanyl, and naphthyl. The carbocyclic ring can be optionally substituted by one or more substituents such as those described herein.
[0034] "Cycloalkyl" refers to a stable, fully saturated monocyclic or polycyclic hydrocarbon radical consisting of only carbon atoms and hydrogen atoms, including fused ring systems or bridged ring systems, preferably having 3 to 12 carbon atoms (i.e., C 3~12 cycloalkyl). In certain embodiments, cycloalkyl contains 3 to 10 carbon atoms (i.e., C 3~10 cycloalkyl). In other embodiments, cycloalkyl contains 5 to 7 carbon atoms (i.e., C 5~7 cycloalkyl). Cycloalkyl can be attached to the remainder of the molecule by a single bond. Examples of monocyclic cycloalkyls include cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, and cyclooctyl. Examples of polycyclic cycloalkyl groups include, for example, adamantyl, norbornyl (i.e., bicyclo[2.2.1]heptanyl), norbornenyl, decalinyl, 7,7-dimethyl-bicyclo[2.2.1]heptanyl, and the like. Cycloalkyl can be optionally substituted by one or more substituents such as those described herein.
[0035] "Cycloalkenyl" preferably refers to a stable unsaturated non-aromatic monocyclic or polycyclic hydrocarbon radical consisting only of carbon and hydrogen atoms, having 3 to 12 carbon atoms and containing at least one double bond, and including a fused or bridged ring system (i.e., C 3~12 cycloalkenyl). In certain embodiments, cycloalkenyl contains 3 to 10 carbon atoms (i.e., C 3-10 cycloalkenyl). In other embodiments, cycloalkenyl contains 5 to 7 carbon atoms (i.e., C 5~7 cycloalkenyl). Cycloalkenyl can be attached to the rest of the molecule by a single bond. Examples of monocyclic cycloalkenyls include cyclopentenyl, cyclohexenyl, cycloheptenyl, and cyclooctenyl. Cycloalkenyl can be optionally substituted by one or more substituents such as those described herein.
[0036] "Aryl" refers to a radical derived from an aromatic monocyclic or aromatic polycyclic hydrocarbon ring system by removing a hydrogen atom from a ring carbon atom. The aromatic monocyclic or aromatic polycyclic hydrocarbon ring system contains only hydrogen and carbon, as well as 5 to 18 carbon atoms, and at least one of the rings in the ring system is aromatic, i.e., contains a cyclic delocalized (4n + 2)π - electron system according to Hückel's theory. Examples of ring systems from which aryl groups are derived include, but are not limited to, groups such as benzene, fluorene, indane, indene, tetralin, and naphthalene. Aryl can be optionally substituted by one or more substituents such as those described herein.
[0037] "C x~y carbocycle" means including a group containing x to y carbons within the ring. For example, the term "C 3~6 carbocycle" can be a saturated, unsaturated or aromatic ring system containing 3 to 6 carbon atoms, and any of those carbon atoms can be optionally substituted as provided herein.
[0038] As used herein, the term "heterocyclic ring" refers to a saturated, unsaturated, non-aromatic, or aromatic ring containing one or more heteroatoms. Exemplary heteroatoms include N, O, Si, P, B, and S atoms. Heterocyclic rings include 3- to 10-membered monocyclic rings and 6- to 12-membered bicyclic rings. Each ring of the bicyclic heterocyclic ring can be selected from saturated, unsaturated, and aromatic rings. In some embodiments, the heterocyclic ring contains at least one heteroatom selected from oxygen, nitrogen, sulfur, or any combination thereof. In some embodiments, the heterocyclic ring contains at least one heteroatom selected from oxygen, nitrogen, or any combination thereof. In some embodiments, the heterocyclic ring contains at least one heteroatom selected from oxygen, sulfur, or any combination thereof. In some embodiments, the heterocyclic ring contains at least one heteroatom selected from nitrogen, sulfur, or any combination thereof. The heterocyclic ring can be attached to the rest of the molecule via any atom of the heterocyclic ring whose valence is acceptable, such as a carbon or nitrogen atom of the heterocyclic ring. In some embodiments, the heterocyclic ring is a heteroaryl. In some embodiments, the heterocyclic ring is a heterocycloalkyl. Exemplary heterocyclic rings include pyrrolidinyl, pyrrolyl, imidazolyl, pyrazolyl, triazolyl, piperidinyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, thiophenyl, oxazolyl, thiazolyl, morpholinyl, indazolyl, indolyl, and quinolinyl. The heterocyclic ring can be optionally substituted by one or more substituents such as those described herein. The bicyclic heterocyclic ring can be a fused, bridged, or spiro ring system. In an exemplary embodiment, a heterocyclic ring, such as pyridyl, can be fused to a saturated or unsaturated ring, such as cyclohexane, cyclopentane, or cyclohexene. The heterocyclic ring can be optionally substituted by one or more substituents such as those described herein.
[0039] "Heterocycloalkyl" refers to a stable 3- to 12-membered non-aromatic ring radical containing 2 to 12 carbon atoms and at least 1 heteroatom, each heteroatom being selected from N, O, Si, P, B, and S atoms. In some embodiments, the heterocycloalkyl contains at least 1 heteroatom selected from oxygen, nitrogen, sulfur, or any combination thereof. In some embodiments, the heterocycloalkyl contains at least 1 heteroatom selected from oxygen, nitrogen, or any combination thereof. In some embodiments, the heterocycloalkyl contains at least 1 heteroatom selected from oxygen, sulfur, or any combination thereof. In some embodiments, the heterocycloalkyl contains at least 1 heteroatom selected from nitrogen, sulfur, or any combination thereof. The heterocycloalkyl can be selected from monocyclic or bicyclic, and fused or bridged ring systems. The heteroatoms in the heteroaryl radical are optionally oxidized. When present, one or more nitrogen atoms are optionally quaternized. The heterocycloalkyl radical is partially or fully saturated. The heterocycloalkyl is attached to the remainder of the molecule through any atom of the heterocycloalkyl for which the valence is allowed, such as any carbon or nitrogen atom of the heterocycloalkyl. Examples of heterocycloalkyl radicals include, but are not limited to, dioxolanyl, thienyl[1,3]dithianyl, decahydroisoquinolyl, imidazolinyl, imidazolidinyl, isothiazolidinyl, isoxazolidinyl, morpholinyl, octahydroindolyl, octahydroisoindolyl, 2-oxopiperazinyl, 2-oxopiperidinyl, 2-oxopyrrolidinyl, oxazolidinyl, piperidinyl, piperazinyl, 4-piperidonyl, pyrrolidinyl, pyrazolidinyl, quinuclidinyl, thiazolidinyl, tetrahydrofuryl, trithianyl, tetrahydropyranyl, thiomorpholinyl, thiamorpholinyl, 1-oxothiomorpholinyl, and 1,1-dioxothiomorpholinyl. The heterocycloalkyl can be optionally substituted by one or more substituents such as those described herein.
[0040] The term "heteroaryl" refers to a radical derived from a 3- to 12-membered aromatic ring radical containing 1 to 11 carbon atoms and at least 1 heteroatom, each heteroatom being optionally selected from N, O, and S. In some embodiments, heteroaryl contains at least 1 heteroatom selected from oxygen, nitrogen, sulfur, or any combination thereof. In some embodiments, heteroaryl contains at least 1 heteroatom selected from oxygen, nitrogen, or any combination thereof. In some embodiments, heteroaryl contains at least 1 heteroatom selected from oxygen, sulfur, or any combination thereof. In some embodiments, heteroaryl contains at least 1 heteroatom selected from nitrogen, sulfur, or any combination thereof. As used herein, a heteroaryl ring may be selected from monocyclic or bicyclic and fused or bridged ring systems, with at least one of the rings in the ring system being aromatic, i.e., containing a cyclic delocalized (4n + 2)π-electron system according to Hückel's theory. The heteroatom(s) in a heteroaryl radical may optionally be oxidized. When present, one or more nitrogen atoms are optionally quaternized. Heteroaryl may be attached to the remainder of the molecule via any atom of the heteroaryl for which the valence is permissible, such as a carbon or nitrogen atom of the heteroaryl. Heteroaryl includes an aromatic monocyclic structure, preferably a 5- to 6-membered ring, the ring structure of which contains at least 1 heteroatom, preferably 1 to 4 heteroatoms, more preferably 1 or 2 heteroatoms. Examples of heteroaryl groups include pyrrole, furan, thiophene, imidazole, oxazole, thiazole, pyrazole, pyridine, pyrazine, pyridazine, and pyrimidine. Heteroaryl may optionally be substituted by one or more substituents such as those described herein. Heteroaryl also includes polycyclic ring systems having two or more rings in which two or more atoms are common to two adjacent rings, with at least one of the rings being heteroaromatic, for example, the other rings may be aromatic or non-aromatic carbocyclic, or heterocyclic. Heteroaryl may optionally be substituted by one or more substituents such as those described herein.
[0041] The "X-membered heterocyclic ring" refers to the number of atoms within the ring, i.e., it refers to X. For example, a 5-membered heteroaryl ring or a 5-membered aromatic heterocyclic ring has 5 atoms within the ring, such as triazole, oxazole, thiophene, etc.
[0042] "Alkoxy" refers to a radical bonded through an oxygen atom of the formula -O-alkyl, where alkyl is the alkyl chain defined above.
[0043] "Halo" or "halogen" refers to halogen substituents such as bromo, chloro, fluoro, and iodo substituents.
[0044] As used herein, the terms "haloalkyl" or "haloalkane" refer to an alkyl radical as defined above that is substituted by one or more halogen radicals, such as trifluoromethyl, dichloromethyl, bromomethyl, 2,2,2-trifluoroethyl, 1-fluoromethyl-2-fluoroethyl, etc. In some embodiments, the alkyl portion of the fluoroalkyl radical is optionally further substituted. Examples of halogen-substituted alkanes ("haloalkanes") include halomethanes (e.g., chloromethane, bromomethane, fluoromethane, iodomethane), di- and trihalomethanes (e.g., trichloromethane, tribromomethane, trifluoromethane, triiodomethane), 1-haloethane, 2-haloethane, 1,2-dihaloethane, 1-halopropane, 2-halopropane, 3-halopropane, 1,2-dihalopropane, 1,3-dihalopropane, 2,3-dihalopropane, 1,2,3-trihalopropane, and any other suitable combination of an alkane (or substituted alkane) and a halogen (e.g., Cl, Br, F, and I). When the alkyl group is substituted with two or more halogen radicals, each halogen can be independently selected, for example, from 1-chloro, 2-fluoroethane.
[0045] The term "substituted" refers to hydrogen on one or more carbons or substitutable heteroatoms, such as NH or NH of a compound2 refers to a moiety having a substituent to replace. "Substituted" or "substituted with" is understood to include the implicit condition that such substitution results in a stable compound, i.e., a compound that does not undergo spontaneous transformation such as rearrangement, cyclization, elimination, etc., in accordance with the acceptable valences of the substituted atom and the substituent. In certain embodiments, substituted refers to a moiety having a substituent that replaces two hydrogen atoms on the same carbon atom, such as replacing two hydrogen atoms on a single carbon with an oxo, imino, or thioxo group. As used herein, the term "substituted" is intended to include all acceptable substituents of an organic compound. From a broad perspective, acceptable substituents include acyclic and cyclic, branched and unbranched, carbocyclic and heterocyclic, aromatic and non-aromatic substituents of an organic compound. The acceptable substituents can be one or more and can be the same or different for a suitable organic compound.
[0046] In some embodiments, examples of substituents may include any of the substituents described herein, for example, halogen, hydroxy, oxo (=O), thioxo (=S), cyano (-CN), nitro (-NO 2 ), imino (=N-H), oximo (=N-OH), hydrazino (=N-NH 2 ), -R b -OR a , -R b -OC(O)-R a , -R b -OC(O)-OR a , -R b -OC(O)-N(R a ) 2 , -R b -N(R a ) 2 , -R b -C(O)R a , -R b -C(O)OR a , -R b -C(O)N(R a ) 2 , -R b -O-R c -C(O)N(R a ) 2 , -Rb -N(R a )C(O)OR a 、 -R b -N(R a )C(O)R a 、 -R b -N(R a )S(O) t R a (where t is 1 or 2), -R b -S(O) t R a (where t is 1 or 2), -R b -S(O) t OR a (where t is 1 or 2), and -R b -S(O) t N(R a ) 2 (where t is 1 or 2), and alkyl, alkenyl, alkynyl, aryl, aralkyl, aralkenyl, aralkynyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heterocycloalkylalkyl, heteroaryl, and heteroarylalkyl, any of which may be alkyl, alkenyl, alkynyl, halogen, haloalkyl, haloalkenyl, haloalkynyl, oxo(=O), thioxo(=S), cyano(-CN), nitro(-NO 2 )、 imino(=N-H), oximo(=N-OH), hydrazine(=N-NH 2 ), -R b -OR a 、 -R b -OC(O)-R a 、 -R b -OC(O)-OR a 、 -R b -OC(O)-N(R a ) 2 、 -R b -N(R a ) 2 、 -R b -C(O)R a 、 -R b -C(O)OR a 、 -R b -C(O)N(R a ) 2 、 -R b -O-R c-C(O)N(R a ) 2 、-R b -N(R a )C(O)OR a 、-R b -N(R a )C(O)R a 、-R b -N(R a )S(O) t R a (where t is 1 or 2), -R b -S(O) t R a (where t is 1 or 2), -R b -S(O) t OR a (where t is 1 or 2) and -R b -S(O) t N(R a ) 2 may be optionally substituted by, where each R a is independently selected from hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, heterocycloalkyl, heterocycloalkylalkyl, heteroaryl, or heteroarylalkyl, and each R a with a valence that is permitted is alkyl, alkenyl, alkynyl, halogen, haloalkyl, haloalkenyl, haloalkynyl, oxo(=O), thioxo(=S), cyano(-CN), nitro(-NO 2 ), imino(=N-H), oximo(=N-OH), hydrazine(=N-NH 2 ), -R b -OR a 、-R b -OC(O)-R a 、-R b -OC(O)-OR a 、-R b -OC(O)-N(R a ) 2 、-R b -N(R a ) 2 、-R b -C(O)R a 、-R b -C(O)OR a 、-Rb -C(O)N(R a ) 2 、-R b -O-R c -C(O)N(R a ) 2 、-R b -N(R a )C(O)OR a 、-R b -N(R a )C(O)R a 、-R b -N(R a )S(O) t R a (wherein, t is 1 or 2), -R b -S(O) t R a (wherein, t is 1 or 2), -R b -S(O) t OR a (wherein, t is 1 or 2) and -R b -S(O) t N(R a ) 2 (wherein, t is 1 or 2) may be optionally substituted, and each R b is independently selected from a direct bond or a linear or branched alkylene chain, alkenylene chain or alkynylene chain, and each R c is a linear or branched alkylene chain, alkenylene chain or alkynylene chain. It will be understood by those skilled in the art that the substituents themselves may be substituted as appropriate.
[0047] The term "salt" or "pharmaceutically acceptable salt" refers to salts derived from various organic and inorganic counterions well known in the art. Pharmaceutically acceptable acid addition salts can be formed with inorganic acids and organic acids. Pharmaceutically acceptable base addition salts can be formed using inorganic bases and / or organic bases.
[0048] As used herein, the term "pharmaceutically acceptable" refers to compounds, materials, compositions, and / or dosage forms that are suitable for use in contact with the tissues of humans and animals within the scope of sound medical judgment, without excessive toxicity, irritation, allergic response, or other problems or complications, or commensurate with a reasonable benefit / risk ratio.
[0049] As used herein, the phrases "pharmaceutically acceptable excipient" or "pharmaceutically acceptable carrier" mean a pharmaceutically acceptable material, composition, or vehicle, such as a liquid or solid filler, diluent, excipient, solvent, or encapsulating material. Each carrier must be "acceptable" in the sense of being compatible with the other ingredients of the formulation and not injurious to the patient.
[0050] The terms "subject", "individual", and "patient" may be used interchangeably and refer to humans, as well as non-human mammals (e.g., non-human primates, dogs, horses, cats, pigs, cows, ungulates, rabbits, etc.). In various embodiments, the subject can be a human (e.g., an adult male, an adult female, an adolescent male, an adolescent female, a male child, a female child) under the care of a physician or other patient in a hospital, either as an outpatient or in other clinical settings. In certain embodiments, the subject may not be under the care or prescription of a physician or other healthcare provider.
[0051] As used herein, the phrase "subject in need" refers to a subject as described below who has or is at risk of having a medical condition to be prophylactically or therapeutically treated with a compound or salt described herein.
[0052] The terms "administer", "administered", "administering", and "administration" are defined as providing a composition to a subject via a route known in the art, including but not limited to intravenous, intraarterial, oral, parenteral, buccal, topical, transdermal, rectal, intramuscular, subcutaneous, intraosseous, transmucosal, or intraperitoneal routes of administration. In certain embodiments, an oral route of administering the composition can be used. The terms "administer", "administered", "administering", and "administration" with respect to a compound are to be understood to mean providing the compound of the invention or a prodrug of the compound of the invention to an individual in need thereof.
[0053] As used herein, "treatment" or "treating" refers to an approach for obtaining a beneficial or desired result, including but not limited to therapeutic and / or prophylactic benefits, with respect to a disease, disorder, or medical condition. In certain embodiments, treatment or treating involves administering to a subject a compound or composition disclosed herein. A therapeutic benefit can include eradication or amelioration of the underlying disease being treated. Also, a therapeutic benefit can be achieved by eradication or amelioration of one or more of the physiological symptoms associated with the underlying disease, such as observing an improvement in the subject despite the possibility that the subject may still be afflicted with the underlying disease. In certain embodiments, for prophylactic benefit, the composition is administered to a subject at risk of developing a particular disease or to a subject reporting one or more of the physiological symptoms of a disease, even in the absence of a diagnosis of that disease. Treating can include, for example, reducing, delaying, or alleviating the severity of one or more symptoms of a disease or condition, or reducing the frequency with which a symptom, such as a disease, defect, disorder, or adverse condition, is experienced by a patient. Treating can be used herein to refer to a method that provides a level of treatment or amelioration of a disease or condition, and can contemplate a range of results directed thereto, including but not limited to complete prevention of the condition.
[0054] In certain embodiments, the term "prevent" or "prevention" as related to a disease or disorder may refer to a compound that reduces the occurrence of a disorder or condition in a treated sample compared to an untreated control sample, or delays or reduces the severity of onset of one or more symptoms of a disorder or condition in a treated sample compared to an untreated control sample, in a statistical sample.
[0055] "Therapeutic effect", as the term is used herein, encompasses the above-described therapeutic and / or prophylactic benefits. Prophylactic effects include delaying or eliminating the appearance of a disease or condition, delaying or eliminating the onset of symptoms of a disease or condition, slowing, stopping, or reversing the progression of a disease or condition, or any combination thereof.
[0056] Compound In one aspect, provided herein is a compound having the structure of formula (I), or a pharmaceutically acceptable salt or solvate thereof,
[0057]
Chemical formula
[0058]
Chemical formula
[0059]
Number
[0060] In some embodiments, B is an optionally substituted 3- to 12-membered heterocyclic ring. In some embodiments, B is an optionally substituted 3- to 12-membered saturated heterocyclic ring. In some embodiments, B is an optionally substituted 3- to 12-membered unsaturated heterocyclic ring. In some embodiments, B is an optionally substituted 6- to 12-membered aromatic heterocyclic ring. In some embodiments, B is selected from a 3-membered heterocyclic ring, a 4-membered heterocyclic ring, a 5-membered heterocyclic ring, a 6-membered heterocyclic ring, a 7-membered heterocyclic ring, an 8-membered heterocyclic ring, a 9-membered heterocyclic ring, a 10-membered heterocyclic ring, an 11-membered heterocyclic ring, and a 12-membered heterocyclic ring, any one of which is optionally substituted. In some embodiments, B is selected from a 3- to 4-membered heterocyclic ring, a 3- to 5-membered heterocyclic ring, a 3- to 6-membered heterocyclic ring, a 3- to 7-membered heterocyclic ring, a 3- to 8-membered heterocyclic ring, a 3- to 9-membered heterocyclic ring, a 3- to 10-membered heterocyclic ring, a 3- to 11-membered heterocyclic ring, and a 3- to 12-membered heterocyclic ring, any one of which is optionally substituted. In some embodiments, B is selected from a 3- to 8-membered monocyclic heterocyclic ring and a 6- to 12-membered bicyclic heterocyclic ring, any one of which is optionally substituted. In some embodiments, B is an optionally substituted 3- to 8-membered monocyclic heterocyclic ring. In some embodiments, B is an optionally substituted 6- to 12-membered bicyclic heterocyclic ring. In some embodiments, the optionally substituted 6- to 12-membered bicyclic heterocyclic ring of B is selected from a 6- to 12-membered bridged heterocyclic ring, a 6- to 12-membered spirocyclic heterocyclic ring, and a 6- to 12-membered fused heterocyclic ring, any one of which is optionally substituted. In some embodiments, the optional substituents of B are as defined herein. In some embodiments, the optional substituents of B are as defined in formula (I).
[0061] In some embodiments, B is an optionally substituted C 3~12 carbon ring. In some embodiments, B is an optionally substituted saturated C 3~12 carbon ring. In some embodiments, B is an optionally substituted unsaturated C3~12 It is a carbon ring. In some embodiments, B is an optionally substituted aromatic C 8~12 It is a carbon ring. In some embodiments, B is C 3 carbon ring, C 4 carbon ring, C 5 carbon ring, C 6 carbon ring, C 7 carbon ring, C 8 carbon ring, C 9 carbon ring, C 10 carbon ring, C 10 carbon ring, C 11 carbon ring, and C 12 selected from carbon rings, and any one of these is optionally substituted. In some embodiments, B is C 3~4 carbon ring, C 3~5 carbon ring, C 3~6 carbon ring, C 3~7 carbon ring, C 3~8 carbon ring, C 3~9 carbon ring, C 3~10 carbon ring, C 3~11 carbon ring, and C 3~12 selected from carbon rings, and any one of these is optionally substituted. In some embodiments, B is a monocyclic C 3~8 carbon ring and a bicyclic C 6~12 selected from carbon rings, and any one of these is optionally substituted. In some embodiments, the optional substituent of B is as defined herein. In some embodiments, the optional substituent of B is as defined in formula (I).
[0062] In some embodiments, for the compound or salt of formula (I), B is a 3- to 12-membered heterocyclic ring optionally substituted with one or more substituents independently selected from the following: halogen, -OR 17 , -SR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)OR 17 , -OC(O)R 17 , -OC(O)N(R 17 )2 , -C(O)N(R 17 ) 2 , -N(R 17 )C(O)R 17 , -N(R 17 )C(O)OR 17 , -N(R 17 )C(O)N(R 17 ) 2 , -N(R 17 )C(S)N(R 17 ) 2 , -N(R 17 )S(O) 2 (R 17 )、-S(O)R 17 , -S(O) 2 R 17 , -S(O) 2 N(R 17 ) 2 , -NO 2 , =O, =S, =NR 17 , -N 3 , and -CN, C 1~6 alkyl, C 2~6 alkenyl, and C 2~6 alkynyl, each of which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 17 , -SR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)OR 17 , -OC(O)R 17 , -OC(O)N(R 17 ) 2 , -C(O)N(R 17 ) 2 , -N(R 17 )C(O)R 17 , -N(R 17 )C(O)OR 17 , -N(R 17 )C(O)N(R 17 ) 2 , -N(R 17 )C(S)N(R 17 ) 2 , -N(R 17 )S(O) 2(R 17 )、 -S(O)R 17 、 -S(O) 2 R 17 、 -S(O) 2 N(R 17 ) 2 、 -NO 2 、 =O、 =S、 =NR 17 、 -N 3 、 and -CN, C 3~10 A carbocyclic ring and a 3 - to 10 - membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from halogen, C 1~6 alkyl, C 1~6 haloalkyl, -OR 17 、 -SR 17 、 -N(R 17 ) 2 、 -C(O)R 17 、 -C(O)OR 17 、 -OC(O)R 17 、 -OC(O)N(R 17 ) 2 、 -C(O)N(R 17 ) 2 、 -N(R 17 )C(O)R 17 、 -N(R 17 )C(O)OR 17 、 -N(R 17 )C(O)N(R 17 ) 2 、 -N(R 17 )C(S)N(R 17 ) 2 、 -N(R 17 )S(O) 2 (R 17 )、 -S(O)R 17 、 -S(O) 2 R 17 、 -S(O) 2 N(R 17 ) 2 、 -NO 2 、 =O、 =S、 =NR 17 、 -N 3 、 and optionally substituted with one or more substituents independently selected from the following, and, C 3~10 A carbocyclic ring and a 3 - to 10 - membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 17 , -SR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)OR 17 , -OC(O)R 17 , -OC(O)N(R 17 ) 2 , -C(O)N(R 17 ) 2 , -N(R 17 )C(O)R 17 , -N(R 17 )C(O)OR 17 , -N(R 17 )C(O)N(R 17 ) 2 , -N(R 17 )C(S)N(R 17 ) 2 , -N(R 17 )S(O) 2 (R 17 ), -S(O)R 17 , -S(O) 2 R 17 , -S(O) 2 N(R 17 ) 2 , -NO 2 , =O, =S, =NR 17 , -N 3 , and -CN, C 1~6 alkyl, which is halogen, -OR 17 , -SR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)OR 17 , -OC(O)R 17 , -OC(O)N(R 17 ) 2 , -C(O)N(R 17 ) 2 , -N(R 17 )C(O)R 17 , -N(R 17 )C(O)OR 17 , -N(R 17 )C(O)N(R 17 ) 2 , -N(R 17)C(S)N(R 17 ) 2 、-N(R 17 )S(O) 2 (R 17 )、-S(O)R 17 、-S(O) 2 R 17 、-S(O) 2 N(R 17 ) 2 、-NO 2 、=O、=S、=NR 17 、-N 3 、and one or more substituents independently selected from -CN, and optionally substituted with C 3~10 a carbocyclic ring and a 3- to 10-membered heterocyclic ring, each of which is independently selected from halogen, C 1~6 alkyl, C 1~6 haloalkyl, -OR 17 、-SR 17 、-N(R 17 ) 2 、-C(O)R 17 、-NO 2 、=O、=S、=NR 17 、-N 3 、and -CN, and optionally substituted with one or more substituents independently selected from
[0063] In some embodiments, for the compound or salt of formula (I), B is a 3- to 12-membered heterocyclic ring optionally substituted with one or more substituents independently selected from: halogen, -OR 17 、-SR 17 、-N(R 17 ) 2 、-C(O)R 17 、-C(O)OR 17 、-NO 2 、-CN, C 1~6 alkyl which is independently selected from halogen, -OR 17 、-SR 17 、-N(R 17 ) 2 、-C(O)R 17 、-C(O)OR 17 、-NO 2 、-CN, C3~10 Optionally substituted with one or more substituents independently selected from a carbon ring and a 3- to 10-membered heterocyclic ring, and C 3~10 The carbon ring and the 3- to 10-membered heterocyclic ring are each halogen, -OR 17 , -SR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)OR 17 , -NO 2 , -CN, and those optionally substituted with one or more substituents independently selected therefrom, and C 3~10 A carbon ring and a 3- to 10-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from halogen, -OR 17 , -SR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)OR 17 , -NO 2 , -CN, and C 1~6 An alkyl which is optionally substituted with one or more substituents independently selected from halogen, -OR 17 , -SR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)OR 17 , -NO 2 , and -CN.
[0064] In some embodiments, B is a 6- to 12-membered bicyclic heterocyclic ring selected from a 6- to 12-membered fused heterocyclic ring, a 6- to 12-membered spirocyclic heterocyclic ring, and a 6- to 12-membered bridged heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from halogen, -OR 17 , -SR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)OR 17 , -NO 2 , -CN, C 1~6 alkyl, and C1-6 alkyl is halogen, -OR17 、 -SR 17 、 -N(R 17 ) 2 、 -C(O)R 17 、 -C(O)OR 17 、 -NO 2 、 and is optionally substituted with one or more substituents independently selected from -CN. In some embodiments, B is a 6- to 12-membered bridged heterocyclic ring, halogen, -OR 17 、 -SR 17 、 -N(R 17 ) 2 、 -C(O)R 17 、 -C(O)OR 17 、 -NO 2 、 -CN, and C 1~6 alkyl is optionally substituted with one or more substituents independently selected from -CN. C1-C6 alkyl is halogen, -OR 17 、 -SR 17 、 -N(R 17 ) 2 、 -C(O)R 17 、 -C(O)OR 17 、 -NO 2 、 and is optionally substituted with one or more substituents independently selected from -CN. In some embodiments, B is a 6- to 12-membered fused heterocyclic ring, halogen, -OR 17 、 -SR 17 、 -N(R 17 ) 2 、 -C(O)R 17 、 -C(O)OR 17 、 -NO 2 、 -CN, and C 1~6 alkyl is optionally substituted with one or more substituents independently selected from -CN. C1-C6 alkyl is halogen, -OR 17 、 -SR 17 、 -N(R 17 ) 2 、 -C(O)R 17 、 -C(O)OR 17 、 -NO 2 、 and is optionally substituted with one or more substituents independently selected from -CN. In some embodiments, B is a 6- to 12-membered spirocyclic heterocyclic ring, halogen, -OR 17 、 -SR17 、 -N(R 17 ) 2 、 -C(O)R 17 、 -C(O)OR 17 、 -NO 2 、 -CN, and C 1~6 is optionally substituted with one or more substituents independently selected from alkyl, and C1-6 alkyl is halogen, -OR 17 、 -SR 17 、 -N(R 17 ) 2 、 -C(O)R 17 、 -C(O)OR 17 、 -NO 2 、 and -CN. In some embodiments, B is a 9- to 12-membered spirocyclic heterocycle and is optionally substituted with one or more substituents independently selected from halogen, -OR 17 、 -N(R 17 ) 2 、 -C(O)R 17 、 -NO 2 、 -CN and C 1~6 alkyl. In some embodiments, B is
[0065]
Chemical formula
[0066] In some embodiments, C is an optionally substituted C 3~12 carbocyclic ring. In some embodiments, C is an optionally substituted saturated C 3~12 carbocyclic ring. In some embodiments, C is an optionally substituted unsaturated C 3~12 carbocyclic ring. In some embodiments, C is an optionally substituted aromatic C 8~12 carbocyclic ring. In some embodiments, C is a C 3 carbocyclic ring, C 4 carbocyclic ring, C 5 carbocyclic ring, C 6 carbocyclic ring, C 7 carbocyclic ring, C 8Carbon ring, C 9 Carbon ring, C 10 Carbon ring, C 10 Carbon ring, C 11 Carbon ring, and C 12 Selected from carbon rings, any one of which is optionally substituted. In some embodiments, C is C 3~4 Carbon ring, C 3~5 Carbon ring, C 3~6 Carbon ring, C 3~7 Carbon ring, C 3~8 Carbon ring, C 3~9 Carbon ring, C 3~10 Carbon ring, C 3~11 Carbon ring, and C 3~12 Selected from carbon rings, any one of which is optionally substituted. In some embodiments, C is C 3~8 Monocyclic carbon ring and C 6~12 Selected from bicyclic carbon rings, any one of which is optionally substituted. In some embodiments, C is optionally substituted C 3~8 Is a monocyclic carbon ring. In some embodiments, C is optionally substituted C 6~12 Is a bicyclic carbon ring. In some embodiments, C of C 6~12 The bicyclic carbon ring is C 6~12 Spirocyclic carbon ring, C 6~12 Fused carbon ring, and C 6~12 Selected from bridged carbon rings, any one of which is optionally substituted. In some embodiments, the optional substituent of C is as defined herein. In some embodiments, the optional substituent of C is as defined in formula (I).
[0067] In some embodiments, for the compound or salt of formula (I), C is C 3~10 Selected from a carbon ring and a 3- to 10-membered heterocyclic ring, -OR 18A Or -C(O)R 18A And is optionally substituted with, R 18A Is selected from the following: Hydrogen, C 1~6 An alkyl which is halogen, -O-C 1~6Alkyl, -O-C 1~6 Haloalkyl, -NH 2、 -NO 2 , =O, -CN, C 3~10 is optionally substituted with another substituent independently selected from carbocyclic rings and 3- to 10-membered heterocyclic rings, and each C 3~10 carbocyclic ring and 3- to 10-membered heterocyclic ring are optionally substituted with one or more substituents independently selected from halogen, -OH, C 1~6 alkyl, C 1~6 haloalkyl, -O-C 1~6 alkyl, -O-C 1~6 haloalkyl, -NH 2、 -NO 2 , =O, and -CN, and those optionally substituted with one or more substituents independently selected from, and C 3~6 carbocyclic rings and 3- to 6-membered heterocyclic rings optionally substituted with one or more substituents independently selected from the following: halogen, -OH, C 1~6 alkyl, C 1~6 haloalkyl, -O-C 1~6 alkyl, -O-C 1~6 haloalkyl, -NH 2、 -NO 2 , =O, -CN, C 3~6 carbocyclic rings and 3- to 6-membered heterocyclic rings.
[0068] In some embodiments, for the compound or salt of formula (I), C is C 3~10 selected from carbocyclic rings and 3- to 10-membered heterocyclic rings and is optionally substituted with -OR 18A or -C(O)R 18A , and R 18A is, R 18A is C 1~6 selected from alkyl, which is optionally substituted with another substituent independently selected from halogen, C 3~10 carbocyclic rings and 3- to 10-membered heterocyclic rings. In some embodiments, C is C 3~10 selected from carbocyclic rings and 3- to 10-membered heterocyclic rings and is optionally substituted with -OR 18A or -C(O)R 18A , and R 18A is C 1~6Selected from alkyl, which is halogen, C 3~10 Optionally substituted with another substituent independently selected from carbocyclic rings and 3- to 10-membered heterocyclic rings. In some embodiments, C is C 3~10 A carbocyclic ring and a 3- to 10-membered heterocyclic ring, optionally substituted with -OR 18A Or -C(O)R 18A And is optionally substituted with R 18A Is selected from C 3~6 Carbocyclic rings and 3- to 6-membered heterocyclic rings, which are halogen, -OH, C 1~6 Alkyl, C 1~6 Haloalkyl, -O-C 1~6 Alkyl, -O-C 1~6 Haloalkyl, -NH 2、 -NO 2 , =O, -CN, C 3~6 Optionally substituted with one or more substituents independently selected from carbocyclic rings and 3- to 6-membered heterocyclic rings. In some embodiments, C is
[0069]
Chemical formula
[0070] In some embodiments, for the compound or salt of formula (I), C is C 3~12 A carbocyclic ring, optionally substituted with one or more substituents independently selected from the following: Halogen, -OR 18 , -SR 18 , -N(R 18 ) 2 , -C(O)R 18 , -C(O)OR 18 , -OC(O)R 18 , -OC(O)N(R 18 ) 2 , -C(O)N(R 18 ) 2 , -N(R 18 )C(O)R 18 , -N(R 18 )C(O)OR 18 , -N(R 18 )C(O)N(R18 ) 2 , -N(R 18 )C(S)N(R 18 ) 2 , -N(R 18 )S(O) 2 (R 18 ), -S(O)R 18 , -S(O) 2 R 18 , -S(O) 2 N(R 18 ) 2 , -NO 2 , =O, =S, =NR 18 , -N 3 , and -CN, C 1~6 Alkyl, C 2~6 Alkenyl, and C 2~6 Alkynyl, each of which is optionally substituted with one or more substituents independently selected from: Halogen, -OR 18 , -SR 18 , -N(R 18 ) 2 , -C(O)R 18 , -C(O)OR 18 , -OC(O)R 18 , -OC(O)N(R 18 ) 2 , -C(O)N(R 18 ) 2 , -N(R 18 )C(O)R 18 , -N(R 18 )C(O)OR 18 , -N(R 18 )C(O)N(R 18 ) 2 , -N(R 18 )C(S)N(R 18 ) 2 , -N(R 18 )S(O) 2 (R 18 ), -S(O)R 18 , -S(O) 2 R 18 , -S(O) 2 N(R 18 ) 2 , -NO 2 , =O, =S, =NR18 ,-N 3 , and -CN, and C 3~12 a carbocyclic ring and a 3- to 12-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18A , -SR 18A , -N(R 18A ) 2 , -C(O)R 18A , -C(O)OR 18A , -OC(O)R 18A , -OC(O)N(R 18A ) 2 , -C(O)N(R 18A ) 2 , -N(R 18A )C(O)R 18A , -N(R 18A )C(O)OR 18A , -N(R 18A )C(O)N(R 18A ) 2 , -N(R 18A )C(S)N(R 18A ) 2 , -N(R 18A )S(O) 2 (R 18A ), -S(O)R 18A , -S(O) 2 R 18A , -S(O) 2 N(R 18A ) 2 , -NO 2 , =O, =S, =NR 18A , -N 3 , -CN, C 1~10 alkyl, C 3~10 a carbocyclic ring and a 3- to 10-membered heterocyclic ring, where C 1~10 alkyl, C 3~10 the carbocyclic ring and the 3- to 10-membered heterocyclic ring are each halogen, -OR 18A , -SR 18A , -N(R 18A ) 2 , -C(O)R 18A , -C(O)OR 18A , -OC(O)R 18A , -OC(O)N(R 18A )2 ,-C(O)N(R 18A ) 2 ,-N(R 18A )C(O)R 18A ,-N(R 18A )C(O)OR 18A ,-N(R 18A )C(O)N(R 18A ) 2 ,-N(R 18A )C(S)N(R 18A ) 2 ,-N(R 18A )S(O) 2 (R 18A )、-S(O)R 18A 、-S(O) 2 R 18A 、-S(O) 2 N(R 18A ) 2 、-NO 2 、=O、=S、=NR 18A 、-N 3 、-CN、C 1~6 alkyl、C 1~6 haloalkyl、C 3~6 carbocyclic ring、-C 3~6 carbocyclic ring-(C 1~6 haloalkyl), and those optionally substituted with one or more substituents independently selected from 3- to 6-membered heterocyclic rings, and, C 3~6 carbocyclic rings and 3- to 6-membered heterocyclic rings, each of which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 、-SR 18 、-N(R 18 ) 2 、-C(O)R 18 、-NO 2 、=O、=S、=NR 18 、-N 3 、-CN、and C 1~6 alkyl which is halogen, -OR 18A 、-SR 18A 、-N(R 18A ) 2 、-C(O)R 18A 、-C(O)OR 18A 、-OC(O)R18A ,-OC(O)N(R 18A ) 2 ,-C(O)N(R 18A ) 2 ,-N(R 18A )C(O)R 18A ,-N(R 18A )C(O)OR 18A ,-N(R 18A )C(O)N(R 18A ) 2 ,-N(R 18A )C(S)N(R 18A ) 2 ,-N(R 18A )S(O) 2 (R 18A )、-S(O)R 18A 、-S(O) 2 R 18A 、-S(O) 2 N(R 18A ) 2 、-NO 2 、=O、=S、=NR 18A 、-N 3 、-CN、C 3~6 is optionally substituted with one or more substituents independently selected from a carbocyclic ring and 3- to 6-membered heterocyclic rings, and the C 3~6 carbocyclic ring and 3- to 6-membered heterocyclic rings are each halogen, -OR 18A ,-SR 18A ,-N(R 18A ) 2 ,-C(O)R 18A ,-C(O)OR 18A ,-OC(O)R 18A ,-OC(O)N(R 18A ) 2 ,-C(O)N(R 18A ) 2 ,-N(R 18A )C(O)R 18A 、-N(R 18A )C(O)OR 18A 、-N(R 18A )C(O)N(R 18A ) 2 、-N(R 18A )C(S)N(R 18A ) 2 、-N(R 18A )S(O) 2 (R18A )、 -S(O)R 18A 、 -S(O) 2 R 18A 、 -S(O) 2 N(R 18A ) 2 、 -NO 2 、 =O、 =S、 =NR 18A 、 -N 3 、 and optionally substituted with one or more substituents independently selected from -CN.
[0071] In some embodiments, for the compound or salt of formula (I), C is a carbocycle optionally substituted with one or more substituents independently selected from: 3~10 a carbocycle optionally substituted with one or more substituents independently selected from: halogen, -OR 18 、 -SR 18 、 -N(R 18 ) 2 、 -C(O)R 18 、 -C(O)OR 18 、 -OC(O)R 18 、 -OC(O)N(R 18 ) 2 、 -C(O)N(R 18 ) 2 、 -N(R 18 )C(O)R 18 、 -NO 2 、 and -CN, C 1~6 an alkyl optionally substituted with one or more substituents independently selected from: halogen, -OR 18 、 -SR 18 、 -N(R 18 ) 2 、 -C(O)R 18 、 -C(O)OR 18 、 -OC(O)R 18 、 -OC(O)N(R 18 ) 2 、 -C(O)N(R 18 ) 2 、 -N(R 18 )C(O)R 18 、 -NO 2 、 and -CN, and C 3~12A carbon ring and a 3- to 12-membered heterocyclic ring, each of which is independently selected from halogen, -OR 18A , -SR 18A , -N(R 18A ) 2 , -C(O)R 18A , -C(O)OR 18A , -OC(O)R 18A , -OC(O)N(R 18A ) 2 , -C(O)N(R 18A ) 2 , -N(R 18A )C(O)R 18A , -NO 2 , -CN, C 1~6 alkyl, C 3~6 carbon ring and 3- to 6-membered heterocyclic ring are each independently optionally substituted with one or more substituents selected from: 1~6 alkyl, C 3~6 carbon ring and 3- to 6-membered heterocyclic ring are each independently selected from halogen, -OR 18A , -SR 18A , -N(R 18A ) 2 , -C(O)R 18A , -C(O)OR 18A , -OC(O)R 18A , -OC(O)N(R 18A ) 2 , -C(O)N(R 18A ) 2 , -N(R 18A )C(O)R 18A , -NO 2 , -CN, C 1~6 alkyl, C 1~6 haloalkyl, C 3~6 carbon ring, -C 3~6 carbon ring-(C 1~6 haloalkyl), and 3- to 6-membered heterocyclic ring are each independently optionally substituted with one or more substituents selected from: C 3~6 carbon ring and 3- to 6-membered heterocyclic ring, each of which is independently optionally substituted with one or more substituents selected from: halogen, -OR 18 , -SR 18 , -N(R 18 ) 2, -C(O)R 18 , -NO 2 , and -CN, and C 1~6 alkyl, which is halogen, -OR 18A , -SR 18A , -N(R 18A ) 2 , -C(O)R 18A , -C(O)OR 18A , -OC(O)R 18A , -OC(O)N(R 18A ) 2 , -C(O)N(R 18A ) 2 , -N(R 18A )C(O)R 18A , -NO 2 , -CN, C 3~6 is optionally substituted with one or more substituents independently selected from carbocyclic rings and 3- to 6-membered heterocyclic rings, and C 3~6 carbocyclic rings and 3- to 6-membered heterocyclic rings are each halogen, -OR 18A , -SR 18A , -N(R 18A ) 2 , -C(O)R 18A , -C(O)OR 18A , -OC(O)R 18A , -OC(O)N(R 18A ) 2 , -C(O)N(R 18A ) 2 , -N(R 18A )C(O)R 18A , -NO 2 , -CN, and is optionally substituted with one or more substituents independently selected therefrom.
[0072] In some embodiments, for the compound or salt of formula (I), C is a C 3~6 carbocyclic ring and is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 , -SR 18 , -N(R 18 ) 2 , -C(O)R 18 , -C(O)OR 18 , -OC(O)R18 ,-OC(O)N(R 18 ) 2 ,-C(O)N(R 18 ) 2 ,-N(R 18 )C(O)R 18 ,-NO 2 ,and -CN, C 1~6 alkyl, optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 , -SR 18 , -N(R 18 ) 2 , -C(O)R 18 , -C(O)OR 18 , -OC(O)R 18 , -OC(O)N(R 18 ) 2 , -C(O)N(R 18 ) 2 , -N(R 18 )C(O)R 18 , -NO 2 ,and -CN, and, C 3~12 a carbocyclic ring and a 3- to 12-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from halogen, -OR 18A , -SR 18A , -N(R 18A ) 2 , -C(O)R 18A , -C(O)OR 18A , -OC(O)R 18A , -OC(O)N(R 18A ) 2 , -C(O)N(R 18A ) 2 , -N(R 18A )C(O)R 18A , -NO 2 , -CN, C 1~6 alkyl, C 3~6 a carbocyclic ring and a 3- to 6-membered heterocyclic ring, optionally substituted with one or more substituents independently selected from C 1~6 alkyl, C 3~6 a carbocyclic ring and a 3- to 6-membered heterocyclic ring, each of which is independently halogen, -OR 18A , -SR 18A , -N(R 18A) 2 、 -C(O)R 18A 、 -C(O)OR 18A 、 -OC(O)R 18A 、 -OC(O)N(R 18A ) 2 、 -C(O)N(R 18A ) 2 、 -N(R 18A )C(O)R 18A 、 -NO 2 、 -CN, C 1~6 alkyl, C 1~6 haloalkyl, C 3~6 carbocyclic, -C 3~6 carbocyclic-(C 1~6 haloalkyl), and those optionally substituted with one or more substituents independently selected from 3- to 6-membered heterocycles, and, C 3~6 carbocyclic and 3- to 6-membered heterocyclic, each of which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 、 -SR 18 、 -N(R 18 ) 2 、 -C(O)R 18 、 -NO 2 、 and -CN, and, C 1~6 alkyl which is halogen, -OR 18A 、 -SR 18A 、 -N(R 18A ) 2 、 -C(O)R 18A 、 -C(O)OR 18A 、 -OC(O)R 18A 、 -OC(O)N(R 18A ) 2 、 -C(O)N(R 18A ) 2 、 -N(R 18A )C(O)R 18A 、 -NO 2 、 -CN, C 3~6 carbocyclic and 3- to 6-membered heterocyclic independently selected from one or more substituents optionally substituted, C 3~6 carbocyclic and 3- to 6-membered heterocyclic are each halogen, -OR 18A 、 -SR18A , -N(R 18A ) 2 , -C(O)R 18A , -C(O)OR 18A , -OC(O)R 18A , -OC(O)N(R 18A ) 2 , -C(O)N(R 18A ) 2 , -N(R 18A )C(O)R 18A , -NO 2 One or more substituents independently selected from -CN, and optionally substituted therewith.
[0073] In some embodiments, for the compound or salt of formula (I), C is phenyl, optionally substituted with one or more substituents independently selected from: Halogen, -OR 18 , -SR 18 , -N(R 18 ) 2 , -C(O)R 18 , -C(O)OR 18 , -OC(O)R 18 , -OC(O)N(R 18 ) 2 , -C(O)N(R 18 ) 2 , -N(R 18 )C(O)R 18 , -NO 2 , and -CN, and C 1~6 Alkyl, optionally substituted with one or more substituents independently selected from: Halogen, -OR 18 , -SR 18 , -N(R 18 ) 2 , -C(O)R 18 , -C(O)OR 18 , -OC(O)R 18 , -OC(O)N(R 18 ) 2 , -C(O)N(R 18 ) 2 , -N(R 18 )C(O)R 18 , -NO2 and -CN, and C 3~12 a carbocyclic ring and a 3- to 12-membered heterocyclic ring, each of which is halogen, -OR 18A , -SR 18A , -N(R 18A ) 2 , -C(O)R 18A , -C(O)OR 18A , -OC(O)R 18A , -OC(O)N(R 18A ) 2 , -C(O)N(R 18A ) 2 , -N(R 18A )C(O)R 18A , -NO 2 , -CN, C 1~6 alkyl, C 3~6 a carbocyclic ring and a 3- to 6-membered heterocyclic ring are each independently optionally substituted with one or more substituents selected from 1~6 alkyl, C 3~6 a carbocyclic ring and a 3- to 6-membered heterocyclic ring are each halogen, -OR 18A , -SR 18A , -N(R 18A ) 2 , -C(O)R 18A , -C(O)OR 18A , -OC(O)R 18A , -OC(O)N(R 18A ) 2 , -C(O)N(R 18A ) 2 , -N(R 18A )C(O)R 18A , -NO 2 , -CN, C 1~6 alkyl, C 1~6 haloalkyl, C 3~6 a carbocyclic ring, -C 3~6 a carbocyclic ring-(C 1~6 haloalkyl), and are each independently optionally substituted with one or more substituents selected from 3- to 6-membered heterocyclic rings.
[0074] In some embodiments, for the compound or salt of formula (I), C is phenyl and is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 , -N(R 18 ) 2 , -NO 2 , and -CN, and, C 1~6 alkyl which is optionally substituted with one or more substituents independently selected from halogen, -OR 18 , -N(R 18 ) 2 , -NO 2 , and -CN, and a 3- to 12-membered saturated heterocyclic ring which is optionally substituted with one or more substituents independently selected from halogen, -OR 18A , -NO 2 , -CN, C 1~6 alkyl, C 3~6 carbocyclic ring and 3- to 6-membered heterocyclic ring, and C 1~6 alkyl, C 3~6 carbocyclic ring and 3- to 6-membered heterocyclic ring are each optionally substituted with one or more substituents independently selected from halogen, -OR 18A , -N(R 18A ) 2 , -NO 2 , -CN, C 1~6 alkyl, C 1~6 haloalkyl, C 3~6 carbocyclic ring, -C 3~6 carbocyclic ring-(C 1~6 haloalkyl), and a 3- to 6-membered heterocyclic ring which is optionally substituted with one or more substituents independently selected therefrom.
[0075] In some embodiments, for the compound or salt of formula (I), C is phenyl and is optionally substituted with one or more substituents independently selected from: halogen, -OR 18 , -N(R 18 ) 2 , -NO 2 , and -CN, and, C 1~6 alkyl which is optionally substituted with one or more substituents independently selected from halogen, -OR 18 , -N(R 18 ) 2 , -NO 2and optionally substituted with one or more substituents independently selected from -CN, and 3- to 7-membered heterocycloalkyl, halogen, -OR 18A , -NO 2 , -CN, C 1~6 alkyl, C 3~6 optionally substituted with one or more substituents independently selected from carbocyclic rings and 3- to 6-membered heterocyclic rings, C 1~6 alkyl, C 3~6 carbocyclic rings and 3- to 6-membered heterocyclic rings are each halogen, -OR 18A , -N(R 18A ) 2 , -NO 2 , -CN, C 1~6 alkyl, C 1~6 haloalkyl, C 3~6 carbocyclic ring, -C 3~6 carbocyclic ring-(C 1~6 haloalkyl), and optionally substituted with one or more substituents independently selected from 3- to 6-membered heterocyclic rings.
[0076] In some embodiments, for the compound or salt of formula (I), C is phenyl and is optionally substituted with one or more substituents independently selected from: halogen, -OR 18 , -N(R 18 ) 2 , -NO 2 , and -CN, and C 1~6 alkyl which is optionally substituted with one or more substituents independently selected from: halogen, -OR 18 , -N(R 18 ) 2 , -NO 2 , -CN, and azetidinyl, piperidinyl, piperazinyl, and azapanil, each of which is halogen, -OR 18A , -NO 2 , -CN, C 1~6 alkyl, C 3~6 optionally substituted with one or more substituents independently selected from carbocyclic rings and 3- to 6-membered heterocyclic rings, C1~6 Alkyl, C 3~6 The carbocyclic ring and the 3- to 6-membered heterocyclic ring are each independently selected from halogen, -OR 18A , -N(R 18A ), 2 , -NO 2 , -CN, C 1~6 alkyl, C 1~6 haloalkyl, C 3~6 carbocyclic ring, -C 3~6 carbocyclic ring-(C 1~6 haloalkyl), and are optionally substituted with one or more substituents independently selected from 3- to 6-membered heterocyclic rings, R 18 and R 18A each is independently, each time it appears, hydrogen, halogen, C 1~6 alkyl, and C 1~6 haloalkyl.
[0077] In some embodiments, for the compound or salt of formula (I), C is phenyl and is optionally substituted with one or more substituents independently selected from: halogen, -OR 18 , -N(R 18 ), 2 , -NO 2 , and -CN, and C 1~6 alkyl which is optionally substituted with piperidinyl, piperazinyl, and azapanyl, each of which is halogen, -OR 18A , -NO 2 , -CN, C 1~6 alkyl, C 3~6 carbocyclic ring and 3- to 6-membered heterocyclic ring are each independently selected from halogen, -OR 1~6 , -N(R 3~6 ), 18A , -NO 18A ), 2 , -NO 2 , -CN, C 1~6 alkyl, C 1~6 haloalkyl, C 3~6 carbocyclic ring, -C 3~6 carbocyclic ring-(C 1~6(haloalkyl), and optionally substituted with one or more substituents independently selected from 3- to 6-membered heterocycles, R 18 and R 18A are, independently for each occurrence, hydrogen, halogen, C 1~6 alkyl, and C 1~6 haloalkyl. In some embodiments, C is
[0078]
Chemical formula
[0079] In some embodiments, for the compound or salt of formula (I), C is phenyl and is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 , -N(R 18 ) 2 , -NO 2 , and -CN, and C 1~6 alkyl which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 , -N(R 18 ) 2 , -NO 2 , and -CN, and an 8- to 12-membered spirocyclic saturated heterocycle which is optionally substituted with halogen, -OR 18A , -NO 2 , -CN, C 1~6 alkyl, C 3~6 carbocyclic ring and optionally substituted with one or more substituents independently selected from 3- to 6-membered heterocycles, C 1~6 alkyl, C 3~6 carbocyclic ring and 3- to 6-membered heterocycles are each halogen, -OR 18A , -N(R 18A ) 2 , -NO 2 , -CN, C 1~6 alkyl, C 1~6 haloalkyl, C 3~6Those optionally substituted with one or more substituents independently selected from a carbon ring and 3- to 6-membered heterocycles.
[0080] In some embodiments, for the compound or salt of formula (I), C is phenyl, optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 , -N(R 18 ) 2 , -NO 2 , and -CN, and C 1~6 alkyl, optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 , -N(R 18 ) 2 , -NO 2 , and -CN, and 6-azaspiro[2.5]octanyl, 2-oxa-8-azaspiro[4.5]decanil, 3-azaspiro[5.5]undecanyl, and 2,9-diazaspiro[5.5]undecanyl, each of which is optionally substituted with halogen, -OR 18A , -NO 2 , -CN, C 1~6 alkyl, C 3~6 a carbon ring and optionally substituted with one or more substituents independently selected from 3- to 6-membered heterocycles, C 1~6 alkyl, C 3~6 a carbon ring and 3- to 6-membered heterocycles are each optionally substituted with halogen, -OR 18A , -N(R 18A ) 2 , -NO 2 , -CN, C 1~6 alkyl, C 1~6 haloalkyl, C 3~6 a carbon ring, and optionally substituted with one or more substituents independently selected from 3- to 6-membered heterocycles, R 18 and R 18A each of which is independently, at each occurrence, hydrogen, halogen, C 1~6 alkyl, and C 1~6 haloalkyl.
[0081] In some embodiments, for the compound or salt of formula (I), C is phenyl, optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 , -N(R 18 ), 2 , -NO 2 , and -CN, and C 1~6 is alkyl, optionally substituted with one or more of 6-azaspiro[2.5]octanyl, 2-oxa-8-azaspiro[4.5]decanil, 3-azaspiro[5.5]undecanyl, and 2,9-diazaspiro[5.5]undecanyl, each of which is optionally substituted with halogen, -OR 18A , -NO 2 , -CN, C 1~6 alkyl, C 3~6 carbocyclic ring and one or more substituents independently selected from 3- to 6-membered heterocyclic rings, and C 1~6 alkyl, C 3~6 carbocyclic ring and 3- to 6-membered heterocyclic ring are each optionally substituted with halogen, -OR 18A , -N(R 18A ), 2 , -NO 2 , -CN, C 1~6 alkyl, C 1~6 haloalkyl, C 3~6 carbocyclic ring, and one or more substituents independently selected from 3- to 6-membered heterocyclic rings, and each of R 18 and R 18A is independently, each time it appears, selected from hydrogen, halogen, C 1~6 alkyl, and C 1~6 haloalkyl. In some embodiments, C is
[0082]
Chemical formula
[0083] In some embodiments, for the compound or salt of formula (I), C is phenyl, optionally substituted with one or more substituents independently selected from: halogen, -OR 18 , -N(R 18 ) 2 , -NO 2 , and -CN, and C 1~6 alkyl, optionally substituted with one or more substituents independently selected from: halogen, -OR 18 , -N(R 18 ) 2 , -NO 2 , and -CN, and an 8- to 10-membered bridged saturated heterocyclic ring, optionally substituted with one or more substituents independently selected from halogen, -OR 18A , -NO 2 , -CN, C 1~6 alkyl, C 3~6 a carbocyclic ring and a 3- to 6-membered heterocyclic ring, each optionally substituted with one or more substituents independently selected from halogen, -OR 1~6 alkyl, C 3~6 a carbocyclic ring and a 3- to 6-membered heterocyclic ring, each optionally substituted with one or more substituents independently selected from halogen, -OR 18A , -N(R 18A ) 2 , -NO 2 , -CN, C 1~6 alkyl, C 1~6 haloalkyl, C 3~6 a carbocyclic ring, and a 3- to 6-membered heterocyclic ring, each optionally substituted with one or more substituents independently selected from those described above.
[0084] In some embodiments, for the compound or salt of formula (I), C is phenyl, optionally substituted with one or more substituents independently selected from: halogen, -OR 18 , -N(R 18 ) 2 , -NO 2 , and -CN, and C 1~6 alkyl, optionally substituted with one or more substituents independently selected from: halogen, -OR 18 , -N(R 18 ) 2 , -NO 2 , and -CN, and, 8-oxa-3-azabicyclo[3.2.1]octanyl, which is optionally substituted with one or more substituents independently selected from halogen, -OR 18A , -NO 2 , -CN, C 1~6 alkyl, C 3~6 carbocyclic ring and 3- to 6-membered heterocyclic ring, and is optionally substituted with one or more substituents independently selected from halogen, -OR 1~6 alkyl, C 3~6 carbocyclic ring and 3- to 6-membered heterocyclic ring are each optionally substituted with one or more substituents independently selected from halogen, -OR 18A , -N(R 18A ) 2 , -NO 2 , -CN, C 1~6 alkyl, C 1~6 haloalkyl, C 3~6 carbocyclic ring, and 3- to 6-membered heterocyclic ring, and is optionally substituted with one or more substituents independently selected from halogen, -OR 18 and R 18A and each of R 1~6 alkyl, and C 1~6 haloalkyl.
[0085] In some embodiments, for the compound or salt of formula (I), C is phenyl and is optionally substituted with one or more substituents independently selected from: halogen, -OR 18 , -N(R 18 ) 2 , -NO 2 , and -CN, and, C 1~6 alkyl which is optionally substituted with 8-oxa-3-azabicyclo[3.2.1]octanyl, and is optionally substituted with one or more substituents independently selected from halogen, -OR 18A , -NO 2 , -CN, C 1~6 alkyl, C 3~6 carbocyclic ring and 3- to 6-membered heterocyclic ring, and is optionally substituted with one or more substituents independently selected from halogen, -OR 1~6 alkyl, C3~6 The carbon ring and the 3- to 6-membered heterocyclic ring are each optionally substituted with one or more substituents independently selected from halogen, -OR 18A , -N(R 18A ), 2 , -NO 2 , -CN, C 1~6 alkyl, C 1~6 haloalkyl, C 3~6 carbon ring, and 3- to 6-membered heterocyclic ring, and each of R 18 and R 18A is independently, each time it appears, selected from hydrogen, halogen, C 1~6 alkyl, and C 1~6 haloalkyl.
[0086] In some embodiments, for the compound or salt of formula (I), C is phenyl and is optionally substituted with one or more substituents independently selected from: -OR 18 , -CN, and C 1~6 alkyl which is optionally substituted with 8-oxa-3-azabicyclo[3.2.1]octanyl, and is optionally substituted with a substituent independently selected from halogen, -OR 18A , -NO 2 , -CN, and C 1~6 alkyl. In some embodiments, C is
[0087]
Chemical formula
[0088] In some embodiments, for the compound or salt of formula (I), C is phenyl and is optionally substituted with one or more substituents independently selected from: halogen, -OR 18 , -N(R 18 ), 2 , -NO 2 , and -CN, and C 1~6An alkyl group, optionally substituted with one or more substituents independently selected from the following: Halogen, -OR 18 , -N(R 18 ) 2 , -NO 2 , and -CN, and A 6- to 10-membered fused saturated heterocyclic ring, optionally substituted with one or more substituents independently selected from halogen, -OR 18A , -NO 2 , -CN, C 1~6 alkyl, C 3~6 a carbocyclic ring and a 3- to 6-membered heterocyclic ring, each optionally substituted with one or more substituents independently selected from halogen, -OR 1~6 alkyl, C 3~6 a carbocyclic ring and a 3- to 6-membered heterocyclic ring, each optionally substituted with one or more substituents independently selected from halogen, -OR 18A , -N(R 18A ) 2 , -NO 2 , -CN, C 1~6 alkyl, C 1~6 haloalkyl, C 3~6 a carbocyclic ring, and a 3- to 6-membered heterocyclic ring, each optionally substituted with one or more substituents independently selected from those described above.
[0089] In some embodiments, for the compound or salt of formula (I), C is phenyl, optionally substituted with one or more substituents independently selected from the following: Halogen, -OR 18 , -N(R 18 ) 2 , -NO 2 , and -CN, and C 1~6 an alkyl group, optionally substituted with one or more substituents independently selected from the following: Halogen, -OR 18 , -N(R 18 ) 2 , -NO 2 , and -CN, and octahydro-1H-isoindolyl, optionally substituted with halogen, -OR 18A , -NO 2 , -CN, C 1~6 alkyl, C3~6 Optionally substituted with one or more substituents independently selected from a carbon ring and one or more 3- to 6-membered heterocyclic rings, C 1~6 alkyl, C 3~6 The carbon ring and the 3- to 6-membered heterocyclic ring are each independently halogen, -OR 18A , -N(R 18A ) 2 , -NO 2 , -CN, C 1~6 alkyl, C 1~6 haloalkyl, C 3~6 a carbon ring, and optionally substituted with one or more substituents independently selected from one or more 3- to 6-membered heterocyclic rings, R 18 and R 18A each independently, at each occurrence, is selected from hydrogen, halogen, C 1~6 alkyl, and C 1~6 haloalkyl.
[0090] In some embodiments, for the compound or salt of formula (I), C is phenyl, halogen, -OR 18 , -N(R 18 ) 2 , -NO 2 , and -CN, and C 1~6 alkyl which is optionally substituted with one or more substituents independently selected from halogen, -OR 18A , -NO 2 , -CN, and C 1~6 alkyl, and optionally substituted with one or more substituents independently selected from one or more octahydro-1H-isoindolyls which are optionally substituted with one or more substituents independently selected from halogen, -OR
[0091]
Chemical formula
[0092] In some embodiments, for the compound or salt of formula (I), C is C 6~12 a carbon ring, which is C 3~6Optionally substituted with one or more substituents independently selected from a carbon ring and 3- to 6-membered heterocyclic rings, each of which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 , -SR 18 , -N(R 18 ) 2 , -C(O)R 18 , -NO 2 , =O, =S, =NR 18 , -N 3 , -CN, and C 1~6 alkyl, which is optionally substituted with one or more substituents independently selected from halogen, -OR 18A , -SR 18A , -N(R 18A ) 2 , -C(O)R 18A , -C(O)OR 18A , -OC(O)R 18A , -OC(O)N(R 18A ) 2 , -C(O)N(R 18A ) 2 , -N(R 18A )C(O)R 18A , -N(R 18A )C(O)OR 18A , -N(R 18A )C(O)N(R 18A ) 2 , -N(R 18A )C(S)N(R 18A ) 2 , -N(R 18A )S(O) 2 (R 18A ), -S(O)R 18A , -S(O) 2 R 18A , -S(O) 2 N(R 18A ) 2 , -NO 2 , =O, =S, =NR 18A , -N 3 , -CN, C 3~6 Optionally substituted with one or more substituents independently selected from a carbon ring and 3- to 6-membered heterocyclic rings, C 3~6 The carbon ring and 3- to 6-membered heterocyclic rings are each optionally substituted with halogen, -OR 18A, -SR 18A , -N(R 18A ) 2 , -C(O)R 18A , -C(O)OR 18A , -OC(O)R 18A , -OC(O)N(R 18A ) 2 , -C(O)N(R 18A ) 2 , -N(R 18A )C(O)R 18A , -N(R 18A )C(O)OR 18A , -N(R 18A )C(O)N(R 18A ) 2 , -N(R 18A )C(S)N(R 18A ) 2 , -N(R 18A )S(O) 2 (R 18A ), -S(O)R 18A , -S(O) 2 R 18A , -S(O) 2 N(R 18A ) 2 , -NO 2 , =O, =S, =NR 18A , -N 3 , and optionally substituted with one or more substituents independently selected from -CN.
[0093] In some embodiments, for the compound or salt of formula (I), C is a C 8~12 condensed carbocycle, optionally substituted with one or more substituents independently selected from: a 5- to 6-membered heteroaryl, optionally substituted with one or more substituents independently selected from: halogen, -OR 18 , -SR 18 , -N(R 18 ) 2 , -NO 2 , -CN, and, C 1~6 alkyl, substituted with halogen, -OR 18A , -N(R 18A ) 2 , -NO 2, -CN, C 3~6 Optionally substituted with one or more substituents independently selected from a carbon ring and a 3- to 6-membered heterocyclic ring, C 3~6 The carbon ring and the 3- to 6-membered heterocyclic ring are each halogen, -OR 18A , -N(R 18A ) 2 , -NO 2 , -CN, and are optionally substituted with one or more substituents independently selected therefrom, R 18 and R 18A Each of which is independently, for each occurrence, hydrogen, halogen, C 1~6 alkyl, and C 1~6 haloalkyl.
[0094] In some embodiments, for the compound or salt of formula (I), C is C 8~12 A fused carbon ring, optionally substituted with one or more substituents independently selected from the following, and optionally substituted with one or more substituents independently selected from a 5- to 6-membered heteroaryl: C 1~6 alkyl, which is halogen, C 3~6 Optionally substituted with one or more substituents independently selected from a carbon ring and a 3- to 6-membered heterocyclic ring, C 3~6 The carbon ring and the 3- to 6-membered heterocyclic ring are each optionally substituted with one or more substituents independently selected from halogen. In some embodiments, for the compound or salt of formula (I), C is
[0095]
Chemical formula
[0096] In some embodiments, C is an optionally substituted 3- to 12-membered heterocyclic ring. In some embodiments, C is an optionally substituted 3- to 12-membered saturated heterocyclic ring. In some embodiments, C is an optionally substituted 3- to 12-membered unsaturated heterocyclic ring. In some embodiments, C is an optionally substituted 6- to 12-membered aromatic heterocyclic ring. In some embodiments, C is selected from a 3-membered heterocyclic ring, a 4-membered heterocyclic ring, a 5-membered heterocyclic ring, a 6-membered heterocyclic ring, a 7-membered heterocyclic ring, an 8-membered heterocyclic ring, a 9-membered heterocyclic ring, a 10-membered heterocyclic ring, an 11-membered heterocyclic ring, and a 12-membered heterocyclic ring, any one of which is optionally substituted. In some embodiments, C is selected from a 3- to 4-membered heterocyclic ring, a 3- to 5-membered heterocyclic ring, a 3- to 6-membered heterocyclic ring, a 3- to 7-membered heterocyclic ring, a 3- to 8-membered heterocyclic ring, a 3- to 9-membered heterocyclic ring, a 3- to 10-membered heterocyclic ring, a 3- to 11-membered heterocyclic ring, and a 3- to 12-membered heterocyclic ring, any one of which is optionally substituted. In some embodiments, C is selected from a 3- to 8-membered monocyclic heterocyclic ring and a 6- to 12-membered bicyclic heterocyclic ring, any one of which is optionally substituted. In some embodiments, C is an optionally substituted 3- to 8-membered monocyclic heterocyclic ring. In some embodiments, C is an optionally substituted 6- to 12-membered bicyclic heterocyclic ring. In some embodiments, the optionally substituted 6- to 12-membered bicyclic heterocyclic ring of C is selected from a 6- to 12-membered bridged heterocyclic ring, a 6- to 12-membered spirocyclic heterocyclic ring, and a 6- to 12-membered fused heterocyclic ring, any one of which is optionally substituted. In some embodiments, the optional substituent of C is as defined herein. In some embodiments, the optional substituent of C is as defined in formula (I).
[0097] In some embodiments, for the compound or salt of formula (I), C is an optionally substituted 3- to 12-membered heterocyclic ring independently selected from one or more of the following substituents: halogen, -OR 18 , -SR 18 , -N(R 18 ) 2 , -C(O)R 18 , -C(O)OR 18 , -OC(O)R18 、 -OC(O)N(R 18 ) 2 、 -C(O)N(R 18 ) 2 、 -N(R 18 )C(O)R 18 、 -N(R 18 )C(O)OR 18 、 -N(R 18 )C(O)N(R 18 ) 2 、 -N(R 18 )C(S)N(R 18 ) 2 、 -N(R 18 )S(O) 2 (R 18 )、 -S(O)R 18 、 -S(O) 2 R 18 、 -S(O) 2 N(R 18 ) 2 、 -NO 2 、 =O、 =S、 =NR 18 、 -N 3 、 and -CN, C 1~6 alkyl, C 2~6 alkenyl, and C 2~6 alkynyl, each of which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 、 -SR 18 、 -N(R 18 ) 2 、 -C(O)R 18 、 -C(O)OR 18 、 -OC(O)R 18 、 -OC(O)N(R 18 ) 2 、 -C(O)N(R 18 ) 2 、 -N(R 18 )C(O)R 18 、 -N(R 18 )C(O)OR 18 、 -N(R 18 )C(O)N(R 18 ) 2 、 -N(R 18 )C(S)N(R 18 ) 2, -N(R 18 )S(O) 2 (R 18 ), -S(O)R 18 , -S(O) 2 R 18 , -S(O) 2 N(R 18 ) 2 , -NO 2 , =O, =S, =NR 18 , -N 3 , and -CN, and, C 3~12 a carbocyclic ring and a 3- to 12-membered heterocyclic ring, any of which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18A , -SR 18A , -N(R 18A ) 2 , -C(O)R 18A , -C(O)OR 18A , -OC(O)R 18A , -OC(O)N(R 18A ) 2 , -C(O)N(R 18A ) 2 , -N(R 18A )C(O)R 18A , -N(R 18A )C(O)OR 18A , -N(R 18A )C(O)N(R 18A ) 2 , -N(R 18A )C(S)N(R 18A ) 2 , -N(R 18A )S(O) 2 (R 18A ), -S(O)R 18A , -S(O) 2 R 18A , -S(O) 2 N(R 18A ) 2 , -NO 2 , =O, =S, =NR 18A , -N 3 , -CN, C 1~10 alkyl, C 3~10 a carbocyclic ring and a 3- to 10-membered heterocyclic ring, C 1~10 alkyl, C3~10 The carbon ring and the 3- to 10-membered heterocyclic ring are each independently selected from halogen, -OR 18A , -SR 18A , -N(R 18A ) 2 , -C(O)R 18A , -C(O)OR 18A , -OC(O)R 18A , -OC(O)N(R 18A ) 2 , -C(O)N(R 18A ) 2 , -N(R 18A )C(O)R 18A , -N(R 18A )C(O)OR 18A , -N(R 18A )C(O)N(R 18A ) 2 , -N(R 18A )C(S)N(R 18A ) 2 , -N(R 18A )S(O) 2 (R 18A ), -S(O)R 18A , -S(O) 2 R 18A , -S(O) 2 N(R 18A ) 2 , -NO 2 , =O, =S, =NR 18A , -N 3 , -CN, C 1~6 alkyl, C 1~6 haloalkyl, C 3~6 carbon ring, -C 3~6 carbon ring-(C 1~6 haloalkyl), and are optionally substituted with one or more substituents independently selected from 3- to 6-membered heterocyclic rings, and C 3~6 carbon rings and 3- to 6-membered heterocyclic rings, each of which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 , -SR 18 , -N(R 18 ) 2 , -C(O)R 18 , -NO 2 , =O, =S, =NR18 , -N 3 , -CN, and C 1~6 alkyl, which is optionally substituted with one or more substituents independently selected from halogen, -OR 18A , -SR 18A , -N(R 18A ) 2 , -C(O)R 18A , -C(O)OR 18A , -OC(O)R 18A , -OC(O)N(R 18A ) 2 , -C(O)N(R 18A ) 2 , -N(R 18A )C(O)R 18A , -N(R 18A )C(O)OR 18A , -N(R 18A )C(O)N(R 18A ) 2 , -N(R 18A )C(S)N(R 18A ) 2 , -N(R 18A )S(O) 2 (R 18A ), -S(O)R 18A , -S(O) 2 R 18A , -S(O) 2 N(R 18A ) 2 , -NO 2 , =O, =S, =NR 18A , -N 3 , -CN, C 3~6 is optionally substituted with one or more substituents independently selected from carbocyclic rings and 3- to 6-membered heterocyclic rings, and C 3~6 carbocyclic rings and 3- to 6-membered heterocyclic rings are each halogen, -OR 18A , -SR 18A , -N(R 18A ) 2 , -C(O)R 18A , -C(O)OR 18A , -OC(O)R 18A , -OC(O)N(R 18A ) 2 , -C(O)N(R 18A ) 2 , -N(R 18A )C(O)R18A , -N(R 18A )C(O)OR 18A , -N(R 18A )C(O)N(R 18A ) 2 , -N(R 18A )C(S)N(R 18A ) 2 , -N(R 18A )S(O) 2 (R 18A ), -S(O)R 18A , -S(O) 2 R 18A , -S(O) 2 N(R 18A ) 2 , -NO 2 , =O, =S, =NR 18A , -N 3 , and one or more substituents independently selected from -CN, optionally substituted.
[0098] In some embodiments, for the compound or salt of formula (I), C is pyridinyl, optionally substituted with one or more substituents independently selected from: halogen, -OR 18 , -N(R 18 ) 2 , -C(O)R 18 , -NO 2 , and -CN, and C 1~6 alkyl, optionally substituted with one or more substituents independently selected from: halogen, -OR 18 , -N(R 18 ) 2 , -C(O)R 18 , -NO 2 , and -CN, and C 3~12 carbocyclic and 3- to 12-membered heterocyclic rings, each optionally substituted with one or more substituents independently selected from: halogen, -OR 18A , -N(R 18A ) 2 , -C(O)R 18A , -NO2 、 -CN, C 1~6 alkyl, C 3~6 a carbocyclic ring and a 3- to 6-membered heterocyclic ring, C 1~6 alkyl, C 3~6 the carbocyclic ring and the 3- to 6-membered heterocyclic ring are each independently optionally substituted with one or more substituents selected from halogen, -OR 18A , -N(R 18A ) 2 , -C(O)R 18A , -NO 2 , -CN, C 1~6 alkyl, C 1~6 haloalkyl, C 3~6 a carbocyclic ring, -C 3~6 a carbocyclic ring-(C 1~6 haloalkyl), and are each independently optionally substituted with one or more substituents selected from a 3- to 6-membered heterocyclic ring, R 18 and R 18A each independently, for each occurrence, is selected from hydrogen, halogen, C 1~6 alkyl, and C 1~6 haloalkyl.
[0099] In some embodiments, for the compound or salt of formula (I), C is pyridinyl and is optionally substituted with one or more substituents independently selected from: halogen, -OR 18 , -NO 2 , and -CN, and C 1~6 alkyl, where C 3~12 is optionally substituted with one or more substituents independently selected from a carbocyclic ring and a 3- to 12-membered heterocyclic ring, any of which is optionally substituted with one or more substituents independently selected from: halogen, C 1~6 alkyl, C 3~6 a carbocyclic ring and a 3- to 6-membered heterocyclic ring, C 1~6 alkyl, C 3~6 the carbocyclic ring and the 3- to 6-membered heterocyclic ring are each independently optionally substituted with one or more substituents selected from halogen, -OR 18A , -N(R 18A ) 2 -NO 2 , -CN, C 1~6 alkyl, C 1~6Optionally substituted with one or more substituents independently selected from haloalkyl, R 18 and R 18A each independently, for each occurrence, is selected from hydrogen, halogen, C 1~6 alkyl, and C 1~6 haloalkyl. In some embodiments, C is selected from
[0100]
Chemical formula
[0101] In some embodiments, for the compound or salt of formula (I), C is selected from 8- to 12-membered bicyclic heterocycles optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 , -SR 18 , -N(R 18 ) 2 , -C(O)R 18 , -C(O)OR 18 , -OC(O)R 18 , -OC(O)N(R 18 ) 2 , -C(O)N(R 18 ) 2 , -N(R 18 )C(O)R 18 , =O, -NO 2 , and -CN, C 1~6 alkyl which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 , -SR 18 , -N(R 18 ) 2 , -C(O)R 18 , -C(O)OR 18 , -OC(O)R 18 , -OC(O)N(R 18 ) 2 , -C(O)N(R 18 ) 2 , -N(R 18 )C(O)R18 、 -NO 2 、 and -CN, and C 3~12 a carbocyclic ring and a 3- to 12-membered heterocyclic ring, each of which is halogen, -OR 18A 、 -SR 18A 、 -N(R 18A ) 2 、 -C(O)R 18A 、 -C(O)OR 18A 、 -OC(O)R 18A 、 -OC(O)N(R 18A ) 2 、 -C(O)N(R 18A ) 2 、 -N(R 18A )C(O)R 18A 、 -NO 2 、 -CN, C 1~6 alkyl, C 3~6 a carbocyclic ring and a 3- to 6-membered heterocyclic ring are each optionally substituted with one or more substituents independently selected from 1~6 alkyl, C 3~6 a carbocyclic ring and a 3- to 6-membered heterocyclic ring are each halogen, -OR 18A 、 -SR 18A 、 -N(R 18A ) 2 、 -C(O)R 18A 、 -C(O)OR 18A 、 -OC(O)R 18A 、 -OC(O)N(R 18A ) 2 、 -C(O)N(R 18A ) 2 、 -N(R 18A )C(O)R 18A 、 -NO 2 、 -CN, C 1~6 alkyl, C 1~6 haloalkyl, C 3~6 a carbocyclic ring, -C 3~6 a carbocyclic ring-(C 1~6 haloalkyl), and a 3- to 6-membered heterocyclic ring are each optionally substituted with one or more substituents independently selected from, and C 3~6 a carbocyclic ring and a 3- to 6-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 , -SR 18 , -N(R 18 ) 2 , -C(O)R 18 , -NO 2 , and -CN, and, C 1~6 alkyl, which is optionally substituted with one or more substituents independently selected from halogen, -OR 18A , -SR 18A , -N(R 18A ) 2 , -C(O)R 18A , -C(O)OR 18A , -OC(O)R 18A , -OC(O)N(R 18A ) 2 , -C(O)N(R 18A ) 2 , -N(R 18A )C(O)R 18A , -NO 2 , -CN, C 3~6 carbocyclic ring and 3- to 6-membered heterocyclic ring are each optionally substituted with one or more substituents independently selected from halogen, -OR 3~6 , -SR 18A , -SR 18A , -N(R 18A ) 2 , -C(O)R 18A , -C(O)OR 18A , -OC(O)R 18A , -OC(O)N(R 18A ) 2 , -C(O)N(R 18A ) 2 , -N(R 18A )C(O)R 18A , -NO 2 , -CN and is optionally substituted with one or more substituents independently selected therefrom.
[0102] In some embodiments, for the compound or salt of formula (I), C is an 8- to 12-membered bicyclic heterocyclic ring optionally substituted with one or more substituents independently selected from: halogen, -OR 18 , -SR 18 , -N(R 18 )2 , -C(O)R 18 , -C(O)OR 18 , -OC(O)R 18 , -OC(O)N(R 18 ) 2 , -C(O)N(R 18 ) 2 , -N(R 18 )C(O)R 18 , -NO 2 , and -CN, and, C 1~6 alkyl which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 , -SR 18 , -N(R 18 ) 2 , -C(O)R 18 , -C(O)OR 18 , -OC(O)R 18 , -OC(O)N(R 18 ) 2 , -C(O)N(R 18 ) 2 , -N(R 18 )C(O)R 18 , =O, -NO 2 , and -CN, and, C 3~12 a carbocyclic ring and a 3- to 12-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from halogen, -OR 18A , -SR 18A , -N(R 18A ) 2 , -C(O)R 18A , -C(O)OR 18A , -OC(O)R 18A , -OC(O)N(R 18A ) 2 , -C(O)N(R 18A ) 2 , -N(R 18A )C(O)R 18A , -NO 2 , -CN, C 1~6 alkyl, C 3~6 optionally substituted with one or more substituents independently selected from a carbocyclic ring and a 3- to 6-membered heterocyclic ring, C 1~6 alkyl, C 3~6The carbon ring and 3- to 6-membered heterocyclic ring are each independently selected from halogen, -OR 18A , -SR 18A , -N(R 18A ), 2 , -C(O)R 18A , -C(O)OR 18A , -OC(O)R 18A , -OC(O)N(R 18A ), 2 , -C(O)N(R 18A ), 2 , -N(R 18A )(C(O)R 18A , -NO 2 , -CN, C 1~6 alkyl, C 1~6 haloalkyl, C 3~6 carbon ring, -C 3~6 carbon ring-(C 1~6 haloalkyl), and are optionally substituted with one or more substituents independently selected from 3- to 6-membered heterocyclic rings.
[0103] In some embodiments, for the compound or salt of formula (I), C is an 8- to 12-membered bicyclic heterocyclic ring optionally substituted with one or more substituents independently selected from:[[]] halogen, -OR 18 , -SR 18 , -N(R 18 ), 2 , -C(O)R 18 , -C(O)OR 18 , -OC(O)R 18 , -OC(O)N(R 18 ), 2 , -C(O)N(R 18 ), 2 , -N(R 18 )(C(O)R 18 , =O, -NO 2 , and -CN, and C 1~6 alkyl which is optionally substituted with one or more substituents independently selected from:[[]] halogen, -OR 18 , -SR 18 , -N(R 18 ), 2 , -C(O)R18 、 -C(O)OR 18 、 -OC(O)R 18 、 -OC(O)N(R 18 ) 2 、 -C(O)N(R 18 ) 2 、 -N(R 18 )C(O)R 18 、 -NO 2 、 and -CN, and 3 - to 8 - membered monocyclic heteroalkyl, which is optionally substituted with one or more substituents independently selected from halogen, -OR 18A 、 -SR 18A 、 -N(R 18A ) 2 、 -C(O)R 18A 、 -C(O)OR 18A 、 -OC(O)R 18A 、 -OC(O)N(R 18A ) 2 、 -C(O)N(R 18A ) 2 、 -N(R 18A )C(O)R 18A 、 -NO 2 、 -CN, C 1~6 alkyl, C 3~6 carbocyclic ring and 3 - to 6 - membered heterocyclic ring are each optionally substituted with one or more substituents independently selected from halogen, -OR 1~6 alkyl, C 3~6 carbocyclic ring and 3 - to 6 - membered heterocyclic ring are each independently halogen, -OR 18A 、 -SR 18A 、 -N(R 18A ) 2 、 -C(O)R 18A 、 -C(O)OR 18A 、 -OC(O)R 18A 、 -OC(O)N(R 18A ) 2 、 -C(O)N(R 18A ) 2 、 -N(R 18A )C(O)R 18A 、 -NO 2 、 -CN, C 1~6 alkyl, C 1~6 haloalkyl, C 3~6 carbocyclic ring, -C 3~6 carbocyclic ring-(C 1~6(haloalkyl), and one or more substituents independently selected from 3- to 6-membered heterocyclic rings, which may be optionally substituted.
[0104] In some embodiments, for the compound or salt of formula (I), C is an 8- to 12-membered bicyclic heterocyclic ring optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 , -N(R 18 ) 2 , -C(O)R 18 , =O, -NO 2 , and -CN, and C 1~6 alkyl which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 , -N(R 18 ) 2 , -C(O)R 18 , -NO 2 , and -CN, and 3- to 8-membered monocyclic heterocycloalkyl which is optionally substituted with halogen, -OR 18A , -N(R 18A ) 2 , -C(O)R 18A , -NO 2 , -CN, C 1~6 alkyl, C 3~6 carbocyclic ring and one or more substituents independently selected from 3- to 6-membered heterocyclic rings, which may be optionally substituted.
[0105] In some embodiments, for the compound or salt of formula (I), C is an 8- to 12-membered bicyclic heterocyclic ring optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 , -N(R 18 ) 2 , -C(O)R 18 , =O, -NO 2 , and -CN, and C 1~6 alkyl which is halogen, C 1~6 alkyl, C 3~6One or more substituents independently selected from 3- to 8-membered monocyclic heterocycloalkyls, optionally substituted with one or more substituents independently selected from carbon rings and 3- to 6-membered heterocyclic rings. In some embodiments, C is
[0106]
Chemical formula
[0107] In some embodiments, for the compound or salt of formula (I), C is an 8- to 12-membered bicyclic heterocyclic ring optionally substituted with one or more substituents independently selected from the following: Halogen, -OR 18 -SR 18 -N(R 18 ) 2 -C(O)R 18 -C(O)OR 18 -OC(O)R 18 -OC(O)N(R 18 ) 2 -C(O)N(R 18 ) 2 -N(R 18 )C(O)R 18 =O, -NO 2 and -CN, and C 1~6 alkyl, optionally substituted with one or more substituents independently selected from the following: Halogen, -OR 18 -SR 18 -N(R 18 ) 2 -C(O)R 18 -C(O)OR 18 -OC(O)R 18 -OC(O)N(R 18 ) 2 -C(O)N(R 18 ) 2 -N(R 18 )C(O)R 18 -NO 2 and -CN, and A 3- to 12-membered bicyclic heterocyclic ring, which is optionally substituted with one or more substituents independently selected from halogen, -OR 18A , -SR 18A , -N(R 18A ) 2 , -C(O)R 18A , -C(O)OR 18A , -OC(O)R 18A , -OC(O)N(R 18A ) 2 , -C(O)N(R 18A ) 2 , -N(R 18A )C(O)R 18A , -NO 2 , -CN, C 1~6 alkyl, C 3~6 is optionally substituted with one or more substituents independently selected from a carbocyclic ring and a 3- to 6-membered heterocyclic ring, C 1~6 alkyl, C 3~6 the carbocyclic ring and the 3- to 6-membered heterocyclic ring are each optionally substituted with one or more substituents independently selected from halogen, -OR 18A , -SR 18A , -N(R 18A ) 2 , -C(O)R 18A , -C(O)OR 18A , -OC(O)R 18A , -OC(O)N(R 18A ) 2 , -C(O)N(R 18A ) 2 , -N(R 18A )C(O)R 18A , -NO 2 , -CN, C 1~6 alkyl, C 1~6 haloalkyl, C 3~6 a carbocyclic ring, -C 3~6 a carbocyclic ring-(C 1~6 haloalkyl), and is optionally substituted with one or more substituents independently selected from a 3- to 6-membered heterocyclic ring.
[0108] In some embodiments, for the compound or salt of formula (I), C is an 8- to 12-membered bicyclic heterocyclic ring optionally substituted with one or more substituents independently selected from: halogen, -OR 18 , -SR 18 , -N(R18 ) 2 、 -C(O)R 18 、 -C(O)OR 18 、 -OC(O)R 18 、 -OC(O)N(R 18 ) 2 、 -C(O)N(R 18 ) 2 、 -N(R 18 )C(O)R 18 、 =O、 -NO 2 、 and -CN, and, C 1~6 alkyl which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 、 -SR 18 、 -N(R 18 ) 2 、 -C(O)R 18 、 -C(O)OR 18 、 -OC(O)R 18 、 -OC(O)N(R 18 ) 2 、 -C(O)N(R 18 ) 2 、 -N(R 18 )C(O)R 18 、 -NO 2 、 and -CN, and, a 6 - 12 - membered spirocyclic heterocyclic ring which is optionally substituted with one or more substituents independently selected from halogen, -OR 18A 、 -SR 18A 、 -N(R 18A ) 2 、 -C(O)R 18A 、 -C(O)OR 18A 、 -OC(O)R 18A 、 -OC(O)N(R 18A ) 2 、 -C(O)N(R 18A ) 2 、 -N(R 18A )C(O)R 18A 、 -NO 2 、 -CN, C 1~6 alkyl, C 3~6 is optionally substituted with one or more substituents independently selected from carbocyclic rings and 3 - 6 - membered heterocyclic rings, C 1~6 alkyl, C 3~6The carbon ring and 3- to 6-membered heterocyclic rings are each independently selected from halogen, -OR 18A , -SR 18A , -N(R 18A ), 2 , -C(O)R 18A , -C(O)OR 18A , -OC(O)R 18A , -OC(O)N(R 18A ), 2 , -C(O)N(R 18A ), 2 , -N(R 18A )(C(O)R 18A , -NO 2 , -CN, C 1~6 alkyl, C 1~6 haloalkyl, C 3~6 carbon ring, -C 3~6 carbon ring-(C 1~6 haloalkyl), and are optionally substituted with one or more substituents independently selected from 3- to 6-membered heterocyclic rings.
[0109] In some embodiments, for the compound or salt of formula (I), C is an 8- to 12-membered bicyclic heterocyclic ring optionally substituted with one or more substituents independently selected from: halogen, -OR 18 , -N(R 18 ), 2 , -C(O)R 18 , =O, -NO 2 , and -CN, and C 1~6 alkyl which is optionally substituted with one or more substituents independently selected from: halogen, -OR 18 , -N(R 18 ), 2 , -C(O)R 18 , -NO 2 , and -CN, and a 6- to 12-membered spirocyclic heterocyclic ring which is halogen, -OR 18A , -N(R 18A ), 2 , -C(O)R 18A , -NO 2 , -CN, C 1~6 alkyl, C3~6 Optionally substituted with one or more substituents independently selected from a carbon ring and a 3- to 6-membered heterocyclic ring.
[0110] In some embodiments, for the compound or salt of formula (I), C is an 8- to 12-membered bicyclic heterocyclic ring, optionally substituted with one or more substituents independently selected from: C 1~6 alkyl, halogen, -OR 18A , -N(R 18A ) 2 , -C(O)R 18A , -NO 2 , -CN, C 1~6 alkyl, C 3~6 Optionally substituted with one or more substituents independently selected from a carbon ring and a 3- to 6-membered heterocyclic ring, and optionally substituted with one or more substituents independently selected from a 6- to 12-membered spirocyclic heterocyclic ring. In some embodiments, C is
[0111]
Chemical formula
[0112] In some embodiments, for the compound or salt of formula (I), C is an 8- to 12-membered bicyclic heterocyclic ring, optionally substituted with one or more substituents independently selected from: halogen, -OR 18 , -SR 18 , -N(R 18 ) 2 , -C(O)R 18 , -C(O)OR 18 , -OC(O)R 18 , -OC(O)N(R 18 ) 2 , -C(O)N(R 18 ) 2 , -N(R 18 )C(O)R 18 , =O, -NO 2 , and -CN, and C 1~6An alkyl optionally substituted with one or more substituents independently selected from the following: Halogen, -OR 18 , -SR 18 , -N(R 18 ) 2 , -C(O)R 18 , -C(O)OR 18 , -OC(O)R 18 , -OC(O)N(R 18 ) 2 , -C(O)N(R 18 ) 2 , -N(R 18 )C(O)R 18 , -NO 2 , and -CN, and A 6- to 12-membered bridged heterocyclic ring optionally substituted with one or more substituents independently selected from halogen, -OR 18A , -SR 18A , -N(R 18A ) 2 , -C(O)R 18A , -C(O)OR 18A , -OC(O)R 18A , -OC(O)N(R 18A ) 2 , -C(O)N(R 18A ) 2 , -N(R 18A )C(O)R 18A , -NO 2 , -CN, C 1~6 alkyl, C 3~6 optionally substituted with one or more substituents independently selected from carbocyclic ring and 3- to 6-membered heterocyclic ring, and C 1~6 alkyl, C 3~6 carbocyclic ring and 3- to 6-membered heterocyclic ring are each optionally substituted with one or more substituents independently selected from halogen, -OR 18A , -SR 18A , -N(R 18A ) 2 , -C(O)R 18A , -C(O)OR 18A , -OC(O)R 18A , -OC(O)N(R 18A ) 2 , -C(O)N(R 18A ) 2 , -N(R 18A )C(O)R 18A , -NO2 、 -CN, C 1~6 alkyl, C 1~6 haloalkyl, C 3~6 carbocyclic, -C 3~6 carbocyclic-(C 1~6 haloalkyl), and optionally substituted with one or more substituents independently selected from 3- to 6-membered heterocycles.
[0113] In some embodiments, for the compound or salt of formula (I), C is an 8- to 12-membered bicyclic heterocycle optionally substituted with one or more substituents independently selected from: halogen, -OR 18 , -N(R 18 ) 2 , -C(O)R 18 , =O, -NO 2 , and -CN, and C 1~6 alkyl which is optionally substituted with one or more substituents independently selected from: halogen, -OR 18 , -N(R 18 ) 2 , -C(O)R 18 , -NO 2 , and -CN, and a 6- to 12-membered bridged heterocycle which is optionally substituted with one or more substituents independently selected from halogen, -OR 18A , -N(R 18A ) 2 , -C(O)R 18A , -NO 2 , -CN, C 1~6 alkyl, C 3~6 carbocyclic and optionally substituted with one or more substituents independently selected from 3- to 6-membered heterocycles.
[0114] In some embodiments, for the compound or salt of formula (I), C is an 8- to 12-membered bicyclic heterocycle optionally substituted with one or more substituents independently selected from: C 1~6 alkyl which is halogen, -OR 18A , -N(R 18A ) 2 , -C(O)R 18A, -NO 2 , -CN, C 1~6 Alkyl, C 3~6 Optionally substituted with one or more substituents independently selected from carbocyclic rings and 3- to 6-membered heterocyclic rings, and optionally substituted with one or more substituents independently selected from 6- to 12-membered bridged heterocyclic rings. In some embodiments, C is
[0115]
Chem.
[0116] In one aspect, provided herein is a compound having the structure of formula (I-a), or a pharmaceutically acceptable salt or solvate thereof,
[0117]
Chem.
[0118]
Chem.
[0119]
Math.
[0120] In one aspect, provided herein is a compound having the structure of formula (II), or a pharmaceutically acceptable salt or solvate thereof,
[0121]
Chemical formula
[0122] In one aspect, provided herein is a compound having the structure of formula (III), or a pharmaceutically acceptable salt or solvate thereof,
[0123] [Chemical formula] or a pharmaceutically acceptable salt thereof, wherein X 4 is selected from N and C(R 2 ),
[0124]
Number
[0125] In some embodiments, for the compounds or salts of formula (I), (I-a), (II) or (III), m is 0, 1, 2, and 3. In some embodiments, m is 0, 1, or 2. In some embodiments, m is 0, or 1. In some embodiments, m is 1, 2, or 3. In some embodiments, m is 1, or 2. In some embodiments, m is 0. In some embodiments, m is 1. In some embodiments, m is 2. In some embodiments, m is 3.
[0126] In some embodiments, for the compounds or salts of formula (I), (I-a), (II) or (III), n is 0, 1, or 2. In some embodiments, n is 0 or 1. In some embodiments, n is 1 or 2. In some embodiments, n is 0. In some embodiments, n is 1. In some embodiments, n is 2.
[0127] In some embodiments, for the compounds or salts of formula (I), (I-a), (II) or (III), p is 0, 1, 2, 3, and 4. In some embodiments, p is 0, 1, 2, or 3. In some embodiments, p is 0, 1, or 2. In some embodiments, p is 0, or 1. In some embodiments, p is 1, 2, or 3. In some embodiments, p is 1 or 2. In some embodiments, p is 2 or 3. In some embodiments, p is 0. In some embodiments, p is 1. In some embodiments, p is 2. In some embodiments, p is 3. In some embodiments, p is 4. In some embodiments, p is 5.
[0128] In some embodiments, for the compound or salt of formula (I), A is,
[0129]
Chem.
[0130]
Chem.
[0131]
Chem.
[0132]
Chem.
[0133]
Chem.
[0134]
Chem.
[0135] In some embodiments, for the compound or salt of formula (I), A is,
[0136]
Chem.
[0137] [Chemical formula] and n is 0 or 1. In some embodiments, A is
[0138] [Chemical formula] and n is 0. In some embodiments, A is
[0139] [Chemical formula] and n is 1. In some embodiments, A is
[0140] [Chemical formula] and n is 0 or 1. In some embodiments, A is
[0141] [Chemical formula] and n is 0. In some embodiments, A is
[0142] [Chemical formula] and n is 1.
[0143] In some embodiments, for the compound or salt of formula (I) or (II), X 1 , X 2 , and X 3 are each independently selected from N and C(R 2 ), and X 1 , X 2 , and X3 At least one of them is C(R 2 ). In some embodiments, X 1 is N, and X 2 and X 3 are each independently selected from N and C(R 2 ), and at least one of X 2 and X 3 is C(R 2 ). In some embodiments, X 2 is N, and X 1 and X 3 are each independently selected from N and C(R 2 ), and at least one of X 1 and X 3 is C(R 2 ). In some embodiments, X 3 is N, and X 2 and X 3 are each independently selected from N and C(R 2 ), and at least one of X 2 and X 3 is C(R 2 ). In some embodiments, X 1 is C(R 2 ), and X 2 and X 3 are each independently selected from N and C(R 2 ). In some embodiments, X 2 is C(R 2 ), and X 1 and X 3 are each independently selected from N and C(R 2 ). In some embodiments, X 3 is C(R 2 ), and X 2 and X 3 are each independently selected from N and C(R 2 ).
[0144] In some embodiments, for the compound or salt of formula (I) or (III), X 4 is N and C(R 2) is selected from. In some embodiments, X 4 is C(R 2 ). In some embodiments, X 4 is N. In some embodiments,
[0145]
Number
[0146] In some embodiments, for the compound or salt of formula (I), (I-a), (II) or (III), each R 1 is independently selected from: halogen, -OR 11 , -SR 11 , -N(R 11 ) 2 , -C(O)R 11 , -C(O)OR 11 , -OC(O)R 11 , -OC(O)N(R 11 ) 2 , -C(O)N(R 11 ) 2 , -N(R 11 )C(O)R 11 , -N(R 11 )C(O)OR 11 , -N(R11 )C(O)N(R 11 ) 2 , -N(R 11 )C(S)N(R 11 ) 2 , -N(R 11 )S(O) 2 (R 11 ), -S(O)R 11 , -S(O) 2 R 11 , -S(O) 2 N(R 11 ) 2 , -NO 2 , and -CN, C 1~6 Alkyl, C 2~6 Alkenyl, and C 2~6 alkynyl, each of which is halogen, -OR 11 , -SR 11 , -N(R 11 ) 2 , optionally substituted by one or more substituents independently selected from: =O, =S, and -CN; and C 3~6 Carbocyclic rings and 3- to 6-membered heterocyclic rings, each of which is independently selected from halogen, C 1~4 Alkyl, C 1~4 Haloalkyl, -OR 11 , -SR 11 , -N(R 11 ) 2 Optionally substituted with one or more substituents independently selected from: =O, =S, and -CN.
[0147] In some embodiments, for a compound or salt of Formula (I), (Ia), (II), or (III), each R 1 is independently selected from: Halogen, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, -OR 11 , -SR 11 , -N(R 11 ) 2 , -C(O)R 11 , -C(O)OR11 、 -OC(O)R 11 、 -OC(O)N(R 11 ) 2 、 -C(O)N(R 11 ) 2 、 -N(R 11 )C(O)R 11 、 -NO 2、 and -CN, and, C 3~6 a carbocyclic ring and a 3- to 6-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from halogen, C 1~4 alkyl, C 1~4 haloalkyl, -OR 11 、 -SR 11 、 -N(R 11 ) 2 、 =O, =S, and -CN.
[0148] In some embodiments, for the compounds or salts of formula (I), (I-a), (II) or (III), each R 1 is independently halogen, C 1~6 alkyl, C 2~6 alkenyl, C 2~6 alkynyl, C 1~6 haloalkyl, -OR 11 、 -SR 11 、 -N(R 11 ) 2 、 -C(O)R 11 、 -C(O)OR 11 、 -OC(O)R 11 、 -OC(O)N(R 11 ) 2 、 -C(O)N(R 11 ) 2 、 -N(R 11 )C(O)R 11 、 -NO 2、 and -CN. In some embodiments, each R 1 is independently halogen, C 1~6 alkyl, C 2~6 alkenyl, C 2~6 alkynyl, C 1~6 haloalkyl, -OR 11 、 -N(R 11 ) 2, -C(O)R 11 , -C(O)OR 11 , -OC(O)R 11 , -C(O)N(R 11 ) 2 , -N(R 11 )C(O)R 11 , -NO 2、 and -CN. In some embodiments, each R 1 is independently selected from halogen, C 1~6 alkyl, C 2~6 alkenyl, C 2~6 alkynyl, C 1~6 haloalkyl, -OR 11 , -N(R 11 ) 2 , -NO 2、 and -CN. In some embodiments, each R 1 is independently selected from halogen, C 1~6 alkyl, C 2~6 alkenyl, C 2~6 alkynyl, C 1~6 haloalkyl, -OR 11 , and -CN. In some embodiments, each R 1 is independently selected from halogen, C 1~6 alkyl, and C 1~6 haloalkyl. In some embodiments, each R 1 is independently selected from halogen and C 1~6 alkyl. In some embodiments, each R 1 is independently selected from halogen. In some embodiments, each R 1 is independently selected from C 1~6 alkyl.
[0149] In some embodiments, for the compounds or salts of formula (I), (I-a), (II) or (III), each R 1 is independently selected from C 3~6 carbocyclic ring and 3- to 6-membered heterocyclic ring, each of which is halogen, C 1~4 alkyl, C 1~4 haloalkyl, -OR 11 , -SR 11 , -N(R11 ) 2 optionally substituted with one or more substituents independently selected from =O, =S, and -CN. In one aspect, provided herein are compounds having the structure of formula (I), (I-a), (II), or (III), or a pharmaceutically acceptable salt or solvate thereof, wherein each R 1 is independently selected from C 3~6 carbocyclic rings and 3- to 6-membered heterocyclic rings, each of which is optionally substituted with one or more substituents independently selected from halogen, C 1~4 alkyl, C 1~4 haloalkyl, -OR 11 , -N(R 11 ) 2 , =O, and -CN. In some embodiments, each R 1 is independently selected from C 3~4 carbocyclic rings and 3- to 4-membered heterocyclic rings, each of which is optionally substituted with one or more substituents independently selected from halogen, C 1~4 alkyl, C 1~4 haloalkyl, -OR 11 , -SR 11 , -N(R 11 ) 2 , =O, =S, and -CN. In some embodiments, each R 1 is independently selected from C 3~4 carbocyclic rings and 3- to 4-membered heterocyclic rings, each of which is optionally substituted with one or more substituents independently selected from halogen, C 1~4 alkyl, C 1~4 haloalkyl, -OR 11 , -SR 11 , -N(R 11 ) 2 , =O, =S, and -CN. In some embodiments, each R 1 is independently selected from C 3~4 carbocyclic rings and 3- to 4-membered heterocyclic rings, each of which is optionally substituted with one or more substituents independently selected from halogen, C 1~4 alkyl, C 1~4 haloalkyl, -OR 11 , -N(R 11 ) 2is optionally substituted with one or more substituents independently selected from =O, and -CN. In some embodiments, each R 1 is independently selected from C 3~4 carbocyclic rings and 3- to 4-membered heterocyclic rings, each of which is optionally substituted with one or more substituents independently selected from halogen, C 1~4 alkyl, and C 1~4 haloalkyl. In some embodiments, each R 1 is independently selected from C 3~4 carbocyclic rings and 3- to 4-membered heterocyclic rings, each of which is optionally substituted with one or more substituents independently selected from halogen and C 1~4 alkyl.
[0150] In some embodiments, for the compounds or salts of formula (I), (I-a), (II) or (III), each R 2 is independently selected from: hydrogen, halogen, -OR 12 , -SR 12 , -N(R 12 ) 2 , -C(O)R 12 , -C(O)OR 12 , -OC(O)R 12 , -OC(O)N(R 12 ) 2 , -C(O)N(R 12 ) 2 , -N(R 12 )C(O)R 12 , -N(R 12 )C(O)OR 12 , -N(R 12 )C(O)N(R 12 ) 2 , -N(R 12 )C(S)N(R 12 ) 2 , -N(R 12 )S(O) 2 (R 12 ), -S(O)R 12 , -S(O) 2 R 12 , -S(O) 2 N(R12 ) 2 、 -NO 2、 and -CN, C 1~6 alkyl, C 2~6 alkenyl, and C 2~6 alkynyl, each of which is optionally substituted by one or more substituents independently selected from halogen, -OR 12 , -SR 12 , -N(R 12 ) 2 , =O, =S, and -CN, and C 3~6 carbocyclic ring and 3- to 6-membered heterocyclic ring, each of which is optionally substituted by one or more substituents independently selected from halogen, C 1~4 alkyl, C 1~4 haloalkyl, -OR 12 , -SR 12 , -N(R 12 ) 2 , =O, =S, and -CN.
[0151] In some embodiments, for the compounds or salts of formula (I), (I-a), (II) or (III), each R 2 is independently hydrogen, halogen, C 1~6 alkyl, C 2~6 alkenyl, C 2~6 alkynyl, C 1~6 haloalkyl, -OR 12 , -SR 12 , -N(R 12 ) 2 , -C(O)R 12 , -C(O)OR 12 , -OC(O)R 12 , -OC(O)N(R 12 ) 2 , -C(O)N(R 12 ) 2 , -N(R 12 )C(O)R 12 , -NO 2、 and -CN. In some embodiments, each R 2 is independently halogen, C 1~6 alkyl, C 2~6Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, -OR 12 , -N(R 12 ) 2 , -C(O)R 12 , -C(O)OR 12 , -OC(O)R 12 , -C(O)N(R 12 ) 2 , -N(R 12 )C(O)R 12 , -NO 2、 and -CN. In some embodiments, each R 2 is independently selected from halogen, C 1~6 alkyl, C 2~6 alkenyl, C 2~6 alkynyl, C 1~6 haloalkyl, -OR 12 , -N(R 12 ) 2 , -NO 2、 and -CN. In some embodiments, each R 2 is independently selected from halogen, C 1~6 alkyl, C 2~6 alkenyl, C 2~6 alkynyl, C 1~6 haloalkyl, -OR 12 , and -CN. In some embodiments, each R 2 is independently selected from halogen, C 1~6 alkyl, and C 1~6 haloalkyl. In some embodiments, each R 2 is independently selected from halogen and C 1~6 alkyl. In some embodiments, each R 2 is independently selected from halogen. In some embodiments, each R 2 is independently selected from C 1~6 alkyl.
[0152] In some embodiments, for the compounds or salts of formula (I), (I-a), (II) or (III), each R 2 is independently C 3~6Selected from a carbon ring and a 3- to 6-membered heterocyclic ring, each of which is halogen, C 1~4 alkyl, C 1~4 haloalkyl, -OR 12 、-SR 12 、-N(R 12 ) 2 、=O、=S, and -CN, and is optionally substituted with one or more substituents independently selected therefrom. In one aspect, provided herein is a compound having the structure of formula (I), (I-a), (II) or (III), or a pharmaceutically acceptable salt or solvate thereof, wherein each R 2 is independently selected from a carbon ring and a 3- to 6-membered heterocyclic ring, each of which is halogen, C 3~6 alkyl, C 1~4 haloalkyl, -OR 1~4 、-N(R 12 ) 12 、=O, and -CN, and is optionally substituted with one or more substituents independently selected therefrom. In some embodiments, each R 2 is independently selected from a carbon ring and a 3- to 4-membered heterocyclic ring, each of which is halogen, C 2 alkyl, C 3~4 haloalkyl, -OR 1~4 、-SR 1~4 、-N(R 12 ) 12 、=O、=S, and -CN, and is optionally substituted with one or more substituents independently selected therefrom. In some embodiments, each R 12 is independently selected from a carbon ring and a 3- to 4-membered heterocyclic ring, each of which is halogen, C 2 alkyl, C 2 haloalkyl, -OR 3~4 、-SR 1~4 、-N(R 1~4 ) 12 、=O、=S, and -CN, and is optionally substituted with one or more substituents independently selected therefrom. In some embodiments, each R 12 is independently selected from a carbon ring and a 3- to 4-membered heterocyclic ring, each of which is halogen, C 12 ) 2 、=O、=S, and -CN, and is optionally substituted with one or more substituents independently selected therefrom. In some embodiments, each R 2 is independently selected from a carbon ring and a 3- to 4-membered heterocyclic ring, each of which is halogen, C 3~4 alkyl, C 1~4Alkyl, C 1~4 Haloalkyl, -OR 12 , -N(R 12 ) 2 , =O, and -CN, and is optionally substituted with one or more substituents independently selected from. In some embodiments, each R 2 is independently selected from C 3~4 carbocyclic rings and 3- to 4-membered heterocyclic rings, each of which is optionally substituted with one or more substituents independently selected from halogen, C 1~4 alkyl, and C 1~4 haloalkyl. In some embodiments, each R 2 is independently selected from C 3~4 carbocyclic rings and 3- to 4-membered heterocyclic rings, each of which is optionally substituted with one or more substituents independently selected from halogen and C 1~4 alkyl.
[0153] In some embodiments, for the compounds or salts of formula (I), (I-a), (II) or (III), R 3 is independently selected from hydrogen and C 1~6 alkyl. In some embodiments, R 3 is independently selected from hydrogen, methyl, ethyl, propyl and butyl. In some embodiments, R 3 is independently selected from hydrogen, methyl and ethyl. In some embodiments, R 3 is independently selected from hydrogen and methyl. In some embodiments, R 3 is selected from hydrogen. In some embodiments, R 3 is selected from methyl.
[0154] In some embodiments, for the compounds or salts of formula (I), (I-a), (II) or (III), R 4a and R 4b are each independently hydrogen, halogen, -OR 13 , -SR 13 , -N(R 13 ) 2 , -C(O)R 13 , -NO2 , -CN, and C 1~6 selected from alkyl, and C1-C6 alkyl is optionally substituted with one or more substituents independently selected from halogen, -OR 13 , -SR 13 , -N(R 13 ), -C(O)R 2 , -NO 13 , and -CN. In some embodiments, R 2、 and R 4a are each independently hydrogen, halogen, -OR 4b , -SR 13 , -N(R 13 ), -C(O)R 13 ), -NO 2 , -CN, and C 13 alkyl. In some embodiments, R 2 and R 1~6 are each independently hydrogen, halogen, -OR 4a , -N(R 4b ), -NO 13 , -CN, and C 13 alkyl. In some embodiments, R 2 and R 2 are each independently hydrogen, halogen, -OR 1~6 , -N(R 4a ), -NO 4b , -CN, and C 13 alkyl. In some embodiments, R 13 and R 2 are each independently hydrogen, halogen, -CN, and C 1~6 alkyl. In some embodiments, R 4a and R 4b are each independently hydrogen, halogen, and C 1~6 alkyl. In some embodiments, R 4a and R 4b are each independently hydrogen, halogen, and C 1~6 alkyl. In some embodiments, R 4a and R 4b are each independently hydrogen, halogen, C 1~3 alkyl, and C 1~3 haloalkyl. In some embodiments, R4a and R 4b are each independently selected from hydrogen and halogen. In some embodiments, R 4a and R 4b are each hydrogen.
[0155] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), R 5 is independently selected from hydrogen and C 1~6 alkyl. In some embodiments, R 5 is independently selected from hydrogen, methyl, and ethyl. In some embodiments, R 5 is hydrogen. In some embodiments, R 5 is methyl.
[0156] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), Z is a bond, -C(O)-, -C(R 15 ) 2 -, -C(O)C(R 15 ) 2 -, -C(O)[C(R 15 ) 2 q S-, -C(=N-CN)-, -C(O)O-, -C(O)N(R 16 )-, -C(S)-, -C(S)N(R 16 )-, -S(O)-, and -S(O) 2 -. In some embodiments, Z is a bond, -C(O)-, -C(R 15 ) 2 -, -C(O)C(R 15 ) 2 -, -C(O)[C(R 15 ) 2 q S-, -C(=N-CN)-, -C(O)O-, -C(O)N(R 16 )-, -C(S)N(R 16 )-, and -S(O) 2 -. In some embodiments, Z is a bond, -C(O)-, -C(R 15 ) 2 -, -C(O)C(R 15 ) 2 -, -C(O)[C(R 15 ) 2 q S-, -C(=N-CN)-, -C(O)O-, and -S(O) 2 - are selected from. In some embodiments, Z is a bond, -C(O)-, -C(R 15 ) 2 -, -C(O)C(R 15 ) 2 -, -C(O)[C(R 15 ) 2 q S-, and -C(=N-CN)- are selected from. In some embodiments, Z is -C(O)-, -C(R 15 ) 2 -, -C(O)C(R 15 ) 2 -, -C(O)[C(R 15 ) 2 q S-, and -C(=N-CN)- are selected from. In some embodiments, Z is -C(O)-. In some embodiments, Z is -C(R 15 ) 2 -. In some embodiments, Z is -C(O)C(R 15 ) 2 -. In some embodiments, Z is -C(O)[C(R 15 ) 2 q S-. In some embodiments, Z is -C(=N-CN)-.
[0157] In some embodiments, for the compounds or salts of formula (I), (I-a), (II) or (III), q is selected from 1, 2, and 3. In some embodiments, q is selected from 1 and 2. In some embodiments, q is 1. In some embodiments, q is 2.
[0158] In some embodiments, for the compounds or salts of formula (I), (I-a), (II) or (III), R 11 and R 12 is, independently for each occurrence, hydrogen and C 1~6 alkyl, and C1-6 alkyl is optionally substituted with one or more substituents independently selected from halogen, -OH, -NH 2 , -O-C 1~6 alkyl, -O-C 1~6 haloalkyl, =O, and -CN. In some embodiments, R 11 and R 12 are, independently for each occurrence, hydrogen and C 1~6 alkyl, and C1-6 alkyl is optionally substituted with one or more substituents independently selected from halogen, -OH, -NH 2 , =O, and -CN. In some embodiments, R 11 and R 12 are, independently for each occurrence, hydrogen and C 1~6 alkyl, and C1-6 alkyl is optionally substituted with one or more substituents independently selected from halogen, -OH, -NH 2 , and =O. In some embodiments, R 11 and R 12 are, independently for each occurrence, hydrogen and C 1~6 alkyl, and C1-6 alkyl is optionally substituted with one or more substituents independently selected from halogen, -OH, and =O. In some embodiments, R 11 and R 12 are, independently for each occurrence, hydrogen and C 1~6 alkyl, and C1-6 alkyl is optionally substituted with one or more substituents independently selected from halogen and =O. In some embodiments, R 11 and R 12 are, independently for each occurrence, hydrogen, C 1~6 alkyl, and C 1~6 haloalkyl. In some embodiments, R 11 and R 12 are, independently for each occurrence, hydrogen and C 1~6 alkyl. In some embodiments, R 11 and R12 Each occurrence of is independently hydrogen.
[0159] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), R 13 is independently, for each occurrence, hydrogen and C 1~6 alkyl. In some embodiments, R 13 is independently, for each occurrence, hydrogen and C 1~4 alkyl. In some embodiments, each R 13 is hydrogen.
[0160] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), R 14 is selected from hydrogen, C 1~6 alkyl, and C 3~6 carbocyclic ring, and each of C 1~6 alkyl and C 3~6 carbocyclic ring is optionally substituted with one or more substituents independently selected from halogen, -OH, -NH 2 , -O-C 1~6 alkyl, -O-C 1~6 haloalkyl, =O, and -CN. In some embodiments, R 14 is selected from hydrogen, C 1~6 alkyl, and C 3~6 carbocyclic ring, and each of C 1~6 alkyl and C 3~6 carbocyclic ring is optionally substituted with one or more substituents independently selected from halogen, -OH, -NH 2 , -O-C 1~6 alkyl, -O-C 1~6 haloalkyl, =O, and -CN. In some embodiments, R 14 is selected from hydrogen, C 1~6 alkyl, and C 3~6 carbocyclic ring, and each of C 1~6 alkyl and C 3~6 carbocyclic ring is halogen, -OH, -O-C 1~6It is optionally substituted with one or more substituents independently selected from alkyl, ═O, and -CN. In some embodiments, R 14 is hydrogen, C 1~6 alkyl, and C 3~6 selected from carbocycles, each of C 1~6 alkyl and C 3~6 carbocycle is optionally substituted with one or more substituents independently selected from halogen, -OH, -O-C 1~6 alkyl, and ═O. In some embodiments, R 14 is selected from hydrogen and C 1~6 alkyl, and is optionally substituted with one or more substituents independently selected from halogen, -OH, -O-C 1~6 alkyl, and ═O. In some embodiments, R 14 is hydrogen, C 1~6 alkyl, and C 1~6 selected from haloalkyl. In some embodiments, R 14 is selected from hydrogen.
[0161] In some embodiments, for the compound or salt of formula (I), (I-a), (II) or (III), R 14a and R 14b are each independently selected from hydrogen, C 1~6 alkyl, and C 3~6 selected from carbocycles, each of C 1~6 alkyl and C 3~6 carbocycle is optionally substituted with one or more substituents independently selected from halogen, -OH, -NH 2 , -O-C 1~6 alkyl, -O-C 1~6 haloalkyl, ═O, and -CN, or R 14a and R 14b together form a C 3~6 carbocycle or a 3- to 6-membered heterocycle, each of which is halogen, -OH, C 1~6 alkyl, -C 1~6 haloalkyl, -O-C 1~6 alkyl, -O-C 1~6Optionally substituted with one or more substituents independently selected from haloalkyl, =O, and -CN. In some embodiments, R 14a and R 14b are each independently selected from hydrogen, C 1~6 alkyl, and C 3~6 carbocyclic ring, and each of C 1~6 alkyl and C 3~6 carbocyclic ring is optionally substituted with one or more substituents independently selected from halogen, -OH, -O-C 1~6 alkyl, =O, and -CN, or R 14a and R 14b together form a C 3~6 carbocyclic ring or a 3- to 6-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from halogen, -OH, C 1~6 alkyl, -C 1~6 haloalkyl, -O-C 1~6 alkyl, -O-C 1~6 haloalkyl, =O, and -CN. In some embodiments, R 14a and R 14b are each independently selected from hydrogen, C 1~6 alkyl, and C 3~6 carbocyclic ring, and each of C 1~6 alkyl and C 3~6 carbocyclic ring is optionally substituted with one or more substituents independently selected from halogen, -OH, and =O, or R 14a and R 14b together form a C 3~6 carbocyclic ring or a 3- to 6-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from halogen, -OH, C 1~6 alkyl, -C 1~6 haloalkyl, and =O.
[0162] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), R 14a and R 14b are each independently selected from: hydrogen and C 1~6An alkyl, wherein the C1-C6 alkyl is optionally substituted with one or more substituents independently selected from halogen, -OH, -NH 2 , -O-C 1~6 alkyl, -O-C 1~6 haloalkyl, =O, and -CN, or R 14a and R 14b together form a C 3~6 carbocyclic ring or a 3- to 6-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from halogen, -OH, -NH 2 , C 1~6 alkyl, -C 1~6 haloalkyl, -O-C 1~6 alkyl, -O-C 1~6 haloalkyl, =O, and -CN.
[0163] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), R 14a and R 14b are each independently selected from: hydrogen and C 1~6 alkyl, wherein the C1-C6 alkyl is optionally substituted with one or more substituents independently selected from halogen, -OH, -NH 2 , -O-C 1~6 alkyl, -O-C 1~6 haloalkyl, =O, and -CN, or R 14a and R 14b together form a C 3~6 carbocyclic ring or a 3- to 6-membered heterocyclic ring.
[0164] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), R 14a and R 14b are each independently selected from hydrogen and C 1~6 alkyl, and the C1-C6 alkyl is halogen, -OH, -NH 2 , -O-C 1~6Alkyl, -O-C 1~6 is optionally substituted with one or more substituents independently selected from haloalkyl, =O, and -CN. In some embodiments, R 14a and R 14b are each independently selected from hydrogen and C 1~6 alkyl, and C1-6 alkyl is optionally substituted with one or more substituents independently selected from halogen, -OH, -O-C 1~6 alkyl, -O-C 1~6 haloalkyl, and =O. In some embodiments, R 14a and R 14b are each independently selected from hydrogen and C 1~6 alkyl, and C1-6 alkyl is optionally substituted with one or more substituents independently selected from halogen and =O. In some embodiments, R 14a and R 14b are each independently selected from hydrogen and C 1~6 alkyl. In some embodiments, R 14a and R 14b are each independently hydrogen.
[0165] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), R 15 is independently, at each occurrence, selected from hydrogen, halogen, =O, -CN, C 1~6 alkyl, C 1~6 haloalkyl, C 3~6 carbocycle, and 3- to 6-membered heterocycle, or two R 15 together form a C 3~6 carbocycle. In some embodiments, R 15 is independently, at each occurrence, selected from hydrogen, halogen, =O, -CN, C 1~6 alkyl, C 1~6 haloalkyl, C 3~6 carbocycle, and 3- to 6-membered heterocycle. In some embodiments, R 15 is independently, at each occurrence, selected from hydrogen, halogen, =O, -CN, C 1~6 alkyl, C 1~6Haloalkyl, C 3~6 is selected from a carbocyclic ring, and a 3- to 6-membered heterocyclic ring. In some embodiments, R 15 is, independently for each occurrence, hydrogen, halogen, =O, -CN, C 1~6 alkyl, C 1~6 haloalkyl, and a 3- to 6-membered heterocyclic ring. In some embodiments, R 15 is, independently for each occurrence, hydrogen, halogen, =O, C 1~6 alkyl, C 1~6 haloalkyl, and a 3- to 6-membered heterocyclic ring. In some embodiments, R 15 is, independently for each occurrence, hydrogen, halogen, C 1~6 alkyl, C 1~6 haloalkyl, and a 3- to 6-membered heterocyclic ring. In some embodiments, R 15 is, independently for each occurrence, hydrogen, halogen, C 1~6 alkyl, and a 3- to 6-membered heterocyclic ring. In some embodiments, R 15 is, independently for each occurrence, hydrogen, halogen, and C 1~6 alkyl. In some embodiments, R 15 is, independently for each occurrence, hydrogen, and C 1~6 alkyl. In some embodiments, R 15 is, independently for each occurrence, hydrogen, and halogen. In some embodiments, each R 15 is hydrogen.
[0166] In some embodiments, for the compound or salt of formula (I), (I-a), (II) or (III), R 16 is, for each occurrence, selected from hydrogen and C 1~6 alkyl. In some embodiments, R 16 is, for each occurrence, selected from hydrogen and C 1~4 alkyl. In some embodiments, R 16 is, for each occurrence, selected from hydrogen and C 1~4 alkyl. In some embodiments, each R 16 is hydrogen.
[0167] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), B is C 3~10 selected from carbocycles and 3- to 10-membered heterocycles, each of which is optionally substituted with one or more substituents independently selected from: halogen, -OR 17 -SR 17 -N(R 17 ) 2 -C(O)R 17 -C(O)OR 17 -OC(O)R 17 -OC(O)N(R 17 ) 2 -C(O)N(R 17 ) 2 -N(R 17 )C(O)R 17 -N(R 17 )C(O)OR 17 -N(R 17 )C(O)N(R 17 ) 2 -N(R 17 )C(S)N(R 17 ) 2 -N(R 17 )S(O) 2 (R 17 )-S(O)R 17 -S(O) 2 R 17 -S(O) 2 N(R 17 ) 2 -NO 2 =O, =S, =NR 17 -N 3 and -CN, C 1~6 alkyl, C 2~6 alkenyl, and C 2~6 alkynyl, each of which is optionally substituted with one or more substituents independently selected from: halogen, -OR 17 -SR 17 -N(R 17 ) 2 -C(O)R 17 , -C(O)OR 17 , -OC(O)R 17 , -OC(O)N(R 17 ) 2 , -C(O)N(R 17 ) 2 , -N(R 17 )C(O)R 17 , -N(R 17 )C(O)OR 17 , , -N(R 17 )C(O)N(R 17 ) 2 , -N(R 17 )C(S)N(R 17 ) 2 , -N(R 17 )S(O) 2 (R 17 , -S(O)R 17 , , -S(O) 2 R 17 , -S(O) 2 , -S(O) 17 ) 2 , -NO 2 , =O, =S, =NR 17 , -N 3 , and -CN, C 3~10 a carbocyclic ring and a 3- to 10-membered heterocyclic ring, each of which is independently selected from halogen, C 1~6 alkyl, C 1~6 haloalkyl, -OR 17 , -SR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)OR 17 , -OC(O)R 17 , -OC(O)N(R 17 ) 2 , -C(O)N(R 17 ) 2 , -N(R 17 )C(O)R 17 , -N(R 17 )C(O)OR 17 , -N(R 17 )C(O)N(R 17 ) 2 , -N(R 17)C(S)N(R 17 ) 2 、-N(R 17 )S(O) 2 (R 17 )、-S(O)R 17 、-S(O) 2 R 17 、-S(O) 2 N(R 17 ) 2 、-NO 2 、=O、=S、=NR 17 、-N 3 、and optionally substituted with one or more substituents independently selected from -CN, and C 3~10 a carbocyclic ring and a 3- to 10-membered heterocyclic ring, each optionally substituted with one or more substituents independently selected from: halogen, -OR 17 、-SR 17 、-N(R 17 ) 2 、-C(O)R 17 、-C(O)OR 17 、-OC(O)R 17 、 -OC(O)N(R 17 ) 2 、-C(O)N(R 17 ) 2 、-N(R 17 )C(O)R 17 、-N(R 17 )C(O)OR 17 、 -N(R 17 )C(O)N(R 17 ) 2 、-N(R 17 )C(S)N(R 17 ) 2 、-N(R 17 )S(O) 2 (R 17 )、-S(O)R 17 、 -S(O) 2 R 17 、-S(O) 2 N(R 17 ) 2 、-NO 2 、=O、=S、=NR17 ,-N 3 , and -CN, C 1~6 alkyl which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 17 , -SR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)OR 17 , -OC(O)R 17 , -OC(O)N(R 17 ) 2 , -C(O)N(R 17 ) 2 , -N(R 17 )C(O)R 17 , -N(R 17 )C(O)OR 17 , -N(R 17 )C(O)N(R 17 ) 2 , -N(R 17 )C(S)N(R 17 ) 2 , -N(R 17 )S(O) 2 (R 17 ), -S(O)R 17 , -S(O) 2 R 17 , -S(O) 2 N(R 17 ) 2 , -NO 2 , =O, =S, =NR 17 , -N 3 , and -CN, and, C 3~10 a carbocyclic ring and a 3- to 10-membered heterocyclic ring, each of which is halogen, C 1~6 alkyl, C 1~6 haloalkyl, -OR 17 , -SR 17 , -N(R 17 ) 2 , -C(O)R 17 , -NO 2 , =O, =S, =NR 17 , -N 3and optionally substituted with one or more substituents independently selected from -CN.
[0168] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), B is C 3~10 selected from carbocyclic rings and 3- to 10-membered heterocyclic rings, each of which is optionally substituted with one or more substituents independently selected from: halogen, -OR 17 , -SR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)OR 17 , -OC(O)R 17 , -C(O)N(R 17 ) 2 , -N(R 17 )C(O)R 17 , -N(R 17 )S(O) 2 (R 17 ), -S(O) 2 R 17 , -S(O) 2 N(R 17 ) 2 , -NO 2 , =O, =S, and -CN, C 1~6 alkyl, C 2~6 alkenyl, and C 2~6 alkynyl, each of which is optionally substituted with one or more substituents independently selected from: halogen, -OR 17 , -SR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)OR 17 , -OC(O)R 17 , -C(O)N(R 17 ) 2 , -N(R 17 )C(O)R 17 , -N(R 17 )S(O) 2 (R 17 ), -S(O)2 R 17 、 -S(O) 2 N(R 17 ) 2 、 =O、 and -CN, C 3~10 a carbocyclic ring and a 3- to 10-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from halogen, C 1~6 alkyl, C 1~6 haloalkyl, -OR 17 、 -SR 17 、 -N(R 17 ) 2 、 -C(O)R 17 、 -C(O)OR 17 、 -OC(O)R 17 、 -C(O)N(R 17 ) 2 、 -N(R 17 )C(O)R 17 、 -N(R 17 )S(O) 2 (R 17 )、 -S(O) 2 R 17 、 -S(O) 2 N(R 17 ) 2 、 -NO 2 、 =O、 =S、 =NR 17 、 and -CN, and C 3~10 a carbocyclic ring and a 3- to 10-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 17 、 -SR 17 、 -N(R 17 ) 2 、 -C(O)R 17 、 -C(O)OR 17 、 -OC(O)R 17 、 -C(O)N(R 17 ) 2 、 -N(R 17 )C(O)R 17 、 -N(R 17 )S(O) 2 (R 17 )、 -S(O) 2 R 17 、 -S(O)2 N(R 17 ) 2 、 =O, =S, and -CN, C 1~6 alkyl, optionally substituted with one or more substituents independently selected from the following: halogen, -OR 17 、 -SR 17 、 -N(R 17 ) 2 、 -C(O)R 17 、 -C(O)OR 17 、 -OC(O)R 17 、 -C(O)N(R 17 ) 2 、 -N(R 17 )C(O)R 17 、 N(R 17 )S(O) 2 (R 17 )、 -S(O) 2 N(R 17 ) 2 、 =O, and -CN, and C 3~10 a carbocyclic ring and a 3- to 10-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from halogen, C 1~6 alkyl, C 1~6 haloalkyl, -OR 17 、 -N(R 17 ) 2 、 =O, and -CN.
[0169] In some embodiments, for the compound or salt of formula (I), (I-a), (II) or (III), B is C 3~10 selected from a carbocyclic ring and a 3- to 10-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from: halogen, -OR 17 、 -N(R 17 ) 2 、 -C(O)R 17 、 -C(O)N(R 17 ) 2 、 -N(R 17 )C(O)R 17 、 -N(R 17 )S(O)2 (R 17 )、 -S(O) 2 R 17 、 -S(O) 2 N(R 17 ) 2 、 =O、 and -CN, C 1~6 alkyl, C 2~6 alkenyl, and C 2~6 alkynyl, each of which is optionally substituted with one or more substituents independently selected from: halogen, -OR 17 、 -SR 17 、 -N(R 17 ) 2 、 -C(O)R 17 、 -C(O)N(R 17 ) 2 、 -N(R 17 )C(O)R 17 、 =O、 and -CN, C 3~10 carbocyclic and 3 - to 10 - membered heterocyclic rings, each of which is optionally substituted with one or more substituents independently selected from halogen, C 1~6 alkyl, C 1~6 haloalkyl, -OR 17 、 -N(R 17 ) 2 、 -C(O)R 17 、 =O、 and -CN, and C 3~10 carbocyclic and 3 - to 10 - membered heterocyclic rings, each of which is optionally substituted with one or more substituents independently selected from: halogen, -OR 17 、 -N(R 17 ) 2 、 -C(O)R 17 、 -C(O)N(R 17 ) 2 、 -N(R 17 )C(O)R 17 、 =O、 and -CN, C 1~6 alkyl which is optionally substituted with one or more substituents independently selected from: halogen, -OR 17 、 -N(R17 ) 2 、 -C(O)R 17 、 -C(O)N(R 17 ) 2 、 -N(R 17 )C(O)R 17 、 =O、 and -CN, and, C 3~10 a carbocyclic ring and a 3- to 10-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from halogen, C 1~6 alkyl, C 1~6 haloalkyl, and -CN.
[0170] In some embodiments, for the compounds or salts of formula (I), (I-a), (II) or (III), B is C 3~10 selected from a carbocyclic ring and a 3- to 10-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from: halogen, -OR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)N(R 17 ) 2 , -N(R 17 )S(O) 2 (R 17 ), -S(O) 2 R 17 , and -CN, C 1~6 alkyl which is optionally substituted with one or more substituents independently selected from halogen, -SR 17 , C 3~10 a carbocyclic ring, and a 3- to 10-membered heterocyclic ring, and the C 3~10 carbocyclic ring and 3- to 10-membered heterocyclic ring are optionally substituted with one or more substituents independently selected from halogen, C 1~6 alkyl, and C 1~6 haloalkyl, and, C 3~10 a carbocyclic ring and a 3- to 10-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from: =O, -CN, C 1~6An alkyl group which is optionally substituted with one or more substituents independently selected from halogen and -OR 17 and a C 3~10 carbocyclic ring.
[0171] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), R 17 is independently, at each occurrence, selected from: hydrogen, a C 1~6 alkyl group which is optionally substituted with one or more substituents independently selected from: halogen, -OR 21 , -SR 21 , -N(R 21 ) 2 , -C(O)R 21 , -C(O)OR 21 , -OC(O)R 21 , -OC(O)N(R 21 ) 2 , -C(O)N(R 21 ) 2 , -N(R 21 )C(O)R 21 , -NO 2 , =O, =S, =NR 21 , and -CN, and a C 3~10 carbocyclic ring and a 3- to 10-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from: halogen, C 1~6 alkyl, C 1~6 haloalkyl, -OR 21 , -SR 21 , -N(R 21 ) 2 , -C(O)R 21 , -C(O)OR 21 , -OC(O)R 21 , -OC(O)N(R 21 ) 2 , -C(O)N(R 21 ) 2 , -N(R 21 )C(O)R 21 , -N(R 21 )C(O)OR 21 、-N(R 21 )C(O)N(R 21 ) 2 、-N(R 21 )C(S)N(R 21 ) 2 、-N(R 21 )S(O) 2 (R 21 )、 -S(O)R 21 、-S(O) 2 R 21 、-S(O) 2 N(R 21 ) 2 、-NO 2 、=O、=S、=NR 17 、-CN、C 3~6 a carbon ring, and a 3- to 6-membered heterocyclic ring.
[0172] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), R 17 is, independently, at each occurrence, selected from: hydrogen, C 1~6 alkyl which is optionally substituted with one or more substituents independently selected from halogen, -OR 21 、-N(R 21 ) 2 、-C(O)R 21 、-C(O)OR 21 、-OC(O)R 21 、-C(O)N(R 21 ) 2 、-N(R 21 )C(O)R 21 、=O, and -CN, and C 3~10 a carbon ring and a 3- to 10-membered heterocyclic ring, each of which is independently selected from halogen, C 1~6 alkyl, C 1~6 haloalkyl -OR 21 、-N(R 21 ) 2 、-C(O)R 21 、-C(O)OR 21 、-OC(O)R21 , -C(O)N(R 21 ) 2 , -N(R 21 )C(O)R 21 , -N(R 21 )S(O) 2 (R 21 ), -S(O)R 21 , -S(O) 2 R 21 , -S(O) 2 N(R 21 ) 2 , =O, -CN, C 3~6 arbon ring, and one or more substituents independently selected from 3- to 6-membered heterocyclic rings, optionally substituted.
[0173] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), R 17 is independently, at each occurrence, selected from: Hydrogen, C 1~6 alkyl which is optionally substituted with one or more substituents independently selected from halogen, -OR 21 , -N(R 21 ) 2 , -C(O)N(R 21 ) 2 , -N(R 21 )C(O)R 21 , =O, and -CN, and C 3~10 arbon ring and 3- to 10-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from halogen, C 1~6 alkyl, C 1~6 haloalkyl -OR 21 , -N(R 21 ) 2 , -C(O)R 21 , -C(O)N(R 21 ) 2 , -N(R 21 )C(O)R 21 , =O, C 3~6 arbon ring, and one or more substituents independently selected from 3- to 6-membered heterocyclic rings, optionally substituted.
[0174] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), R 17 is, independently for each occurrence, selected from: hydrogen, C 1~6 alkyl optionally substituted with one or more substituents independently selected from halogen, -OR 21 , -SR 21 , -N(R 21 ) 2 , and -CN, and C 3~10 carbocyclic ring and 3- to 10-membered heterocyclic ring, each optionally substituted with one or more substituents independently selected from halogen, C 1~6 alkyl, C 1~6 haloalkyl, -OC(O)N(R 21 ) 2 , and C 3~6 carbocyclic ring.
[0175] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), R 17 is, independently for each occurrence, selected from: hydrogen, C 1~6 alkyl optionally substituted with one or more substituents independently selected from halogen and -N(R 21 ) 2 , and C 3~10 carbocyclic ring and 3- to 10-membered heterocyclic ring, each optionally substituted with one or more substituents independently selected from -OC(O)N(R 21 ) 2 , and C 3~6 carbocyclic ring. In some embodiments, R 17 is, independently for each occurrence, selected from: hydrogen and C 1~6 alkyl optionally substituted with one or more substituents independently selected from halogen, -OR 21 , -SR 21 , -N(R 21 ) 2 , and -CN. In some embodiments, R 17is, independently for each occurrence, selected from the following: hydrogen and C 1~6 alkyl which is optionally substituted with one or more substituents independently selected from halogen, -N(R 21 ) 2 , and -CN. In some embodiments, R 17 is, independently for each occurrence, selected from the following: hydrogen and C 1~6 alkyl which is optionally substituted with one or more substituents independently selected from halogen and -N(R 21 ) 2 . In some embodiments, R 17 is, independently for each occurrence, selected from the following: hydrogen, and C 3~10 carbocyclic ring and 3- to 10-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from halogen, C 1~6 alkyl, C 1~6 haloalkyl, -OC(O)N(R 21 ) 2 , and C 3~6 carbocyclic ring. In some embodiments, R 17 is, independently for each occurrence, selected from the following: hydrogen, and C 3~10 carbocyclic ring and 3- to 10-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from halogen, C 1~6 alkyl, -OC(O)N(R 21 ) 2 , and C 3~6 carbocyclic ring. In some embodiments, R 17 is, independently for each occurrence, selected from the following: hydrogen, and C 3~10 carbocyclic ring and 3- to 10-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from -OC(O)N(R 21 ) 2 , and C 3~6 carbocyclic ring.
[0176] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), R 18 and R 21is, independently for each occurrence, hydrogen, C 1~6 alkyl, C 1~6 haloalkyl, C 1~6 hydroxyalkyl, and C 1~6 aminoalkyl. In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), R 18 and R 21 are, independently for each occurrence, hydrogen, C 1~6 alkyl, C 1~6 haloalkyl, and C 1~6 hydroxyalkyl. In some embodiments, R 18 and R 21 are, independently for each occurrence, hydrogen, C 1~6 alkyl, and C 1~6 haloalkyl. In some embodiments, R 18 and R 21 are, independently for each occurrence, hydrogen and C 1~6 alkyl.
[0177] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), R 21 is, independently for each occurrence, hydrogen, C 1~6 alkyl, C 1~6 haloalkyl, and C 1~6 hydroxyalkyl. In some embodiments, R 21 is, independently for each occurrence, hydrogen, C 1~6 alkyl, and C 1~6 haloalkyl. In some embodiments, R 21 is, independently for each occurrence, hydrogen and C 1~6 alkyl. In some embodiments, R 21 is, independently for each occurrence, C 1~6 alkyl. In some embodiments, each R 21 is hydrogen.
[0178] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), B is C 3~10 selected from a carbocyclic ring and a 3- to 10-membered heterocyclic ring, each of which is independently selected from halogen, C 1~6 alkyl, C 1~6 haloalkyl, O-C 1~6 alkyl, -O-C 1~6 haloalkyl, =O, -CN, acetyl, difluoroacetyl,
[0179]
Chemical formula
[0180] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), B is C 3~10 selected from a carbocyclic ring and a 3- to 10-membered heterocyclic ring, each of which is independently selected from halogen, C 1~6 alkyl, C 1~6 haloalkyl, O-C 1~6 alkyl, -O-C 1~6 haloalkyl, =O, -CN, acetyl, difluoroacetyl,
[0181]
Chemical formula
[0182] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), B is phenyl, naphthyl, C 3~10 selected from cycloalkyl, a 5- to 6-membered monocyclic heterocyclic ring, and a 7- to 10-membered bicyclic heterocyclic ring, any of which is optionally substituted. In some embodiments, B is phenyl, C 3~7 monocyclic cycloalkyl, and a 5- to 6-membered monocyclic heterocyclic ring, any of which is optionally substituted. In some embodiments, B is naphthyl, C7~10 Selected from bicyclic cycloalkyl and 7- to 10-membered bicyclic heterocycles, any of which is optionally substituted. In some embodiments, B is optionally substituted phenyl. In some embodiments, B is optionally substituted naphthyl. In some embodiments, B is optionally substituted C 3~10 cycloalkyl. In some embodiments, B is an optionally substituted 5- to 6-membered monocyclic heterocycle. In some embodiments, B is an optionally substituted 7- to 10-membered bicyclic heterocycle.
[0183] In some embodiments, for the compounds or salts of formula (I), (I-a), (II) or (III), B is selected from phenyl, naphthyl, cyclopropyl, cyclohexyl, bicyclo[2.2.2]octane, adamantane, thiazole, pyrrole, pyrazole, pyridine, pyrimidine, pyrazine, indole, indazole, benzimidazole, indoline, azaindole, azaindoline, 1,3-dihydrobenzo[c]isothiazole, tetrahydropyran, azetidine, pyrrolidine, piperidine, quinuclidine, azepane, and 8-azabicyclo[3.2.1]octane, any of which is optionally substituted. In some embodiments, B is selected from phenyl, naphthyl, cyclopropyl, cyclohexyl, bicyclo[2.2.2]octane, adamantane, thiazole, pyrazole, pyridine, indole, indazole, benzimidazole, indoline, 1,3-dihydrobenzo[c]isothiazole, tetrahydropyran, azetidine, pyrrolidine, piperidine, quinuclidine, azepane, and 8-azabicyclo[3.2.1]octane, any of which is optionally substituted. In some embodiments, B is selected from phenyl, cyclohexyl, pyrazole, pyridine, indole, indazole, benzimidazole, indoline, 1,3-dihydrobenzo[c]isothiazole, pyrrolidine, piperidine, pyrrolidine, and piperidine, any of which is optionally substituted. In some embodiments, B is selected from phenyl, indole, indazole, benzimidazole, and 1,3-dihydrobenzo[c]isothiazole, any of which is optionally substituted. In some embodiments, B is optionally substituted phenyl.
[0184] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), B is selected from phenyl, cyclopropyl, cyclohexyl, thiazole, pyrrole, pyrazole, pyridine, pyrimidine, pyrazine, indole, indazole, tetrahydropyran, azetidine, pyrrolidine, piperidine, and azepane, any of which is optionally substituted. In some embodiments, B is selected from phenyl, cyclopropyl, cyclohexyl, thiazole, pyrazole, pyridine, indole, indazole, tetrahydropyran, azetidine, pyrrolidine, piperidine, and azepane, any of which is optionally substituted. In some embodiments, B is selected from naphthyl, bicyclo[2.2.2]octane, adamantane, indole, indazole, benzimidazole, indoline, azaindole, azaindoline, 1,3-dihydrobenzo[c]isothiazole, quinuclidine, and 8-azabicyclo[3.2.1]octane, any of which is optionally substituted. In some embodiments, B is selected from naphthyl, bicyclo[2.2.2]octane, adamantane, indole, indazole, benzimidazole, indoline, 1,3-dihydrobenzo[c]isothiazole, quinuclidine, and 8-azabicyclo[3.2.1]octane, any of which is optionally substituted.
[0185] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), any substituent on B is independently, at each occurrence, selected from the following: halogen, -OR 17 -SR 17 -N(R 17 ) 2 -C(O)R 17 -C(O)OR 17 -OC(O)R 17 - -OC(O)N(R 17 ) 2 -C(O)N(R 17 ) 2 -N(R 17 )C(O)R 17, -N(R 17 )C(O)OR 17 , -N(R 17 )C(O)N(R 17 ) 2 、 -N(R 17 )C(S)N(R 17 ) 2 , -N(R 17 )S(O) 2 (R 17 ), -S(O)R 17 , -S(O) 2 R 17 , -S(O) 2 N(R 17 ) 2 , -NO 2 , =O, =S, =NR 17 , -N 3 , and -CN, C 1~6 alkyl, C 2~6 alkenyl, and C 2~6 alkynyl, each of which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 17 , -SR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)OR 17 , -OC(O)R 17 , -OC(O)N(R 17 ) 2 , -C(O)N(R 17 ) 2 , -N(R 17 )C(O)R 17 , -N(R 17 )C(O)OR 17 , -N(R 17 )C(O)N(R 17 ) 2 , -N(R 17 )C(S)N(R 17 ) 2 , -N(R 17 )S(O) 2 (R 17 ), -S(O)R 17 , -S(O) 2 R 17 , -S(O) 2 N(R 17 ) 2 , -NO 2 , =O, =S, =NR 17 , -N 3 , and -CN, C 3~10 Carbocycles and 3- to 10-membered heterocycles, each of which is independently selected from halogen, C 1~6 Alkyl, C 1~6 Haloalkyl, -OR 17 , -SR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)OR 17 , -OC(O)R 17 , -OC(O)N(R 17 ) 2 , -C(O)N(R 17 ) 2 , -N(R 17 )C(O)R 17 , -N(R 17 )C(O)OR 17 , -N(R 17 )C(O)N(R 17 ) 2 , -N(R 17 )C(S)N(R 17 ) 2 , -N(R 17 )S(O) 2 (R 17 ), -S(O)R 17 , -S(O) 2 R 17 , -S(O) 2 N(R 17 ) 2 , -NO 2 , =O, =S, =NR 17 , -N 3 -, and -CN, C 3~10 Carbocycles and 3- to 10-membered heterocycles, each of which is optionally substituted with one or more substituents independently selected from: Halogen, -OR17 , -SR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)OR 17 , -OC(O)R 17 , -OC(O)N(R 17 ) 2 , -C(O)N(R 17 ) 2 , -N(R 17 )C(O)R 17 , -N(R 17 )C(O)OR 17 , -N(R 17 )C(O)N(R 17 ) 2 , -N(R 17 )C(S)N(R 17 ) 2 , -N(R 17 )S(O) 2 (R 17 ), -S(O)R 17 , -S(O) 2 R 17 , -S(O) 2 N(R 17 ) 2 , -NO 2 , =O, =S, =NR 17 , -N 3 , and -CN, C 1~6 Alkyl, optionally substituted with one or more substituents independently selected from: halogen, -OR 17 , -SR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)OR 17 , -OC(O)R 17 , -OC(O)N(R 17 ) 2 , -C(O)N(R 17 ) 2 , -N(R 17 )C(O)R 17 , -N(R 17 )C(O)OR17 ,-N(R 17 )C(O)N(R 17 ) 2 ,-N(R 17 )C(S)N(R 17 ) 2 ,-N(R 17 )S(O) 2 (R 17 )、-S(O)R 17 ,-S(O) 2 R 17 ,-S(O) 2 N(R 17 ) 2 ,-NO 2 、=O、=S、=NR 17 ,-N 3 、and -CN, and, C 3~10 a carbocyclic ring and a 3- to 10-membered heterocyclic ring, each of which is independently selected from halogen, C 1~6 alkyl, C 1~6 haloalkyl, -OR 17 ,-SR 17 ,-N(R 17 ) 2 ,-C(O)R 17 ,-NO 2 、=O、=S、=NR 17 ,-N 3 、and -CN and is optionally substituted with one or more substituents independently selected therefrom.
[0186] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), any substituent on B is independently, at each occurrence, selected from: halogen, -OR 17 -SR 17 ,-N(R 17 ) 2 ,-C(O)R 17 ,-C(O)OR 17 ,-OC(O)R 17 ,-OC(O)N(R 17 ) 2 、 -C(O)N(R 17 ) 2 ,-N(R 17 )C(O)R 17, -N(R 17 )C(O)OR 17 , -N(R 17 )C(O)N(R 17 ) 2 , -N(R 17 )C(S)N(R 17 ) 2 , -N(R 17 )S(O) 2 (R 17 ), -S(O)R 17 , -S(O) 2 R 17 , -S(O) 2 N(R 17 ) 2 , and -CN, C 1~6 alkyl optionally substituted with one or more substituents independently selected from the following: halogen, -OR 17 , -SR 17 , -N(R 17 ) 2 , -C(O)R 17 , -N(R 17 )C(O)R 17 , -N(R 17 )C(O)OR 17 , -N(R 17 )S(O) 2 (R 17 ), -S(O) 2 N(R 17 ) 2 , =O, -CN, and C 3~10 a carbocyclic ring and a 3- to 10-membered heterocyclic ring, each optionally substituted with one or more substituents independently selected from the following: halogen, C 1~6 alkyl, C 1~6 haloalkyl, -OR 17 , -SR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)OR 17 , -C(O)N(R 17 ) 2 , -N(R 17 )S(O) 2 (R17 ) - S(O) 2 R 17 =O, =S, and - CN, and C 3~10 a carbocyclic ring and a 3 - to 10 - membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from the following: halogen, - OR 17 , - SR 17 , - N(R 17 ) 2 , - C(O)R 17 , - C(O)OR 17 , - C(O)N(R 17 ) 2 , -(R 17 )S(O) 2 (R 17 ), - S(O)R 17 , - S(O) 2 R 17 =O, =S, - CN, and C 1~6 alkyl which is optionally substituted with one or more substituents independently selected from halogen, - OR 17 , - SR 17 , - N(R 17 ) 2 =O, =S, and - CN.
[0187] In some embodiments, for the compounds or salts of formula (I), (I - a), (II) or (III), any substituent on B is independently, at each occurrence, selected from: halogen, - OR 17 , - N(R 17 ) 2 , - C(O)R 17 , - C(O)N(R 17 ) 2 , - N(R 17 )S(O) 2 (R 17 ), - S(O) 2 R 17 , and - CN, C 1~6An alkyl which is optionally substituted with one or more substituents independently selected from halogen and 3- to 10-membered heterocycles, and the 3- to 10-membered heterocycle is halogen, C 1~6 alkyl, and C 1~6 optionally substituted with one or more substituents independently selected from haloalkyl, and C 3~10 a carbocyclic ring and a 3- to 10-membered heterocycle, each of which is optionally substituted with one or more substituents independently selected from halogen, C 1~6 alkyl, and C 1~6 optionally substituted with one or more substituents independently selected from haloalkyl.
[0188] In some embodiments, for the compounds or salts of formula (I), (I-a), (II) or (III), any substituent on B is independently, at each occurrence, selected from the following: halogen, -N(R 17 ) 2 , -N(R 17 )S(O) 2 (R 17 ), and -CN, C 1~6 an alkyl which is optionally substituted with one or more substituents independently selected from halogen and 3- to 10-membered heterocycles, and the 3- to 10-membered heterocycle is optionally substituted with one or more substituents independently selected from halogen and C 1~6 alkyl, and a 3- to 10-membered heterocycle which is optionally substituted with one or more substituents independently selected from C 1~6 alkyl and C 1~6 haloalkyl.
[0189] In some embodiments, for the compounds or salts of formula (I), (I-a), (II), or (III), B is substituted with 1, 2, 3, 4, or 5 substituents. In some embodiments, B is substituted with 1, 2, 3, or 4 substituents. In some embodiments, B is substituted with 1, 2, or 3 substituents. In some embodiments, B is substituted with 2 or 3 substituents. In some embodiments, B is substituted with 1 or 2 substituents. In some embodiments, B is substituted with 1 substituent. In some embodiments, B is substituted with 2 substituents. In some embodiments, B is substituted with 3 substituents. In some embodiments, B is substituted with 4 substituents. In some embodiments, B is substituted with 5 substituents.
[0190] In some embodiments, for the compounds or salts of formula (I), (I-a), (II) or (III), B is phenyl, naphthyl, C 3~10 cycloalkyl, a 5- to 6-membered monocyclic heterocycle, and a 7- to 10-membered bicyclic heterocycle, any of which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 17 , -SR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)OR 17 , -OC(O)R 17 , -C(O)N(R 17 ) 2 , -N(R 17 )C(O)R 17 , -N(R 17 )S(O) 2 (R 17 ), -S(O) 2 R 17 , -S(O) 2 N(R 17 ) 2 , -NO 2 , =O, =S, and -CN, C 1~6 alkyl, C 2~6 alkenyl, and C2~6 An alkynyl group, optionally substituted with one or more substituents independently selected from the following: Halogen, -OR 17 , -SR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)OR 17 , -OC(O)R 17 , -C(O)N(R 17 ) 2 , -N(R 17 )C(O)R 17 , -N(R 17 )S(O) 2 (R 17 ), -S(O) 2 R 17 , -S(O) 2 N(R 17 ) 2 , =O, and -CN, C 3~10 A carbocyclic ring and a 3- to 10-membered heterocyclic ring, each optionally substituted with one or more substituents independently selected from halogen, C 1~6 alkyl, C 1~6 haloalkyl, -OR 17 , -SR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)OR 17 , -OC(O)R 17 , -C(O)N(R 17 ) 2 , -N(R 17 )C(O)R 17 , -N(R 17 )S(O) 2 (R 17 ), -S(O) 2 R 17 , -S(O) 2 N(R 17 ) 2 , -NO 2 , =O, =S, =NR 17 , and -CN, and C 3~10A carbon ring and a 3- to 10-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 17 -SR 17 -N(R 17 ) 2 -C(O)R 17 -C(O)OR 17 -OC(O)R 17 -C(O)N(R 17 ) 2 -N(R 17 )C(O)R 17 -N(R 17 )S(O) 2 (R 17 )-S(O) 2 R 17 -S(O) 2 N(R 17 ) 2 =O, =S, and -CN, C 1~6 alkyl, which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 17 -SR 17 -N(R 17 ) 2 -C(O)R 17 - -C(O)OR 17 -OC(O)R 17 -C(O)N(R 17 ) 2 -N(R 17 )C(O)R 17 N(R 17 )S(O) 2 (R 17 )-S(O) 2 N(R 17 ) 2 =O, and -CN, and C 3~10 a carbon ring and a 3- to 10-membered heterocyclic ring, each of which is halogen, C 1~6 alkyl, C 1~6 haloalkyl, -OR 17 -N(R 17 ) 2One or more substituents independently selected from =O and -CN, and optionally substituted thereby.
[0191] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), B is phenyl, naphthyl, C 3~10 Selected from cycloalkyl, 5- to 6-membered monocyclic heterocycles, and 7- to 10-membered bicyclic heterocycles, any of which is optionally substituted with one or more substituents independently selected from the following: Halogen, -OR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)N(R 17 ) 2 , -N(R 17 )C(O)R 17 , -N(R 17 )S(O) 2 (R 17 ), -S(O) 2 R 17 , -S(O) 2 N(R 17 ) 2 , =O, and -CN, C 1~6 Alkyl, C 2~6 Alkenyl, and C 2~6 Alkynyl, each of which is optionally substituted with one or more substituents independently selected from the following: Halogen, -OR 17 , -SR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)N(R 17 ) 2 , -N(R 17 )C(O)R 17 , =O, and -CN, C 3~10 A carbocyclic ring and a 3- to 10-membered heterocyclic ring, each of which is halogen, C 1~6 Alkyl, C 1~6 Haloalkyl, -OR 17 , -N(R 17 ) 2 , -C(O)R17 One or more substituents independently selected from =O and -CN, optionally substituted, and C 3~10 A carbocyclic ring and a 3- to 10-membered heterocyclic ring, each optionally substituted with one or more substituents independently selected from the following: Halogen, -OR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)N(R 17 ) 2 , -N(R 17 )C(O)R 17 , =O, and -CN, C 1~6 Alkyl optionally substituted with one or more substituents independently selected from halogen, -OR 17 , -N(R 17 ) 2 , -C(O)R 17 , , -C(O)N(R 17 ) 2 , -N(R 17 )C(O)R 17 , =O, and -CN, optionally substituted, and C 3~10 A carbocyclic ring and a 3- to 10-membered heterocyclic ring, each optionally substituted with one or more substituents independently selected from halogen, C 1~6 alkyl, C 1~6 haloalkyl, and -CN.
[0192] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), B is selected from phenyl, naphthyl, C 3~10 cycloalkyl, a 5- to 6-membered monocyclic heterocyclic ring, and a 7- to 10-membered bicyclic heterocyclic ring, any of which is optionally substituted with one or more substituents independently selected from the following: Halogen, -OR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)N(R 17 )2 , -N(R 17 )S(O) 2 (R 17 ), -S(O) 2 R 17 , and -CN, C 1~6 alkyl, optionally substituted with one or more substituents independently selected from halogen, -SR 17 , C 3~10 carbocyclic ring, and 3- to 10-membered heterocyclic ring, and the C 3~10 carbocyclic ring and 3- to 10-membered heterocyclic ring are optionally substituted with one or more substituents independently selected from halogen, C 1~6 alkyl, and C 1~6 haloalkyl, and, C 3~10 carbocyclic ring and 3- to 10-membered heterocyclic ring, each optionally substituted with one or more substituents independently selected from the following: =O, -CN, C 1~6 alkyl, optionally substituted with one or more substituents independently selected from halogen, and -OR 17 , and C 3~10 carbocyclic ring.
[0193] In some embodiments, for the compound or salt of formula (I), (I-a), (II) or (III), B is selected from phenyl, naphthyl, C 3~10 cycloalkyl, 5- to 6-membered monocyclic heterocyclic ring, and 7- to 10-membered bicyclic heterocyclic ring, any of which is optionally substituted with one or more substituents independently selected from halogen, C 1~6 alkyl, C 1~6 haloalkyl, O-C 1~6 alkyl, -O-C 1~6 haloalkyl, =O, -CN, acetyl, difluoroacetyl,
[0194]
Chemical formula
[0195] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), B is selected from phenyl, naphthyl, cyclopropyl, cyclohexyl, bicyclo[2.2.2]octane, adamantane, thiazole, pyrazole, pyridine, indole, indazole, benzimidazole, indoline, 1,3-dihydrobenzo[c]isothiazole, tetrahydropyran, azetidine, pyrrolidine, piperidine, quinuclidine, azepane, and 8-azabicyclo[3.2.1]octane, any of which is optionally substituted with one or more substituents independently selected from: halogen, -OR 17 -SR 17 -N(R 17 ) 2 -C(O)R 17 -C(O)OR 17 -OC(O)R 17 -C(O)N(R 17 ) 2 -N(R 17 )C(O)R 17 -N(R 17 )S(O) 2 (R 17 )-S(O) 2 R 17 -S(O) 2 -S(O)N(R 17 ) 2 -NO 2 =O, =S, and -CN, C 1~6 alkyl, C 2~6 alkenyl, and C 2~6 alkynyl, each of which is optionally substituted with one or more substituents independently selected from: halogen, -OR 17 -SR 17 -N(R 17 ) 2 -C(O)R 17 -C(O)OR 17 -OC(O)R 17 -C(O)N(R 17 ) 2 -N(R 17 )C(O)R17 、 -N(R 17 )S(O) 2 (R 17 )、 -S(O) 2 R 17 、 -S(O) 2 N(R 17 ) 2 、 =O、 and -CN, C 3~10 a carbocyclic ring and a 3 - to 10 - membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from halogen, C 1~6 alkyl, C 1~6 haloalkyl, -OR 17 、 -SR 17 、 -N(R 17 ) 2 、 -C(O)R 17 、 -C(O)OR 17 、 -OC(O)R 17 、 -C(O)N(R 17 ) 2 、 -N(R 17 )C(O)R 17 、 -N(R 17 )S(O) 2 (R 17 )、 -S(O) 2 R 17 、 -S(O) 2 N(R 17 ) 2 、 -NO 2 、 =O、 =S、 =NR 17 、 and -CN, and C 3~10 a carbocyclic ring and a 3 - to 10 - membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 17 、 -SR 17 、 -N(R 17 ) 2 、 -C(O)R 17 、 -C(O)OR 17 、 -OC(O)R 17 、 -C(O)N(R 17 ) 2 、 -N(R 17 )C(O)R 17 、 -N(R 17 )S(O)2 (R 17 )、 -S(O) 2 R 17 、 -S(O) 2 N(R 17 ) 2 、 =O、 =S、 and -CN, C 1~6 alkyl which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 17 、 -SR 17 、 -N(R 17 ) 2 、 -C(O)R 17 、 -C(O)OR 17 、 -OC(O)R 17 、 -C(O)N(R 17 ) 2 、 -N(R 17 )C(O)R 17 、 N(R 17 )S(O) 2 (R 17 )、 -S(O) 2 N(R 17 ) 2 、 =O、 and -CN, and C 3~10 carbocyclic ring and 3- to 10-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from halogen, C 1~6 alkyl, C 1~6 haloalkyl, -OR 17 、 -N(R 17 ) 2 、 =O、 and -CN.
[0196] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), B is selected from phenyl, naphthyl, cyclopropyl, cyclohexyl, bicyclo[2.2.2]octane, adamantane, thiazole, pyrazole, pyridine, indole, indazole, benzimidazole, indoline, 1,3-dihydrobenz[c]isothiazole, tetrahydropyran, azetidine, pyrrolidine, piperidine, quinuclidine, azepane, and 8-azabicyclo[3.2.1]octane, any of which is optionally substituted with one or more substituents independently selected from: halogen, -OR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)N(R 17 ) 2 , -N(R 17 )C(O)R 17 , -N(R 17 )S(O) 2 (R 17 ), -S(O) 2 R 17 , -S(O) 2 N(R 17 ) 2 , =O, and -CN, C 1~6 alkyl, C 2~6 alkenyl, and C 2~6 alkynyl, each of which is optionally substituted with one or more substituents independently selected from: halogen, -OR 17 , -SR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)N(R 17 ) 2 , -N(R 17 )C(O)R 17 , =O, and -CN, C 3~10 carbocyclic and 3- to 10-membered heterocyclic rings, each of which is halogen, C 1~6 alkyl, C 1~6 haloalkyl, -OR 17, -N(R 17 ) 2 , -C(O)R 17 , =O, and one or more substituents independently selected from -CN, optionally substituted; and C 3~10 A carbocyclic ring and a 3- to 10-membered heterocyclic ring, each optionally substituted with one or more substituents independently selected from the following: Halogen, -OR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)N(R 17 ) 2 , -N(R 17 )C(O)R 17 , =O, and -CN, C 1~6 An alkyl group, optionally substituted with one or more substituents independently selected from the following: halogen, -OR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)N(R 17 ) 2 , -N(R 17 )C(O)R 17 , =O, and -CN, and C 3~10 A carbocyclic ring and a 3- to 10-membered heterocyclic ring, each optionally substituted with one or more substituents independently selected from halogen, C 1~6 alkyl, C 1~6 haloalkyl, and -CN.
[0197] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), B is selected from phenyl, naphthyl, cyclopropyl, cyclohexyl, bicyclo[2.2.2]octane, adamantane, thiazole, pyrazole, pyridine, indole, indazole, benzimidazole, indoline, 1,3-dihydrobenzo[c]isothiazole, tetrahydropyran, azetidine, pyrrolidine, piperidine, quinuclidine, azepane, and 8-azabicyclo[3.2.1]octane, any of which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)N(R 17 ) 2 , -N(R 17 )S(O) 2 (R 17 ), -S(O) 2 R 17 , and -CN, C 1~6 alkyl, which is optionally substituted with one or more substituents independently selected from halogen, -SR 17 , C 3~10 carbocyclic ring, and 3- to 10-membered heterocyclic ring, and C 3~10 carbocyclic ring and 3- to 10-membered heterocyclic ring are optionally substituted with one or more substituents independently selected from halogen, C 1~6 alkyl, and C 1~6 haloalkyl, and, C 3~10 carbocyclic ring and 3- to 10-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from the following: =O, -CN, C 1~6 alkyl, which is optionally substituted with one or more substituents independently selected from halogen, and -OR 17 , and C 3~10 carbocyclic ring.
[0198] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), B is selected from phenyl, naphthyl, cyclopropyl, cyclohexyl, bicyclo[2.2.2]octane, adamantane, thiazole, pyrazole, pyridine, indole, indazole, benzimidazole, indoline, 1,3-dihydrobenz[c]isothiazole, tetrahydropyran, azetidine, pyrrolidine, piperidine, quinuclidine, azepane, and 8-azabicyclo[3.2.1]octane, any of which is optionally substituted, and any of which is halogen, C 1~6 alkyl, C 1~6 haloalkyl, O-C 1~6 alkyl, -O-C 1~6 haloalkyl, =O, -CN, acetyl, difluoroacetyl,
[0199]
Chemical formula
[0200] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), B is C 3~7 selected from monocyclic carbocycles and 5- to 6-membered monocyclic heterocycles, any of which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 17 , -SR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)OR 17 , -OC(O)R 17 , -C(O)N(R 17 ) 2 , -N(R 17 )C(O)R 17 , -N(R 17 )S(O) 2 (R 17 ), -S(O) 2 R 17 , -S(O) 2N(R 17 ) 2 、 -NO 2 、 =O, =S, and -CN, C 1~6 alkyl, C 2~6 alkenyl, and C 2~6 alkynyl, each of which is optionally substituted with one or more substituents independently selected from: halogen, -OR 17 、 -SR 17 、 -N(R 17 ) 2 、 -C(O)R 17 、 -C(O)OR 17 、 -OC(O)R 17 、 -C(O)N(R 17 ) 2 、 -N(R 17 )C(O)R 17 、 -N(R 17 )S(O) 2 (R 17 )、 -S(O) 2 R 17 、 -S(O) 2 N(R 17 ) 2 、 =O, and -CN, C 3~10 carbocyclic and 3 - to 10 - membered heterocyclic rings, each of which is halogen, C 1~6 alkyl, C 1~6 haloalkyl, -OR 17 、 -SR 17 、 -N(R 17 ) 2 、 -C(O)R 17 、 -C(O)OR 17 、 -OC(O)R 17 、 -C(O)N(R 17 ) 2 、 -N(R 17 )C(O)R 17 、 -N(R 17 )S(O) 2 (R 17 )、 -S(O) 2 R 17 、 -S(O) 2 N(R 17 ) 2 、 -NO 2, =O, =S, =NR 17 , and optionally substituted with one or more substituents independently selected from, and C 3~10 a carbocyclic ring and a 3- to 10-membered heterocyclic ring, each optionally substituted with one or more substituents independently selected from: halogen, -OR 17 , -SR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)OR 17 , -OC(O)R 17 , -C(O)N(R 17 ) 2 , -N(R 17 )C(O)R 17 , -N(R 17 )S(O) 2 (R 17 ), -S(O) 2 R 17 , -S(O) 2 N(R 17 ) 2 , =O, =S, and -CN, C 1~6 alkyl optionally substituted with one or more substituents independently selected from: halogen, -OR 17 , -SR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)OR 17 , -OC(O)R 17 , -C(O)N(R 17 ) 2 , -N(R 17 )C(O)R 17 , N(R 17 )S(O) 2 (R 17 ), -S(O) 2 N(R 17 ) 2 , =O, and -CN, and C 3~10 a carbocyclic ring and a 3- to 10-membered heterocyclic ring, each of which is halogen, C 1~6Alkyl, C 1~6 Haloalkyl, -OR 17 , -N(R 17 ) 2 , =O, and -CN, and is optionally substituted with one or more substituents independently selected from the following.
[0201] In some embodiments, for a compound or salt of formula (I), (I-a), (II), or (III), B is C 3~7 Selected from monocyclic carbocycles and 5- to 6-membered monocyclic heterocycles, each of which is optionally substituted with one or more substituents independently selected from the following: Halogen, -OR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)N(R 17 ) 2 , -N(R 17 )C(O)R 17 , -N(R 17 )S(O) 2 (R 17 ), -S(O) 2 R 17 , -S(O) 2 N(R 17 ) 2 , =O, and -CN, C 1~6 Alkyl, C 2~6 Alkenyl, and C 2~6 Alkynyl, each of which is optionally substituted with one or more substituents independently selected from the following: Halogen, -OR 17 , -SR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)N(R 17 ) 2 , -N(R 17 )C(O)R 17 , =O, and -CN, C 3~10 Carbocycle and 3- to 10-membered heterocycle, each of which is halogen, C 1~6 Alkyl, C 1~6 Haloalkyl, -OR17 , -N(R 17 ), 2 , -C(O)R 17 , =O, and -CN, and one or more substituents independently selected from the group consisting of those optionally substituted, and C 3~10 a carbocyclic ring and a 3- to 10-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 17 , -N(R 17 ), 2 , -C(O)R 17 , -C(O)N(R 17 ), 2 , -N(R 17 )C(O)R 17 , =O, and -CN, C 1~6 alkyl which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 17 , -N(R 17 ), 2 , -C(O)R 17 , -C(O)N(R 17 ), 2 , -N(R 17 )C(O)R 17 , =O, and -CN, and C 3~10 a carbocyclic ring and a 3- to 10-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from halogen, C 1~6 alkyl, C 1~6 haloalkyl, and -CN.
[0202] In some embodiments, for the compounds or salts of formula (I), (I-a), (II) or (III), B is selected from a monocyclic carbocyclic ring and a 5- to 6-membered monocyclic heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from the following: 3~7 halogen, -OR , -N(R 17 ), 17 ), 2 , -C(O)R17 、 -C(O)N(R 17 ) 2 、 -N(R 17 )S(O) 2 (R 17 )、 -S(O) 2 R 17 、 and -CN, C 1~6 alkyl, optionally substituted with one or more substituents independently selected from halogen, -SR 17 、 C 3~10 carbocyclic ring, and 3- to 10-membered heterocyclic ring, and C 3~10 carbocyclic ring and 3- to 10-membered heterocyclic ring are optionally substituted with one or more substituents independently selected from halogen, C 1~6 alkyl, and C 1~6 haloalkyl, and, C 3~10 carbocyclic ring and 3- to 10-membered heterocyclic ring, each optionally substituted with one or more substituents independently selected from the following: =O, -CN, C 1~6 alkyl, optionally substituted with one or more substituents independently selected from halogen, and -OR 17 selected therefrom, and C 3~10 carbocyclic ring.
[0203] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), B is C 3~7 selected from monocyclic carbocyclic rings and 5- to 6-membered monocyclic heterocyclic rings, each optionally substituted with one or more substituents independently selected from halogen, C 1~6 alkyl, C 1~6 haloalkyl, O-C 1~6 alkyl, -O-C 1~6 haloalkyl, =O, -CN, acetyl, difluoroacetyl,
[0204] [Chemical formula] and is optionally substituted with one or more substituents independently selected therefrom.
[0205] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), B is selected from phenyl, cyclopropyl, cyclohexyl, thiazole, pyrazole, pyridine, indole, indazole, tetrahydropyran, azetidine, pyrrolidine, piperidine, and azepane, any of which is optionally substituted with one or more substituents independently selected from: halogen, -OR 17 , -SR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)OR 17 , -OC(O)R 17 , -C(O)N(R 17 ) 2 , -N(R 17 )C(O)R 17 , -N(R 17 )S(O) 2 (R 17 ), -S(O) 2 R 17 , -S(O) 2 N(R 17 ) 2 , -NO 2 , =O, =S, and -CN, C 1~6 alkyl, C 2~6 alkenyl, and C 2~6 alkynyl, each of which is optionally substituted with one or more substituents independently selected from: halogen, -OR 17 , -SR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)OR 17 , -OC(O)R 17 , , -C(O)N(R 17 ) 2 , -N(R 17 )C(O)R 17 , -N(R 17 )S(O) 2 (R 17 ), -S(O) 2 R 17、 -S(O) 2 N(R 17 ) 2 、 =O, and -CN, C 3~10 a carbocyclic ring and a 3- to 10-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from halogen, C 1~6 alkyl, C 1~6 haloalkyl, -OR 17 、 -SR 17 、 -N(R 17 ) 2 、 -C(O)R 17 、 -C(O)OR 17 、 -OC(O)R 17 、 -C(O)N(R 17 ) 2 、 -N(R 17 )C(O)R 17 、 -N(R 17 )S(O) 2 (R 17 )、 -S(O) 2 R 17 、 -S(O) 2 N(R 17 ) 2 、 -NO 2 、 =O, =S, =NR 17 、 and -CN, and C 3~10 a carbocyclic ring and a 3- to 10-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 17 、 -SR 17 、 -N(R 17 ) 2 、 -C(O)R 17 、 -C(O)OR 17 、 -OC(O)R 17 、 -C(O)N(R 17 ) 2 、 -N(R 17 )C(O)R 17 、 -N(R 17 )S(O) 2 (R 17 )、 -S(O) 2 R 17 、 -S(O) 2 N(R 17 )2 、 =O, =S, and -CN, C 1~6 alkyl, optionally substituted with one or more substituents independently selected from the following: halogen, -OR 17 , -SR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)OR 17 , -OC(O)R 17 , -C(O)N(R 17 ) 2 , -N(R 17 )C(O)R 17 , N(R 17 )S(O) 2 (R 17 ), -S(O) 2 N(R 17 ) 2 , =O, and -CN, and C 3~10 a carbocyclic ring and a 3- to 10-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from halogen, C 1~6 alkyl, C 1~6 haloalkyl, -OR 17 , -N(R 17 ) 2 , =O, and -CN.
[0206] In some embodiments, for a compound or salt of formula (I), (I-a), (II), or (III), B is selected from phenyl, cyclopropyl, cyclohexyl, thiazole, pyrazole, pyridine, indole, indazole, tetrahydropyran, azetidine, pyrrolidine, piperidine, and azepane, any of which is optionally substituted with one or more substituents independently selected from: halogen, -OR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)N(R 17 ) 2 , -N(R 17 )C(O)R 17, -N(R 17 )S(O) 2 (R 17 ), -S(O) 2 R 17 , -S(O) 2 N(R 17 ) 2 , =O, and -CN, C 1~6 alkyl, C 2~6 alkenyl, and C 2~6 alkynyl, each of which is optionally substituted with one or more substituents independently selected from: halogen, -OR 17 , -SR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)N(R 17 ) 2 , -N(R 17 )C(O)R 17 , =O, and -CN, C 3~10 carbocyclic and 3- to 10-membered heterocyclic rings, each of which is optionally substituted with one or more substituents independently selected from halogen, C 1~6 alkyl, C 1~6 haloalkyl, -OR 17 , -N(R 17 ) 2 , -C(O)R 17 , =O, and -CN, and C 3~10 carbocyclic and 3- to 10-membered heterocyclic rings, each of which is optionally substituted with one or more substituents independently selected from: halogen, -OR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)N(R 17 ) 2 , -N(R 17 )C(O)R 17 , =O, and -CN, C 1~6 alkyl which is optionally substituted with one or more substituents independently selected from: halogen, -OR17 , -N(R 17 ), 2 , -C(O)R 17 , , -C(O)N(R 17 ), 2 , -N(R 17 ),C(O)R 17 , =O, and -CN, and C 3~10 a carbocyclic ring and a 3- to 10-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from halogen, C 1~6 alkyl, C 1~6 haloalkyl, and -CN.
[0207] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), B is selected from phenyl, cyclopropyl, cyclohexyl, thiazole, pyrazole, pyridine, indole, indazole, tetrahydropyran, azetidine, pyrrolidine, piperidine, and azepane, any of which is optionally substituted with one or more substituents independently selected from: halogen, -OR 17 , -N(R 17 ), 2 , -C(O)R 17 , -C(O)N(R 17 ), 2 , -N(R 17 ),S(O) 2 (R 17 ), -S(O) 2 R 17 , and -CN, C 1~6 alkyl which is optionally substituted with one or more substituents independently selected from halogen, -SR 17 , C 3~10 a carbocyclic ring, and a 3- to 10-membered heterocyclic ring, and the C 3~10 carbocyclic ring and 3- to 10-membered heterocyclic ring are optionally substituted with one or more substituents independently selected from halogen, C 1~6 alkyl, and C 1~6 haloalkyl, and C 3~10A carbon ring and a 3- to 10-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from the following: =O, -CN, C 1~6 alkyl, which is optionally substituted with one or more substituents independently selected from halogen, and -OR 17 and is optionally substituted with one or more substituents independently selected from C 3~10 a carbon ring.
[0208] In some embodiments, for the compound or salt of formula (I), (I-a), (II) or (III), B is selected from phenyl, cyclopropyl, cyclohexyl, thiazole, pyrazole, pyridine, indole, indazole, tetrahydropyran, azetidine, pyrrolidine, piperidine, and azepane, any of which is halogen, C 1~6 alkyl, C 1~6 haloalkyl, O-C 1~6 alkyl, -O-C 1~6 haloalkyl, =O, -CN, acetyl, difluoroacetyl,
[0209]
Chemical formula
[0210] In some embodiments, for the compound or salt of formula (I), (I-a), (II) or (III), B is C 7~10 selected from a bicyclic carbon ring and a 7- to 10-membered bicyclic heterocyclic ring, any of which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 17 , -SR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)OR 17 , -OC(O)R 17 , -C(O)N(R 17 ) 2 , -N(R 17 )C(O)R 17, -N(R 17 )S(O) 2 (R 17 ), -S(O) 2 R 17 , -S(O) 2 N(R 17 ) 2 , -NO 2 , =O, =S, and -CN, C 1~6 alkyl, C 2~6 alkenyl, and C 2~6 alkynyl, each of which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 17 , -SR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)OR 17 , -OC(O)R 17 , , -C(O)N(R 17 ) 2 , -N(R 17 )C(O)R 17 , -N(R 17 )S(O) 2 (R 17 ), -S(O) 2 R 17 , -S(O) 2 N(R 17 ) 2 , =O, and -CN, C 3~10 carbocyclic ring and 3- to 10-membered heterocyclic ring, each of which is halogen, C 1~6 alkyl, C 1~6 haloalkyl, -OR 17 , -SR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)OR 17 , -OC(O)R 17 , -C(O)N(R 17 ) 2 , -N(R 17 )C(O)R 17 , -N(R 17 )S(O) 2 (R17 )、 -S(O) 2 R 17 、 -S(O) 2 N(R 17 ) 2 、 -NO 2 、 =O、 =S、 =NR 17 、 and one or more substituents independently selected from -CN, and optionally substituted with one or more substituents independently selected from the following: C 3~10 a carbocyclic ring and a 3- to 10-membered heterocyclic ring, each optionally substituted with one or more substituents independently selected from the following: halogen, -OR 17 、 -SR 17 、 -N(R 17 ) 2 、 -C(O)R 17 、 -C(O)OR 17 、 -OC(O)R 17 、 -C(O)N(R 17 ) 2 、 -N(R 17 )C(O)R 17 、 -N(R 17 )S(O) 2 (R 17 、 -S(O) 2 R 17 、 -S(O) 2 N(R 17 ) 2 、 =O、 =S、 and -CN, C 1~6 alkyl optionally substituted with one or more substituents independently selected from the following: halogen, -OR 17 、 -SR 17 、 -N(R 17 ) 2 、 -C(O)R 17 、 -C(O)OR 17 、 -OC(O)R 17 、 -C(O)N(R 17 ) 2 、 -N(R 17 )C(O)R 17 、 N(R 17 )S(O) 2 (R 17 、 -S(O) 2 N(R17 ) 2 =O, -CN, and C 3~10 a carbocyclic ring and a 3- to 10-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from halogen, C 1~6 alkyl, C 1~6 haloalkyl, -OR 17 , -N(R 17 ) 2 , =O, and -CN.
[0211] In some embodiments, for the compound or salt of formula (I), (I-a), (II), or (III), B is selected from a bicyclic carbocyclic ring and a 7- to 10-membered bicyclic heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from: 7~10 halogen, -OR , -N(R 17 ), -C(O)R 17 ), -C(O)N(R 2 ), -N(R 17 )(O)R, -N(R 17 )(O)N(R 2 ), -N(R 17 )(O)S(O)(R 17 ), -S(O)(R 17 ), -S(O)(O)N(R 2 ), =O, and -CN, 17 C 2 alkyl, C 17 alkenyl, and C 2 alkynyl, each of which is optionally substituted with one or more substituents independently selected from: 17 ), -SR 2 , =O, and -CN, C 1~6 alkyl, C 2~6 alkenyl, and C 2~6 alkynyl, each of which is optionally substituted with one or more substituents independently selected from: halogen, -OR 17 , -SR 17 , -N(R 17 ), -C(O)R 2 , -C(O)N(R 17 ), -N(R 17 )(O)R, -N(R 2 )(O)N(R 17 ), -N(R 17, =O, and -CN, C 3~10 A carbocyclic ring and a 3- to 10-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from halogen, C 1~6 alkyl, C 1~6 haloalkyl, -OR 17 , -N(R 17 ) 2 , -C(O)R 17 , =O, and -CN, and C 3~10 A carbocyclic ring and a 3- to 10-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)N(R 17 ) 2 , -N(R 17 )C(O)R 17 , =O, and -CN, C 1~6 An alkyl which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)N(R 17 ) 2 , -N(R 17 )C(O)R 17 , =O, and -CN, and C 3~10 A carbocyclic ring and a 3- to 10-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from halogen, C 1~6 alkyl, C 1~6 haloalkyl, and -CN.
[0212] In some embodiments, for the compound or salt of formula (I), (I-a), (II) or (III), B is C 7~10Selected from bicyclic carbon rings and 7- to 10-membered bicyclic heterocycles, each of which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)N(R 17 ) 2 , -N(R 17 )S(O) 2 (R 17 ), -S(O) 2 R 17 , and -CN, C 1~6 alkyl, optionally substituted with one or more substituents independently selected from halogen, -SR 17 , C 3~10 carbon ring, and 3- to 10-membered heterocycle, and C 3~10 carbon ring and 3- to 10-membered heterocycle are optionally substituted with one or more substituents independently selected from halogen, C 1~6 alkyl, and C 1~6 haloalkyl, and C 3~10 carbon ring and 3- to 10-membered heterocycle, each of which is optionally substituted with one or more substituents independently selected from the following: =O, -CN, C 1~6 alkyl, optionally substituted with one or more substituents independently selected from halogen, and -OR 17 , and C 3~10 carbon ring.
[0213] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), B is selected from a bicyclic carbon ring and a 7- to 10-membered bicyclic heterocycle, each of which is halogen, C 7~10 alkyl, C 1~6 haloalkyl, O-C 1~6 alkyl, -O-C 1~6 haloalkyl, =O, -CN, acetyl, difluoroacetyl, 1~6
[0214] [Chemistry] optionally substituted with one or more substituents independently selected from
[0215] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), B is selected from naphthyl, bicyclo[2.2.2]octane, adamantane, indole, indazole, benzimidazole, indoline, 1,3-dihydrobenz[c]isothiazole, quinuclidine, and 8-azabicyclo[3.2.1]octane, any of which is optionally substituted with one or more substituents independently selected from: halogen, -OR 17 , -SR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)OR 17 , -OC(O)R 17 , -C(O)N(R 17 ) 2 , -N(R 17 )C(O)R 17 , -N(R 17 )S(O) 2 (R 17 ), -S(O) 2 R 17 , -S(O) 2 N(R 17 ) 2 , -NO 2 , =O, =S, and -CN, C 1~6 alkyl, C 2~6 alkenyl, and C 2~6 alkynyl, each of which is optionally substituted with one or more substituents independently selected from: halogen, -OR 17 , -SR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)OR 17 , -OC(O)R 17 , -C(O)N(R 17 ) 2 、-N(R 17 )C(O)R 17 、-N(R 17 )S(O) 2 (R 17 )、-S(O) 2 R 17 、-S(O) 2 N(R 17 ) 2 、=O、and -CN, C 3~10 a carbocyclic ring and a 3- to 10-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from halogen, C 1~6 alkyl, C 1~6 haloalkyl, -OR 17 、-SR 17 、-N(R 17 ) 2 、-C(O)R 17 、-C(O)OR 17 、-OC(O)R 17 、-C(O)N(R 17 ) 2 、-N(R 17 )C(O)R 17 、-N(R 17 )S(O) 2 (R 17 )、-S(O) 2 R 17 、-S(O) 2 N(R 17 ) 2 、-NO 2 、=O、=S、=NR 17 、and -CN, and C 3~10 a carbocyclic ring and a 3- to 10-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 17 、-SR 17 、-N(R 17 ) 2 、-C(O)R 17 、-C(O)OR 17 、-OC(O)R 17 、-C(O)N(R 17 )2 , -N(R 17 )C(O)R 17 , -N(R 17 )S(O) 2 (R 17 ), -S(O) 2 R 17 , -S(O) 2 N(R 17 ) 2 , =O, =S, and -CN, C 1~6 alkyl, optionally substituted with one or more substituents independently selected from the following: halogen, -OR 17 , -SR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)OR 17 , -OC(O)R 17 , -C(O)N(R 17 ) 2 , -N(R 17 )C(O)R 17 , N(R 17 )S(O) 2 (R 17 ), -S(O) 2 N(R 17 ) 2 , =O, and -CN, and C 3~10 a carbocyclic ring and a 3- to 10-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from halogen, C 1~6 alkyl, C 1~6 haloalkyl, -OR 17 , -N(R 17 ) 2 , =O, and -CN.
[0216] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), B is selected from naphthyl, bicyclo[2.2.2]octane, adamantane, indole, indazole, benzimidazole, indoline, 1,3-dihydrobenz[c]isothiazole, quinuclidine, and 8-azabicyclo[3.2.1]octane, any of which is optionally substituted with one or more substituents independently selected from: halogen, -OR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)N(R 17 ) 2 , -N(R 17 )C(O)R 17 , -N(R 17 )S(O) 2 (R 17 ), -S(O) 2 R 17 , -S(O) 2 N(R 17 ) 2 , =O, and -CN, C 1~6 alkyl, C 2~6 alkenyl, and C 2~6 alkynyl, each of which is optionally substituted with one or more substituents independently selected from: halogen, -OR 17 , -SR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)N(R 17 ) 2 , -N(R 17 )C(O)R 17 , =O, and -CN, C 3~10 carbocyclic and 3- to 10-membered heterocyclic rings, each of which is halogen, C 1~6 alkyl, C 1~6 haloalkyl, -OR 17 , -N(R 17 ) 2 , -C(O)R 17One or more substituents independently selected from =O and -CN, optionally substituted, and C 3~10 A carbocyclic ring and a 3- to 10-membered heterocyclic ring, each optionally substituted with one or more substituents independently selected from the following: Halogen, -OR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)N(R 17 ) 2 , -N(R 17 )C(O)R 17 , =O, and -CN, C 1~6 Alkyl optionally substituted with one or more substituents independently selected from the following: halogen, -OR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)N(R 17 ) 2 , -N(R 17 )C(O)R 17 , =O, and -CN, and C 3~10 A carbocyclic ring and a 3- to 10-membered heterocyclic ring, each optionally substituted with one or more substituents independently selected from halogen, C 1~6 alkyl, C 1~6 haloalkyl, and -CN.
[0217] In some embodiments, for a compound or salt of formula (I), (I-a), (II), or (III), B is selected from naphthyl, bicyclo[2.2.2]octane, adamantane, indole, indazole, benzimidazole, indoline, 1,3-dihydrobenzo[c]isothiazole, quinuclidine, and 8-azabicyclo[3.2.1]octane, any of which is optionally substituted with one or more substituents independently selected from the following: Halogen, -OR 17 , -N(R 17 ) 2, -C(O)R 17 , -C(O)N(R 17 ) 2 , -N(R 17 )S(O) 2 (R 17 ), -S(O) 2 R 17 , and -CN, C 1~6 alkyl, optionally substituted with one or more substituents independently selected from halogen, -SR 17 , C 3~10 carbocyclic ring, and 3- to 10-membered heterocyclic ring, and C 3~10 carbocyclic ring and 3- to 10-membered heterocyclic ring are optionally substituted with one or more substituents independently selected from halogen, C 1~6 alkyl, and C 1~6 haloalkyl, and, C 3~10 carbocyclic ring and 3- to 10-membered heterocyclic ring, each optionally substituted with one or more substituents independently selected from the following: =O, -CN, C 1~6 alkyl, optionally substituted with one or more substituents independently selected from halogen, and -OR 17 , and C 3~10 carbocyclic ring.
[0218] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), B is selected from naphthyl, bicyclo[2.2.2]octane, adamantane, indole, indazole, benzimidazole, indoline, 1,3-dihydrobenzo[c]isothiazole, quinuclidine, and 8-azabicyclo[3.2.1]octane, any of which is optionally substituted with halogen, C 1~6 alkyl, C 1~6 haloalkyl, O-C 1~6 alkyl, -O-C 1~6 haloalkyl, =O, -CN, acetyl, difluoroacetyl,
[0219] [Chemical formula] Optionally substituted with one or more substituents independently selected from
[0220] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), B is
[0221]
Chemical formula
[0222] In some embodiments, for a compound or salt of formula (I), (I-a), (II), or (III), B is
[0223]
Chemical formula
[0224] In some embodiments, for the compounds or salts of formula (I), (I-a), (II) or (III), B is
[0225]
Chemical formula
[0226] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), s is 0, 1, 2, and 3. In some embodiments, s is 0, 1, or 2. In some embodiments, s is 1, 2, or 3. In some embodiments, s is 0 or 1. In some embodiments, s is 1 or 2. In some embodiments, s is 2 or 3. In some embodiments, s is 0. In some embodiments, s is 1. In some embodiments, s is 2. In some embodiments, s is 3.
[0227] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), r is 0, 1, or 2. In some embodiments, r is 0 or 1. In some embodiments, r is 1 or 2. In some embodiments, r is 0. In some embodiments, r is 1. In some embodiments, r is 2.
[0228] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), R 6 and R 6’ are each independently selected from: hydrogen, halogen, -OR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)OR 17 , -OC(O)R 17 , -C(O)N(R 17 ) 2 , -N(R 17 )C(O)R 17 , -N(R 17 )S(O) 2 (R 17 ), -S(O) 2 R 17 , -S(O) 2 N(R 17 ) 2 , -CN, and C 1~6 alkyl optionally substituted with one or more substituents independently selected from: halogen, -OR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)OR 17 , -OC(O)R 17 , -C(O)N(R 17 ) 2 , -N(R 17 )C(O)R 17 , -N(R 17 )S(O) 2 (R 17 ), -S(O) 2 R 17 , -S(O) 2 N(R 17 ) 2 , =O, and -CN, C 3~10 a carbocyclic ring and a 3- to 10-membered heterocyclic ring, each of which is independently selected from halogen, -OR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)OR 17 , -OC(O)R 17 , -C(O)N(R 17 ) 2 , -N(R 17 )C(O)R 17 , -N(R 17 )S(O) 2 (R 17 ), -S(O) 2 R 17 , -S(O) 2 N(R 17 ) 2 , =O, and -CN, and is optionally substituted with one or more substituents independently selected therefrom.
[0229] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), R 6 and R 6’ are each independently selected from: hydrogen, halogen, -OR 17 , -N(R 17 ) 2 , and C 1~6 alkyl, which is halogen, -OR 17, -N(R 17 ) 2 , C 3~10 a carbon ring, and optionally substituted with one or more substituents independently selected from 3- to 10-membered heterocyclic rings, each of which is optionally substituted with one or more substituents independently selected from halogen, -OR 17 , -N(R 17 ) 2 , =O, and -CN. In some embodiments, R 6 and R 6’ are each independently selected from: hydrogen, halogen, and C 1~6 alkyl, optionally substituted with one or more substituents independently selected from halogen, C 3~10 a carbon ring, and 3- to 10-membered heterocyclic rings, each of which is optionally substituted with one or more substituents independently selected from halogen, =O, and -CN. In some embodiments, R 6 and R 6’ are each independently selected from: halogen, and C 1~6 alkyl, optionally substituted with one or more substituents independently selected from halogen and 3- to 10-membered heterocyclic rings, each of which is optionally substituted with one or more substituents independently selected from halogen.
[0230] In some embodiments, for the compound or salt of formula (I), (I-a), (II) or (III), R 6 , and R 6’ are each independently selected from: hydrogen, halogen, -OR 17 , -SR 17 , -N(R 41 ) 2 , -C(O)R 41 , -C(O)OR 17 , -OC(O)R 17 , -OC(O)N(R 17 ) 2 , -C(O)N(R 17 ) 2 , -N(R 17 )C(O)R 17 , -N(R 17)C(O)OR 17 、 -N(R 17 )C(O)N(R 17 ) 2 、 -N(R 17 )S(O) 2 (R 17 )、 -S(O)R 17 、 -S(O) 2 R 17 、 -S(O) 2 N(R 17 ) 2 、 -NO 2 、 -N 3 、 -CN, and C 1~6 alkyl optionally substituted with one or more substituents independently selected from halogen, -OH, -O-C 1~6 alkyl, -O-C 1~6 haloalkyl -NH 2 、 -NO 2 、 =O, and -CN. In some embodiments, R 6 and R 6’ are each independently selected from: hydrogen, halogen, -OR 17 、 -SR 17 、 -N(R 41 ) 2 、 -C(O)R 41 、 -C(O)OR 17 、 -OC(O)R 17 、 -C(O)N(R 17 ) 2 、 -N(R 17 )C(O)R 17 、 -N(R 17 )S(O) 2 (R 17 )、 -S(O)R 17 、 -S(O) 2 R 17 、 -S(O) 2 N(R 17 ) 2 、 -CN, and C 1~6 alkyl optionally substituted with one or more substituents independently selected from halogen, -OH, -O-C 1~6 alkyl, -O-C 1~6 haloalkyl, =O, and -CN. In some embodiments, R 6and R 6’ is, independently of each other, selected from the following: hydrogen, halogen, -OR 17 , -SR 17 , -N(R 41 ) 2 , -C(O)R 41 , -C(O)OR 17 , -OC(O)R 17 , -C(O)N(R 17 ) 2 , -N(R 17 )C(O)R 17 , -CN, and C 1~6 alkyl which is optionally substituted with one or more substituents independently selected from halogen, -OH, -O-C 1~6 alkyl, and =O. In some embodiments, R 6 and R 6’ are, independently of each other, selected from the following: hydrogen, halogen, -OR 17 , -SR 17 , -N(R 41 ) 2 , -CN, and C 1~6 alkyl which is optionally substituted with one or more substituents independently selected from halogen and =O. In some embodiments, R 6 and R 6’ are, independently of each other, selected from hydrogen, halogen, -OR 17 , -N(R 41 ) 2 , -CN, C 1~6 alkyl, and C 1~6 haloalkyl. In some embodiments, R 6 and R 6’ are, independently of each other, selected from hydrogen, halogen, C 1~6 alkyl, and C 1~6 haloalkyl. In some embodiments, R 6 and R 6’ are, independently of each other, selected from halogen, C 1~6 alkyl, and C 1~6 haloalkyl. In some embodiments, R 6 and R 6’is independently selected from halogen. In some embodiments, R 6 and R 6’ are each independently selected from fluoro.
[0231] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), R 7 , and R 8 are each independently selected from: hydrogen, halogen, -OR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)OR 17 , -OC(O)R 17 , -C(O)N(R 17 ) 2 , -N(R 17 )C(O)R 17 , -N(R 17 )S(O) 2 (R 17 ), -S(O) 2 R 17 , -S(O) 2 N(R 17 ) 2 , and -CN, C 1~6 alkyl optionally substituted with one or more substituents independently selected from: halogen, -OR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)OR 17 , -OC(O)R 17 , -C(O)N(R 17 ) 2 , -N(R 17 )C(O)R 17 , -N(R 17 )S(O) 2 (R 17 ), -S(O) 2 R 17 , -S(O) 2 N(R 17 ) 2, =O, and -CN, C 3~10 A carbocyclic ring and a 3- to 10-membered heterocyclic ring, each of which is independently selected from halogen, -OR 17 , -SR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)OR 17 , -OC(O)R 17 , -C(O)N(R 17 ) 2 , -N(R 17 )C(O)R 17 , -N(R 17 )S(O) 2 (R 17 ), -S(O) 2 R 17 , -S(O) 2 N(R 17 ) 2 , =O, and -CN, and is optionally substituted with one or more substituents independently selected therefrom, and C 3~10 A carbocyclic ring and a 3- to 10-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from the following: Halogen, -OR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)OR 17 , -OC(O)R 17 , -C(O)N(R 17 ) 2 , -N(R 17 )C(O)R 17 , -N(R 17 )S(O) 2 (R 17 ), -S(O)R 17 , -S(O) 2 R 17 , -S(O) 2 N(R 17 ) 2 , =O, and -CN.
[0232] In some embodiments, for the compounds or salts of formula (I), (I-a), (II) or (III), R 7and R 8 is independently selected from the following: hydrogen, halogen, -OR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)OR 17 , -OC(O)R 17 , -C(O)N(R 17 ) 2 , -N(R 17 )C(O)R 17 , -N(R 17 )S(O) 2 (R 17 ), -S(O) 2 R 17 , -S(O) 2 N(R 17 ) 2 , and -CN, C 1~6 alkyl optionally substituted with one or more substituents independently selected from the following: halogen, -OR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)OR 17 , -OC(O)R 17 , -C(O)N(R 17 ) 2 , -N(R 17 )C(O)R 17 , -N(R 17 )S(O) 2 (R 17 ), -S(O) 2 R 17 , -S(O) 2 N(R 17 ) 2 , =O, and -CN, C 3~10 a carbocyclic ring and a 3- to 10-membered heterocyclic ring, each of which is halogen, -OR 17 , -SR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)OR 17 , -OC(O)R 17, -C(O)N(R 17 ) 2 , -N(R 17 )C(O)R 17 , -N(R 17 )S(O) 2 (R 17 ), -S(O) 2 R 17 , -S(O) 2 N(R 17 ) 2 , =O, and one or more substituents independently selected from -CN, and C 3~10 a carbocyclic ring and a 3- to 10-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)OR 17 , -OC(O)R 17 , -C(O)N(R 17 ) 2 , -N(R 17 )C(O)R 17 , -N(R 17 )S(O) 2 (R 17 ), -S(O)R 17 , -S(O) 2 R 17 , -S(O) 2 N(R 17 ) 2 , =O, and -CN.
[0233] In some embodiments, for the compounds or salts of formula (I), (I-a), (II) or (III), R 7 , and R 8 are each independently selected from the following: halogen, -OR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)N(R 17 ) 2 , -N(R 17 )S(O) 2(R 17 )、 -S(O) 2 R 17 、 and -CN, C 1~6 alkyl, optionally substituted with one or more substituents independently selected from halogen and 3- to 10-membered heterocycles, wherein the 3- to 10-membered heterocycle is optionally substituted with one or more substituents independently selected from halogen, C 1~6 alkyl, and C 1~6 haloalkyl, and C 3~10 carbocycles and 3- to 10-membered heterocycles, each optionally substituted with one or more substituents independently selected from halogen, C 1~6 alkyl, and C 1~6 haloalkyl.
[0234] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), R 7 , and R 8 are each independently selected from: halogen, -N(R 17 ) 2 , -N(R 17 )S(O) 2 (R 17 ), and -CN, C 1~6 alkyl, optionally substituted with one or more substituents independently selected from halogen and 3- to 10-membered heterocycles, wherein the 3- to 10-membered heterocycle is optionally substituted with one or more substituents independently selected from halogen and C 1~6 alkyl, and C 1~6 alkyl and C 1~6 haloalkyl, optionally substituted with one or more substituents independently selected from, a 3- to 10-membered heterocycle.
[0235] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), B is
[0236] [Chemical]
[0237] [Chemical]
[0238] [Chemical] selected from.
[0239] In some embodiments, for the compound or salt of formula (I), (I-a), (II) or (III), B is
[0240] [Chemical]
[0241] [Chemical]
[0242] [Chemical] selected from.
[0243] In some embodiments, for the compound or salt of formula (I), (I-a), (II) or (III), B is
[0244] [Chemical]
[0245] [Chemical]
[0246] [Chemical] selected from.
[0247] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), B is
[0248] [Chemical formula] selected from.
[0249] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), B is halogen, C 1~6 alkyl, C 1~6 haloalkyl, O-C 1~6 alkyl, -O-C 1~6 haloalkyl, =O, -CN, acetyl, difluoroacetyl,
[0250] [Chemical formula] selected from.
[0251] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), C is selected from C 5~10 a carbocyclic ring and a 5- to 10-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 , -SR 18 , -N(R 18 ) 2 , -C(O)R 18 , -C(O)OR 18 , -OC(O)R 18 , -OC(O)N(R 18 ) 2 , -C(O)N(R 18 ) 2 , -N(R 18 )C(O)R 18 , -N(R 18)C(O)OR 18 , -N(R 18 )C(O)N(R 18 ) 2 , -N(R 18 )C(S)N(R 18 ) 2 , -N(R 18 )S(O) 2 (R 18 ), -S(O)R 18 , -S(O) 2 R 18 , -S(O) 2 N(R 18 ) 2 , -NO 2 , =O, =S, =NR 18 , -N 3 , and -CN, C 1~6 Alkyl, C 2~6 Alkenyl, and C 2~6 Alkynyl, each of which is optionally substituted with one or more substituents independently selected from: Halogen, -OR 18 , -SR 18 , -N(R 18 ) 2 , -C(O)R 18 , -C(O)OR 18 , -OC(O)R 18 , -OC(O)N(R 18 ) 2 , -C(O)N(R 18 ) 2 , -N(R 18 )C(O)R 18 , -N(R 18 )C(O)OR 18 , -N(R 18 )C(O)N(R 18 ) 2 , -N(R 18 )C(S)N(R 18 ) 2 , -N(R 18 )S(O) 2 (R 18 ), -S(O)R 18 , -S(O)2 R 18 、 -S(O) 2 N(R 18 ) 2 、 -NO 2 、 =O、 =S、 =NR 18 、 -N 3 、 -CN、 C 3~6 a carbon ring and a 3- to 6-membered heterocyclic ring, provided that C 3~6 the carbon ring and the 3- to 6-membered heterocyclic ring are each optionally substituted with one or more substituents independently selected from halogen, C 1~4 alkyl, and C 1~4 haloalkyl, and C 3~6 a carbon ring and a 3- to 6-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from halogen, C 1~6 alkyl, C 1~6 haloalkyl, -OR 18 、 -SR 18 、 -N(R 18 ) 2 、 -C(O)R 18 、 -NO 2 、 =O、 =S、 =NR 18 、 -N 3 、 and -CN.
[0252] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), C is C 5~10 the carbon ring is optionally substituted with one or more substituents independently selected from: halogen, -OR 18 、 -SR 18 、 -N(R 18 ) 2 、 -C(O)R 18 、 -C(O)OR 18 、 -OC(O)R 18 、 -OC(O)N(R 18 ) 2 、 -C(O)N(R 18 ) 2 、 -N(R 18 )C(O)R 18 、 -N(R 18)C(O)OR 18 , -N(R 18 )C(O)N(R 18 ) 2 , -N(R 18 )C(S)N(R 18 ) 2 , -N(R 18 )S(O) 2 (R 18 ), -S(O)R 18 , -S(O) 2 R 18 , -S(O) 2 N(R 18 ) 2 , -NO 2 , =O, =S, =NR 18 , -N 3 , and -CN, C 1~6 Alkyl, C 2~6 Alkenyl, and C 2~6 Alkynyl, each of which is optionally substituted with one or more substituents independently selected from: Halogen, -OR 18 , -SR 18 , -N(R 18 ) 2 , -C(O)R 18 , -C(O)OR 18 , -OC(O)R 18 , -OC(O)N(R 18 ) 2 , -C(O)N(R 18 ) 2 , -N(R 18 )C(O)R 18 , -N(R 18 )C(O)OR 18 , -N(R 18 )C(O)N(R 18 ) 2 , -N(R 18 )C(S)N(R 18 ) 2 , -N(R 18 )S(O) 2 (R 18 ), -S(O)R 18 , -S(O)2 R 18 、 -S(O) 2 N(R 18 ) 2 、 -NO 2 、 =O、 =S、 =NR 18 、 -N 3 、 -CN、 C 3~6 a carbon ring and a 3- to 6-membered heterocyclic ring, wherein the carbon ring and the 3- to 6-membered heterocyclic ring are each optionally substituted with one or more substituents independently selected from halogen, C 3~6 a carbon ring and a 3- to 6-membered heterocyclic ring, wherein the carbon ring and the 3- to 6-membered heterocyclic ring are each optionally substituted with one or more substituents independently selected from halogen, C 1~4 alkyl, and C 1~4 haloalkyl. C 3~6 a carbon ring and a 3- to 6-membered heterocyclic ring, wherein each of them is optionally substituted with one or more substituents independently selected from halogen, C 1~6 alkyl, C 1~6 haloalkyl, -OR 18 、 -SR 18 、 -N(R 18 ) 2 、 -C(O)R 18 、 -NO 2 、 =O、 =S、 =NR 18 、 -N 3 、 and -CN.
[0253] In some embodiments, for the compound or salt of formula (I), (I-a), (II) or (III), C is a 5- to 10-membered heterocyclic ring, and each of them is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 、 -SR 18 、 -N(R 18 ) 2 、 -C(O)R 18 、 -C(O)OR 18 、 -OC(O)R 18 、 -OC(O)N(R 18 ) 2 、 -C(O)N(R 18 ) 2 、 -N(R 18 )C(O)R 18 、 -N(R 18 )C(O)OR 18, -N(R 18 )C(O)N(R 18 ) 2 , , -N(R 18 )C(S)N(R 18 ) 2 , -N(R 18 )S(O) 2 (R 18 ), -S(O)R 18 , -S(O) 2 R 18 , -S(O) 2 N(R 18 ) 2 , -NO 2 , =O, =S, =NR 18 , -N 3 , and -CN, C 1~6 alkyl, C 2~6 alkenyl, and C 2~6 alkynyl, each of which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 , -SR 18 , -N(R 18 ) 2 , -C(O)R 18 , -C(O)OR 18 , -OC(O)R 18 , , -OC(O)N(R 18 ) 2 , -C(O)N(R 18 ) 2 , -N(R 18 )C(O)R 18 , -N(R 18 )C(O)OR 18 , , -N(R 18 )C(O)N(R 18 ) 2 , -N(R 18 )C(S)N(R 18 ) 2 , -N(R 18 )S(O) 2 (R 18 ), -S(O)R 18 , , -S(O) 2 R 18, -S(O) 2 N(R 18 ) 2 , -NO 2 , =O, =S, =NR 18 , -N 3 , -CN, C 3~6 a carbon ring and a 3- to 6-membered heterocyclic ring, wherein the C 3~6 carbon ring and the 3- to 6-membered heterocyclic ring are each optionally substituted with one or more substituents independently selected from halogen, C 1~4 alkyl, and C 1~4 haloalkyl. C 3~6 a carbon ring and a 3- to 6-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from halogen, C 1~6 alkyl, C 1~6 haloalkyl, -OR 18 , -SR 18 , -N(R 18 ) 2 , -C(O)R 18 , -NO 2 , =O, =S, =NR 18 , -N 3 , and -CN.
[0254] In some embodiments, for the compound or salt of formula (I), (I-a), (II) or (III), C is C 5~10 selected from a carbon ring and a 5- to 10-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from: halogen, -OR 18 , -SR 18 , -N(R 18 ) 2 , -C(O)R 18 , -C(O)OR 18 , -OC(O)R 18 , -C(O)N(R 18 ) 2 , -N(R 18 )C(O)R 18 , -N(R 18 )S(O) 2 (R 18 ), -S(O)R 18 , -S(O) 2 R18 、 -S(O) 2 N(R 18 ) 2 、 -NO 2 、 =O, and -CN, C 1~6 alkyl, C 2~6 alkenyl, and C 2~6 alkynyl, each of which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 、 -SR 18 、 -N(R 18 ) 2 、 -C(O)R 18 、 -C(O)OR 18 、 -OC(O)R 18 、 -C(O)N(R 18 ) 2 、 -N(R 18 )C(O)R 18 、 -N(R 18 )S(O) 2 (R 18 )、 -S(O)R 18 、 -S(O) 2 R 18 、 -S(O) 2 N(R 18 ) 2 、 -NO 2 、 =O、 -CN、 C 3~6 carbocyclic and 3- to 6-membered heterocyclic rings, where C 3~6 carbocyclic and 3- to 6-membered heterocyclic rings are optionally substituted with one or more substituents independently selected from halogen, C 1~4 alkyl, and C 1~4 haloalkyl, and C 3~6 carbocyclic and 3- to 6-membered heterocyclic rings, each of which is optionally substituted with one or more substituents independently selected from halogen, C 1~6 alkyl, C 1~6 haloalkyl, -OR 18 、 -N(R 18 ) 2 、 -C(O)R 18 、 -NO 2 、 =O, and -CN.
[0255] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), C is selected from: C 5~10 a carbocyclic ring and a 5- to 10-membered heterocyclic ring, halogen, -OR 18 , -SR 18 , -N(R 18 ) 2 , -C(O)R 18 , -C(O)OR 18 , -C(O)N(R 18 ) 2 , -S(O)R 18 , -S(O) 2 R 18 , -NO 2 , =O, =S, and -CN, C 1~6 alkyl and C 2~6 alkenyl, each of which is optionally substituted with one or more substituents independently selected from: halogen, -OR 18 , -SR 18 , -N(R 18 ) 2 , -C(O)R 18 , , -C(O)OR 18 , -OC(O)R 18 , -OC(O)N(R 18 ) 2 , -C(O)N(R 18 ) 2 , -N(R 18 )C(O)R 18 , -N(R 18 )C(O)OR 18 , , -N(R 18 )C(O)N(R 18 ) 2 , -N(R 18 )C(S)N(R 18 ) 2 , -N(R 18 )S(O) 2 (R 18 ), -S(O) 2 N(R 18 ) 2 , -NO 2, =O, =S, -CN, and a 3- to 6-membered heterocyclic ring, optionally substituted with one or more substituents independently selected from the following: halogen, C 1~4 alkyl, and C 1~4 haloalkyl, C 3~6 a carbocyclic ring and a 3- to 6-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from: 1~6 halogen, C 1~6 alkyl, and C
[0256] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), C is C 5~10 selected from a carbocyclic ring and a 5- to 10-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from: halogen, -OR 18 , -N(R 18 ) 2 , -C(O)R 18 , -C(O)OR 18 , -OC(O)R 18 , -C(O)N(R 18 ) 2 , -N(R 18 )C(O)R 18 , -N(R 18 )S(O) 2 (R 18 ), -S(O) 2 N(R 18 ) 2 , =O, and -CN, C 1~6 alkyl, C 2~6 alkenyl, and C 2~6 alkynyl, each of which is optionally substituted with one or more substituents independently selected from: halogen, -OR 18 , -N(R 18 ) 2 , -C(O)OR 18 , -OC(O)R 18 , -C(O)N(R 18 ) 2 , -N(R18 )C(O)R 18 、 -N(R 18 )S(O) 2 (R 18 )、 -S(O) 2 N(R 18 ) 2 、 =O、 -CN、 C 3~6 a carbon ring and a 3- to 6-membered heterocyclic ring, provided that C 3~6 the carbon ring and the 3- to 6-membered heterocyclic ring are each optionally substituted with one or more substituents independently selected from halogen, C 1~4 alkyl, and C 1~4 haloalkyl, and, C 3~6 a carbon ring and a 3- to 6-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from halogen, C 1~6 alkyl, C 1~6 haloalkyl, -OR 18 、 -N(R 18 ) 2 、 -C(O)R 18 、 =O, and -CN.
[0257] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), C is selected from a carbon ring and a 5- to 10-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from: 5~10 halogen, -OR 、 -N(R 18 、 =O, and -CN, 18 ) 2 、 =O, and -CN, C 1~6 alkyl and C 2~6 alkenyl, each of which is optionally substituted with one or more substituents independently selected from: halogen, -OR 18 、 -N(R 18 ) 2 、 =O, -CN, and a 3- to 6-membered heterocyclic ring optionally substituted with one or more substituents independently selected from halogen, C 1~4 alkyl, and C 1~4 haloalkyl, and, C 3~6 A carbon ring and a 3- to 6-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from halogen, C 1~6 alkyl, and C 1~6 haloalkyl.
[0258] In some embodiments, for the compound or salt of formula (I), (I-a), (II) or (III), C is selected from 5- to 10-membered heterocyclic rings optionally substituted with one or more substituents independently selected from the following: -OR 18 , -N(R 18 ), 2 , and =O, C 1~6 alkyl and C 2~6 alkenyl, each of which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 , -N(R 18 ), 2 , and a 3- to 6-membered heterocyclic ring optionally substituted with one or more substituents independently selected from halogen, and C 3~6 a carbon ring and a 3- to 6-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from halogen, C 1~6 alkyl, and C 1~6 haloalkyl.
[0259] In some embodiments, for the compound or salt of formula (I), (I-a), (II) or (III), R 18 is independently, at each occurrence, hydrogen, C 1~6 alkyl, C 1~6 haloalkyl, and C 1~6 hydroxyalkyl. In some embodiments, R 18 is independently, at each occurrence, hydrogen, C 1~6 alkyl, and C 1~6 haloalkyl. In some embodiments, R 18 is independently, at each occurrence, hydrogen and C 1~6is selected from alkyl. In some embodiments, R 18 is, independently for each occurrence, C 1~6 selected from alkyl. In some embodiments, each R 18 is hydrogen.
[0260] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), C is C 5~10 selected from a carbocyclic ring and a 5- to 10-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from the following: halogen, =O, -N(CH 3 ) 2、 C 1~6 alkyl, C 2~6 alkenyl, C 1~6 haloalkyl, -O-C 1~6 alkyl, -O-C 1~6 haloalkyl,
[0261]
Chemical formula
[0262] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), C is C 3~6 selected from a monocyclic carbocyclic ring, a 5- to 6-membered monocyclic heterocyclic ring, and a 7- to 10-membered bicyclic heterocyclic ring, each of which is optionally substituted. In some embodiments, C is selected from phenyl, a 5- to 6-membered monocyclic heterocyclic ring, and a 7- to 10-membered bicyclic heterocyclic ring, each of which is optionally substituted. In some embodiments, C is selected from phenyl, a 5- to 6-membered monocyclic heterocyclic ring, and a 7- to 10-membered bicyclic heterocyclic ring, each of which is optionally substituted. In some embodiments, C is C 3~6 selected from a monocyclic carbocyclic ring and a 5- to 6-membered monocyclic heterocyclic ring, each of which is optionally substituted. In some embodiments, C is selected from phenyl and a 5- to 6-membered monocyclic heterocyclic ring, each of which is optionally substituted. In some embodiments, C is selected from a 7- to 10-membered bicyclic heterocyclic ring, each of which is optionally substituted.
[0263] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), C is selected from phenyl, pyridine, pyridin-2-one, pyrimidone, pyrimidinedione, pyrazine, pyridazin-3-one, isoquinoline, naphthyridine, phthalazine, naphthyridin-2-one, 5,6,7,8-tetrahydronaphthyridin-2-one, triazolo[1,5-a]pyrazine, imidazo[1,2-a]pyrazine, pyrazolo[1,5-a]pyrazine, pyrido[4,3-d]pyrimidine-2,4-dione, pyrido[3,4-d]pyrimidine-2,4-dione, quinazoline-2,4-dione, quinolin-2-one, 3,4-dihydroquinolin-2-one, isoindolin-1-one, and 1,3-dihydro-benzo[d]imidazol-2-one, each of which is optionally substituted. In some embodiments, C is selected from phenyl, pyridine, pyridin-2-one, pyrimidinedione, pyrazine, pyridazin-3-one, isoquinoline, naphthyridine, phthalazine, naphthyridin-2-one, 5,6,7,8-tetrahydronaphthyridin-2-one, triazolo[1,5-a]pyrazine, imidazo[1,2-a]pyrazine, pyrazolo[1,5-a]pyrazine, pyrido[4,3-d]pyrimidine-2,4-dione, pyrido[3,4-d]pyrimidine-2,4-dione, quinazoline-2,4-dione, quinolin-2-one, 3,4-dihydroquinolin-2-one, isoindolin-1-one, and 1,3-dihydro-benzo[d]imidazol-2-one, each of which is optionally substituted. In some embodiments, C is selected from phenyl, pyridine, pyridin-2-one, pyrimidinedione, pyrazine, and pyridazin-3-one, each of which is optionally substituted.In some embodiments, C is selected from isoquinoline, naphthyridine, phthalazine, naphthyridin-2-one, 5,6,7,8-tetrahydronaphthyridin-2-one, triazolo[1,5-a]pyrazine, imidazo[1,2-a]pyrazine, pyrazolo[1,5-a]pyrazine, pyrido[4,3-d]pyrimidine-2,4-dione, pyrido[3,4-d]pyrimidine-2,4-dione, quinazoline-2,4-dione, quinolin-2-one, 3,4-dihydroquinolin-2-one, isoindolin-1-one, and 1,3-dihydro-benzo[d]imidazol-2-one, each of which is optionally substituted.
[0264] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), the optional substituent on C is independently, at each occurrence, selected from: halogen, -OR 18 , -SR 18 , -N(R 18 ) 2 , -C(O)R 18 , -C(O)OR 18 , -OC(O)R 18 , -OC(O)N(R 18 ) 2 , -C(O)N(R 18 ) 2 , -N(R 18 )C(O)R 18 , -N(R 18 )C(O)OR 18 , -N(R 18 )C(O)N(R 18 ) 2 , -N(R 18 )C(S)N(R 18 ) 2 , -N(R 18 )S(O) 2 (R 18 ), -S(O)R 18 , -S(O) 2 R 18 , -S(O) 2 N(R 18 ) 2 , -NO 2, =O, =S, =NR 18 , -N 3 , and -CN, C 1~6 alkyl, C 2~6 alkenyl, and C 2~6 alkynyl, each of which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 , -SR 18 , -N(R 18 ) 2 , -C(O)R 18 , -C(O)OR 18 , -OC(O)R 18 , -OC(O)N(R 18 ) 2 , -C(O)N(R 18 ) 2 , -N(R 18 )C(O)R 18 , -N(R 18 )C(O)OR 18 , -N(R 18 )C(O)N(R 18 ) 2 , -N(R 18 )C(S)N(R 18 ) 2 , -N(R 18 )S(O) 2 (R 18 ), -S(O)R 18 , -S(O) 2 R 18 , -S(O) 2 N(R 18 ) 2 , -NO 2 , =O, =S, =NR 18 , -N 3 , -CN, C 3~6 carbocyclic and 3- to 6-membered heterocyclic rings, where C 3~6 the carbocyclic and 3- to 6-membered heterocyclic rings are optionally substituted with one or more substituents independently selected from halogen, C 1~4 alkyl, and C 1~4 haloalkyl, and C3~6 A carbon ring and a 3- to 6-membered heterocyclic ring, each of which is independently selected from halogen, C 1~6 alkyl, C 1~6 haloalkyl, -OR 18 , -SR 18 , -N(R 18 ), -C(O)R 2 , -C(O)OR 18 , -NO 2 , =O, =S, =NR 18 , -N 3 , and -CN, and is optionally substituted with one or more substituents independently selected therefrom.
[0265] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), the optional substituent on C is independently, at each occurrence, selected from: halogen, -OR 18 , -SR 18 , -N(R 18 ), -C(O)R 2 , -C(O)OR 18 , -C(O)N(R 18 ), -S(O)R 18 , 2 , -S(O) 18 R , -NO 2 , =O, =S, and -CN, 18 C 2 alkyl and C alkenyl, each of which is optionally substituted with one or more substituents independently selected from: halogen, -OR 1~6 , -SR 2~6 , -N(R 18 ), -C(O)R 18 , , -C(O)OR 18 , -C(O)R 2 , , -C(O)OR 18 , -OC(O)R 18 , -OC(O)N(R 18 ), -C(O)N(R 2 ), -N(R 18 ), -N(R 2 ), -N(R 18 ), -N(R 18 ), -N(R18 )C(O)OR 18 、 -N(R 18 )C(O)N(R 18 ) 2 、-N(R 18 )C(S)N(R 18 ) 2 、-N(R 18 )S(O) 2 (R 18 )、-S(O) 2 N(R 18 ) 2 、-NO 2 、=O、=S、 -CN, and a 3- to 6-membered heterocyclic ring optionally substituted with one or more substituents independently selected from the following: halogen, C 1~4 alkyl, and C 1~4 haloalkyl, C 3~6 a carbocyclic ring and a 3- to 6-membered heterocyclic ring, each optionally substituted with one or more substituents independently selected from halogen, C 1~6 alkyl, and C 1~6 haloalkyl.
[0266] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), any optional substituent on C is independently, at each occurrence, selected from: halogen, -OR 18 , -SR 18 , -N(R 18 ) 2 , -C(O)R 18 , -C(O)OR 18 , -OC(O)R 18 , -C(O)N(R 18 ) 2 , -N(R 18 )C(O)R 18 , -N(R 18 )S(O) 2 (R 18 ), -S(O)R 18 , -S(O) 2 R 18 , -S(O) 2 N(R 18 )2 , -NO 2 , =O, and -CN, C 1~6 alkyl, C 2~6 alkenyl, and C 2~6 alkynyl, each of which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 , -SR 18 , -N(R 18 ) 2 , -C(O)R 18 , -C(O)OR 18 , -OC(O)R 18 , -C(O)N(R 18 ) 2 , -N(R 18 )C(O)R 18 , -N(R 18 )S(O) 2 (R 18 ), -S(O)R 18 , -S(O) 2 R 18 , -S(O) 2 N(R 18 ) 2 , -NO 2 , =O, -CN, C 3~6 carbocyclic ring and 3- to 6-membered heterocyclic ring, where C 3~6 the carbocyclic ring and 3- to 6-membered heterocyclic ring are optionally substituted with one or more substituents independently selected from halogen, C 1~4 alkyl, and C 1~4 haloalkyl, and C 3~6 carbocyclic ring and 3- to 6-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from halogen, C 1~6 alkyl, C 1~6 haloalkyl, -OR 18 , -N(R 18 ) 2 , -C(O)R 18 , -NO 2 , =O, and -CN.
[0267] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), any optional substituent on C is independently, at each occurrence, selected from the following: halogen, -OR 18 , -N(R 18 ) 2 , =O, and -CN, C 1~6 alkyl and C 2~6 alkenyl, each of which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 , -N(R 18 ) 2 , =O, -CN, and a 3- to 6-membered heterocyclic ring optionally substituted with one or more substituents independently selected from halogen, C 1~4 alkyl, and C 1~4 haloalkyl, and C 3~6 a carbocyclic ring and a 3- to 6-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from halogen, C 1~6 alkyl, and C 1~6 haloalkyl.
[0268] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), any optional substituent on C is independently, at each occurrence, selected from the following: -OR 18 , -N(R 18 ) 2 , and =O, C 1~6 alkyl and C 2~6 alkenyl, each of which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 , -N(R 18 ) 2 , and a 3- to 6-membered heterocyclic ring optionally substituted with one or more substituents independently selected from halogen, C 3~6 a carbocyclic ring and a 3- to 6-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from halogen, C 1~6Alkyl, and C 1~6 Optionally substituted with one or more substituents independently selected from haloalkyl.
[0269] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), the optional substituent on C is independently, each occurrence, selected from: halogen, =O, -N(CH 3 ) 2、 C 1~6 alkyl, C 2~6 alkenyl, C 1~6 haloalkyl, -O-C 1~6 alkyl, -O-C 1~6 haloalkyl,
[0270]
Chemical formula
[0271] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), C is selected from phenyl, pyridine, pyridin-2-one, pyrimidinedione, pyrazine, pyridazin-3-one, isoquinoline, naphthyridine, phthalazine, naphthyridin-2-one, 5,6,7,8-tetrahydronaphthyridin-2-one, triazolo[1,5-a]pyrazine, imidazo[1,2-a]pyrazine, pyrazolo[1,5-a]pyrazine, pyrido[4,3-d]pyrimidine-2,4-dione, pyrido[3,4-d]pyrimidine-2,4-dione, quinazoline-2,4-dione, quinolin-2-one, 3,4-dihydroquinolin-2-one, isoindolin-1-one, and 1,3-dihydro-benzo[d]imidazol-2-one, each of which is optionally substituted with one or more substituents independently selected from: halogen, -OR 18 -SR 18 -N(R 18 ) 2 -C(O)R 18 -C(O)OR 18 -OC(O)R 18 、 -OC(O)N(R 18 ) 2 , -C(O)N(R 18 ) 2 , -N(R 18 )C(O)R 18 , -N(R 18 )C(O)OR 18 , -N(R 18 )C(O)N(R 18 ) 2 , -N(R 18 )C(S)N(R 18 ) 2 , -N(R 18 )S(O) 2 (R 18 ), -S(O)R 18 , -S(O) 2 R 18 , -S(O) 2 N(R 18 ) 2 , -NO 2 , =O, =S, =NR 18 , -N 3 , and -CN, C 1~6 Alkyl, C 2~6 Alkenyl, and C 2~6 Alkynyl, each of which is optionally substituted with one or more substituents independently selected from: Halogen, -OR 18 , -SR 18 , -N(R 18 ) 2 , -C(O)R 18 , -C(O)OR 18 , -OC(O)R 18 , -OC(O)N(R 18 ) 2 , -C(O)N(R 18 ) 2 , -N(R 18 )C(O)R 18 , -N(R 18 )C(O)OR 18 , -N(R 18 )C(O)N(R 18 ) 2 , -N(R 18C(S)N(R 18 ) 2 、-N(R 18 )S(O) 2 (R 18 )、-S(O)R 18 、 -S(O) 2 R 18 、-S(O) 2 N(R 18 ) 2 、-NO 2 、=O、=S、=NR 18 、-N 3 、-CN、C 3~6 A carbon ring and a 3- to 6-membered heterocyclic ring, C 3~6 wherein the carbon ring and the 3- to 6-membered heterocyclic ring are each optionally substituted with one or more substituents independently selected from halogen, C 1~4 alkyl, and C 1~4 haloalkyl, and C 3~6 A carbon ring and a 3- to 6-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from halogen, C 1~6 alkyl, C 1~6 haloalkyl, -OR 18 、-SR 18 、-N(R 18 ) 2 、-C(O)R 18 、-NO 2 、=O、=S、=NR 18 、-N 3 、and -CN.
[0272] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), C is selected from phenyl, pyridine, pyridin-2-one, pyrimidinedione, pyrazine, pyridazin-3-one, isoquinoline, naphthyridine, phthalazine, naphthyridin-2-one, 5,6,7,8-tetrahydronaphthyridin-2-one, triazolo[1,5-a]pyrazine, imidazo[1,2-a]pyrazine, pyrazolo[1,5-a]pyrazine, pyrido[4,3-d]pyrimidine-2,4-dione, pyrido[3,4-d]pyrimidine-2,4-dione, quinazoline-2,4-dione, quinolin-2-one, 3,4-dihydroquinolin-2-one, isoindolin-1-one, and 1,3-dihydro-benzo[d]imidazol-2-one, each of which is optionally substituted with one or more substituents independently selected from: halogen, -OR 18 , -N(R 18 ) 2 , -C(O)R 18 , -C(O)OR 18 , -OC(O)R 18 , -C(O)N(R 18 ) 2 , -N(R 18 )C(O)R 18 , -N(R 18 )S(O) 2 (R 18 ), -S(O) 2 N(R 18 ) 2 , =O, and -CN, C 1~6 alkyl, C 2~6 alkenyl, and C 2~6 alkynyl, each of which is optionally substituted with one or more substituents independently selected from: halogen, -OR 18 , -N(R 18 ) 2 , -C(O)OR 18 , -OC(O)R 18 , -C(O)N(R 18 ) 2 , -N(R 18 )C(O)R 18 , -N(R18 )S(O) 2 (R 18 )、-S(O) 2 N(R 18 ) 2 、=O、-CN、C 3~6 a carbon ring and a 3- to 6-membered heterocyclic ring, provided that C 3~6 the carbon ring and the 3- to 6-membered heterocyclic ring are each optionally substituted with one or more substituents independently selected from halogen, C 1~4 alkyl, and C 1~4 haloalkyl; and C 3~6 a carbon ring and a 3- to 6-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from halogen, C 1~6 alkyl, C 1~6 haloalkyl, -OR 18 、-N(R 18 ) 2 、-C(O)R 18 、=O、and -CN.
[0273] In some embodiments, for a compound or salt of formula (I), (I-a), (II), or (III), C is selected from phenyl, pyridine, pyridin-2-one, pyrimidinedione, pyrazine, pyridazin-3-one, isoquinoline, naphthyridine, phthalazine, naphthyridin-2-one, 5,6,7,8-tetrahydronaphthyridin-2-one, triazolo[1,5-a]pyrazine, imidazo[1,2-a]pyrazine, pyrazolo[1,5-a]pyrazine, pyrido[4,3-d]pyrimidine-2,4-dione, pyrido[3,4-d]pyrimidine-2,4-dione, quinazoline-2,4-dione, quinolin-2-one, 3,4-dihydroquinolin-2-one, isoindolin-1-one, and 1,3-dihydro-benzo[d]imidazol-2-one, each of which is optionally substituted with one or more substituents independently selected from: -OR 18 、-N(R 18 ) 2 、and =O, C 1~6 alkyl and C 2~6An alkenyl, each of which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 , -N(R 18 ), 2 , and a 3- to 6-membered heterocyclic ring optionally substituted with one or more substituents independently selected from halogen, and C 3~6 a carbocyclic ring and a 3- to 6-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from halogen, C 1~6 alkyl, and C 1~6 haloalkyl.
[0274] In some embodiments, for the compound or salt of formula (I), (I-a), (II) or (III), C is selected from phenyl, pyridine, pyridin-2-one, pyrimidinedione, pyrazine, pyridazin-3-one, isoquinoline, naphthyridine, phthalazine, naphthyridin-2-one, 5,6,7,8-tetrahydronaphthyridin-2-one, triazolo[1,5-a]pyrazine, imidazo[1,2-a]pyrazine, pyrazolo[1,5-a]pyrazine, pyrido[4,3-d]pyrimidine-2,4-dione, pyrido[3,4-d]pyrimidine-2,4-dione, quinazoline-2,4-dione, quinolin-2-one, 3,4-dihydroquinolin-2-one, isoindolin-1-one, and 1,3-dihydro-benzo[d]imidazol-2-one, each of which is optionally substituted with one or more substituents independently selected from the following: halogen, =O, -N(CH 3 ), 2、 C 1~6 alkyl, C 2~6 alkenyl, C 1~6 haloalkyl, -O-C 1~6 alkyl, -O-C 1~6 haloalkyl,
[0275]
Chemical formula
[0276] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), C is C 3~6 selected from monocyclic carbocycles and 5- to 6-membered monocyclic heterocycles, each of which is optionally substituted with one or more substituents independently selected from: halogen, -OR 18 -SR 18 -N(R 18 ) 2 -C(O)R 18 -C(O)OR 18 -OC(O)R 18 -OC(O)N(R 18 ) 2 -C(O)N(R 18 ) 2 -N(R 18 )C(O)R 18 -N(R 18 )C(O)OR 18 -N(R 18 )C(O)N(R 18 ) 2 -N(R 18 )C(S)N(R 18 ) 2 -N(R 18 )S(O) 2 (R 18 )-S(O)R 18 -S(O) 2 R 18 -S(O) 2 N(R 18 ) 2 -NO 2 =O, =S, =NR 18 -N 3 and -CN, C 1~6 alkyl, C 2~6 alkenyl, and C 2~6 alkynyl, each of which is optionally substituted with one or more substituents independently selected from: halogen, -OR 18 -SR 18 -N(R 18 ) 2 -C(O)R 18 、 -C(O)OR 18 、 -OC(O)R 18 、 -OC(O)N(R 18 ) 2 、 -C(O)N(R 18 ) 2 、 -N(R 18 )C(O)R 18 、 -N(R 18 )C(O)OR 18 、 -N(R 18 )C(O)N(R 18 ) 2 、 -N(R 18 )C(S)N(R 18 ) 2 、 -N(R 18 )S(O) 2 (R 18 、 -S(O)R 18 、 -S(O) 2 R 18 、 -S(O) 2 N(R 18 ) 2 、 -NO 2 、 =O、 =S、 =NR 18 、 -N 3 、 -CN、 C 3~6 carbon rings and 3- to 6-membered heterocyclic rings, where C 3~6 the carbon rings and 3- to 6-membered heterocyclic rings are each optionally substituted with one or more substituents independently selected from halogen, C 1~4 alkyl, and C 1~4 haloalkyl, and C 3~6 carbon rings and 3- to 6-membered heterocyclic rings, where each of them is independently selected from halogen, C 1~6 alkyl, C 1~6 haloalkyl, -OR 18 、 -SR 18 、 -N(R 18 ) 2 、 -C(O)R 18 、 -NO 2 、 =O、 =S、 =NR 18 、 -N 3 、 and -CN and are optionally substituted with one or more substituents.
[0277] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), C is C 3~6 a monocyclic carbocyclic ring and 5- to 6-membered a monocyclic heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from: halogen, -OR 18 , -N(R 18 ) 2 , -C(O)R 18 , -C(O)OR 18 , -OC(O)R 18 , -C(O)N(R 18 ) 2 , -N(R 18 )C(O)R 18 , -N(R 18 )S(O) 2 (R 18 ), -S(O) 2 N(R 18 ) 2 , =O, and -CN, C 1~6 alkyl, C 2~6 alkenyl, and C 2~6 alkynyl, each of which is optionally substituted with one or more substituents independently selected from: halogen, -OR 18 , -N(R 18 ) 2 , -C(O)OR 18 , -OC(O)R 18 , -C(O)N(R 18 ) 2 , -N(R 18 )C(O)R 18 , -N(R 18 )S(O) 2 (R 18 ), -S(O) 2 N(R 18 ) 2 , =O, -CN, C 3~6 a carbocyclic ring and a 3- to 6-membered heterocyclic ring, C 3~6 the carbocyclic ring and the 3- to 6-membered heterocyclic ring are halogen, C 1~4 alkyl, and C 1~4Optionally substituted with one or more substituents independently selected from haloalkyl, and C 3~6 A carbocyclic ring and a 3- to 6-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from halogen, C 1~6 alkyl, C 1~6 haloalkyl, -OR 18 , -N(R 18 ) 2 , -C(O)R 18 , =O, and -CN.
[0278] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), C is a C 3~6 monocyclic carbocyclic ring and a 5- to 6-membered monocyclic heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from the following: -OR 18 , -N(R 18 ) 2 , and =O, C 1~6 alkyl and C 2~6 alkenyl, each of which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 , -N(R 18 ) 2 , and a 3- to 6-membered heterocyclic ring optionally substituted with one or more substituents independently selected from halogen, and C 3~6 A carbocyclic ring and a 3- to 6-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from halogen, C 1~6 alkyl, and C 1~6 haloalkyl.
[0279] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), C is a C 3~6 monocyclic carbocyclic ring and a 5- to 6-membered Selected from monocyclic heterocycles, each of which is optionally substituted with one or more substituents independently selected from the following: halogen, =O, -N(CH 3 ) 2、 C 1~6 alkyl, C 2~6 alkenyl, C 1~6 haloalkyl, -O-C 1~6 alkyl, -O-C 1~6 haloalkyl,
[0280]
Chemical formula
[0281] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), C is selected from phenyl, pyridine, pyridin-2-one, pyrimidinedione, pyrazine, and pyridazin-3-one, each of which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 , -SR 18 , -N(R 18 ) 2 , -C(O)R 18 , -C(O)OR 18 , -OC(O)R 18 , -OC(O)N(R 18 ) 2 , -C(O)N(R 18 ) 2 , -N(R 18 )C(O)R 18 , -N(R 18 )C(O)OR 18 , -N(R 18 )C(O)N(R 18 ) 2 , , -N(R 18 )C(S)N(R 18 ) 2 , -N(R 18 )S(O) 2 (R 18 ), -S(O)R 18 , -S(O) 2 R18 , -S(O) 2 N(R 18 ) 2 , -NO 2 , =O, =S, =NR 18 , -N 3 , and -CN, C 1~6 Alkyl, C 2~6 Alkenyl, and C 2~6 Alkynyl, each of which is optionally substituted with one or more substituents independently selected from: Halogen, -OR 18 , -SR 18 , -N(R 18 ) 2 , -C(O)R 18 , -C(O)OR 18 , -OC(O)R 18 , -OC(O)N(R 18 ) 2 , -C(O)N(R 18 ) 2 , -N(R 18 )C(O)R 18 , -N(R 18 )C(O)OR 18 , -N(R 18 )C(O)N(R 18 ) 2 , -N(R 18 )C(S)N(R 18 ) 2 , -N(R 18 )S(O) 2 (R 18 ), -S(O)R 18 , -S(O) 2 R 18 , -S(O) 2 N(R 18 ) 2 , -NO 2 , =O, =S, =NR 18 , -N 3 , -CN,C 3~6 Carbocycles and 3- to 6-membered heterocycles, C 3~6 The carbocyclic ring and the 3- to 6-membered heterocyclic ring are 1~4 Alkyl, and C1~4 Optionally substituted with one or more substituents independently selected from haloalkyl, and C 3~6 A carbocyclic ring and a 3- to 6-membered heterocyclic ring, each of which is independently selected from halogen, C 1~6 alkyl, C 1~6 haloalkyl, -OR 18 , -SR 18 , -N(R 18 ) 2 , -C(O)R 18 , -NO 2 , =O, =S, =NR 18 , -N 3 , and -CN, and is optionally substituted with one or more substituents independently selected therefrom.
[0282] In some embodiments, for the compounds or salts of formula (I), (I-a), (II) or (III), C is selected from phenyl, pyridine, pyridin-2-one, pyrimidinedione, pyrazine, and pyridazin-3-one, each of which is optionally substituted with one or more substituents independently selected from: halogen, -OR 18 , -N(R 18 ) 2 , -C(O)R 18 , -C(O)OR 18 , -OC(O)R 18 , -C(O)N(R 18 ) 2 , -N(R 18 )C(O)R 18 , -N(R 18 )S(O) 2 (R 18 ), -S(O) 2 N(R 18 ) 2 , =O, and -CN, C 1~6 alkyl, C 2~6 alkenyl, and C 2~6 alkynyl, each of which is optionally substituted with one or more substituents independently selected from: halogen, -OR 18 , -N(R 18 )2 、 -C(O)OR 18 、 -OC(O)R 18 、 -C(O)N(R 18 ) 2 、 -N(R 18 )C(O)R 18 、 -N(R 18 )S(O) 2 (R 18 )、 -S(O) 2 N(R 18 ) 2 、 =O、 -CN、 C 3~6 a carbon ring and a 3- to 6-membered heterocyclic ring, provided that C 3~6 the carbon ring and the 3- to 6-membered heterocyclic ring are each optionally substituted with one or more substituents independently selected from halogen, C 1~4 alkyl, and C 1~4 haloalkyl, and C 3~6 a carbon ring and a 3- to 6-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from halogen, C 1~6 alkyl, C 1~6 haloalkyl, -OR 18 、 -N(R 18 ) 2 、 -C(O)R 18 、 =O, and -CN.
[0283] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), C is selected from phenyl, pyridine, pyridin-2-one, pyrimidinedione, pyrazine, and pyridazin-3-one, each of which is optionally substituted with one or more substituents independently selected from: -OR 18 、 -N(R 18 ) 2 、 and =O, C 1~6 alkyl and C 2~6 alkenyl, each of which is optionally substituted with one or more substituents independently selected from: halogen, -OR 18 、 -N(R 18 ) 2and a 3- to 6-membered heterocyclic ring optionally substituted with one or more substituents independently selected from halogen, and C 3~6 a carbocyclic ring and a 3- to 6-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from halogen, C 1~6 alkyl, and C 1~6 haloalkyl.
[0284] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), C is selected from phenyl, pyridine, pyridin-2-one, pyrimidinedione, pyrazine, and pyridazin-3-one, each of which is optionally substituted with one or more substituents independently selected from the following: halogen, =O, -N(CH 3 ) 2、 C 1~6 alkyl, C 2~6 alkenyl, C 1~6 haloalkyl, -O-C 1~6 alkyl, -O-C 1~6 haloalkyl,
[0285]
Chemical formula
[0286] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), C is selected from 7- to 10-membered bicyclic heterocyclic rings, each of which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 、-SR 18 、-N(R 18 ) 2 、-C(O)R 18 、-C(O)OR 18 、-OC(O)R 18 、 -OC(O)N(R 18 ) 2 、-C(O)N(R 18 ) 2 、-N(R 18)C(O)R 18 , -N(R 18 )C(O)OR 18 , -N(R 18 )C(O)N(R 18 ) 2 , -N(R 18 )C(S)N(R 18 ) 2 , -N(R 18 )S(O) 2 (R 18 ), -S(O)R 18 , -S(O) 2 R 18 , -S(O) 2 N(R 18 ) 2 , -NO 2 , =O, =S, =NR 18 , -N 3 , and -CN, C 1~6 Alkyl, C 2~6 Alkenyl, and C 2~6 Alkynyl, each of which is optionally substituted with one or more substituents independently selected from: Halogen, -OR 18 , -SR 18 , -N(R 18 ) 2 , -C(O)R 18 , -C(O)OR 18 , -OC(O)R 18 , -OC(O)N(R 18 ) 2 , -C(O)N(R 18 ) 2 , -N(R 18 )C(O)R 18 , -N(R 18 )C(O)OR 18 , -N(R 18 )C(O)N(R 18 ) 2 , -N(R 18 )C(S)N(R 18 ) 2 , -N(R 18 )S(O) 2 (R 18 ), -S(O)R18 , -S(O) 2 R 18 、-S(O) 2 N(R 18 ) 2 、-NO 2 、=O、=S、=NR 18 、-N 3 、-CN、C 3~6 a carbon ring and a 3- to 6-membered heterocyclic ring, wherein C 3~6 the carbon ring and the 3- to 6-membered heterocyclic ring are each optionally substituted with one or more substituents independently selected from halogen, C 1~4 alkyl, and C 1~4 haloalkyl, and C 3~6 a carbon ring and a 3- to 6-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from halogen, C 1~6 alkyl, C 1~6 haloalkyl, -OR 18 、-SR 18 、-N(R 18 ) 2 、-C(O)R 18 、-NO 2 、=O、=S、=NR 18 、-N 3 、and -CN.
[0287] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), C is selected from 7- to 10-membered bicyclic heterocyclic rings, each of which is optionally substituted with one or more substituents independently selected from: halogen, -OR 18 、-N(R 18 ) 2 、-C(O)R 18 、-C(O)OR 18 、-OC(O)R 18 、-C(O)N(R 18 ) 2 、-N(R 18 )C(O)R 18 、-N(R 18 )S(O) 2 (R 18)、 -S(O) 2 N(R 18 ) 2 、 =O、 and -CN, C 1~6 alkyl, C 2~6 alkenyl, and C 2~6 alkynyl, each of which is optionally substituted with one or more substituents independently selected from: halogen, -OR 18 、 -N(R 18 ) 2 、 -C(O)OR 18 、 -OC(O)R 18 、 -C(O)N(R 18 ) 2 、 -N(R 18 )C(O)R 18 、 -N(R 18 )S(O) 2 (R 18 )、 -S(O) 2 N(R 18 ) 2 、 =O、 -CN、 C 3~6 carbocyclic ring and 3- to 6-membered heterocyclic ring, where C 3~6 carbocyclic ring and 3- to 6-membered heterocyclic ring are optionally substituted with one or more substituents independently selected from halogen, C 1~4 alkyl, and C 1~4 haloalkyl, and C 3~6 carbocyclic ring and 3- to 6-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from halogen, C 1~6 alkyl, C 1~6 haloalkyl, -OR 18 、 -N(R 18 ) 2 、 -C(O)R 18 、 =O、 and -CN.
[0288] In some embodiments, for the compound or salt of formula (I), (I-a), (II) or (III), C is selected from 7- to 10-membered bicyclic heterocyclic rings, each of which is optionally substituted with one or more substituents independently selected from: -OR18 , -N(R 18 ) 2 , and =O, C 1~6 alkyl and C 2~6 alkenyl, each of which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 , -N(R 18 ) 2 , and a 3- to 6-membered heterocyclic ring optionally substituted with one or more substituents independently selected from halogen, and C 3~6 carbocyclic ring and 3- to 6-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from halogen, C 1~6 alkyl, and C 1~6 haloalkyl.
[0289] In some embodiments, for the compound or salt of formula (I), (I-a), (II) or (III), C is selected from 7- to 10-membered bicyclic heterocyclic rings, each of which is optionally substituted with one or more substituents independently selected from the following: halogen, =O, -N(CH 3 ) 2、 C 1~6 alkyl, C 2~6 alkenyl, C 1~6 haloalkyl, -O-C 1~6 alkyl, -O-C 1~6 haloalkyl,
[0290]
Chemical formula
[0291] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), C is selected from isoquinoline, naphthyridine, phthalazine, naphthyridin-2-one, 5,6,7,8-tetrahydronaphthyridin-2-one, triazolo[1,5-a]pyrazine, imidazo[1,2-a]pyrazine, pyrazolo[1,5-a]pyrazine, pyrido[4,3-d]pyrimidine-2,4-dione, pyrido[3,4-d]pyrimidine-2,4-dione, quinazoline-2,4-dione, quinolin-2-one, 3,4-dihydroquinolin-2-one, isoindolin-1-one, and 1,3-dihydro-benzo[d]imidazol-2-one, each of which is optionally substituted with one or more substituents independently selected from: halogen, -OR 18 -SR 18 -N(R 18 ) 2 -C(O)R 18 -C(O)OR 18 -OC(O)R 18 -OC(O)N(R 18 ) 2 -C(O)N(R 18 ) 2 -N(R 18 )C(O)R 18 -N(R 18 )C(O)OR 18 -N(R 18 )C(O)N(R 18 ) 2 -N(R 18 )C(S)N(R 18 ) 2 -N(R 18 )S(O) 2 (R 18 )-S(O)R 18 -S(O) 2 R 18 -S(O) 2 N(R 18 ) 2 -NO 2 =O, =S, =NR 18 -N 3 and -CN, C1~6 alkyl, C 2~6 alkenyl, and C 2~6 alkynyl, each of which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 , -SR 18 , -N(R 18 ) 2 , -C(O)R 18 , -C(O)OR 18 , -OC(O)R 18 , -OC(O)N(R 18 ) 2 , -C(O)N(R 18 ) 2 , -N(R 18 )C(O)R 18 , -N(R 18 )C(O)OR 18 , -N(R 18 )C(O)N(R 18 ) 2 , -N(R 18 )C(S)N(R 18 ) 2 , -N(R 18 )S(O) 2 (R 18 ), -S(O)R 18 , -S(O) 2 R 18 , -S(O) 2 N(R 18 ) 2 , -NO 2 , =O, =S, =NR 18 , -N 3 , -CN, C 3~6 carbocyclic rings and 3- to 6-membered heterocyclic rings, where C 3~6 carbocyclic rings and 3- to 6-membered heterocyclic rings are optionally substituted with one or more substituents independently selected from halogen, C 1~4 alkyl, and C 1~4 haloalkyl, and C 3~6 carbocyclic rings and 3- to 6-membered heterocyclic rings, each of which is halogen, C 1~6 alkyl, C 1~6Haloalkyl, -OR 18 , -SR 18 , -N(R 18 ) 2 , -C(O)R 18 , -NO 2 , =O, =S, =NR 18 , -N 3 , and -CN, optionally substituted with one or more substituents independently selected from:
[0292] In some embodiments, for a compound or salt of formula (I), (I-a), (II) or (III), C is selected from isoquinoline, naphthyridine, phthalazine, naphthyridin-2-one, 5,6,7,8-tetrahydronaphthyridin-2-one, triazolo[1,5-a]pyrazine, imidazo[1,2-a]pyrazine, pyrazolo[1,5-a]pyrazine, pyri...
Claims
1. A compound of formula (I), 【Number】 or a pharmaceutically acceptable salt thereof: [wherein, A is 【Number】 selected from X 1 , X 2 , X 3 , and X 4 are each independently selected from N and C(R 2 ), and at least one of X 1 , X 2 , and X 3 is C(R 2 ), 【Number 1】 represents a single bond or a double bond, m is 0, 1, 2, or 3, n is 0, 1, or 2, p is 0, 1, 2, or 3, Each R 1 is independently halogen, -OR 11 , -SR 11 , -N(R 11 ), 2 , -C(O)R 11 , -C(O)OR 11 , -OC(O)R 11 , -OC(O)N(R 11 ) 2 、-C(O)N(R 11 ) 2 、-N(R 11 )C(O)R 11 、-N(R 11 )C(O)OR 11 、 -N(R 11 )(O)N(R 11 ) 2 、-N(R 11 )(S)N(R 11 ) 2 、-N(R 11 )(O) 2 (R 11 )、-S(O)R 11 、-S(O) 2 R 11 、-S(O) 2 N(R 11 ) 2 、-NO 2 、and -CN, C 1~6 alkyl, C 2~6 alkenyl, and C 2~6 alkynyl, each of which is optionally substituted by one or more substituents independently selected from halogen, -OR 11 , -SR 11 , -N(R 11 ), 2 =O, =S, and -CN, and is optionally substituted by one or more substituents independently selected from halogen, -OR C 3~6 a carbon ring and a 3- to 6-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from halogen, C 1~4 alkyl, C 1~4 haloalkyl, -OR 11 , -SR 11 , -N(R 11 ), 2 =O, =S, and -CN, and is selected from those optionally substituted with one or more substituents independently selected from the group consisting of Each R 2 is independently Hydrogen, halogen, -OR 12 , -SR 12 , -N(R 12 ), 2 , -C(O)R 12 , -C(O)OR 12 , -OC(O)R 12 , -OC(O)N(R 12 ), 2 , -C(O)N(R 12 ), 2 , -N(R 12 ),C(O)R 12 , -N(R 12 ),C(O)OR 12 , () 12 () 12 ) 2 () 12 () 12 ) 2 () 12 () 2 () 12 () 12 (O) 2 R 12 (O) 2 () 12 ) 2 -NO 2、 及び-CN、 C 1~6 alkyl, C 2~6 alkenyl, and C 2~6 alkynyl, each of which is optionally substituted by one or more substituents independently selected from halogen, -OR 12 , -SR 12 , -N(R 12 ), 2 =O, =S, and -CN, and C 3~6 a carbon ring and a 3- to 6-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from halogen, C 1~4 alkyl, C 1~4 haloalkyl, -OR 12 , -SR 12 , -N(R 12 ), 2 =O, =S, and -CN, and is selected from those optionally substituted with one or more substituents independently selected from the group consisting of R 3 is hydrogen or C 1~6 alkyl, and R 4a and R 4b are each independently Hydrogen, halogen, -OR 13 , -SR 13 , -N(R 13 ), 2 , -C(O)R 13 , -NO 2 , -CN, and C 1~6 alkyl optionally substituted with one or more substituents independently selected from halogen, -OR 13 , -SR 13 , -N(R 13 ), 2 , -C(O)R 13 , -NO 2、 and -CN, R 5 is hydrogen or C 1~6 alkyl, and Y is a bond, -O-, -N(R 14 )-, or -C(R 14a )(R 14b )- and Z is Combination, -C(O)-, -C(R 15 ) 2 -, -C(O)C(R 15 ) 2 -, -C(O)[C(R 15 ) 2 q S-, -C(=N-CN)-, -C(O)O-, -C(O)N(R 16 )-, -C(S)-, -C(S)N(R 16 )-, -S(O)-, and -S(O) 2 -, selected from, wherein q is 1, 2, and 3, B is C 3~12 a carbocyclic ring and a 3- to 12-membered heterocyclic ring, each of which is halogen, -OR 17 , -SR 17 , -N(R 17 ), 2 , -C(O)R 17 , -C(O)OR 17 , -OC(O)R 17 , -OC(O)N(R 17 ) 2 、-C(O)N(R 17 ) 2 、-N(R 17 )C(O)R 17 、-N(R 17 )C(O)OR 17 、-N(R 17 )C(O)N(R 17 ) 2 、-N(R 17 )C(S)N(R 17 ) 2 、-N(R 17 )S(O) 2 (R 17 )、-S(O)R 17 、-S(O) 2 R 17 、-S(O) 2 N(R 17 ) 2 、-NO 2 、=O、=S、=NR 17 、-N 3 、及び-CN、 C 1~6 alkyl, C 2~6 alkenyl, and C 2~6 alkynyl, each of which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 17 , -SR 17 , -N(R 17 ), 2 , -C(O)R 17 , -C(O)OR 17 , -OC(O)R 17 , -OC(O)N(R 17 ), 2 , -C(O)N(R 17 ), 2 , -N(R 17 ),C(O)R 17 , -N(R 17 ),C(O)OR 17 , -N(R 17 ),C(O)N(R 17 ), 2 , -N(R 17 ),C(S)N(R 17 ), 2 , -N(R 17 ),S(O 2 (R 17 ), -S(O)R 17 , -S(O 2 R 17 , -S(O 2 N(R 17 ), 2 , -NO 2 , =O, =S, =NR 17 , -N 3 , and -CN, C 3~10 A carbon ring and a 3- to 10-membered heterocyclic ring, each of which is independently selected from halogen, C 1~6 alkyl, C 1~6 haloalkyl, -OR 17 -SR 17 -N(R 17 ) 2 -C(O)R 17 -C(O)OR 17 -OC(O)R 17 -OC(O)N(R 17 ) 2 -C(O)N(R 17 ) 2 -N(R 17 )C(O)R 17 -N(R 17 )C(O)OR 17 -N(R 17 )C(O)N(R 17 ) 2 -N(R 17 )C(S)N(R 17 ) 2 -N(R 17 )S(O) 2 (R 17 )-S(O)R 17 -S(O) 2 R 17 -S(O) 2 N(R 17 ) 2 -NO 2 =O, =S, =NR 17 -N 3 and -CN, and optionally substituted with one or more substituents independently selected from, and C 3~10 A carbon ring and a 3- to 10-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 17 , -SR 17 , -N(R 17 ), 2 , -C(O)R 17 , -C(O)OR 17 , -OC(O)R 17 , -OC(O)N(R 17 ) 2 , -C(O)N(R 17 ) 2 , -N(R 17 )C(O)R 17 , -N(R 17 )C(O)OR 17 , -N(R 17 ),C(O)N(R 17 ), 2 -N(R 17 ),C(S)N(R 17 ), 2 -N(R 17 ),S(O) 2 (R 17 ),-S(O)R 17 -S(O) 2 R 17 -S(O) 2 N(R 17 ), 2 -NO 2 =O,=S,=NR 17 -N 3 and -CN, C 1~6 an alkyl optionally substituted with one or more substituents independently selected from halogen, -OR 17 , -SR 17 , -N(R 17 ), -C(O)R 2 , -C(O)OR 17 , -OC(O)R 17 , -OC(O)N(R 17 ), -C(O)N(R 17 ), -C(O)N(R 2 ), -N(R 17 ), -N(R 2 ), -N(R 17 )C(O)R 17 ), -N(R 17 )C(O)OR 17 ), -N(R 17 )C(O)N(R 17 ), -N(R 2 ), -N(R 17 )C(S)N(R 17 ), -N(R 2 ), -N(R 17 )S(O) 2 (R 17 ), -S(O)R 17 ), -S(O) 2 R 17 ), -S(O) 2 N(R 17 ), -NO 2 , =O, =S, =NR 2 , -N 17 , and -CN, and 3 optionally substituted with one or more substituents independently selected from halogen, -OR C 3~10 A carbon ring and a 3- to 10-membered heterocyclic ring, each of which is halogen, C 1~6 alkyl, C 1~6 haloalkyl, -OR 17 , -SR 17 , -N(R 17 ), 2 , -C(O)R 17 , -NO 2 , =O, =S, =NR 17 , -N 3 , and -CN, and is optionally substituted with one or more substituents independently selected from those optionally substituted with one or more substituents independently selected from the group consisting of C is C 3~12 selected from a carbocyclic ring and a 3- to 12-membered heterocyclic ring, each of which halogen, -OR 18 , -OR 18A , -SR 18 , -N(R 18 ), 2 , -C(O)R 18 , -C(O)R 18A , -C(O)OR 18 , -OC(O)R 18 , -OC(O)N(R 18 ), 2 , -C(O)N(R 18 ), 2 , -N(R 18 ),C(O)R 18 , -N(R 18 ),C(O)OR 18 , -N(R 18 ),C(O)N(R 18 ), 2 , -N(R 18 ),C(S)N(R 18 ), 2 , -N(R 18 ),S(O) 2 (R 18 ), -S(O)R 18 , -S(O) 2 R 18 , -S(O) 2 ,N(R 18 ), 2 , -NO 2 , =O, =S, =NR 18 , -N 3 , and -CN, C 1~6 alkyl, C 2~6 alkenyl, and C 2~6 alkynyl, each of which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 , -SR 18 , -N(R 18 ), 2 , -C(O)R 18 , -C(O)OR 18 , -OC(O)R 18 , -OC(O)N(R 18 ) 2 、-C(O)N(R 18 ) 2 、-N(R 18 )C(O)R 18 、-N(R 18 )C(O)OR 18 、 -N(R 18 ),C(O)N(R 18 ), 2 -N(R 18 ),C(S)N(R 18 ), 2 -N(R 18 ),S(O) 2 (R 18 ),-S(O)R 18 -S(O) 2 R 18 -S(O) 2 N(R 18 ), 2 -NO 2 =O,=S,=NR 18 -N 3 and -CN, and, C 3~12 A carbon ring and a 3- to 12-membered heterocyclic ring, each of which is independently selected from halogen, -OR 18A , -SR 18A , -N(R 18A ), -C(O)R 2 , -C(O)OR 18A , -OC(O)R 18A , -OC(O)N(R 18A ), -C(O)N(R 18A ), -N(R 2 ), -N(R 18A ), -N(R 2 ), -N(R 18A ), -N(R 18A ), -N(R 18A ), -N(R 18A ), -N(R 18A ), -N(R 18A ), -N(R 2 ), -N(R 18A ), -N(R 18A ), -N(R 2 ), -N(R 18A ), -S(O) 2 (R 18A ), -S(O)R 18A ), -S(O) 2 R 18A ), -S(O) 2 N(R 18A ), -NO 2 , =O, =S, =NR 2 , -N 18A , -CN, C 3 alkyl, C 1~10 carbon ring and 3- to 10-membered heterocyclic ring are each independently optionally substituted with one or more substituents selected from halogen, -OR 3~10 carbon ring and 3- to 10-membered heterocyclic ring are each independently optionally substituted with one or more substituents selected from halogen, -OR 1~10 , -SR 3~10 , -N(R 18A ), -C(O)R 18A , -C(O)OR 18A , -OC(O)R 2 , -OC(O)N(R 18A ), -C(O)N(R 18A ), -N(R 18A ), -C(O)N(R 18A ), -N(R 2 ), -N(R 18A ), -N(R 2 ), -N(R 18A ), -N(R 18A , -N(R 18A )(C(O)OR 18A , -N(R 18A )(C(O)N(R 18A )) 2 , -N(R 18A )(C(S)N(R 18A )) 2 , -N(R 18A )(S(O) 2 (R 18A ), -S(O)R 18A , -S(O) 2 R 18A , -S(O) 2 N(R 18A )) 2 , -NO 2 , =O, =S, =NR 18A , -N 3 , -CN, C 1~6 alkyl, C 1~6 haloalkyl, C 3~6 carbocyclic, -C 3~6 carbocyclic-(C 1~6 (haloalkyl)), and those optionally substituted with one or more substituents independently selected from 3- to 6-membered heterocycles, and, C 3~6 A carbon ring and a 3- to 6-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from halogen, -OR 18 , -SR 18 , -N(R 18 ), -C(O)R 2 , -NO 18 , =O, =S, =NR 2 , -N 18 , -CN, and is optionally substituted with one or more substituents independently selected from halogen, -OR 3 , -SR 1~6 An alkyl group, which is optionally substituted with one or more substituents independently selected from halogen, -OR 18A , -SR 18A , -N(R 18A ), -C(O)R 2 , -C(O)OR 18A , -OC(O)R 18A , -OC(O)N(R 18A ), -C(O)N(R 18A ), -N(R 2 ), -C(O)N(R 18A ), -N(R 2 ), -N(R 18A ), -N(R 18A ), -N(R 18A ), -N(R 18A ), -N(R 18A ), -N(R 18A ), -N(R 2 ), -N(R 18A ), -N(R 18A ), -N(R 2 ), -N(R 18A ), -S(O) 2 (R 18A ), -S(O)R 18A ), -S(O) 2 R 18A ), -S(O) 2 N(R 18A ), -NO 2 , =O, =S, =NR 2 , -N 18A , -CN, and is optionally substituted with one or more substituents independently selected from a carbon ring and a 3- to 6-membered heterocyclic ring, and the C 3 carbon ring and 3- to 6-membered heterocyclic ring are each independently selected from halogen, -OR 3~6 , -SR 3~6 , -N(R 18A ), -C(O)R 18A , -N(R 18A ) 2 , -C(O)R 18A , -C(O)OR 18A , -OC(O)R 18A , -OC(O)N(R 18A ), 2 , -C(O)N(R 18A ), 2 , -N(R 18A ), C(O)R 18A , -N(R 18A ), C(O)OR 18A , -N(R 18A ), C(O)N(R 18A ), 2 , -N(R 18A ), C(S)N(R 18A ), 2 , -N(R 18A ), S(O) 2 (R 18A ), -S(O)R 18A , -S(O) 2 R 18A , -S(O) 2 N(R 18A ), 2 , -NO 2 , =O, =S, =NR 18A , -N 3 , and optionally substituted with one or more substituents independently selected from one or more substituents independently selected from -CN, R 11 and R 12 are each independently, for each occurrence, selected from hydrogen and C 1~6 alkyl, said C 1~6 alkyl being optionally substituted with one or more substituents independently selected from halogen, -OH, -NH 2 , -O-C 1~6 alkyl, -O-C 1~6 haloalkyl, =O, and CN R 14 is selected from hydrogen, C 1~6 alkyl, and C 3~6 carbocyclic ring, each of said C 1~6 alkyl and C 3~6 carbocyclic ring being optionally substituted with one or more substituents independently selected from halogen, -OH, -NH 2 , -O-C 1~6 alkyl, -O-C 1~6 haloalkyl, =O, and -CN; R 13 is independently, for each occurrence, selected from hydrogen and C 1~6 alkyl, R 14a and R 14b are each independently Hydrogen, C 1~6 alkyl, and C 3~6 a carbocyclic ring, wherein each of said C 1~6 alkyl and C 3~6 carbocyclic ring is optionally substituted with one or more substituents independently selected from halogen, -OH, -NH 2 , -O-C 1~6 alkyl, -O-C 1~6 haloalkyl, =O, and -CN, or R 14a and R 14b together form a C 3~6 carbocyclic ring or a 3- to 6-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from halogen, -OH, -NH 2 , C 1~6 alkyl, -C 1~6 haloalkyl, -O-C 1~6 alkyl, -O-C 1~6 haloalkyl, =O, and -CN R 15 is, independently for each occurrence, hydrogen, halogen, =O, -CN, C 1~6 alkyl, C 1~6 haloalkyl, C 3~6 a carbocyclic ring, and a 3- to 6-membered heterocyclic ring, or two Rs 15 are taken together to form a C 3~6 carbocyclic ring, R 16 is, for each occurrence, selected from hydrogen and C 1~6 alkyl, R 17 independently, for each occurrence, hydrogen, C 1~6 an alkyl, optionally substituted with one or more substituents independently selected from halogen, -OR 21 , -SR 21 , -N(R 21 ), 2 , -C(O)R 21 , -C(O)OR 21 , -OC(O)R 21 , -OC(O)N(R 21 ), 2 , -C(O)N(R 21 ), 2 , -N(R 21 ),C(O)R 21 , -NO 2 , =O, =S, =NR 21 , and -CN, and C 3~10 A carbon ring and a 3- to 10-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from the following: halogen, C 1~6 alkyl, C 1~6 haloalkyl - OR 21 , - SR 21 , - N(R 21 ), - C(O)R 2 , 21 -C(O)OR 21 、-OC(O)R 21 、-OC(O)N(R 21 ) 2 、-C(O)N(R 21 ) 2 、-N(R 21 )C(O)R 21 、 -N(R 21 )(C(O)OR 21 ), -N(R 21 )(C(O)N(R 21 )) 2 , -N(R 21 )(C(S)N(R 21 )) 2 , -N(R 21 )(S(O) 2 (R 21 ), -S(O)R 21 , -S(O) 2 R 21 , -S(O) 2 N(R 21 )) 2 , -NO 2 , =O, =S, =NR 17 , -CN, C 3~6 carbon ring, and 3- to 6-membered heterocyclic ring, selected from R 18 and R 21 are each independently, upon each occurrence, hydrogen, C 1~6 alkyl, C 1~6 haloalkyl, C 1~6 hydroxyalkyl, and C 1~6 aminoalkyl, selected from R 18A appears each time as hydrogen, C 1~6 is alkyl, optionally substituted with another substituent independently selected from halogen, -O-C 1~6 alkyl, -O-C 1~6 haloalkyl, -NH 2、 -NO 2 , =O, -CN, C 3~10 is optionally substituted with another substituent independently selected from a carbocyclic ring and a 3- to 10-membered heterocyclic ring, where each C 3~10 carbocyclic ring and 3- to 10-membered heterocyclic ring is optionally substituted with one or more substituents independently selected from halogen, -OH, C 1~6 alkyl, C 1~6 haloalkyl, -O-C 1~6 alkyl, -O-C 1~6 haloalkyl, -NH 2、 -NO 2 , =O, and -CN, and C 3~10 A carbon ring and a 3- to 10-membered heterocyclic ring, which are optionally substituted with one or more substituents independently selected from halogen, -OH, C 1~6 alkyl, C 1~6 haloalkyl, -O-C 1~6 alkyl, -O-C 1~6 haloalkyl, -NH 2、 -NO 2 , =O, -CN, C 3~6 a carbon ring and a 3- to 6-membered heterocyclic ring, and are optionally substituted with one or more substituents independently selected therefrom].
2. where B is halogen, -OR 17 , -SR 17 , -N(R 17 ), 2 , -C(O)R 17 , -C(O)OR 17 , -OC(O)R 17 , -OC(O)N(R 17 ), 2 -C(O)N(R 17 ), 2 -N(R 17 ),C(O)R 17 -N(R 17 ),C(O)OR 17 -N(R 17 ),C(O)N(R 17 ), 2 -N(R 17 ),C(S)N(R 17 ), 2 -N(R 17 ),S(O) 2 (R 17 ),-S(O)R 17 -S(O) 2 R 17 -S(O) 2 N(R 17 ), 2 -NO 2 =O,=S,=NR 17 -N 3 and-CN, C 1~6 alkyl, C 2~6 alkenyl, and C 2~6 alkynyl, each of which is optionally substituted with one or more substituents independently selected from the following: Halogen, -OR 17 , -SR 17 , -N(R 17 ), 2 , -C(O)R 17 , -C(O)OR 17 , -OC(O)R 17 , -OC(O)N(R 17 ), 2 , -C(O)N(R 17 ), 2 , -N(R 17 ),C(O)R 17 , -N(R 17 ),C(O)OR 17 , -N(R 17 ),C(O)N(R 17 ), 2 , -N(R 17 ),C(S)N(R 17 ), 2 , -N(R 17 ),S(O) 2 (R 17 ), -S(O)R 17 , -S(O) 2 R 17 , -S(O) 2 ,N(R 17 ), 2 , -NO 2 , =O, =S, =NR 17 , -N 3 , and -CN, C 3~10 A carbon ring and a 3- to 10-membered heterocyclic ring, each of which is independently selected from halogen, C 1~6 alkyl, C 1~6 haloalkyl, -OR 17 、-SR 17 、-N(R 17 ) 2 、-C(O)R 17 、-C(O)OR 17 、-OC(O)R 17 、-OC(O)N(R 17 ) 2 、-C(O)N(R 17 ) 2 、-N(R 17 )C(O)R 17 、-N(R 17 )C(O)OR 17 、-N(R 17 )C(O)N(R 17 ) 2 、-N(R 17 )C(S)N(R 17 ) 2 、-N(R 17 )S(O) 2 (R 17 )、-S(O)R 17 、-S(O) 2 R 17 、-S(O) 2 N(R 17 ) 2 、-NO 2 、=O、=S、=NR 17 、-N 3 、and -CN, and is optionally substituted with one or more substituents independently selected from these, and C 3~10 A carbon ring and a 3- to 10-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 17 , -SR 17 , -N(R 17 ), 2 , -C(O)R 17 , -C(O)OR 17 , -OC(O)R 17 , -OC(O)N(R 17 ), 2 , -C(O)N(R 17 ), 2 , -N(R 17 ),C(O)R 17 , -N(R 17 ),C(O)OR 17 , -N(R 17 ),C(O)N(R 17 ), 2 , -N(R 17 ),C(S)N(R 17 ), 2 , -N(R 17 ),S(O) 2 (R 17 ), -S(O)R 17 , -S(O) 2 R 17 , -S(O) 2 ,N(R 17 ), 2 , -NO 2 , =O, =S, =NR 17 , -N 3 , and -CN, C 1~6 Alkyl, halogen, -OR 17 , -SR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)OR 17 , -OC(O)R 17 , -OC(O)N(R 17 ) 2 , -C(O)N(R 17 ) 2 , -N(R 17 ) C(O)R 17 , -N(R 17 ) C(O)OR 17 , -N(R 17 ) C(O)N(R 17 ) 2 , -N(R 17 ) C(S)N(R 17 ) 2 , -N(R 17 ) S (O) 2 (R 17 ), -S(O)R 17 , -S(O) 2 R 17 , -S(O) 2 N (R 17 ) 2 , -NO 2 , =O, =S, =NR 17 , -N 3 -, and -CN, C 3~10 A carbon ring and a 3- to 10-membered heterocyclic ring, each of which is halogen, C 1~6 alkyl, C 1~6 haloalkyl, -OR 17 , -SR 17 , -N(R 17 ), 2 , -C(O)R 17 , -NO 2 , =O, =S, =NR 17 , -N 3 , and -CN, and is optionally substituted with one or more substituents independently selected from the group consisting of a 3- to 12-membered heterocyclic ring optionally substituted with one or more substituents independently selected from the group consisting of the compound or salt according to claim 1.
3. where B is Halogen, -OR 17 , -SR 17 , -N(R 17 ), 2 , -C(O)R 17 , -C(O)OR 17 , -NO 2 , -CN, C 1~6 is an alkyl group, optionally substituted with one or more substituents independently selected from halogen, -OR 17 , -SR 17 , -N(R 17 ), -C(O)R 2 , -C(O)OR 17 , -NO 17 , -CN, C 2 is optionally substituted with one or more substituents independently selected from a carbocyclic ring and a 3- to 10-membered heterocyclic ring, and the C 3~10 carbocyclic ring and the 3- to 10-membered heterocyclic ring are each optionally substituted with one or more substituents independently selected from halogen, -OR 3~10 , -SR 17 , -N(R 17 ), -C(O)R 17 , -C(O)OR 2 , -NO 17 , -CN, and 17 , -NO 2 , -CN, and those optionally substituted with one or more substituents independently selected from -CN, and C 3~10 Carbocycles and 3- to 10-membered heterocycles, each of which is selected from the group consisting of halogen, —OR 17 , -SR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)OR 17 , -NO 2 , -CN; 1~6 Alkyl, halogen, -OR 17 , -SR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)OR 17 , -NO 2 3. The compound or salt of claim 2, wherein the heterocyclic ring is a 3- to 12-membered heterocycle optionally substituted with one or more substituents independently selected from:
4. B is a 6- to 12-membered bicyclic heterocycle selected from a 6- to 12-membered fused heterocycle, a 6- to 12-membered spirocyclic heterocycle, and a 6- to 12-membered bridged heterocycle, each of which is selected from halogen, -OR 17 , -SR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)OR 17 , -NO 2 , -C.N., C. 1~6 and optionally substituted with one or more substituents independently selected from alkyl, halogen, -OR 17 , -SR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)OR 17 , -NO 2 4. The compound or salt of claim 3, optionally substituted with one or more substituents independently selected from:
5. B is one or more substituents independently selected from halogen, -OR 17 , -SR 17 , -N(R 17 ), 2 , -C(O)R 17 , -C(O)OR 17 , -NO 2 , -CN, and C 1~6 is a 6- to 12-membered spirocyclic heterocyclic ring optionally substituted with one or more substituents independently selected from alkyl, wherein the C1-6 alkyl is optionally substituted with one or more substituents independently selected from halogen, -OR 17 , -SR 17 , -N(R 17 ), 2 , -C(O)R 17 , -C(O)OR 17 , -NO 2 , and -CN, the compound or salt according to claim 4.
6. where B is 【Chemical Formula 3】 The compound or salt according to claim 5, wherein it is
7. C is C 3~10 selected from a carbocyclic ring and a 3- to 10-membered heterocyclic ring, -OR 18A or -C(O)R 18A optionally substituted with, R 18A is hydrogen, C 1~6 is alkyl, optionally substituted with another substituent independently selected from halogen, -O-C 1~6 alkyl, -O-C 1~6 haloalkyl, -NH 2、 -NO 2 , =O, -CN, C 3~10 optionally substituted with another substituent independently selected from carbocyclic rings and 3- to 10-membered heterocyclic rings, where each C 3~10 carbocyclic ring and 3- to 10-membered heterocyclic ring is optionally substituted with one or more substituents independently selected from halogen, -OH, C 1~6 alkyl, C 1~6 haloalkyl, -O-C 1~6 alkyl, -O-C 1~6 haloalkyl, -NH 2、 -NO 2 , =O, and -CN, and C 3~6 A carbon ring and a 3- to 6-membered heterocyclic ring, which are optionally substituted with one or more substituents independently selected from halogen, -OH, C 1~6 alkyl, C 1~6 haloalkyl, -O-C 1~6 alkyl, -O-C 1~6 haloalkyl, -NH 2、 -NO 2 , =O, -CN, C 3~6 A carbon ring and a 3- to 6-membered heterocyclic ring, which are optionally substituted with one or more substituents independently selected therefrom, the compound or salt according to any one of claims 1 to 6.
8. where C is 【Chemical 4】 selected from The compound or salt according to claim 7, wherein it is
9. C is C 3~12 a carbocyclic ring, and the C3-12 carbocyclic ring is halogen, -OR 18 , -SR 18 , -N(R 18 ), 2 , -C(O)R 18 , -C(O)OR 18 , -OC(O)R 18 , -OC(O)N(R 18 ), 2 , -C(O)N(R 18 ), 2 , -N(R 18 ),C(O)R 18 , -N(R 18 ),C(O)OR 18 , -N(R 18 ),C(O)N(R 18 ), 2 , -N(R 18 ),C(S)N(R 18 ), 2 , -N(R 18 ),S(O 2 (R 18 ), -S(O)R 18 , -S(O 2 R 18 , -S(O 2 N(R 18 ), 2 , -NO 2 , =O, =S, =NR 18 , -N 3 , and -CN, C 1~6 alkyl, C 2~6 alkenyl, and C 2~6 alkynyl, each of which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 , -SR 18 , -N(R 18 ), 2 , -C(O)R 18 , -C(O)OR 18 , -OC(O)R 18 , -OC(O)N(R 18 ), 2 , -C(O)N(R 18 ), 2 , -N(R 18 ),C(O)R 18 , -N(R 18 ),C(O)OR 18 , -N(R 18 ),C(O)N(R 18 ), 2 , -N(R 18 ),C(S)N(R 18 ), 2 , -N(R 18 ),S(O) 2 (R 18 ), -S(O)R 18 , -S(O) 2 R 18 , -S(O) 2 ,N(R 18 ), 2 , -NO 2 , =O, =S, =NR 18 , -N 3 , and -CN, and, C 3~12 A carbon ring and a 3- to 12-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from the following: Halogen, -OR 18A , -SR 18A , -N(R 18A ), 2 , -C(O)R 18A , -C(O)OR 18A , -OC(O)R 18A , -OC(O)N(R 18A ), 2 , -C(O)N(R 18A ), 2 , -N(R 18A ),C(O)R 18A , -N(R 18A ),C(O)OR 18A , -N(R 18A ),C(O)N(R 18A ), 2 , -N(R 18A ),C(S)N(R 18A ), 2 , -N(R 18A ),S(O) 2 (R 18A ), -S(O)R 18A , -S(O) 2 R 18A , -S(O) 2 ,N(R 18A ), 2 , -NO 2 , =O, =S, =NR 18A , -N 3 , -CN, C 1~10 alkyl, C 3~10 carbocyclic ring and 3- to 10-membered heterocyclic ring, where C 1~10 alkyl, C 3~10 carbocyclic ring and 3- to 10-membered heterocyclic ring are each halogen, -OR 18A , -SR 18A , -N(R 18A ), 2 , -C(O)R 18A , -C(O)OR 18A , -OC(O)R 18A , -OC(O)N(R 18A ), 2 , -C(O)N(R 18A ), 2 , -N(R 18A ),C(O)R 18A , -N(R 18A ),C(O)OR 18A , -N(R 18A ), C(O)N(R 18A ), 2 , -N(R 18A ), C(S)N(R 18A ), 2 , -N(R 18A ), S(O) 2 (R 18A ), -S(O)R 18A , -S(O) 2 R 18A , -S(O) 2 N(R 18A ), 2 , -NO 2 , =O, =S, =NR 18A , -N 3 , -CN, C 1~6 alkyl, C 1~6 haloalkyl, C 3~6 carbocyclic, -C 3~6 carbocyclic-(C 1~6 (haloalkyl), and those optionally substituted with one or more substituents independently selected from 3- to 6-membered heterocycles, and C 3~6 A carbon ring and a 3- to 6-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 , -SR 18 , -N(R 18 ), 2 , -C(O)R 18 , -NO 2 , =O, =S, =NR 18 , -N 3 , -CN, and C 1~6 an alkyl group, which is optionally substituted with one or more substituents independently selected from halogen, -OR 18A , -SR 18A , -N(R 18A ), -C(O)R 2 , -C(O)OR 18A , -OC(O)R 18A , -OC(O)N(R 18A ), -C(O)N(R 18A ), -N(R 2 ), -N(R 18A ), -N(R 2 ), -N(R 18A ), -N(R 18A ), -N(R 18A ), -N(R 18A ), -N(R 18A ), -N(R 18A ), -N(R 2 ), -N(R 18A ), -N(R 18A ), -N(R 2 ), -N(R 18A ), -S(O) 2 (R 18A ), -S(O)R 18A , -S(O) 2 R 18A , -S(O) 2 , -S(O) 18A , -NO 2 , =O, =S, =NR 2 , -N 18A , -CN, C 3 is optionally substituted with one or more substituents independently selected from a carbocyclic ring and 3- to 6-membered heterocyclic rings, and the C 3~6 carbocyclic ring and 3- to 6-membered heterocyclic rings are each independently selected from halogen, -OR 3~6 , -SR 18A , -N(R 18A ), -C(O)R 18A , -C(O)OR 2 , -OC(O)R 18A , -OC(O)N(R 18A ), -C(O)N(R 18A ), -N(R 18A ), -N(R 2 ), -N(R 18A ), -N(R 2 ), -N(R 18A ), -N(R 18A ), -N(R 18A ), -N(R 18A , -N(R 18A ),C(O)N(R 18A ), 2 , -N(R 18A ),C(S)N(R 18A ), 2 , -N(R 18A ),S(O) 2 (R 18A ), -S(O)R 18A , -S(O) 2 R 18A , -S(O) 2 N(R 18A ), 2 , -NO 2 , =O, =S, =NR 18A , -N 3 , and optionally substituted with one or more substituents independently selected from -CN, a compound or salt according to any one of claims 1 to 6, optionally substituted with one or more substituents independently selected from the above.
10. C is C 3~10 a carbocyclic ring, and the C3-10 carbocyclic ring is halogen, -OR 18 , -SR 18 , -N(R 18 ), 2 , -C(O)R 18 , -C(O)OR 18 , -OC(O)R 18 , -OC(O)N(R 18 ), 2 , -C(O)N(R 18 ), 2 , -N(R 18 ),C(O)R 18 , -NO 2 , and -CN, C 1~6 alkyl optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 , -SR 18 , -N(R 18 ), 2 , -C(O)R 18 , -C(O)OR 18 , -OC(O)R 18 , -OC(O)N(R 18 ), 2 , -C(O)N(R 18 ), 2 , -N(R 18 ),C(O)R 18 , -NO 2 , and -CN, and, C 3~12 A carbon ring and a 3- to 12-membered heterocyclic ring, each of which is independently selected from halogen, -OR 18A , -SR 18A , -N(R 18A ), 2 , -C(O)R 18A , -C(O)OR 18A , -OC(O)R 18A , -OC(O)N(R 18A ), 2 , -C(O)N(R 18A ), 2 , -N(R 18A ),C(O)R 18A , -NO 2 , -CN, C 1~6 alkyl, C 3~6 carbon ring and 3- to 6-membered heterocyclic ring, and is optionally substituted with one or more substituents independently selected therefrom, and C 1~6 alkyl, C 3~6 carbon ring and 3- to 6-membered heterocyclic ring are each independently selected from halogen, -OR 18A , -SR 18A , -N(R 18A ), 2 , -C(O)R 18A , -C(O)OR 18A , -OC(O)R 18A , -OC(O)N(R 18A ), 2 , -C(O)N(R 18A ), 2 , -N(R 18A ),C(O)R 18A , -NO 2 , -CN, C 1~6 alkyl, C 1~6 haloalkyl, C 3~6 carbon ring, -C 3~6 carbon ring-(C 1~6 haloalkyl), and is optionally substituted with one or more substituents independently selected from 3- to 6-membered heterocyclic rings, and C 3~6 A carbon ring and a 3- to 6-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 , -SR 18 , -N(R 18 ), 2 , -C(O)R 18 , -NO 2 , and -CN, and, C 1~6 is alkyl, optionally substituted with one or more substituents independently selected from halogen, -OR 18A , -SR 18A , -N(R 18A ), -C(O)R 2 , -C(O)OR 18A , -OC(O)R 18A , -OC(O)N(R 18A ), -C(O)N(R 18A ), -N(R 2 ), -C(O)R 18A ), -N(R 2 ), -N(R 18A ), -C(O)R 18A , -NO 2 , -CN, C 3~6 optionally substituted with one or more substituents independently selected from one or more substituents independently selected from carbocyclic rings and 3- to 6-membered heterocyclic rings, where the C 3~6 carbocyclic rings and 3- to 6-membered heterocyclic rings are each optionally substituted with one or more substituents independently selected from halogen, -OR 18A , -SR 18A , -N(R 18A ), -C(O)R 2 , -C(O)OR 18A , -OC(O)R 18A , -OC(O)N(R 18A ), -C(O)N(R 18A ), -N(R 2 ), -C(O)N(R 18A ), -N(R 2 ), -N(R 18A ), -C(O)R 18A , -NO 2 , -CN, and the compound or salt according to claim 9, optionally substituted with one or more substituents independently selected from those optionally substituted with one or more substituents independently selected from those.
11. where C is phenyl, and the phenyl is halogen, -OR 18 , -SR 18 , -N(R 18 ), 2 , -C(O)R 18 , -C(O)OR 18 , -OC(O)R 18 , -OC(O)N(R 18 ), 2 , -C(O)N(R 18 ), 2 , -N(R 18 ),C(O)R 18 , -NO 2 , and -CN, and, C 1~6 An alkyl optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 , -SR 18 , -N(R 18 ), 2 , -C(O)R 18 , -C(O)OR 18 , -OC(O)R 18 , -OC(O)N(R 18 ), 2 , -C(O)N(R 18 ), 2 , -N(R 18 ),C(O)R 18 , -NO 2 , and -CN, and, C 3~12 A carbon ring and a 3- to 12-membered heterocyclic ring, each of which is independently selected from halogen, -OR 18A , -SR 18A , -N(R 18A ), -C(O)R 2 , -C(O)OR 18A , -OC(O)R 18A , -OC(O)N(R 18A ), -C(O)N(R 18A ), -N(R 2 ), -C(O)N(R 18A ), -N(R 2 ), -N(R 18A ), -N(R 18A ), -NO 2 , -CN, C 1~6 alkyl, C 3~6 carbon ring and one or more substituents independently selected from 3- to 6-membered heterocyclic rings, optionally substituted with one or more substituents independently selected from halogen, -OR 1~6 alkyl, C 3~6 carbon ring and 3- to 6-membered heterocyclic rings are each independently selected from halogen, -OR 18A , -SR 18A , -N(R 18A ), -C(O)R 2 , -C(O)OR 18A , -OC(O)R 18A , -OC(O)N(R 18A ), -C(O)N(R 18A ), -N(R 2 ), -C(O)N(R 18A ), -N(R 2 ), -N(R 18A ), -N(R 18A ), -NO 2 , -CN, C 1~6 alkyl, C 1~6 haloalkyl, C 3~6 carbon ring, -C 3~6 carbon ring-(C 1~6 haloalkyl), and one or more substituents independently selected from 3- to 6-membered heterocyclic rings, optionally substituted with one or more substituents independently selected from halogen, -OR The compound or salt according to claim 10, optionally substituted with one or more substituents independently selected from halogen, -OR
12. where C is phenyl, and the phenyl is halogen, -OR 18 , -N(R 18 ), 2 , -NO 2 , and -CN, and C 1~6 Alkyl, halogen, -OR 18 , -N(R 18 ) 2 , -NO 2 and -CN, and 3- to 12-membered saturated heterocyclic rings each optionally substituted with one or more substituents independently selected from halogen, -OR 18A , -NO 2 , -C.N., C. 1~6 Alkyl, C 3~6 Optionally substituted with one or more substituents independently selected from carbocycle and 3- to 6-membered heterocycle; 1~6 Alkyl, C 3~6 The carbocyclic ring and the 3- to 6-membered heterocyclic ring are each independently selected from halogen, —OR 18A , -N(R 18A ) 2 , -NO 2 , -C.N., C. 1~6 Alkyl, C 1~6 Haloalkyl, C 3~6 Carbocycle, -C 3~6 Carbocycle - (C 1~6 12. The compound or salt of claim 11, optionally substituted with one or more substituents independently selected from: alkyl, alkyl haloalkyl, and 3- to 6-membered heterocycle.
13. where C is phenyl, and the phenyl is halogen, -OR 18 , -N(R 18 ), 2 , -NO 2 , and -CN, and C 1~6 Alkyl, halogen, -OR 18 , -N(R 18 ) 2 , -NO 2 and -CN, and 3- to 7-membered heterocycloalkyl, optionally substituted with one or more substituents independently selected from halogen, -OR 18A , -NO 2 , -C.N., C. 1~6 Alkyl, C 3~6 Optionally substituted with one or more substituents independently selected from carbocycle and 3- to 6-membered heterocycle; 1~6 Alkyl, C 3~6 The carbocyclic ring and the 3- to 6-membered heterocyclic ring are each independently selected from halogen, —OR 18A , -N(R 18A ) 2 , -NO 2 , -C.N., C. 1~6 Alkyl, C 1~6 Haloalkyl, C 3~6 Carbocycle, -C 3~6 Carbocycle - (C 1~6 13. The compound or salt of claim 12, optionally substituted with one or more substituents independently selected from: alkyl, alkyl haloalkyl, and 3- to 6-membered heterocycle.
14. where C is phenyl, and the phenyl is halogen, -OR 18 , -N(R 18 ), 2 , -NO 2 , and -CN, and C 1~6 alkyl optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 , -N(R 18 ), 2 , -NO 2 , -CN, and, Azetidinyl, piperidinyl, piperazinyl, and azapanyl, each of which is halogen, -OR 18A , -NO 2 , -CN, C 1~6 alkyl, C 3~6 carbocyclic ring and one or more substituents independently selected from 3- to 6-membered heterocyclic rings, optionally substituted with, C 1~6 alkyl, C 3~6 carbocyclic ring and 3- to 6-membered heterocyclic ring are each halogen, -OR 18A , -N(R 18A ), -NO 2 , -CN, C 2 , -CN, C 1~6 alkyl, C 1~6 haloalkyl, C 3~6 carbocyclic ring, -C 3~6 carbocyclic ring-(C 1~6 haloalkyl), and one or more substituents independently selected from 3- to 6-membered heterocyclic rings, optionally substituted with, R 18 and R 18A each is independently, at each occurrence, hydrogen, halogen, C 1~6 alkyl, and C 1~6 haloalkyl, optionally substituted with one or more substituents independently selected from, the compound or salt according to claim 13.
15. where C is 【Chemical Formula 5】 selected from The compound or salt according to claim 14, wherein it is
16. where C is phenyl, and the phenyl is halogen, -OR 18 , -N(R 18 ), 2 , -NO 2 , and -CN, and C 1~6 alkyl optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 , -N(R 18 ), 2 , -NO 2 , and -CN, and, An 8- to 12-membered spirocyclic saturated heterocyclic ring, which is optionally substituted with one or more substituents independently selected from halogen, -OR 18A , -NO 2 , -CN, C 1~6 alkyl, C 3~6 a carbocyclic ring and a 3- to 6-membered heterocyclic ring, and which is optionally substituted with one or more substituents independently selected from halogen, -OR 1~6 alkyl, C 3~6 a carbocyclic ring and a 3- to 6-membered heterocyclic ring are each optionally substituted with one or more substituents independently selected from halogen, -OR 18A , -N(R 18A ), -NO 2 , -CN, C 2 alkyl, C 1~6 haloalkyl, C 1~6 a carbocyclic ring, and a 3- to 6-membered heterocyclic ring, and which is optionally substituted with one or more substituents independently selected from those, and which is optionally substituted with one or more substituents independently selected from halogen, -OR 3~6 a carbocyclic ring, and a 3- to 6-membered heterocyclic ring, and which is optionally substituted with one or more substituents independently selected from those, and which is optionally substituted with one or more substituents independently selected from halogen, -OR
17. where C is phenyl, and the phenyl is halogen, -OR 18 , -N(R 18 ), 2 , -NO 2 , and -CN, and C 1~6 An alkyl optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 , -N(R 18 ), 2 , -NO 2 , and -CN, and, 6-azaspiro[2.5]octanyl, 2-oxa-8-azaspiro[4.5]decanil, 3-azaspiro[5.5]undecanyl, and 2,9-diazaspiro[5.5]undecanyl, each of which is independently selected from halogen, -OR 18A , -NO 2 , -CN, C 1~6 alkyl, C 3~6 carbocyclic ring and one or more substituents independently selected from 3- to 6-membered heterocyclic rings, and is optionally substituted with one or more substituents, C 1~6 alkyl, C 3~6 carbocyclic ring and 3- to 6-membered heterocyclic ring are each independently selected from halogen, -OR 18A , -N(R 18A ), -NO 2 , -CN, C 2 , -CN, C 1~6 alkyl, C 1~6 haloalkyl, C 3~6 carbocyclic ring, and 3- to 6-membered heterocyclic ring, and is optionally substituted with one or more substituents independently selected from the group consisting of, R 18 and R 18A each of which is independently, at each occurrence, hydrogen, halogen, C 1~6 alkyl, and C 1~6 haloalkyl, and is optionally substituted with one or more substituents independently selected from the group consisting of, the compound or salt according to claim 16.
18. where C is 【Chemical Formula 6】 selected from The compound or salt according to claim 17, wherein it is
19. where C is phenyl, and the phenyl is halogen, -OR 18 , -N(R 18 ), 2 , -NO 2 , and -CN, and, C 1~6 alkyl optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 , -N(R 18 ), 2 , -NO 2 , and -CN, and, 8-10 membered bridged saturated heterocycle, 18A , -NO 2 , -C.N., C. 1~6 Alkyl, C 3~6 Optionally substituted with one or more substituents independently selected from carbocycle and 3- to 6-membered heterocycle; 1~6 Alkyl, C 3~6 The carbocyclic ring and the 3- to 6-membered heterocyclic ring are each independently selected from halogen, —OR 18A , -N(R 18A ) 2 , -NO 2 , -C.N., C. 1~6 Alkyl, C 1~6 Haloalkyl, C 3~6 13. The compound or salt of claim 12, optionally substituted with one or more substituents independently selected from a carbocycle, and a 3- to 6-membered heterocycle.
20. where C is phenyl, and the phenyl is halogen, -OR 18 , -N(R 18 ), 2 , -NO 2 , and -CN, and, C 1~6 alkyl optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 , -N(R 18 ), 2 , -NO 2 , and -CN, and, 8-oxa-3-azabicyclo[3.2.1]octanyl, optionally substituted with one or more substituents independently selected from halogen, -OR 18A , -NO 2 , -CN, C 1~6 alkyl, C 3~6 carbocyclic ring and 3- to 6-membered heterocyclic ring, and C 1~6 alkyl, C 3~6 carbocyclic ring and 3- to 6-membered heterocyclic ring are each optionally substituted with one or more substituents independently selected from halogen, -OR 18A , -N(R 18A ), -NO 2 , -CN, C 2 alkyl, C 1~6 haloalkyl, C 1~6 carbocyclic ring, and 3- to 6-membered heterocyclic ring, and each of R 3~6 and R 18 is independently optionally substituted, for each occurrence, with one or more substituents independently selected from hydrogen, halogen, C 18A alkyl, and C 1~6 haloalkyl, the compound or salt according to claim 16. 1~6
21. where C is 【Chemical Formula 7】 selected from The compound or salt according to claim 20, wherein it is
22. where C is phenyl, and the phenyl is halogen, -OR 18 , -N(R 18 ), 2 , -NO 2 , and -CN, and, C 1~6 An alkyl optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 , -N(R 18 ), 2 , -NO 2 , and -CN, and A 6- to 10-membered fused saturated heterocyclic ring, which is optionally substituted with one or more substituents independently selected from halogen, -OR 18A , -NO 2 , -CN, C 1~6 alkyl, C 3~6 a carbocyclic ring and a 3- to 6-membered heterocyclic ring, and which is optionally substituted with one or more substituents independently selected from halogen, -OR 1~6 alkyl, C 3~6 a carbocyclic ring and a 3- to 6-membered heterocyclic ring are each optionally substituted with one or more substituents independently selected from halogen, -OR 18A , -N(R 18A ), -NO 2 , -CN, C 2 alkyl, C 1~6 haloalkyl, C 1~6 a carbocyclic ring, and a 3- to 6-membered heterocyclic ring, and which is optionally substituted with one or more substituents independently selected therefrom, and which is optionally substituted with one or more substituents independently selected from halogen, -OR 3~6 a carbocyclic ring, and a 3- to 6-membered heterocyclic ring, and which is optionally substituted with one or more substituents independently selected therefrom, the compound or salt according to claim 12.
23. where C is phenyl, and the phenyl is halogen, -OR 18 , -N(R 18 ), 2 , -NO 2 , and -CN, and C 1~6 An alkyl optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 , -N(R 18 ), 2 , -NO 2 , and -CN, and, Octahydro-1H-isoindolyl, optionally substituted with one or more substituents independently selected from halogen, -OR 18A , -NO 2 , -CN, C 1~6 alkyl, C 3~6 carbocyclic ring and 3- to 6-membered heterocyclic ring, and optionally substituted with one or more substituents independently selected from halogen, -OR 1~6 alkyl, C 3~6 carbocyclic ring and 3- to 6-membered heterocyclic ring are each optionally substituted with one or more substituents independently selected from halogen, -OR 18A , -N(R 18A ), -NO 2 , -CN, C 2 alkyl, C 1~6 haloalkyl, C 1~6 carbocyclic ring, and 3- to 6-membered heterocyclic ring, and optionally substituted with one or more substituents independently selected from halogen, -OR 3~6 wherein each of R 18 and R 18A is independently optionally substituted, at each occurrence, with one or more substituents independently selected from hydrogen, halogen, C 1~6 alkyl, and C 1~6 haloalkyl, the compound or salt according to claim 16.
24. where C is [Chemical 8] The compound or salt according to claim 23, wherein it is
25. C is C 6~12 a carbocyclic ring, and the C6-12 carbocyclic ring is C 3~6 optionally substituted with one or more substituents independently selected from a carbocyclic ring and a 3- to 6-membered heterocyclic ring, each of which is halogen, -OR 18 , -SR 18 , -N(R 18 ), 2 , -C(O)R 18 , -NO 2 , =O, =S, =NR 18 , -N 3 , -CN, and C 1~6 is alkyl, and is optionally substituted with one or more substituents independently selected from halogen, -OR 18A , -SR 18A , -N(R 18A ), -C(O)R 2 , -C(O)OR 18A , -OC(O)R 18A , -OC(O)N(R 18A ), -C(O)N(R 18A ), -N(R 2 ), -N(R 18A ), -N(R 2 ), -N(R 18A )C(O)R 18A ), -N(R 18A )C(O)OR 18A ), -N(R 18A )C(O)N(R 18A ), -N(R 2 )C(S)N(R 18A ), -N(R 18A ), -N(R 2 ), -N(R 18A )S(O) 2 (R 18A ), -S(O)R 18A ), -S(O) 2 R 18A ), -S(O) 2 N(R 18A ), -NO 2 , =O, =S, =NR 2 , -N 18A , -CN, C 3 is optionally substituted with one or more substituents independently selected from carbocyclic rings and 3- to 6-membered heterocyclic rings, and the C 3~6 carbocyclic rings and 3- to 6-membered heterocyclic rings are each independently selected from halogen, -OR 3~6 , -SR 18A , -N(R 18A ), -C(O)R 18A ), -C(O)OR 2 , -OC(O)R 18A , -OC(O)N(R 18A ), -C(O)N(R 18A ), -C(O)N(R 18A ), -N(R 2 ), -N(R 18A ), -N(R 2 ), -N(R 18A )C(O)R 18A ), -N(R 18A )C(O)OR 18A , -N(R 18A ),C(O)N(R 18A ), 2 , -N(R 18A ),C(S)N(R 18A ), 2 , -N(R 18A ),S(O) 2 (R 18A ), -S(O)R 18A , -S(O) 2 R 18A , -S(O) 2 N(R 18A ), 2 , -NO 2 , =O, =S, =NR 18A , -N 3 , and optionally substituted with one or more substituents independently selected from one or more substituents independently selected from -CN, the compound or salt according to claim 9.
26. C is C 8~12 a condensed carbon ring, and the C8-12 condensed carbon ring is halogen, -OR 18 , -SR 18 , -N(R 18 ), 2 , -NO 2 , -CN, and, C 1~6 Alkyl, halogen, -OR 18A , -N(R 18A ) 2 , -NO 2 , -C.N., C. 3~6 is optionally substituted with one or more substituents independently selected from a carbocycle and a 3- to 6-membered heterocycle; 3~6 The carbocyclic ring and the 3- to 6-membered heterocyclic ring are each independently selected from halogen, —OR 18A , -N(R 18A ) 2 , -NO 2 , -CN; and R 18 and R 18A Each of the following is independently selected from each occurrence: hydrogen, halogen, C 1~6 Alkyl, and C 1~6 26. The compound or salt of claim 25, optionally substituted with one or more substituents independently selected from: haloalkyl; and 5-6 membered heteroaryl, optionally substituted with one or more substituents independently selected from:
27. where C is 【Chemical Formula 9】 The compound or salt according to claim 26, wherein it is
28. where C is a 3- to 12-membered heterocyclic ring, and the 3- to 12-membered heterocyclic ring is halogen, -OR 18 , -SR 18 , -N(R 18 ), 2 , -C(O)R 18 , -C(O)OR 18 , -OC(O)R 18 , -OC(O)N(R 18 ), 2 , -C(O)N(R 18 ), 2 , -N(R 18 ),C(O)R 18 , -N(R 18 ),C(O)OR 18 , -N(R 18 ),C(O)N(R 18 ), 2 , -N(R 18 ),C(S)N(R 18 ), 2 , -N(R 18 ),S(O) 2 (R 18 ), -S(O)R 18 , -S(O) 2 R 18 , -S(O) 2 N(R 18 ), 2 , -NO 2 , =O, =S, =NR 18 , -N 3 , and -CN, C 1~6 alkyl, C 2~6 alkenyl, and C 2~6 alkynyl, each of which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 , -SR 18 , -N(R 18 ), 2 , -C(O)R 18 , -C(O)OR 18 , -OC(O)R 18 , -OC(O)N(R 18 ), 2 , -C(O)N(R 18 ), 2 , -N(R 18 ),C(O)R 18 , -N(R 18 ),C(O)OR 18 , -N(R 18 ),C(O)N(R 18 ), 2 , -N(R 18 ),C(S)N(R 18 ), 2 , -N(R 18 ),S(O 2 )(R 18 ), -S(O)R 18 , -S(O 2 R 18 , -S(O 2 ),N(R 18 ), 2 , -NO 2 , =O, =S, =NR 18 , -N 3 , and -CN, and, C 3~12 A carbon ring and a 3- to 12-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from the following: Halogen, -OR 18A , -SR 18A , -N(R 18A ), 2 , -C(O)R 18A , -C(O)OR 18A , -OC(O)R 18A , -OC(O)N(R 18A ), 2 , -C(O)N(R 18A ), 2 , -N(R 18A ),C(O)R 18A , -N(R 18A ),C(O)OR 18A , -N(R 18A ),C(O)N(R 18A ), 2 , -N(R 18A ),C(S)N(R 18A ), 2 , -N(R 18A ),S(O) 2 (R 18A ), -S(O)R 18A , -S(O) 2 R 18A , -S(O) 2 N(R 18A ), 2 , -NO 2 , =O, =S, =NR 18A , -N 3 , -CN, C 1~10 alkyl, C 3~10 carbocyclic ring and 3- to 10-membered heterocyclic ring, where C 1~10 alkyl, C 3~10 carbocyclic ring and 3- to 10-membered heterocyclic ring are each halogen, -OR 18A , -SR 18A , -N(R 18A ), 2 , -C(O)R 18A , -C(O)OR 18A , -OC(O)R 18A , -OC(O)N(R 18A ), 2 , -C(O)N(R 18A ), 2 , -N(R 18A ),C(O)R 18A , -N(R 18A ),C(O)OR 18A , -N(R 18A ), C(O)N(R 18A ), 2 , -N(R 18A ), C(S)N(R 18A ), 2 , -N(R 18A ), S(O) 2 (R 18A ), -S(O)R 18A , -S(O) 2 R 18A , -S(O) 2 N(R 18A ), 2 , -NO 2 , =O, =S, =NR 18A , -N 3 , -CN, C 1~6 alkyl, C 1~6 haloalkyl, C 3~6 carbocyclic, -C 3~6 carbocyclic-(C 1~6 (haloalkyl), and those optionally substituted with one or more substituents independently selected from 3- to 6-membered heterocycles, and C 3~6 A carbon ring and a 3- to 6-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 , -SR 18 , -N(R 18 ), 2 , -C(O)R 18 , -NO 2 , =O, =S, =NR 18 , -N 3 , -CN, and C 1~6 is an alkyl group optionally substituted with one or more substituents independently selected from halogen, -OR 18A , -SR 18A , -N(R 18A ), -C(O)R 2 , -C(O)OR 18A , -OC(O)R 18A , -OC(O)N(R 18A ), -C(O)N(R 18A ), -N(R 2 ), -N(R 18A ), -N(R 2 ), -N(R 18A ), -N(R 18A ), -N(R 18A ), -N(R 18A ), -N(R 18A ), -N(R 18A ), -N(R 2 ), -N(R 18A ), -N(R 18A ), -N(R 2 ), -N(R 18A ), -S(O) 2 (R 18A ), -S(O)R 18A ), -S(O) 2 R 18A ), -S(O) 2 N(R 18A ), -NO 2 , =O, =S, =NR 2 , -N 18A , -CN, C 3 is optionally substituted with one or more substituents independently selected from a carbocyclic ring and a 3- to 6-membered heterocyclic ring, and the C 3~6 carbocyclic ring and the 3- to 6-membered heterocyclic ring are each independently selected from halogen, -OR 3~6 , -SR 18A , -N(R 18A ), -C(O)R 18A ), -C(O)OR 2 , -OC(O)R 18A , -OC(O)N(R 18A ), -C(O)N(R 18A ), -N(R 18A ), -N(R 2 ), -N(R 18A ), -N(R 2 ), -N(R 18A ), -N(R 18A ), -N(R 18A ), -N(R 18A , -N(R 18A ), C(O)N(R 18A ), 2 , -N(R 18A ), C(S)N(R 18A ), 2 , -N(R 18A ), S(O) 2 (R 18A ), -S(O)R 18A , -S(O) 2 R 18A , -S(O) 2 N(R 18A ), 2 , -NO 2 , =O, =S, =NR 18A , -N 3 , and optionally substituted with one or more substituents independently selected from one or more substituents independently selected from -CN, the compound or salt according to any one of claims 1 to 6.
29. where C is pyridinyl, and the pyridinyl is halogen, -OR 18 , -N(R 18 ), 2 , -C(O)R 18 , -NO 2 , and -CN, C 1~6 alkyl optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 , -N(R 18 ), 2 , -C(O)R 18 , -NO 2 , and -CN, and, C 3~12 A carbon ring and a 3- to 12-membered heterocyclic ring, any of which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18A , -N(R 18A ), 2 , -C(O)R 18A , -NO 2 , -CN, C 1~6 alkyl, C 3~6 a carbocyclic ring and a 3- to 6-membered heterocyclic ring, where the C 1~6 alkyl, C 3~6 carbocyclic ring and the 3- to 6-membered heterocyclic ring are each optionally substituted with one or more substituents independently selected from halogen, -OR 18A , -N(R 18A ), 2 , -C(O)R 18A , -NO 2 , -CN, C 1~6 alkyl, C 1~6 haloalkyl, C 3~6 a carbocyclic ring, -C 3~6 carbocyclic ring-(C 1~6 haloalkyl), and a 3- to 6-membered heterocyclic ring, and is optionally substituted with one or more substituents independently selected from the above, R 18 and R 18A each of which is independently, for each occurrence, hydrogen, halogen, C 1~6 alkyl, and C 1~6 haloalkyl, a compound or salt according to claim 28.
30. where C is 【Chemical Formula 10】 selected from The compound or salt according to claim 29, wherein it is
31. where C is selected from 8- to 12-membered bicyclic heterocyclic rings, and the 8- to 12-membered bicyclic heterocyclic ring is halogen, -OR 18 , -SR 18 , -N(R 18 ), 2 , -C(O)R 18 , -C(O)OR 18 , -OC(O)R 18 , -OC(O)N(R 18 ), 2 , -C(O)N(R 18 ), 2 , -N(R 18 ),C(O)R 18 , =O, -NO 2 , and -CN, C 1~6 alkyl optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 , -SR 18 , -N(R 18 ), 2 , -C(O)R 18 , -C(O)OR 18 , -OC(O)R 18 , -OC(O)N(R 18 ), 2 , -C(O)N(R 18 ), 2 , -N(R 18 ),C(O)R 18 , -NO 2 , and -CN, and, C 3~12 a carbon ring and a 3- to 12-membered heterocyclic ring, each of which is independently selected from halogen, -OR 18A , -SR 18A , -N(R 18A ), 2 , -C(O)R 18A , -C(O)OR 18A , -OC(O)R 18A , -OC(O)N(R 18A ), 2 , -C(O)N(R 18A ), 2 , -N(R 18A )C(O)R 18A , -NO 2 , -CN, C 1~6 alkyl, C 3~6 a carbon ring and a 3- to 6-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from halogen, -OR 1~6 alkyl, C 3~6 a carbon ring and a 3- to 6-membered heterocyclic ring are each independently selected from halogen, -OR 18A , -SR 18A , -N(R 18A ), 2 , -C(O)R 18A , -C(O)OR 18A , -OC(O)R 18A , -OC(O)N(R 18A ), 2 , -C(O)N(R 18A ), 2 , -N(R 18A )C(O)R 18A , -NO 2 , -CN, C 1~6 alkyl, C 1~6 haloalkyl, C 3~6 a carbon ring, -C 3~6 a carbon ring-(C 1~6 haloalkyl), and a 3- to 6-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected therefrom, and C 3~6 A carbon ring and a 3- to 6-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 , -SR 18 , -N(R 18 ), 2 , -C(O)R 18 , -NO 2 , and -CN, and, C 1~6 is alkyl, and is optionally substituted with one or more substituents independently selected from halogen, -OR 18A , -SR 18A , -N(R 18A ), -C(O)R 2 , -C(O)OR 18A , -OC(O)R 18A , -OC(O)N(R 18A ), -C(O)N(R 18A ), -N(R 2 ), -C(O)R 18A ), -N(R 2 ), -N(R 18A ), -C(O)R 18A , -NO 2 , -CN, C 3~6 is optionally substituted with one or more substituents independently selected from one or more substituents independently selected from carbocyclic rings and 3- to 6-membered heterocyclic rings, and the C 3~6 carbocyclic rings and 3- to 6-membered heterocyclic rings are each optionally substituted with one or more substituents independently selected from halogen, -OR 18A , -SR 18A , -N(R 18A ), -C(O)R 2 , -C(O)OR 18A , -OC(O)R 18A , -OC(O)N(R 18A ), -C(O)N(R 18A ), -N(R 2 ), -C(O)N(R 18A ), -N(R 2 ), -N(R 18A ), -C(O)R 18A , -NO 2 , -CN, and is optionally substituted with one or more substituents independently selected from those optionally substituted with one or more substituents independently selected from those, the compound or salt according to claim 28.
32. where C is an 8- to 12-membered bicyclic heterocyclic ring, and the 8- to 12-membered bicyclic heterocyclic ring is halogen, -OR 18 , -SR 18 , -N(R 18 ), 2 , -C(O)R 18 , -C(O)OR 18 , -OC(O)R 18 , -OC(O)N(R 18 ), 2 , -C(O)N(R 18 ), 2 , -N(R 18 ),C(O)R 18 , -NO 2 , and -CN, and, C 1~6 An alkyl optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 , -SR 18 , -N(R 18 ), 2 , -C(O)R 18 , -C(O)OR 18 , -OC(O)R 18 , -OC(O)N(R 18 ), 2 , -C(O)N(R 18 ), 2 , -N(R 18 ),C(O)R 18 , =O, -NO 2 , and -CN, and, C 3~12 A carbon ring and a 3- to 12-membered heterocyclic ring, each of which is independently selected from halogen, -OR 18A , -SR 18A , -N(R 18A ), -C(O)R 2 , -C(O)OR 18A , -OC(O)R 18A , -OC(O)N(R 18A ), -C(O)N(R 18A ), -N(R 2 ), -C(O)N(R 18A ), -N(R 2 ), -N(R 18A ), -C(O)R 18A , -NO 2 , -CN, C 1~6 alkyl, C 3~6 carbon ring and 3- to 6-membered heterocyclic ring, and is optionally substituted with one or more substituents independently selected therefrom, C 1~6 alkyl, C 3~6 carbon ring and 3- to 6-membered heterocyclic ring are each independently selected from halogen, -OR 18A , -SR 18A , -N(R 18A ), -C(O)R 2 , -C(O)OR 18A , -OC(O)R 18A , -OC(O)N(R 18A ), -C(O)N(R 18A ), -N(R 2 ), -C(O)N(R 18A ), -N(R 2 ), -N(R 18A ), -C(O)R 18A , -NO 2 , -CN, C 1~6 alkyl, C 1~6 haloalkyl, C 3~6 carbon ring, -C 3~6 carbon ring-(C 1~6 haloalkyl), and is optionally substituted with one or more substituents independently selected therefrom, and is optionally substituted with one or more substituents independently selected from those described above, the compound or salt according to claim 31.
33. where C is an 8- to 12-membered bicyclic heterocyclic ring, and the 8- to 12-membered bicyclic heterocyclic ring is halogen, -OR 18 , -SR 18 , -N(R 18 ), 2 , -C(O)R 18 , -C(O)OR 18 , -OC(O)R 18 , -OC(O)N(R 18 ), 2 , -C(O)N(R 18 ), 2 , -N(R 18 ),C(O)R 18 , =O, -NO 2 , and -CN, and, C 1~6 alkyl optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 , -SR 18 , -N(R 18 ), 2 , -C(O)R 18 , -C(O)OR 18 , -OC(O)R 18 , -OC(O)N(R 18 ), 2 , -C(O)N(R 18 ), 2 , -N(R 18 ),C(O)R 18 , -NO 2 , and -CN, and, A 3- to 8-membered monocyclic heterocycloalkyl, optionally substituted with one or more substituents independently selected from halogen, -OR 18A , -SR 18A , -N(R 18A ), -C(O)R 2 , -C(O)OR 18A , -OC(O)R 18A , -OC(O)N(R 18A ), -C(O)N(R 18A ), -N(R 2 ), -C(O)N(R 18A ), -N(R 2 ), -N(R 18A )C(O)R 18A , -NO 2 , -CN, C 1~6 alkyl, C 3~6 carbocyclic ring and one or more substituents independently selected from 3- to 6-membered heterocyclic rings, optionally substituted with one or more substituents independently selected from halogen, -OR 1~6 , -SR 3~6 , -N(R 18A ), -C(O)R 18A , -C(O)OR 18A , -OC(O)R 2 , -OC(O)N(R 18A ), -C(O)N(R 18A ), -N(R 18A ), -C(O)N(R 18A ), -N(R 2 ), -N(R 18A ), -N(R 2 ), -N(R 18A )C(O)R 18A , -NO 2 , -CN, C 1~6 alkyl, C 1~6 haloalkyl, C 3~6 carbocyclic ring, -C 3~6 carbocyclic ring-(C 1~6 haloalkyl), and one or more substituents independently selected from 3- to 6-membered heterocyclic rings, optionally substituted with one or more substituents independently selected from the above, the compound or salt according to claim 32, optionally substituted with one or more substituents independently selected from the above.
34. where C is an 8- to 12-membered bicyclic heterocyclic ring, and the 8- to 12-membered bicyclic heterocyclic ring is halogen, -OR 18 , -N(R 18 ), 2 , -C(O)R 18 , =O, -NO 2 , and -CN, and, C 1~6 alkyl optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 , -N(R 18 ), 2 , -C(O)R 18 , -NO 2 , and -CN, and, 3-8 membered monocyclic heterocycloalkyl, 18A , -N(R 18A ) 2 , -C(O)R 18A , -NO 2 , -C.N., C. 1~6 Alkyl, C 3~6 Optionally substituted with one or more substituents independently selected from a carbocycle and a 3- to 6-membered heterocycle.
35. where C is 【Chemical 11】 selected from The compound or salt according to claim 34, wherein it is
36. C is an 8- to 12-membered bicyclic heterocyclic ring, and the 8- to 12-membered bicyclic heterocyclic ring is halogen, -OR 18 , -SR 18 , -N(R 18 ), 2 , -C(O)R 18 , -C(O)OR 18 , -OC(O)R 18 , -OC(O)N(R 18 ), 2 , -C(O)N(R 18 ), 2 , -N(R 18 ),C(O)R 18 , =O, -NO 2 , and -CN, and, C 1~6 alkyl optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 , -SR 18 , -N(R 18 ), 2 , -C(O)R 18 , -C(O)OR 18 , -OC(O)R 18 , -OC(O)N(R 18 ), 2 , -C(O)N(R 18 ), 2 , -N(R 18 ),C(O)R 18 , -NO 2 , and -CN, and, A 3- to 12-membered bicyclic heterocyclic ring, which is optionally substituted with one or more substituents independently selected from halogen, -OR 18A , -SR 18A , -N(R 18A ), 2 , -C(O)R 18A , -C(O)OR 18A , -OC(O)R 18A , -OC(O)N(R 18A ), 2 , -C(O)N(R 18A ), 2 , -N(R 18A )C(O)R 18A , -NO 2 , -CN, C 1~6 alkyl, C 3~6 a carbocyclic ring and a 3- to 6-membered heterocyclic ring, and is optionally substituted with one or more substituents independently selected therefrom, C 1~6 alkyl, C 3~6 a carbocyclic ring and a 3- to 6-membered heterocyclic ring are each optionally substituted with one or more substituents independently selected from halogen, -OR 18A , -SR 18A , -N(R 18A ), 2 , -C(O)R 18A , -C(O)OR 18A , -OC(O)R 18A , -OC(O)N(R 18A ), 2 , -C(O)N(R 18A ), 2 , -N(R 18A )C(O)R 18A , -NO 2 , -CN, C 1~6 alkyl, C 1~6 haloalkyl, C 3~6 a carbocyclic ring, -C 3~6 a carbocyclic ring-(C 1~6 haloalkyl), and a 3- to 6-membered heterocyclic ring, and is optionally substituted with one or more substituents independently selected therefrom, and is optionally substituted with one or more substituents independently selected therefrom, the compound or salt according to claim 32.
37. C is an 8- to 12-membered bicyclic heterocyclic ring, and the 8- to 12-membered bicyclic heterocyclic ring is halogen, -OR 18 , -SR 18 , -N(R 18 ), 2 , -C(O)R 18 , -C(O)OR 18 , -OC(O)R 18 , -OC(O)N(R 18 ), 2 , -C(O)N(R 18 ), 2 , -N(R 18 ),C(O)R 18 , =O, -NO 2 , and -CN, and, C 1~6 alkyl optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 , -SR 18 , -N(R 18 ), 2 , -C(O)R 18 , -C(O)OR 18 , -OC(O)R 18 , -OC(O)N(R 18 ), 2 , -C(O)N(R 18 ), 2 , -N(R 18 ),C(O)R 18 , -NO 2 , and -CN, and, A 6- to 12-membered spirocyclic heterocyclic ring, which is optionally substituted with one or more substituents independently selected from halogen, -OR 18A , -SR 18A , -N(R 18A ), 2 , -C(O)R 18A , -C(O)OR 18A , -OC(O)R 18A , -OC(O)N(R 18A ), 2 , -C(O)N(R 18A ), 2 , -N(R 18A )C(O)R 18A , -NO 2 , -CN, C 1~6 alkyl, C 3~6 carbocyclic ring and 3- to 6-membered heterocyclic ring, and is optionally substituted with one or more substituents independently selected from halogen, -OR 1~6 , -SR 3~6 , -N(R 18A ), 18A , -C(O)R 18A ), 2 , -C(O)OR 18A , -OC(O)R 18A , -OC(O)N(R 18A ), 18A ), 2 , -C(O)N(R 18A ), 2 , -N(R 18A )C(O)R 18A , -NO 2 , -CN, C 1~6 alkyl, C 1~6 haloalkyl, C 3~6 carbocyclic ring, -C 3~6 carbocyclic ring-(C 1~6 haloalkyl), and 3- to 6-membered heterocyclic ring, and is optionally substituted with one or more substituents independently selected therefrom, and is optionally substituted with one or more substituents independently selected from those described above, the compound or salt according to claim 36.
38. C is an 8- to 12-membered bicyclic heterocyclic ring, and the 8- to 12-membered bicyclic heterocyclic ring is halogen, -OR 18 , -N(R 18 ), 2 , -C(O)R 18 , =O, -NO 2 , and -CN, and, C 1~6 alkyl optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 , -N(R 18 ), 2 , -C(O)R 18 , -NO 2 , and -CN, and, 6- to 12-membered spirocyclic heterocycles, 18A , -N(R 18A ) 2 , -C(O)R 18A , -NO 2 , -C.N., C. 1~6 Alkyl, C 3~6 Optionally substituted with one or more substituents independently selected from: a carbocycle and a 3- to 6-membered heterocycle.
39. C is 【Chemical 12】 The compound or salt according to claim 38, which is selected from
40. C is an 8- to 12-membered bicyclic heterocyclic ring, and the 8- to 12-membered bicyclic heterocyclic ring is halogen, -OR 18 , -SR 18 , -N(R 18 ), 2 , -C(O)R 18 , -C(O)OR 18 , -OC(O)R 18 , -OC(O)N(R 18 ), 2 , -C(O)N(R 18 ), 2 , -N(R 18 ),C(O)R 18 , =O, -NO 2 , and -CN, and, C 1~6 alkyl optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 , -SR 18 , -N(R 18 ), 2 , -C(O)R 18 , -C(O)OR 18 , -OC(O)R 18 , -OC(O)N(R 18 ), 2 , -C(O)N(R 18 ), 2 , -N(R 18 ),C(O)R 18 , -NO 2 , and -CN, and, A 6- to 12-membered bridged complex ring, which is optionally substituted with one or more substituents independently selected from halogen, -OR 18A , -SR 18A , -N(R 18A ), 2 , -C(O)R 18A , -C(O)OR 18A , -OC(O)R 18A , -OC(O)N(R 18A ), 2 , -C(O)N(R 18A ), 2 , -N(R 18A )C(O)R 18A , -NO 2 , -CN, C 1~6 alkyl, C 3~6 a carbocyclic ring and a 3- to 6-membered heterocyclic ring, which are each optionally substituted with one or more substituents independently selected from halogen, -OR 1~6 , -SR 3~6 , -N(R 18A ), 18A , -C(O)R 18A ), 2 , -C(O)OR 18A , -OC(O)R 18A , -OC(O)N(R 18A ), 18A ), 2 , -C(O)N(R 18A ), 2 , -N(R 18A )C(O)R 18A , -NO 2 , -CN, C 1~6 alkyl, C 1~6 haloalkyl, C 3~6 a carbocyclic ring, -C 3~6 a carbocyclic ring-(C 1~6 haloalkyl), and a 3- to 6-membered heterocyclic ring, which are each optionally substituted with one or more substituents independently selected therefrom, and which is optionally substituted with one or more substituents independently selected from those described above, the compound or salt according to claim 36.
41. C is an 8- to 12-membered bicyclic heterocyclic ring, and the 8- to 12-membered bicyclic heterocyclic ring is halogen, -OR 18 , -N(R 18 ), 2 , -C(O)R 18 , =O, -NO 2 , and -CN, and, C 1~6 alkyl optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 , -N(R 18 ), 2 , -C(O)R 18 , -NO 2 , and -CN, and, A 6- to 12-membered bridged heterocycle, 18A , -N(R 18A ) 2 , -C(O)R 18A , -NO 2 , -C.N., C. 1~6 Alkyl, C 3~6 40. The compound or salt of claim 39, optionally substituted with one or more substituents independently selected from: a carbocycle and a 3- to 6-membered heterocycle.
42. C is 【Chemical 13】 The compound or salt according to claim 41, which is selected from
43. The compound according to claim 1, wherein formula (I) is represented by the structure of formula (I-a), 【Number】 or a pharmaceutically acceptable salt thereof, wherein A is 【Number】 selected from X 1 , X 2 , X 3 , and X 4 are each independently selected from N and C(R 2 ), and at least one of X 1 , X 2 , and X 3 is C(R 2 ), 【Number 2】 represents a single bond or a double bond, m is 0, 1, 2, or 3, n is 0, 1, or 2, p is 0, 1, 2, or 3, Each R 1 is, independently, halogen, -OR 11 , -SR 11 , -N(R 11 ), 2 , -C(O)R 11 , -C(O)OR 11 , -OC(O)R 11 , -OC(O)N(R 11 ) 2 、-C(O)N(R 11 ) 2 、-N(R 11 )C(O)R 11 、-N(R 11 )C(O)OR 11 、 -N(R 11 )(C(O)N(R 11 )) 2 、-N(R 11 )(C(S)N(R 11 )) 2 、-N(R 11 )(S(O) 2 (R 11 ))、-S(O)R 11 、-S(O) 2 R 11 、-S(O) 2 N(R 11 )) 2 、-NO 2 、and -CN, C 1~6 alkyl, C 2~6 alkenyl, and C 2~6 alkynyl, each of which is optionally substituted by one or more substituents independently selected from halogen, -OR 11 , -SR 11 , -N(R 11 ), 2 =O, =S, and -CN, and is optionally substituted by one or more substituents independently selected from halogen, -OR C 3~6 a carbon ring and a 3- to 6-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from halogen, C 1~4 alkyl, C 1~4 haloalkyl, -OR 11 , -SR 11 , -N(R 11 ), 2 =O, =S, and -CN, and is selected from those optionally substituted with one or more substituents independently selected therefrom Each R 2 is, independently, Hydrogen, halogen, -OR 12 , -SR 12 , -N(R 12 ), 2 , -C(O)R 12 , -C(O)OR 12 , -OC(O)R 12 , -OC(O)N(R 12 ) 2 、-C(O)N(R 12 ) 2 、-N(R 12 )C(O)R 12 、-N(R 12 )C(O)OR 12 、 -N(R 12 ),C(O)N(R 12 ), 2 -N(R 12 ),C(S)N(R 12 ), 2 -N(R 12 ),S(O) 2 (R 12 ),-S(O)R 12 -S(O) 2 R 12 -S(O) 2 N(R 12 ), 2 -NO 2、 and -CN, C 1~6 alkyl, C 2~6 alkenyl, and C 2~6 alkynyl, each of which is optionally substituted by one or more substituents independently selected from halogen, -OR 12 , -SR 12 , -N(R 12 ), 2 =O, =S, and -CN, and C 3~6 A carbon ring and a 3- to 6-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from halogen, C 1~4 alkyl, C 1~4 haloalkyl, -OR 12 , -SR 12 , -N(R 12 ), 2 =O, =S, and -CN, and is selected from those optionally substituted with one or more substituents independently selected from the group consisting of: R 3 is hydrogen or C 1~6 alkyl, and R 4a and R 4b are each independently Hydrogen, halogen, -OR 13 , -SR 13 , -N(R 13 ), 2 , -C(O)R 13 , -NO 2 , -CN, and C 1~6 alkyl, optionally substituted with one or more substituents independently selected from halogen, -OR 13 , -SR 13 , -N(R 13 ), 2 , -C(O)R 13 , -NO 2、 and -CN, R 5 is hydrogen or C 1~6 alkyl, and Y is a bond, -O-, -N(R 14 )-, or -C(R 14a )(R 14b )-, and Z is Combination, -C(O)-, -C(R 15 ) 2 -, -C(O)C(R 15 ) 2 -, -C(O)[C(R 15 ) 2 q S-, -C(=N-CN)-, -C(O)O-, -C(O)N(R 16 )-, -C(S)-, -C(S)N(R 16 )-, -S(O)-, and -S(O) 2 -, selected from, wherein q is 1, 2, and 3, B is C 3~10 a carbocyclic ring and a 3- to 10-membered heterocyclic ring, each of which is halogen, -OR 17 , -SR 17 , -N(R 17 ), 2 , -C(O)R 17 , -C(O)OR 17 , -OC(O)R 17 , -OC(O)N(R 17 ), -C(O)N(R 2 ), -N(R 17 )(C(O)R 2 ), -N(R 17 )(C(O)OR 17 ), -N(R 17 )(C(O)N(R 17 ), -N(R 17 )(C(S)N(R 17 ), -N(R 2 )(S(O)(R 17 ), -S(O)(R 17 ), -S(O)(R 2 ), -S(O)(N(R 17 ), -NO 2 ), =O, =S, =NR 17 ), -N 17 ), -S(O)(R 2 ), -S(O)(N(R 17 ), -S(O)(N(R 2 ), -NO 17 ), =O, =S, =NR 2 ), -NO 2 ), =O, =S, =NR 17 ), -N 3 ), and -CN, C 1~6 alkyl, C 2~6 alkenyl, and C 2~6 alkynyl, each of which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 17 , -SR 17 , -N(R 17 ), 2 , -C(O)R 17 , -C(O)OR 17 , -OC(O)R 17 , -OC(O)N(R 17 ), 2 , -C(O)N(R 17 ), 2 , -N(R 17 ),C(O)R 17 , -N(R 17 ),C(O)OR 17 , -N(R 17 ),C(O)N(R 17 ), 2 , -N(R 17 ),C(S)N(R 17 ), 2 , -N(R 17 ),S(O) 2 (R 17 ), -S(O)R 17 , -S(O) 2 R 17 , -S(O) 2 N(R 17 ), 2 , -NO 2 , =O, =S, =NR 17 , -N 3 , and -CN, C 3~10 a carbon ring and a 3- to 10-membered heterocyclic ring, each of which is independently selected from halogen, C 1~6 alkyl, C 1~6 haloalkyl, -OR 17 -SR 17 -N(R 17 ) 2 -C(O)R 17 -C(O)OR 17 -OC(O)R 17 -OC(O)N(R 17 ) 2 -C(O)N(R 17 ) 2 -N(R 17 )C(O)R 17 -N(R 17 )C(O)OR 17 -N(R 17 )C(O)N(R 17 ) 2 -N(R 17 )C(S)N(R 17 ) 2 -N(R 17 )S(O) 2 (R 17 )-S(O)R 17 -S(O) 2 R 17 -S(O) 2 N(R 17 ) 2 -NO 2 =O, =S, =NR 17 -N 3 and -CN, and optionally substituted with one or more substituents independently selected from C 3~10 A carbon ring and a 3- to 10-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 17 , -SR 17 , -N(R 17 ), 2 , -C(O)R 17 , -C(O)OR 17 , -OC(O)R 17 , -OC(O)N(R 17 ) 2 、-C(O)N(R 17 ) 2 、-N(R 17 )C(O)R 17 、-N(R 17 )C(O)OR 17 、 -N(R 17 ),C(O)N(R 17 ), 2 -N(R 17 ),C(S)N(R 17 ), 2 -N(R 17 ),S(O) 2 (R 17 ),-S(O)R 17 -S(O) 2 R 17 -S(O) 2 N(R 17 ), 2 -NO 2 =O,=S,=NR 17 -N 3 and-CN, C 1~6 Alkyl, halogen, -OR 17 , -SR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)OR 17 , -OC(O)R 17 , -OC(O)N(R 17 ) 2 , -C(O)N(R 17 ) 2 , -N(R 17 ) C(O)R 17 , -N(R 17 ) C(O)OR 17 , -N(R 17 ) C(O)N(R 17 ) 2 , -N(R 17 ) C(S)N(R 17 ) 2 , -N(R 17 ) S (O) 2 (R 17 ), -S(O)R 17 , -S(O) 2 R 17 , -S(O) 2 N (R 17 ) 2 , -NO 2 , =O, =S, =NR 17 , -N 3 -, and -CN, C 3~10 a carbon ring and a 3- to 10-membered heterocyclic ring, each of which is independently selected from halogen, C 1~6 alkyl, C 1~6 haloalkyl, -OR 17 , -SR 17 , -N(R 17 ), 2 , -C(O)R 17 , -NO 2 , =O, =S, =NR 17 , -N 3 , and -CN, and is optionally substituted with one or more substituents independently selected from those optionally substituted with one or more substituents independently selected from the group consisting of C is C 5~10 selected from a carbocyclic ring and a 5- to 10-membered heterocyclic ring, each of which is halogen, -OR 18 , -SR 18 , -N(R 18 ), 2 , -C(O)R 18 , -C(O)OR 18 , -OC(O)R 18 , -OC(O)N(R 18 ) 2 、-C(O)N(R 18 ) 2 、-N(R 18 )C(O)R 18 、-N(R 18 )C(O)OR 18 、-N(R 18 )C(O)N(R 18 ) 2 、-N(R 18 )C(S)N(R 18 ) 2 、-N(R 18 )S(O) 2 (R 18 )、-S(O)R 18 、-S(O) 2 R 18 、-S(O) 2 N(R 18 ) 2 、-NO 2 、=O、=S、=NR 18 、-N 3 、及び-CN、 C 1~6 alkyl, C 2~6 alkenyl, and C 2~6 alkynyl, each of which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 18 , -SR 18 , -N(R 18 ), 2 , -C(O)R 18 , -C(O)OR 18 , -OC(O)R 18 , -OC(O)N(R 18 ) 2 、-C(O)N(R 18 ) 2 、-N(R 18 )C(O)R 18 、-N(R 18 )C(O)OR 18 、 -N(R 18 )(C(O)N(R 18 )) 2 、-N(R 18 )(C(S)N(R 18 )) 2 、-N(R 18 )(S(O) 2 (R 18 ))、-S(O)R 18 、-S(O) 2 R 18 、-S(O) 2 N(R 18 )) 2 、-NO 2 、=O、=S、=NR 18 、-N 3 、and -CN, and, C 3~6 A carbon ring and a 3- to 6-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from halogen, C 1~4 alkyl, and C 1~4 haloalkyl, and C 3~6 A carbon ring and a 3- to 6-membered heterocyclic ring, each of which is independently selected from halogen, C 1~6 alkyl, C 1~6 haloalkyl, -OR 18 , -SR 18 , -N(R 18 ), 2 , -C(O)R 18 , -NO 2 , =O, =S, =NR 18 , -N 3 , and -CN, and is optionally substituted with one or more substituents independently selected from those optionally substituted with one or more substituents independently selected from the group consisting of R 11 and R 12 are each independently, at each occurrence, selected from hydrogen and C 1~6 alkyl, wherein said C 1~6 alkyl is optionally substituted with one or more substituents independently selected from halogen, -OH, -NH 2 , -O-C 1~6 alkyl, -O-C 1~6 haloalkyl, =O, and CN R 14 is selected from hydrogen, C 1~6 alkyl, and C 3~6 carbocyclic ring, wherein each of said C 1~6 alkyl and C 3~6 carbocyclic ring is optionally substituted with one or more substituents independently selected from halogen, -OH, -NH 2 , -O-C 1~6 alkyl, -O-C 1~6 haloalkyl, =O, and -CN; R 13 is, independently for each occurrence, selected from hydrogen and C 1~6 alkyl, R 14a and R 14b are each independently Hydrogen, C 1~6 alkyl, and C 3~6 a carbocyclic ring, wherein each of said C 1~6 alkyl and C 3~6 carbocyclic ring is optionally substituted with one or more substituents independently selected from halogen, -OH, -NH 2 , -O-C 1~6 alkyl, -O-C 1~6 haloalkyl, =O, and -CN, or R 14a and R 14b together form a C 3~6 carbocyclic ring or a 3- to 6-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from halogen, -OH, -NH 2 , C 1~6 alkyl, -C 1~6 haloalkyl, -O-C 1~6 alkyl, -O-C 1~6 haloalkyl, =O, and -CN R 15 is, independently for each occurrence, hydrogen, halogen, =O, -CN, C 1~6 alkyl, C 1~6 haloalkyl, C 3~6 a carbocyclic ring, and a 3- to 6-membered heterocyclic ring, or two Rs 15 together form a C 3~6 carbocyclic ring, R 16 is, for each occurrence, selected from hydrogen and C 1~6 alkyl, R 17 independently, for each occurrence, hydrogen, C 1~6 alkyl optionally substituted with one or more substituents independently selected from the following: halogen, -OR 21 , -SR 21 , -N(R 21 ), 2 , -C(O)R 21 , -C(O)OR 21 , -OC(O)R 21 , -OC(O)N(R 21 ) 2 、-C(O)N(R 21 ) 2 、-N(R 21 )C(O)R 21 、-NO 2 、=O、=S、=NR 21 、and -CN, and, C 3~10 A carbon ring and a 3- to 10-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from the following: halogen, C 1~6 alkyl, C 1~6 haloalkyl - OR 21 , - SR 21 , - N(R 21 ), - C(O)R 2 , 21 , -C(O)OR 21 、-OC(O)R 21 、-OC(O)N(R 21 ) 2 、-C(O)N(R 21 ) 2 、-N(R 21 )C(O)R 21 、 -N(R 21 ), C(O)OR 21 -N(R 21 ), C(O)N(R 21 ), 2 -N(R 21 ), C(S)N(R 21 ), 2 -N(R 21 ), S(O) 2 (R 21 ), -S(O)R 21 -S(O) 2 R 21 -S(O) 2 N(R 21 ), 2 -NO 2 =O, =S, =NR 17 -CN, C 3~6 carbon ring, and 3- to 6-membered heterocyclic ring, selected from R 18 and R 21 are each independently, for each occurrence, hydrogen, C 1~6 alkyl, C 1~6 haloalkyl, C 1~6 hydroxyalkyl, and C 1~6 aminoalkyl, selected compounds or salts.
44. A is 【Chemical 16】 The compound or salt according to claim 43, wherein A is
45. A is 【Chemical 17】 The compound or salt according to claim 44, which is selected from
46. A is 【Chemical Formula 18】 The compound or salt according to claim 45, wherein A is
47. A is 【Chemical Formula 19】 The compound or salt according to claim 45, wherein A is
48. A is 【Chemical 20】 The compound or salt according to claim 43, wherein A is
49. A is 【Chemical 21】 The compound or salt according to claim 48, wherein A is and n is 0 or 1.
50. The compound or salt according to any one of claims 43 to 49, wherein Y is a bond.
51. R 4a and R 4b each independently is hydrogen, halogen, C 1~3 alkyl, and C 1~3 haloalkyl, a compound or salt according to any one of claims 43 to 50.
52. R 4a and R 4b is each hydrogen or halogen, the compound or salt according to claim 51.
53. R 5 The compound or salt according to any one of claims 43 to 52, wherein R is hydrogen.
54. R 3 The compound or salt according to any one of claims 43 to 53, wherein R is hydrogen, methyl, or ethyl.
55. R 3 The compound or salt according to claim 54, wherein R is hydrogen.
56. Z is selected from bonding, -C(O)-, -C(R 15 ) 2 -, -C(O)C(R 15 ) 2 -, -C(O)[C(R 15 ) 2 p S-, -C(=N-CN)-, and -S(O) 2 -, a compound or salt according to any one of claims 43 to 55.
57. The compound or salt according to claim 56, wherein Z is -C(O)-.
58. B is phenyl, naphthyl, C 3~10 cycloalkyl, a 5- to 6-membered monocyclic heterocycle, and a 7- to 10-membered bicyclic heterocycle, any of which is optionally substituted, the compound or salt according to any one of claims 43 to 57.
59. The compound or salt according to claim 58, wherein B is selected from phenyl, naphthyl, cyclopropyl, cyclohexyl, bicyclo[2.2.2]octane, adamantane, thiazole, pyrrole, pyrazole, pyridine, pyrimidine, pyrazine, indole, indazole, benzimidazole, indoline, azaindole, azaindoline, 1,3-dihydrobenzo[c]isothiazole, tetrahydropyran, azetidine, pyrrolidine, piperidine, quinuclidine, azepane, and 8-azabicyclo[3.2.1]octane, any of which is optionally substituted.
60. The compound or salt according to claim 59, wherein B is selected from phenyl, cyclohexyl, pyrazole, pyridine, indole, indazole, benzimidazole, indoline, 1,3-dihydrobenzo[c]isothiazole, pyrrolidine, piperidine, pyrrolidine, and piperidine, any of which is optionally substituted.
61. The compound or salt according to any one of claims 43 to 60, wherein B is substituted with one, two, or three substituents.
62. The compound or salt according to claim 61, wherein B is substituted with two or three substituents.
63. Any substituent on B is, independently for each occurrence, halogen, -OR 17 -SR 17 , -N(R 17 ) 2 , -C(O)R 17 , -C(O)OR 17 , -OC(O)R 17 , -OC(O)N(R 17 ) 2 , -C(O)N(R 17 ) 2 、-N(R 17 )C(O)R 17 、-N(R 17 )C(O)OR 17 、-N(R 17 )C(O)N(R 17 ) 2 、-N(R 17 )C(S)N(R 17 ) 2 、-N(R 17 )S(O) 2 (R 17 )、-S(O)R 17 、-S(O) 2 R 17 、-S(O) 2 N(R 17 ) 2 、及び-CN、 C 1~6 alkyl optionally substituted with one or more substituents independently selected from the following: halogen, -OR 17 , -SR 17 , -N(R 17 ), 2 , -C(O)R 17 , -N(R 17 ),C(O)R 17 , -N(R 17 ),C(O)OR 17 , -N(R 17 ),S(O 2 (R 17 ), -S(O 2 ),N(R 17 ), 2 , =O, -CN, and C 3~10 A carbon ring and a 3- to 10-membered heterocyclic ring, each of which is independently selected from halogen, C 1~6 alkyl, C 1~6 haloalkyl, -OR 17 , -SR 17 , -N(R 17 ), -C(O)R 2 , -C(O)OR 17 , -C(O)N(R 17 ), -N(R 17 ), -N(R 2 ), -N(R 17 ), -S(O) 2 (R 17 ), -S(O) 2 R 17 , =O, =S, and -CN, and optionally substituted with one or more substituents independently selected from the group consisting of C 3~10 A carbon ring and a 3- to 10-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from the following: halogen, -OR 17 , -SR 17 , -N(R 17 ), 2 , -C(O)R 17 , -C(O)OR 17 , -C(O)N(R 17 ), 2 , -(R 17 ), -S(O) 2 (R 17 ), -S(O)R 17 , -S(O) 2 R 17 , =O, =S, -CN, and, C 1~6 an alkyl optionally substituted with one or more substituents independently selected from halogen, -OR 17 , -SR 17 , -N(R 17 ), 2 =O, =S, and -CN, the compound or salt according to any one of claims 43 to 62
64. Any substituent on B is, independently for each occurrence, halogen, -OR 17 , -N(R 17 ), 2 , -C(O)R 17 , -C(O)N(R 17 ), 2 , -N(R 17 ),S(O) 2 (R 17 ), -S(O) 2 R 17 , and -CN, C 1~6 an alkyl optionally substituted with one or more substituents independently selected from halogen and a 3- to 10-membered heterocyclic ring, wherein the 3- to 10-membered heterocyclic ring is optionally substituted with one or more substituents independently selected from halogen, C 1~6 alkyl, and C 1~6 haloalkyl, and C 3~10 a carbon ring and a 3- to 10-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from halogen, C 1~6 alkyl, and C 1~6 haloalkyl, the compound or salt according to claim 63, selected from those optionally substituted with one or more substituents independently selected from the group consisting of
65. Any substituent on B is, independently for each occurrence, Halogen, -N(R 17 ), 2 -N(R 17 ), -N(R 2 )(R 17 ), and -CN, C 1~6 an alkyl optionally substituted with one or more substituents independently selected from halogen and a 3- to 10-membered heterocyclic ring, wherein the 3- to 10-membered heterocyclic ring is optionally substituted with one or more substituents independently selected from halogen and C 1~6 an alkyl, and A 3- to 10-membered complex ring, which is C 1~6 Optionally substituted with one or more substituents independently selected from alkyl and C 1~6 The compound or salt according to claim 64, selected from those optionally substituted with haloalkyl.
66. R 17 is, independently, for each occurrence, hydrogen, C 1~6 an alkyl optionally substituted with one or more substituents independently selected from halogen, -OR 21 , -SR 21 , -N(R 21 ), 2 and -CN, and C 3~10 A carbon ring and a 3- to 10-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from halogen, C 1~6 alkyl, C 1~6 haloalkyl, -OC(O)N(R 21 ) 2 , and C 3~6 The compound or salt according to any one of claims 43 to 65, which is selected from those optionally substituted with one or more substituents independently selected from a carbon ring.
67. R 21 is independently, for each occurrence, hydrogen and C 1~6 alkyl, a compound or salt according to any one of claims 43 to 66.
68. Any substituent on B is, independently, for each occurrence, halogen, C 1~6 alkyl, C 1~6 haloalkyl, O-C 1~6 alkyl, -O-C 1~6 haloalkyl, =O, -CN, acetyl, difluoroacetyl, 【Chemical 22】 The compound or salt according to claim 63, selected from
69. B is 【Chemical 23】 【Chemical 24】 【Chemical Formula 25】 The compound or salt according to any one of claims 43 to 57, selected from
70. B is 【Chemical 26】 The compound or salt according to any one of claims 43 to 57, selected from
71. B is 【Chemical 27】 【Chemical formula 28】 【Chemical formula 29】 The compound or salt according to any one of claims 43 to 57, selected from
72. C is phenyl, a 5- to 6-membered monocyclic heterocyclic ring, or a 7- to 10-membered bicyclic heterocyclic ring, each of which is optionally substituted, the compound or salt according to any one of claims 43 to 70.
73. C is selected from phenyl, pyridine, pyridin-2-one, pyrimidon, pyrimidinedione, pyrazine, pyridazin-3-one, isoquinoline, naphthyridine, phthalazine, naphthyridin-2-one, 5,6,7,8-tetrahydronaphthyridin-2-one, triazolo[1,5-a]pyrazine, imidazo[1,2-a]pyrazine, pyrazolo[1,5-a]pyrazine, pyrido[4,3-d]pyrimidine-2,4-dione, pyrido[3,4-d]pyrimidine-2,4-dione, quinazoline-2,4-dione, quinolin-2-one, 3,4-dihydroquinolin-2-one, isoindolin-1-one, and 1,3-dihydro-benzo[d]imidazol-2-one, each of which is optionally substituted, the compound or salt according to claim 71.
74. Any optional substituent on said one or more C's is, independently, each time it occurs, halogen, -OR 18 , -SR 18 , -N(R 18 ), 2 , -C(O)R 18 , -C(O)OR 18 , -C(O)N(R 18 ), 2 , -S(O)R 18 , -S(O) 2 R 18 , -NO 2 , =O, =S, and -CN, C 1~6 alkyl and C 2~6 alkenyl, each of which is halogen, -OR 18 , -SR 18 , -N(R 18 ), -C(O)R 2 , -C(O)OR 18 , -OC(O)R 18 , -OC(O)N(R 18 ), -C(O)N(R 18 ), -N(R 2 ), -C(O)N(R 18 ), -N(R 2 ), -N(R 18 ), -N(R 18 ), -N(R 18 ), -N(R 18 ), -N(R 18 ), -N(R 18 ), -N(R 2 ), -N(R 18 ), -N(R 18 ), -N(R 2 ), -N(R 18 ), -N(R 2 ), -S(O) 18 ), -S(O) 2 N(R 18 ), -NO 2 , =O, =S, -CN, and one or more substituents independently selected from halogen, C 2 alkyl, and C 1~4 alkyl, and optionally substituted with one or more substituents independently selected from C 1~4 haloalkyl, a 3- to 6-membered heterocyclic ring optionally substituted with one or more substituents independently selected therefrom, and C 3~6 a carbon ring and a 3- to 6-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from halogen, C 1~6 alkyl, and C 1~6 haloalkyl, the compound or salt according to any one of claims 1 to 73.
75. Any optional substituent on said C is, independently, each time it occurs, halogen, -OR 18 , -N(R 18 ), 2 , =O, and -CN, C 1~6 alkyl and C 2~6 alkenyl, each of which is halogen, -OR 18 , -N(R 18 ), 2 =O, -CN, and one or more substituents independently selected from halogen, C 1~4 alkyl, and C 1~4 haloalkyl, and optionally substituted with one or more substituents independently selected from 3- to 6-membered heterocycles, and C 3~6 A carbon ring and a 3- to 6-membered heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from halogen, C 1~6 alkyl, and C 1~6 haloalkyl, the compound or salt according to claim 74, which is selected from those optionally substituted with one or more substituents independently selected from the group consisting of
76. R 18 is, independently, for each occurrence, hydrogen and C 1~6 alkyl, a compound or a salt according to any one of claims 43 to 75.
77. Any optional substituent on said C is, independently, for each occurrence, halogen, =O, -N(CH 3 ) 2、 C 1~6 alkyl, C 2~6 alkenyl, C 1~6 haloalkyl, -O-C 1~6 alkyl, -O-C 1~6 haloalkyl, 【Chemical Formula 30】 selected from, the compound or salt according to any one of claims 43 to 74.
78. C is 【Chemical 31】 【Chemical 32】 selected from, the compound or salt according to any one of claims 43 to 70.
79. C is 【Chemical 33】 selected from, the compound or salt according to any one of claims 43 to 70.
80. C is 【Chemical 34】 【Chemical 35】 【Chemical Formula 36】 【Chemical 37】 【Chemical 38】 【Chemical 39】 【Chemical 40】 【Chemical 41】 【Chemical 42】 【Chemical 43】 selected from, the compound or salt according to any one of claims 43 to 71.
81. The compound or salt of formula I or formula (I-a) is selected from the compounds or salts of Table 1, Table 2, Table 3, Table 4, Table 14, Table 15, Table 16, Table 17, Table 18, Table 19, Table 20, Table 21, Table 22, Table 23, Table 24, Table 25, Table 26, Table 27, or Table 28, the compound or salt according to claim 43.
82. A pharmaceutical composition comprising a pharmaceutically acceptable excipient and the compound or salt according to any one of claims 1 to 81.
83. A method thereof in a subject in need of modulation of alpha4beta7 integrin, the method comprising administering to the subject the compound or salt according to any one of claims 1 to 81 or the pharmaceutical composition according to claim 82.
84. A method of treating an inflammatory disease or condition, the method comprising administering to a subject in need thereof the compound or salt according to any one of claims 1 to 81 or the pharmaceutical composition according to claim 82.
85. The method according to claim 84, wherein the inflammatory disease or condition is selected from inflammatory bowel disease, ulcerative colitis, Crohn's disease, graft-versus-host disease, type 1 diabetes, immune-mediated colitis, checkpoint inhibitor-induced colitis, and primary sclerosing cholangitis.
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