Quinolinone amide compounds and their uses
Quinolinone amide compounds address the limitations of current HCM treatments by targeting underlying causes, improving ventricular function, and reducing the risk of complications through pharmaceutical interventions.
Patent Information
- Authority / Receiving Office
- JP · JP
- Patent Type
- Applications
- Current Assignee / Owner
- EDGEWISE THERAPEUTICS INC
- Filing Date
- 2024-03-26
- Publication Date
- 2026-05-11
AI Technical Summary
Current medical treatments for heart diseases, particularly hypertrophic cardiomyopathy (HCM), are limited in efficacy and often focus on symptom relief rather than addressing the underlying causes, with many patients requiring invasive procedures that carry significant morbidity and mortality risks.
Development of pharmaceutical compositions comprising quinolinone amide compounds and their pharmaceutically acceptable salts, which target the underlying causes of heart diseases such as HCM, improving ventricular relaxation, reducing left ventricular hypertrophy, and promoting healthy ventricular remodeling.
The compounds effectively modify the natural history of HCM and related cardiac disorders by reducing the risk of complications like sudden cardiac death, atrial fibrillation, and the need for invasive therapies, while improving diastolic function and ventricular filling.
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Figure 2026514388000001_ABST
Abstract
Description
[Technical Field]
[0001] cross reference This application claims the benefit of U.S. Provisional Patent Application No. 63 / 492,441, filed on 27 March 2023, which is incorporated herein by reference in its entirety. [Background technology]
[0002] Background of the Invention More than 80 million people suffer from one or more forms of heart disease, which is a leading cause of death in the population, with nearly 18 million deaths each year. The development of heart disease can be due to either genetic characteristics or lifestyle. The cardiomyocyte is involuntary striated muscle that has electrical impulses in the form of cardiac action potentials. Cardiac action potentials induce the release of calcium from the sarcoplasmic reticulum. Cardiomyopathy is a disease of the cardiomyocyte that can result in symptoms including but not limited to heart failure, irregular heartbeat, short respiration, fatigue, and weakness, and those affected are at increased risk of sudden cardiac death.
[0003] Many medical treatments for heart disease are limited to treating symptoms rather than addressing the underlying causes of the disease. Furthermore, some treatments become less effective as the duration of the disease increases. Therefore, there remains a need to develop novel compounds for improved treatment of heart disease.
[0004] Hypertrophic cardiomyopathy (HCM) is a chronic, progressive disease of the cardiac sarcomere. The etiology of HCM is multifactorial; a significant proportion of affected individuals have at least one mutation in a gene encoding cardiac sarcomeric proteins. Regardless of the cause of HCM, in many cases, excessive myosin-actin cross-bridge formation during systole and diastole leads to hyperkinetic contraction and relaxation disorders. Over time, this excessive stress leads to tissue remodeling, histologically characterized by myocyte hypertrophy, myofilamentous disorder, microvascular remodeling, and fibrosis. HCM can be hereditary (e.g., genetic) or non-hereditary. HCM includes hyperosmotic, monogenic, autosomal dominant cardiomyopathy. Such HCM can be caused by one or more of the more than 1,000 known point mutations in any one of the proteins contributing to the sarcomere, the functional unit of the cardiomyocyte. It is known that approximately 1 in 500 individuals in the general population have left ventricular hypertrophy that cannot be explained by other known causes (e.g., hypertension or valvular heart disease), and that many of these individuals may have HCM once other hereditary causes (e.g., lysosomal storage disorders), metabolic, or invasive causes have been ruled out.
[0005] Pharmacological treatments for HCM are limited, and the symptoms of many patients are empirically managed with beta-blockers, non-dihydropyridine calcium channel blockers, and / or disopyramides. None of these agents are labeled for the treatment of HCM, and essentially, rigorous clinical trial evidence to guide their use is unavailable. In approximately 60% of patients with HCM, left ventricular outflow tract obstruction impairs blood flow and creates a pressure gradient between the LV lumen and the aorta. In patients with hemodynamically significant outflow tract obstruction (gradient > 50 mmHg), surgical myocardial resection or alcohol septal ablation may be used to alleviate hemodynamic obstruction, although clinical morbidity and mortality are significant. Novel therapeutic agents and methods are provided herein to address the long-standing need for improved treatment of HCM and related cardiac disorders. [Overview of the project] [Means for solving the problem]
[0006] Summary of the Invention In certain aspects, this disclosure provides a pharmaceutical composition comprising a compound or salt disclosed herein and a pharmaceutically acceptable additive. This disclosure provides compounds and salts thereof for use in the treatment of diseases. In certain aspects, this disclosure provides compounds of formulas (I), (II-A), (IV), and (III), their pharmaceutical compositions, and methods of use in the treatment of diseases. In some aspects, a method of treating a heart disease may include the step of administering one of the compounds or salts of formulas (I), (II-A), (IV), or (III) to an individual in need. References
[0007] All publications, patents, and patent applications referenced herein are incorporated herein by reference to the same extent as each individual publication, patent, or patent application is specifically incorporated by reference. [Modes for carrying out the invention]
[0008] Detailed description of the invention Preferred embodiments of the present invention are shown and described herein, but it will be apparent to those skilled in the art that such embodiments are provided only as examples. Many variations, modifications, and substitutions can now be conceived by those skilled in the art without departing from the present invention. It should be understood that various modifications to the embodiments of the present invention described herein may be used in carrying out the present invention. The following claims define the scope of the present invention, and methods and structures within the scope of these claims, as well as their equivalents, are intended to be covered by the claims.
[0009] In a particular context, the present disclosure provides a method for treating a heart disease in an individual requiring treatment for the heart disease, the method comprising the step of administering an effective amount of a compound of formula (I), (II-A), (IV), or (III).
[0010] Diseases treated by the methods described herein include, but are not limited to, cardiomyopathy, hypertrophic cardiomyopathy (HCM), abnormal heart rhythms, aortic disease, Marfan syndrome, coronary artery disease, heart attack, heart failure, rhematic heart disease, peripheral vascular disease, stroke, deep vein thrombosis, and pulmonary embolism.
[0011] Cardiomyopathy is a heart disease in which the heart may become abnormally enlarged, thickened, and / or stiffened, and may have few or no symptoms in its early stages. As the disease progresses, symptoms include, but are not limited to, shortness of breath, fatigue, arrhythmias, syncope, and the development of heart failure. Types of cardiomyopathy include, but are not limited to, arrhythmic right ventricular dysplasia, dilated cardiomyopathy, hypertrophic cardiomyopathy, restrictive cardiomyopathy, and takotsubo cardiomyopathy.
[0012] Hypertrophic cardiomyopathy (HCM) can be hereditary (e.g., genetic) or non-hereditary (e.g., non-genetic). HCM can be obstructive or non-obstructive. Hereditary hypertrophic cardiomyopathy (HCM) includes a group of hyperosmotic, monogenic, autosomal dominant cardiomyopathy disorders. HCM can be caused by one or more of the more than 1,000 known point mutations in any one of the proteins that contribute to sarcomeres, the functional units of cardiomyocytes.
[0013] In approximately two-thirds of HCM subjects, the left ventricular outflow tract (LVOT), the pathway through which blood flows out of the heart, is obstructed by hypertrophied and diseased muscle, restricting blood flow from the heart to other parts of the body (obstructive HCM). In other subjects, the hypertrophied myocardium does not obstruct the LVOT, and the disease is driven by diastolic dysfunction resulting from hypertrophied and hardened myocardium (non-obstructive HCM). In both obstructive and non-obstructive HCM subjects, exertion can lead to fatigue or shortness of breath, impairing the subject's ability to participate in daily living activities. HCM is also associated with an increased risk of atrial fibrillation, stroke, heart failure, and sudden cardiac death.
[0014] While currently available treatments for HCM may be varied in their effectiveness in alleviating symptoms, their efficacy may decrease as the duration of the disease increases. Therefore, patients may be empirically managed with beta-blockers, non-dihydropyridine calcium channel blockers, and / or disopyramides. Mabacamten may also be used. In approximately 60% of patients with HCM, obstruction of the left ventricular outflow tract impairs blood flow and creates a pressure gradient between the LV lumen and the aorta. In patients with hemodynamically significant outflow tract obstruction (gradient > 50 mmHg), surgical myocardial resection or alcohol septal ablation may be used to alleviate hemodynamic obstruction, although clinical morbidity and mortality are significant. Novel therapeutic agents and methods addressing the long-standing need for improved treatment of HCM and related cardiac disorders are provided herein.
[0015] The compounds of the present invention, or their pharmaceutically acceptable salts, may modify the natural history of HCM and other diseases, rather than merely temporarily alleviating symptoms. The mechanisms by which they provide clinical benefit to HCM patients may be extended to patients with other forms of heart disease that share similar pathophysiology, with or without demonstrable genetic influences. For example, effective treatment of HCM by improving ventricular relaxation during diastole may also be effective in a broader population characterized by diastolic dysfunction. The compounds of the present invention, or their pharmaceutically acceptable salts, may specifically target the underlying causes of these conditions or act on other downstream pathways. Thus, the compounds of the present invention, or their pharmaceutically acceptable salts, may also benefit patients with diastolic heart failure with preserved ejection fraction, ischemic heart disease, angina pectoris, or restrictive cardiomyopathy. The compounds of the present invention or their pharmaceutically acceptable salts may also promote healthy ventricular remodeling of left ventricular hypertrophy resulting from volumetric or pressure overload (e.g., chronic mitral regurgitation, chronic aortic stenosis, or chronic systemic hypertension) in conjunction with treatments aimed at correcting or mitigating the primary cause of volumetric or pressure overload (valve repair / replacement, effective antihypertensive treatment). By reducing left ventricular filling pressure, the compounds may reduce the risk of pulmonary edema and respiratory failure. Reducing or eliminating functional mitral regurgitation and / or lowering left atrial pressure may reduce the risk of paroxysmal or permanent atrial fibrillation, and consequently reduce the associated risk of arterial thromboembolic complications, including but not limited to cerebral artery embolic stroke. Reducing or eliminating either dynamic and / or static left ventricular outflow tract obstruction may reduce the likelihood of needing either surgical or percutaneous septal reduction therapy, which carries its associated risk of short-term and long-term complications. The compound or its pharmaceutically acceptable salts may reduce the severity of chronic ischemic conditions associated with HCM, thereby reducing the risk of sudden cardiac death (SCD) or its equivalent (frequent and / or recurrent ICD discharge) and / or the need for potentially toxic antiarrhythmic drugs in patients with implantable cardioverter-defibrillators.The compound or its pharmaceutically acceptable salt may be useful in reducing or eliminating the need for concomitant medications that carry their attendant potential toxicity, drug-drug interactions, and / or side effects. The compound or its pharmaceutically acceptable salt may reduce interstitial myocardial fibrosis and / or slow its progression, and may halt or reverse left ventricular hypertrophy. Definitions
[0016] 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.
[0017] As used herein and in the claims, the singular forms "a", "an", and "the" include plural referents unless the context clearly dictates otherwise.
[0018] The term "C x~y " or "C x ~C y " (when used with a chemical moiety such as alkyl, alkenyl, or alkynyl), means a group containing some carbon atoms from x or more carbon atoms to y or fewer carbon atoms in the chemical moiety, provided the following. The terms "C x~y " or "C x ~C y " are not meant to limit the number of carbon atoms that can be attached to the chemical moiety when the chemical moiety is substituted with a second chemical moiety. For example, the term "C 1~6 alkyl" or "C1~C6 alkyl" refers to a substituted or unsubstituted saturated hydrocarbon group containing a straight-chain alkyl group (e.g., a linear alkyl group) and a branched alkyl group having 1, 2, 3, 4, 5, or 6 carbon atoms, and any substituents of C 1~6 alkyl may have any number of carbon atoms, including a plurality. For example, when C 1~6 alkyl is optionally substituted with a second chemical moiety containing 2 carbon atoms, C 1~6It should be understood that alkyl groups can contain between 1 and 8 carbon atoms.
[0019] The term “C x~y "Alkenil" and "C x~y "Alkynyl" refers to a substituted or unsubstituted unsaturated aliphatic group that is similar in length and possible substitutions to the aforementioned alkyl groups, but each contains at least one double or triple bond.
[0020] "Amino" refers to the -NH2 portion.
[0021] "Cyano" refers to the -CN portion.
[0022] "Nitro" refers to the -NO2 portion.
[0023] "Oxa" refers to the -O- part.
[0024] "Oxo" refers to the O part.
[0025] "Thioxo" refers to the S portion.
[0026] "Imino" refers to the =NH part.
[0027] "Oxymo" refers to the =N-OH portion.
[0028] "Hydrazino" refers to the =N-NH2 portion.
[0029] "Alkyl" refers to a fully saturated, linear (e.g., linear) or branched (e.g., nonlinear) hydrocarbon moiety consisting only of carbon and hydrogen atoms. In certain embodiments, "alkyl" contains 1 to 15 carbon atoms (e.g., C1 to C15). 15 Alkyl). In certain embodiments, alkyl contains 1 to 13 carbon atoms (e.g., C1 to C13). 13Alkyl). In certain embodiments, the alkyl contains 1 to 8 carbon atoms (e.g., C1-C8 alkyl). In certain embodiments, the alkyl contains 1 to 6 carbon atoms (e.g., C1-C6 alkyl). In other embodiments, the alkyl contains 1 to 5 carbon atoms (e.g., C1-C5 alkyl). In other embodiments, the alkyl contains 1 to 4 carbon atoms (e.g., C1-C4 alkyl). In other embodiments, the alkyl contains 1 to 3 carbon atoms (e.g., C1-C3 alkyl). In other embodiments, the alkyl contains 1 to 2 carbon atoms (e.g., C1-C2 alkyl). In other embodiments, the alkyl contains 1 carbon atom (e.g., C1 alkyl, e.g., methyl). In other embodiments, the alkyl contains 5 to 15 carbon atoms (e.g., C5-C 15 Alkyl). In other embodiments, the alkyl group contains 5 to 8 carbon atoms (e.g., C5-C8 alkyl). In other embodiments, the alkyl group contains 2 to 5 carbon atoms (e.g., C2-C5 alkyl). In other embodiments, the alkyl group contains 3 to 5 carbon atoms (e.g., C3-C5 alkyl). In other embodiments, the alkyl group is selected from methyl, ethyl, 1-propyl (n-propyl), 1-methylethyl (2-propyl, iso-propyl), 1-butyl (n-butyl), 1-methylpropyl (sec-butyl), 2-methylpropyl (iso-butyl), 1,1-dimethylethyl (tert-butyl), and 1-pentyl (n-pentyl). The alkyl group is bonded to the rest of the molecule by a single bond.
[0030] "Aminoalkyl" refers to a portion bonded via a nitrogen atom in the form of -N(H)(alkyl) or N(alkyl)(alkyl). When the portion is N(alkyl)(alkyl), the two alkyl groups bonded to the nitrogen may be the same alkyl group or different alkyl groups.
[0031] "Alkoxy" refers to the part of the formula -O-alkyl (alkyl is an alkyl chain as defined earlier) that is bonded via an oxygen atom.
[0032] An "alkenyl" refers to a linear (e.g., linear) or branched (e.g., nonlinear) hydrocarbon moiety consisting only of carbon and hydrogen atoms, wherein the moiety contains at least one carbon-carbon double bond. In certain embodiments, an alkenyl contains 2 to 12 carbon atoms. In certain embodiments, an alkenyl contains 2 to 8 carbon atoms. In other embodiments, an alkenyl contains 2 to 4 carbon atoms. Alkenyls are bonded to the rest of the molecule by single bonds, such as ethenyl (e.g., vinyl), propa-1-enyl (e.g., allyl), buta-1-enyl, penta-1-enyl, penta-1,4-dienyl, etc.
[0033] "Alkynyl" refers to a linear (e.g., linear) or branched (e.g., nonlinear) hydrocarbon portion consisting only of carbon and hydrogen atoms, wherein the portion contains at least one carbon-carbon triple bond. In some embodiments, the alkynyl contains 2 to 12 carbon atoms. In some embodiments, the alkynyl optionally further contains at least one carbon-carbon double bond. In certain embodiments, the alkynyl contains 2 to 8 carbon atoms. In other embodiments, the alkynyl contains 2 to 6 carbon atoms. In other embodiments, the alkynyl contains 2 to 4 carbon atoms. The alkynyl is bonded to the rest of the molecule by single bonds, such as ethynyl, propynyl, butynyl, pentynyl, hexynyl, etc.
[0034] An "alkylene" or "alkylene chain" refers to a linear (e.g., straight) or branched (e.g., nonlinear) divalent hydrocarbon portion. An "alkylene" or "alkylene chain" can link a portion of a molecule to a second portion. An "alkylene" or "alkylene chain" consists only of carbon and hydrogen atoms (substitution of alkylene with one or more substituents containing non-hydrogen atoms such as N, O, and S may be specified). An "alkylene" or "alkylene chain" does not have to contain unsaturation (even if it is an alkylene bond to the rest of the molecule). In certain embodiments, an "alkylene" or "alkylene chain" contains 1 to 12 carbon atoms, such as methylene, ethylene, propylene, n-butylene, etc. An alkylene chain can be bonded to a portion of a molecule via one single bond and to a second portion via one single bond. The bonding points of the alkylene chain to the rest of the molecule and the second part can be via one carbon atom in the alkylene chain or via any two carbon atoms in the alkylene. In certain embodiments, the alkylene contains 1 to 8 carbon atoms (e.g., C1-C8 alkylene). In other embodiments, the alkylene contains 1 to 5 carbon atoms (e.g., C1-C5 alkylene). In other embodiments, the alkylene contains 1 to 4 carbon atoms (e.g., C1-C4 alkylene). In other embodiments, the alkylene contains 1 to 3 carbon atoms (e.g., C1-C3 alkylene). In other embodiments, the alkylene contains 1 to 2 carbon atoms (e.g., C1-C2 alkylene). In other embodiments, the alkylene contains 1 carbon atom (e.g., C1 alkylene). In other embodiments, the alkylene contains 5 to 8 carbon atoms (e.g., C5-C8 alkylene). In other embodiments, the alkylene contains 2 to 5 carbon atoms (e.g., C2-C5 alkylene). In other embodiments, the alkylene contains 3 to 5 carbon atoms (e.g., C3-C5 alkylene).
[0035] An "alkenylene" or "alkenylene chain" refers to a linear (e.g., straight) or branched divalent hydrocarbon portion. An "alkenylene" or "alkenylene chain" can link a portion of a molecule to a second portion. An "alkenylene" or "alkenylene chain" consists only of carbon and hydrogen atoms (substitutions of alkenylene with one or more substituents containing non-hydrogen atoms such as N, O, and S may be specified). An "alkenylene" or "alkenylene chain" contains at least one carbon-carbon double bond. In certain embodiments, an "alkenylene" or "alkenylene chain" contains 2 to 12 carbon atoms. An alkenylene chain can be bonded to a portion of a molecule via one single bond and to a second portion via one single bond. The bonding points of the alkenylene chain to the rest of the molecule and to the second portion can be via one carbon atom in the alkenylene chain or via any two carbon atoms in the alkenylene chain. In certain embodiments, the alkenylene contains 2 to 8 carbon atoms (e.g., C2-C8 alkenylene). In other embodiments, the alkenylene contains 2 to 5 carbon atoms (e.g., C2-C5 alkenylene). In other embodiments, the alkenylene contains 2 to 4 carbon atoms (e.g., C2-C4 alkenylene). In other embodiments, the alkenylene contains 2 to 3 carbon atoms (e.g., C2-C3 alkenylene). In other embodiments, the alkenylene contains 5 to 8 carbon atoms (e.g., C5-C8 alkenylene). In other embodiments, the alkenylene contains 2 to 5 carbon atoms (e.g., C2-C5 alkenylene). In other embodiments, the alkenylene contains 3 to 5 carbon atoms (e.g., C3-C5 alkenylene).
[0036] An "alkynylene" or "alkynylene chain" refers to a linear (e.g., straight) or branched divalent hydrocarbon portion. An "alkynylene" or "alkynylene chain" can link a portion of a molecule to a second portion. An "alkynylene" or "alkynylene chain" consists only of carbon and hydrogen (substitutions of alkynylene with one or more substituents containing non-hydrogen atoms such as N, O, and S may be specified). An "alkynylene" or "alkynylene chain" contains at least one carbon-carbon triple bond. In certain embodiments, an "alkynylene" or "alkynylene chain" contains 2 to 12 carbon atoms. An alkynylene chain can be bonded to a portion of a molecule via one single bond and to a second portion via one single bond. The bonding points of the alkynylene chain to the rest of the molecule and the second portion can be via one carbon atom in the alkynylene chain or via any two carbon atoms in the alkynylene chain. In certain embodiments, the alkynylene contains 2 to 8 carbon atoms (e.g., C2-C8 alkynylene). In other embodiments, the alkynylene contains 2 to 5 carbon atoms (e.g., C2-C5 alkynylene). In other embodiments, the alkynylene contains 2 to 4 carbon atoms (e.g., C2-C4 alkynylene). In other embodiments, the alkynylene contains 2 to 3 carbon atoms (e.g., C2-C3 alkynylene). In other embodiments, the alkynylene contains 2 carbon atoms (e.g., C2 alkynylene). In other embodiments, the alkynylene contains 5 to 8 carbon atoms (e.g., C5-C8 alkynylene). In other embodiments, the alkynylene contains 3 to 5 carbon atoms (e.g., C3-C5 alkynylene).
[0037] The term "carbocyclic ring," as used herein, refers to a saturated or unsaturated (e.g., aromatic or unaromatically unsaturated) ring or ring system in which each atom of the ring is carbon. The term "carbocyclic ring" includes "aryl," "cycloalkenyl," and "cycloalkyl." For example, the term "carbocyclic ring" includes 3- to 12-membered monocyclic rings (e.g., 3- to 10-membered monocyclic rings) and 4- to 20-membered polycyclic ring systems (e.g., 5- to 15-membered spiropolycyclic ring systems, 5- to 15-membered bridging polycyclic ring systems, or 4- to 15-membered condensed polycyclic ring systems). For example, a carbocyclic ring is a 4- to 15-membered bicyclic ring (e.g., 5- to 15-membered spirodicyclic rings, 5- to 15-membered bridging bicyclic ring systems, or 4- to 15-membered condensed bicyclic ring systems). For example, a carbocyclic ring is a tricyclic ring system that may be bridging, condensed, spiro, or a combination thereof. For example, examples of carbocyclic rings include tetracyclic ring systems that can be bridged, condensed, spiro, or a combination thereof. For example, examples of carbocyclic rings include condensed and bridged ring systems, condensed and spiro ring systems, bridged and spiro ring systems, and condensed and bridged ring systems that are also spiro. Each ring in a polycyclic carbocyclic ring may be selected from saturated and unsaturated (e.g., aromatic or non-aromatic unsaturated) rings. In exemplary embodiments, the aromatic ring of a polycyclic carbocyclic ring, e.g., phenyl, may be condensed to a saturated or unsaturated ring (e.g., cyclohexane, cyclopentane, cyclohexene, or phenyl). Examples of polycyclic carbocyclic rings include any combination of saturated and unsaturated (e.g., aromatic or non-aromatic unsaturated) rings, as long as the bond valency allows. For example, a polycyclic carbocyclic ring may be a spiro-bicyclic ring, e.g., spiropentane. For example, polycyclic carbocyclic rings include any combination of ring sizes such as 2-2 spiro ring systems (e.g., spiro[2.2]pentane), 3-3 spiro ring systems, 4-4 spiro ring systems, 4-5 fused ring systems (e.g., bicyclo[4.5.0] fused ring systems), 5-5 fused ring systems, 5-6 fused ring systems, 6-6 fused ring systems (e.g., naphthalene), 5-7 fused ring systems, 6-7 fused ring systems, 5-8 fused ring systems, and 6-8 fused ring systems.Examples of carbocyclic compounds include cyclopentyl, cyclohexyl, cyclohexenyl, adamantyl, phenyl, indanyl, naphthyl, trans-bicyclo[4.4.0]decane, cis-bicyclo[4.4.0]decane, spiro[3.4]octane, fluorantene, and bicyclo[1.1.1]pentanyl.
[0038] The term "aryl" refers to an aromatic monocyclic or aromatic polycyclic hydrocarbon ring system containing a delocalized (4n+2)π-electron system of at least one ring structure that obeys Hückel's rule, where n is an integer equal to or greater than 0. In some embodiments, the aromatic monocyclic or aromatic polycyclic hydrocarbon ring system contains only hydrogen and carbon atoms. In some embodiments, the aromatic monocyclic or polycyclic system contains 3 to 20 carbon atoms. In some embodiments, at least one of the rings in the polycyclic aromatic ring system is aromatic. In some embodiments, the aromatic monocyclic or aromatic polycyclic hydrocarbon ring system contains a delocalized (4n+2)π-electron system of a ring structure that obeys Hückel's rule. In some embodiments, ring systems from which an aryl group is derived include, but are not limited to, groups such as benzene, fluorene, indan, indene, anthracene, tetralin, and naphthalene. In some embodiments, the aryl substituent is uncharged (e.g., neutral). In some embodiments, the aryl substituent is charge-free. In some embodiments, the aryl substituent does not carry a net charge. In some embodiments, the aryl substituent does not carry a net charge and is not zwitterionic. In some embodiments, none of the carbon atoms of the aryl substituent are charged. In some embodiments, none of the carbon atoms of the aryl substituent are charged.
[0039] The term "cycloalkyl" refers to a saturated ring in which each atom of the ring is carbon. Examples of cycloalkyls include monocyclic and polycyclic rings such as 3-10 membered monocyclic rings, 5-12 membered bicyclic rings, 5-12 membered spirodicyclic rings, and 5-12 membered bridging rings. In certain embodiments, the cycloalkyl contains 3-10 carbon atoms. In other embodiments, the cycloalkyl contains 3-7 carbon atoms. In other embodiments, the cycloalkyl contains 5-7 carbon atoms. The cycloalkyl may be bonded to the rest of the molecule by single bonds. Examples of monocyclic cycloalkyls include, for example, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, and cyclooctyl. Examples of polycyclic cycloalkyl compounds, though not limited to these, include adamantyl, spiropentane, norbornyl (e.g., bicyclo[2.2.1]heptanyl), dekalinyl, 7,7-dimethylbicyclo[2.2.1]heptanyl, bicyclo[1.1.1]pentanyl, and spiropentane.
[0040] The term "cycloalkenyl" refers to a saturated ring in which each atom of the ring is carbon, and there is at least one double bond between any two ring carbon atoms. Examples of cycloalkenyls include monocyclic and polycyclic rings, such as 3-10 membered monocyclic rings and 4-12 membered bicyclic rings (e.g., 5-12 membered bridging bicyclic rings, 4-12 membered fused bicyclic rings, and 5-12 membered spiro-dicyclic rings). In other embodiments, cycloalkenyls contain 5-7 carbon atoms. Cycloalkenyls may be bonded to the rest of the molecule by single bonds. Examples of monocyclic cycloalkenyls include, for example, cyclopentenyl, cyclohexenyl, cycloheptenyl, and cyclooctenyl.
[0041] The term "halo," or "halogen" or "halide," means fluoro, chloro, bromo, or iodine. In some embodiments, the halo is fluoro, chloro, or bromo. In some embodiments, the halo is fluoro or chloro. In some embodiments, the halo is fluoro. In some embodiments, the halo is chloro.
[0042] The term "haloalkyl" refers to an alkyl group as previously defined, substituted with one or more halogens, such as trifluoromethyl, dichloromethyl, bromomethyl, 2,2,2-trifluoroethyl, 1-chloromethyl-2-fluoroethyl, etc. In some embodiments, the alkyl portion of the haloalkyl group is further substituted as necessary, as described herein.
[0043] The term “heterocycle,” as used herein, refers to a saturated or unsaturated (e.g., aromatic or non-aromatic unsaturated) ring or ring system in which one or more heteroatoms are members of the ring or ring system. Examples of heteroatoms include N, O, Si, P, B, and S atoms. Examples of heterocycles include 3- to 12-membered monocyclic rings (e.g., 3- to 10-membered monocyclic rings) and 4- to 20-membered polycyclic ring systems (e.g., 4- to 15-membered fused polycyclic ring systems, 5- to 15-membered spiropolycyclic ring systems, and 5- to 15-membered bridging polycyclic ring systems). Examples of heterocycles include 4- to 20-membered bicyclic ring systems (e.g., 4- to 15-membered fused bicyclic ring systems, 5- to 15-membered spirodicyclic ring systems, and 5- to 15-membered bridging bicyclic ring systems). Examples of heterocycles include tricyclic ring systems that may be bridging, fused, spiro, or combinations thereof. For example, heterocycles include tetracyclic ring systems that can be bridged, condensed, spiro, or a combination thereof. For example, heterocycles include condensed and bridged ring systems, condensed and spiro ring systems, bridged and spiro ring systems, and condensed and bridged ring systems that are also spiro. Each ring in a polycyclic heterocycle can be selected from saturated and unsaturated (e.g., aromatic or non-aromatic unsaturated) rings. Polycyclic heterocycles include any combination of saturated and unsaturated (e.g., aromatic or non-aromatic unsaturated) rings, as long as the bond valency allows. In exemplary embodiments, an aromatic ring, such as pyridyl or phenyl, can be condensed in the heterocycle to a saturated or unsaturated ring, such as cyclohexane, cyclopentane, morpholine, piperidine, or cyclohexene, as long as at least one atom in the resulting condensed ring system is a heteroatom. Examples of polycyclic heterocycles include any combination of ring sizes such as 3-3 spiro, 4-5 fused ring systems, 5-5 fused ring systems, 5-6 fused ring systems, 6-6 fused ring systems, 5-7 fused ring systems, 6-7 fused ring systems, 5-8 fused ring systems, and 6-8 fused ring systems. Examples of bicyclic heterocycles include spiro dicyclic rings, such as 5- to 12-membered spiro dicyclic rings, such as 2-oxa-6-azaspiro[3.3]heptane. In some embodiments, the heterocycle contains multiple heteroatoms. In some embodiments, the heterocycle contains nitrogen, oxygen,The heterocycle includes atoms selected from nitrogen and sulfur. In some embodiments, the heterocycle includes multiple atoms selected from nitrogen, oxygen, and sulfur. In some embodiments, the heterocycle includes one or more atoms selected from nitrogen, oxygen, and sulfur. In some embodiments, the heterocycle includes one or more atoms selected from nitrogen and oxygen. In some embodiments, the heterocycle includes one or more atoms selected from nitrogen and sulfur. In some embodiments, the heterocycle includes one or more atoms selected from oxygen and sulfur. In some embodiments, the heterocycle includes one or more atoms selected from nitrogen. In some embodiments, the heterocycle includes one or more atoms selected from oxygen. In some embodiments, the heterocycle includes one or more atoms selected from sulfur. Non-limiting examples of heterocycles include pyridine, pyrrole, indole, carbazole, piperidine, oxazole, morpholine, thiophene, benzothiophene, furan, tetrahydrofuran, and pyran. Non-restrictive examples of heterocyclic compounds include azepinyl, acridinyl, benzimidazolyl, benzoindolyl, 1,3-benzodioxolyl, benzofuranil, benzoxazolyl, benzo[d]thiazolyl, benzothiadiazolyl, benzo[b][1,4]dioxepinyl, benzo[b][1,4]oxazinyl, 1,4-benzodioxanil, benzonaphthofuranil, benzoxazolyl, benzodioxolyl, benzodioxynil, benzopyranil, benzopyranonil, benzofuranil, benzothienyl (benzothioff). (enyl), benzothieno[3,2-d]pyrimidinyl, benzotriazolyl, benzo[4,6]imidazo[1,2-a]pyrimidinyl, carbazolyl, cinnolinyl, cyclopenta[d]pyrimidinyl, 6,7-dihydro-5H-cyclopenta[4,5]thieno[2,3-d]pyrimidinyl, 5,6-dihydrobenzo[h]quinazolinyl, 5,6-dihydrobenzo[h]cinnolinyl, 6,7-dihydro-5H-benzo[6,7]cyclohepta[1,2-c]pyridazinyl, dibenzofuranyl, dibenzothiophenyl, furanyl, furanonyl,Flo[3,2-c]pyridinyl, 5,6,7,8,9,10-hexahydrocycloocta[d]pyrimidinyl, 5,6,7,8,9,10-hexahydrocycloocta[d]pyridazinyl, 5,6,7,8,9,10-hexahydrocycloocta[d]pyridinyl, isothiazolyl, imidazolyl, indazolyl, indolyl, indazolyl, isoindolyl, indolinyl, isoindolinyl, isoquinolyl, indolidinyl Isooxazolyl, 5,8-methano-5,6,7,8-tetrahydroquinazolinyl, naphthilidinyl, 1,6-naphthilidinol, oxadiazolyl, 2-oxoazepinyl, oxazolyl, oxyranil, 5,6,6a,7,8,9,10,10a-octahydrobenzo[h]quinazolinyl, 1-phenyl-1H-pyrrolyl, phenazinyl, phenothiazinyl, phenoxadinyl, phthalazinyl, pteridinyl, prinyl Pyrrolyl, pyrazolyl, pyrazolo[3,4-d]pyrimidinyl, pyridinyl, pyrido[3,2-d]pyrimidinyl, pyrido[3,4-d]pyrimidinyl, pyrazinyl, pyrimidinyl, pyridadinyl, pyrrolyl, quinazolinyl, quinoxalinyl, quinolinyl, isoquinolinyl, tetrahydroquinolinyl, 5,6,7,8-tetrahydroquinazolinyl, 5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrim Examples include dinyl, 6,7,8,9-tetrahydro-5H-cyclohepta[4,5]thieno[2,3-d]pyrimidinyl, 5,6,7,8-tetrahydropyrido[4,5-c]pyridazinyl, thiazolyl, thiadiazolyl, triazolyl, tetrazolyl, triazinyl, thieno[2,3-d]pyrimidinyl, thieno[3,2-d]pyrimidinyl, thieno[2,3-c]pyrimidinyl, and thiophenyl (e.g., thienyl).
[0044] In some embodiments, the heterocycle is bonded to the molecule by carbon atoms. In some embodiments, the heterocycle is bonded to the molecule by nitrogen atoms.
[0045] In some embodiments, the heterocycle comprises a portion selected from heteroaryl, heterocycloalkyl, and heterocycloalkenyl. In some embodiments, the heterocycle is heteroaryl. In some embodiments, the heterocycle is heterocycloalkyl. In some embodiments, the heterocycle is heterocycloalkenyl.
[0046] In some embodiments, the heterocycle includes atoms selected from nitrogen and oxygen. In some embodiments, the heterocycle includes atoms selected from nitrogen and sulfur. In some embodiments, the heterocycle includes atoms selected from oxygen and sulfur. In some embodiments, the heterocycle includes atoms selected from nitrogen. In some embodiments, the heterocycle includes atoms selected from oxygen. In some embodiments, the heterocycle includes atoms selected from sulfur.
[0047] In some embodiments, the heterocycle contains 1 to 8 heteroatoms. In some embodiments, the heterocycle contains 1 to 5 heteroatoms. In some embodiments, the heterocycle contains 1 to 3 heteroatoms. In some embodiments, the heterocycle contains 1 to 2 heteroatoms. In some embodiments, the heterocycle contains 1 heteroatom. In some embodiments, the heterocycle contains 2 heteroatoms. In some embodiments, the heterocycle contains 3 heteroatoms. In some embodiments, the heterocycle contains 4 heteroatoms. In some embodiments, the heterocycle contains 5 heteroatoms. In some embodiments, the heterocycle contains 6 heteroatoms.
[0048] In some embodiments, the heteroring includes 3-membered, 4-membered, 5-membered, 6-membered, 7-membered, 8-membered, 9-membered, 10-membered, 11-membered, 12-membered, 13-membered, 14-membered, or 15- to 20-membered rings. In some embodiments, the heteroring is 3- to 10-membered. In some embodiments, the heteroring is 3- to 6-membered. In some embodiments, the heteroring is 5- to 6-membered. In some embodiments, the heteroring is 9- to 10-membered. In some embodiments, the heteroring is 9- to 11-membered. In some embodiments, the heteroring is 9- to 15-membered.
[0049] In some embodiments, the heterocycle is monosubstituted, disubstituted, trisubstituted, tetrasubstituted, or pentasubstituted (e.g., with additional substituents in addition to the bond sites). In some embodiments, the total number of substituents (e.g., atoms other than hydrogen) on the heterocycle (e.g., bonded to the ring of the heterocycle) is 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, or more.
[0050] In some embodiments, one or more nitrogen atoms in a molecule or part (e.g., in a heterocycle) may be quaternized as needed, if present. In some embodiments, the heterocyclic substituent is positively charged. In some embodiments, the heterocyclic part is neutral. In some embodiments, the heterocyclic substituent is zwitterionic, and, as an alternative or addition, in some embodiments, the heterocyclic substituent is uncharged. In some embodiments, the heterocyclic substituent is not charge-bearing. In some embodiments, the heterocyclic substituent is not charge-bearing. In some embodiments, none of the atoms in the heterocyclic substituent are charge-bearing. In some embodiments, the heterocyclic substituent is neither charge-bearing nor zwitterionic. The term “heteroaryl” refers to a portion derived from an aromatic monocyclic or aromatic polycyclic cyclic system in which one or more heteroatoms are members of a cyclic system, the cyclic system comprising a delocalized cyclic (4n+2)π-electron system of at least one cyclic structure that obeys Hückel’s rule, where n is an integer equal to or greater than 0. In some embodiments, one or more heteroatoms are members of a cyclic system (e.g., an aromatic ring) that constitutes a delocalized cyclic (4n+2)π-electron system of the cyclic structure. Exemplary heteroatoms include N, O, Si, P, B, and S atoms. In some embodiments, the heteroaryl includes an aromatic ring in which one or more heteroatoms are members of a cyclic system to which one or more non-aromatic rings may be fused, each of which may contain one or more heteroatoms. In some embodiments, the heteroaryl includes one or more heteroatoms selected from nitrogen, oxygen, and sulfur. In some embodiments, the heteroaryl includes multiple heteroatoms selected from nitrogen, oxygen, and sulfur. In certain embodiments, “heteroaryl” comprises rings and ring systems containing 3 to 20 atoms. In some embodiments, “heteroaryl” comprises rings and ring systems containing 2 to 17 carbon atoms, as well as 1 to 6 heteroatoms selected from nitrogen, oxygen, and sulfur. As used herein,The heteroaryl moiety is a monocyclic or polycyclic (e.g., bicyclic, tricyclic, or tetracyclic) ring system in which at least one of the rings is aromatic and contains, for example, a delocalized (4n+2)π electron system of a ring system that follows Hückel's rule. Examples of heteroaryls include fused ring systems, bridging ring systems, and spiro ring systems. The heteroatom(s) of the heteroaryl moiety are oxidized as needed. One or more nitrogen atoms, if present, are quaternized as needed. The heteroaryl is bonded to the rest of the molecule via any atom of the ring. Examples of heteroaryls, though not limited to these, include acridinyl, benzimidazolyl, benzoindolyl, 1,3-benzodioxolyl, benzofuranil, benzoxazolyl, benzo[d]thiazolyl, benzothiadiazolyl, benzo[b][1,4]dioxepinyl, benzo[b][1,4]oxazinyl, 1,4-benzodioxanil, benzonaphthofuranil, benzoxazolyl, benzodioxolyl, benzodioxynil, benzopyranil, benzopyranonil, benzofuranil, benzothienyl (benzothiophenyl), benzothieno[3,2-d]pyrimidinyl, benzotriazolyl, benzo[4,6]imidazo[1,2-a]pyrimidinyl, carbazolyl, sinnolinyl, cyclopenta[d]pyrimidinyl, and 6,7-dihydro-5H-cyclopenta[4,5]thieno[2,3-d]. Pyrimidinyl, 5,6-dihydrobenzo[h]quinazolinyl, 5,6-dihydrobenzo[h]sinnolinyl, 6,7-dihydro-5H-benzo[6,7]cyclohepta[1,2-c]pyridazinyl, dibenzofuranyl, dibenzothiophenyl, furanyl, furo[3,2-c]pyridinyl, 5,6,7,8,9,10-hexahydrocycloocta[d]pyrimidinyl, 5,6,7,8,9,10-hexahydrocycloo Kuta[d]pyridazinyl, 5,6,7,8,9,10-hexahydrocycloocta[d]pyridinyl, isothiazolyl, imidazolyl, indazolyl, indolyl, isoindolyl, indolinyl, isoindolyl, isoquinolyl, indolidinyl, isoxazolyl, 5,8-methano-5,6,7,8-tetrahydroquinazolinyl, naphthylidinyl, 1,6-naphthylidinonyl, oxadiazolyl, oxazolyl,5,6,6a,7,8,9,10,10a-Octahydrobenzo[h]quinazolinyl, 1-phenyl-1H-pyrrolyl, phenazinyl, phenothiazinyl, phenoxadinyl, phthalazinyl, pteridinyl, purinyl, pyrrolyl, pyrazolyl, pyrazolo[3,4-d]pyrimidinyl, pyridinyl, pyrido[3,2-d]pyrimidinyl, pyrido[3,4-d]pyrimidinyl, pyrazinyl, pyrimidinyl, pyridadinyl, pyrrolyl, quinazolinyl, quinoxalinyl, quinolinyl, isoquinolinyl, tetrahydroquinolinyl, 5,6,7,8 Examples include tetrahydroquinazolinyl, 5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidinyl, 6,7,8,9-tetrahydro-5H-cyclohepta[4,5]thieno[2,3-d]pyrimidinyl, 5,6,7,8-tetrahydropyrido[4,5-c]pyridazinyl, thiazolyl, thiadiazolyl, triazolyl, tetrazolyl, triazinyl, thieno[2,3-d]pyrimidinyl, thieno[3,2-d]pyrimidinyl, thieno[2,3-c]pyrimidinyl, and thiophenyl (e.g., thienyl). In some embodiments, further examples of "heteroaryl" include 5,6,7,8-tetrahydroquinoline; 1,2,3,4-tetrahydro-1,8-naphthyridine; 6,7-dihydro-5H-cyclopenta[b]pyridine; 2,3-dihydro-1H-pyrrolo[2,3-b]pyridine; 4,5,6,7-tetrahydrobenzofuran; 4,5,6,7-tetrahydroflu[2,3-b]pyridine; 5,6-dihydro-4H-cyclopenta[b]furan; and 4,5-dihydrothieno[2,3-b]furan. In some embodiments, the heteroaryl substituent is positively or negatively charged. In some embodiments, the heteroaryl substituent is neutral. In some embodiments, the heteroaryl substituent is zwitterionic, and, as an alternative or addition, in some embodiments, the heteroaryl substituent is uncharged. In some embodiments, the heteroaryl substituent does not carry a charge. In some embodiments, the heteroaryl substituent does not carry a net charge. In some embodiments, the heteroaryl substituent does not carry a net charge and is not zwitterionic.
[0051] The term "heterocyclic ring" includes "heteroaryl," "heterocycloalkenyl," and "heterocycloalkyl."
[0052] The term "heterocycloalkyl" refers to a portion containing a saturated ring (for example, a ring in which the bonds connecting the members of the ring are only single bonds), wherein the saturated ring contains carbon atoms and one or more heteroatoms as members, and the saturated ring may be fused to, bridged to, or spiro to a further ring as it may be, the further ring may contain only carbon atoms as members, or the further ring may contain one or more heteroatoms as members. In some embodiments, the heterocycloalkyl may be covalently bonded to one or more carbocyclic or heterocyclic rings. Exemplary heteroatoms include N, O, Si, P, B, and S atoms. Examples of heterocycloalkyls include monocyclic and polycyclic rings such as 3- to 10-membered monocyclic rings, 6- to 12-membered bicyclic rings, 5- to 12-membered spirodicyclic rings, or 5- to 12-membered bridging rings. The heteroatoms of the heterocycloalkyl group are oxidized as needed. One or more nitrogen atoms, if present, are quaternized as needed. The heterocycloalkyl group is bonded to the rest of the molecule via any atom of the heterocycloalkyl group, e.g., any carbon or nitrogen atom of the heterocycloalkyl group, if the bonding valency allows. Examples of heterocycloalkyl groups, though not limited to them, include dioxolanil, thienyl[1,3]dithianil, decahydroisoquinolyl, imidazolinil, imidazolidinil, isothiazolidinil, isooxazolidinil, morpholinil, octahydroindolyl, octahydroisoindolyl, 2-oxopiperazinil, 2-oxopiperidinil, 2-oxopyrrolidinil, oxazolidinil, piperidinil, piperazinil, 4-piperidonil, pyrrolidinil, pyrazolidinil, quinuclidinil, thiazolidinil, tetrahydrofuryl, trithianil, tetrahydropyranil, thiomorpholinil, thiamorpholinil, 1-oxo-thiomorpholinil, 2-oxa-6-azaspiro[3.3]heptane, and 1,1-dioxo-thiomorpholinil. In some embodiments, the heterocycloalkyl group contains one heteroatom.In some embodiments, the heterocycloalkyl comprises one heteroatom selected from N, O, and S. In some embodiments, the heterocycloalkyl comprises multiple heteroatoms. In some embodiments, the heterocycloalkyl comprises multiple heteroatoms selected from N, O, and S.
[0053] The term "heterocycloalkenyl" refers to a portion containing an unsaturated ring (e.g., a ring having single or double bonds connecting its members), wherein the unsaturated ring contains multiple carbon atoms and one or more heteroatoms, and this unsaturated ring may be fused to, bridged to, or spiro to a further ring, which may contain only multiple carbon atoms as members, or which may contain one or more heteroatoms as members; and at least one double bond exists between two ring carbon atoms (e.g., carbon atoms that are members of this unsaturated ring). Heterocycloalkenyls do not include heteroaryl rings. Exemplary heteroatoms include N, O, Si, P, B, and S atoms. Examples of heterocycloalkenyls include monocyclic and polycyclic rings such as 3- to 10-membered monocyclic rings, 6- to 12-membered bicyclic rings, and 5- to 12-membered bridging rings. In other embodiments, the heterocycloalkenyl contains 5 to 7 ring atoms. The heterocycloalkenyl may be attached to the rest of the molecule by single bonds. Examples of monocyclic cycloalkenyls include, for example, pyrroline (dihydropyrrole), pyrazoline (dihydropyrazole), imidazoline (dihydroimidazole), triazoline (dihydrotriazole), dihydrofuran, dihydrothiophene, oxazoline (dihydroxazole), isoxazoline (dihydroisoxazole), thiazoline (dihydrothiazole), isothiazolin (dihydroisothiazole), oxadiazoline (dihydroxadiazole), thiadiazoline (dihydrothiadiazole), dihydropyridine, tetrahydropyridine, dihydropyridazine, tetrahydropyridazine, dihydropyrimidine, tetrahydropyrimidine, dihydropyrazine, tetrahydropyrazine, pyran, dihydropyran, thiopyran, dihydrothiopyran, dioxin, dihydrodioxin, oxazine, dihydrooxazine, thiaazine, and dihydrothiazine.
[0054] The "spirocyclic" part (e.g., the "spiro" part) (e.g., a spirocyclic heterocycle, a spirocyclic heterocycloalkenyl, a spirocyclic carbocycle, a spirocyclic heterocycloalkyl, a spirocyclic cycloalkenyl, or a spirocyclic cycloalkyl) is a spirocyclic system (e.g., a bicyclic, tricyclic, or tetracyclic system) in which two rings share exactly one atom. Examples of spirocyclic parts include: [ka] These include, but are not limited to, the following:
[0055] A spirocyclic heterocycle contains a spirocyclic portion that includes at least one heteroatom in the ring system of the spirocyclic portion. Examples of spirocyclic heterocycles include: [ka] These include, but are not limited to, the following:
[0056] A spirocyclic carbocycle contains a spirocyclic portion that consists only of carbon atoms. Examples of spirocyclic carbocycles include: [ka] These include, but are not limited to, the following:
[0057] A "condensed" part (e.g., a condensed heterocycle, condensed carbocycle, condensed heterocycloalkyl, or condensed cycloalkyl) is a polycyclic system (e.g., bicyclic, tricyclic, or tetracyclic) in which two rings share exactly two atoms. Examples of condensed parts include: [ka] These include, but are not limited to, the following:
[0058] A "condensed" heterocycle contains a condensed moiety that includes at least one heteroatom in the ring system of the condensed moiety. Examples of condensed heterocycles include: [ka] These include, but are not limited to, the following:
[0059] A "condensed" carbocyclic ring contains a condensed portion that consists only of carbon atoms within the ring system of this condensed portion. Examples of condensed carbocyclic rings include: [ka] These include, but are not limited to, the following:
[0060] A "bridged" portion (e.g., a bridged heterocycle, bridged carbocycle, bridged heterocycloalkyl, bridged heterocycloalkenyl, or bridged cycloalkyl) is a polycyclic system (e.g., bicyclic, tricyclic, tetracyclic) comprising two or more bridgeheads, where in at least one combination of two bridgeheads, each bridgehead in the combination is separated from the other bridgehead in the combination by three bridges, each bridge containing at least one atom, and each of these three bridges does not contain any atom that is the same as any of the other two bridges.
[0061] In some embodiments, the “bridged” portion (e.g., bridged heterocycle, bridged carbocycle, bridged heterocycloalkyl, bridged heterocycloalkenyl, or bridged cycloalkyl) is a polycyclic system (e.g., bicyclic, tricyclic, tetracyclic) comprising two or more bridgeheads, where in at least one pair of the two bridgeheads, each bridgehead in the pair is separated from the other bridgehead in the pair by three bridges, each bridge comprising at least one atom, and each of the three bridges comprising none of the atoms that are the same as any of the other two bridges.
[0062] In some embodiments, the bridgehead atoms form a nexus between two or more rings, sp 3 - These are hybrid carbon or nitrogen atoms. In some embodiments, the bridges include one or more atoms connecting two bridgehead atoms.
[0063] Examples of bridge sections include: [ka] These include, but are not limited to, the following:
[0064] A "bridged" carbocyclic ring contains a bridged portion that consists only of carbon atoms. Examples of bridged carbocyclic rings include: [ka] [ka] These include, but are not limited to, the following:
[0065] A "bridged" heteroring is a ring containing a bridged portion that includes at least one heteroatom in the bridged portion's ring system. Examples of bridged heterorings include: [ka] These include, but are not limited to, the following:
[0066] The term “substituted” refers to a moiety of a compound having a substituent that replaces hydrogen atoms on one or more carbon atoms or substituteable heteroatoms (e.g., NH or NH2). It is understood that “substituted” or “substituted with” implies that such substitution follows the acceptable bond valency of the substituted atom and its substituent, and further implies that the substitution results in a stable compound (e.g., a compound that does not undergo rapid rearrangement, cyclization, elimination, etc.). In particular embodiments, “substituted” refers to a moiety having a substituent that replaces two hydrogen atoms on the same carbon atom (e.g., two hydrogen atoms on a single carbon atom are replaced with an oxo, imino, oxime, hydrazone, or thioxo group). As used herein, the term “substituted” is intended to include all acceptable substituents of an organic compound. In a broad sense, acceptable substituents include acyclic and cyclic, branched and unbranched, carbocyclic and heterocyclic, aromatic and non-aromatic substituents of an organic compound. The acceptable substituents may be one or more for a given organic compound, and may be the same or different.
[0067] In some embodiments, the term "one or more substituents" may mean one substituent, or two substituents, or three substituents, or four substituents, or five substituents, or six substituents, or more than six substituents. In some embodiments, the term "one or more substituents" may mean one substituent. In some embodiments, the term "one or more substituents" may mean two substituents. In some embodiments, the term "one or more substituents" may mean three substituents. In some embodiments, the term "one or more substituents" may mean four substituents. In some embodiments, the term "one or more substituents" may mean five substituents. In some embodiments, the term "one or more substituents" may mean five or more substituents. In some embodiments, the term "one or more substituents" may mean one substituent to ten substituents. In some embodiments, the term "one or more substituents" may mean at least one substituent. In some embodiments, the term "one or more substituents" may refer to up to 10 substituents. In some embodiments, the term "one or more substituents" may refer to up to 5 substituents. In some embodiments, the term "one or more substituents" may refer to up to 2 substituents. In some embodiments, the term "one or more substituents" may refer to 1 to 2 substituents.In some embodiments, the term "one or more substituents" means one substituent to one substituent, one substituent to three substituents, one substituent to four substituents, one substituent to five substituents, one substituent to six substituents, one substituent to seven substituents, one substituent to ten substituents, two substituents to three substituents, two substituents to four substituents, two substituents to five substituents, two substituents to six substituents, two substituents to seven substituents, two substituents to ten substituents, A substituent can be any substituent with 3 to 4 substituents, 3 to 5 substituents, 3 to 6 substituents, 3 to 7 substituents, 3 to 10 substituents, 4 to 5 substituents, 4 to 6 substituents, 4 to 7 substituents, 4 to 10 substituents, 5 to 6 substituents, 5 to 7 substituents, 5 to 10 substituents, 6 to 7 substituents, 6 to 10 substituents, or 7 to 10 substituents. In some embodiments, the term "one or more substituents" can mean one substituent, two substituents, three substituents, four substituents, five substituents, six substituents, seven substituents, or ten substituents.
[0068] In some embodiments, the substituents may include, for example, any of the following substituents described herein: halogen, hydroxyl, oxo (=O), thioxo (=S), cyano (-CN), nitro (-NO2), imino (=NH), oxime (=N-OH), hydrazino (=N-NH2), -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 -OR 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 Ure a (where t is 1 or 2), and -R b -S(O) t N(R a )2 (where t is 1 or 2); as well as alkyl, alkenyl, alkynyl, aryl, aralkyl, aralkenyl, aralquinyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heterocycloalkylalkyl, heteroaryl, and heteroarylalkyl, any of which is alkyl, alkenyl, alkynyl, halogen, haloalkyl, haloalkenyl, haloalkynyl, oxo (=O), thioxo (=S), cyano (-CN), nitro (-NO2), imino (=NH), oxime (=N-OH), hydrazine (=N-NH2), -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 -ORc -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(where t is 1 or 2) may be optionally substituted; where each R a is independently selected from hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, heterocycloalkyl, heterocycloalkylalkyl, heteroaryl, or heteroarylalkyl, where each R a is, if the valence allows, alkyl, alkenyl, alkynyl, halogen, haloalkyl, haloalkenyl, haloalkynyl, oxo(=O), thioxo(=S), cyano(-CN), nitro(-NO2), imino(=N-H), oxime(=N-OH), hydrazine(=N-NH2), -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、-Rb -OR 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 Ure a (where t is 1 or 2) and -R b -S(O) t N(R a )2 (where t is 1 or 2) can be substituted as needed; and here each R b These are independently selected from directly bonded, linear, or branched alkylene, alkenylene, or alkynylene chains, and each R c These are linear or branched alkylene, alkenylene, or alkynylene chains.
[0069] A double bond with an oxygen atom, such as an oxo group, is represented herein as both "=O" and "(O)". A double bond with a nitrogen atom is represented as both "=NR" and "(NR)". A double bond with a sulfur atom is represented as both "=S" and "(S)".
[0070] When used herein, the phrases “parenteral administration” and “administered parenterally” mean, but are not limited to, administration other than enteral administration and local administration, usually by injection, including, but are not limited to, intravenous, intramuscular, intra-arterial, intrathecal, intra-articular, intraorbital, intracardiac, intradermal, intraperitoneal, transtracheal, subcutaneous, subepidermal, intra-articular, subcapsular, subarachnoid, intraspinal, and intrasternal injections and infusions.
[0071] The phrase “pharmaceutically acceptable” is used herein to mean a compound, material, composition, and / or dosage form that is suitable for use in contact with human and animal tissues without excessive toxicity, irritation, allergic reactions, or other problems or complications, and that is commensurate with a reasonable profit-benefit ratio, within the bounds of appropriate medical judgment.
[0072] The phrase “pharmaceutically acceptable additive” or “pharmaceutically acceptable carrier,” as used herein, means a pharmaceutically acceptable material, composition or vehicle, such as a liquid or solid filler, diluent, additive, solvent or encapsulating material. Each carrier must be “acceptable” in the sense that it is compatible with the other components of the formulation and is not harmful to the patient. Some examples of materials that can act as pharmaceutically acceptable carriers include: (1) sugars, e.g., lactose, glucose and sucrose; (2) starches, e.g., corn starch and potato starch; (3) cellulose and its derivatives, e.g., sodium carboxymethylcellulose, ethylcellulose and cellulose acetate; (4) powdered tragacanth; (5) malt; (6) gelatin; (7) talc; (8) excipients, e.g., cocoa butter and suppository wax; (9) oils, e.g., peanut oil, cottonseed oil, safflower oil, sesame oil, olive oil, corn oil. Examples include (10) soybean oil, (11) glycols, such as propylene glycol, (12) polyols, such as glycerin, sorbitol, mannitol, and polyethylene glycol, (13) esters, such as ethyl oleate and ethyl laurate, (14) agar, (15) buffers, such as magnesium hydroxide and aluminum hydroxide, (16) alginic acid, (17) water free of pyrogens, (18) isotonic saline, (19) Ringer's solution, (16) ethyl alcohol, (17) phosphate buffer, and (18) other non-toxic suitable substances used in pharmaceutical formulations.
[0073] The term "salt" or "pharmaceutically acceptable salt" refers to salts derived from various organic and inorganic counterions known in the art. pharmaceutically acceptable acid addition salts can be formed using inorganic and / or organic acids. Examples of inorganic acids that can derive salts include hydrochloric acid, hydrobromic acid, sulfuric acid, nitric acid, and phosphoric acid. Examples of organic acids that can derive salts include acetic acid, propionic acid, glycolic acid, pyruvic acid, oxalic acid, maleic acid, malonic acid, succinic acid, fumaric acid, tartaric acid, citric acid, benzoic acid, cinnamic acid, mandelic acid, methanesulfonic acid, ethanesulfonic acid, p-toluenesulfonic acid, and salicylic acid. pharmaceutically acceptable base addition salts can be formed using inorganic and / or organic bases. Examples of inorganic bases that can derive salts include sodium, potassium, lithium, ammonium, calcium, magnesium, iron, zinc, copper, manganese, and aluminum. Examples of organic bases that can induce salt formation include primary, secondary, and tertiary amines, substituted amines including naturally occurring substituted amines, cyclic amines, and basic ion exchange resins, specifically isopropylamine, trimethylamine, diethylamine, triethylamine, tripropylamine, and ethanolamine. In some embodiments, pharmaceutically acceptable base addition salts are selected from ammonium, potassium, sodium, calcium, and magnesium salts.
[0074] As used herein, “treatment” or “to treat” refers to a method for obtaining beneficial or desired outcomes with respect to a disease, disorder, or medical condition, including, but not limited to, therapeutic and / or preventive benefits. Therapeutic benefits may include, for example, the eradication or alleviation of the underlying disease being treated. Therapeutic benefits may also include, for example, the eradication or alleviation of one or more physiological symptoms associated with the underlying disease, such that improvement is observed in the subject even though the subject may still have the underlying disease. In certain embodiments, with respect to preventive benefits, the composition is administered to a subject at risk of developing the disease, or to a subject reporting one or more physiological symptoms of the disease, even if the specific disease has not been diagnosed. Treatment by administration of the compounds described herein does not require the involvement of a medical professional.
[0075] Chemical entities having a carbon-carbon double bond or a carbon-nitrogen double bond may exist in Z- or E- form (or cis- or trans- form). Furthermore, some chemical entities may exist in various tautomerized forms. Unless otherwise specified, the compounds described herein are intended to include all Z-, E-, and tautomerized forms as well.
[0076] A "tautomer" refers to a molecule in which a proton shift can occur from one atom of the molecule to another atom of the same molecule. The compounds presented herein exist as tautomers in certain embodiments. In environments where tautomerization is possible, a chemical equilibrium of tautomers exists. The exact ratio of tautomers depends on several factors, including physical conditions, temperature, solvent, and pH. Some examples of tautomer equilibrium include: [ka] These are some examples.
[0077] The compounds disclosed herein, in some embodiments, for example, 2 H, 3 H, 11 C,13 C and / or 14 It is used in different concentrated isotopic forms in which the C content is concentrated. In a particular embodiment, the compound is deuterated at at least one position. Such deuterated forms can be prepared by the procedures described in U.S. Patents 5,846,514 and 6,334,997. As described in U.S. Patents 5,846,514 and 6,334,997, deuteration can improve metabolic stability and / or efficacy, and thus increase the duration of action of the drug.
[0078] Unless otherwise stated, the compounds described herein are intended to include compounds that differ only in the presence of one or more isotopically enriched atoms. For example, one or more protons may be replaced by one or more deuterium (two hydrogen atoms) or tritium (three hydrogen atoms), or a combination thereof, or one or more in the structure. 12 The carbon atom, in its structure, is one or more 13 C atom, one or more 14 Compounds having the structure of the present invention, except that they are replaced by C atoms or combinations thereof, are within the scope of this disclosure.
[0079] The compounds disclosed herein may optionally contain unnatural proportions of atomic isotopes in one or more atoms constituting such compounds. For example, the compounds may include, for example, deuterium ( 2 H), tritium ( 3 H), Iodine-125( 125 I) or carbon-14 ( 14 It can be labeled with one or more isotopes, such as C). 2 H, 3 H, 11 C, 13 C, 14 C, 15 C, 12 N, 13 N, 15 N, 16 N, 17 O, 18 O,14 F, 15 F, 16 F, 17 F, 18 F, 33 S, 34 S, 35 S, 36 S, 35 Cl, 37 Cl, 79 Br, 81 Br, and 125 All isotopic substitutions by I are intended. All isotopic variants of the compounds of the present invention, whether radioactive or not, are included within the scope of the present invention.
[0080] In certain embodiments, the compounds disclosed herein are 1 Some or all of the H atoms 2 It is replaced by a hydrogen atom. Methods for synthesizing deuterium-containing compounds are known in the art and include, but are not limited to, the following synthesis methods.
[0081] Deuterium-substituted compounds are synthesized using various methods, such as those described in Dean, Dennis C.; Editor. Recent Advances in the Synthesis and Applications of Radiolabeled Compounds for Drug Discovery and Development. [In: Curr., Pharm. Des., 2000; 6(10)] 2000, 110pp; George W.; Varma, Rajender S. The Synthesis of Radiolabeled Compounds via Organometallic Intermediates, Tetrahedron, 1989, 45(21), 6601-21; and Evans, E. Anthony. Synthesis of radiolabeled compounds, J. Radioanal. Chem., 1981, 64(1-2), 9-32.
[0082] Deuterated starting materials are readily available and are subjected to the synthetic methods described herein to provide for the synthesis of deuterium-containing compounds. Many deuterium-containing reagents and components are commercially available from chemical suppliers such as MilliporeSigma.
[0083] This disclosure includes salts, in particular pharmaceutically acceptable salts, of the compounds described herein. Compounds of this disclosure that form salts (in particular pharmaceutically acceptable salts) by comprising one or more sufficiently acidic functional groups, one or more sufficiently basic functional groups, or both one or more sufficiently acidic functional groups and one or more sufficiently basic functional groups may react with any of several inorganic or organic bases or inorganic or organic acids or combinations thereof to form salts. Alternatively, intrinsically charged compounds, such as compounds having quaternary nitrogen, may form salts with appropriate counterions.
[0084] The compounds and salts described herein may, in some cases, exist as diastereomers, enantiomers, or other stereoisomers. Unless otherwise specified (e.g., in tables of biological data), the structures disclosed herein are intended, explicitly or implicitly, to include all diastereomer (e.g., epimer) forms and enantiomers, as well as mixtures thereof. Separation of stereoisomers may be carried out by chromatography, or by forming diastereomers and separating them by recrystallization, chromatography, or any combination thereof. (Jean Jacques, Andre Collet, Samuel H. Wilen, “Enantiomers, Racemates and Resolutions”, John Wiley And Sons, Inc., 1981, is incorporated herein by reference.) Stereoiomers may also be obtained by stereoselective synthesis.
[0085] In certain embodiments, a compound or a salt of a compound may be a prodrug. For example, in some embodiments, a hydroxyl group in the parent compound is presented as an ester or carbonate, or a carboxylic acid present in the parent compound is presented as an ester. The term “prodrug” is intended to encompass compounds that are converted to the pharmaceuticals of this disclosure under physiological conditions. One method for creating a prodrug involves comprising one or more selected moieties that are hydrolyzed under physiological conditions to expose a desired molecule. In other embodiments, the prodrug is converted by the enzymatic activity of a host animal, such as in specific target cells in the host animal. For example, esters or carbonates (e.g., esters or carbonates of alcohols or carboxylic acids, and esters of phosphonic acids) may be prodrugs of this disclosure. In some embodiments, amine prodrugs may depend on enzymatic activation. In some embodiments, amine prodrugs may depend on physiological and chemical conditions for drug release. In some embodiments, the amine prodrug may be selected from amides, carbonates, N-acyloxyalkyl derivatives, N-acyloxycarbonyl derivatives, β-aminoketones, (oxodioxolenyl)methyl derivatives, N-Mannich bases, imines (e.g., Schiff bases), enamines, enaminones, azo compounds, lactonizable systems, tetrahydrothiadiazine-2-thione, redox systems, or PEG.
[0086] As described herein, prodrug forms of the compounds described herein that are metabolized in vivo to produce compounds are included in the claims. In some cases, some of the compounds described herein may be prodrugs for other derivatives or active compounds.
[0087] Prodrugs are often useful because, in certain situations, they may be easier to administer than the parent drug. For example, a prodrug may be available when administered orally, whereas the parent drug is not bioavailable when administered orally. Prodrugs can help enhance the cellular permeability of a compound compared to the parent drug. Prodrugs may also have improved solubility in pharmaceutical compositions compared to the parent drug. Prodrugs may be designed as reversible drug derivatives for use as denaturants to enhance drug transport to site-specific tissues or increase intracellular drug retention.
[0088] In some embodiments, the design of the prodrug increases the lipophilicity of the pharmaceutical product. In some embodiments, the design of the prodrug increases its effective water solubility. For example, Fedorak et al., Am.J.Physiol.,269:G210-218(1995), McLoed et al.,Gastroenterol,106:405-413(1994), Hochhaus et al.,Biomed.Chrom.,6:283-286(1992), J.Larsen and H.Bundgaard, Int.J.Pharmaceutics,37,87(1987), J.Larsen et al.,Int.J.Pharmaceutics,47,103(1988), Sinkula et al.,J.Pharm.Sci.,64:181-210(1975), T.Higuchi and V.Stella,Pro-drugs as Novel Delivery Systems,Vol.14 of the ACSSymposium Series, and Edward See B. Roche, Bioreversible Carriers in Drug Design, American Pharmaceutical Association and Pergamon Press, 1987 (all such disclosures are incorporated herein by reference). According to another embodiment, the present disclosure provides a method for producing the compounds defined above. The compounds can be synthesized using the prior art. Advantageously, these compounds can be synthesized from readily available starting materials.
[0089] The synthetic chemical transformations and methodologies useful for the synthesis of the compounds described herein are known in the art and include, for example, those described in R. Larock, Comprehensive Organic Transformations (1989), T.W. Greene and P.G. M. Wuts, Protective Groups in Organic Synthesis, 2nd ed. (1991), L. Fieser and M. Fieser, Fieser and Fieser's Reagents for Organic Synthesis (1994), and L. Paquette, ed., Encyclopedia of Reagents for Organic Synthesis (1995). compound
[0090] The following is a consideration of compounds and salts that may be used in the methods of this disclosure. In certain embodiments, these compounds and salts are described in formulas (I), (II), and (III). In certain embodiments, these compounds and salts are described in formulas (I), (II-A), (IV), and (III).
[0091] In one phase, equation (I): [ka] A compound represented by or a salt thereof is disclosed herein, in formula (I): X 1 , X 2 , and X 3 These are independently selected from C(R) and N, where X 1 , X 2 , and X 3 At least one of them is N, and X 1 , X 2 , and X 3 Two or fewer of these are N; X 4 is selected from C(R); Each R is independent: Hydrogen, halogen, -NO2, -CN, -N3, -OR 8 , -SR 8 , -N(R 8 )2, -C(O)R 8 ,-C(O)N(R 8 )2, -N(R 8 )C(O)R 8 , -N(R 8 )C(O)N(R 8 )2, -OC(O)N(R 8 )2, -N(R 8 )C(O)OR 8 , -C(O)OR 8 ,-OC(O)R 8 ,-S(O)R 8 , and -S(O)2R 8 ; C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkynnyl, where each of these is a halogen, -OR 8 , -SR 8 , -N(R 8 )2, -C(O)R 8 ,-C(O)N(R 8 )2, -N(R 8 )C(O)R 8 , -C(O)OR 8 ,-OC(O)R 8 , -N(R 8 )C(O)N(R 8 )2, -OC(O)N(R 8 )2, -N(R 8 )C(O)OR 8 ,-S(O)R 8 -S(O)2R 8 -NO2, =O, =S, =N(R 8 ), -CN, C 3~10 It is optionally substituted with one or more substituents independently selected from carbocyclic and 3- to 10-membered heterocycles, where this C 3~10 Carbon rings and 3- to 10-membered heterocycles are R 7 Those which are independently selected and each is substituted as necessary by one or more substituents; and C 3~10Carbon rings and 3- to 10-membered heterocycles, each of which is a halogen, -OR 8 , -SR 8 , -N(R 8 )2, -C(O)R 8 ,-C(O)N(R 8 )2, -N(R 8 )C(O)R 8 , -N(R 8 )C(O)N(R 8 )2, -OC(O)N(R 8 )2, -N(R 8 )C(O)OR 8 , -C(O)OR 8 ,-OC(O)R 8 ,-S(O)R 8 -S(O)2R 8 -NO2, =O-, =S, =N(R 8 ), -CN, C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 It is optionally substituted with one or more substituents independently selected from the alkynyl, where C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl is R 7 One or more substituents, independently selected from the original, each substituted as needed. Selected from; R 1 teeth: hydrogen; C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkynnyl, where each of these is a halogen, -OR 8a , -SR 8a , -N(R 8a )2, -C(O)R 8a ,-C(O)N(R 8a )2, -N(R 8a )C(O)R 8a , -C(O)OR 8a ,-OC(O)R 8a , -N(R 8a )C(O)N(R 8a )2, -OC(O)N(R8a )2, -N(R 8a )C(O)OR 8a ,-S(O)R 8a -S(O)2R 8a -NO2, =O, =S, =N(R 8a ), -CN, C 3~10 The carbon ring is optionally substituted with one or more substituents independently selected from 3-membered to 10-membered heterocycles, where this C 3~10 Carbon rings and 3- to 10-membered heterocycles are R 7a Those which are independently selected and each is substituted as necessary by one or more substituents; and C 3~10 Carbon rings and 3- to 10-membered heterorings, each of which is a halogen, -OR 8a , -SR 8a , -N(R 8a )2, -C(O)R 8a ,-C(O)N(R 8a )2, -N(R 8a )C(O)R 8a , -N(R 8a )C(O)N(R 8a )2, -OC(O)N(R 8a )2, -N(R 8a )C(O)OR 8a , -C(O)OR 8a ,-OC(O)R 8a ,-S(O)R 8a -S(O)2R 8a -NO2, =O-, =S, =N(R 8a ), -CN, C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 It is optionally substituted with one or more substituents independently selected from the alkynyl, where C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl is R 7a One or more substituents, independently selected from the original, each substituted as needed. Selected from; or R 1 is R2 Together with C 3~10 They form a carbon ring, or a 3- to 10-membered heterocycle, each of which is a halogen, -OR 8a , -SR 8a , -N(R 8a )2, -C(O)R 8a ,-C(O)N(R 8a )2, -N(R 8a )C(O)R 8a , -N(R 8a )C(O)N(R 8a )2, -OC(O)N(R 8a )2, -N(R 8a )C(O)OR 8a , -C(O)OR 8a ,-OC(O)R 8a ,-S(O)R 8a -S(O)2R 8a -NO2, =O-, =S, =N(R 8a ), -CN, C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 It is optionally substituted with one or more substituents independently selected from the alkynyl, where C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl is R 7b Each substituent is substituted as needed by one or more substituents selected independently of the original; R 2 teeth: hydrogen; C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkynnyl, where each of these is a halogen, -OR 8b , -SR 8b , -N(R 8b )2, -C(O)R 8b ,-C(O)N(R 8b )2, -N(R 8b )C(O)R 8b , -C(O)OR 8b ,-OC(O)R 8b , -N(R 8b )C(O)N(R 8b)2, -OC(O)N(R 8b )2, -N(R 8b )C(O)OR 8b ,-S(O)R 8b -S(O)2R 8b -NO2, =O, =S, =N(R 8b ), -CN, C 3~10 The carbon ring is optionally substituted with one or more substituents independently selected from 3-membered to 10-membered heterocycles, where this C 3~10 Carbon rings and 3- to 10-membered heterocycles are R 7b Those which are independently selected and each is substituted as necessary by one or more substituents; and C 3~10 Carbon rings and 3- to 10-membered heterorings, each of which is a halogen, -OR 8b , -SR 8b , -N(R 8b )2, -C(O)R 8b ,-C(O)N(R 8b )2, -N(R 8b )C(O)R 8b , -N(R 8b )C(O)N(R 8b )2, -OC(O)N(R 8b )2, -N(R 8b )C(O)OR 8b , -C(O)OR 8b ,-OC(O)R 8b ,-S(O)R 8b -S(O)2R 8b -NO2, =O-, =S, =N(R 8b ), -CN, -N3, C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 It is optionally substituted with one or more substituents independently selected from the alkynyl, where C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl is R 7b One or more substituents, independently selected from the original, each substituted as needed. Selected from; or R 1 is R 2 Together with C 3~10 They form a carbon ring, or a 3- to 10-membered heterocycle, each of which is a halogen, -OR 8a , -SR 8a , -N(R 8a )2, -C(O)R 8a ,-C(O)N(R 8a )2, -N(R 8a )C(O)R 8a , -N(R 8a )C(O)N(R 8a )2, -OC(O)N(R 8a )2, -N(R 8a )C(O)OR 8a , -C(O)OR 8a ,-OC(O)R 8a ,-S(O)R 8a -S(O)2R 8a -NO2, =O-, =S, =N(R 8a ), -CN, C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 It is optionally substituted with one or more substituents independently selected from the alkynyl, where C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl is R 7b Each substituent is substituted as needed by one or more substituents selected independently of the original; R 3 teeth: Hydrogen, halogen, -OR 8c , -SR 8c , -N(R 8c )2, -NO2, and -CN; and R 7c C as needed, substituted with one or more substituents independently selected from 1~6 Alkyl Selected from; R 4 teeth: Hydrogen, halogen, -OR 8d , -SR 8d , -N(R8d )2, -NO2, and -CN; and Halogen, -OR 8d , -SR 8d , -N(R 8d )2, -NO2, and -CN, C 3~10 A carbon ring and a carbon ring, optionally substituted with one or more substituents independently selected from 3-membered to 10-membered heterocycles. 1~6 It is alkyl, and here this C 3~10 Carbon rings and 3- to 10-membered heterocycles are R 7d One or more substituents, independently selected from the original, each substituted as needed. Selected from; R 4 'teeth: Hydrogen, halogen, -OR 8d , -SR 8d , -N(R 8d )2, -NO2, and -CN; and Halogen, -OR 8d , -SR 8d , -N(R 8d )2, -NO2, and -CN, C 3~10 A carbon ring and a carbon ring, optionally substituted with one or more substituents independently selected from 3-membered to 10-membered heterocycles. 1~6 It is alkyl, and here this C 3~10 Carbon rings and 3- to 10-membered heterocycles are R 7d One or more substituents, independently selected from the original, each substituted as needed. Selected from; Or R 4 and R 4 'together with C 3~10 It forms a carbon ring, or a 3-membered to 10-membered heterocycle, and here this C 3~10 A carbon ring, or a 3- to 10-membered heterocycle, is R 7d It is optionally replaced by one or more substituents selected independently of it; R 5 teeth: Hydrogen, halogen, -OR 8e , -SR 8e, -N(R 8e )2, -NO2, -CN, C 1~6 Alkyl, C 3~10 Selected from carbon rings and 3-membered to 10-membered heterorings, where this C 1~6 Alkyl, C 3~10 Carbon rings and 3- to 10-membered heterocycles are R 7e Each substituent is substituted as needed by one or more substituents selected independently of the original; R 6 teeth: Hydrogen, halogen, -OR 8f , -SR 8f , -N(R 8f )2, -NO2, and -CN; and R 7f C as needed, substituted with one or more substituents independently selected from 1~6 Alkyl Selected from; Each R 7 , R 7a , R 7b , R 7c , R 7d , R 7e , and R 7f Independently: Halogen, -OR 8g , -SR 8g , -N(R 8g )2, -C(O)R 8g ,-C(O)N(R 8g )2, -N(R 8g )C(O)R 8g , -N(R 8g )C(O)N(R 8g )2, -OC(O)N(R 8g )2, -N(R 8g )C(O)OR 8g , -C(O)OR 8g ,-OC(O)R 8g ,-S(O)R 8g -S(O)2R 8g -NO2, =O, =S, =N(R 8g ), and -CN; and C 1~3 Alkyl, C 2~3 Alkenyl and C 2~3Alkynnyl, where each of these is a halogen, -OR 8g , -SR 8g , -N(R 8g )2, -C(O)R 8g ,-C(O)N(R 8g )2, -N(R 8g )C(O)R 8g , -N(R 8g )C(O)N(R 8g )2, -OC(O)N(R 8g )2, -N(R 8g )C(O)OR 8g , -C(O)OR 8g ,-OC(O)R 8g ,-S(O)R 8g -S(O)2R 8g -NO2, =O, =S, =N(R 8g ), and one or more substituents selected independently of -CN as needed. Selected from; Each R 8 , R 8a , R 8b , R 8c , R 8d , R 8e , R 8f , and R 8g Independently: Hydrogen and halogens; and C 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl and C 3~10 A carbon ring, each of which is a halogen, -CN, -OH, -SH, -NO2, -NH2, =O, =S, -OC 1~6 Alkyl, -SC 1~6 Alkyl, -N(C 1~6 Alkyl)2,-NH(C 1~6 Alkyl), C 3~10 A carbon ring, or a 3-membered to 10-membered heterocycle, substituted as needed with one or more substituents independently selected from these; and C 3~10 Carbon rings and 3- to 10-membered heterocycles, each of which is a halogen, -CN, -OH, -SH, -NO2, -NH2, =O, =S, -OC1~6 Alkyl, -SC 1~6 Alkyl, -SO2-C 1~6 Alkyl, -N(C 1~6 Alkyl)2,-NH(C 1~6 Alkyl), C 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 3~10 Carbon rings, 3-membered to 10-membered heterocycles, and C 1~6 Substituted as needed with one or more substituents independently selected from the haloalkyl group. Selected from.
[0092] In certain embodiments, with respect to a compound or salt of formula (I) or formula (I'), X 1 , X 2 , and X 3 These are independently selected from C(R) and N, where X 1 , X 2 , and X 3 At least one of them is N, and X 1 , X 2 , and X 3 Two or fewer of these are N. In some embodiments, X 1 In some embodiments, X 1 is C(R). In some embodiments, X 2 In some embodiments, X 2 is C(R). In some embodiments, X 3 In some embodiments, X 3 is C(R). In some embodiments, X 1 is N, and X 2 is C(R), and X 3 is C(R). In some embodiments, X 1 C(R) and X 2 is N, and X 3 is C(R). In some embodiments, X 1 C(R) and X 2 is C(R), and X3 In some embodiments, X 1 is N, and X 2 is C(R), and X 3 It is N.
[0093] In certain embodiments, with respect to a compound or salt of formula (I) or formula (I'), R may be any suitable functional group known to those skilled in the art. In some embodiments, each R may independently be: hydrogen, halogen, -NO2, -CN, -N3, -OR 8 , -SR 8 , -N(R 8 )2, -C(O)R 8 ,-C(O)N(R 8 )2, -N(R 8 )C(O)R 8 , -N(R 8 )C(O)N(R 8 )2, -OC(O)N(R 8 )2, -N(R 8 )C(O)OR 8 , -C(O)OR 8 ,-OC(O)R 8 ,-S(O)R 8 , and -S(O)2R 8 ;C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkynnyl, where each of these is a halogen, -OR 8 , -SR 8 , -N(R 8 )2, -C(O)R 8 ,-C(O)N(R 8 )2, -N(R 8 )C(O)R 8 , -C(O)OR 8 ,-OC(O)R 8 , -N(R 8 )C(O)N(R 8 )2, -OC(O)N(R 8 )2, -N(R 8 )C(O)OR 8 ,-S(O)R 8 -S(O)2R 8 -NO2, =O, =S, =N(R 8), -CN, C 3~10 It is optionally substituted with one or more substituents independently selected from carbocyclic and 3- to 10-membered heterocycles, where this C 3~10 Carbon rings and 3- to 10-membered heterocycles have one or more R 7 Each of these is replaced as needed; and C 3~10 Carbon rings and 3- to 10-membered heterocycles, each of which is a halogen, -OR 8 , -SR 8 , -N(R 8 )2, -C(O)R 8 ,-C(O)N(R 8 )2, -N(R 8 )C(O)R 8 , -N(R 8 )C(O)N(R 8 )2, -OC(O)N(R 8 )2, -N(R 8 )C(O)OR 8 , -C(O)OR 8 ,-OC(O)R 8 ,-S(O)R 8 -S(O)2R 8 -NO2, =O-, =S, =N(R 8 ), -CN, C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 It is optionally substituted with one or more substituents independently selected from the alkynyl, where C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl is one or more R 7 Each is then selected from those that have been replaced as needed.
[0094] In certain embodiments, with respect to compounds or salts of formula (I) or formula (I'), each R is independently: hydrogen, halogen, -NO2, -CN, -N3, -OR 8 , -SR 8 , -N(R 8 )2, -C(O)R 8 ,-C(O)N(R 8 )2, -N(R8 )C(O)R 8 , and -N(R 8 )C(O)N(R 8 )2;C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkynnyl, where each of these is a halogen, -OR 8 , -SR 8 , -N(R 8 )2, -NO2, =O, =S, =N(R 8 ) which are substituted as needed with one or more substituents independently selected from; and C 3~10 Selected from carbon rings and 3- to 10-membered heterocycles. In some embodiments, each R is independently hydrogen, halogen, -CN, -N3, -OR 8 , -SR 8 , -N(R 8 )2, -C(O)R 8 ,-C(O)N(R 8 )2, and -N(R 8 )C(O)R 8 ;C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkynnyl, where each of these is a halogen, -OR 8 Substituting as necessary with one or more substituents independently selected from; and C 3~10 Selected from carbon rings and 3- to 10-membered heterocycles. In some embodiments, each R is independently: hydrogen, halogen, -CN, -N3, -OR 8 , -SR 8 , -N(R 8 )2;C 1~6 Alkyl and C 2~6 Alkynnyls, each of which is optionally substituted with one or more substituents independently selected from halogens; and C 3~10 Selected from carbon rings and 3- to 10-membered heterocycles. In some embodiments, each R is independently -F, -Cl, -Br, -I, -CN, -N3, -OR 8 , -SR 8 , -N(R8 )2, -CF3, methyl, ethyl, cyclopropyl, -CCMe, phenyl, morpholinyl, and pyrrolidinyl are selected. In some embodiments, each R is independently: -F, -Cl, -Br, -I, -CN, -N3, -OR 8 , -SR 8 , -N(R 8 )2, -CF3, methyl, ethyl, cyclopropyl, -CCMe, phenyl, morpholinyl, and pyrrolidinyl, where each R is selected. 8The following are independently selected from the group consisting of hydrogen, methyl, ethyl, propyl, isopropyl, cyclopropyl, isobutyl, -CF3, -CH2CF3, -CH2CHF2, -CH2CF(Me)2, -CH2CHMe2, and -CH2-phenyl. In some embodiments, each R is independently selected from:-H,-F,Cl,-Br,-I,-CN,-N3,-OH,-OMe,-OEt,-O-propyl,-O-isopropyl,-O-butyl,-O-isobutyl,-OCF3,-OCH2CFMe2,-OCH2CHF2,-OCH2CF3,-OCH2CF(CH3)2,-O-cyclopropyl,-SMe,-SEt,-NH2,-NHMe,-NHEt,-NH-propyl,-NH-cyclopropyl,-NH-butyl,-NH-isobutyl,-NH-cyclobutyl,-NMe2,-NEt2,-NH-phenyl,-Me,-Et,-cyclopropyl,-n-propyl,-isopropyl,-CF3,-CCMe,-morpholinyl, and pyrrolidinyl. In some embodiments, each R is independently selected from:-H,-F,Cl,-Br,-I,-OH,-Me,-Et,-OCH2CF3,-OCH2CHF2,-OMe,-cyclopropyl,-CN,-OEt,-CF3,-O-CF3,-O-cyclopropyl,-n-propyl, isopropyl,-OCH2CF(CH3)2,-O-propyl,-O-isopropyl,-OCH2CFMe2,-SMe,-NHMe,-NH2,-NHEt,-CCMe,-NMe2,-NEt2,-N3,-NH-cyclopropyl,-NH-isobutyl,-NH-phenyl,-morpholinyl, pyrrolidinyl In several embodiments, each R is independently selected from:-H,-F,Cl,-Br,-I,-CN,-N3,-OH,-OMe,-OEt,-O-propyl,-O-isopropyl,-OCF3,-OCH2CFMe2,-OCH2CHF2,-OCH2CF3,-OCH2CF(CH3)2,-O-cyclopropyl,-SMe,-NH2,-NHMe,-NHEt,-NH-cyclopropyl,-NH-isobutyl,-NMe2,-NEt2,-NH-phenyl,-Me,-Et,-cyclopropyl,-n-propyl,-isopropyl,-CF3,-CCMe,-morpholinyl, and pyrrolidinyl.In some embodiments, each R is independently selected from: -H, -F, Cl, -Br, -I, -CN, -N3, -OH, -OMe, -OEt, -O-propyl, -O-isopropyl, -OCF3, -OCH2CFMe2, -OCH2CHF2, -OCH2CF3, -OCH2CF(CH3)2, -O-cyclopropyl, -SMe, -NH2, -NHMe, -NHEt, -NEt2, -Me, -Et, -cyclopropyl, -n-propyl, isopropyl, -CF3, and -CCMe.
[0095] In certain embodiments, with respect to a compound or salt of formula (I) or formula (I'), R 1 R can be any suitable functional group known to those skilled in the art. In some embodiments, R 1 ha: hydrogen; C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkynnyl, where each of these is a halogen, -OR 8a , -SR 8a , -N(R 8a )2, -C(O)R 8a ,-C(O)N(R 8a )2, -N(R 8a )C(O)R 8a , -C(O)OR 8a ,-OC(O)R 8a , -N(R 8a )C(O)N(R 8a )2, -OC(O)N(R 8a )2, -N(R 8a )C(O)OR 8a ,-S(O)R 8a -S(O)2R 8a -NO2, =O, =S, =N(R 8a ), -CN, C 3~10 The carbon ring is optionally substituted with one or more substituents independently selected from 3-membered to 10-membered heterocycles, where this C 3~10 Carbon rings and 3- to 10-membered heterocycles have one or more R 7a Each of these is replaced as needed; and C 3~10Carbon rings and 3- to 10-membered heterorings, each of which is a halogen, -OR 8a , -SR 8a , -N(R 8a )2, -C(O)R 8a ,-C(O)N(R 8a )2, -N(R 8a )C(O)R 8a , -N(R 8a )C(O)N(R 8a )2, -OC(O)N(R 8a )2, -N(R 8a )C(O)OR 8a , -C(O)OR 8a ,-OC(O)R 8a ,-S(O)R 8a -S(O)2R 8a -NO2, =O-, =S, =N(R 8a ), -CN, C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 It is optionally substituted with one or more substituents independently selected from the alkynyl, where C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl is one or more R 7a Each is selected from those that have been replaced as needed; or R 1 is R 2 Together with C 3~10 They form a carbon ring, or a 3- to 10-membered heterocycle, each of which is a halogen, -OR 8a , -SR 8a , -N(R 8a )2, -C(O)R 8a ,-C(O)N(R 8a )2, -N(R 8a )C(O)R 8a , -N(R 8a )C(O)N(R 8a )2, -OC(O)N(R 8a )2, -N(R 8a )C(O)OR 8a , -C(O)OR 8a ,-OC(O)R 8a ,-S(O)R 8a-S(O)2R 8a -NO2, =O-, =S, =N(R 8a ), -CN, C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 It is optionally substituted with one or more substituents independently selected from the alkynyl, where C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl is one or more R 7b Each is replaced as needed. In some embodiments, R 1 ha: hydrogen; C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkynnyl, where each of these is a halogen, -OR 8a , -SR 8a , -N(R 8a )2, -C(O)R 8a ,-S(O)R 8a -S(O)2R 8a Substituted as necessary with one or more substituents independently selected from -NO2 and -CN; and C 3~10 Carbon rings and 3- to 10-membered heterorings, each of which is a halogen, -OR 8a , -SR 8a , -N(R 8a )2, -C(O)R 8a -NO2, -CN, C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 It is optionally substituted with one or more substituents independently selected from the alkynyl, where C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl is one or more R 7a Then, each is selected from those that have been substituted as needed, or R 1 is R 2 Together with C 3~10 They form a carbon ring, or a 3- to 10-membered heterocycle, each of which is a halogen, -OR8a , -SR 8a , -N(R 8a )2, -C(O)R 8a ,-S(O)R 8a -S(O)2R 8a -NO2, -CN, C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 It is optionally substituted with one or more substituents independently selected from the alkynyl, where C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl is one or more R 7b Each is replaced as needed. In some embodiments, R 1 is hydrogen; C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkynnyl, where each of these is a halogen, -OR 8a , -SR 8a , -N(R 8a )2, -C(O)R 8a ,-S(O)R 8a -S(O)2R 8a Substituted as necessary with one or more substituents independently selected from -NO2 and -CN; and C 3~10 Carbon rings and 3- to 10-membered heterocycles, each of which is a halogen, -C(O)R 8a ,-CN,C 1~6 Selected from those that are optionally substituted with one or more substituents independently of alkyl, or R 1 is R 2 Together with C 3~10 They form a carbon ring, or a 3- to 10-membered heterocycle, each of which is a halogen, -OR 8a , -SR 8a , -N(R 8a )2, -C(O)R 8a , -NO2, -CN, and C 1~6 It is optionally substituted with one or more substituents independently selected from the alkyl, where C1~6 Alkyl is one or more R 7b It is replaced as needed. In some embodiments, R 1 is hydrogen, methyl, -CH2OH, -CH2CH2OH, C(Me)2OH, -CH2OMe, or R 1 is R 2 Together with C 3~10 A carbon ring or a 3- to 10-membered heterocycle is formed, each of which is optionally substituted with one or more substituents independently selected from -F, -COMe, -CN, and methyl. In some embodiments, R 1 is hydrogen, methyl, -CH2OH, -CH2CH2OH, C(Me)2OH, -CH2OMe, or R 1 is R 2 Together with: [ka] These form a structure, each of which is optionally substituted with one or more fluoro, -C(O)Me, -CN, and methyl groups.
[0096] In certain embodiments, with respect to a compound or salt of formula (I) or formula (I'), R 2 R can be any suitable functional group known to those skilled in the art. In some embodiments, R 2 ha: hydrogen; C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkynnyl, where each of these is a halogen, -OR 8b , -SR 8b , -N(R 8b )2, -C(O)R 8b ,-C(O)N(R 8b )2, -N(R 8b )C(O)R 8b , -C(O)OR 8b ,-OC(O)R 8b , -N(R 8b )C(O)N(R 8b )2, -OC(O)N(R 8b )2, -N(R8b )C(O)OR 8b ,-S(O)R 8b -S(O)2R 8b -NO2, =O, =S, =N(R 8b ), -CN, C 3~10 The carbon ring is optionally substituted with one or more substituents independently selected from 3-membered to 10-membered heterocycles, where this C 3~10 Carbon rings and 3- to 10-membered heterocycles have one or more R 7b Each of these is replaced as needed; and C 3~10 Carbon rings and 3- to 10-membered heterorings, each of which is a halogen, -OR 8b , -SR 8b , -N(R 8b )2, -C(O)R 8b ,-C(O)N(R 8b )2, -N(R 8b )C(O)R 8b , -N(R 8b )C(O)N(R 8b )2, -OC(O)N(R 8b )2, -N(R 8b )C(O)OR 8b , -C(O)OR 8b ,-OC(O)R 8b ,-S(O)R 8b -S(O)2R 8b -NO2, =O-, =S, =N(R 8b ), -CN, C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 It is optionally substituted with one or more substituents independently selected from the alkynyl, where C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl is one or more R 7b Each is selected from those that have been replaced as needed; or R 1 is R 2 Together with C 3~10 They form a carbon ring, or a 3- to 10-membered heterocycle, each of which is a halogen, -OR 8a , -SR8a , -N(R 8a )2, -C(O)R 8a ,-C(O)N(R 8a )2, -N(R 8a )C(O)R 8a , -N(R 8a )C(O)N(R 8a )2, -OC(O)N(R 8a )2, -N(R 8a )C(O)OR 8a , -C(O)OR 8a ,-OC(O)R 8a ,-S(O)R 8a -S(O)2R 8a -NO2, =O-, =S, =N(R 8a ), -CN, C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 It is optionally substituted with one or more substituents independently selected from the alkynyl, where C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl is one or more R 7b Each is replaced as needed.
[0097] In certain embodiments, with respect to a compound or salt of formula (I) or formula (I'), R 2 ha: Hydrogen, C 1~6 Alkyl, and C 2~6 Alkenyls, each of which is a halogen, -OR 8b , -SR 8b , -N(R 8b )2, -C(O)R 8b ,-S(O)R 8b -S(O)2R 8b -NO2, -CN, C 3~10 The carbon ring is optionally substituted with one or more substituents independently selected from 3-membered to 10-membered heterocycles, where this C 3~10 Carbon rings and 3- to 10-membered heterocycles have one or more R 7b Each of these is replaced as needed; and C 3~10A carbon ring and a 3- to 10-member heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from halogen, -OR 8b , -SR 8b , -N(R 8b )2, -C(O)R 8b , -S(O)R 8b , -S(O)2R 8b , -NO2, -CN, C 1~6 alkyl, C 2~6 alkenyl, and C 2~6 alkynyl, and where C 1~6 alkyl, C 2~6 alkenyl, and C 2~6 alkynyl are each selected from those optionally substituted with one or more R 7b ; or R 1 together with R 2 forms a C 3~10 carbon ring or a 3- to 10-member heterocyclic ring, each of which is optionally substituted with one or more substituents independently selected from halogen, -OR 8a , -SR 8a , -N(R 8a )2, -C(O)R 8a , -S(O)R 8a , -S(O)2R 8a , -NO2, -CN, C 1~6 alkyl, C 2~6 alkenyl, and C 2~6 alkynyl, and where C 1~6 alkyl, C 2~6 alkenyl, and C 2~6 alkynyl are each optionally substituted with one or more R 7b . In some embodiments, R 2 is: hydrogen, C 1~6 alkyl, and C 2~6 alkenyl, each of which is optionally substituted with halogen, -OR 8b , -SR 8b , -N(R 8b )2, -C(O)R 8b , -S(O)R 8b , -S(O)2R8b -NO2, -CN, C 3~10 The carbon ring is optionally substituted with one or more substituents independently selected from 3-membered to 10-membered heterocycles, where this C 3~10 Carbon rings and 3- to 10-membered heterocycles have one or more R 7b Each of these is replaced as needed; and C 3~10 Carbon rings and 3- to 10-membered heterorings, each of which is a halogen, -OR 8b , -C(O)R 8b -S(O)2R 8b , -CN, and C 1~6 It is optionally substituted with one or more substituents independently selected from the alkyl, where C 1~6 Alkyl is one or more R 7b Selected from those that have been replaced as needed; or R 1 is R 2 Together with C 3~10 They form a carbon ring, or a 3- to 10-membered heterocycle, each of which is a halogen, -C(O)R 8a , -CN, and C 1~6 It is optionally substituted with one or more substituents independently selected from the alkyl, where C 1~6 Alkyl is one or more R 7b It is replaced as needed. In some embodiments, R 2 is hydrogen, C 1~6 Alkyl, and C 2~6 Alkenyls, each of which is a halogen, -OR 8b , C 3~10 Carbon rings, and those optionally substituted with one or more substituents independently selected from 3-membered to 10-membered heterocycles; and C 3~10 Carbon rings and 3- to 10-membered heterorings, each of which is a halogen, -OR 8b , -C(O)R 8b -S(O)2R 8b , -CN, and C 1~6Selected from those that are optionally substituted with one or more substituents independently of the alkyl; or R 1 is R 2 Together with C 3~10 They form a carbon ring, or a 3- to 10-membered heterocycle, each of which is a halogen, -C(O)R 8a , -CN, and C 1~6 It is optionally substituted with one or more substituents independently selected from the alkyl, where C 1~6 Alkyl is one or more R 7b It is replaced as needed. In some embodiments, R 2 is hydrogen, C 1~2 It is alkyl, phenyl, or pyridinyl, where this C 1~2 The alkyl group is optionally substituted with one or more substituents independently selected from -OH and phenyl, where this phenyl or pyridinyl group is optionally substituted with one or more substituents independently selected from -F, -OH, -OMe, -COMe, -SO2Me, -CN, and methyl. In some embodiments, R 2 R is phenyl or pyridinyl, where this phenyl or pyridinyl is optionally substituted with one or more substituents independently selected from -F, -OH, -OMe, -COMe, -SO2Me, -CN, and methyl. In some embodiments, R 2 is R 1 Together with: [ka] These form a structure, each of which is optionally substituted with one or more fluoro, -C(O)Me, -CN, and methyl groups.
[0098] In certain embodiments, with respect to a compound or salt of formula (I) or formula (I'), R 3 R can be any suitable functional group known to those skilled in the art. In some embodiments, R3 is: hydrogen, halogen, -OR 8c , -SR 8c , -N(R 8c )2, -NO2, and -CN; and one or more R 7c substituted C 1~6 alkyl selected therefrom. In some embodiments, R 3 is: hydrogen, halogen, -OR 8c , -CN, and C 1~6 alkyl selected therefrom. In some embodiments, R 3 is selected from hydrogen and C 1~6 alkyl. In some embodiments, R 3 is selected from hydrogen and C 1~3 alkyl. In some embodiments, R 3 is hydrogen.
[0099] In some embodiments,
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[0100] In certain embodiments, with respect to a compound or salt of formula (I) or formula (I'), R 4 R can be any suitable functional group known to those skilled in the art. In some embodiments, each R 4 These are independently hydrogen, halogen, and -OR 8d , -SR 8d , -N(R 8d )2, -NO2, and -CN; as well as halogens, -OR 8d , -SR 8d , -N(R 8d )2, -NO2, and -CN, C 3~10 A carbon ring and a carbon ring, optionally substituted with one or more substituents independently selected from 3-membered to 10-membered heterocycles. 1~6 It is alkyl, and here this C 3~10 Carbon rings and 3- to 10-membered heterocycles have one or more R 7d Each is selected from those which are replaced as needed. In some embodiments, each R 4 These are independently hydrogen, halogen, and -OR 8d , and -CN; as well as halogen, -OR 8d , and -CN, C 3~10 A carbon ring and a carbon ring, optionally substituted with one or more substituents independently selected from 3-membered to 10-membered heterocycles. 1~6 It is alkyl, and here this C 3~10 Carbon rings and 3- to 10-membered heterocycles have one or more R 7d Each is selected from those which are replaced as needed. In some embodiments, each R 4 These are independently hydrogen, halogen, and -OR 8d , -SR 8d , -N(R 8d )2, -NO2, and -CN; and C 3~10 A carbon ring is optionally substituted with one or more substituents independently selected from the carbon ring. 1~6 Selected from alkyl groups. In some embodiments, each R 4 These are independently hydrogen, halogens; and C 3~10A carbon ring is optionally substituted with one or more substituents independently selected from the carbon ring. 1~6 Selected from alkyl groups. In some embodiments, each R 4 R is independently selected from C1 alkyl groups optionally substituted with hydrogen, -F, and phenyl. In some embodiments, each R 4 R is independently hydrogen or methyl. In some embodiments, each R 4 is hydrogen. In some embodiments, each R 4 It is methyl.
[0101] In certain embodiments, with respect to a compound or salt of formula (I) or formula (I'), R 4’ R can be any suitable functional group known to those skilled in the art. In some embodiments, each R 4’ These are independently hydrogen, halogen, and -OR 8d , -SR 8d , -N(R 8d )2, -NO2, and -CN; as well as halogens, -OR 8d , -SR 8d , -N(R 8d )2, -NO2, and -CN, C 3~10 A carbon ring and a carbon ring, optionally substituted with one or more substituents independently selected from 3-membered to 10-membered heterocycles. 1~6 It is alkyl, and here this C 3~10 Carbon rings and 3- to 10-membered heterocycles have one or more R 7d Each is selected from those which are replaced as needed. In some embodiments, each R 4’ These are independently hydrogen, halogen, and -OR 8d , and -CN; as well as halogen, -OR 8d , and -CN, C 3~10 A carbon ring and a carbon ring, optionally substituted with one or more substituents independently selected from 3-membered to 10-membered heterocycles. 1~6 It is alkyl, and here this C 3~10 Carbon rings and 3- to 10-membered heterocycles have one or more R 7dEach is selected from those which are replaced as needed. In some embodiments, each R 4’ These are independently hydrogen, halogen, and -OR 8d , -SR 8d , -N(R 8d )2, -NO2, and -CN; and C 3~10 A carbon ring is optionally substituted with one or more substituents independently selected from the carbon ring. 1~6 Selected from alkyl groups. In some embodiments, each R 4’ These are independently hydrogen, halogens; and C 3~10 A carbon ring is optionally substituted with one or more substituents independently selected from the carbon ring. 1~6 Selected from alkyl groups. In some embodiments, each R 4’ R is independently selected from C1 alkyl groups optionally substituted with hydrogen, -F, and phenyl. In some embodiments, each R 4’ R is independently hydrogen or methyl. In some embodiments, each R 4’ is hydrogen. In some embodiments, each R 4’ It is methyl. 5 R can be any suitable functional group known to those skilled in the art. In some embodiments, R 5 is hydrogen, halogen, -OR 8e , -SR 8e , -N(R 8e )2, -NO2, -CN, C 1~6 Alkyl, C 3~10 Selected from carbon rings and 3-membered to 10-membered heterorings, where this C 1~6 Alkyl, C 3~10 Carbon rings and 3- to 10-membered heterocycles have one or more R 7e Each is replaced as needed.
[0102] In certain embodiments, with respect to a compound or salt of formula (I) or formula (I'), R 5 ha: hydrogen, halogen, -OR 8e , -N(R 8e )2, -CN, C 1~6Alkyl, C 3~10 Selected from carbon rings and 3-membered to 10-membered heterorings, where this C 1~6 Alkyl, C 3~10 Carbon rings and 3- to 10-membered heterocycles have one or more R 7e Each is replaced as needed. In some embodiments, R 5 ha: hydrogen, halogen, -OR 8e , -N(R 8e )2, -CN, C 1~6 Alkyl, and C 3~10 Selected from the carbon ring, here this C 1~6 Alkyl, and C 3~10 A carbon ring has one or more R 7e Each is replaced as needed. In some embodiments, R 5 ha: hydrogen, halogen, -OR 8e , -N(R 8e )2, -CN, C 1~3 Alkyl, and C 3~6 Selected from the carbon ring, here this C 1~6 Alkyl, and C 3~10 A carbon ring has one or more R 7e Each is replaced as needed. In some embodiments, R 5 H: Hydrogen, -Cl, -OH, -OMe, -NHMe, -CN, C 1~2 Selected from alkyl and cyclopropyl, where this C 1~2 Alkyl and cyclopropyl groups are each optionally substituted with one or more -F groups. In some embodiments, R 5 The element is selected from hydrogen, -Cl, -OH, -OMe, -NHMe, -CN, methyl, ethyl, -CF3, -CHF2, and cyclopropyl.
[0103] In certain embodiments, with respect to a compound or salt of formula (I) or formula (I'), R 6 R can be any suitable functional group known to those skilled in the art. In some embodiments, R 6 ha: hydrogen, halogen, -OR 8f , -SR8f , -N(R 8f )2, -NO2, and -CN; as well as one or more R 7f C replaced as needed 1~6 Selected from alkyl. In some embodiments, R 6 ha: hydrogen, halogen, -OR 8f ; and one or more R 7f C replaced as needed 1~6 Selected from alkyl. In some embodiments, R 6 ha: hydrogen, halogen, -OR 8f , and C 1~6 Selected from alkyl. In some embodiments, R 6 is hydrogen and C 1~6 Selected from alkyl. In some embodiments, R 6 is hydrogen and C 1~3 Selected from alkyl. In some embodiments, R 6 It is hydrogen.
[0104] In certain embodiments, with respect to a compound or salt of formula (I) or formula (I'), R 7 , R 7a , R 7b , R 7c , R 7d , R 7e , and R 7f Each of these may be any suitable functional group known to those skilled in the art. In some embodiments, R 7 , R 7a , R 7b , R 7c , R 7d , R 7e , and R 7f Each of these is independent of halogen, -OR 8g , -SR 8g , -N(R 8g )2, -C(O)R 8g ,-C(O)N(R 8g )2, -N(R 8g )C(O)R 8g , -N(R 8g )C(O)N(R 8g)2, -OC(O)N(R 8g )2, -N(R 8g )C(O)OR 8g , -C(O)OR 8g ,-OC(O)R 8g ,-S(O)R 8g -S(O)2R 8g -NO2, =O, =S, =N(R 8g ), and -CN; as well as C 1~3 Alkyl, C 2~3 Alkenyl and C 2~3 Alkynnyl, where each of these is a halogen, -OR 8g , -SR 8g , -N(R 8g )2, -C(O)R 8g ,-C(O)N(R 8g )2, -N(R 8g )C(O)R 8g , -N(R 8g )C(O)N(R 8g )2, -OC(O)N(R 8g )2, -N(R 8g )C(O)OR 8g , -C(O)OR 8g ,-OC(O)R 8g ,-S(O)R 8g -S(O)2R 8g -NO2, =O, =S, =N(R 8g ), and are selected from those which are optionally substituted with one or more substituents independently selected from -CN.
[0105] In certain embodiments, with respect to a compound or salt of formula (I) or formula (I'), each R 7 These are independently: halogen, -OR 8g , -N(R 8g )2, -C(O)R 8g , and C 1~3 Selected from alkyl groups. In some embodiments, each R 7 These are independently: halogen, -OR 8g , and C 1~3 Selected from alkyl groups. In some embodiments, each R 7These are independently selected from halogen, -OH, and -OMe.
[0106] In some embodiments, each R 7a These are independently: halogen, -OR 8g , -N(R 8g )2, -C(O)R 8g , and C 1~3 Selected from alkyl groups. In some embodiments, each R 7a These are independently: halogen, -OR 8g , and C 1~3 Selected from alkyl groups. In some embodiments, each R 7a These are independently selected from halogen, -OH, and -OMe.
[0107] In some embodiments, each R 7b These are independently: halogen, -OR 8g , -N(R 8g )2, -C(O)R 8g , and C 1~3 Selected from alkyl groups. In some embodiments, each R 7b These are independently: halogen, -OR 8g , and C 1~3 Selected from alkyl groups. In some embodiments, each R 7b These are independently selected from halogen, -OH, and -OMe.
[0108] In some embodiments, each R 7c These are independently: halogen, -OR 8g , -N(R 8g )2, -C(O)R 8g , and C 1~3 Selected from alkyl groups. In some embodiments, each R 7c These are independently: halogen, -OR 8g , and C 1~3 Selected from alkyl groups. In some embodiments, each R 7c These are independently selected from halogen, -OH, and -OMe.
[0109] In some embodiments, each R 7d These are independently: halogen, -OR 8g , -N(R 8g )2, -C(O)R 8g , and C 1~3 Selected from alkyl groups. In some embodiments, each R 7d These are independently: halogen, -OR 8g , and C 1~3 Selected from alkyl groups. In some embodiments, each R 7d These are independently selected from halogen, -OH, and -OMe.
[0110] In some embodiments, each R 7e These are independently: halogen, -OR 8g , -N(R 8g )2, -C(O)R 8g , and C 1~3 Selected from alkyl groups. In some embodiments, each R 7e These are independently: halogen, -OR 8g , and C 1~3 Selected from alkyl groups. In some embodiments, each R 7e R is independently selected from halogen, -OH, and -OMe. In some embodiments, each R 7e It is fluoro.
[0111] In some embodiments, each R 7f These are independently: halogen, -OR 8g , -N(R 8g )2, -C(O)R 8g , and C 1~3 Selected from alkyl groups. In some embodiments, each R 7f These are independently: halogen, -OR 8g , and C 1~3 Selected from alkyl groups. In some embodiments, each R 7f These are independently selected from halogen, -OH, and -OMe.
[0112] In certain embodiments, with respect to a compound or salt of formula (I) or formula (I'), R 8 , R 8a , R 8b , R 8c , R 8d , R 8e , R 8f , and R 8g Each of these may be any suitable functional group known to those skilled in the art. In some embodiments, R 8 , R 8a , R 8b , R 8c , R 8d , R 8e , R 8f , and R 8g Each of them independently consists of hydrogen and halogen; as well as C 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl and C 3~10 A carbon ring, each of which is a halogen, -CN, -OH, -SH, -NO2, -NH2, =O, =S, -OC 1~6 Alkyl, -SC 1~6 Alkyl, -N(C 1~6 Alkyl)2,-NH(C 1~6 Alkyl), C 3~10 A carbon ring, or a 3-membered to 10-membered heterocycle, substituted as needed with one or more substituents independently selected from these; and C 3~10 Carbon rings and 3- to 10-membered heterocycles, each of which is a halogen, -CN, -OH, -SH, -NO2, -NH2, =O, =S, -OC 1~6 Alkyl, -SC 1~6 Alkyl, -SO2-C 1~6 Alkyl, -N(C 1~6 Alkyl)2,-NH(C 1~6 Alkyl), C 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 3~10 Carbon rings, 3-membered to 10-membered heterocycles, and C 1~6 The haloalkyl group is selected from those that are optionally substituted with one or more substituents independently selected from the haloalkyl group.
[0113] In certain embodiments, with respect to a compound or salt of formula (I) or formula (I'), each R 8 These are independently: hydrogen and halogens; as well as C 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl and C 3~10 A carbon ring, each of which is a halogen, -CN, -OH, -SH, -NO2, -NH2, C 3~10 A carbon ring, or a 3-membered to 10-membered heterocycle, substituted as needed with one or more substituents independently selected from these; and C 3~10 A carbon ring, each of which is a halogen, -CN, -OH, -SH, -NO2, -NH2, =O, =S, -OC 1~6 Alkyl, -SC 1~6 Alkyl, -SO2-C 1~6 Alkyl, -N(C 1~6 Alkyl)2,-NH(C 1~6 Alkyl), C 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 3~10 Carbon rings, 3-membered to 10-membered heterocycles, and C 1~6 Selected from those independently of the haloalkyl, and optionally substituted with one or more substituents. In some embodiments, each R 8 These are independently: hydrogen and halogens; as well as C 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl and C 3~10 A carbon ring, each of which is a halogen, -CN, -OH, -NH2, C 3~10 Carbon rings, and C 3~10 The carbon ring is optionally substituted with one or more substituents independently selected from the carbon ring, each of which may be a halogen, -CN, -OH, or -OC. 1~6 Alkyl, -SC 1~6 Alkyl, -SO2-C 1~6 Alkyl, -N(C 1~6 Alkyl)2,-NH(C1~6 Alkyl), C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Selected from those which are optionally substituted with one or more substituents independently selected from the alkynyl. In some embodiments, each R 8 Hydrogen is independent of C 1~6 Alkyl, and C 3~10 A carbon ring, where each of these is a halogen, C 3~10 Those which are optionally substituted with one or more substituents independently selected from the carbon ring; and C 3~10 A carbon ring is selected, each of which is optionally substituted with -OH. In some embodiments, each R 8 These are hydrogen, methyl, ethyl, propyl, isopropyl, cyclopropyl, isobutyl, -CF3, -CH2CF3, -CH2CHF2, -CH2CF(Me)2, -CH2CHMe2, or -CH2-phenyl.
[0114] In some embodiments, each R 8a These are independently: hydrogen, halogen, C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Selected from alkynyl. In some embodiments, each R 8a These are independently: hydrogen and C 1~6 Selected from alkyl groups. In some embodiments, each R 8a The atoms are independently selected from hydrogen and methyl.
[0115] In some embodiments, each R 8b These are independently: hydrogen, halogen, C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Selected from alkynyl. In some embodiments, each R 8b These are independently: hydrogen and C 1~6 Selected from alkyl groups. In some embodiments, each R 8bThe atoms are independently selected from hydrogen and methyl.
[0116] In some embodiments, each R 8c These are independently: hydrogen, halogen, C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Selected from alkynyl. In some embodiments, each R 8c These are independently: hydrogen and C 1~6 Selected from alkyl groups. In some embodiments, each R 8c The atoms are independently selected from hydrogen and methyl.
[0117] In some embodiments, each R 8d These are independently: hydrogen, halogen, C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Selected from alkynyl. In some embodiments, each R 8d These are independently: hydrogen and C 1~6 Selected from alkyl groups. In some embodiments, each R 8d The atoms are independently selected from hydrogen and methyl.
[0118] In some embodiments, each R 8e These are independently: hydrogen, halogen, C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Selected from alkynyl. In some embodiments, each R 8e These are independently: hydrogen and C 1~6 Selected from alkyl groups. In some embodiments, each R 8e R is independently selected from hydrogen and methyl. In some embodiments, each R e It is hydrogen independently.
[0119] In some embodiments, each R 8f These are independently: hydrogen, halogen, C 1~6 Alkyl, C 2~6 Alkenyl and C2~6 Selected from alkynyl. In some embodiments, each R 8f These are independently: hydrogen and C 1~6 Selected from alkyl groups. In some embodiments, each R 8f The atoms are independently selected from hydrogen and methyl.
[0120] In some embodiments, each R 8g These are independently: hydrogen, halogen, C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Selected from alkynyl. In some embodiments, each R 8g These are independently: hydrogen and C 1~6 Selected from alkyl groups. In some embodiments, each R 8g The atoms are independently selected from hydrogen and methyl.
[0121] In certain embodiments, with respect to a compound or salt of formula (I) or formula (I'), X 2 is N, and X 1 is C(R), and X 3 is C(R). In some embodiments, X 2 is N, and X 1 is C(R), and X 3 is C(H). In some embodiments, R 1 It is CH3, and R 2 teeth, [ka] In some embodiments, R 1 It is CH3, and R 2 teeth, [ka] In some embodiments, R 1 It is CH2OH, and R 2 teeth, [ka] In some embodiments, R 1 It is CH2OH, and R 2 teeth, [ka] That is the case.
[0122] In certain embodiments, with respect to a compound or salt of formula (I) or formula (I'), X 2 is N, and X 1 is C(CH3), and X 3 is C(R). In some embodiments, X 2 is N, and X 1 is C(CH3), and X 3 is C(H). In some embodiments, X 2 is N, and X 1 is C(CH3), and X 3 is C(H), and R 5 is CH3. In some embodiments, X 2 is N, and X 1 is C(CH3), and X 3 is C(H), and R 6 H is H. In some embodiments, X 2 is N, and X 1 is C(CH3), and X 3 is C(H), and R 4 H is H, and R 4 ' is H. In some embodiments, X 2 is N, and X 1 is C(CH3), and X 3 is C(H), and R 3 H is H. In some embodiments, X 2 is N, and X 1 is C(CH3), and X 3 is C(H), and R 1 is CH3. In some embodiments, X 2 is N, and X 1 is C(CH3), and X 3is C(H), and R 1 is CH2OH. In some embodiments, X 2 is N, and X 1 is C(CH3), and X 3 is C(H), and R 2 teeth, [ka] In some embodiments, X 2 is N, and X 1 is C(CH3), and X 3 is C(H), and R 2 teeth, [ka] In some embodiments, X 2 is N, and X 1 is C(CH3), and X 3 is C(H), and R 1 It is CH3, and R 2 teeth, [ka] In some embodiments, X 2 is N, and X 1 is C(CH3), and X 3 is C(H), and R 1 It is CH3, and R 2 teeth, [ka] In some embodiments, X 2 is N, and X 1 is C(CH3), and X 3 is C(H), and R 1 It is CH2OH, and R 2 teeth, [ka] In some embodiments, X 2is N, and X 1 is C(CH3), and X 3 is C(H), and R 1 It is CH2OH, and R 2 teeth, [ka] In some embodiments, X 2 is N, and X 1 is C(CH3), and X 3 is C(H), and R 5 It is CH3, and R 2 teeth, [ka] In some embodiments, X 2 is N, and X 1 is C(CH3), and X 3 is C(H), and R 5 It is CH3, and R 2 teeth, [ka] In some embodiments, X 2 is N, and X 1 is C(CH3), and X 3 is C(H), and R 1 It is CH3, and R 5 It is CH3, and R 2 teeth, [ka] In some embodiments, X 2 is N, and X 1 is C(CH3), and X 3 is C(H), and R 1 It is CH3, and R 5 It is CH3, and R 2 teeth, [ka] In some embodiments, X 2 is N, and X 1 is C(CH3), and X 3 is C(H), and R 1 It is CH2OH, and R 5 It is CH3, and R 2 teeth, [ka] In some embodiments, X 2 is N, and X 1 is C(CH3), and X 3 is C(H), and R 1 It is CH2OH, and R 5 It is CH3, and R 2 teeth, [ka] That is the case.
[0123] In certain embodiments, with respect to a compound or salt of formula (I) or formula (I'), X 2 is N, and X 1 is C(CN), and X 3 is C(R). In some embodiments, X 2 is N, and X 1 is C(CN), and X 3 is C(H). In some embodiments, X 2 is N, and X 1 C(CN) and X 3 is C(H), and R 5 is CH3. In some embodiments, X 2 is N, and X 1 C(CN) and X 3 is C(H), and R 6 H is H. In some embodiments, X 2 is N, and X 1 C(CN) and X 3 is C(H), and R 4 H is H, and R 4' is H. In some embodiments, X 2 is N, and X 1 C(CN) and X 3 is C(H), and R 3 H is H. In some embodiments, X 2 is N, and X 1 C(CN) and X 3 is C(H), and R 1 is CH3. In some embodiments, X 2 is N, and X 1 C(CN) and X 3 is C(H), and R 1 is CH2OH. In some embodiments, X 2 is N, and X 1 C(CN) and X 3 is C(H), and R 2 teeth, [ka] In some embodiments, X 2 is N, and X 1 C(CN) and X 3 is C(H), and R 2 teeth, [ka] In some embodiments, X 2 is N, and X 1 C(CN) and X 3 is C(H), and R 1 It is CH3, and R 2 teeth, [ka] In some embodiments, X 2 is N, and X 1 C(CN) and X 3 is C(H), and R 1 It is CH3, and R 2 teeth, [ka] In some embodiments, X 2 is N, and X 1 C(CN) and X 3 is C(H), and R 1 It is CH2OH, and R 2 teeth, [ka] In some embodiments, X 2 is N, and X 1 C(CN) and X 3 is C(H), and R 1 It is CH2OH, and R 2 teeth, [ka] In some embodiments, X 2 is N, and X 1 C(CN) and X 3 is C(H), and R 5 It is CH3, and R 2 teeth, [ka] In some embodiments, X 2 is N, and X 1 C(CN) and X 3 is C(H), and R 5 It is CH3, and R 2 teeth, [ka] In some embodiments, X 2 is N, and X 1 C(CN) and X 3 is C(H), and R 1 It is CH3, and R 5 It is CH3, and R 2 teeth, [ka] In some embodiments, X 2 is N, and X 1 C(CN) and X 3 is C(H), and R 1 It is CH3, and R 5 It is CH3, and R 2 teeth, [ka] In some embodiments, X 2 is N, and X 1 C(CN) and X 3 is C(H), and R 1 It is CH2OH, and R 5 It is CH3, and R 2 teeth, [ka] In some embodiments, X 2 is N, and X 1 C(CN) and X 3 is C(H), and R 1 It is CH2OH, and R 5 It is CH3, and R 2 teeth, [ka] That is the case.
[0124] In some embodiments, compounds of formula (I) or formula (I') are compounds 138, 139, 140, 141, 142, 143, 144, 145, 146, 147, 148, 149, 150, 151, 152, 153, 154, 155, 156, 157, 158, 159, 160, 161, 162, 163, 164, 165, 166, 167, 168, 169, 170, 171, 172, 173, 174, 175, 176, 177, 178, 179, 180, 181, 182, 183, 184, 185, 186, 187, 188, 189, 190, 19 1, 192, 193, 194, 195, 196, 197, 198, 199, 200, 201, 202, 203, 204, 205, 206, 207, 208, 209, 210, 211, 212, 213, 214, 215, 216, 217, 218, 219, 220, 221, 222 ,223,224,225,226,227,228,229,230,231,232,233,234,235,236,237,238,239,240,241,242,243,244,245,246,247,248,249,250,251,252,253, 254, 255, 256, 257, 258, 259, 260, 261, 262, 263, 264, 265, 266, 267, 268, 269, 270, 271, 272, 273, 274, 275, 276, 277, 278, 279, 280, 281, 282, 283, 284, 2 85, 286, 287, 288, 289, 290, 291, 292, 293, 294, 295, 296, 297, 298, 299, 300, 301, 302, 303, 304, 305, 306, 307, 308, 309, 310, 311, 312, 313, 314, 315, 31 6, 317, 318, 319, 320, 321, 322, 323, 324, 325, 326, 327, 328, 329, 330, 331, 332, 333, 334, 335, 336, 337, 338, 339, 340, 341, 342, 343, 344, 345, 346, 347 ,348,349,350,351,352,353,354,355,356,357,358,359,360,361,362,363,364,365,366,367,368,369,370,371,372,373,374,375,376,377,378,379, 380, 381, 382, 383, 384, 385, 386, 387, 388, 389, 390, 391, 392, 393, 394, 395, 396, 397, 398, 399, 400, 401, 402, 403, 404, 405, 406, 407, 408, 409, 410, 411, 412, 413, 414, 415, 416, 417, 418, 419, 420, 421, 422, 423, 424, 425, 426, 427, 428, 429, 430, 431, 432, 433, 434, 435, 436, 437, 438, 439, 440, 441, 442, 443, 444, 445, 446, 447, 448, 449, 450, 451, 452, 453, 454, 455, 456, 457, 458, 459, 460, 461, 462, 463, 464, 465, 466, 467, 468, 469, 470, 471, 472, 473, 474, 475, 476, 477, 478, 479, 480, 481, 482, 483, 484, 485, 486, 487, 488, 489, 490, 491, 492, 493, 494, 495, 496, 497, 498, 499, 500, 501, Selected from 3001, 3002, 3003, 3004, 3005, 3006, 3007, 3008, 3009, 3010, 3011, 3012, 3013, 3502, 3503, 3504, 3505, 3506, 3507, 3508, 3509, 3510, 3511, 3512, 3513, 3514, 3515, 3516, 3517, 3518, and 3519.
[0125] In some embodiments, compounds of formula (I) or formula (I') are compounds 147, 209, 274, 283, 373, 402, 409, 152, 168, 382, 391, 401, 149, 150, 177, 357, 370, 377, 380, 385, 439, 305, 355, 139, 170, 174, 185, 225, 256, 288, 492, 227, 242, 332, 374, 172, 381, 406, 407, 187, 196, 202, 230, 359, 420, 3514, 219, 386, 145, 160, 162, 246, 392, 3 51, 353, 366, 387, 3009, 405, 433, 469, 3502, 376, 414, 154, 167, 365, 262, 384, 173, 3508, 3515, 266, 447, 281, 375, 394, 285, 264, 369, 195, 181, 198, 15 6, 183, 161, 348, 138, 3509, 217, 363, 464, 430, 158, 151, 3510, 193, 204, 232, 419, 3516, 146, 243, 3511, 192, 434, 448, 456, 241, 3010, 179, 389, 349, 35 04, 458, 468, 248, 399, 163, 347, 3519, 143, 350, 489, 169, 3012, 308, 388, 221, 3517, 444, 364, 159, 396, 189, 477, 276, 3001, 361, 255, 428, 476, 411, 4 73, 486, 460, 282, 400, 491, 3512, 368, 395, 191, 3505, 166, 424, 148, 3518, 484, 354, 208, 415, 367, 445, 438, 379, 186, 343, 260, 188, 393, 273, 164, 427 ,250,3507,352,418,398,3011,165,197,200,371,459,275,176,327,441,3503,342,483,472,463,178,284,239,426,3513,410,478,194,155,224, 211, 455, 454, 226, 190, 229, 245, 238, 182, 338, 453, 362, 344, 417, 3004, 299, 345, 431, 306, 488, 223, 157, 212, 432, 278, 304, 254, 153, 413, 171, 358,Selected from 289, 482, 210, 457, 435, 440, 247, 340, 236, 403, 286, 485, 452, 462, 336, 412, 279, 296, 437, 461, and 425.
[0126] In some embodiments, compounds of formula (I) or formula (I') are compounds 147, 209, 274, 283, 373, 402, 409, 152, 168, 382, 391, 401, 149, 150, 177, 357, 370, 377, 380, 385, 439, 305, 355, 139, 170, 174, 185, 225, 256, 288, 492, 227, 242, 332, 374, 172, 381, 406, 407, 187, 196, 202, 230, 359, 420, 3514, 219, 386, 145, 16 0, 162, 246, 392, 351, 353, 366, 387, 3009, 405, 433, 469, 3502, 376, 414, 154, 167, 365, 262, 384, 173, 3508, 3515, 266, 447, 281, 375, 394, 285, 264, 369, 195, 181, 198, 156, 183, 161, 348, 138, 3509, 217, 363, 464, 430, 158, 151, 3510, 193, 204, 232, 419, 3516, 146, 243, 3511, 192, 434, 4 48, 456, 241, 3010, 179, 389, 349, 3504, 458, 468, 248, 399, 163, 347, 3519, 143, 350, 489, 169, 3012, 308, 388, 221, 3517, 444, 364, 159, 396, 189, 477, 276, 3001, 361, 255, 428, 476, 411, 473, 486, 460, 282, 400, 491, 3512, 368, 395, 191, 3505, 166, 424, 148, 3518, 484, 354, 208, 415, 367 Selected from 445, 438, 379, 186, 343, 260, 188, 393, 273, 164, 427, 250, 3507, 352, 418, 398, 3011, 165, 197, 200, 371, 459, 275, 176, 327, 441, 3503, 342, 483, 472, 463, 178, 284, 239, 426, 3513, 410, 478, 194, 155, 224, 211, 455, 454, 226, 190, 229, 245, 238, 182, 338, 453, 362, 344, and 417.
[0127] In some embodiments, compounds of formula (I) or formula (I') are compounds 147, 209, 274, 283, 373, 402, 409, 152, 168, 382, 391, 401, 149, 150, 177, 357, 370, 377, 380, 385, 439, 305, 355, 139, 170, 17 4, 185, 225, 256, 288, 492, 227, 242, 332, 374, 172, 381, 406, 407, 187, 196, 202, 230, 359, 420, 3514, 219, 386, 145, 160, 162, 246, 392, 351, 353, 366, 387, 3009, 405, 4 33, 469, 3502, 376, 414, 154, 167, 365, 262, 384, 173, 3508, 3515, 266, 447, 281, 375, 394, 285, 264, 369, 195, 181, 198, 156, 183, 161, 348, 138, 3509, 217, 363, 464, 43 Selected from 0, 158, 151, 3510, 193, 204, 232, 419, 3516, 146, 243, 3511, 192, 434, 448, 456, 241, 3010, 179, 389, 349, 3504, 458, 468, 248, 399, 163, 347, 3519, 143, and 350.
[0128] In some embodiments, the compound of formula (I) or formula (I') is selected from compounds 147, 209, 274, 283, 373, 402, 409, 152, 168, 382, 391, 401, 149, 150, 177, 357, 370, 377, 380, 385, 439, 305, 355, 139, 170, 174, 185, 225, 256, 288, 492, 227, 242, 332, 374, 172, 381, 406, and 407.
[0129] In some embodiments, compounds of formula (I) or formula (I') are compounds 185, 152, 177, 283, 149, 162, 147, 373, 274, 3514, 209, 355, 246, 285, 139, 198, 464, 402, 256, 401, 332, 288, 382, 3515, 391, 377, 3508, 173, 357, 381, 353, 3502, 492, 385, 407, 374, 406, 393, 439, 3509, 242, 394, 154, 174, 305, 489, 409, 227, 433, 262, 150, 146, 380, 476, 202, 151, 365, 230, 351, 170, 266, 405, 167, 282, 138, 161, 3510, 376, 187, 486, 366, 468, 3516, 386, 469, 255, 158, 428, 350, 403, 3517, 179, 3009, 243, 160, 420, 225, 181, 477, 392, 3511, 264, 232, 363, 195, 248, 148, 156, 396, 487, 3010, 168, 36 1, 456, 172, 434, 273, 241, 196, 375, 364, 3504, 488, 349, 281, 3503, 3007, 379, 472, 193, 159, 183, 348, 143, 473, 217, 219, 448, 438, 204, 327, 245, 417, 343, 208, 145, 447, 169, 284, 239, 238, 491, 430, 384, 308, 415, 3505, 189, 414, 192, 276, 461, 483, 3519, 424, 3001, 399, 3507 Selected from 435, 176, 178, 347, 445, 444, 164, 427, 254, 157, 463, 460, 352, 397, 478, 269, 229, 212, 182, 367, 388, 188, 475, 404, 368, 390, 190, 221, 395, 370, 418, 354, 197, 431, 345, 342, 454, 211, 358, 3012, 398, 369, 223, 3513, 155, 482, 258, 426, 199, 471, 432, 250, 277, and 344.
[0130] In some embodiments, compounds of formula (I) or formula (I') are compounds 185, 152, 177, 283, 149, 162, 147, 373, 274, 3514, 209, 355, 246, 285, 139, 198, 464, 402, 256, 401, 332, 288, 382, 3515, 391, 377, 3508, 173 ,357,381,353,3502,492,385,407,374,406,393,439,3509,242,394,154,174,305,489,409,227,433,262,150,146,380,476,202,151,365,230,351,170,266,405,167,282,138 ,161,3510,376,187,486,366,468,3516,386,469,255,158,428,350,403,3517,179,3009,243,160,420,225,181,477,392,3511,264,232,363,195,248,148,156,396,487,3010 Selected from 168, 361, 456, 172, 434, 273, 241, 196, 375, 364, 3504, 488, 349, 281, 3503, 3007, 379, 472, 193, 159, 183, 348, 143, 473, 217, 219, 448, 438, 204, 327, 245, 417, 343, and 208.
[0131] In some embodiments, a compound of formula (I) or formula (I') is selected from the compounds.
[0132] In some embodiments, compounds of formula (I) or formula (I') are compounds 185, 152, 177, 283, 149, 162, 147, 373, 274, 3514, 209, 355, 246, 285, 139, 198, 464, 402, 256, 401, 332, 288, 382, 3515, 391, 377, 35 Select from 08, 173, 357, 381, 353, 3502, 492, 385, 407, 374, 406, 393, 439, 3509, 242, 394, 154, 174, 305, 489, 409, 227, 433, 262, 150, 146, 380, 476, 202, 151, 365, 230, and 351.
[0133] In some embodiments, the compound of formula (I) or formula (I') is selected from compounds 185, 152, and 177.
[0134] In some embodiments, compounds of formula (I) or formula (I') are compounds 152, 283, 373, 209, 355, 382, 391, 377, 381, 380, 185, 177, 149, 162, 274, 285, 139, 198, 402, 256, 401, 288, 173, 407, 374, 406, 393, 242, 305, 230, 232, 246, 464, 385, 394, 409, 433, 365, 170, 167, 376, 386, 160, 225, 361, 414, 422, 332, 154, 405, 366, 363, 172, 384 ,359,3514,187,447,360,147,3515,357,353,351,158,350,3508,227,392,204,3502,174,395,150,428,181,439,168,202,151,161,195,159,262, 179, 434, 349, 415, 219, 276, 3509, 208, 169, 3510, 243, 248, 241, 375, 448, 417, 444, 196, 352, 403, 420, 354, 387, 419, 200, 486, 421, 266, 156, 476, 398 ,344,3516,430,389,489,3511,226,492,367,473,399,281,423,282,347,404,411,379,400,224,371,3517,435,383,472,362,206,445,368,364,4 16, 432, 284, 348, 370, 456, 469, 396, 192, 264, 236, 438, 143, 157, 3010, 239, 327, 388, 255, 217, 3512, 193, 183, 410, 431, 189, 3503, 245, 273, 201, 350 4, 203, 164, 176, 488, 194, 429, 155, 437, 279, 425, 207, 443, 343, 304, 325, 372, 182, 477, 254, 308, 345, 178, 397, 441, 427, 146, 418, 186, 212, 221, 275 ,346,269,289,148,3012,278,440,138,238,475,153,378,166,487,145,265,468,191,3001,229,197,454,424,446,247,3505,306,233,455,3513,Select from 3004, 210, 390, 483, 491, 213, 286, 141, 453, 3518, 463, 470, 458, 413, 342, 163, 442, 426, 436, 408, 199, 218, 171, 369, 474, 467, 223, 250, 299, 234, 211, 214, 280, 335, 188, 261, 338, 318, 484, 180, 260, 480, 320, 303, 140, 490, 465, 165, 3011, 478, 293, and 277.
[0135] In some embodiments, compounds of formula (I) or formula (I') are compounds 152, 283, 373, 209, 355, 382, 391, 377, 381, 380, 185, 177, 149, 162, 274, 285, 139, 198, 402, 256, 401, 288, 173, 407, 374, 406, 393, 242, 305, 230, 232, 246, 464, 385, 394, 409, 433, 365, 170, 167, 376, 386, 160, 225, 361, 414, 422, 332, 154, 405, 366, 363, 172, 384 ,359,3514,187,447,360,147,3515,357,353,351,158,350,3508,227,392,204,3502,174,395,150,428,181,439,168,202,151,161,195,159,262, 179, 434, 349, 415, 219, 276, 3509, 208, 169, 3510, 243, 248, 241, 375, 448, 417, 444, 196, 352, 403, 420, 354, 387, 419, 200, 486, 421, 266, 156, 476, 398 ,344,3516,430,389,489,3511,226,492,367,473,399,281,423,282,347,404,411,379,400,224,371,3517,435,383,472,362,206,445,368,364,4 16, 432, 284, 348, 370, 456, 469, 396, 192, 264, 236, 438, 143, 157, 3010, 239, 327, 388, 255, 217, 3512, 193, 183, 410, 431, 189, 3503, 245, 273, 201, 350 4, 203, 164, 176, 488, 194, 429, 155, 437, 279, 425, 207, 443, 343, 304, 325, 372, 182, 477, 254, 308, 345, 178, 397, 441, 427, 146, 418, 186, 212, 221, 275 ,346,269,289,148,3012,278,440,138,238,475,153,378,166,487,145,265,468,191,3001,229,197,454,424,446,247,3505,306,233,455,3513,Selected from 3004, 210, 390, 483, 491, 213, 286, 141, 453, 3518, 463, and 470.
[0136] In some embodiments, compounds of formula (I) or formula (I') are compounds 152, 283, 373, 209, 355, 382, 391, 377, 381, 380, 185, 177, 149, 162, 274, 285, 139, 198, 402, 256, 401, 288, 173, 407, 374, 406, 393, 242, 305, 230, 232, 246, 464, 385, 394, 409, 433, 365, 1 70, 167, 376, 386, 160, 225, 361, 414, 422, 332, 154, 405, 366, 363, 172, 384, 359, 3514, 187, 447, 360, 147, 3515, 357, 353, 351, 158, 350, 3508, 227, 392, 204, 3502, 174, 395, 150, 428, 181, 439, 168, 202, 151, 161, 195, 159, 262, 1 79, 434, 349, 415, 219, 276, 3509, 208, 169, 3510, 243, 248, 241, 375, 448, 417, 444, 196, 352, 403, 420, 354, 387, 419, 200, 486, 421, 266, 156, 476, 398, 344, 3516, 430, 389, 489, 3511, 226, 492, 367, 473, 399, 281, 423, 282, 347, 4 Select from 04, 411, 379, 400, 224, 371, 3517, 435, 383, 472, 362, 206, 445, 368, 364, 416, 432, 284, 348, 370, 456, 469, 396, 192, 264, 236, 438, 143, 157, 3010, 239, 327, 388, 255, 217, 3512, 193, 183, 410, 431, 189, 3503, 245, and 273.
[0137] In some embodiments, compounds of formula (I) or formula (I') are compounds 152, 283, 373, 209, 355, 382, 391, 377, 381, 380, 185, 177, 149, 162, 274, 285, 139, 198, 402, 256, 401, 288, 173, 407, 374, 406, 393, 242, 305, 230, 232, 246, 464, 385, 394, 4 Selected from 09, 433, 365, 170, 167, 376, 386, 160, 225, 361, 414, 422, 332, 154, 405, 366, 363, 172, 384, 359, 3514, 187, 447, 360, 147, 3515, 357, 353, 351, 158, 350, 3508, 227, 392, 204, 3502, 174, 395, 150, 428, and 181.
[0138] In one phase, equation (I-ep): [ka] A compound represented by or a salt thereof is disclosed herein, in formula (I-ep): X 1 is selected from C(R) and N; X 2 is selected from C(R) and N; X 3 is selected from C(R) and N; X 4 is selected from C(R) and N; Here X 1 , X 2 , and X 3 At least one of them is N, and X 1 , X 2 , and X 3 Two or fewer of these are N; X 4 is selected from C(R); Each R is independent: Hydrogen; halogen, -NO2, -CN, -OH, -O(C) 1~6 Alkyl), -O(C 1~6 Haloalkyl), -SH, -S(C) 1~6Alkyl), -NH2, -NH(C 1~6 Alkyl), and -N(C 1~6 Alkyl)2; Halogen, -NO2, -CN, -OH, -O(C) 1~6 Alkyl), -O(C 1~6 Haloalkyl), -SH, -S(C) 1~6 Alkyl), -NH2, -NH(C 1~6 Alkyl), and -N(C 1~6 C is optionally substituted with one or more substituents independently selected from alkyl)2. 1~6 alkyl; and C 3~10 Carbon rings and 3- to 10-membered heterocycles; and C 3~10 A carbon ring and a 3-membered to 10-membered heterocycle, each of which is a halogen, -NO2, -CN, -OH, -O(C 1~6 Alkyl), -O(C 1~6 Haloalkyl), -SH, -S(C) 1~6 Alkyl), -NH2, -NH(C 1~6 Alkyl), -N(C 1~6 Alkyl)2, C 1~6 Haloalkyl and C 1~6 Substituted as needed with one or more substituents independently selected from alkyl groups. Selected from; R 1 teeth: hydrogen; Halogen, -NO2, -CN, -OH, -O(C) 1~6 Alkyl), -O(C 1~6 Haloalkyl), -SH, -S(C) 1~6 Alkyl), -NH2, -NH(C 1~6 Alkyl), -N(C 1~6 Alkyl)2, C 3~10 C is optionally substituted with one or more substituents independently selected from carbocyclic and 3- to 10-membered heterocycles. 1~6 alkyl; and C 3~10 A carbon ring and a 3-membered to 10-membered heterocycle, each of which is a halogen, -NO2, -CN, -OH, -O(C1~6 Alkyl), -O(C 1~6 Haloalkyl), -SH, -S(C) 1~6 Alkyl), -NH2, -NH(C 1~6 Alkyl), -N(C 1~6 Alkyl)2, C 1~6 Alkyl, and C 1~6 Substituted as needed with one or more substituents independently selected from the haloalkyl group. Selected from; or R 1 is R 2 Together with C 3~10 They form a carbon ring, or a 3- to 10-membered heterocycle, each of which is a halogen, -NO2, -CN, -OH, -O(C 1~6 Alkyl), -O(C 1~6 Haloalkyl), -SH, -S(C) 1~6 Alkyl), -NH2, -NH(C 1~6 Alkyl), and -N(C 1~6 Alkyl)2, and C 1~6 Substituting as needed with one or more substituents independently selected from alkyl; R 2 teeth: hydrogen; C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkynnyl, each of which is a halogen, -NO2, -CN, -OH, -O(C) 1~6 Alkyl), -O(C 1~6 Haloalkyl), -SH, -S(C) 1~6 Alkyl), -NH2, -NH(C 1~6 Alkyl), -N(C 1~6 Alkyl)2, C 3~10 Those which are optionally substituted with one or more substituents independently selected from carbocyclic and 3- to 10-membered heterocycles; and C 3~10 A carbon ring and a 3-membered to 10-membered heterocycle, each of which is a halogen, -NO2, -CN, -OH, -O(C 1~6 Alkyl), -O(C 1~6Haloalkyl), -SH, -S(C) 1~6 Alkyl), -NH2, -NH(C 1~6 Alkyl), -N(C 1~6 Alkyl)2, C 1~6 Alkyl, and C 1~6 Substituted as needed with one or more substituents independently selected from the haloalkyl group. Selected from; or R 1 is R 2 Together with C 3~10 They form a carbon ring, or a 3- to 10-membered heterocycle, each of which is a halogen, -NO2, -CN, -OH, -O(C 1~6 Alkyl), -O(C 1~6 Haloalkyl), -SH, -S(C) 1~6 Alkyl), -NH2, -NH(C 1~6 Alkyl), -N(C 1~6 Alkyl)2, and C 1~6 Substituting as needed with one or more substituents independently selected from alkyl; R 3 teeth: hydrogen Selected from; R 4 teeth: Hydrogen, halogen, -NO2, -CN, -OH, -O(C) 1~6 Alkyl), -O(C 1~6 Haloalkyl), -SH, -S(C) 1~6 Alkyl), -NH2, -NH(C 1~6 Alkyl), -N(C 1~6 Alkyl)2; Halogen, -NO2, -CN, -OH, -O(C) 1~6 Alkyl), -O(C 1~6 Haloalkyl), -SH, -S(C) 1~6 Alkyl), -NH2, -NH(C 1~6 Alkyl), and -N(C 1~6 C is optionally substituted with one or more substituents independently selected from alkyl)2. 1~6 alkyl; C 3~10A carbon ring and a 3-membered to 10-membered heterocycle, where this C 3~10 Carbon rings and 3- to 10-membered heterocycles are halogens, -NO2, -CN, -OH, -O(C) 1~6 Alkyl), -O(C 1~6 Haloalkyl), -SH, -S(C) 1~6 Alkyl), -NH2, -NH(C 1~6 Alkyl), and -N(C 1~6 Alkyl)2 is independently selected and substituted with one or more substituents as needed. Selected from; R 4 'teeth: Hydrogen, halogens; Halogen, -CN, -OH, -O(C 1~3 Alkyl), -O(C 1~3 Haloalkyl), -NH2, -NH(C) 1~6 Alkyl), and -N(C 1~6 C is optionally substituted with one or more substituents independently selected from alkyl)2. 1~3 alkyl; C 3~10 A carbon ring and a 3-membered to 10-membered heterocycle, where this C 3~10 Carbon rings and 3- to 10-membered heterocycles are halogens, -CN, -OH, -O(C 1~3 Alkyl), -O(C 1~3 Haloalkyl), -NH2, -NH(C) 1~6 Alkyl), and -N(C 1~6 Alkyl)2 is independently selected and substituted with one or more substituents as needed. Selected from; Or R 4 and R 4 'together with C 3~10 They form a carbon ring or a 3- to 10-membered heterocycle, each of which is: halogen, -NO2, -CN, -OH, -O(C 1~6 Alkyl), -O(C 1~6 Haloalkyl), -SH, -S(C) 1~6 Alkyl), -NH2, -NH(C 1~6 Alkyl), and -N(C1~6 Alkyl)2, and C 1~6 Substituting as needed with one or more substituents independently selected from alkyl; R 5 teeth: Hydrogen, halogen, -OH, -O(C) 1~6 Alkyl), -O(C 1~6 Haloalkyl), -SH, -S(C) 1~6 Alkyl), -NH2, -NH(C 1~6 Alkyl), -N(C 1~6 Alkyl)2,-NO2,-CN,C 1~6 Alkyl, C 3~10 Selected from carbon rings and 3-membered to 10-membered heterorings, where this C 1~6 Alkyl, C 3~10 Carbon rings, and 3- to 10-membered heterocycles, are halogens, -NO2, -CN, -OH, -O(C) 1~6 Alkyl), -O(C 1~6 Haloalkyl), -SH, -S(C) 1~6 Alkyl), -NH2, -NH(C 1~6 Alkyl), and -N(C 1~6 Each substituent is optionally substituted with one or more substituents independently selected from alkyl)2; R 6 teeth: hydrogen Selected from.
[0139] In one phase, equation (II): [ka] A compound represented by or a salt thereof is disclosed herein, in formula (II): n is 1, 2, 3, or 4; p is 1, 2, or 3; X 11 C(R 17a ) and N are selected; X 12 C(R 17b ) and N are selected; X 13C(R 17c ) and N are selected; Y 11 C(R 17d ) selected from; Y 12 C(R 17e ) selected from; Each R 11 Independently: Halogen, -NO2, -CN, -N3, -OR 19a , -SR 19a , -N(R 19a )2, -C(O)R 19a ,-C(O)N(R 19a )2, -N(R 19a )C(O)R 19a , -N(R 19a )C(O)N(R 19a )2, -OC(O)N(R 19a )2, -N(R 19a )C(O)OR 19a , -C(O)OR 19a ,-OC(O)R 19a ,-S(O)R 19a , and -S(O)2R 19a ; C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkynnyl, where each of these is a halogen, -OR 19a , -SR 19a , -N(R 19a )2, -C(O)R 19a ,-C(O)N(R 19a )2, -N(R 19a )C(O)R 19a , -C(O)OR 19a ,-OC(O)R 19a , -N(R 19a )C(O)N(R 19a )2, -OC(O)N(R 19a )2, -N(R 19a )C(O)OR 19a ,-S(O)R 19a -S(O)2R 19a -NO2, =O, =S, =N(R 19a ), -N3, -CN, C 3~10It is optionally substituted with one or more substituents independently selected from carbocyclic and 3- to 10-membered heterocycles, where this C 3~10 Carbon rings and 3- to 10-membered heterocycles have one or more R 18a Each of these is replaced as needed; and C 3~10 Carbon rings and 3- to 10-membered heterocycles, each of which is a halogen, -OR 19a , -SR 19a , -N(R 19a )2, -C(O)R 19a ,-C(O)N(R 19a )2, -N(R 19a )C(O)R 19a , -N(R 19a )C(O)N(R 19a )2, -OC(O)N(R 19a )2, -N(R 19a )C(O)OR 19a , -C(O)OR 19a ,-OC(O)R 19a ,-S(O)R 19a -S(O)2R 19a -NO2, =O-, =S, =N(R 19a ), -N3, -CN, C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 It is optionally substituted with one or more substituents independently selected from the alkynyl, where C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl is one or more R 18a Each is replaced as needed. Selected from; R 12 teeth: Hydrogen, halogen, -NO2, -N3, -CN, -OR 19b , -SR 19b , -N(R 19b )2, -C(O)R 19b ,-C(O)N(R 19b )2, -N(R 19b )C(O)R 19b , -N(R19b )C(O)N(R 19b )2, -OC(O)N(R 19b )2, -N(R 19b )C(O)OR 19b , -C(O)OR 19b ,-OC(O)R 19b ,-S(O)R 19b , and -S(O)2R 19b ; C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkynnyl, where each of these is a halogen, -OR 19b , -SR 19b , -N(R 19b )2, -C(O)R 19b ,-C(O)N(R 19b )2, -N(R 19b )C(O)R 19b , -C(O)OR 19b ,-OC(O)R 19b , -N(R 19b )C(O)N(R 19b )2, -OC(O)N(R 19b )2, -N(R 19b )C(O)OR 19b ,-S(O)R 19b -S(O)2R 19b -NO2, =O, =S, =N(R 19b ), -N3, -CN, C 3~10 It is optionally substituted with one or more substituents independently selected from carbocyclic and 3- to 10-membered heterocycles, where this C 3~10 Carbon rings and 3- to 10-membered heterocycles have one or more R 18b Each of these is replaced as needed; and C 3~10 Carbon rings and 3- to 10-membered heterocycles, each of which is a halogen, -OR 19b , -SR 19b , -N(R 19b )2, -C(O)R 19b ,-C(O)N(R 19b )2, -N(R 19b )C(O)R 19b , -N(R19b )C(O)N(R 19b )2, -OC(O)N(R 19b )2, -N(R 19b )C(O)OR 19b , -C(O)OR 19b ,-OC(O)R 19b ,-S(O)R 19b -S(O)2R 19b -NO2, =O-, =S, =N(R 19b ), -N3, -CN, C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 It is optionally substituted with one or more substituents independently selected from the alkynyl, where C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl is one or more R 18b Each is replaced as needed. Selected from; R 13 teeth: Hydrogen, halogen, -OR 19c , -SR 19c , -N(R 19c )2, -N3, -NO2, and -CN; and Halogen, -OR 19c , -SR 19c , -N(R 19c )C as needed, substituted with one or more substituents independently selected from -N3, -NO2, and -CN 1~6 alkyl; and C 3~10 Carbon rings and 3- to 10-membered heterocycles, each of which is a halogen, -OR 19c , -SR 19c , -N(R 19c )2, -C(O)R 19c ,-C(O)N(R 19c )2, -N(R 19c )C(O)R 19c , -N(R 19c )C(O)N(R 19c )2, -OC(O)N(R 19c )2, -N(R 19c)C(O)OR 19c , -C(O)OR 19c ,-OC(O)R 19c ,-S(O)R 19c -S(O)2R 19c , -NO2, -N3, =O-, =S, =N(R 19c ), and one or more substituents selected independently of -CN as needed. Selected from; R 14 teeth: Hydrogen, halogen, -OR 19d , -SR 19d , -N(R 19d )2, -N3, -NO2, and -CN; and C 1~6 Alkyl, halogen, -OR 19d , -SR 19d , -N(R 19d )2, -N3, -NO2, and -CN, which are substituted as needed with one or more substituents independently selected from these; and C 3~10 Carbon rings and 3- to 10-membered heterocycles, each of which is a halogen, -OR 19d , -SR 19d , -N(R 19d )2, -C(O)R 19d ,-C(O)N(R 19d )2, -N(R 19d )C(O)R 19d , -N(R 19d )C(O)N(R 19d )2, -OC(O)N(R 19d )2, -N(R 19d )C(O)OR 19d , -C(O)OR 19d ,-OC(O)R 19d ,-S(O)R 19d -S(O)2R 19d , -NO2, -N3, =O-, =S, =N(R 19d ), and one or more substituents selected independently of -CN as needed. Selected from; or R13 is R 14 Together with C 3~10 It forms a carbon ring, or a 3-membered to 10-membered heterocycle, and here this C 3~10 A carbon ring, or a 3- to 10-membered heterocycle, has one or more R 18c It is replaced as needed; R 14’ teeth: Hydrogen, halogen, -OR 19d , -SR 19d , -N(R 19d )2, -N3, -NO2, and -CN; and C 1~6 Alkyl, halogen, -OR 19d , -SR 19d , -N(R 19d )2, -N3, -NO2, and -CN, which are substituted as needed with one or more substituents independently selected from these; and C 3~10 Carbon rings and 3- to 10-membered heterocycles, each of which is a halogen, -OR 19d , -SR 19d , -N(R 19d )2, -C(O)R 19d ,-C(O)N(R 19d )2, -N(R 19d )C(O)R 19d , -N(R 19d )C(O)N(R 19d )2, -OC(O)N(R 19d )2, -N(R 19d )C(O)OR 19d , -C(O)OR 19d ,-OC(O)R 19d ,-S(O)R 19d -S(O)2R 19d , -NO2, -N3, =O-, =S, =N(R 19d ), and one or more substituents selected independently of -CN as needed. Selected from; or R 13 is R 14’ Together with C 3~10It forms a carbon ring, or a 3-membered to 10-membered heterocycle, and here this C 3~10 A carbon ring, or a 3- to 10-membered heterocycle, has one or more R 18c It is replaced as needed; R 15 teeth: Hydrogen, halogen, -OR 19e , -SR 19e , -N(R 19e )2, -N3, -NO2, and -CN; and One or more R 18d C replaced as needed 1~6 Alkyl Selected from; or R 15 is R 17a Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed; or R 15 is R 17b Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed; R 16 teeth: Hydrogen, halogen, -OR 19f , -SR 19f -N(R 19f )2, -N3, -NO2, and -CN; and One or more R 18e C replaced as needed 1~6 Alkyl Selected from; or R 16 is R 17a Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed; or R 16 is R 17bTogether with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed; Each R 17a Independently: Hydrogen, halogen, -OR 19g , -SR 19g , -N(R 19g )2, -N3, -NO2, -CN, -N3; and C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl, each of which has one or more R 18f Those that are replaced as needed Selected from; or R 15 is R 17a Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed; or R 16 is R 17a Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed; Each R 17b Independently: Hydrogen, halogen, -OR 19g , -SR 19g , -N(R 19g )2, -N3, -NO2, -CN, -N3; and C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl, each of which has one or more R 18f Those that are replaced as needed Selected from; or R 15 is R 17b Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18fIt is replaced as needed; or R 16 is R 17b Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed; each R 17c Independently: Hydrogen, halogen, -OR 19g , -SR 19g , -N(R 19g )2, -N3, -NO2, -CN, -N3; and C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl, each of which has one or more R 18f Those that are replaced as needed Selected from; Each R 17d Independently: Hydrogen, halogen, -OR 19g , -SR 19g , -N(R 19g )2, -N3, -NO2, -CN, -N3; and C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl, each of which has one or more R 18f Those that are replaced as needed Selected from; Each R 17e Independently: Hydrogen, halogen, -OR 19g , -SR 19g , -N(R 19g )2, -N3, -NO2, -CN, -N3; and C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl, each of which has one or more R 18f Those that are replaced as needed Selected from; Each R 18a Independently: Halogen, -OR 19h , -SR 19h , -N(R 19h )2, -C(O)R 19h ,-C(O)N(R 19h )2, -N(R 19h )C(O)R 19h , -N(R 19h )C(O)N(R 19h )2, -OC(O)N(R 19h )2, -N(R 19h )C(O)OR 19h , -C(O)OR 19h ,-OC(O)R 19h ,-S(O)R 19h -S(O)2R 19h , -N3, -NO2, =O, =S, =N(R 19h ), and -CN; and C 1~3 Alkyl, C 2~3 Alkenyl and C 2~3 Alkynnyl, where each of these is a halogen, -OR 19h , -SR 19h , -N(R 19h )2, -C(O)R 19h ,-C(O)N(R 19h )2, -N(R 19h )C(O)R 19h , -N(R 19h )C(O)N(R 19h )2, -OC(O)N(R 19h )2, -N(R 19h )C(O)OR 19h , -C(O)OR 19h ,-OC(O)R 19h ,-S(O)R 19h -S(O)2R 19h , -N3, -NO2, =O, =S, =N(R 19h ), and one or more substituents selected independently of -CN as needed. Selected from; Each R 18b Independently: Halogen, -OR 19h , -SR 19h , -N(R 19h)2, -C(O)R 19h ,-C(O)N(R 19h )2, -N(R 19h )C(O)R 19h , -N(R 19h )C(O)N(R 19h )2, -OC(O)N(R 19h )2, -N(R 19h )C(O)OR 19h , -C(O)OR 19h ,-OC(O)R 19h ,-S(O)R 19h -S(O)2R 19h , -NO2, -N3, =O, =S, =N(R 19h ), and -CN; and C 1~3 Alkyl, C 2~3 Alkenyl and C 2~3 Alkynnyl, where each of these is a halogen, -OR 19h , -SR 19h , -N(R 19h )2, -C(O)R 19h ,-C(O)N(R 19h )2, -N(R 19h )C(O)R 19h , -N(R 19h )C(O)N(R 19h )2, -OC(O)N(R 19h )2, -N(R 19h )C(O)OR 19h , -C(O)OR 19h ,-OC(O)R 19h ,-S(O)R 19h -S(O)2R 19h , -NO2, -N3, =O, =S, =N(R 19h ), and one or more substituents selected independently of -CN as needed. Selected from; Each R 18c Independently: Halogen, -OR 19h , -SR 19h , -N(R 19h )2, -C(O)R 19h ,-C(O)N(R 19h )2, -N(R 19h)C(O)R 19h , -N(R 19h )C(O)N(R 19h )2, -OC(O)N(R 19h )2, -N(R 19h )C(O)OR 19h , -C(O)OR 19h ,-OC(O)R 19h ,-S(O)R 19h -S(O)2R 19h , -NO2, -N3, =O, =S, =N(R 19h ), and -CN; and C 1~3 Alkyl, C 2~3 Alkenyl and C 2~3 Alkynnyl, where each of these is a halogen, -OR 19h , -SR 19h , -N(R 19h )2, -C(O)R 19h ,-C(O)N(R 19h )2, -N(R 19h )C(O)R 19h , -N(R 19h )C(O)N(R 19h )2, -OC(O)N(R 19h )2, -N(R 19h )C(O)OR 19h , -C(O)OR 19h ,-OC(O)R 19h ,-S(O)R 19h -S(O)2R 19h , -NO2, -N3, =O, =S, =N(R 19h ), and one or more substituents selected independently of -CN as needed. Selected from; Each R 18d Independently: Halogen, -OR 19h , -SR 19h , -N(R 19h )2, -C(O)R 19h ,-C(O)N(R 19h )2, -N(R 19h )C(O)R 19h , -N(R 19h )C(O)N(R 19h)2, -OC(O)N(R 19h )2, -N(R 19h )C(O)OR 19h , -C(O)OR 19h ,-OC(O)R 19h ,-S(O)R 19h -S(O)2R 19h , -NO2, -N3, =O, =S, =N(R 19h ), and -CN; and C 1~3 Alkyl, C 2~3 Alkenyl and C 2~3 Alkynnyl, where each of these is a halogen, -OR 19h , -SR 19h , -N(R 19h )2, -C(O)R 19h ,-C(O)N(R 19h )2, -N(R 19h )C(O)R 19h , -N(R 19h )C(O)N(R 19h )2, -OC(O)N(R 19h )2, -N(R 19h )C(O)OR 19h , -C(O)OR 19h ,-OC(O)R 19h ,-S(O)R 19h -S(O)2R 19h , -NO2, -N3, =O, =S, =N(R 19h ), and one or more substituents selected independently of -CN as needed. Selected from; Each R 18e Independently: Halogen, -OR 19h , -SR 19h , -N(R 19h )2, -C(O)R 19h ,-C(O)N(R 19h )2, -N(R 19h )C(O)R 19h , -N(R 19h )C(O)N(R 19h )2, -OC(O)N(R 19h )2, -N(R 19h )C(O)OR 19h, -C(O)OR 19h ,-OC(O)R 19h ,-S(O)R 19h -S(O)2R 19h , -NO2, -N3, =O, =S, =N(R 19h ), and -CN; and C 1~3 Alkyl, C 2~3 Alkenyl and C 2~3 Alkynnyl, where each of these is a halogen, -OR 19h , -SR 19h , -N(R 19h )2, -C(O)R 19h ,-C(O)N(R 19h )2, -N(R 19h )C(O)R 19h , -N(R 19h )C(O)N(R 19h )2, -OC(O)N(R 19h )2, -N(R 19h )C(O)OR 19h , -C(O)OR 19h ,-OC(O)R 19h ,-S(O)R 19h -S(O)2R 19h , -NO2, -N3, =O, =S, =N(R 19h ), and one or more substituents selected independently of -CN as needed. Selected from; Each R 18f Independently: Halogen, -OR 19h , -SR 19h , -N(R 19h )2, -C(O)R 19h ,-C(O)N(R 19h )2, -N(R 19h )C(O)R 19h , -N(R 19h )C(O)N(R 19h )2, -OC(O)N(R 19h )2, -N(R 19h )C(O)OR 19h , -C(O)OR 19h ,-OC(O)R 19h ,-S(O)R 19h-S(O)2R 19h -NO2, =O, =S, =N(R 19h ), and -CN; and C 1~3 Alkyl, C 2~3 Alkenyl and C 2~3 Alkynnyl, where each of these is a halogen, -OR 19h , -SR 19h , -N(R 19h )2, -C(O)R 19h ,-C(O)N(R 19h )2, -N(R 19h )C(O)R 19h , -N(R 19h )C(O)N(R 19h )2, -OC(O)N(R 19h )2, -N(R 19h )C(O)OR 19h , -C(O)OR 19h ,-OC(O)R 19h ,-S(O)R 19h -S(O)2R 19h , -NO2, -N3, =O, =S, =N(R 19h ), and one or more substituents selected independently of -CN as needed. Selected from; Each R 19a Independently: Hydrogen; and C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkynnyl, where each of these is a halogen, -CN, -OH, -SH, -NO2, -NH2, -N3, =O, =S, -OC 1~6 Alkyl, -SC 1~6 Alkyl, -N(C 1~6 Alkyl)2,-NH(C 1~6 Alkyl), C 3~10 A carbon ring, or a 3-membered to 10-membered heterocycle, substituted as necessary with one or more substituents independently selected from these; and C 3~10Carbon rings and 3- to 10-membered heterocycles, each of which is a halogen, -CN, -OH, -SH, -NO2, -NH2, -N3, =O, =S, -OC 1~6 Alkyl, -SC 1~6 Alkyl, -N(C 1~6 Alkyl)2,-NH(C 1~6 Alkyl), C 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 3~10 Carbon rings, 3-membered to 10-membered heterocycles, and C 1~6 Substituted as needed with one or more substituents independently selected from the haloalkyl group. Selected from; Each R 19b Independently: Hydrogen; and C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkynnyl, where each of these is a halogen, -CN, -OH, -SH, -NO2, -NH2, -N3, =O, =S, -OC 1~6 Alkyl, -SC 1~6 Alkyl, -N(C 1~6 Alkyl)2,-NH(C 1~6 Alkyl), C 3~10 A carbon ring, or a 3-membered to 10-membered heterocycle, substituted as necessary with one or more substituents independently selected from these; and C 3~10 Carbon rings and 3- to 10-membered heterocycles, each of which is a halogen, -CN, -OH, -SH, -NO2, -NH2, -N3, =O, =S, -OC 1~6 Alkyl, -SC 1~6 Alkyl, -N(C 1~6 Alkyl)2,-NH(C 1~6 Alkyl), C 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 3~10 Carbon rings, 3-membered to 10-membered heterocycles, and C 1~6Substituted as needed with one or more substituents independently selected from the haloalkyl group. Selected from; Each R 19c Independently: Hydrogen; and C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkynnyl, where each of these is a halogen, -CN, -OH, -SH, -NO2, -NH2, -N3, =O, =S, -OC 1~6 Alkyl, -SC 1~6 Alkyl, -N(C 1~6 Alkyl)2,-NH(C 1~6 Alkyl), C 3~10 A carbon ring, or a 3-membered to 10-membered heterocycle, substituted as necessary with one or more substituents independently selected from these; and C 3~10 Carbon rings and 3- to 10-membered heterocycles, each of which is a halogen, -CN, -OH, -SH, -NO2, -NH2, -N3, =O, =S, -OC 1~6 Alkyl, -SC 1~6 Alkyl, -N(C 1~6 Alkyl)2,-NH(C 1~6 Alkyl), C 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 3~10 Carbon rings, 3-membered to 10-membered heterocycles, and C 1~6 Substituted as needed with one or more substituents independently selected from the haloalkyl group. Selected from; Each R 19d Independently: Hydrogen; and C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkynnyl, where each of these is a halogen, -CN, -OH, -SH, -NO2, -NH2, =O, -N3, =S, -OC 1~6 Alkyl, -SC 1~6 Alkyl, -N(C1~6 Alkyl)2,-NH(C 1~6 Alkyl), C 3~10 A carbon ring, or a 3-membered to 10-membered heterocycle, substituted as necessary with one or more substituents independently selected from these; and C 3~10 Carbon rings and 3- to 10-membered heterocycles, each of which is a halogen, -CN, -OH, -SH, -NO2, -NH2, -N3, =O, =S, -OC 1~6 Alkyl, -SC 1~6 Alkyl, -N(C 1~6 Alkyl)2,-NH(C 1~6 Alkyl), C 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 3~10 Carbon rings, 3-membered to 10-membered heterocycles, and C 1~6 Substituted as needed with one or more substituents independently selected from the haloalkyl group. Selected from; Each R 19e Independently: Hydrogen; and C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkynnyl, each of which is a halogen, -CN, -OH, -SH, -NO2, -NH2, =O, =S, -N3, -OC 1~6 Alkyl, -SC 1~6 Alkyl, -N(C 1~6 Alkyl)2,-NH(C 1~6 Alkyl), C 3~10 A carbon ring, or a 3-membered to 10-membered heterocycle, substituted as necessary with one or more substituents independently selected from these; and C 3~10 Carbon rings and 3- to 10-membered heterocycles, each of which is a halogen, -CN, -OH, -SH, -NO2, -NH2, -N3, =O, =S, -OC 1~6 Alkyl, -SC 1~6 Alkyl, -N(C 1~6 Alkyl)2,-NH(C 1~6Alkyl), C 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 3~10 Carbon rings, 3-membered to 10-membered heterocycles, and C 1~6 Substituted as needed with one or more substituents independently selected from the haloalkyl group. Selected from; Each R 19f Independently: Hydrogen; and C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkynnyl, where each of these is a halogen, -CN, -OH, -SH, -NO2, -NH2, =O, -N3, =S, -OC 1~6 Alkyl, -SC 1~6 Alkyl, -N(C 1~6 Alkyl)2,-NH(C 1~6 Alkyl), C 3~10 A carbon ring, or a 3-membered to 10-membered heterocycle, substituted as necessary with one or more substituents independently selected from these; and C 3~10 Carbon rings and 3- to 10-membered heterocycles, each of which is a halogen, -CN, -OH, -SH, -NO2, -NH2, -N3, =O, =S, -OC 1~6 Alkyl, -SC 1~6 Alkyl, -N(C 1~6 Alkyl)2,-NH(C 1~6 Alkyl), C 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 3~10 Carbon rings, 3-membered to 10-membered heterocycles, and C 1~6 Substituted as needed with one or more substituents independently selected from the haloalkyl group. Selected from; Each R 19g Independently: Hydrogen; and C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6Alkynnyl, where each of these is a halogen, -CN, -OH, -SH, -NO2, -NH2, =O, -N3, =S, -OC 1~6 Alkyl, -SC 1~6 Alkyl, -N(C 1~6 Alkyl)2,-NH(C 1~6 Alkyl), C 3~10 A carbon ring, or a 3-membered to 10-membered heterocycle, substituted as necessary with one or more substituents independently selected from these; and C 3~10 Carbon rings and 3- to 10-membered heterocycles, each of which is a halogen, -CN, -OH, -SH, -NO2, -NH2, -N3, =O, =S, -OC 1~6 Alkyl, -SC 1~6 Alkyl, -N(C 1~6 Alkyl)2,-NH(C 1~6 Alkyl), C 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 3~10 Carbon rings, 3-membered to 10-membered heterocycles, and C 1~6 Substituted as needed with one or more substituents independently selected from the haloalkyl group. Selected from; and Each R 19h Independently: Hydrogen; and C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkynnyl, where each of these is a halogen, -CN, -OH, -SH, -NO2, -NH2, =O, -N3, =S, -OC 1~6 Alkyl, -SC 1~6 Alkyl, -N(C 1~6 Alkyl)2,-NH(C 1~6 Alkyl), C 3~10 A carbon ring, or a 3-membered to 10-membered heterocycle, substituted as necessary with one or more substituents independently selected from these; and C 3~10Carbon rings and 3- to 10-membered heterocycles, each of which is a halogen, -CN, -OH, -SH, -NO2, -NH2, -N3, =O, =S, -OC 1~6 Alkyl, -SC 1~6 Alkyl, -N(C 1~6 Alkyl)2,-NH(C 1~6 Alkyl), C 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 3~10 Carbon rings, 3-membered to 10-membered heterocycles, and C 1~6 Substituted as needed with one or more substituents independently selected from the haloalkyl group. Selected from; Here, at least one R 11 If it is OMe: R 16 teeth: Halogen, -OR 19f , -SR 19f -N(R 19f )2, -N3, -NO2, and -CN; and One or more R 18e C replaced as needed 1~6 Alkyl Selected from; or R 16 is R 17a Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed; or R 16 is R 17b Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed; R 15 and R 17a This means they do not form a ring together; R 15 and R 17b This means they do not form a ring together; R 16 and R 17aThis means that they do not form a ring together; and R 16 and R 17b They do not form a ring together.
[0140] In one phase, equation (II): [ka] A compound represented by or a salt thereof is disclosed herein, in formula (II): n is 1, 2, 3, or 4; p is 1; X 11 C(R 17a ) and N are selected; X 12 C(R 17b ) and N are selected; X 13 C(R 17c ) and N are selected; Y 11 C(R 17d ) selected from; Y 12 C(R 17e ) selected from; Each R 11 Independently: Halogen, -NO2, -CN, -N3, -OR 19a , -SR 19a , -N(R 19a )2, -C(O)R 19a ,-C(O)N(R 19a )2, -N(R 19a )C(O)R 19a , -N(R 19a )C(O)N(R 19a )2, -OC(O)N(R 19a )2, -N(R 19a )C(O)OR 19a , -C(O)OR 19a ,-OC(O)R 19a ,-S(O)R 19a , and -S(O)2R 19a ; C 1~6 Alkyl, C 2~6Alkenyl and C 2~6 Alkynnyl, where each of these is a halogen, -OR 19a , -SR 19a , -N(R 19a )2, -C(O)R 19a ,-C(O)N(R 19a )2, -N(R 19a )C(O)R 19a , -C(O)OR 19a ,-OC(O)R 19a , -N(R 19a )C(O)N(R 19a )2, -OC(O)N(R 19a )2, -N(R 19a )C(O)OR 19a ,-S(O)R 19a -S(O)2R 19a -NO2, =O, =S, =N(R 19a ), -CN, C 3~10 It is optionally substituted with one or more substituents independently selected from carbocyclic and 3- to 10-membered heterocycles, where this C 3~10 Carbon rings and 3- to 10-membered heterocycles have one or more R 18a Each of these is replaced as needed; and C 3~10 Carbon rings and 3- to 10-membered heterocycles, each of which is a halogen, -OR 19a , -SR 19a , -N(R 19a )2, -C(O)R 19a ,-C(O)N(R 19a )2, -N(R 19a )C(O)R 19a , -N(R 19a )C(O)N(R 19a )2, -OC(O)N(R 19a )2, -N(R 19a )C(O)OR 19a , -C(O)OR 19a ,-OC(O)R 19a ,-S(O)R 19a -S(O)2R 19a -NO2, =O-, =S, =N(R 19a ), -CN, C 1~6 Alkyl, C2~6 Alkenyl and C 2~6 It is optionally substituted with one or more substituents independently selected from the alkynyl, where C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl is one or more R 18a Each is replaced as needed. Selected from; R 12 teeth: Hydrogen, halogen, -NO2, -CN, -OR 19b , -SR 19b , -N(R 19b )2, -C(O)R 19b ,-C(O)N(R 19b )2, -N(R 19b )C(O)R 19b , -N(R 19b )C(O)N(R 19b )2, -OC(O)N(R 19b )2, -N(R 19b )C(O)OR 19b , -C(O)OR 19b ,-OC(O)R 19b ,-S(O)R 19b , and -S(O)2R 19b ; C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkynnyl, where each of these is a halogen, -OR 19b , -SR 19b , -N(R 19b )2, -C(O)R 19b ,-C(O)N(R 19b )2, -N(R 19b )C(O)R 19b , -C(O)OR 19b ,-OC(O)R 19b , -N(R 19b )C(O)N(R 19b )2, -OC(O)N(R 19b )2, -N(R 19b )C(O)OR 19b ,-S(O)R 19b -S(O)2R19b -NO2, =O, =S, =N(R 19b ), -CN, C 3~10 It is optionally substituted with one or more substituents independently selected from carbocyclic and 3- to 10-membered heterocycles, where this C 3~10 Carbon rings and 3- to 10-membered heterocycles have one or more R 18b Each of these is replaced as needed; and C 3~10 Carbon rings and 3- to 10-membered heterocycles, each of which is a halogen, -OR 19b , -SR 19b , -N(R 19b )2, -C(O)R 19b ,-C(O)N(R 19b )2, -N(R 19b )C(O)R 19b , -N(R 19b )C(O)N(R 19b )2, -OC(O)N(R 19b )2, -N(R 19b )C(O)OR 19b , -C(O)OR 19b ,-OC(O)R 19b ,-S(O)R 19b -S(O)2R 19b -NO2, =O-, =S, =N(R 19b ), -CN, C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 It is optionally substituted with one or more substituents independently selected from the alkynyl, where C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl is one or more R 18b Each is replaced as needed. Selected from; R 13 teeth: Hydrogen, halogen, -OR 19c , -SR 19c , -N(R 19c )2, -NO2, and -CN; and Halogen, -OR19c , -SR 19c , -N(R 19c )C as needed, substituted with one or more substituents independently selected from -NO2 and -CN 1~6 alkyl; and C 3~10 Carbon rings and 3- to 10-membered heterocycles, each of which is a halogen, -OR 19c , -SR 19c , -N(R 19c )2, -C(O)R 19c ,-C(O)N(R 19c )2, -N(R 19c )C(O)R 19c , -N(R 19c )C(O)N(R 19c )2, -OC(O)N(R 19c )2, -N(R 19c )C(O)OR 19c , -C(O)OR 19c ,-OC(O)R 19c ,-S(O)R 19c -S(O)2R 19c -NO2, =O-, =S, =N(R 19c ), and one or more substituents selected independently of -CN as needed. Selected from; R 14 teeth: Hydrogen, halogen, -OR 19d , -SR 19d , -N(R 19d )2, -NO2, and -CN; and C 1~6 Alkyl, halogen, -OR 19d , -SR 19d , -N(R 19d )2, -NO2, and -CN, which are substituted as needed with one or more substituents independently selected from these; and C 3~10 Carbon rings and 3- to 10-membered heterocycles, each of which is a halogen, -OR 19d , -SR 19d , -N(R 19d )2, -C(O)R19d ,-C(O)N(R 19d )2, -N(R 19d )C(O)R 19d , -N(R 19d )C(O)N(R 19d )2, -OC(O)N(R 19d )2, -N(R 19d )C(O)OR 19d , -C(O)OR 19d ,-OC(O)R 19d ,-S(O)R 19d -S(O)2R 19d -NO2, =O-, =S, =N(R 19d ), and one or more substituents selected independently of -CN as needed. Selected from; or R 13 is R 14 Together with C 3~10 It forms a carbon ring, or a 3-membered to 10-membered heterocycle, and here this C 3~10 A carbon ring, or a 3- to 10-membered heterocycle, has one or more R 18c It is replaced as needed; R 14’ teeth: Hydrogen, halogen, -OR 19d , -SR 19d , -N(R 19d )2, -NO2, and -CN; and C 1~6 Alkyl, halogen, -OR 19d , -SR 19d , -N(R 19d )2, -NO2, and -CN, which are substituted as needed with one or more substituents independently selected from these; and C 3~10 Carbon rings and 3- to 10-membered heterocycles, each of which is a halogen, -OR 19d , -SR 19d , -N(R 19d )2, -C(O)R 19d ,-C(O)N(R 19d )2, -N(R 19d )C(O)R 19d , -N(R19d )C(O)N(R 19d )2, -OC(O)N(R 19d )2, -N(R 19d )C(O)OR 19d , -C(O)OR 19d ,-OC(O)R 19d ,-S(O)R 19d -S(O)2R 19d -NO2, =O-, =S, =N(R 19d ), and one or more substituents selected independently of -CN as needed. Selected from; or R 13 is R 14’ Together with C 3~10 It forms a carbon ring, or a 3-membered to 10-membered heterocycle, and here this C 3~10 A carbon ring, or a 3- to 10-membered heterocycle, has one or more R 18c It is replaced as needed; R 15 teeth: Hydrogen, halogen, -OR 19e , -SR 19e , -N(R 19e )2, -NO2, and -CN; and One or more R 18d C replaced as needed 1~6 Alkyl Selected from; or R 15 is R 17a Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed; or R 15 is R 17b Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed; R 16 teeth: Hydrogen, halogen, -OR 19f , -SR 19f -N(R19f )2, -NO2, and -CN; and One or more R 18e C replaced as needed 1~6 Alkyl Selected from; or R 16 is R 17a Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed; or R 16 is R 17b Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed; Each R 17a , R 17b , R 17c , R 17d , and R 17e Independently: Hydrogen, halogen, -OR 19g , -SR 19g , -N(R 19g )2, -NO2, -CN, -N3; and C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl, each of which has one or more R 18f Those that are replaced as needed Selected from; or R 15 is R 17a Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed; or R 15 is R 17b Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed; or R 16 is R17a Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed; R 16 is R 17b Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed; each R 18a Independently: Halogen, -OR 19h , -SR 19h , -N(R 19h )2, -C(O)R 19h ,-C(O)N(R 19h )2, -N(R 19h )C(O)R 19h , -N(R 19h )C(O)N(R 19h )2, -OC(O)N(R 19h )2, -N(R 19h )C(O)OR 19h , -C(O)OR 19h ,-OC(O)R 19h ,-S(O)R 19h -S(O)2R 19h -NO2, =O, =S, =N(R 19h ), and -CN; and C 1~3 Alkyl, C 2~3 Alkenyl and C 2~3 Alkynnyl, where each of these is a halogen, -OR 19h , -SR 19h , -N(R 19h )2, -C(O)R 19h ,-C(O)N(R 19h )2, -N(R 19h )C(O)R 19h , -N(R 19h )C(O)N(R 19h )2, -OC(O)N(R 19h )2, -N(R 19h )C(O)OR 19h , -C(O)OR 19h ,-OC(O)R 19h ,-S(O)R19h -S(O)2R 19h -NO2, =O, =S, =N(R 19h ), and one or more substituents selected independently of -CN as needed. Selected from; Each R 18b Independently: Halogen, -OR 19h , -SR 19h , -N(R 19h )2, -C(O)R 19h ,-C(O)N(R 19h )2, -N(R 19h )C(O)R 19h , -N(R 19h )C(O)N(R 19h )2, -OC(O)N(R 19h )2, -N(R 19h )C(O)OR 19h , -C(O)OR 19h ,-OC(O)R 19h ,-S(O)R 19h -S(O)2R 19h -NO2, =O, =S, =N(R 19h ), and -CN; and C 1~3 Alkyl, C 2~3 Alkenyl and C 2~3 Alkynnyl, where each of these is a halogen, -OR 19h , -SR 19h , -N(R 19h )2, -C(O)R 19h ,-C(O)N(R 19h )2, -N(R 19h )C(O)R 19h , -N(R 19h )C(O)N(R 19h )2, -OC(O)N(R 19h )2, -N(R 19h )C(O)OR 19h , -C(O)OR 19h ,-OC(O)R 19h ,-S(O)R 19h -S(O)2R 19h -NO2, =O, =S, =N(R 19h), and one or more substituents selected independently of -CN as needed. Selected from; Each R 18c Independently: Halogen, -OR 19h , -SR 19h , -N(R 19h )2, -C(O)R 19h ,-C(O)N(R 19h )2, -N(R 19h )C(O)R 19h , -N(R 19h )C(O)N(R 19h )2, -OC(O)N(R 19h )2, -N(R 19h )C(O)OR 19h , -C(O)OR 19h ,-OC(O)R 19h ,-S(O)R 19h -S(O)2R 19h -NO2, =O, =S, =N(R 19h ), and -CN; and C 1~3 Alkyl, C 2~3 Alkenyl and C 2~3 Alkynnyl, where each of these is a halogen, -OR 19h , -SR 19h , -N(R 19h )2, -C(O)R 19h ,-C(O)N(R 19h )2, -N(R 19h )C(O)R 19h , -N(R 19h )C(O)N(R 19h )2, -OC(O)N(R 19h )2, -N(R 19h )C(O)OR 19h , -C(O)OR 19h ,-OC(O)R 19h ,-S(O)R 19h -S(O)2R 19h -NO2, =O, =S, =N(R 19h ), and one or more substituents selected independently of -CN as needed. Selected from; Each R 18d Independently: Halogen, -OR 19h , -SR 19h , -N(R 19h )2, -C(O)R 19h ,-C(O)N(R 19h )2, -N(R 19h )C(O)R 19h , -N(R 19h )C(O)N(R 19h )2, -OC(O)N(R 19h )2, -N(R 19h )C(O)OR 19h , -C(O)OR 19h ,-OC(O)R 19h ,-S(O)R 19h -S(O)2R 19h -NO2, =O, =S, =N(R 19h ), and -CN; and C 1~3 Alkyl, C 2~3 Alkenyl and C 2~3 Alkynnyl, where each of these is a halogen, -OR 19h , -SR 19h , -N(R 19h )2, -C(O)R 19h ,-C(O)N(R 19h )2, -N(R 19h )C(O)R 19h , -N(R 19h )C(O)N(R 19h )2, -OC(O)N(R 19h )2, -N(R 19h )C(O)OR 19h , -C(O)OR 19h ,-OC(O)R 19h ,-S(O)R 19h -S(O)2R 19h -NO2, =O, =S, =N(R 19h ), and one or more substituents selected independently of -CN as needed. Selected from; Each R 18e Independently: Halogen, -OR 19h , -SR19h , -N(R 19h )2, -C(O)R 19h ,-C(O)N(R 19h )2, -N(R 19h )C(O)R 19h , -N(R 19h )C(O)N(R 19h )2, -OC(O)N(R 19h )2, -N(R 19h )C(O)OR 19h , -C(O)OR 19h ,-OC(O)R 19h ,-S(O)R 19h -S(O)2R 19h -NO2, =O, =S, =N(R 19h ), and -CN; and C 1~3 Alkyl, C 2~3 Alkenyl and C 2~3 Alkynnyl, where each of these is a halogen, -OR 19h , -SR 19h , -N(R 19h )2, -C(O)R 19h ,-C(O)N(R 19h )2, -N(R 19h )C(O)R 19h , -N(R 19h )C(O)N(R 19h )2, -OC(O)N(R 19h )2, -N(R 19h )C(O)OR 19h , -C(O)OR 19h ,-OC(O)R 19h ,-S(O)R 19h -S(O)2R 19h -NO2, =O, =S, =N(R 19h ), and one or more substituents selected independently of -CN as needed. Selected from; Each R 18f Independently: Halogen, -OR 19h , -SR 19h , -N(R 19h )2, -C(O)R 19h ,-C(O)N(R 19h)2, -N(R 19h )C(O)R 19h , -N(R 19h )C(O)N(R 19h )2, -OC(O)N(R 19h )2, -N(R 19h )C(O)OR 19h , -C(O)OR 19h ,-OC(O)R 19h ,-S(O)R 19h -S(O)2R 19h -NO2, =O, =S, =N(R 19h ), and -CN; and C 1~3 Alkyl, C 2~3 Alkenyl and C 2~3 Alkynnyl, where each of these is a halogen, -OR 19h , -SR 19h , -N(R 19h )2, -C(O)R 19h ,-C(O)N(R 19h )2, -N(R 19h )C(O)R 19h , -N(R 19h )C(O)N(R 19h )2, -OC(O)N(R 19h )2, -N(R 19h )C(O)OR 19h , -C(O)OR 19h ,-OC(O)R 19h ,-S(O)R 19h -S(O)2R 19h -NO2, =O, =S, =N(R 19h ), and one or more substituents selected independently of -CN as needed. Selected from; Each R 19a Independently: Hydrogen; and C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkynnyl, where each of these is a halogen, -CN, -OH, -SH, -NO2, -NH2, =O, =S, -OC 1~6 Alkyl, -SC 1~6Alkyl, -N(C 1~6 Alkyl)2,-NH(C 1~6 Alkyl), C 3~10 A carbon ring, or a 3-membered to 10-membered heterocycle, substituted as necessary with one or more substituents independently selected from these; and C 3~10 Carbon rings and 3- to 10-membered heterocycles, each of which is a halogen, -CN, -OH, -SH, -NO2, -NH2, =O, =S, -OC 1~6 Alkyl, -SC 1~6 Alkyl, -N(C 1~6 Alkyl)2,-NH(C 1~6 Alkyl), C 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 3~10 Carbon rings, 3-membered to 10-membered heterocycles, and C 1~6 Substituted as needed with one or more substituents independently selected from the haloalkyl group. Selected from; Each R 19b Independently: Hydrogen; and C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkynnyl, where each of these is a halogen, -CN, -OH, -SH, -NO2, -NH2, =O, =S, -OC 1~6 Alkyl, -SC 1~6 Alkyl, -N(C 1~6 Alkyl)2,-NH(C 1~6 Alkyl), C 3~10 A carbon ring, or a 3-membered to 10-membered heterocycle, substituted as necessary with one or more substituents independently selected from these; and C 3~10 Carbon rings and 3- to 10-membered heterocycles, each of which is a halogen, -CN, -OH, -SH, -NO2, -NH2, =O, =S, -OC 1~6 Alkyl, -SC 1~6 Alkyl, -N(C 1~6 Alkyl)2,-NH(C 1~6Alkyl), C 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 3~10 Carbon rings, 3-membered to 10-membered heterocycles, and C 1~6 Substituted as needed with one or more substituents independently selected from the haloalkyl group. Selected from; Each R 19c Independently: Hydrogen; and C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkynnyl, where each of these is a halogen, -CN, -OH, -SH, -NO2, -NH2, =O, =S, -OC 1~6 Alkyl, -SC 1~6 Alkyl, -N(C 1~6 Alkyl)2,-NH(C 1~6 Alkyl), C 3~10 A carbon ring, or a 3-membered to 10-membered heterocycle, substituted as necessary with one or more substituents independently selected from these; and C 3~10 Carbon rings and 3- to 10-membered heterocycles, each of which is a halogen, -CN, -OH, -SH, -NO2, -NH2, =O, =S, -OC 1~6 Alkyl, -SC 1~6 Alkyl, -N(C 1~6 Alkyl)2,-NH(C 1~6 Alkyl), C 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 3~10 Carbon rings, 3-membered to 10-membered heterocycles, and C 1~6 Substituted as needed with one or more substituents independently selected from the haloalkyl group. Selected from; Each R 19d Independently: Hydrogen; and C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6Alkynnyl, where each of these is a halogen, -CN, -OH, -SH, -NO2, -NH2, =O, =S, -OC 1~6 Alkyl, -SC 1~6 Alkyl, -N(C 1~6 Alkyl)2,-NH(C 1~6 Alkyl), C 3~10 A carbon ring, or a 3-membered to 10-membered heterocycle, substituted as necessary with one or more substituents independently selected from these; and C 3~10 Carbon rings and 3- to 10-membered heterocycles, each of which is a halogen, -CN, -OH, -SH, -NO2, -NH2, =O, =S, -OC 1~6 Alkyl, -SC 1~6 Alkyl, -N(C 1~6 Alkyl)2,-NH(C 1~6 Alkyl), C 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 3~10 Carbon rings, 3-membered to 10-membered heterocycles, and C 1~6 Substituted as needed with one or more substituents independently selected from the haloalkyl group. Selected from; Each R 19e Independently: Hydrogen; and C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkynnyl, where each of these is a halogen, -CN, -OH, -SH, -NO2, -NH2, =O, =S, -OC 1~6 Alkyl, -SC 1~6 Alkyl, -N(C 1~6 Alkyl)2,-NH(C 1~6 Alkyl), C 3~10 A carbon ring, or a 3-membered to 10-membered heterocycle, substituted as necessary with one or more substituents independently selected from these; and C 3~10Carbon rings and 3- to 10-membered heterocycles, each of which is a halogen, -CN, -OH, -SH, -NO2, -NH2, =O, =S, -OC 1~6 Alkyl, -SC 1~6 Alkyl, -N(C 1~6 Alkyl)2,-NH(C 1~6 Alkyl), C 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 3~10 Carbon rings, 3-membered to 10-membered heterocycles, and C 1~6 Substituted as needed with one or more substituents independently selected from the haloalkyl group. Selected from; Each R 19f Independently: Hydrogen; and C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkynnyl, where each of these is a halogen, -CN, -OH, -SH, -NO2, -NH2, =O, =S, -OC 1~6 Alkyl, -SC 1~6 Alkyl, -N(C 1~6 Alkyl)2,-NH(C 1~6 Alkyl), C 3~10 A carbon ring, or a 3-membered to 10-membered heterocycle, substituted as necessary with one or more substituents independently selected from these; and C 3~10 Carbon rings and 3- to 10-membered heterocycles, each of which is a halogen, -CN, -OH, -SH, -NO2, -NH2, =O, =S, -OC 1~6 Alkyl, -SC 1~6 Alkyl, -N(C 1~6 Alkyl)2,-NH(C 1~6 Alkyl), C 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 3~10 Carbon rings, 3-membered to 10-membered heterocycles, and C 1~6 Substituted as needed with one or more substituents independently selected from the haloalkyl group. Selected from; Each R 19g Independently: Hydrogen; and C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkynnyl, where each of these is a halogen, -CN, -OH, -SH, -NO2, -NH2, =O, =S, -OC 1~6 Alkyl, -SC 1~6 Alkyl, -N(C 1~6 Alkyl)2,-NH(C 1~6 Alkyl), C 3~10 A carbon ring, or a 3-membered to 10-membered heterocycle, substituted as necessary with one or more substituents independently selected from these; and C 3~10 Carbon rings and 3- to 10-membered heterocycles, each of which is a halogen, -CN, -OH, -SH, -NO2, -NH2, =O, =S, -OC 1~6 Alkyl, -SC 1~6 Alkyl, -N(C 1~6 Alkyl)2,-NH(C 1~6 Alkyl), C 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 3~10 Carbon rings, 3-membered to 10-membered heterocycles, and C 1~6 Substituted as needed with one or more substituents independently selected from the haloalkyl group. Selected from; and Each R 19h Independently: Hydrogen; and C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkynnyl, where each of these is a halogen, -CN, -OH, -SH, -NO2, -NH2, =O, =S, -OC 1~6 Alkyl, -SC 1~6 Alkyl, -N(C 1~6 Alkyl)2,-NH(C 1~6 Alkyl), C 3~10A carbon ring, or a 3-membered to 10-membered heterocycle, substituted as necessary with one or more substituents independently selected from these; and C 3~10 Carbon rings and 3- to 10-membered heterocycles, each of which is a halogen, -CN, -OH, -SH, -NO2, -NH2, =O, =S, -OC 1~6 Alkyl, -SC 1~6 Alkyl, -N(C 1~6 Alkyl)2,-NH(C 1~6 Alkyl), C 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 3~10 Carbon rings, 3-membered to 10-membered heterocycles, and C 1~6 Substituted as needed with one or more substituents independently selected from the haloalkyl group. Selected from; Here, at least one R 11 If it is OMe, R 16 It is not hydrogen; R 15 and R 17a This means they do not form a ring together; R 15 and R 17b This means they do not form a ring together; R 16 and R 17a This means that they do not form a ring together; and R 16 and R 17b This means they do not form a ring together; Here R 16 ga: halogen, -OR 19f , -SR 19f -N(R 19f )2, -NO2, and -CN; as well as one or more R 18e C replaced as needed 1~6 If selected from alkyl groups; Y 11 Furthermore, it is selected from N; and Y 12 Furthermore, it is selected from N; Here R 16 R 17a Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f If replaced as needed; Y 11 Furthermore, it is selected from N; and Y 12 Furthermore, it is selected from N; and Here R 16 R 17b Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f If replaced as needed; Y 11 Furthermore, it is selected from N; and Y 12 Furthermore, it is selected from N.
[0141] In some embodiments, the compound of formula (II) or formula (II'), the variables n and p can each be any suitable variables known to those skilled in the art. In some embodiments, n is 1, 2, 3, or 4. In some embodiments, n is 0, 1, 2, 3, or 4. In some embodiments, n is 1, 2, or 3. In some embodiments, n is 1. In some embodiments, n is 2. In some embodiments, n is 3. In some embodiments, n is 4. In some embodiments, n is 1 or 2. In some embodiments, n is 0 or 1. In some embodiments, n is 0 or 2. In some embodiments, n is 0 or 3. In some embodiments, n is 0 or 4. In some embodiments, n is 1 or 2. In some embodiments, n is 1 or 3. In some embodiments, n is 1 or 4. In some embodiments, n is 2 or 3. In some embodiments, n is 2 or 4. In some embodiments, n is 3 or 4. In some embodiments, n is 0, 1, or 2. In some embodiments, n is 0, 1, or 3. In some embodiments, n is 0, 1, or 4. In some embodiments, n is 0, 2, or 3. In some embodiments, n is 0, 2, or 4. In some embodiments, n is 0, 3, or 4. In some embodiments, n is 1, 2, or 3. In some embodiments, n is 1, 2, or 4. In some embodiments, n is 2, 3, or 4. In some embodiments, n is 0, 1, 2, or 3. In some embodiments, n is 0, 1, 2, or 4. In some embodiments, n is 1, 2, 3, or 4. In some embodiments, p is 1. In some embodiments, p is 0. In some embodiments, p is 2. In some embodiments, p is 3. In some embodiments, p is 0 or 1.In some embodiments, p is 0 or 2. In some embodiments, p is 0 or 3. In some embodiments, p is 1 or 2. In some embodiments, p is 1 or 3. In some embodiments, p is 2 or 3. In some embodiments, p is 4. In some embodiments, p is 1 or 4. In some embodiments, p is 1, 2, or 3. In some embodiments, p is 0, 1, or 2. In some embodiments, p is 0, 1, or 3.
[0142] In certain embodiments, with respect to a compound or salt of formula (II) or formula (II'), each R 11 These are independently halogen, -NO2, -N3, -CN, and -OR 19a , -SR 19a , -N(R 19a )2, -C(O)R 19a ; Halogen, -OR 19a , -SR 19a , -N(R 19a )2, -C(O)R 19a ,-C(O)N(R 19a )2, -N(R 19a )C(O)R 19a , -C(O)OR 19a ,-OC(O)R 19a , -N(R 19a )C(O)N(R 19a )2, -OC(O)N(R 19a )2, -N(R 19a )C(O)OR 19a ,-S(O)R 19a -S(O)2R 19a -NO2, =O, =S, =N(R 19a ), -CN, C 3~10 C is optionally substituted with one or more substituents independently selected from carbocyclic and 3- to 10-membered heterocycles. 1~6 Alkyl; as well as halogen, -OR 19a , -SR 19a , -N(R 19a )2, -C(O)R 19a ,-C(O)N(R19a )2, -N(R 19a )C(O)R 19a , -N(R 19a )C(O)N(R 19a )2, -OC(O)N(R 19a )2, -N(R 19a )C(O)OR 19a , -C(O)OR 19a ,-OC(O)R 19a ,-S(O)R 19a -S(O)2R 19a -NO2, =O-, =S, =N(R 19a ), -CN, -N3, C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 C as needed, substituted with one or more substituents independently selected from the alkynyl 3~10 Selected from the carbon ring. In some embodiments, each R 11 These are independently halogen, -N3, -CN, and -OR 19a , -N(R 19a )2, -C(O)R 19a ;C 1~6 alkyl; and C 3~10 Selected from the carbon ring. In some embodiments, each R 11 These are independently: halogen, -N3, -CN, -OR 19a , C 1~6 Alkyl, and C 3~10 Selected from the carbon ring. In some embodiments, each R 11 is -Cl, -F, -Br, -N3, -CN, -OH, -OMe, methyl, or cyclopropyl. In some embodiments, each R 11 R is independently selected from -Cl, -F, -CN, methyl, and cyclopropyl. In some embodiments, each R 11 R is independently selected from -F, -CN, and methyl. In some embodiments, each R 11 R is independently selected from -F and -CN. In some embodiments, R 11 R is selected from halogens. In some embodiments, R 11It is selected from halogens, and Y 12 is selected from C(CN), C(H), and C(F). In some embodiments, R 11 It is selected from halogens, and Y 12 is selected from C(CN). In some embodiments, R 11 It is selected from halogens, and Y 11 is selected from C(H). In some embodiments, R 11 It is selected from halogen, and X 13 is selected from N and C(H). In some embodiments, R 11 It is selected from halogen, and X 1 and X 2 In some embodiments, R 11 It is selected from halogen, and X 11 R is selected from N, C(H), and C(F). In some embodiments, R 11 It is selected from halogen, and X 12 This is selected from N, C(H), and C(F).
[0143] In some embodiments, R 11 is selected from F. In some embodiments, R 11 is selected from F, and Y 12 is selected from C(CN), C(H), and C(F). In some embodiments, R 11 is selected from F, and Y 12 is selected from C(CN). In some embodiments, R 11 is selected from F, and Y 11 is selected from C(H). In some embodiments, R 11 It is selected from F, and X 13 is selected from N and C(H). In some embodiments, R 11 It is selected from F, and X 1 and X 2 In some embodiments, R11 It is selected from F, and X 11 R is selected from N, C(H), and C(F). In some embodiments, R 11 It is selected from F, and X 12 This is selected from N, C(H), and C(F).
[0144] In certain embodiments, with respect to a compound or salt of formula (II) or formula (II'), X 11 is N, and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN). In some embodiments, X 11 is N, and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), and R 16 is a C1 alkyl group which is substituted as needed. In some embodiments, X 11 is N, and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), and R 16 is -CH3. In some embodiments, X 11 is N, and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), and R 15 H is H. In some embodiments, X 11 is N, and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 C(CN) and R 14 H is H, and R 14 ' is H. In some embodiments, X 11is N, and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), and R 12 H is H. In some embodiments, X 11 is N, and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), and R 13 X is selected from CH3, H, and cyclopropyl. In some embodiments, X 11 is N, and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), and R 13 is selected from CH3. In some embodiments, X 11 is N, and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), and R 13 X is selected from cyclopropyl. In some embodiments, X 11 is N, and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), and R 13 is selected from H. In some embodiments, X 11 is N, and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), and R 11 The is selected from CH3, cyclopropyl, F, Cl, Br, CF3, CN, N3, OH, and OMe. In some embodiments, X 11 is N, and X12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), and R 11 X is selected from CH3, F, Cl, Br, CF3, and CN. In some embodiments, X 11 is N, and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), and R 11 X is selected from F, Cl, and CN. In some embodiments, X 11 is N, and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), and R 11 X is selected from F and CN. In some embodiments, X 11 is N, and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), and R 11 is selected from F. In some embodiments, X 11 is N, and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), and R 11 X is selected from CN. In some embodiments, X 11 is N, and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), and n is 1 or 2. In some embodiments, X 11 is N, and X 12 is N, and X 13 is C(H) and Y11 is C(H), and Y 12 is C(CN) and n is 1. In some embodiments, X 11 is N, and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN) and n is 2. In some embodiments, X 11 is N, and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), n is 1 or 2, and R 11 X is selected from CN and F. In some embodiments, X 11 is N, and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), n is 1 or 2, and R 11 X is selected from CN. In some embodiments, X 11 is N, and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), n is 1 or 2, and R 11 X is selected from CN. In some embodiments, X 11 is N, and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), n is 1 or 2, and R 11 is selected from F. In some embodiments, X 11 is N, and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12is C(CN), n is 2, and R 11 X is selected from CN and F. In some embodiments, X 11 is N, and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), n is 2, and R 11 X is selected from CN. In some embodiments, X 11 is N, and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), n is 2, and R 11 is selected from F. In some embodiments, X 11 is N, and X 12 is C(H) and X 13 is N, and Y 11 is C(H), and Y 12 is C(CN). In some embodiments, X 11 is N, and X 12 is C(H) and X 13 is N, and Y 11 is C(H), and Y 12 is C(CN). In some embodiments, X 11 is N, and X 12 is C(H) and X 13 is N, and Y 11 is C(H), and Y 12 is C(CN), and R 16 is a C1 alkyl group which is substituted as needed. In some embodiments, X 11 is N, and X 12 is C(H) and X 13 is N, and Y 11 is C(H), and Y 12 is C(CN), and R 16 is -CH3. In some embodiments, X 11 is N, and X 12is C(H) and X 13 is N, and Y 11 is C(H), and Y 12 is C(CN), and R 15 H is H. In some embodiments, X 11 is N, and X 12 is C(H) and X 13 is N, and Y 11 is C(H), and Y 12 C(CN) and R 14 H is H, and R 14 ' is H. In some embodiments, X 11 is N, and X 12 is C(H) and X 13 is N, and Y 11 is C(H), and Y 12 is C(CN), and R 12 H is H. In some embodiments, X 11 is N, and X 12 is C(H) and X 13 is N, and Y 11 is C(H), and Y 12 is C(CN), and R 13 X is selected from CH3, H, and cyclopropyl. In some embodiments, X 11 is N, and X 12 is C(H) and X 13 is N, and Y 11 is C(H), and Y 12 is C(CN), and R 13 is selected from CH3. In some embodiments, X 11 is N, and X 12 is C(H) and X 13 is N, and Y 11 is C(H), and Y 12 is C(CN), and R 13 X is selected from cyclopropyl. In some embodiments, X 11 is N, and X 12 is C(H) and X 13 is N, and Y 11is C(H), and Y 12 is C(CN), and R 13 is selected from H. In some embodiments, X 11 is N, and X 12 is C(H) and X 13 is N, and Y 11 is C(H), and Y 12 is C(CN), and R 11 The is selected from CH3, cyclopropyl, F, Cl, Br, CF3, CN, N3, OH, and OMe. In some embodiments, X 11 is N, and X 12 is C(H) and X 13 is N, and Y 11 is C(H), and Y 12 is C(CN), and R 11 X is selected from CH3, F, Cl, Br, CF3, and CN. In some embodiments, X 11 is N, and X 12 is C(H) and X 13 is N Ri, Y 11 is C(H), and Y 12 is C(CN), and R 11 X is selected from F, Cl, and CN. In some embodiments, X 11 is N, and X 12 is C(H) and X 13 is N, and Y 11 is C(H), and Y 12 is C(CN), and R 11 X is selected from F and CN. In some embodiments, X 11 is N, and X 12 is C(H) and X 13 is N, and Y 11 is C(H), and Y 12 is C(CN), and R 11 is selected from F. In some embodiments, X 11 is N, and X 12 is C(H) and X13 is N, and Y 11 is C(H), and Y 12 is C(CN), and R 11 X is selected from CN. In some embodiments, X 11 is N, and X 12 is C(H) and X 13 is N, and Y 11 is C(H), and Y 12 is C(CN), and n is 1 or 2. In some embodiments, X 11 is N, and X 12 is C(H) and X 13 is N, and Y 11 is C(H), and Y 12 is C(CN) and n is 1. In some embodiments, X 11 is N, and X 12 is C(H) and X 13 is N, and Y 11 is C(H), and Y 12 is C(CN) and n is 2. In some embodiments, X 11 is N, and X 12 is C(H) and X 13 is N, and Y 11 is C(H), and Y 12 is C(CN), n is 1 or 2, and R 11 X is selected from CN and F. In some embodiments, X 11 is N, and X 12 is C(H) and X 13 is N, and Y 11 is C(H), and Y 12 is C(CN), n is 1 or 2, and R 11 X is selected from CN. In some embodiments, X 11 is N, and X 12 is C(H) and X 13 is N, and Y 11 is C(H), and Y 12 is C(CN), n is 1 or 2, and R11 X is selected from CN. In some embodiments, X 11 is N, and X 12 is C(H) and X 13 is N, and Y 11 is C(H), and Y 12 is C(CN), n is 1 or 2, and R 11 is selected from F. In some embodiments, X 11 is N, and X 12 is C(H) and X 13 is N, and Y 11 is C(H), and Y 12 is C(CN), n is 2, and R 11 X is selected from CN and F. In some embodiments, X 11 is N, and X 12 is C(H) and X 13 is N, and Y 11 is C(H), and Y 12 is C(CN), n is 2, and R 11 X is selected from CN. In some embodiments, X 11 is N, and X 12 is C(H) and X 13 is N, and Y 11 is C(H), and Y 12 is C(CN), n is 2, and R 11 It is selected from F. In some embodiments, X 11 C(F) and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN). In some embodiments, X 11 C(F) and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN). In some embodiments, X 11 C(F) and X12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), and R 16 is a C1 alkyl group which is substituted as needed. In some embodiments, X 11 C(F) and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), and R 16 is -CH3. In some embodiments, X 11 C(F) and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), and R 15 H is H. In some embodiments, X 11 C(F) and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 C(CN) and R 14 H is H, and R 14 ' is H. In some embodiments, X 11 C(F) and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), and R 12 H is H. In some embodiments, X 11 C(F) and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), and R 13 X is selected from CH3, H, and cyclopropyl. In some embodiments, X 11 C(F) and X 12 is N, and X13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), and R 13 is selected from CH3. In some embodiments, X 11 C(F) and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), and R 13 X is selected from cyclopropyl. In some embodiments, X 11 C(F) and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), and R 13 is selected from H. In some embodiments, X 11 C(F) and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), and R 11 The is selected from CH3, cyclopropyl, F, Cl, Br, CF3, CN, N3, OH, and OMe. In some embodiments, X 11 C(F) and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), and R 11 X is selected from CH3, F, Cl, Br, CF3, and CN. In some embodiments, X 11 C(F) and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), and R 11 X is selected from F, Cl, and CN. In some embodiments, X 11 C(F) and X12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), and R 11 X is selected from F and CN. In some embodiments, X 11 C(F) and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), and R 11 is selected from F. In some embodiments, X 11 C(F) and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), and R 11 X is selected from CN. In some embodiments, X 11 C(F) and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), and n is 1 or 2. In some embodiments, X 11 C(F) and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN) and n is 1. In some embodiments, X 11 C(F) and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN) and n is 2. In some embodiments, X 11 C(F) and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12is C(CN), n is 1 or 2, and R 11 X is selected from CN and F. In some embodiments, X 11 C(F) and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), n is 1 or 2, and R 11 X is selected from CN. In some embodiments, X 11 C(F) and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), n is 1 or 2, and R 11 X is selected from CN. In some embodiments, X 11 C(F) and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), n is 1 or 2, and R 11 is selected from F. In some embodiments, X 11 C(F) and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), n is 2, and R 11 X is selected from CN and F. In some embodiments, X 11 C(F) and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), n is 2, and R 11 X is selected from CN. In some embodiments, X 11 C(F) and X 12 is N, and X 13 is C(H) and Y 11is C(H), and Y 12 is C(CN), n is 2, and R 11 It is selected from F.
[0145] In a particular embodiment, with respect to a compound of formula (II) or formula (II'), [ka] teeth, [ka] isn't it.
[0146] In certain embodiments, with respect to a compound of formula (II) or formula (II'), n is 1 or 2.
[0147] In certain embodiments, with respect to a compound of formula (II) or formula (II'), n is 1 or 2; and [ka] teeth, [ka] isn't it.
[0148] In one phase, equation (II-A): [ka] A compound represented by or a salt thereof is disclosed herein, in formula (II-A): X 11 C(R 17a ) and N are selected; X 12 C(R 17b ) and N are selected; X 13 C(R 17c ) and N are selected; Y 11 C(R 17d ) and N are selected; Y 12 C(R 17e ) and N are selected; Each R 11a , R 11b , R 11c , and R 11d Independently: Hydrogen, halogen, -NO2, -CN, -N3, -OR 19a , -SR 19a , -N(R 19a )2, -C(O)R 19a ,-C(O)N(R 19a )2, -N(R 19a )C(O)R 19a , -N(R 19a )C(O)N(R 19a )2, -OC(O)N(R 19a )2, -N(R 19a )C(O)OR 19a , -C(O)OR 19a ,-OC(O)R 19a ,-S(O)R 19a , and -S(O)2R 19a ; C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkynnyl, where each of these is a halogen, -OR 19a , -SR 19a , -N(R 19a )2, -C(O)R 19a ,-C(O)N(R 19a )2, -N(R 19a )C(O)R 19a , -C(O)OR 19a ,-OC(O)R 19a , -N(R 19a )C(O)N(R 19a )2, -OC(O)N(R 19a )2, -N(R 19a )C(O)OR 19a ,-S(O)R 19a -S(O)2R 19a -NO2, =O, =S, =N(R 19a ), -CN, C 3~10It is optionally substituted with one or more substituents independently selected from carbocyclic and 3- to 10-membered heterocycles, where this C 3~10 Carbon rings and 3- to 10-membered heterocycles are R 18a Those which are independently selected and each is substituted as necessary by one or more substituents; and C 3~10 Carbon rings and 3- to 10-membered heterocycles, each of which is a halogen, -OR 19a , -SR 19a , -N(R 19a )2, -C(O)R 19a ,-C(O)N(R 19a )2, -N(R 19a )C(O)R 19a , -N(R 19a )C(O)N(R 19a )2, -OC(O)N(R 19a )2, -N(R 19a )C(O)OR 19a , -C(O)OR 19a ,-OC(O)R 19a ,-S(O)R 19a -S(O)2R 19a -NO2, =O-, =S, =N(R 19a ), -CN, C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 It is optionally substituted with one or more substituents independently selected from the alkynyl, where C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl is R 18a One or more substituents, independently selected from the original, each substituted as needed. Selected from; Here R 11a , R 11b , and R 11c When each is hydrogen; R 11d It is not hydrogen; Here R 11b If it is -OCH3; R 11c It is not -OMe; R12 teeth: Hydrogen, halogen, -NO2, -CN, -OR 19b , -SR 19b , -N(R 19b )2, -C(O)R 19b ,-C(O)N(R 19b )2, -N(R 19b )C(O)R 19b , -N(R 19b )C(O)N(R 19b )2, -OC(O)N(R 19b )2, -N(R 19b )C(O)OR 19b , -C(O)OR 19b ,-OC(O)R 19b ,-S(O)R 19b , and -S(O)2R 19b ; C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkynnyl, where each of these is a halogen, -OR 19b , -SR 19b , -N(R 19b )2, -C(O)R 19b ,-C(O)N(R 19b )2, -N(R 19b )C(O)R 19b , -C(O)OR 19b ,-OC(O)R 19b , -N(R 19b )C(O)N(R 19b )2, -OC(O)N(R 19b )2, -N(R 19b )C(O)OR 19b ,-S(O)R 19b -S(O)2R 19b -NO2, =O, =S, =N(R 19b ), -CN, C 3~10 It is optionally substituted with one or more substituents independently selected from carbocyclic and 3- to 10-membered heterocycles, where this C 3~10 Carbon rings and 3- to 10-membered heterocycles are R 18b Those which are independently selected and each is substituted as necessary by one or more substituents; and C3~10 Carbon rings and 3- to 10-membered heterocycles, each of which is a halogen, -OR 19b , -SR 19b , -N(R 19b )2, -C(O)R 19b ,-C(O)N(R 19b )2, -N(R 19b )C(O)R 19b , -N(R 19b )C(O)N(R 19b )2, -OC(O)N(R 19b )2, -N(R 19b )C(O)OR 19b , -C(O)OR 19b ,-OC(O)R 19b ,-S(O)R 19b -S(O)2R 19b -NO2, =O-, =S, =N(R 19b ), -CN, C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 It is optionally substituted with one or more substituents independently selected from the alkynyl, where C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl is R 18b One or more substituents, independently selected from the original, each substituted as needed. Selected from; R 13 teeth: Hydrogen, halogen, -OR 19c , -SR 19c , -N(R 19c )2, -NO2, and -CN; and Halogen, -OR 19c , -SR 19c , -N(R 19c )C as needed, substituted with one or more substituents independently selected from -NO2 and -CN 1~6 alkyl; and C 3~10 Carbon rings and 3- to 10-membered heterocycles, each of which is a halogen, -OR 19c , -SR19c , -N(R 19c )2, -C(O)R 19c ,-C(O)N(R 19c )2, -N(R 19c )C(O)R 19c , -N(R 19c )C(O)N(R 19c )2, -OC(O)N(R 19c )2, -N(R 19c )C(O)OR 19c , -C(O)OR 19c ,-OC(O)R 19c ,-S(O)R 19c -S(O)2R 19c Substituted as needed with one or more substituents independently selected from -NO2 and -CN Selected from; R 14 teeth: Hydrogen, halogen, -OR 19d , -SR 19d , -N(R 19d )2, -NO2, and -CN; and C 1~6 Alkyl, halogen, -OR 19d , -SR 19d , -N(R 19d )2, -NO2, and -CN, which are substituted as needed with one or more substituents independently selected from these; and C 3~10 Carbon rings and 3- to 10-membered heterocycles, each of which is a halogen, -OR 19d , -SR 19d , -N(R 19d )2, -C(O)R 19d ,-C(O)N(R 19d )2, -N(R 19d )C(O)R 19d , -N(R 19d )C(O)N(R 19d )2, -OC(O)N(R 19d )2, -N(R 19d )C(O)OR 19d , -C(O)OR 19d ,-OC(O)R 19d ,-S(O)R19d -S(O)2R 19d -NO2, =O-, =S, =N(R 19d ), and one or more substituents selected independently of -CN as needed. Selected from; R 14’ teeth: Hydrogen, halogen, -OR 19d , -SR 19d , -N(R 19d )2, -NO2, and -CN; and C 1~6 Alkyl, halogen, -OR 19d , -SR 19d , -N(R 19d )2, -NO2, and -CN, which are substituted as needed with one or more substituents independently selected from these; and C 3~10 Carbon rings and 3- to 10-membered heterocycles, each of which is a halogen, -OR 19d , -SR 19d , -N(R 19d )2, -C(O)R 19d ,-C(O)N(R 19d )2, -N(R 19d )C(O)R 19d , -N(R 19d )C(O)N(R 19d )2, -OC(O)N(R 19d )2, -N(R 19d )C(O)OR 19d , -C(O)OR 19d ,-OC(O)R 19d ,-S(O)R 19d -S(O)2R 19d -NO2, =O-, =S, =N(R 19d ), and one or more substituents selected independently of -CN as needed. Selected from; or R 14 is R 14’ Together with C 3~10 It forms a carbon ring, or a 3-membered to 10-membered heterocycle, and here this C 3~10A carbon ring, or a 3- to 10-membered heterocycle, is R 18c It is optionally replaced by one or more substituents selected independently of it; R 15 teeth: Hydrogen, halogen, -OR 19e , -SR 19e , -N(R 19e )2, -NO2, and -CN; and R 18d C as needed, substituted with one or more substituents independently selected from 1~6 Alkyl Selected from; or R 15 is R 17a Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed; or R 15 is R 17b Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is R 18f It is optionally replaced by one or more substituents selected independently of it; R 16 teeth: Hydrogen, halogen, -OR 19f , -SR 19f -N(R 19f )2, -NO2, and -CN; and One or more R 18e C replaced as needed 1~6 Alkyl Selected from; or R 16 is R 17a Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed; or R 16 is R 17b Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R18f It is replaced as needed; Each R 17a , R 17b , R 17c , R 17d , and R 17e Independently: Hydrogen, halogen, -OR 19g , -SR 19g , -N(R 19g )2, -NO2, -CN, -N3; and C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl, each of which has one or more R 18f Those that are replaced as needed Selected from; or R 15 is R 17a Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed; or R 15 is R 17b Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed; or R 16 is R 17a Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed; or R 16 is R 17b Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed; or R 15 , R 16 , and R 17b These elements combine to form a bridged heteroring, where this bridged heteroring consists of one or more R elements. 18fIt is replaced as needed; Each R 18a , R 18b , R 18c , R 18d , R 18e , and R 18f Independently: Halogen, -OR 19h , -SR 19h , -N(R 19h )2, -C(O)R 19h ,-C(O)N(R 19h )2, -N(R 19h )C(O)R 19h , -N(R 19h )C(O)N(R 19h )2, -OC(O)N(R 19h )2, -N(R 19h )C(O)OR 19h , -C(O)OR 19h ,-OC(O)R 19h ,-S(O)R 19h -S(O)2R 19h -NO2, =O, =S, =N(R 19h ), and -CN; and C 1~3 Alkyl, C 2~3 Alkenyl and C 2~3 Alkynnyl, where each of these is a halogen, -OR 19h , -SR 19h , -N(R 19h )2, -C(O)R 19h ,-C(O)N(R 19h )2, -N(R 19h )C(O)R 19h , -N(R 19h )C(O)N(R 19h )2, -OC(O)N(R 19h )2, -N(R 19h )C(O)OR 19h , -C(O)OR 19h ,-OC(O)R 19h ,-S(O)R 19h -S(O)2R 19h -NO2, =O, =S, =N(R 19h ), and one or more substituents selected independently of -CN as needed. Selected from; Each R 19a , R 19b , R 19c , R 19d , R 19e , R 19f , R 19g , and R 19h Independently: Hydrogen; and C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkynnyl, where each of these is a halogen, -CN, -OH, -SH, -NO2, -NH2, =O, =S, -OC 1~6 Alkyl, -SC 1~6 Alkyl, -N(C 1~6 Alkyl)2,-NH(C 1~6 Alkyl), C 3~10 A carbon ring, or a 3-membered to 10-membered heterocycle, substituted as necessary with one or more substituents independently selected from these; and C 3~10 Carbon rings and 3- to 10-membered heterocycles, each of which is a halogen, -CN, -OH, -SH, -NO2, -NH2, =O, =S, -OC 1~6 Alkyl, -SC 1~6 Alkyl, -N(C 1~6 Alkyl)2,-NH(C 1~6 Alkyl), C 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 3~10 Carbon rings, 3-membered to 10-membered heterocycles, and C 1~6 Substituted as needed with one or more substituents independently selected from the haloalkyl group. Selected from.
[0149] In certain embodiments, with respect to a compound or salt of formula (II), formula (II'), or formula (II-A), X 11 C(R 17a ) and N are selected. In some embodiments, X 11 C(R 17a) is selected from. In some embodiments, X 11 is selected from N. In a particular embodiment, with respect to a compound or salt of formula (II), X 12 C(R 17b ) and N are selected. In some embodiments, X 12 C(R 17b ) is selected from. In some embodiments, X 12 is selected from N. In a particular embodiment, with respect to a compound or salt of formula (II), X 13 C(R 17c ) and N are selected. In some embodiments, X 13 C(R 17c ) is selected from. In some embodiments, X 13 It is selected from N.
[0150] In certain embodiments, with respect to a compound or salt of formula (II), formula (II-A), or formula (II'), Y 11 C(R 17d ) is selected from. In some embodiments, Y 11 C(R 17d ) and N are selected. In some embodiments, Y 11 is selected from N. In a particular embodiment, with respect to a compound or salt of formula (II), Y 12 C(R 17e ) is selected from. In some embodiments, Y 12 C(R 17e ) and N are selected.
[0151] In certain embodiments, with respect to a compound or salt of formula (II), formula (II-A), or formula (II'), each R 11 R can be any suitable functional group known to those skilled in the art. In some embodiments, each R 11 These are independently: halogen, -NO2, -N3, -CN, -OR 19a , -SR 19a , -N(R 19a )2, -C(O)R 19a,-C(O)N(R 19a )2, -N(R 19a )C(O)R 19a , -N(R 19a )C(O)N(R 19a )2, -OC(O)N(R 19a )2, -N(R 19a )C(O)OR 19a , -C(O)OR 19a ,-OC(O)R 19a ,-S(O)R 19a , and -S(O)2R 19a ;C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkynnyl, where each of these is a halogen, -OR 19a , -SR 19a , -N(R 19a )2, -C(O)R 19a ,-C(O)N(R 19a )2, -N(R 19a )C(O)R 19a , -C(O)OR 19a ,-OC(O)R 19a , -N(R 19a )C(O)N(R 19a )2, -OC(O)N(R 19a )2, -N(R 19a )C(O)OR 19a ,-S(O)R 19a -S(O)2R 19a -NO2, =O, =S, =N(R 19a ), -CN, C 3~10 It is optionally substituted with one or more substituents independently selected from carbocyclic and 3- to 10-membered heterocycles, where this C 3~10 Carbon rings and 3- to 10-membered heterocycles have one or more R 18a Each of these is replaced as needed; and C 3~10 Carbon rings and 3- to 10-membered heterocycles, each of which is a halogen, -OR 19a , -SR 19a , -N(R 19a )2, -C(O)R 19a ,-C(O)N(R 19a )2, -N(R19a )C(O)R 19a , -N(R 19a )C(O)N(R 19a )2, -OC(O)N(R 19a )2, -N(R 19a )C(O)OR 19a , -C(O)OR 19a ,-OC(O)R 19a ,-S(O)R 19a -S(O)2R 19a -NO2, =O-, =S, =N(R 19a ), -CN, C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 It is optionally substituted with one or more substituents independently selected from the alkynyl, where C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl is one or more R 18a Each is then selected from those that have been replaced as needed.
[0152] In certain embodiments, with respect to a compound or salt of formula (II-A), each R 11a , R 11b , R 11c , and R 11d These are independently hydrogen, halogen, -NO2, -N3, -CN, -OR 19a , -SR 19a , -N(R 19a )2, -C(O)R 19a ;C 1~6 Alkyl, which is a halogen, -OR 19a , -SR 19a , -N(R 19a )2, -C(O)R 19a ,-C(O)N(R 19a )2, -N(R 19a )C(O)R 19a , -C(O)OR 19a ,-OC(O)R 19a , -N(R 19a )C(O)N(R 19a )2, -OC(O)N(R 19a )2, -N(R 19a)C(O)OR 19a ,-S(O)R 19a -S(O)2R 19a -NO2, =O, =S, =N(R 19a ), -CN, C 3~10 Those which are optionally substituted with one or more substituents independently selected from carbon rings and 3- to 10-membered heterocycles; and C 3~10 It is a carbon ring, and this is a halogen, -OR 19a , -SR 19a , -N(R 19a )2, -C(O)R 19a ,-C(O)N(R 19a )2, -N(R 19a )C(O)R 19a , -N(R 19a )C(O)N(R 19a )2, -OC(O)N(R 19a )2, -N(R 19a )C(O)OR 19a , -C(O)OR 19a ,-OC(O)R 19a ,-S(O)R 19a -S(O)2R 19a -NO2, =O-, =S, =N(R 19a ), -CN, -N3, C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Selected from those which are optionally substituted with one or more substituents independently selected from the alkynyl. In some embodiments, each R 11a , R 11b , R 11c , and R 11d These are independently hydrogen, halogen, -N3, -CN, and -OR 19a , -N(R 19a )2, -C(O)R 19a ;C 1~6 alkyl; and C 3~10 Selected from the carbon ring. In some embodiments, each R 11a , R 11b , R 11c , and R 11d These are independently: hydrogen, halogen, -N3, -CN, -OR 19a , C1~6 Alkyl, and C 3~10 Selected from the carbon ring. In some embodiments, each R 11a , R 11b , R 11c , and R 11d R is -H, -Cl, -F, -Br, -N3, -CN, -OH, -OMe, methyl, or cyclopropyl. In some embodiments, each R 11a , R 11b , R 11c , and R 11d R is independently selected from -H, -Cl, -F, -CN, methyl, and cyclopropyl. In some embodiments, each R 11a , R 11b , R 11c , and R 11d R is independently selected from -H, -F, -CN, and methyl. In some embodiments, each R 11a , R 11b , R 11c , and R 11d R is independently selected from -H, -F, and -CN. In some embodiments, R 11a , R 11b , and R 11c When each is hydrogen; R 11d It is not hydrogen. In some embodiments, R 11b If it is -OCH3; R 11c is not -OMe. In some embodiments, R 11a , R 11b , and R 11c When each is hydrogen; R 11d is not hydrogen; and R 11b If it is -OCH3; R 11c is not -OMe. In some embodiments, R 11a , R 11b , R 11c , and R 11d Each of these independently consists of hydrogen, -Cl, -F, -Br, -CN, N3, -OH, -OMe, methyl, cyclopropyl, -CH2N(CH3)2, CF3, and [ka] Selected from; here R 11a , R 11b , and R 11c When each is hydrogen; R 11d R is selected from -Cl, -F, -Br, -CN, N3, -OH, -OMe, methyl, cyclopropyl, -CH2N(CH3)2, and CF3; where R 11b If it is -OCH3; R 11c R is independently selected from hydrogen, -Cl, -F, -Br, -CN, N3, -OH, methyl, cyclopropyl, -CH2N(CH3)2, and CF3. In some embodiments, R 11a , R 11b , R 11c , and R 11d Each is independently selected from hydrogen, -F, -CN, and methyl; where R 11a , R 11b , and R 11c When each is hydrogen; R 11d The methyl group is selected from -F, -CN, and methyl.
[0153] In certain embodiments, with respect to a compound or salt of formula (II), formula (II-A), or formula (II'), R 12 R can be any suitable functional group known to those skilled in the art. In some embodiments, R 12 H: Hydrogen, halogen, -NO2, -N3, -CN, -OR 19b , -SR 19b , -N(R 19b )2, -C(O)R 19b ,-C(O)N(R 19b )2, -N(R 19b )C(O)R 19b , -N(R 19b )C(O)N(R 19b )2, -OC(O)N(R 19b )2, -N(R 19b )C(O)OR 19b , -C(O)OR 19b ,-OC(O)R 19b ,-S(O)R 19b , and -S(O)2R 19b ;C1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkynnyl, where each of these is a halogen, -OR 19b , -SR 19b , -N(R 19b )2, -C(O)R 19b ,-C(O)N(R 19b )2, -N(R 19b )C(O)R 19b , -C(O)OR 19b ,-OC(O)R 19b , -N(R 19b )C(O)N(R 19b )2, -OC(O)N(R 19b )2, -N(R 19b )C(O)OR 19b ,-S(O)R 19b -S(O)2R 19b -NO2, =O, =S, =N(R 19b ), -CN, C 3~10 It is optionally substituted with one or more substituents independently selected from carbocyclic and 3- to 10-membered heterocycles, where this C 3~10 Carbon rings and 3- to 10-membered heterocycles have one or more R 18b Each of these is replaced as needed; and C 3~10 Carbon rings and 3- to 10-membered heterocycles, each of which is a halogen, -OR 19b , -SR 19b , -N(R 19b )2, -C(O)R 19b ,-C(O)N(R 19b )2, -N(R 19b )C(O)R 19b , -N(R 19b )C(O)N(R 19b )2, -OC(O)N(R 19b )2, -N(R 19b )C(O)OR 19b , -C(O)OR 19b ,-OC(O)R 19b ,-S(O)R 19b -S(O)2R 19b -NO2, =O-, =S, =N(R 19b ), -CN, C1~6 Alkyl, C 2~6 Alkenyl and C 2~6 It is optionally substituted with one or more substituents independently selected from the alkynyl, where C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl is one or more R 18b Each is selected from those which are replaced as needed. In some embodiments, R 12 H: Hydrogen, halogen, -NO2, -CN, -OR 19b , -SR 19b , -N(R 19b )2, -C(O)R 19b ; and C 1~6 Alkyl, which is a halogen, -OR 19b , -SR 19b , -N(R 19b )2, -C(O)R 19b ,-C(O)N(R 19b )2, -N(R 19b )C(O)R 19b , -C(O)OR 19b ,-OC(O)R 19b , -N(R 19b )C(O)N(R 19b )2, -OC(O)N(R 19b )2, -N(R 19b )C(O)OR 19b ,-S(O)R 19b -S(O)2R 19b -NO2, =O, =S, =N(R 19b ), -CN, C 3~10 Selected from those independently selected from carbon rings and 3- to 10-membered heterocycles, which may be substituted as needed with one or more substituents. In some embodiments, R 12 is hydrogen, halogen, -OR 19b , and C 1~6 Selected from alkyl. In some embodiments, R 12 is hydrogen or C 1~6 It is alkyl. In some embodiments, R 12 It is hydrogen.
[0154] In certain embodiments, with respect to a compound or salt of formula (II), formula (II-A), or formula (II'), R 13 R can be any suitable functional group known to those skilled in the art. In some embodiments, R 13 ha: hydrogen, halogen, -OR 19c , -SR 19c , -N(R 19c )2, -NO2, and -CN; as well as halogens, -OR 19c , -SR 19c , -N(R 19c )C as needed, substituted with one or more substituents independently selected from -NO2 and -CN 1~6 Alkyl; and C 3~10 Carbon rings and 3- to 10-membered heterocycles, each of which is a halogen, -OR 19c , -SR 19c , -N(R 19c )2, -C(O)R 19c ,-C(O)N(R 19c )2, -N(R 19c )C(O)R 19c , -N(R 19c )C(O)N(R 19c )2, -OC(O)N(R 19c )2, -N(R 19c )C(O)OR 19c , -C(O)OR 19c ,-OC(O)R 19c ,-S(O)R 19c -S(O)2R 19c -NO2, =O-, =S, =N(R 19c ), and are selected from those which may be substituted as needed with one or more substituents independently selected from -CN; or R 13 is R 14 Together with C 3~10 It forms a carbon ring, or a 3-membered to 10-membered heterocycle, and here this C 3~10 A carbon ring, or a 3- to 10-membered heterocycle, has one or more R 18c It is replaced as needed. In some embodiments, R 13ha: hydrogen, halogen, -OR 19c , -SR 19c , -N(R 19c )2; and C 1~6 Alkyl, halogen, -OR 19c , -SR 19c , -N(R 19c )2, -NO2, and -CN, which are optionally substituted with one or more substituents independently selected from these; and C 3~10 It is a carbon ring, and this is a halogen, -OR 19c , -SR 19c , -N(R 19c )2, -C(O)R 19c ,-C(O)N(R 19c )2, -N(R 19c )C(O)R 19c , -N(R 19c )C(O)N(R 19c )2, -OC(O)N(R 19c )2, -N(R 19c )C(O)OR 19c , -C(O)OR 19c ,-OC(O)R 19c ,-S(O)R 19c -S(O)2R 19c -NO2, =O-, =S, =N(R 19c ), and are selected from those which may be substituted as needed with one or more substituents independently selected from -CN; or R 13 is R 14 Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18c It is replaced as needed.
[0155] In certain embodiments, with respect to a compound or salt of formula (II), formula (II-A), or formula (II'), R 13 ha: hydrogen, halogen, -OR 19c , C 1~6 Alkyl, and C 3~10 Selected from a carbocyclic ring; or R 13 is R 14Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18c It is replaced as needed. In some embodiments, R 13 ha: hydrogen, -OR 19c , C 1~6 Alkyl and C 3~10 Selected from a carbocyclic ring; or R 13 is R 14 Together with them, they form a 3-membered to 10-membered heteroring. In some embodiments, R 13 is hydrogen, -OH, -OMe, methyl, cyclopropyl, or R 13 is R 14 Together with it, it forms pyridinyl. In some embodiments, R 13 R is hydrogen, -OH, -OMe, methyl, or cyclopropyl. In some embodiments, R 13 R is selected from hydrogen, methyl, ethyl, -OH, -OMe, -CF3, -C(H)F2, -N(H)Me, and cyclopropyl. In some embodiments, R 13 R is selected from hydrogen. In some embodiments, 13 It is selected from methyl.
[0156] In certain embodiments, with respect to a compound or salt of formula (II) or formula (II-A), R 14 R can be any suitable functional group known to those skilled in the art. In some embodiments, R 14 These are independently: hydrogen, halogen, -OR 19d , -SR 19d , -N(R 19d )2, -NO2, and -CN; and C 1~6 Alkyl, halogen, -OR 19d , -SR 19d , -N(R 19d )2, -NO2, and -CN, which are optionally substituted with one or more substituents independently selected from these; and C 3~10 Carbon rings and 3- to 10-membered heterocycles, each of which is a halogen, -OR19d , -SR 19d , -N(R 19d )2, -C(O)R 19d ,-C(O)N(R 19d )2, -N(R 19d )C(O)R 19d , -N(R 19d )C(O)N(R 19d )2, -OC(O)N(R 19d )2, -N(R 19d )C(O)OR 19d , -C(O)OR 19d ,-OC(O)R 19d ,-S(O)R 19d -S(O)2R 19d -NO2, =O-, =S, =N(R 19d ), and are selected from those which may be substituted as needed with one or more substituents independently selected from -CN; or R 13 is R 14 Together with C 3~10 It forms a carbon ring, or a 3-membered to 10-membered heterocycle, and here this C 3~10 A carbon ring, or a 3- to 10-membered heterocycle, has one or more R 18c It is replaced as needed. In some embodiments, R 14 These are independently: hydrogen, halogen, -OR 19d , -SR 19d , -N(R 19d )2, -NO2, and -CN; and C 1~6 Alkyl, halogen, -OR 19d , -SR 19d , -N(R 19d )2, -NO2, and -CN, which are optionally substituted with one or more substituents independently selected from these; and C 3~10 Carbon rings and 3- to 10-membered heterocycles, each of which is a halogen, -OR 19d , -SR 19d , -N(R 19d )2, -C(O)R 19d ,-C(O)N(R 19d )2, -N(R 19d )C(O)R 19d , -N(R19d )C(O)N(R 19d )2, -OC(O)N(R 19d )2, -N(R 19d )C(O)OR 19d , -C(O)OR 19d ,-OC(O)R 19d ,-S(O)R 19d -S(O)2R 19d -NO2, =O-, =S, =N(R 19d ), and are selected from those which are optionally substituted with one or more substituents independently selected from -CN.
[0157] In certain embodiments, with respect to a compound or salt of formula (II) or formula (II-A), R 14 ha: hydrogen, halogen, -OR 19d , -SR 19d , -N(R 19d )2; and C 1~6 Alkyl, halogen, -OR 19d , -SR 19d , -N(R 19d ) Selected from those which are substituted as needed with one or more substituents independently selected from -NO2 and -CN; or R 13 is R 14 Together with C 3~10 It forms a carbon ring, or a 3-membered to 10-membered heterocycle, and here this C 3~10 A carbon ring, or a 3- to 10-membered heterocycle, has one or more R 18c It is replaced as needed. In some embodiments, R 14 ha: hydrogen, halogen, -OR 19d , -SR 19d , -N(R 19d )2; and C 1~6 Alkyl, halogen, -OR 19d , -SR 19d , -N(R 19d )2, -NO2, and -CN are selected independently and optionally substituted with one or more substituents. In some embodiments, R 14ha: hydrogen, halogen, -OR 19d , and C 1~6 Selected from alkyl groups; or R 13 is R 14 Together with C 3~10 It forms a carbon ring or a 3- to 10-membered heterocycle. In some embodiments, R 14 ha: hydrogen, halogen, -OR 19d , and C 1~6 Selected from alkyl. In some embodiments, R 14 is hydrogen, C 1~6 It is alkyl, or R 13 is R 14 Together with C 3~10 It forms a carbon ring or a 3- to 10-membered heterocycle. In some embodiments, R 14 is hydrogen or C 1~6 It is alkyl. In some embodiments, R 14 is hydrogen, methyl, or R 13 is R 14 Together with it, it forms pyridinyl. In some embodiments, R 14 is hydrogen or methyl. In some embodiments, R 14 R is selected from hydrogen, methyl, and fluoro. In some embodiments, R 14 R is selected from hydrogen. In some embodiments, 14 R is selected from hydrogen and methyl. In some embodiments, R 14 R is selected from hydrogen and fluoro. In some embodiments, 14 R is selected from methyl and fluoro. In some embodiments, 14 R is selected from hydrogen and cyano. In some embodiments, 14 is selected from cyanoside. In some embodiments, R 14 and R 14’ Together with these, they form a cyclopropane ring which is optionally substituted with one or more substituents selected from -F and -CH3.
[0158] In certain embodiments, with respect to a compound or salt of formula (II) or formula (II-A), R 14’ R can be any suitable functional group known to those skilled in the art. In some embodiments, R 14’ These are independently: hydrogen, halogen, -OR 19d , -SR 19d , -N(R 19d )2, -NO2, and -CN; and C 1~6 Alkyl, halogen, -OR 19d , -SR 19d , -N(R 19d )2, -NO2, and -CN, which are optionally substituted with one or more substituents independently selected from these; and C 3~10 Carbon rings and 3- to 10-membered heterocycles, each of which is a halogen, -OR 19d , -SR 19d , -N(R 19d )2, -C(O)R 19d ,-C(O)N(R 19d )2, -N(R 19d )C(O)R 19d , -N(R 19d )C(O)N(R 19d )2, -OC(O)N(R 19d )2, -N(R 19d )C(O)OR 19d , -C(O)OR 19d ,-OC(O)R 19d ,-S(O)R 19d -S(O)2R 19d -NO2, =O-, =S, =N(R 19d ), and are selected from those which may be substituted as needed with one or more substituents independently selected from -CN; or R 13 is R 14’ Together with C 3~10 It forms a carbon ring, or a 3-membered to 10-membered heterocycle, and here this C 3~10 A carbon ring, or a 3- to 10-membered heterocycle, has one or more R 18c It is replaced as needed. In some embodiments, R 14’ These are independently: hydrogen, halogen, -OR19d , -SR 19d , -N(R 19d )2, -NO2, and -CN; and C 1~6 Alkyl, halogen, -OR 19d , -SR 19d , -N(R 19d )2, -NO2, and -CN, which are optionally substituted with one or more substituents independently selected from these; and C 3~10 Carbon rings and 3- to 10-membered heterocycles, each of which is a halogen, -OR 19d , -SR 19d , -N(R 19d )2, -C(O)R 19d ,-C(O)N(R 19d )2, -N(R 19d )C(O)R 19d , -N(R 19d )C(O)N(R 19d )2, -OC(O)N(R 19d )2, -N(R 19d )C(O)OR 19d , -C(O)OR 19d ,-OC(O)R 19d ,-S(O)R 19d -S(O)2R 19d -NO2, =O-, =S, =N(R 19d ), and are selected from those which are optionally substituted with one or more substituents independently selected from -CN.
[0159] In certain embodiments, with respect to a compound or salt of formula (II) or formula (II-A), R 14’ ha: hydrogen, halogen, -OR 19d , -SR 19d , -N(R 19d )2; and C 1~6 Alkyl, halogen, -OR 19d , -SR 19d , -N(R 19d ) Selected from those which are substituted as needed with one or more substituents independently selected from -NO2 and -CN; or R 13 is R 14’Together with C 3~10 It forms a carbon ring, or a 3-membered to 10-membered heterocycle, and here this C 3~10 A carbon ring, or a 3- to 10-membered heterocycle, has one or more R 18c It is replaced as needed. In some embodiments, R 14’ ha: hydrogen, halogen, -OR 19d , -SR 19d , -N(R 19d )2; and C 1~6 Alkyl, halogen, -OR 19d , -SR 19d , -N(R 19d )2, -NO2, and -CN are selected independently and optionally substituted with one or more substituents. In some embodiments, R 14’ ha: hydrogen, halogen, -OR 19d , and C 1~6 Selected from alkyl groups; or R 13 is R 14’ Together with C 3~10 It forms a carbon ring or a 3- to 10-membered heterocycle. In some embodiments, R 14’ ha: hydrogen, halogen, -OR 19d , and C 1~6 Selected from alkyl. In some embodiments, R 14’ is hydrogen, C 1~6 It is alkyl, or R 13 is R 14’ Together with C 3~10 It forms a carbon ring or a 3- to 10-membered heterocycle. In some embodiments, R 14’ is hydrogen or C 1~6 It is alkyl. In some embodiments, R 14’ is hydrogen, methyl, or R 13 is R 14’ Together with it, it forms pyridinyl. In some embodiments, R 14’ is hydrogen or methyl. In some embodiments, R 14’ R is selected from hydrogen, methyl, and fluoro. In some embodiments, R14’ R is selected from hydrogen. In some embodiments, 14’ R is selected from hydrogen and methyl. In some embodiments, R 14’ R is selected from hydrogen and fluoro. In some embodiments, 14’ R is selected from methyl and fluoro. In some embodiments, 14’ R is selected from hydrogen and cyano. In some embodiments, 14’ The cyanoacrylate is selected from cyanoacrylate. In some embodiments, [ka] teeth: [ka] Selected from. In some embodiments, [ka] teeth: [ka] Selected from. In some embodiments, [ka] teeth: [ka] Selected from. In some embodiments, [ka] teeth: [ka] Selected from. In some embodiments, [ka] teeth: [ka] Selected from. In some embodiments, [ka] teeth: [ka] Selected from.
[0160] In certain embodiments, with respect to a compound or salt of formula (II), formula (II-A), or formula (II'), R 15 R can be any suitable functional group known to those skilled in the art. In some embodiments, R 15 ha: hydrogen, halogen, -OR 19e , -SR 19e , -N(R 19e )2, -NO2, and -CN; as well as one or more R 18d C replaced as needed 1~6 Selected from alkyl groups; or R 15 is R 17a Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed; or R 15 is R 17b Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed. In some embodiments, R 15 ha: hydrogen, -OR 19e , -SR 19e , -N(R 19e )2, and one or more R 18d C replaced as needed 1~6 Selected from alkyl groups; or R 15 is R 17a Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18fIt is replaced as needed; or R 15 is R 17b Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed. In some embodiments, R 15 is: Hydrogen and C 1~6 Selected from alkyl groups; or R 15 is R 17a Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed; or R 15 is R 17b Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed. In some embodiments, R 15 is hydrogen, C 1~6 Is it alkyl; or R 15 is R 17a Together with these, they form a 3- to 10-membered complex ring, where this 3- to 10-membered complex ring has one or more -OR 19h or C 1~3 Substituted with alkyl as needed; or R 15 is R 17b Together with these, they form a 3- to 10-membered complex ring, where this 3- to 10-membered complex ring has one or more -OR 19h or C 1~3 It is substituted with alkyl as needed. In some embodiments, R 15 Is it hydrogen; or R 15 is R 17a The compound that is combined with is tetrahydroisoquinoline, which is optionally substituted with -OH or methyl. In some embodiments, R 15 is R 17b The compound that is combined with is tetrahydroisoquinoline, which is optionally substituted with -OH or methyl. In some embodiments, R 15 It is hydrogen.
[0161] In certain embodiments, with respect to a compound or salt of formula (II), formula (II-A), or formula (II'), R 16 R can be any suitable functional group known to those skilled in the art. In some embodiments, R 16 ha: hydrogen, halogen, -OR 19f , -SR 19f -N(R 19f )2, -NO2, and -CN; as well as one or more R 18e C replaced as needed 1~6 Selected from alkyl groups; or R 16 is R 17a Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed; or R 16 is R 17b Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed. In some embodiments, R 16 ha: hydrogen, halogen, -OR 19f , -SR 19f -N(R 19f )2; and one or more R 18e C replaced as needed 1~6 Selected from alkyl groups; or R 16 is R 17a Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed; or R 16 is R 17b Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed. In some embodiments, R 16 is hydrogen, -OR 19h C replaced as needed 1~3 It is alkyl; or R 16 is R17a Together with these, they form a 3- to 10-membered heterocycle, where this 3- to 10-membered heterocycle consists of halogens, -OR 19h , -SR 19h , -N(R 19h )2, and -CN are optionally substituted with one or more substituents selected independently of R 16 is R 17b Together with these, they form a 3- to 10-membered heterocycle, where this 3- to 10-membered heterocycle consists of halogens, -OR 19h , -SR 19h , -N(R 19h )2, and -CN are optionally substituted with one or more substituents selected independently of CN. In some embodiments, R 16 is a C1 alkyl group substituted with hydrogen, -OH as needed, or R 16 is R 17a Together with these, they form dihydrobenzofuranyl or dihydrophlopyridinyl which is optionally substituted with one or more -F or -CN. In some embodiments, R 16 is a C1 alkyl group substituted with hydrogen, -OH as needed, or R 16 is R 17b Together with these, they form dihydrobenzofuranyl or dihydrophlopyridinyl which is optionally substituted with one or more -F or -CN. In some embodiments, R 16 is hydrogen or methyl. In some embodiments, R 16 is methyl. In some embodiments, R 16 is R 17a Together with: [ka] This forms a -F or -CN which may be replaced as needed with one or more -F or -CN in some embodiments, R 16 is R 17a Together with: [ka] This forms a CN which is replaced as needed with one or more CNs. In some embodiments, R 16 is R 17a Together with: [ka] This forms a , which is replaced as needed with one or more -F. In some embodiments, R 16 is R 17b Together with: [ka] This forms a -F or -CN which may be replaced as needed with one or more -F or -CN in some embodiments, R 16 is R 17b Together with: [ka] This forms a CN which is replaced as needed with one or more CNs. In some embodiments, R 16 is R 17b Together with: [ka] This forms a , which is replaced as needed with one or more -F. In some embodiments, R 16 is a C1 alkyl group optionally substituted with hydrogen, -OH. In some embodiments, R 16 is hydrogen, methyl, or CH2OH. In some embodiments, R 16 is methyl or CH2OH. In some embodiments, R 16 It is methyl.
[0162] In certain embodiments, with respect to a compound or salt of formula (II), formula (II-A), or formula (II'), R 16 and R 17aTogether with that, [ka] They form 3-membered to 10-membered complex rings selected from these.
[0163] In certain embodiments, with respect to a compound or salt of formula (II), formula (II-A), or formula (II'), [ka] teeth, [ka] Selected from.
[0164] In some embodiments, R 16 and R 17a Together with that, [ka] They form 3-membered to 10-membered complex rings selected from these.
[0165] In some embodiments, R 16 and R 17b Together with that, [ka] They form 3-membered to 10-membered complex rings selected from these.
[0166] In some embodiments, R 16 and R 17b Together with that, [ka] They form 3-membered to 10-membered complex rings selected from these.
[0167] In certain embodiments, with respect to a compound or salt of formula (II), formula (II-A), or formula (II'), each R 17a , R 17b , R17c , R 17d , and R 17e R can be any suitable functional group known to those skilled in the art. In some embodiments, each R 17a , R 17b , R 17c , R 17d , and R 17e These are independently: hydrogen, halogen, -OR 19g , -SR 19g , -N(R 19g )2, -NO2, and -CN; as well as one or more R 18f C replaced as needed 1~6 Selected from alkyl groups. Or R 15 is R 17a Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed; or R 16 is R 17a Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed; or R 15 is R 17b Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed; or R 16 is R 17b Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed. In some embodiments, each R 17a , R 17b , R 17c , R 17d , and R 17e These are independently: hydrogen, halogen, -OR 19g , -N(R 19g )2, and -CN; as well as one or more R 18f C replaced as needed 1~6 Selected from alkyl groups; or R 15is R 17a Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed; or R 16 is R 17a Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed; or R 15 is R 17b Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed; or R 16 is R 17b Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed.
[0168] In certain embodiments, with respect to a compound or salt of formula (II), formula (II-A), or formula (II'), each R 17a , R 17b , R 17c , R 17d , and R 17e These are independently: hydrogen, halogen, -OR 19g , and -CN; as well as one or more R 18f C replaced as needed 1~6 Selected from alkyl groups; or R 15 is R 17a Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed; or R 15 is R 17b Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed; or R 16 is R 17aTogether with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed; or R 16 is R 17b Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed. In some embodiments, each R 17a , R 17b , R 17c , R 17d , and R 17e These are independently halogen, -CN, or R 15 is R 17a Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed; or R 16 is R 17a Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed; or R 15 is R 17b Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed; or R 16 is R 17b Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed. In some embodiments, each R 17a , R 17b , R 17c , R 17d , and R 17e These are independently -F, -CN; or R 15 is R 17a The combination is tetrahydroisoquinoline substituted with -OH or methyl as needed; or R 16 is R 17aTogether with R, they form dihydrobenzofuranyl or dihydrophlopyridinyl which is optionally substituted with one or more -F or -CN; or R 15 is R 17b The combination is tetrahydroisoquinoline substituted with -OH or methyl as needed; or R 16 is R 17b Together with these, they form dihydrobenzofuranyl or dihydrophlopyridinyl which is optionally substituted with one or more -F or -CN. In some embodiments, each R 17a , R 17b , R 17c , R 17d , and R 17e These are independently either -F or -CN.
[0169] In certain embodiments, with respect to a compound or salt of formula (II), formula (II-A), or formula (II'), R 17a is R 16 Together with: [ka] A is formed, which is optionally substituted with one or more substituents independently selected from -F and -CN. In some embodiments, R 17b is R 16 Together with: [ka] This forms a molecule which is optionally substituted with one or more substituents independently selected from -F and -CN.
[0170] In certain embodiments, with respect to a compound or salt of formula (II), formula (II-A), or formula (II'), each R 17a Independently: Hydrogen, halogen, -OR 19g , -SR 19g , -N(R 19g )2, -NO2, -CN, and -N3; and C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl, each of which has one or more R 18f It is selected from those that have been replaced as needed; or R 15 is R 17a Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed; or R 16 is R 17a Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed.
[0171] In some embodiments, each R 17a Independently: Hydrogen, halogens, and -CN; as well C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkynnyls, each of which is optionally substituted with one or more substituents independently selected from -F and -CN; or R 15 is R 17a Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed; or R 16 is R 17a Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed.
[0172] In some embodiments, each R 17a Independently: Hydrogen, -F, and -CN; and C1 alkyl and C2 alkynyl, each of which is optionally substituted with one or more substituents independently selected from -F and -CN; or R 15 is R 17a Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed; or R 16 is R 17a Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed.
[0173] In some embodiments, each R 17a These are independently selected from: hydrogen, -F, -CN, -CH3, and -CCH; or R 15 is R 17a Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed; or R 16 is R 17a Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed.
[0174] In some embodiments, each R 17a These are independently selected from: hydrogen, -F, -CN, -CH3, and -CCH; or R 15 is R 17a Together with these, they form a 3- to 10-membered heterocycle, where this 3- to 10-membered heterocycle is optionally substituted with one or more substituents independently selected from -F and -CN; or R 16 is R 17aTogether with these, they form a 3- to 10-membered heterocycle, which is optionally substituted with one or more substituents independently selected from -F and -CN.
[0175] In some embodiments, each R 17a These are independently selected from: hydrogen, -F, -CN, -CH3, and -CCH; or R 15 is R 17a Together with -F, they form a 3- to 10-membered heterocycle, where this 3- to 10-membered heterocycle is optionally substituted with one or more substituents independently selected from -F; or R 16 is R 17a Together with -F, they form a 3- to 10-membered heterocycle, which is optionally substituted with one or more substituents independently selected from -F.
[0176] In some embodiments, each R 17a These are independently selected from: hydrogen, -F, -CN, -CH3, and -CCH; or R 15 is R 17a Together with -CN, they form a 3- to 10-membered heterocycle, where this 3- to 10-membered heterocycle is optionally substituted with one or more substituents independently selected from -CN; or R 16 is R 17a Together with the CNs, they form a 3- to 10-membered heterocycle, which is optionally substituted with one or more substituents independently selected from the CNs.
[0177] In some embodiments, each R 17a The elements are independently selected from: hydrogen, -F, -CN, -CH3, and -CCH; or R 16 is R 17a Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R18f It is replaced as needed. In some embodiments, each R 17a The elements are independently selected from: hydrogen, -F, -CN, -CH3, and -CCH; or R 16 is R 17a Together with these, they form a 3- to 10-membered heterocycle, where this 3- to 10-membered heterocycle consists of halogen, -CN, -OH, -OCH3, -SH, -NH2, -NO2, -N3, and C. 1~6 Alkyl, and C 2~6 It is optionally substituted with one or more substituents independently selected from the alkynyl. In some embodiments, each R 17a The elements are independently selected from: hydrogen, -F, -CN, -CH3, and -CCH; or R 16 is R 17a Together with these, they form a 3- to 10-membered heterocycle, where this 3- to 10-membered heterocycle consists of halogen, -CN, and C. 1~6 Alkyl, and C 2~6 It is optionally substituted with one or more substituents independently selected from the alkynyl. In some embodiments, each R 17a The elements are independently selected from: hydrogen, -F, -CN, -CH3, and -CCH; or R 16 is R 17a Together with these, they form a 3- to 10-membered heterocycle, where this 3- to 10-membered heterocycle is optionally substituted with one or more substituents independently selected from halogens, -CN, C1 alkyl, and C2 alkynyl. In some embodiments, each R 17a The elements are independently selected from: hydrogen, -F, -CN, -CH3, and -CCH; or R 16 is R 17a Together with these, they form a 3- to 10-membered heterocycle, where this 3- to 10-membered heterocycle is optionally substituted with one or more substituents independently selected from -F, -CN, -CH3, and -CCH. In some embodiments, each R 17a The elements are independently selected from: hydrogen, -F, -CN, -CH3, and -CCH; or R 16 is R17a Together with these, they form a 3- to 10-membered heterocycle, where this 3- to 10-membered heterocycle is optionally substituted with one or more substituents independently selected from -F and -CN. In some embodiments, each R 17a The elements are independently selected from: hydrogen, -F, -CN, -CH3, and -CCH; or R 16 is R 17a Together with -F, they form a 3- to 10-membered heterocycle, where this 3- to 10-membered heterocycle is optionally substituted with one or more substituents independently selected from -F. In some embodiments, each R 17a The elements are independently selected from: hydrogen, -F, -CN, -CH3, and -CCH; or R 16 is R 17a Together with the CNs, they form a 3- to 10-membered heterocycle, which is optionally substituted with one or more substituents independently selected from the CNs.
[0178] In certain embodiments, with respect to a compound or salt of formula (II), formula (II-A), or formula (II'), R 16 is R 17a Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed. In some embodiments, R 16 is R 17a Together with these, they form a 3- to 10-membered heterocycle, where this 3- to 10-membered heterocycle consists of halogen, -CN, -OH, -OCH3, -SH, -NH2, -NO2, -N3, and C. 1~6 Alkyl, and C 2~6 It is optionally substituted with one or more substituents independently selected from the alkynyl. In some embodiments, R 16 is R 17a Together with these, they form a 3- to 10-membered heterocycle, where this 3- to 10-membered heterocycle consists of halogen, -CN, and C. 1~6 Alkyl, and C 2~6It is optionally substituted with one or more substituents independently selected from the alkynyl. In some embodiments, R 16 is R 17a Together with these, they form a 3- to 10-membered heterocycle, where this 3- to 10-membered heterocycle is optionally substituted with one or more substituents independently selected from halogens, -CN, C1 alkyl, and C2 alkynyl. In some embodiments, R 16 is R 17a Together with these, they form a 3- to 10-membered heterocycle, where this 3- to 10-membered heterocycle is optionally substituted with one or more substituents independently selected from -F, -CN, -CH3, and -CCH. In some embodiments, R 16 is R 17a Together with these, they form a 3- to 10-membered heterocycle, where this 3- to 10-membered heterocycle is optionally substituted with one or more substituents independently selected from -F and -CN. In some embodiments, R 16 is R 17a Together with -F, they form a 3- to 10-membered heterocycle, which is optionally substituted with one or more substituents independently selected from -F. In some embodiments, R 16 is R 17a Together with the CNs, they form a 3- to 10-membered heterocycle, which is optionally substituted with one or more substituents independently selected from the CNs.
[0179] In some embodiments, each R 17a Independently: Hydrogen, halogen, -OR 19g , -SR 19g , -N(R 19g )2, -NO2, -CN, and -N3; and C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl, each of which has one or more R 18fThose that are replaced as needed Selected from.
[0180] In some embodiments, each R 17a Independently: Hydrogen, halogen, -OR 19g , -SR 19g , -N(R 19g )2, -NO2, -CN, and -N3; and C 1~6 Alkyl and C 2~6 Alkinyl, each of which has one or more R 18f Those that are replaced as needed Selected from.
[0181] In some embodiments, each R 17a Independently: Hydrogen, halogen, -OR 19g , -SR 19g , -N(R 19g )2, -NO2, -CN, and -N3; and C 1~6 Alkyl and C 2~6 Alkynnyls, each of which is optionally substituted with one or more substituents independently selected from halogens or CN. Selected from.
[0182] In some embodiments, each R 17a Independently: Hydrogen, halogen, -OR 19g , -N(R 19g )2, -CN, and -N3; and C 1~6 Alkyl and C 2~6 Alkynnyls, each of which is optionally substituted with one or more substituents independently selected from halogens or CN. Selected from.
[0183] In some embodiments, each R 17a Independently: Hydrogen, halogen, -OR 19g , -CN, and -N3; and C 1~6 Alkyl and C 2~6 Alkynnyls, each of which is optionally substituted with one or more substituents independently selected from halogens or CN. Selected from.
[0184] In some embodiments, each R 17a Independently: Hydrogen, halogens, and -CN; as well C 1~6 Alkyl and C 2~6 Alkynnyls, each of which is optionally substituted with one or more substituents independently selected from halogens or CN. Selected from.
[0185] In some embodiments, each R 17a Independently: Hydrogen, halogens, and -CN; as well C 1~3 Alkyl and C 2~3 Alkynnyls, each of which is optionally substituted with one or more substituents independently selected from halogens or CN. Selected from.
[0186] In some embodiments, each R 17a Independently: Hydrogen, halogens, and -CN; as well C1 alkyl and C 2~3 Alkynnyls, each of which is optionally substituted with one or more substituents independently selected from halogens or CN. Selected from.
[0187] In some embodiments, each R 17a Independently: Hydrogen, halogens, and -CN; as well C 1~6 Alkyl and C 2~6 Alkinyl Selected from.
[0188] In some embodiments, each R 17a Independently: Hydrogen, halogens, and -CN; as well C 1~3 Alkyl and C 2~6 Alkinyl Selected from.
[0189] In some embodiments, each R 17a Independently: Hydrogen, halogens, and -CN; as well C1 alkyl and C 2~3 Alkinyl Selected from.
[0190] In some embodiments, each R 17a Independently: Hydrogen, halogens, and -CN; as well C1 alkyl and C2 alkynyl Selected from.
[0191] In some embodiments, each R 17a Independently: Hydrogen, -F, and -CN; and C1 alkyl and C2 alkynyl Selected from.
[0192] In some embodiments, each R 17a The following are independently selected from: hydrogen, -CN, -F, -CH3, and -CCH.
[0193] In some embodiments, each R 17a R is independently selected from hydrogen, -CN, -F, and -CH3. In some embodiments, each R 17aR is independently selected from hydrogen, -CN, -F, and -CCH. In some embodiments, each R 17a R is independently selected from hydrogen, -CN, -CCH, and -CH3. In some embodiments, each R 17a R is independently selected from hydrogen, -CCH, -F, and -CH3. In some embodiments, each R 17a The following are independently selected from: hydrogen, -CCH, -F, and -CH3.
[0194] In some embodiments, each R 17a R is independently selected from hydrogen, -CN, and -F. In some embodiments, each R 17a R is independently selected from hydrogen, -CH3, and -F. In some embodiments, each R 17a R is independently selected from hydrogen, -CH3, and -CN. In some embodiments, each R 17a R is independently selected from hydrogen, -CCH, and -F. In some embodiments, each R 17a The elements are independently selected from hydrogen, -CCH, and -CN.
[0195] In some embodiments, each R 17a R is independently selected from hydrogen and -CN. In some embodiments, each R 17a R is independently selected from hydrogen and -F. In some embodiments, each R 17a R is independently selected from hydrogen and -CH3. In some embodiments, each R 17a These are independently selected from hydrogen and -CCH.
[0196] In some embodiments, each R 17a R is independently selected from hydrogen. In some embodiments, each R 17a R is independently selected from -F. In some embodiments, each R 17a R is independently selected from :-CN. In some embodiments, each R 17aR is independently selected from -CH3. In some embodiments, each R 17a It is independently selected from :-CCH.
[0197] In certain embodiments, with respect to a compound or salt of formula (II), formula (II-A), or formula (II'), each R 17b Independently: Hydrogen, halogen, -OR 19g , -SR 19g , -N(R 19g )2, -NO2, -CN, and -N3; and C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl, each of which has one or more R 18f Those that are replaced as needed Selected from; or R 15 is R 17b Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed; or R 16 is R 17b Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed.
[0198] In some embodiments, each R 17b Independently: Hydrogen, halogen, -OR 19g , -SR 19g , -N(R 19g )2, -NO2, -CN, and -N3; and C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl, each of which has one or more R 18f Those that are replaced as needed Selected from; or R 15 is R 17b Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed; or R 16 is R 17b Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed.
[0199] In some embodiments, each R 17b Independently: Hydrogen, halogens, and -CN; as well C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkynnyls, each of which is optionally substituted with one or more substituents independently selected from -F and -CN. Selected from; or R 15 is R 17b Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed; or R 16 is R 17b Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed.
[0200] In some embodiments, each R 17b Independently: Hydrogen, -F, and -CN; and C1 alkyl and C2 alkynyl compounds, each of which is optionally substituted with one or more substituents independently selected from -F and -CN. Selected from; or R15 is R 17b Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed; or R 16 is R 17b Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed.
[0201] In some embodiments, each R 17b These are independently selected from: hydrogen, -F, -CN, -CH3, and -CCH; or R 15 is R 17b Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed; or R 16 is R 17b Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed.
[0202] In some embodiments, each R 17b These are independently selected from: hydrogen, -F, -CN, -CH3, and -CCH; or R 15 is R 17b Together with these, they form a 3- to 10-membered heterocycle, where this 3- to 10-membered heterocycle is optionally substituted with one or more substituents independently selected from -F and -CN; or R 16 is R 17b Together with these, they form a 3- to 10-membered heterocycle, which is optionally substituted with one or more substituents independently selected from -F and -CN.
[0203] In some embodiments, each R 17b These are independently selected from: hydrogen, -F, -CN, -CH3, and -CCH; or R 15 is R 17b Together with -F, they form a 3- to 10-membered heterocycle, where this 3- to 10-membered heterocycle is optionally substituted with one or more substituents independently selected from -F; or R 16 is R 17b Together with -F, they form a 3- to 10-membered heterocycle, which is optionally substituted with one or more substituents independently selected from -F.
[0204] In some embodiments, each R 17b These are independently selected from: hydrogen, -F, -CN, -CH3, and -CCH; or R 15 is R 17b Together with -CN, they form a 3- to 10-membered heterocycle, where this 3- to 10-membered heterocycle is optionally substituted with one or more substituents independently selected from -CN; or R 16 is R 17b Together with the CNs, they form a 3- to 10-membered heterocycle, which is optionally substituted with one or more substituents independently selected from the CNs.
[0205] In some embodiments, each R 17b The elements are independently selected from: hydrogen, -F, -CN, -CH3, and -CCH; or R 16 is R 17b Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed. In some embodiments, each R 17b The elements are independently selected from: hydrogen, -F, -CN, -CH3, and -CCH; or R 16 is R 17bTogether with these, they form a 3- to 10-membered heterocycle, where this 3- to 10-membered heterocycle consists of halogen, -CN, -OH, -OCH3, -SH, -NH2, -NO2, -N3, and C. 1~6 Alkyl, and C 2~6 It is optionally substituted with one or more substituents independently selected from the alkynyl. In some embodiments, each R 17b The elements are independently selected from: hydrogen, -F, -CN, -CH3, and -CCH; or R 16 is R 17b Together with these, they form a 3- to 10-membered heterocycle, where this 3- to 10-membered heterocycle consists of halogen, -CN, and C. 1~6 Alkyl, and C 2~6 It is optionally substituted with one or more substituents independently selected from the alkynyl. In some embodiments, each R 17b The elements are independently selected from: hydrogen, -F, -CN, -CH3, and -CCH; or R 16 is R 17b Together with these, they form a 3- to 10-membered heterocycle, where this 3- to 10-membered heterocycle is optionally substituted with one or more substituents independently selected from halogens, -CN, C1 alkyl, and C2 alkynyl. In some embodiments, each R 17b The elements are independently selected from: hydrogen, -F, -CN, -CH3, and -CCH; or R 16 is R 17b Together with these, they form a 3- to 10-membered heterocycle, where this 3- to 10-membered heterocycle is optionally substituted with one or more substituents independently selected from -F, -CN, -CH3, and -CCH. In some embodiments, each R 17b The elements are independently selected from: hydrogen, -F, -CN, -CH3, and -CCH; or R 16 is R 17b Together with these, they form a 3- to 10-membered heterocycle, where this 3- to 10-membered heterocycle is optionally substituted with one or more substituents independently selected from -F and -CN. In some embodiments, each R 17bThe elements are independently selected from: hydrogen, -F, -CN, -CH3, and -CCH; or R 16 is R 17b Together with -F, they form a 3- to 10-membered heterocycle, where this 3- to 10-membered heterocycle is optionally substituted with one or more substituents independently selected from -F. In some embodiments, each R 17b The elements are independently selected from: hydrogen, -F, -CN, -CH3, and -CCH; or R 16 is R 17b Together with the CNs, they form a 3- to 10-membered heterocycle, which is optionally substituted with one or more substituents independently selected from the CNs.
[0206] In certain embodiments, with respect to a compound or salt of formula (II), formula (II-A), or formula (II'), R 16 is R 17b Together with these, they form a 3- to 10-membered heteroring, where this 3- to 10-membered heteroring is one or more R 18f It is replaced as needed. In some embodiments, R 16 is R 17b Together with these, they form a 3- to 10-membered heterocycle, where this 3- to 10-membered heterocycle consists of halogen, -CN, -OH, -OCH3, -SH, -NH2, -NO2, -N3, and C. 1~6 Alkyl, and C 2~6 It is optionally substituted with one or more substituents independently selected from the alkynyl. In some embodiments, R 16 is R 17b Together with these, they form a 3- to 10-membered heterocycle, where this 3- to 10-membered heterocycle consists of halogen, -CN, and C. 1~6 Alkyl, and C 2~6 It is optionally substituted with one or more substituents independently selected from the alkynyl. In some embodiments, R 16 is R 17bTogether with these, they form a 3- to 10-membered heterocycle, where this 3- to 10-membered heterocycle is optionally substituted with one or more substituents independently selected from halogens, -CN, C1 alkyl, and C2 alkynyl. In some embodiments, R 16 is R 17b Together with these, they form a 3- to 10-membered heterocycle, where this 3- to 10-membered heterocycle is optionally substituted with one or more substituents independently selected from -F, -CN, -CH3, and -CCH. In some embodiments, R 16 is R 17b Together with these, they form a 3- to 10-membered heterocycle, where this 3- to 10-membered heterocycle is optionally substituted with one or more substituents independently selected from -F and -CN. In some embodiments, R 16 is R 17b Together with -F, they form a 3- to 10-membered heterocycle, which is optionally substituted with one or more substituents independently selected from -F. In some embodiments, R 16 is R 17b Together with the CNs, they form a 3- to 10-membered heterocycle, which is optionally substituted with one or more substituents independently selected from the CNs.
[0207] In some embodiments, each R 17b Independently: Hydrogen, halogen, -OR 19g , -SR 19g , -N(R 19g )2, -NO2, -CN, and -N3; and C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl, each of which has one or more R 18f Those that are replaced as needed Selected from.
[0208] In some embodiments, each R17b Independently: Hydrogen, halogen, -OR 19g , -SR 19g , -N(R 19g )2, -NO2, -CN, and -N3; and C 1~6 Alkyl and C 2~6 Alkinyl, each of which has one or more R 18f Those that are replaced as needed Selected from.
[0209] In some embodiments, each R 17b Independently: Hydrogen, halogen, -OR 19g , -SR 19g , -N(R 19g )2, -NO2, -CN, -N3; and C 1~6 Alkyl and C 2~6 Alkynnyls, each of which is optionally substituted with one or more substituents independently selected from halogens or CN. Selected from.
[0210] In some embodiments, each R 17b Independently: Hydrogen, halogen, -OR 19g , -N(R 19g )2, -CN, and -N3; and C 1~6 Alkyl and C 2~6 Alkynnyls, each of which is optionally substituted with one or more substituents independently selected from halogens or CN. Selected from.
[0211] In some embodiments, each R 17b Independently: Hydrogen, halogen, -OR 19g , -CN, and -N3; and C 1~6 Alkyl and C2~6 Alkynnyls, each of which is optionally substituted with one or more substituents independently selected from halogens or CN. Selected from.
[0212] In some embodiments, each R 17b Independently: Hydrogen, halogens, and -CN; as well C 1~6 Alkyl and C 2~6 Alkynnyls, each of which is optionally substituted with one or more substituents independently selected from halogens or CN. Selected from.
[0213] In some embodiments, each R 17b Independently: Hydrogen, halogens, and -CN; as well C 1~3 Alkyl and C 2~3 Alkynnyls, each of which is optionally substituted with one or more substituents independently selected from halogens or CN. Selected from.
[0214] In some embodiments, each R 17b Independently: Hydrogen, halogens, and -CN; as well C1 alkyl and C 2~3 Alkynnyls, each of which is optionally substituted with one or more substituents independently selected from halogens or CN. Selected from.
[0215] In some embodiments, each R 17b Independently: Hydrogen, halogens, and -CN; as well C 1~6 Alkyl and C 2~6 Alkinyl Selected from.
[0216] In some embodiments, each R 17b Independently: Hydrogen, halogens, and -CN; as well C 1~3 Alkyl and C 2~6 Alkinyl Selected from.
[0217] In some embodiments, each R 17b Independently: Hydrogen, halogens, and -CN; as well C1 alkyl and C 2~3 Alkinyl Selected from.
[0218] In some embodiments, each R 17b Independently: Hydrogen, halogens, and -CN; as well C1 alkyl and C2 alkynyl Selected from.
[0219] In some embodiments, each R 17b Independently: Hydrogen, -F, and -CN; and C1 alkyl and C2 alkynyl Selected from.
[0220] In some embodiments, each R 17b The following are independently selected from: hydrogen, -CN, -F, -CH3, and -CCH.
[0221] In some embodiments, each R 17b R is independently selected from hydrogen, -CN, -F, and -CH3. In some embodiments, each R 17b R is independently selected from hydrogen, -CN, -F, and -CCH. In some embodiments, each R 17b R is independently selected from hydrogen, -CN, -CCH, and -CH3. In some embodiments, each R17b R is independently selected from hydrogen, -CCH, -F, and -CH3. In some embodiments, each R 17b The following are independently selected from: hydrogen, -CCH, -F, and -CH3.
[0222] In some embodiments, each R 17b R is independently selected from hydrogen, -CN, and -F. In some embodiments, each R 17b R is independently selected from hydrogen, -CH3, and -F. In some embodiments, each R 17b R is independently selected from hydrogen, -CH3, and -CN. In some embodiments, each R 17b R is independently selected from hydrogen, -CCH, and -F. In some embodiments, each R 17b The elements are independently selected from hydrogen, -CCH, and -CN.
[0223] In some embodiments, each R 17b R is independently selected from hydrogen and -CN. In some embodiments, each R 17b R is independently selected from hydrogen and -F. In some embodiments, each R 17b R is independently selected from hydrogen and -CH3. In some embodiments, each R 17b These are independently selected from hydrogen and -CCH.
[0224] In some embodiments, each R 17b R is independently selected from hydrogen. In some embodiments, each R 17b R is independently selected from -F. In some embodiments, each R 17b R is independently selected from :-CN. In some embodiments, each R 17b R is independently selected from -CH3. In some embodiments, each R 17b It is independently selected from :-CCH.
[0225] In certain embodiments, with respect to a compound or salt of formula (II), formula (II-A), or formula (II'), each R 17c Independently: Hydrogen, halogen, -OR 19g , -SR 19g , -N(R 19g )2, -NO2, -CN, and -N3; and C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl, each of which has one or more R 18f Those that are replaced as needed Selected from.
[0226] In some embodiments, each R 17c Independently: Hydrogen, halogen, -OR 19g , -SR 19g , -N(R 19g )2, -NO2, -CN, and -N3; and C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl, each of which has one or more R 18f Those that are replaced as needed Selected from.
[0227] In some embodiments, each R 17c Independently: Hydrogen, halogen, -OR 19g , -SR 19g , -N(R 19g )2, -NO2, -CN, and -N3; and C 1~6 Alkyl and C 2~6 Alkinyl, each of which has one or more R 18f Those that are replaced as needed Selected from.
[0228] In some embodiments, each R 17cIndependently: Hydrogen, halogen, -OR 19g , -SR 19g , -N(R 19g )2, -NO2, -CN, and -N3; and C 1~6 Alkyl and C 2~6 Alkynnyls, each of which is optionally substituted with one or more substituents independently selected from halogens or CN. Selected from.
[0229] In some embodiments, each R 17c Independently: Hydrogen, halogen, -OR 19g , -N(R 19g )2, -CN, and -N3; and C 1~6 Alkyl and C 2~6 Alkynnyls, each of which is optionally substituted with one or more substituents independently selected from halogens or CN. Selected from.
[0230] In some embodiments, each R 17c Independently: Hydrogen, halogen, -OR 19g , -CN, and -N3; and C 1~6 Alkyl and C 2~6 Alkynnyls, each of which is optionally substituted with one or more substituents independently selected from halogens or CN. Selected from.
[0231] In some embodiments, each R 17c Independently: Hydrogen, halogens, and -CN; as well C 1~6 Alkyl and C 2~6Alkynnyls, each of which is optionally substituted with one or more substituents independently selected from halogens or CN. Selected from.
[0232] In some embodiments, each R 17c Independently: Hydrogen, halogens, and -CN; as well C 1~3 Alkyl and C 2~3 Alkynnyls, each of which is optionally substituted with one or more substituents independently selected from halogens or CN. Selected from.
[0233] In some embodiments, each R 17c Independently: Hydrogen, halogens, and -CN; as well C1 alkyl and C 2~3 Alkynnyls, each of which is optionally substituted with one or more substituents independently selected from halogens or CN. Selected from.
[0234] In some embodiments, each R 17c Independently: Hydrogen, halogens, and -CN; as well C 1~6 Alkyl and C 2~6 Alkinyl Selected from.
[0235] In some embodiments, each R 17c Independently: Hydrogen, halogens, and -CN; as well C 1~3 Alkyl and C 2~6 Alkinyl Selected from.
[0236] In some embodiments, each R 17c Independently: Hydrogen, halogens, and -CN; as well C1 alkyl and C 2~3 Alkinyl Selected from.
[0237] In some embodiments, each R 17c Independently: Hydrogen, halogens, and -CN; as well C1 alkyl and C2 alkynyl Selected from.
[0238] In some embodiments, each R 17c Independently: Hydrogen, -F, and -CN; and C1 alkyl and C2 alkynyl Selected from.
[0239] In some embodiments, each R 17c The following are independently selected from: hydrogen, -CN, -F, -CH3, and -CCH.
[0240] In some embodiments, each R 17c R is independently selected from hydrogen, -CN, -F, and -CH3. In some embodiments, each R 17c R is independently selected from hydrogen, -CN, -F, and -CCH. In some embodiments, each R 17c R is independently selected from hydrogen, -CN, -CCH, and -CH3. In some embodiments, each R 17c R is independently selected from hydrogen, -CCH, -F, and -CH3. In some embodiments, each R 17c The following are independently selected from: hydrogen, -CCH, -F, and -CH3.
[0241] In some embodiments, each R 17c R is independently selected from hydrogen, -CN, and -F. In some embodiments, each R 17cR is independently selected from hydrogen, -CH3, and -F. In some embodiments, each R 17c R is independently selected from hydrogen, -CH3, and -CN. In some embodiments, each R 17c R is independently selected from hydrogen, -CCH, and -F. In some embodiments, each R 17c The elements are independently selected from hydrogen, -CCH, and -CN.
[0242] In some embodiments, each R 17c R is independently selected from hydrogen and -CN. In some embodiments, each R 17c R is independently selected from hydrogen and -F. In some embodiments, each R 17c R is independently selected from hydrogen and -CH3. In some embodiments, each R 17c These are independently selected from hydrogen and -CCH.
[0243] In some embodiments, each R 17c R is independently selected from hydrogen. In some embodiments, each R 17c R is independently selected from -F. In some embodiments, each R 17c R is independently selected from :-CN. In some embodiments, each R 17c R is independently selected from -CH3. In some embodiments, each R 17c It is independently selected from :-CCH.
[0244] In certain embodiments, with respect to a compound or salt of formula (II), formula (II-A), or formula (II'), each R 17d Independently: Hydrogen, halogen, -OR 19g , -SR 19g , -N(R 19g )2, -NO2, -CN, and -N3; and C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6Alkinyl, each of which has one or more R 18f Those that are replaced as needed Selected from.
[0245] In some embodiments, each R 17d Independently: Hydrogen, halogen, -OR 19g , -SR 19g , -N(R 19g )2, -NO2, -CN, and -N3; and C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl, each of which has one or more R 18f Those that are replaced as needed Selected from.
[0246] In some embodiments, each R 17d Independently: Hydrogen, halogen, -OR 19g , -SR 19g , -N(R 19g )2, -NO2, -CN, and -N3; and C 1~6 Alkyl and C 2~6 Alkinyl, each of which has one or more R 18f Those that are replaced as needed Selected from.
[0247] In some embodiments, each R 17d Independently: Hydrogen, halogen, -OR 19g , -SR 19g , -N(R 19g )2, -NO2, -CN, and -N3; and C 1~6 Alkyl and C 2~6 Alkynnyls, each of which is optionally substituted with one or more substituents independently selected from halogens or CN. Selected from.
[0248] In some embodiments, each R 17d Independently: Hydrogen, halogen, -OR 19g , -N(R 19g )2, -CN, and -N3; and C 1~6 Alkyl and C 2~6 Alkynnyls, each of which is optionally substituted with one or more substituents independently selected from halogens or CN. Selected from.
[0249] In some embodiments, each R 17d Independently: Hydrogen, halogen, -OR 19g , -CN, and -N3; and C 1~6 Alkyl and C 2~6 Alkynnyls, each of which is optionally substituted with one or more substituents independently selected from halogens or CN. Selected from.
[0250] In some embodiments, each R 17d Independently: Hydrogen, halogens, and -CN; as well C 1~6 Alkyl and C 2~6 Alkynnyls, each of which is optionally substituted with one or more substituents independently selected from halogens or CN. Selected from.
[0251] In some embodiments, each R 17d Independently: Hydrogen, halogens, and -CN; as well C 1~3 Alkyl and C 2~3Alkynnyls, each of which is optionally substituted with one or more substituents independently selected from halogens or CN. Selected from.
[0252] In some embodiments, each R 17d Independently: Hydrogen, halogens, and -CN; as well C1 alkyl and C 2~3 Alkynnyls, each of which is optionally substituted with one or more substituents independently selected from halogens or CN. Selected from.
[0253] In some embodiments, each R 17d Independently: Hydrogen, halogens, and -CN; as well C 1~6 Alkyl and C 2~6 Alkinyl Selected from.
[0254] In some embodiments, each R 17d Independently: Hydrogen, halogens, and -CN; as well C 1~3 Alkyl and C 2~6 Alkinyl Selected from.
[0255] In some embodiments, each R 17d Independently: Hydrogen, halogens, and -CN; as well C1 alkyl and C 2~3 Alkinyl Selected from.
[0256] In some embodiments, each R 17d Independently: Hydrogen, halogens, and -CN; as well C1 alkyl and C2 alkynyl Selected from.
[0257] In some embodiments, each R 17d Independently: Hydrogen, -F, and -CN; and C1 alkyl and C2 alkynyl Selected from.
[0258] In some embodiments, each R 17d The following are independently selected from: hydrogen, -CN, -F, -CH3, and -CCH.
[0259] In some embodiments, each R 17d R is independently selected from hydrogen, -CN, -F, and -CH3. In some embodiments, each R 17d R is independently selected from hydrogen, -CN, -F, and -CCH. In some embodiments, each R 17d R is independently selected from hydrogen, -CN, -CCH, and -CH3. In some embodiments, each R 17d R is independently selected from hydrogen, -CCH, -F, and -CH3. In some embodiments, each R 17d The following are independently selected from: hydrogen, -CCH, -F, and -CH3.
[0260] In some embodiments, each R 17d R is independently selected from hydrogen, -CN, and -F. In some embodiments, each R 17d R is independently selected from hydrogen, -CH3, and -F. In some embodiments, each R 17d R is independently selected from hydrogen, -CH3, and -CN. In some embodiments, each R 17d R is independently selected from hydrogen, -CCH, and -F. In some embodiments, each R 17d The elements are independently selected from hydrogen, -CCH, and -CN.
[0261] In some embodiments, each R 17dR is independently selected from hydrogen and -CN. In some embodiments, each R 17d R is independently selected from hydrogen and -F. In some embodiments, each R 17d R is independently selected from hydrogen and -CH3. In some embodiments, each R 17d These are independently selected from hydrogen and -CCH.
[0262] In some embodiments, each R 17d R is independently selected from hydrogen. In some embodiments, each R 17d R is independently selected from -F. In some embodiments, each R 17d R is independently selected from :-CN. In some embodiments, each R 17d R is independently selected from -CH3. In some embodiments, each R 17d It is independently selected from :-CCH.
[0263] In certain embodiments, with respect to a compound or salt of formula (II), formula (II-A), or formula (II'), each R 17e Independently: Hydrogen, halogen, -OR 19g , -SR 19g , -N(R 19g )2, -NO2, -CN, and -N3; and C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl, each of which has one or more R 18f Those that are replaced as needed Selected from.
[0264] In some embodiments, each R 17e Independently: Hydrogen, halogen, -OR 19g , -SR 19g , -N(R 19g )2, -NO2, -CN, and -N3; and C 1~6 Alkyl, C2~6 Alkenyl and C 2~6 Alkinyl, each of which has one or more R 18f Those that are replaced as needed Selected from.
[0265] In some embodiments, each R 17e Independently: Hydrogen, halogen, -OR 19g , -SR 19g , -N(R 19g )2, -NO2, -CN, and -N3; and C 1~6 Alkyl and C 2~6 Alkinyl, each of which has one or more R 18f Those that are replaced as needed Selected from.
[0266] In some embodiments, each R 17e Independently: Hydrogen, halogen, -OR 19g , -SR 19g , -N(R 19g )2, -NO2, -CN, and -N3; and C 1~6 Alkyl and C 2~6 Alkynnyls, each of which is optionally substituted with one or more substituents independently selected from halogens or CN. Selected from.
[0267] In some embodiments, each R 17e Independently: Hydrogen, halogen, -OR 19g , -N(R 19g )2, -CN, and -N3; and C 1~6 Alkyl and C 2~6 Alkynnyls, each of which is optionally substituted with one or more substituents independently selected from halogens or CN. Selected from.
[0268] In some embodiments, each R 17e Independently: Hydrogen, halogen, -OR 19g , -CN, and -N3; and C 1~6 Alkyl and C 2~6 Alkynnyls, each of which is optionally substituted with one or more substituents independently selected from halogens or CN. Selected from.
[0269] In some embodiments, each R 17e Independently: Hydrogen, halogens, and -CN; as well C 1~6 Alkyl and C 2~6 Alkynnyls, each of which is optionally substituted with one or more substituents independently selected from halogens or CN. Selected from.
[0270] In some embodiments, each R 17e Independently: Hydrogen, halogens, and -CN; as well C 1~3 Alkyl and C 2~3 Alkynnyls, each of which is optionally substituted with one or more substituents independently selected from halogens or CN. Selected from.
[0271] In some embodiments, each R 17e Independently: Hydrogen, halogens, and -CN; as well C1 alkyl and C 2~3 Alkynnyls, each of which is optionally substituted with one or more substituents independently selected from halogens or CN. Selected from.
[0272] In some embodiments, each R 17e Independently: Hydrogen, halogens, and -CN; as well C 1~6 Alkyl and C 2~6 Alkinyl Selected from.
[0273] In some embodiments, each R 17e Independently: Hydrogen, halogens, and -CN; as well C 1~3 Alkyl and C 2~6 Alkinyl Selected from.
[0274] In some embodiments, each R 17e Independently: Hydrogen, halogens, and -CN; as well C1 alkyl and C 2~3 Alkinyl Selected from.
[0275] In some embodiments, each R 17e Independently: Hydrogen, halogens, and -CN; as well C1 alkyl and C2 alkynyl Selected from.
[0276] In some embodiments, each R 17e Independently: Hydrogen, -F, and -CN; and C1 alkyl and C2 alkynyl Selected from.
[0277] In some embodiments, each R 17e The following are independently selected from: hydrogen, -CN, -F, -CH3, and -CCH.
[0278] In some embodiments, each R17e R is independently selected from hydrogen, -CN, -F, and -CH3. In some embodiments, each R 17e R is independently selected from hydrogen, -CN, -F, and -CCH. In some embodiments, each R 17e R is independently selected from hydrogen, -CN, -CCH, and -CH3. In some embodiments, each R 17e R is independently selected from hydrogen, -CCH, -F, and -CH3. In some embodiments, each R 17e The following are independently selected from: hydrogen, -CCH, -F, and -CH3.
[0279] In some embodiments, each R 17e R is independently selected from hydrogen, -CN, and -F. In some embodiments, each R 17e R is independently selected from hydrogen, -CH3, and -F. In some embodiments, each R 17e R is independently selected from hydrogen, -CH3, and -CN. In some embodiments, each R 17e R is independently selected from hydrogen, -CCH, and -F. In some embodiments, each R 17e The elements are independently selected from hydrogen, -CCH, and -CN.
[0280] In some embodiments, each R 17e R is independently selected from hydrogen and -CN. In some embodiments, each R 17e R is independently selected from hydrogen and -F. In some embodiments, each R 17e R is independently selected from hydrogen and -CH3. In some embodiments, each R 17e These are independently selected from hydrogen and -CCH.
[0281] In some embodiments, each R 17e R is independently selected from hydrogen. In some embodiments, each R 17e R is independently selected from -F. In some embodiments, each R17e R is independently selected from :-CN. In some embodiments, each R 17e R is independently selected from -CH3. In some embodiments, each R 17e It is independently selected from :-CCH.
[0282] In certain embodiments, with respect to a compound or salt of formula (II), formula (II-A), or formula (II'), R 18a , R 18b , R 18c , R 18d , R 18e , and R 18f Each of these may be any suitable functional group known to those skilled in the art. In some embodiments, R 18a , R 18b , R 18c , R 18d , R 18e , and R 18f Each of these is independent: halogen, -OR 19h , -SR 19h , -N(R 19h )2, -C(O)R 19h ,-C(O)N(R 19h )2, -N(R 19h )C(O)R 19h , -N(R 19h )C(O)N(R 19h )2, -OC(O)N(R 19h )2, -N(R 19h )C(O)OR 19h , -C(O)OR 19h ,-OC(O)R 19h ,-S(O)R 19h -S(O)2R 19h -NO2, =O, =S, =N(R 19h ), and -CN; as well as C 1~3 Alkyl, C 2~3 Alkenyl and C 2~3 Alkynnyl, where each of these is a halogen, -OR 19h , -SR 19h , -N(R 19h )2, -C(O)R 19h ,-C(O)N(R 19h )2, -N(R19h )C(O)R 19h , -N(R 19h )C(O)N(R 19h )2, -OC(O)N(R 19h )2, -N(R 19h )C(O)OR 19h , -C(O)OR 19h ,-OC(O)R 19h ,-S(O)R 19h -S(O)2R 19h -NO2, =O, =S, =N(R 19h ), and are selected as needed to be substituted with one or more substituents independently selected from -CN. In some embodiments, each R 18a These are independently halogen, -OR 19h , -SR 19h , -N(R 19h )2, -C(O)R 19h , -CN, and C 1~3 Selected from alkyl groups. In some embodiments, each R 18a These are independently halogen, -OR 19h , -N(R 19h )2, -CN, and C 1~3 Selected from alkyl groups. In some embodiments, each R 18a These are independently halogen, -OR 19h Selected from , and -CN. In some embodiments, each R 18b These are independently halogen, -OR 19h , -SR 19h , -N(R 19h )2, -C(O)R 19h , -CN, and C 1~3 Selected from alkyl groups. In some embodiments, each R 18b These are independently halogen, -OR 19h , -N(R 19h )2, -CN, and C 1~3 Selected from alkyl groups. In some embodiments, each R 18b These are independently halogen, -OR 19h Selected from , and -CN. In some embodiments, each R 18cThese are independently halogen, -OR 19h , -SR 19h , -N(R 19h )2, -C(O)R 19h , -CN, and C 1~3 Selected from alkyl groups. In some embodiments, each R 18c These are independently halogen, -OR 19h , -N(R 19h )2, -CN, and C 1~3 Selected from alkyl groups. In some embodiments, each R 18c These are independently halogen, -OR 19h Selected from , and -CN. In some embodiments, each R 18d These are independently halogen, -OR 19h , -SR 19h , -N(R 19h )2, -C(O)R 19h , -CN, and C 1~3 Selected from alkyl groups. In some embodiments, each R 18d These are independently halogen, -OR 19h , -N(R 19h )2, -CN, and C 1~3 Selected from alkyl groups. In some embodiments, each R 18d These are independently halogen, -OR 19h Selected from , and -CN. In some embodiments, each R 18e These are independently halogen, -OR 19h , -SR 19h , -N(R 19h )2, -C(O)R 19h , -CN, and C 1~3 Selected from alkyl groups. In some embodiments, each R 18e These are independently halogen, -OR 19h , -N(R 19h )2, -CN, and C 1~3 Selected from alkyl groups. In some embodiments, each R 18e These are independently halogen, -OR 19h Selected from , and -CN. In some embodiments, each R 18e These are independent, -OR19h In some embodiments, each R 18e In some embodiments, each R is independently -OH. 18f These are independently halogen, -OR 19h , -SR 19h , -N(R 19h )2, -C(O)R 19h , -CN, and C 1~3 Selected from alkyl groups. In some embodiments, each R 18f These are independently halogen, -OR 19h , -N(R 19h )2, -CN, and C 1~3 Selected from alkyl groups. In some embodiments, each R 18f These are independently halogen, -OR 19h Selected from , and -CN. In some embodiments, each R 18f R is independently a halogen or -CN. In some embodiments, each R 18f These are independently fluoro or -CN.
[0283] In certain embodiments, with respect to a compound or salt of formula (II), formula (II-A), or formula (II'), R 19a , R 19b , R 19c , R 19d , R 19e , R 19f , R 19g , and R 19h Each of these may be any suitable functional group known to those skilled in the art. In some embodiments, R 19a , R 19b , R 19c , R 19d , R 19e , R 19f , R 19g , and R 19h Each of them independently consists of: hydrogen; and C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkynnyl, where each of these is a halogen, -CN, -OH, -SH, -NO2, -NH2, =O, =S, -OC 1~6Alkyl, -SC 1~6 Alkyl, -N(C 1~6 Alkyl)2,-NH(C 1~6 Alkyl), C 3~10 A carbon ring, or a 3-membered to 10-membered heterocycle, substituted as needed with one or more substituents independently selected from these; and C 3~10 Carbon rings and 3- to 10-membered heterocycles, each of which is a halogen, -CN, -OH, -SH, -NO2, -NH2, =O, =S, -OC 1~6 Alkyl, -SC 1~6 Alkyl, -N(C 1~6 Alkyl)2,-NH(C 1~6 Alkyl), C 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 3~10 Carbon rings, 3-membered to 10-membered heterocycles, and C 1~6 Selected from those independently of the haloalkyl, and optionally substituted with one or more substituents. In some embodiments, each R 19a Hydrogen and C are independent of each other. 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 3~10 Selected from carbocyclic rings and 3- to 10-membered heterocycles. In some embodiments, each R 19a Hydrogen and C are independent of each other. 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Selected from alkynyl. In some embodiments, each R 19a Hydrogen and C are independent of each other. 1~6 Selected from alkyl groups. In some embodiments, each R 19a R is independently selected from hydrogen and methyl. In some embodiments, each R 19a R is independently selected from hydrogen. In some embodiments, each R 19b Hydrogen and C are independent of each other. 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 3~10Selected from carbocyclic rings and 3- to 10-membered heterocycles. In some embodiments, each R 19b Hydrogen and C are independent of each other. 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Selected from alkynyl. In some embodiments, each R 19b Hydrogen and C are independent of each other. 1~6 Selected from alkyl groups. In some embodiments, each R 19b R is independently selected from hydrogen and methyl. In some embodiments, each R 19b R is independently selected from hydrogen. In some embodiments, each R 19c Hydrogen and C are independent of each other. 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 3~10 Selected from carbocyclic rings and 3- to 10-membered heterocycles. In some embodiments, each R 19c Hydrogen and C are independent of each other. 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Selected from alkynyl. In some embodiments, each R 19c Hydrogen and C are independent of each other. 1~6 Selected from alkyl groups. In some embodiments, each R 19c R is independently selected from hydrogen and methyl. In some embodiments, each R 19c R is independently selected from hydrogen. In some embodiments, each R 19d Hydrogen and C are independent of each other. 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 3~10 Selected from carbocyclic rings and 3- to 10-membered heterocycles. In some embodiments, each R 19d Hydrogen and C are independent of each other. 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Selected from alkynyl. In some embodiments, each R 19d Hydrogen and C are independent of each other. 1~6Selected from alkyl groups. In some embodiments, each R 19d R is independently selected from hydrogen and methyl. In some embodiments, each R 19d R is independently selected from hydrogen. In some embodiments, each R 19e Hydrogen and C are independent of each other. 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 3~10 Selected from carbocyclic rings and 3- to 10-membered heterocycles. In some embodiments, each R 19e Hydrogen and C are independent of each other. 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Selected from alkynyl. In some embodiments, each R 19e Hydrogen and C are independent of each other. 1~6 Selected from alkyl groups. In some embodiments, each R 19e R is independently selected from hydrogen and methyl. In some embodiments, each R 19e R is independently selected from hydrogen. In some embodiments, each R 19f Hydrogen and C are independent of each other. 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 3~10 Selected from carbocyclic rings and 3- to 10-membered heterocycles. In some embodiments, each R 19f Hydrogen and C are independent of each other. 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Selected from alkynyl. In some embodiments, each R 19f Hydrogen and C are independent of each other. 1~6 Selected from alkyl groups. In some embodiments, each R 19f R is independently selected from hydrogen and methyl. In some embodiments, each R 19f R is independently selected from hydrogen. In some embodiments, each R 19g Hydrogen and C are independent of each other. 1~6 Alkyl, C 2~6 Alkenil, C2~6 Alkinyl, C 3~10 Selected from carbocyclic rings and 3- to 10-membered heterocycles. In some embodiments, each R 19g Hydrogen and C are independent of each other. 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Selected from alkynyl. In some embodiments, each R 19g Hydrogen and C are independent of each other. 1~6 Selected from alkyl groups. In some embodiments, each R 19g R is independently selected from hydrogen and methyl. In some embodiments, each R 19g R is independently selected from hydrogen. In some embodiments, each R 19h Hydrogen and C are independent of each other. 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 3~10 Selected from carbocyclic rings and 3- to 10-membered heterocycles. In some embodiments, each R 19h Hydrogen and C are independent of each other. 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Selected from alkynyl. In some embodiments, each R 19h Hydrogen and C are independent of each other. 1~6 Selected from alkyl groups. In some embodiments, each R 19h R is independently selected from hydrogen. In some embodiments, each R 19h R is independently selected from hydrogen and methyl. In some embodiments, each R 19h It is independently selected from hydrogen.
[0284] In certain embodiments, with respect to a compound or salt of formula (II), formula (II-A), or formula (II'), Y 12 This is selected from C(CN), C(H), and C(F). In some embodiments, Y 12 is selected from C(CN). In some embodiments, Y 11X is selected from C(H). In some embodiments, X 13 is selected from N and C(H). In some embodiments, X 1 and X 2 In some embodiments, X 11 is selected from N, C(H), and C(F). In some embodiments, X 12 This is selected from N, C(H), and C(F).
[0285] In certain embodiments, with respect to a compound or salt of formula (II), formula (II-A), or formula (II'), X 11 is N, and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN). In some embodiments, X 11 is N, and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), and R 16 is a C1 alkyl group which is substituted as needed. In some embodiments, X 11 is N, and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), and R 16 is -CH3. In some embodiments, X 11 is N, and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), and R 15 H is H. In some embodiments, X 11 is N, and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12C(CN) and R 14 H is H, and R 14 ' is H. In some embodiments, X 11 is N, and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), and R 12 H is H. In some embodiments, X 11 is N, and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), and R 13 X is selected from CH3, H, and cyclopropyl. In some embodiments, X 11 is N, and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), and R 13 is selected from CH3. In some embodiments, X 11 is N, and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), and R 13 X is selected from cyclopropyl. In some embodiments, X 11 is N, and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), and R 13 is selected from H. In some embodiments, X 11 is N, and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), and R 11The is selected from CH3, cyclopropyl, F, Cl, Br, CF3, CN, N3, OH, and OMe. In some embodiments, X 11 is N, and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), and R 11 X is selected from CH3, F, Cl, Br, CF3, and CN. In some embodiments, X 11 is N, and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), and R 11 X is selected from F, Cl, and CN. In some embodiments, X 11 is N, and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), and R 11 X is selected from F and CN. In some embodiments, X 11 is N, and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), and R 11 is selected from F. In some embodiments, X 11 is N, and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), and R 11 X is selected from CN. In some embodiments, X 11 is N, and X 12 is C(H) and X 13 is N, and Y 11 is C(H), and Y 12 is C(CN). In some embodiments, X11 is N, and X 12 is C(H) and X 13 is N, and Y 11 is C(H), and Y 12 is C(CN). In some embodiments, X 11 is N, and X 12 is C(H) and X 13 is N, and Y 11 is C(H), and Y 12 is C(CN), and R 16 is a C1 alkyl group which is substituted as needed. In some embodiments, X 11 is N, and X 12 is C(H) and X 13 is N, and Y 11 is C(H), and Y 12 is C(CN), and R 16 is -CH3. In some embodiments, X 11 is N, and X 12 is C(H) and X 13 is N, and Y 11 is C(H), and Y 12 is C(CN), and R 15 H is H. In some embodiments, X 11 is N, and X 12 is C(H) and X 13 is N, and Y 11 is C(H), and Y 12 C(CN) and R 14 H is H, and R 14 ' is H. In some embodiments, X 11 is N, and X 12 is C(H) and X 13 is N, and Y 11 is C(H), and Y 12 is C(CN), and R 12 H is H. In some embodiments, X 11 is N, and X 12 is C(H) and X 13 is N, and Y 11is C(H), and Y 12 is C(CN), and R 13 X is selected from CH3, H, and cyclopropyl. In some embodiments, X 11 is N, and X 12 is C(H) and X 13 is N, and Y 11 is C(H), and Y 12 is C(CN), and R 13 is selected from CH3. In some embodiments, X 11 is N, and X 12 is C(H) and X 13 is N, and Y 11 is C(H), and Y 12 is C(CN), and R 13 X is selected from cyclopropyl. In some embodiments, X 11 is N, and X 12 is C(H) and X 13 is N, and Y 11 is C(H), and Y 12 is C(CN), and R 13 is selected from H. In some embodiments, X 11 is N, and X 12 is C(H) and X 13 is N, and Y 11 is C(H), and Y 12 is C(CN), and R 11 The is selected from CH3, cyclopropyl, F, Cl, Br, CF3, CN, N3, OH, and OMe. In some embodiments, X 11 is N, and X 12 is C(H) and X 13 is N, and Y 11 is C(H), and Y 12 is C(CN), and R 11 X is selected from CH3, F, Cl, Br, CF3, and CN. In some embodiments, X 11 is N, and X 12 is C(H) and X 13 is N, and Y11 is C(H), and Y 12 is C(CN), and R 11 X is selected from F, Cl, and CN. In some embodiments, X 11 is N, and X 12 is C(H) and X 13 is N, and Y 11 is C(H), and Y 12 is C(CN), and R 11 X is selected from F and CN. In some embodiments, X 11 is N, and X 12 is C(H) and X 13 is N, and Y 11 is C(H), and Y 12 is C(CN), and R 11 is selected from F. In some embodiments, X 11 is N, and X 12 is C(H) and X 13 is N, and Y 11 is C(H), and Y 12 is C(CN), and R 11 X is selected from CN. In some embodiments, X 11 C(F) and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN). In some embodiments, X 11 C(F) and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN). In some embodiments, X 11 C(F) and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), and R 16 is a C1 alkyl group which is substituted as needed. In some embodiments, X11 C(F) and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), and R 16 is -CH3. In some embodiments, X 11 C(F) and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), and R 15 H is H. In some embodiments, X 11 C(F) and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 C(CN) and R 14 H is H, and R 14 ' is H. In some embodiments, X 11 C(F) and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), and R 12 H is H. In some embodiments, X 11 C(F) and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), and R 13 X is selected from CH3, H, and cyclopropyl. In some embodiments, X 11 C(F) and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), and R 13 is selected from CH3. In some embodiments, X 11C(F) and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), and R 13 X is selected from cyclopropyl. In some embodiments, X 11 C(F) and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), and R 13 is selected from H. In some embodiments, X 11 C(F) and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), and R 11 The is selected from CH3, cyclopropyl, F, Cl, Br, CF3, CN, N3, OH, and OMe. In some embodiments, X 11 C(F) and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), and R 11 X is selected from CH3, F, Cl, Br, CF3, and CN. In some embodiments, X 11 C(F) and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), and R 11 X is selected from F, Cl, and CN. In some embodiments, X 11 C(F) and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), and R 11X is selected from F and CN. In some embodiments, X 11 C(F) and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), and R 11 is selected from F. In some embodiments, X 11 C(F) and X 12 is N, and X 13 is C(H) and Y 11 is C(H), and Y 12 is C(CN), and R 11 It is selected from CN.
[0286] In some embodiments, the compound of formula (II) is formula (IIa): [ka] or its salt.
[0287] In some embodiments, the compound of formula (II) is formula (IIb): [ka] or its salt.
[0288] In some embodiments, the compound of formula (II) is formula (IIc): [ka] or its salt.
[0289] In some embodiments, the compound of formula (II) is formula (IId): [ka] or its salt.
[0290] In some embodiments, the compound of formula (II) is formula (IIe): [ka] or its salt.
[0291] In certain circumstances, this disclosure relates to formula (IIf) [ka] We provide a compound or a salt thereof represented by formula (IIf): R 14 teeth: Hydrogen, halogen, -OR 19d , -SR 19d , -N(R 19d )2, -NO2, and -CN; and C 1~6 Alkyl, halogen, -OR 19d , -SR 19d , -N(R 19d )2, -NO2, and -CN, which are substituted as needed with one or more substituents independently selected from these; and C 3~10 Carbon rings and 3- to 10-membered heterocycles, each of which is a halogen, -OR 19d , -SR 19d , -N(R 19d )2, -C(O)R 19d ,-C(O)N(R 19d )2, -N(R 19d )C(O)R 19d , -N(R 19d )C(O)N(R 19d )2, -OC(O)N(R 19d )2, -N(R 19d )C(O)OR 19d , -C(O)OR 19d ,-OC(O)R 19d ,-S(O)R 19d -S(O)2R 19d -NO2, =O-, =S, =N(R 19d ), and one or more substituents selected independently of -CN as needed. Selected from.
[0292] In some embodiments, the compound of formula (IIa) is the compound of formula (II).
[0293] In some embodiments, the compound of formula (IIb) is the compound of formula (II).
[0294] In some embodiments, the compound of formula (IIc) is the compound of formula (II).
[0295] In some embodiments, the compound of formula (IId) is the compound of formula (II).
[0296] In some embodiments, the compound of formula (IIe) is the compound of formula (II).
[0297] In some embodiments, the compound of formula (IIf) is the compound of formula (II).
[0298] In some embodiments, the compound of formula (IIa) is the compound of formula (II-A).
[0299] In some embodiments, the compound of formula (IIb) is the compound of formula (II-A).
[0300] In some embodiments, the compound of formula (IIc) is the compound of formula (II-A).
[0301] In some embodiments, the compound of formula (IId) is the compound of formula (II-A).
[0302] In some embodiments, the compound of formula (IIe) is the compound of formula (II-A).
[0303] In some embodiments, the compound of formula (IIf) is the compound of formula (II-A).
[0304] In some embodiments, this compound [ka] or its salt.
[0305] In some embodiments, the compound of formula (II), formula (II-A), or formula (II') is compound 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 72, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 102, 103, 104, 105, 106, 107, 108, 109, 1 10, 111, 112, 113, 114, 115, 116, 117, 118, 119, 120, 121, 122, 123, 124, 125, 126, 127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 137, 1038, 1039, 1040 ,1041,1042,1043,1044,1045,1046,1047,1048,1049,1050,1051,1052,1053,1054,1055,1056,1057,1058,1059,1060,1061,1062,1063,1064,1065 ,1066,1067,1068,1069,1070,1071,1072,1073,1074,1075,1076,1077,1078,1079,1080,1081,1082,1083,1084,1085,1086,1087,1088,1089,1090 ,1091,1092,1093,1094,1095,1096,1097,1098,1099,1100,1101,1102,1103,1104,1105,1106,1107,1108,1109,1110,1111,1112,1113,1114,1115 ,1116,1117,1118,1119,1120,1121,1122,1123,1124,1125,1126,1127,1128,1129,1130,1131,1132,1133,1134,1135,1136,1137,1138,1139,1140,1141, 1142, 1143, 1144, 1145...
Claims
1. Equation (I): 【Chemistry 279】 A compound or salt thereof represented by formula (I): X 1 , X 2 , and X 3 are each independently selected from C(R), and N, where X 1 , X 2 , and X 3 at least one of which is N, and X 1 , X 2 , and X 3 no more than two of which are N; X 4 is selected from C(R); Each R is independent: Hydrogen, halogen, -NO 2 -CN, -N 3 , -OR 8 , -SR 8 , -N(R 8 ) 2 , -C(O)R 8 , -C(O)N(R 8 ) 2 , -N(R 8 ) C(O)R 8 , -N(R 8 ) C(O)N(R 8 ) 2 , -OC(O)N(R 8 ) 2 , -N(R 8 ) C(O)OR 8 , -C(O)OR 8 , -OC(O)R 8 , -S(O)R 8 , and -S(O) 2 R 8 ; C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkynnyl, each of which is a halogen, -OR 8 , -SR 8 , -N(R 8 ) 2 , -C(O)R 8 , -C(O)N(R 8 ) 2 , -N(R 8 ) C(O)R 8 , -C(O)OR 8 , -OC(O)R 8 , -N(R 8 ) C(O)N(R 8 ) 2 , -OC(O)N(R 8 ) 2 , -N(R 8 ) C(O)OR 8 , -S(O)R 8 , -S(O) 2 R 8 , -NO 2 , =O, =S, =N(R 8 ), -CN, C 3~10 The carbon ring is optionally substituted with one or more substituents independently selected from a carbon ring and a 3-membered to 10-membered heterocycle, where the C 3~10 Carbon rings and 3- to 10-membered heterocycles are R 7 Each of which is substituted as necessary with one or more substituents independently selected from; and C 3~10 A carbon ring and a 3- to 10-member heterocyclic ring, each of which is independently selected from one or more substituents selected from halogen, -OR 8 , -SR 8 , -N(R 8 ), -C(O)R 2 , -C(O)N(R 8 ), -N(R 8 ), -N(R 2 ), -N(R 8 ), -N(R 8 ), -N(R 8 ), -OC(O)N(R 8 ), -N(R 2 ), -C(O)OR 8 ), -OC(O)R 2 ), -S(O)R 8 ), -S(O) 8 R 8 ), -NO 8 ), =O-, =S, =N(R 8 ), -CN, C 2 alkyl, C 8 alkenyl, and C 2 alkynyl, and each is optionally substituted with one or more substituents independently selected from R 8 ), where C 1~6 alkyl, C 2~6 alkenyl, and C 2~6 alkynyl are each optionally substituted with one or more substituents independently selected from R 1~6 alkyl, C 2~6 alkenyl, and C 2~6 alkynyl are each optionally substituted with one or more substituents independently selected from R 7 and each is optionally substituted with one or more substituents independently selected from R Selected from; R 1 teeth: hydrogen; C 1~6 alkyl, C 2~6 alkenyl, and C 2~6 alkynyl, each of which is halogen, -OR 8a , -SR 8a , -N(R 8a ), 2 , -C(O)R 8a , -C(O)N(R 8a ), 2 , -N(R 8a ), C(O)R 8a , -C(O)OR 8a , -OC(O)R 8a , -N(R 8a ), C(O)N(R 8a ), 2 , -OC(O)N(R 8a ), 2 , -N(R 8a ), C(O)OR 8a , -S(O)R 8a , -S(O)[[ID= C 3~10 Carbon rings and 3- to 10-membered heterorings, each of which is a halogen, -OR 8a , -SR 8a , -N(R 8a ) 2 , -C(O)R 8a , -C(O)N(R 8a ) 2 , -N(R 8a ) C(O)R 8a , -N(R 8a ) C(O)N(R 8a ) 2 , -OC(O)N(R 8a ) 2 , -N(R 8a ) C(O)OR 8a , -C(O)OR 8a , -OC(O)R 8a , -S(O)R 8a , -S(O) 2 R 8a , -NO 2 , =O-, =S, =N(R 8a ), -CN, C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 It is optionally substituted with one or more substituents independently selected from the alkynyl, where C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl is R 7a Each of which is substituted as needed by one or more substituents independently selected from the original. Selected from; or R 1 is R 2 Together with C 3~10 They form a carbon ring or a 3- to 10-membered heteroring, each of which is a halogen, -OR 8a , -SR 8a , -N(R 8a ) 2 , -C(O)R 8a , -C(O)N(R 8a ) 2 , -N(R 8a ) C(O)R 8a , -N(R 8a ) C(O)N(R 8a ) 2 , -OC(O)N(R 8a ) 2 , -N(R 8a ) C(O)OR 8a , -C(O)OR 8a , -OC(O)R 8a , -S(O)R 8a , -S(O) 2 R 8a , -NO 2 , =O-, =S, =N(R 8a ), -CN, C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 It is optionally substituted with one or more substituents independently selected from the alkynyl, where C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl is R 7b Each substituent is substituted as needed by one or more substituents selected independently of the original; R 2 teeth: hydrogen; C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkynnyl, each of which is a halogen, -OR 8b , -SR 8b , -N(R 8b ) 2 , -C(O)R 8b , -C(O)N(R 8b ) 2 , -N(R 8b ) C(O)R 8b , -C(O)OR 8b , -OC(O)R 8b , -N(R 8b ) C(O)N(R 8b ) 2 , -OC(O)N(R 8b ) 2 , -N(R 8b ) C(O)OR 8b , -S(O)R 8b , -S(O) 2 R 8b , -NO 2 , =O, =S, =N(R 8b ), -CN, C 3~10 The carbon ring is optionally substituted with one or more substituents independently selected from 3-membered to 10-membered heterocycles, where the C 3~10 Carbon rings and 3- to 10-membered heterocycles are R 7b Each of which is substituted as necessary with one or more substituents independently selected from; and C 3~10 Carbon rings and 3- to 10-membered heterorings, each of which is a halogen, -OR 8b , -SR 8b , -N(R 8b ) 2 , -C(O)R 8b , -C(O)N(R 8b ) 2 , -N(R 8b ) C(O)R 8b , -N(R 8b ) C(O)N(R 8b ) 2 , -OC(O)N(R 8b ) 2 , -N(R 8b ) C(O)OR 8b , -C(O)OR 8b , -OC(O)R 8b , -S(O)R 8b , -S(O) 2 R 8b , -NO 2 , =O-, =S, =N(R 8b ), -CN, -N 3 , C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 It is optionally substituted with one or more substituents independently selected from the alkynyl, where C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl is R 7b Each of which is substituted as needed by one or more substituents independently selected from the original. Selected from; or R 1 is R 2 Together with C 3~10 They form a carbon ring or a 3- to 10-membered heteroring, each of which is a halogen, -OR 8a , -SR 8a , -N(R 8a ) 2 , -C(O)R 8a , -C(O)N(R 8a ) 2 , -N(R 8a ) C(O)R 8a , -N(R 8a ) C(O)N(R 8a ) 2 , -OC(O)N(R 8a ) 2 , -N(R 8a ) C(O)OR 8a , -C(O)OR 8a , -OC(O)R 8a , -S(O)R 8a , -S(O) 2 R 8a , -NO 2 , =O-, =S, =N(R 8a ), -CN, C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 It is optionally substituted with one or more substituents independently selected from the alkynyl, where C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl is R 7b Each substituent is substituted as needed by one or more substituents selected independently of the original; R 3 teeth: Hydrogen, halogen, -OR 8c , -SR 8c , -N(R 8c ) 2 , -NO 2 , and -CN; and R 7c C as needed, substituted with one or more substituents independently selected from 1~6 Alkyl Selected from; R 4 teeth: Hydrogen, halogen, -OR 8d , -SR 8d , -N(R 8d ) 2 , -NO 2 , and -CN; and Halogen, -OR 8d , -SR 8d , -N(R 8d ) 2 , -NO 2 , and -CN, C 3~10 A carbon ring and a carbon ring, optionally substituted with one or more substituents independently selected from 3-membered to 10-membered heterocycles. 1~6 Alkyl, where C 3~10 Carbon rings and 3- to 10-membered heterocycles are R 7d Each of which is substituted as needed by one or more substituents independently selected from the original. Selected from; R 4 'teeth: Hydrogen, halogen, -OR 8d , -SR 8d , -N(R 8d ) 2 , -NO 2 , and -CN; and Halogen, -OR 8d , -SR 8d , -N(R 8d ) 2 , -NO 2 , and -CN, C 3~10 A carbon ring and a carbon ring, optionally substituted with one or more substituents independently selected from 3-membered to 10-membered heterocycles. 1~6 Alkyl, where C 3~10 Carbon rings and 3- to 10-membered heterocycles are R 7d Each of which is substituted as needed by one or more substituents independently selected from the original. Selected from; Or R 4 and R 4 'together with C 3~10 A carbon ring or a 3-membered to 10-membered heterocycle is formed, where the C 3~10 A carbon ring, or a 3- to 10-membered heterocycle, is R 7d It is optionally substituted with one or more substituents selected independently of it; R 5 teeth: Hydrogen, halogen, -OR 8e , -SR 8e , -N(R 8e ) 2 , -NO 2 ,-CN,C 1~6 Alkyl, C 3~10 A carbon ring, and a 3-membered to 10-membered heteroring, where the C 1~6 Alkyl, C 3~10 Carbon rings and 3- to 10-membered heterocycles are R 7e Each of which is substituted as needed by one or more substituents independently selected from the original. Selected from; R 6 teeth: Hydrogen, halogen, -OR 8f , -SR 8f , -N(R 8f ) 2 , -NO 2 , and -CN; and R 7f C as needed, substituted with one or more substituents independently selected from 1~6 Alkyl Selected from; Each R 7 , R 7a , R 7b , R 7c , R 7d , R 7e , and R 7f Independently: Halogen, -OR 8g , -SR 8g , -N(R 8g ) 2 , -C(O)R 8g , -C(O)N(R 8g ) 2 , -N(R 8g ) C(O)R 8g , -N(R 8g ) C(O)N(R 8g ) 2 , -OC(O)N(R 8g ) 2 , -N(R 8g ) C(O)OR 8g , -C(O)OR 8g , -OC(O)R 8g , -S(O)R 8g , -S(O) 2 R 8g , -NO 2 , =O, =S, =N(R 8g ), and -CN; and C 1~3 Alkyl, C 2~3 Alkenyl and C 2~3 Alkynnyl, each of which is a halogen, -OR 8g , -SR 8g , -N(R 8g ) 2 , -C(O)R 8g , -C(O)N(R 8g ) 2 , -N(R 8g ) C(O)R 8g , -N(R 8g ) C(O)N(R 8g ) 2 , -OC(O)N(R 8g ) 2 , -N(R 8g ) C(O)OR 8g , -C(O)OR 8g , -OC(O)R 8g , -S(O)R 8g , -S(O) 2 R 8g , -NO 2 , =O, =S, =N(R 8g ), and as needed, substituted with one or more substituents independently selected from -CN. Selected from; Each R 8 , R 8a , R 8b , R 8c , R 8d , R 8e , R 8f , and R 8g Independently: Hydrogen and halogens; and C 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl and C 3~10 A carbon ring, each of which is a halogen, -CN, -OH, -SH, -NO 2 , -NH 2 , =O, =S, -OC 1~6 Alkyl, -S-C 1~6 Alkyl, -N(C) 1~6 Alkyl) 2 ,-NH(C 1~6 Alkyl), C 3~10 Carbon rings, or those optionally substituted with one or more substituents independently selected from 3-membered to 10-membered heterocycles; and C 3~10 Carbon rings and 3- to 10-membered heterocycles, each of which is a halogen, -CN, -OH, -SH, -NO 2 , -NH 2 , =O, =S, -OC 1~6 Alkyl, -S-C 1~6 Alkyl, -SO 2 -C 1~6 Alkyl, -N(C) 1~6 Alkyl) 2 ,-NH(C 1~6 Alkyl), C 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 3~10 Carbon rings, 3-membered to 10-membered heterocycles, and C 1~6 Substituted as needed with one or more substituents independently selected from the haloalkyl group. A compound or a salt thereof, selected from the following.
2. X 1 The compound or salt according to claim 1, wherein is N.
3. X 1 The compound or salt according to claim 1, wherein is C(R).
4. X 2 A compound or salt according to any one of claims 1 to 3, wherein is N.
5. X 2 A compound or salt according to any one of claims 1 to 3, wherein C(R).
6. Each R independently: Hydrogen, halogen, -CN, -N 3 , -OR 8 , -SR 8 , -N(R 8 ) 2 ; C 1~6 Alkyl and C 2~6 Alkynnyls, each of which is optionally substituted with one or more substituents independently selected from halogens; and C 3~10 Carbon rings and 3- to 10-membered heterocycles A compound or salt according to any one of claims 1 to 5, selected from the above.
7. Each R independently represents: hydrogen, -F, -Cl, -Br, -I, -CN, -N 3 , -OH, -OMe, -OEt, -O(n-Pr), -O(iPr), -O(i-Bu), 【Chemistry 280】 -CF 3 -methyl, -ethyl, cyclopropyl, -CH 2 N(CH 3 ) 2 A compound or salt according to any one of claims 1 to 5, selected from -CCMe, -CCH, phenyl, N-morpholinyl, and N-pyrrolidinyl.
8. Each R 8 These independently produce hydrogen, methyl, ethyl, propyl, isopropyl, cyclopropyl, isobutyl, and -CF 3 ien-CH 2 CF 3 ien-CH 2 CHF 2 ien-CH 2 C(F)(Me) 2 , and -CH 2 - A compound or salt according to any one of claims 1 to 7, selected from phenyl.
9. R 1 However, hydrogen, methyl, -CH 2 OH, -CH 2 CH 2 OH, C(Me) 2 OH, -CH 2 Is it OMe, or R 1 R 2 Together with C 3~10 A carbon ring, or a 3- to 10-membered heterocycle, each of which is optionally substituted with one or more substituents independently selected from -F, -COMe, -CN, and methyl. The compound or salt according to any one of claims 1 to 8.
10. R 1 However, methyl, -CH 2 OH, -CH 2 CH 2 OH, C(Me) 2 OH, or -CH 2 A compound or salt according to any one of claims 1 to 9, wherein the compound is OMe.
11. R 1 A compound or salt according to any one of claims 1 to 10, wherein is methyl.
12. R 2 but: C 3~10 Selected from carbon rings and 3- to 10-membered heterocycles, each of which is a halogen, -OR 8b , -C(O)R 8b , -S(O) 2 R 8b , -CN, and C 1~6 It is optionally substituted with one or more substituents independently selected from alkyl, where C 1~6 Alkyl is one or more R 7b It is replaced as needed; or R 1 R 2 Together with C 3~10 They form a carbon ring or a 3- to 10-membered heteroring, each of which is a halogen, -C(O)R 8a ,-CN,N 3 , and C 1~6 It is optionally substituted with one or more substituents independently selected from alkyl, where C 1~6 Alkyl is one or more R 7b It is replaced as needed. The compound or salt according to any one of claims 1 to 11.
13. R 2 However, these are selected from phenyl, pyridinyl, pyrimidinyl, pyrazinyl, and pyridazinyl, each of which is -F, -OH, -OMe, -COMe, -SO 2 The compound or salt according to any one of claims 1 to 12, optionally substituted with one or more substituents independently selected from Me, -CN, and methyl.
14. R 2 but, 【Chemistry 281】 A compound or salt according to any one of claims 1 to 12, selected from the above.
15. R 1 and R 2 and together, 【Chemistry 282】 C selected from 3~10 A compound or salt according to any one of claims 1 to 8 or 12, which forms a carbocyclic ring or a 3- to 10-membered heterocyclic ring. 【Request Item 16】 【Chemistry 283】 but: 【Chemistry 284】 A compound or salt according to any one of claims 1 to 8, selected from the above.
17. R 3 A compound or salt according to any one of claims 1 to 16, wherein the compound is hydrogen.
18. R 4 Independently: Hydrogen, halogen, -OR 8d , and -CN; and Halogen, -OR 8d , and -CN, C 3~10 A carbon ring and a carbon ring, optionally substituted with one or more substituents independently selected from 3-membered to 10-membered heterocycles. 1~6 Alkyl, where C 3~10 Carbon rings and 3- to 10-membered heterocycles have one or more R 7d Each is replaced as needed. Selected from; and R 4 'but: Hydrogen, halogen, -OR 8d , and -CN; and Halogen, -OR 8d , and -CN, C 3~10 A carbon ring and a carbon ring, optionally substituted with one or more substituents independently selected from 3-membered to 10-membered heterocycles. 1~6 Alkyl, where C 3~10 Carbon rings and 3- to 10-membered heterocycles have one or more R 7d Each is replaced as needed. A compound or salt according to any one of claims 1 to 17, selected from the above.
19. Each R 4 However, hydrogen was selected, and R 4 A compound or salt according to any one of claims 1 to 18, wherein hydrogen is selected from the compound or salt.
20. R 4 is -F, and R 4 A compound or salt according to any one of claims 1 to 18, wherein ' is -F.
21. R 5 but: Hydrogen, halogen, -OR 8e , -N(R 8e ) 2 ,-CN,C 1~6 Alkyl, C 3~10 Selected from carbon rings and 3-membered to 10-membered heterocycles, where the C 1~6 Alkyl, C 3~10 Carbon rings and 3- to 10-membered heterocycles have one or more R 7e The compound or salt according to any one of claims 1 to 20, wherein each is substituted as necessary.
22. R 5 However, hydrogen, -F, -Cl, -OH, -OMe, -NHMe, -CN, C 1~2 Selected from alkyl and cyclopropyl, where C 1~2 The compound or salt according to any one of claims 1 to 21, wherein the alkyl and cyclopropyl groups are each optionally substituted with one or more -F groups.
23. R 5 However, hydrogen and CH 3 A compound or salt according to any one of claims 1 to 22, selected from the above.
24. R 6 A compound or salt according to any one of claims 1 to 23, wherein the compound is hydrogen.
25. Equation (II-A): 【Chemical 285】 A compound or salt thereof represented by formula (II-A): X 11 is C(R 17a ) and N are selected; X 12 is C(R 17b ) and N are selected; X 13 is C(R 17c ) and N are selected; Y 11 is C(R 17d ) and N are selected; Y 12 is C(R 17e ) and N are selected; Each R 11a , R 11b , R 11c , and R 11d Independently: Hydrogen, halogen, -NO 2 -CN, -N 3 , -OR 19a , -SR 19a , -N(R 19a ) 2 , -C(O)R 19a , -C(O)N(R 19a ) 2 , -N(R 19a ) C(O)R 19a , -N(R 19a ) C(O)N(R 19a ) 2 , -OC(O)N(R 19a ) 2 , -N(R 19a ) C(O)OR 19a , -C(O)OR 19a , -OC(O)R 19a , -S(O)R 19a , and -S(O) 2 R 19a ; C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkynnyl, each of which is a halogen, -OR 19a , -SR 19a , -N(R 19a ) 2 , -C(O)R 19a , -C(O)N(R 19a ) 2 , -N(R 19a ) C(O)R 19a , -C(O)OR 19a , -OC(O)R 19a , -N(R 19a ) C(O)N(R 19a ) 2 , -OC(O)N(R 19a ) 2 , -N(R 19a ) C(O)OR 19a , -S(O)R 19a , -S(O) 2 R 19a , -NO 2 , =O, =S, =N(R 19a ), -CN, C 3~10 The carbon ring is optionally substituted with one or more substituents independently selected from a carbon ring and a 3-membered to 10-membered heterocycle, where the C 3~10 Carbon rings and 3- to 10-membered heterocycles are R 18a Each of which is substituted as necessary with one or more substituents independently selected from; and C 3~10 Carbon rings and 3- to 10-membered heterorings, each of which is a halogen, -OR 19a , -SR 19a , -N(R 19a ) 2 , -C(O)R 19a , -C(O)N(R 19a ) 2 , -N(R 19a ) C(O)R 19a , -N(R 19a ) C(O)N(R 19a ) 2 , -OC(O)N(R 19a ) 2 , -N(R 19a ) C(O)OR 19a , -C(O)OR 19a , -OC(O)R 19a , -S(O)R 19a , -S(O) 2 R 19a , -NO 2 , =O-, =S, =N(R 19a ), -CN, C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 It is optionally substituted with one or more substituents independently selected from the alkynyl, where C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl is R 18a Each of which is substituted as needed by one or more substituents independently selected from the original. Selected from; Here R 11a , R 11b , and R 11c If each is hydrogen; R 11d It is not hydrogen; Here R 11b ga-OCH 3 If R 11c It's not -OMe; R 12 teeth: Hydrogen, halogen, -NO 2 -CN, -OR 19b , -SR 19b , -N(R 19b ) 2 , -C(O)R 19b , -C(O)N(R 19b ) 2 , -N(R 19b ) C(O)R 19b , -N(R 19b ) C(O)N(R 19b ) 2 , -OC(O)N(R 19b ) 2 , -N(R 19b ) C(O)OR 19b , -C(O)OR 19b , -OC(O)R 19b , -S(O)R 19b , and -S(O) 2 R 19b ; C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkynnyl, each of which is a halogen, -OR 19b , -SR 19b , -N(R 19b ) 2 , -C(O)R 19b , -C(O)N(R 19b ) 2 , -N(R 19b ) C(O)R 19b , -C(O)OR 19b , -OC(O)R 19b , -N(R 19b ) C(O)N(R 19b ) 2 , -OC(O)N(R 19b ) 2 , -N(R 19b ) C(O)OR 19b , -S(O)R 19b , -S(O) 2 R 19b , -NO 2 , =O, =S, =N(R 19b ), -CN, C 3~10 The carbon ring is optionally substituted with one or more substituents independently selected from a carbon ring and a 3-membered to 10-membered heterocycle, where the C 3~10 Carbon rings and 3- to 10-membered heterocycles are R 18b Each of which is substituted as necessary with one or more substituents independently selected from; and C 3~10 Carbon rings and 3- to 10-membered heterorings, each of which is a halogen, -OR 19b , -SR 19b , -N(R 19b ) 2 , -C(O)R 19b , -C(O)N(R 19b ) 2 , -N(R 19b ) C(O)R 19b , -N(R 19b ) C(O)N(R 19b ) 2 , -OC(O)N(R 19b ) 2 , -N(R 19b ) C(O)OR 19b , -C(O)OR 19b , -OC(O)R 19b , -S(O)R 19b , -S(O) 2 R 19b , -NO 2 , =O-, =S, =N(R 19b ), -CN, C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 It is optionally substituted with one or more substituents independently selected from the alkynyl, where C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl is R 18b Each of which is substituted as needed by one or more substituents independently selected from the original. Selected from; R 13 teeth: Hydrogen, halogen, -OR 19c , -SR 19c , -N(R 19c ) 2 , -NO 2 , and -CN; and Halogen, -OR 19c , -SR 19c , -N(R 19c ) 2 , -NO 2 , and C, which may be substituted as needed with one or more substituents independently selected from -CN. 1~6 alkyl; and C 3~10 Carbon rings and 3- to 10-membered heterorings, each of which is a halogen, -OR 19c , -SR 19c , -N(R 19c ) 2 , -C(O)R 19c , -C(O)N(R 19c ) 2 , -N(R 19c ) C(O)R 19c , -N(R 19c ) C(O)N(R 19c ) 2 , -OC(O)N(R 19c ) 2 , -N(R 19c ) C(O)OR 19c , -C(O)OR 19c , -OC(O)R 19c , -S(O)R 19c , -S(O) 2 R 19c , -NO 2 , and which are optionally substituted with one or more substituents independently selected from -CN. Selected from; R 14 teeth: Hydrogen, halogen, -OR 19d , -SR 19d , -N(R 19d ) 2 , -NO 2 , and -CN; and C 1~6 Alkyl, halogen, -OR 19d , -SR 19d , -N(R 19d ) 2 , -NO 2 , and those which are optionally substituted with one or more substituents independently selected from -CN; and C 3~10 Carbon rings and 3- to 10-membered heterorings, each of which is a halogen, -OR 19d , -SR 19d , -N(R 19d ) 2 , -C(O)R 19d , -C(O)N(R 19d ) 2 , -N(R 19d ) C(O)R 19d , -N(R 19d ) C(O)N(R 19d ) 2 , -OC(O)N(R 19d ) 2 , -N(R 19d ) C(O)OR 19d , -C(O)OR 19d , -OC(O)R 19d , -S(O)R 19d , -S(O) 2 R 19d , -NO 2 , =O-, =S, =N(R 19d ), and as needed, substituted with one or more substituents independently selected from -CN. Selected from; R 14’ teeth: Hydrogen, halogen, -OR 19d , -SR 19d , -N(R 19d ) 2 , -NO 2 , and -CN; and C 1~6 Alkyl, halogen, -OR 19d , -SR 19d , -N(R 19d ) 2 , -NO 2 , and those which are optionally substituted with one or more substituents independently selected from -CN; and C 3~10 Carbon rings and 3- to 10-membered heterorings, each of which is a halogen, -OR 19d , -SR 19d , -N(R 19d ) 2 , -C(O)R 19d , -C(O)N(R 19d ) 2 , -N(R 19d ) C(O)R 19d , -N(R 19d ) C(O)N(R 19d ) 2 , -OC(O)N(R 19d ) 2 , -N(R 19d ) C(O)OR 19d , -C(O)OR 19d , -OC(O)R 19d , -S(O)R 19d , -S(O) 2 R 19d , -NO 2 , =O-, =S, =N(R 19d ), and as needed, substituted with one or more substituents independently selected from -CN. Selected from; or R 14 is R 14’ Together with C 3~10 A carbon ring or a 3-membered to 10-membered heterocycle is formed, where the C 3~10 A carbon ring, or a 3- to 10-membered heterocycle, is R 18c It is optionally substituted with one or more substituents selected independently of it; R 15 teeth: Hydrogen, halogen, -OR 19e , -SR 19e , -N(R 19e ) 2 , -NO 2 , and -CN; and R 18d C as needed, substituted with one or more substituents independently selected from 1~6 Alkyl Selected from; or R 15 is R 17a Together with these, they form a 3- to 10-membered heteroring, where the 3- to 10-membered heteroring is composed of one or more R 18f It is replaced as needed; or R 15 is R 17b Together with these, they form a 3- to 10-membered heteroring, where the 3- to 10-membered heteroring is R 18f It is optionally substituted with one or more substituents selected independently of it; R 16 teeth: Hydrogen, halogen, -OR 19f , -SR 19f -N(R) 19f ) 2 , -NO 2 , and -CN; and One or more R 18e C replaced as needed 1~6 Alkyl Selected from; or R 16 is R 17a Together with these, they form a 3- to 10-membered heteroring, where the 3- to 10-membered heteroring is composed of one or more R 18f It is replaced as needed; or R 16 is R 17b Together with these, they form a 3- to 10-membered heteroring, where the 3- to 10-membered heteroring is composed of one or more R 18f It is replaced as needed; Each R 17a , R 17b , R 17c , R 17d , and R 17e Independently: Hydrogen, halogen, -OR 19g , -SR 19g , -N(R 19g ) 2 , -NO 2 -CN, -N 3 ; and C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl, each of which has one or more R 18f Those that are replaced as needed Selected from; or R 15 is R 17a Together with these, they form a 3- to 10-membered heteroring, where the 3- to 10-membered heteroring is composed of one or more R 18f It is replaced as needed; or R 15 is R 17b Together with these, they form a 3- to 10-membered heteroring, where the 3- to 10-membered heteroring is composed of one or more R 18f It is replaced as needed; or R 16 is R 17a Together with these, they form a 3- to 10-membered heteroring, where the 3- to 10-membered heteroring is composed of one or more R 18f It is replaced as needed; or R 16 is R 17b Together with these, they form a 3- to 10-membered heteroring, where the 3- to 10-membered heteroring is composed of one or more R 18f It is replaced as needed; or R 15 , R 16 , and R 17b These elements combine to form a bridged heteroring, where the bridged heteroring consists of one or more R elements. 18f It is replaced as needed; Each R 18a , R 18b , R 18c , R 18d , R 18e , and R 18f Independently: halogen, -OR 19h , -SR 19h , -N(R 19h ), 2 , -C(O)R 19h , -C(O)N(R 19h ), 2 , -N(R 19h )C(O)R 19h , -N(R 19h )C(O)N(R 19h ), 2 , -OC(O)N(R 19h ), 2 , -N(R 19h )C(O)OR 19h , -C(O)OR 19h , -OC(O)R 19h , -S(O)R 19h , -S(O 2 R 19h , -NO 2 , =O, =S, =N(R 19h ), and -CN; and C 1~3 Alkyl, C 2~3 Alkenyl and C 2~3 Alkynnyl, each of which is a halogen, -OR 19h , -SR 19h , -N(R 19h ) 2 , -C(O)R 19h , -C(O)N(R 19h ) 2 , -N(R 19h ) C(O)R 19h , -N(R 19h ) C(O)N(R 19h ) 2 , -OC(O)N(R 19h ) 2 , -N(R 19h ) C(O)OR 19h , -C(O)OR 19h , -OC(O)R 19h , -S(O)R 19h , -S(O) 2 R 19h , -NO 2 , =O, =S, =N(R 19h ), and as needed, substituted with one or more substituents independently selected from -CN. Selected from; Each R 19a , R 19b , R 19c , R 19d , R 19e , R 19f , R 19g , and R 19h Independently: Hydrogen; and C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkynnyl, each of which is a halogen, -CN, -OH, -SH, -NO 2 , -NH 2 , =O, =S, -OC 1~6 Alkyl, -S-C 1~6 Alkyl, -N(C) 1~6 Alkyl) 2 ,-NH(C 1~6 Alkyl), C 3~10 Carbocyclic rings, or those optionally substituted with one or more substituents independently selected from 3-membered to 10-membered heterocycles; and C 3~10 a carbon ring, and a 3- to 10-member heterocyclic ring, each of which is independently selected from halogen, -CN, -OH, -SH, -NO 2 , -NH 2 , =O, =S, -O-C 1~6 alkyl, -S-C 1~6 alkyl, -N(C 1~6 alkyl) 2 , -NH(C 1~6 alkyl), C 1~6 alkyl, C 2~6 alkenyl, C 2~6 alkynyl, C 3~10 a carbon ring, a 3- to 10-member heterocyclic ring, and C 1~6 haloalkyl, optionally substituted with one or more substituents independently selected therefrom Selected from, A compound or its salt.
26. X 11 is C(R 17a The compound or salt according to claim 25, which is the compound or salt described in claim 25.
27. X 11 The compound or salt according to claim 25, wherein is N.
28. X 12 is C(R 17b The compound or salt according to any one of claims 25 to 27.
29. X 12 A compound or salt according to any one of claims 25 to 27, wherein is N.
30. X 13 is C(R 17c The compound or salt according to any one of claims 25 to 29.
31. X 13 A compound or salt according to any one of claims 25 to 29, wherein is N.
32. X 11 and X 13 A compound or salt according to any one of claims 25, 27-29, or 31, wherein is N.
33. X 11 and X 12 A compound or salt according to any one of claims 25, 27, or 29-31, wherein is N.
34. R 11a , R 11b , R 11c , and R 11d Each of these independently produces hydrogen, halogen, -CN, and -N. 3 , -OR 19a , C 1~6 Alkyl and C 3~10 Selected from the carbocyclic ring; Here R 11a , R 11b , and R 11c If each is hydrogen; R 11d ha: halogen, -CN, -N 3 , -OR 19a , C 1~6 Alkyl and C 3~10 Selected from the carbocyclic ring; Here R 11b ga-OCH 3 If R 11c These are independently: hydrogen, halogen, -CN, -N 3 , -OH, C 1~6 Alkyl and C 3~10 Selected from the carbocyclic ring, The compound or salt according to any one of claims 25 to 34.
35. R 11a , R 11b , R 11c , and R 11d Each of these independently comprises hydrogen, -Cl, -F, -Br, -CN, and N. 3 -OH, -OMe, methyl, cyclopropyl, -CH 2 N(CH 3 ) 2 CF 3 , and 【Chemistry 286】 Selected from; Here R 11a , R 11b , and R 11c If each is hydrogen; R 11d -Cl, -F, -Br, -CN, N 3 -OH, -OMe, methyl, cyclopropyl, -CH 2 N(CH 3 ) 2 , and CF 3 Selected from; Here R 11b ga-OCH 3 If R 11c These are independently hydrogen, -Cl, -F, -Br, -CN, and N 3 -OH, methyl, cyclopropyl, -CH 2 N(CH 3 ) 2 , and CF 3 Selected from, The compound or salt according to any one of claims 25 to 34.
36. R 11a , R 11b , R 11c , and R 11d Each of these is independently selected from hydrogen, -F, -CN, and methyl; Here R 11a , R 11b , and R 11c If each is hydrogen; R 11d is selected from -F, -CN, and methyl. The compound or salt according to any one of claims 25 to 35.
37. R 12 A compound or salt according to any one of claims 25 to 36, wherein is hydrogen.
38. R 13 but: Hydrogen, halogen, -OR 19c , -SR 19c , -N(R 19c ) 2 ; and C 1~6 Alkyl, halogen, -OR 19c , -SR 19c , -N(R 19c ) 2 , -NO 2 , and those which are optionally substituted with one or more substituents independently selected from -CN; and C 3~10 A carbon ring, and a halogen, -OR 19c , -SR 19c , -N(R 19c ) 2 , -C(O)R 19c , -C(O)N(R 19c ) 2 , -N(R 19c ) C(O)R 19c , -N(R 19c ) C(O)N(R 19c ) 2 , -OC(O)N(R 19c ) 2 , -N(R 19c ) C(O)OR 19c , -C(O)OR 19c , -OC(O)R 19c , -S(O)R 19c , -S(O) 2 R 19c , -NO 2 , =O-, =S, =N(R 19c ), and as needed, substituted with one or more substituents independently selected from -CN. A compound or salt according to any one of claims 25 to 37, selected from the above.
39. R 13 but: hydrogen; C 1~6 Alkyl compounds, which are optionally substituted with one or more substituents independently selected from halogens, -OH, -OMe, and -CN; and C 3~10 A carbon ring, optionally substituted with one or more substituents independently selected from halogens, -OH, -OMe, and -CN. Selected from, The compound or salt according to any one of claims 25 to 38.
40. R 13 However, hydrogen, methyl, ethyl, -OH, -OMe, -CF 3 , -C(H)F 2 A compound or salt according to any one of claims 25 to 38, selected from -N(H)Me and cyclopropyl.
41. R 14 However, hydrogen, C 1~6 Selected from alkyl and halogen; and R 14’ However, hydrogen, C 1~6 A compound or salt according to any one of claims 25 to 40, selected from alkyl and halogen compounds.
42. R 14 However, it is selected from hydrogen; R 14’ A compound or salt according to any one of claims 25 to 41, wherein hydrogen is selected.
43. R 14 However, it is selected from hydrogen; R 14’ A compound or salt according to any one of claims 25 to 41, selected from methyl.
44. R 14 However, it was selected from fluoro; and R 14’ A compound or salt according to any one of claims 25 to 41, selected from fluoro.
45. R 14 and R 14’ Together, -F and -CH 3 A compound or salt according to any one of claims 25 to 41, forming a cyclopropane ring optionally substituted with one or more substituents selected from 【Request Item 46】 【Chemistry 287】 However, it forms a bridged heteroring, where the bridged heteroring is one or more R 18f A compound or salt according to any one of claims 25 to 28 or 30 to 45, which is substituted as necessary.
47. R 15 However, hydrogen and C 1~6 Selected from alkyl groups; or R 15 R 17a Together with these, they form a 3- to 10-membered heteroring, where the 3- to 10-membered heteroring is one or more -OR 19h or C 1~3 Substituted with alkyl as needed; or R 15 R 17b Together with these, they form a 3- to 10-membered heteroring, where the 3- to 10-membered heteroring is one or more -OR 19h or C 1~3 A compound or salt according to any one of claims 25 to 45, which is optionally substituted with an alkyl group.
48. R 15 Is it hydrogen; or R 15 R 17a The substance combined with it is tetrahydroisoquinoline substituted with -OH or methyl as needed; or R 15 R 17b The compound or salt according to any one of claims 25 to 45, wherein the compound combined with is tetrahydroisoquinoline, which is optionally substituted with -OH or methyl.
49. R 15 A compound or salt according to any one of claims 25 to 45, wherein is hydrogen.
50. R 16 but: Hydrogen, halogen, -OR 19f , -SR 19f -N(R) 19f ) 2 ; and one or more R 18e C replaced as needed 1~6 Alkyl Selected from; or R 16 R 17a Together with these, they form a 3- to 10-membered heteroring, where the 3- to 10-membered heteroring is composed of one or more R 18f It is replaced as needed; or R 16 R 17b Together with these, they form a 3- to 10-membered heteroring, where the 3- to 10-membered heteroring is composed of one or more R 18f It is replaced as needed. The compound or salt according to any one of claims 25 to 45.
51. R 16 However, C is substituted with hydrogen and -OH as needed. 1 Is it alkyl; or R 16 R 17a Together with these, they form dihydrobenzofuranyl or dihydrophlopyridinyl, each of which may be optionally substituted with one or more substituents independently selected from -F and -CN; or R 16 R 17b The compound or salt according to any one of claims 25 to 45, wherein together with the other, a dihydrobenzofuranyl or dihydrophlopyridinyl is formed, each of which is optionally substituted with one or more substituents independently selected from -F and -CN.
52. R 16 However, hydrogen, methyl, or CH 2 A compound or salt according to any one of claims 25 to 45, wherein the compound is an OH group.
53. R 16 A compound or salt according to any one of claims 25 to 45, wherein is methyl.
54. Each R 17a , R 17b , R 17c , R 17d , and R 17e Independently: Hydrogen, halogen, -OR 19g , and -CN; and C 1~6 Alkyl and C 2~6 Alkinyl, each of which has one or more R 18f Those that are replaced as needed Selected from; or R 15 R 17a Together with these, they form a 3- to 10-membered heteroring, where the 3- to 10-membered heteroring is composed of one or more R 18f It is replaced as needed; or R 15 R 17b Together with these, they form a 3- to 10-membered heteroring, where the 3- to 10-membered heteroring is composed of one or more R 18f It is replaced as needed; or R 16 R 17a Together with these, they form a 3- to 10-membered heteroring, where the 3- to 10-membered heteroring is composed of one or more R 18f It is replaced as needed; or R 16 R 17b Together with these, they form a 3- to 10-membered heteroring, where the 3- to 10-membered heteroring is composed of one or more R 18f It is replaced as needed. The compound or salt according to any one of claims 25 to 53.
55. Each R 17a , R 17b , R 17c , R 17d , and R 17e The following are independently selected from -F and -CN; or R 15 R 17b Together with, it is tetrahydroisoquinoline substituted as needed with -OH or methyl; or R 16 R 17b The compound or salt according to any one of claims 25 to 54, which together with the above to form a dihydrobenzofuranyl or dihydrophlopyridinyl optionally substituted with one or more -F or -CN.
56. Each R 17a , R 17b , R 17c , R 17d , and R 17e The compound or salt according to any one of claims 25 to 54, wherein is independently selected from hydrogen, methyl, -CCH, -F, and -CN.
57. R 16 and R 17a and together, C 3~10 The compound or salt according to any one of claims 25 to 49, each forming a carbocyclic ring or a 3- to 10-membered heterocyclic ring, each of which is optionally substituted with one or more substituents selected from halogens and CNs. 【Request Item 58】 【Chemistry 288】 but, 【Chemistry 289】 A compound or salt according to claim 57, selected from the above.
59. Formula (IV): 【Chemistry 290】 A compound or salt thereof represented by formula (IV): R J This is a 3- to 10-membered heterocycle, where the 3- to 10-membered heterocycle is a halogen, -OR 410b , -SR 410b , -N(R 410b ) 2 , -C(O)R 410b , -C(O)N(R 410b ) 2 , -N(R 410b ) C(O)R 410b , -N(R 410b ) C(O)N(R 410b ) 2 , -OC(O)N(R 410b ) 2 , -N(R 410b ) C(O)OR 410b , -C(O)OR 410b , -OC(O)R 410b , -S(O)R 410b , -S(O) 2 R 410b , -NO 2 , =O, =S, =N(R 410b ), -N 3 ,-CN,C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 It is optionally substituted with one or more substituents independently selected from the alkynyl, where C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl has one or more R 49a Each is replaced as needed; X 41 is C(R 41a ) and N are selected; X 42 is C(R 41b ) and N are selected; X 43 is C(R 41c ) and N are selected; X 44 is C(R 41d ) and N are selected; Here X 41 , X 42 , X 43 , and X 44 N is two or fewer of these; R 41a , R 41b , R 41c , and R 41d Each is independent of the others: hydrogen; ハロゲン、-NO 2 、-N 3 、-CN、-OR 410a 、-SR 410a 、-N(R 410a ) 2 、-C(O)R 410a 、-C(O)N(R 410a ) 2 、-N(R 410a )C(O)R 410a 、-N(R 410a )C(O)N(R 410a ) 2 、-OC(O)N(R 410a ) 2 、-N(R 410a )C(O)OR 410a 、-C(O)OR 410a 、-OC(O)R 410a 、-S(O)R 410a 、および-S(O) 2 R 410a ; C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkynnyl, each of which is a halogen, -OR 410a , -SR 410a , -N(R 410a ) 2 , -C(O)R 410a , -C(O)N(R 410a ) 2 , -N(R 410a ) C(O)R 410a , -C(O)OR 410a , -OC(O)R 410a , -N(R 410a ) C(O)N(R 410a ) 2 , -OC(O)N(R 410a ) 2 , -N(R 410a ) C(O)OR 410a , -S(O)R 410a , -S(O) 2 R 410a , -NO 2 , =O, =S, =N(R 410a ), -N 3 ,-CN,C 3~10 The carbon ring is optionally substituted with one or more substituents independently selected from a carbon ring and a 3-membered to 10-membered heterocycle, where the C 3~10 Carbon rings and 3- to 10-membered heterocycles have one or more R 49a Those which are replaced as needed; and C 3~10 Carbon rings and 3- to 10-membered heterorings, each of which is a halogen, -OR 410a , -SR 410a , -N(R 410a ) 2 , -C(O)R 410a , -C(O)N(R 410a ) 2 , -N(R 410a ) C(O)R 410a , -N(R 410a ) C(O)N(R 410a ) 2 , -OC(O)N(R 410a ) 2 , -N(R 410a ) C(O)OR 410a , -C(O)OR 410a , -OC(O)R 410a , -S(O)R 410a , -S(O) 2 R 410a , -NO 2 , =O, =S, =N(R 410a ), -N 3 ,-CN,C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 It is optionally substituted with one or more substituents independently selected from the alkynyl, where C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl has one or more R 49a Each is replaced as needed. Selected from; Here X 41 C(H) and X 42 C(H) and X 43 If C(H); R 41d It is not hydrogen; R 43 teeth: Hydrogen, halogen, -OR 410x , -SR 410x , -N(R 410x ) 2 , -NO 2 ,-CN,C 1~6 Alkyl, C 3~10 A carbon ring, and a 3-membered to 10-membered heteroring, where the C 1~6 Alkyl, C 3~10 Carbon rings and 3- to 10-membered heterocycles are R 47e Each of which is substituted as needed by one or more substituents independently selected from the original. Selected from; R 4Z teeth: -C(O)R 410z , -C(O)N(R 410z ) 2 , -C(O)OR 410z , and -CN; C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkynnyl, each of which is a halogen, -OR 410z , -SR 410z , -N(R 410z ) 2 , -C(O)R 410z , -C(O)N(R 410z ) 2 , -N(R 410z ) C(O)R 410z , -C(O)OR 410z , -OC(O)R 410z , -N(R 410z ) C(O)N(R 410z ) 2 , -OC(O)N(R 410z ) 2 , -N(R 410z ) C(O)OR 410z , -S(O)R 410z , -S(O) 2 R 410z , -NO 2 , =O, =S, =N(R 410z ), -N 3 ,-CN,C 3~10 The carbon ring is optionally substituted with one or more substituents independently selected from a carbon ring and a 3-membered to 10-membered heterocycle, where the C 3~10 Carbon rings and 3- to 10-membered heterocycles have one or more R 49z Those which are replaced as needed; and C 3~10 Carbon rings and 3- to 10-membered heterorings, each of which is a halogen, -OR 410z , -SR 410z , -N(R 410z ) 2 , -C(O)R 410z , -C(O)N(R 410z ) 2 , -N(R 410z ) C(O)R 410z , -N(R 410z ) C(O)N(R 410z ) 2 , -OC(O)N(R 410z ) 2 , -N(R 410z ) C(O)OR 410z , -C(O)OR 410z , -OC(O)R 410z , -S(O)R 410z , -S(O) 2 R 410z , -NO 2 , =O, =S, =N(R 410z ), -N 3 ,-CN,C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 It is optionally substituted with one or more substituents independently selected from the alkynyl, where C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl has one or more R 49z Each is replaced as needed. Selected from; R 4C teeth: hydrogen; -C(O)R 410c , -C(O)N(R 410c ) 2 , -C(O)OR 410c , and -CN; C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkynnyl, each of which is a halogen, -OR 410c , -SR 410c , -N(R 410c ) 2 , -C(O)R 410c , -C(O)N(R 410c ) 2 , -N(R 410c ) C(O)R 410c , -C(O)OR 410c , -OC(O)R 410c , -N(R 410c ) C(O)N(R 410c ) 2 , -OC(O)N(R 410c ) 2 , -N(R 410c ) C(O)OR 410c , -S(O)R 410c , -S(O) 2 R 410c , -NO 2 , =O, =S, =N(R 410c ), -N 3 ,-CN,C 3~10 The carbon ring is optionally substituted with one or more substituents independently selected from a carbon ring and a 3-membered to 10-membered heterocycle, where the C 3~10 Carbon rings and 3- to 10-membered heterocycles have one or more R 49c Those which are replaced as needed; and C 3~10 Carbon rings and 3- to 10-membered heterorings, each of which is a halogen, -OR 410c , -SR 410c , -N(R 410c ) 2 , -C(O)R 410c , -C(O)N(R 410c ) 2 , -N(R 410c ) C(O)R 410c , -N(R 410c ) C(O)N(R 410c ) 2 , -OC(O)N(R 410c ) 2 , -N(R 410c ) C(O)OR 410c , -C(O)OR 410c , -OC(O)R 410c , -S(O)R 410c , -S(O) 2 R 410c , -NO 2 , =O, =S, =N(R 410c ), -N 3 ,-CN,C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 It is optionally substituted with one or more substituents independently selected from the alkynyl, where C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl has one or more R 49c Each is replaced as needed. Selected from; R 45 teeth: hydrogen; ハロゲン、-OR 410d 、-SR 410d 、-N(R 410d ) 2 、-C(O)R 410d 、-C(O)N(R 410d ) 2 、-N(R 410d )C(O)R 410d 、-C(O)OR 410d 、-OC(O)R 410d 、-N(R 410d )C(O)N(R 410d ) 2 、-OC(O)N(R 410d ) 2 、-N(R 410d )C(O)OR 410d 、-S(O)R 410d 、-S(O) 2 R 410d 、-NO 2 、-N 3 、および-CN; C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkynnyl, each of which is a halogen, -OR 410d , -SR 410d , -N(R 410d ) 2 , -C(O)R 410d , -C(O)N(R 410d ) 2 , -N(R 410d ) C(O)R 410d , -C(O)OR 410d , -OC(O)R 410d , -N(R 410d ) C(O)N(R 410d ) 2 , -OC(O)N(R 410d ) 2 , -N(R 410d ) C(O)OR 410d , -S(O)R 410d , -S(O) 2 R 410d , -NO 2 , =O, =S, =N(R 410d ), -N 3 ,-CN,C 3~10 The carbon ring is optionally substituted with one or more substituents independently selected from a carbon ring and a 3-membered to 10-membered heterocycle, where the C 3~10 Carbon rings and 3- to 10-membered heterocycles have one or more R 49d Those which are replaced as needed; and C 3~10 Carbon rings and 3- to 10-membered heterorings, each of which is a halogen, -OR 410d , -SR 410d , -N(R 410d ) 2 , -C(O)R 410d , -C(O)N(R 410d ) 2 , -N(R 410d ) C(O)R 410d , -N(R 410d ) C(O)N(R 410d ) 2 , -OC(O)N(R 410d ) 2 , -N(R 410d ) C(O)OR 410d , -C(O)OR 410d , -OC(O)R 410d , -S(O)R 410d , -S(O) 2 R 410d , -NO 2 , =O, =S, =N(R 410d ), -N 3 ,-CN,C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 It is optionally substituted with one or more substituents independently selected from the alkynyl, where C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl has one or more R 49d Each is replaced as needed. Selected from; or R 45 is R 46 Together with it, a 3-membered to 10-membered hetero ring or C 3~10 A carbon ring is formed, where the 3-membered to 10-membered heterocycle or C 3~10 A carbon ring has one or more R 49d It is replaced as needed; R 46 teeth: hydrogen; ハロゲン、-OR 410e 、-SR 410e 、-N(R 410e ) 2 、-C(O)R 410e 、-C(O)N(R 410e ) 2 、-N(R 410e )C(O)R 410e 、-C(O)OR 410e 、-OC(O)R 410e 、-N(R 410e )C(O)N(R 410e ) 2 、-OC(O)N(R 410e ) 2 、-N(R 410e )C(O)OR 410e 、-S(O)R 410e 、-S(O) 2 R 410e 、-NO 2 、-N 3 、および-CN; C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkynnyl, each of which is a halogen, -OR 410e , -SR 410e , -N(R 410e ) 2 , -C(O)R 410e , -C(O)N(R 410e ) 2 , -N(R 410e ) C(O)R 410e , -C(O)OR 410e , -OC(O)R 410e , -N(R 410e ) C(O)N(R 410e ) 2 , -OC(O)N(R 410e ) 2 , -N(R 410e ) C(O)OR 410e , -S(O)R 410e , -S(O) 2 R 410e , -NO 2 , =O, =S, =N(R 410e ), -N 3 ,-CN,C 3~10 The carbon ring is optionally substituted with one or more substituents independently selected from a carbon ring and a 3-membered to 10-membered heterocycle, where the C 3~10 Carbon rings and 3- to 10-membered heterocycles have one or more R 49e Those which are replaced as needed; and C 3~10 Carbon rings and 3- to 10-membered heterorings, each of which is a halogen, -OR 410e , -SR 410e , -N(R 410e ) 2 , -C(O)R 410e , -C(O)N(R 410e ) 2 , -N(R 410e ) C(O)R 410e , -N(R 410e ) C(O)N(R 410e ) 2 , -OC(O)N(R 410e ) 2 , -N(R 410e ) C(O)OR 410e , -C(O)OR 410e , -OC(O)R 410e , -S(O)R 410e , -S(O) 2 R 410e , -NO 2 , =O, =S, =N(R 410e ), -N 3 ,-CN,C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 It is optionally substituted with one or more substituents independently selected from the alkynyl, where C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl has one or more R 49e Each is replaced as needed. Selected from; R 47 teeth: hydrogen; -C(O)R 410f , -C(O)N(R 410f ) 2 , -C(O)OR 410f , -S(O)R 410f , and -S(O) 2 R 410f ; Halogen, -OR 410f , -SR 410f , -N(R 410f ) 2 , -C(O)R 410f , -C(O)N(R 410f ) 2 , -N(R 410f ) C(O)R 410f , -C(O)OR 410f , -OC(O)R 410f , -N(R 410f ) C(O)N(R 410f ) 2 , -OC(O)N(R 410f ) 2 , -N(R 410f ) C(O)OR 410f , -S(O)R 410f , -S(O) 2 R 410f , -NO 2 , =O, =S, =N(R 410f ), -N 3 ,-CN,C 3~10 C is optionally substituted with one or more substituents independently selected from carbocyclic and 3- to 10-membered heterocycles. 1~6 Alkyl, where C 3~10 Carbon rings and 3- to 10-membered heterocycles have one or more R 49f Those which are replaced as needed; and C 3~10 Carbon rings and 3- to 10-membered heterorings, each of which is a halogen, -OR 410f , -SR 410f , -N(R 410f ) 2 , -C(O)R 410f , -C(O)N(R 410f ) 2 , -N(R 410f ) C(O)R 410f , -N(R 410f ) C(O)N(R 410f ) 2 , -OC(O)N(R 410f ) 2 , -N(R 410f ) C(O)OR 410f , -C(O)OR 410f , -OC(O)R 410f , -S(O)R 410f , -S(O) 2 R 410f , -NO 2 , =O, =S, =N(R 410f ), -N 3 ,-CN,C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 It is optionally substituted with one or more substituents independently selected from the alkynyl, where C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl has one or more R 49f Each is replaced as needed. Selected from; Each R 47e Independently: Halogen, -OR 410y , -SR 410y , -N(R 410y ) 2 , -C(O)R 410y , -C(O)N(R 410y ) 2 , -N(R 410y ) C(O)R 410y , -N(R 410y ) C(O)N(R 410y ) 2 , -OC(O)N(R 410y ) 2 , -N(R 410y ) C(O)OR 410y , -C(O)OR 410y , -OC(O)R 410y , -S(O)R 410y , -S(O) 2 R 410y , -NO 2 , =O, =S, =N(R 410y ), and -CN; and C 1~3 Alkyl, C 2~3 Alkenyl and C 2~3 Alkynnyl, each of which is a halogen, -OR 410y , -SR 410y , -N(R 410y ) 2 , -C(O)R 410y , -C(O)N(R 410y ) 2 , -N(R 410y ) C(O)R 410y , -N(R 410y ) C(O)N(R 410y ) 2 , -OC(O)N(R 410y ) 2 , -N(R 410y ) C(O)OR 410y , -C(O)OR 410y , -OC(O)R 410y , -S(O)R 410y , -S(O) 2 R 410y , -NO 2 , =O, =S, =N(R 410y ), and as needed, substituted with one or more substituents independently selected from -CN. Selected from; R 48 teeth: hydrogen; -C(O)R 410g , -C(O)N(R 410g ) 2 , -C(O)OR 410g , -S(O)R 410g , and -S(O) 2 R 410g ; Halogen, -OR 410g , -SR 410g , -N(R 410g ) 2 , -C(O)R 410g , -C(O)N(R 410g ) 2 , -N(R 410g ) C(O)R 410g , -C(O)OR 410g , -OC(O)R 410g , -N(R 410g ) C(O)N(R 410g ) 2 , -OC(O)N(R 410g ) 2 , -N(R 410g ) C(O)OR 410g , -S(O)R 410g , -S(O) 2 R 410g , -NO 2 , =O, =S, =N(R 410g ), -N 3 ,-CN,C 3~10 C is optionally substituted with one or more substituents independently selected from carbocyclic and 3- to 10-membered heterocycles. 1~6 Alkyl, where C 3~10 Carbon rings and 3- to 10-membered heterocycles have one or more R 49g Those which are replaced as needed; and C 3~10 Carbon rings and 3- to 10-membered heterorings, each of which is a halogen, -OR 410g , -SR 410g , -N(R 410g ) 2 , -C(O)R 410g , -C(O)N(R 410g ) 2 , -N(R 410g ) C(O)R 410g , -N(R 410g ) C(O)N(R 410g ) 2 , -OC(O)N(R 410g ) 2 , -N(R 410g ) C(O)OR 410g , -C(O)OR 410g , -OC(O)R 410g , -S(O)R 410g , -S(O) 2 R 410g , -NO 2 , =O, =S, =N(R 410g ), -N 3 ,-CN,C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 It is optionally substituted with one or more substituents independently selected from the alkynyl, where C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl has one or more R 49g Each is replaced as needed. Selected from; Each R 49a Independently: Halogen, -OR 410a , -SR 410a , -N(R 410a ) 2 , -C(O)R 410a , -C(O)N(R 410a ) 2 , -N(R 410a ) C(O)R 410a , -N(R 410a ) C(O)N(R 410a ) 2 , -OC(O)N(R 410a ) 2 , -N(R 410a ) C(O)OR 410a , -C(O)OR 410a , -OC(O)R 410a , -S(O)R 410a , -S(O) 2 R 410a , -NO 2 , =O, =S, =N(R 410a ), -N 3 , and -CN; and C 1~3 Alkyl, C 2~3 Alkenyl and C 2~3 Alkynnyl, each of which is a halogen, -OR 410a , -SR 410a , -N(R 410a ) 2 , -C(O)R 410a , -C(O)N(R 410a ) 2 , -N(R 410a ) C(O)R 410a , -N(R 410a ) C(O)N(R 410a ) 2 , -OC(O)N(R 410a ) 2 , -N(R 410a ) C(O)OR 410a , -C(O)OR 410a , -OC(O)R 410a , -S(O)R 410a , -S(O) 2 R 410a , -NO 2 , =O, =S, =N(R 410a ), -N 3 , and which are optionally substituted with one or more substituents independently selected from -CN. Selected from; Each R 49z Independently: Halogen, -OR 410z , -SR 410z , -N(R 410z ) 2 , -C(O)R 410z , -C(O)N(R 410z ) 2 , -N(R 410z ) C(O)R 410z , -N(R 410z ) C(O)N(R 410z ) 2 , -OC(O)N(R 410z ) 2 , -N(R 410z ) C(O)OR 410z , -C(O)OR 410z , -OC(O)R 410z , -S(O)R 410z , -S(O) 2 R 410z , -NO 2 , =O, =S, =N(R 410z ), -N 3 , and -CN; and C 1~3 Alkyl, C 2~3 Alkenyl and C 2~3 Alkynnyl, each of which is a halogen, -OR 410z , -SR 410z , -N(R 410z ) 2 , -C(O)R 410z , -C(O)N(R 410z ) 2 , -N(R 410z ) C(O)R 410z , -N(R 410z ) C(O)N(R 410z ) 2 , -OC(O)N(R 410z ) 2 , -N(R 410z ) C(O)OR 410z , -C(O)OR 410z , -OC(O)R 410z , -S(O)R 410z , -S(O) 2 R 410z , -NO 2 , =O, =S, =N(R 410z ), -N 3 , and which are optionally substituted with one or more substituents independently selected from -CN. Selected from; Each R 49c Independently: Halogen, -OR 410c , -SR 410c , -N(R 410c ) 2 , -C(O)R 410c , -C(O)N(R 410c ) 2 , -N(R 410c ) C(O)R 410c , -N(R 410c ) C(O)N(R 410c ) 2 , -OC(O)N(R 410c ) 2 , -N(R 410c ) C(O)OR 410c , -C(O)OR 410c , -OC(O)R 410c , -S(O)R 410c , -S(O) 2 R 410c , -NO 2 , =O, =S, =N(R 410c ), -N 3 , and -CN; and C 1~3 Alkyl, C 2~3 Alkenyl and C 2~3 Alkynnyl, each of which is a halogen, -OR 410c , -SR 410c , -N(R 410c ) 2 , -C(O)R 410c , -C(O)N(R 410c ) 2 , -N(R 410c ) C(O)R 410c , -N(R 410c ) C(O)N(R 410c ) 2 , -OC(O)N(R 410c ) 2 , -N(R 410c ) C(O)OR 410c , -C(O)OR 410c , -OC(O)R 410c , -S(O)R 410c , -S(O) 2 R 410c , -NO 2 , =O, =S, =N(R 410c ), -N 3 , and which are optionally substituted with one or more substituents independently selected from -CN. Selected from; Each R 49d Independently: Halogen, -OR 410d , -SR 410d , -N(R 410d ) 2 , -C(O)R 410d , -C(O)N(R 410d ) 2 , -N(R 410d ) C(O)R 410d , -N(R 410d ) C(O)N(R 410d ) 2 , -OC(O)N(R 410d ) 2 , -N(R 410d ) C(O)OR 410d , -C(O)OR 410d , -OC(O)R 410d , -S(O)R 410d , -S(O) 2 R 410d , -NO 2 , =O, =S, =N(R 410d ), -N 3 , and -CN; and C 1~3 Alkyl, C 2~3 Alkenyl and C 2~3 Alkynnyl, each of which is a halogen, -OR 410d , -SR 410d , -N(R 410d ) 2 , -C(O)R 410d , -C(O)N(R 410d ) 2 , -N(R 410d ) C(O)R 410d , -N(R 410d ) C(O)N(R 410d ) 2 , -OC(O)N(R 410d ) 2 , -N(R 410d ) C(O)OR 410d , -C(O)OR 410d , -OC(O)R 410d , -S(O)R 410d , -S(O) 2 R 410d , -NO 2 , =O, =S, =N(R 410d ), -N 3 , and which are optionally substituted with one or more substituents independently selected from -CN. Selected from; Each R 49e Independently: Halogen, -OR 410e , -SR 410e , -N(R 410e ) 2 , -C(O)R 410e , -C(O)N(R 410e ) 2 , -N(R 410e ) C(O)R 410e , -N(R 410e ) C(O)N(R 410e ) 2 , -OC(O)N(R 410e ) 2 , -N(R 410e ) C(O)OR 410e , -C(O)OR 410e , -OC(O)R 410e , -S(O)R 410e , -S(O) 2 R 410e , -NO 2 , =O, =S, =N(R 410e ), -N 3 , and -CN; and C 1~3 Alkyl, C 2~3 Alkenyl and C 2~3 Alkynnyl, each of which is a halogen, -OR 410e , -SR 410e , -N(R 410e ) 2 , -C(O)R 410e , -C(O)N(R 410e ) 2 , -N(R 410e ) C(O)R 410e , -N(R 410e ) C(O)N(R 410e ) 2 , -OC(O)N(R 410e ) 2 , -N(R 410e ) C(O)OR 410e , -C(O)OR 410e , -OC(O)R 410e , -S(O)R 410e , -S(O) 2 R 410e , -NO 2 , =O, =S, =N(R 410e ), -N 3 , and which are optionally substituted with one or more substituents independently selected from -CN. Selected from; Each R 49f Independently: Halogen, -OR 410f , -SR 410f , -N(R 410f ) 2 , -C(O)R 410f , -C(O)N(R 410f ) 2 , -N(R 410f ) C(O)R 410f , -N(R 410f ) C(O)N(R 410f ) 2 , -OC(O)N(R 410f ) 2 , -N(R 410f ) C(O)OR 410f , -C(O)OR 410f , -OC(O)R 410f , -S(O)R 410f , -S(O) 2 R 410f , -NO 2 , =O, =S, =N(R 410f ), -N 3 , and -CN; and C 1~3 Alkyl, C 2~3 Alkenyl and C 2~3 Alkynnyl, each of which is a halogen, -OR 410f , -SR 410f , -N(R 410f ) 2 , -C(O)R 410f , -C(O)N(R 410f ) 2 , -N(R 410f ) C(O)R 410f , -N(R 410f ) C(O)N(R 410f ) 2 , -OC(O)N(R 410f ) 2 , -N(R 410f ) C(O)OR 410f , -C(O)OR 410f , -OC(O)R 410f , -S(O)R 410f , -S(O) 2 R 410f , -NO 2 , =O, =S, =N(R 410f ), -N 3 , and which are optionally substituted with one or more substituents independently selected from -CN. Selected from; Each R 49g Independently: Halogen, -OR 410g , -SR 410g , -N(R 410g ) 2 , -C(O)R 410g , -C(O)N(R 410g ) 2 , -N(R 410g ) C(O)R 410g , -N(R 410g ) C(O)N(R 410g ) 2 , -OC(O)N(R 410g ) 2 , -N(R 410g ) C(O)OR 410g , -C(O)OR 410g , -OC(O)R 410g , -S(O)R 410g , -S(O) 2 R 410g , -NO 2 , =O, =S, =N(R 410g ), -N 3 , and -CN; and C 1~3 Alkyl, C 2~3 Alkenyl and C 2~3 Alkynnyl, each of which is a halogen, -OR 410g , -SR 410g , -N(R 410g ) 2 , -C(O)R 410g , -C(O)N(R 410g ) 2 , -N(R 410g ) C(O)R 410g , -N(R 410g ) C(O)N(R 410g ) 2 , -OC(O)N(R 410g ) 2 , -N(R 410g ) C(O)OR 410g , -C(O)OR 410g , -OC(O)R 410g , -S(O)R 410g , -S(O) 2 R 410g , -NO 2 , =O, =S, =N(R 410g ), -N 3 , and which are optionally substituted with one or more substituents independently selected from -CN. Selected from; and Each R 410a , R 410b , R 410c , R 410d , R 410e , R 410f , R 410g , R 410x , R 410y and R 410z Independently: hydrogen; C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkynnyl, each of which is a halogen, -CN, -OH, -SH, -NO 2 , -NH 2 , =O, =S, -OC 1~6 Alkyl, -S-C 1~6 Alkyl, -N(C) 1~6 Alkyl) 2 ,-NH(C 1~6 Alkyl), C 3~10 Carbocyclic rings, or those optionally substituted with one or more substituents independently selected from 3-membered to 10-membered heterocycles; and C 3~10 Carbon rings and 3- to 10-membered heterocycles, each of which is a halogen, -CN, -OH, -SH, -NO 2 , -NH 2 , =O, =S, -OC 1~6 Alkyl, -S-C 1~6 Alkyl, -N(C) 1~6 Alkyl) 2 ,-NH(C 1~6 Alkyl), C 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 3~10 Carbon rings, 3-membered to 10-membered heterocycles, and C 1~6 Substituted as needed with one or more substituents independently selected from the haloalkyl group. Selected from, A compound or its salt.
60. X 41 The compound or salt according to claim 59, wherein is N.
61. X 42 A compound or salt according to any one of claims 59 to 60, wherein is N.
62. X 41 is C(R 41a ) and; X 42 is C(R 41b ) and; X 43 is C(R 41c ) and; X 44 is C(R 41d ) The compound or salt according to claim 59.
63. R 41a , R 41b , R 41c , and R 41d Each is independent of the others: Hydrogen, halogen, -N 3 , -CN, -OR 410a , -SR 410a , -N(R 410a ), 2 , -C(O)R 410a , -C(O)N(R 410a ), 2 , -N(R 410a ),C(O)R 410a , -N(R 410a ),C(O)N(R 410a ), 2 , -C(O)OR 410a ; C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkynnyl, each of which is a halogen, -OR 410a , -SR 410a , -N(R 410a ) 2 , =O, =S, =N(R 410a Substituted as necessary with one or more substituents independently selected from ); C 3~10 A carbon ring and a 3-membered to 10-membered heterocycle, each of which is -F, -Cl, -CN, -OH, -C(O)NH 2 , and C 1~6 Substituted as needed with one or more substituents independently selected from the alkyl group. Selected from, The compound or salt according to any one of claims 59 to 62.
64. R 41a , R 41b , R 41c , and R 41d Each of these independently is: hydrogen, -F, -Cl, -Br, -I, -CN, -N 3 , -OH, -OMe, -OEt, 【Chemistry 291】 -CF 3 -methyl, -ethyl, cyclopropyl, -CH 2 N(CH 3 ) 2 A compound or salt according to any one of claims 59 to 62, selected from -CCMe, -CCH, phenyl, N-morpholinyl, and N-pyrrolidinyl.
65. R 41a , R 41b , R 41c , and R 41d The compound or salt according to any one of claims 59 to 64, wherein each of the following is independently selected from: hydrogen, -F, -Cl, -OH, and -CN.
66. Each R 410a , R 410b , R 410c , R 410d , R 410e , R 410f , R 410g , R 410x , R 410y , and R 410z The following are independently: hydrogen, methyl, ethyl, propyl, isopropyl, cyclopropyl, isobutyl, -CF 3 ien-CH 2 CF 3 ien-CH 2 CHF 2 ien-CH 2 C(F)(Me) 2 , and -CH 2 - A compound or salt according to any one of claims 59 to 65, selected from phenyl.
67. Two R's 410a Together, C 3~10 A compound or salt according to any one of claims 59 to 65, which forms a carbon ring or a 3- to 10-membered heterocycle.
68. R 4Z : Methyl, ethyl, propyl, isopropyl, cyclopropyl, isobutyl, -CF 3 ien-CH 2 CF 3 ien-CH 2 CHF 2 ien-CH 2 C(F)(Me) 2 , and -CH 2 - A compound or salt according to any one of claims 59 to 67, selected from phenyl.
69. R 4Z However, methyl, -CH 2 OH, -CH 2 CH 2 OH, C(Me) 2 OH, or -CH 2 A compound or salt according to any one of claims 59 to 67, wherein the compound is OMe.
70. R 4Z A compound or salt according to any one of claims 59 to 69, wherein is methyl.
71. R 4C A compound or salt according to any one of claims 59 to 70, wherein is hydrogen.
72. R J However, halogen, -OR 410b , -SR 410b , -N(R 410b ) 2 , -C(O)R 410b , -C(O)N(R 410b ) 2 , -N(R 410b ) C(O)R 410b , -N(R 410b ) C(O)N(R 410b ) 2 , -OC(O)N(R 410b ) 2 , -N(R 410b ) C(O)OR 410b , -C(O)OR 410b , -OC(O)R 410b , -S(O)R 410b , -S(O) 2 R 410b , -NO 2 , =O, =S, =N(R 410b ), -N 3 ,-CN,C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 A 5- to 10-membered heteroaryl, optionally substituted with one or more substituents independently selected from the alkynyl, where C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl has one or more R 49a The compound or salt according to any one of claims 59 to 71, wherein each is substituted as necessary.
73. R J However, halogen, -OR 410b , -SR 410b , -N(R 410b ) 2 , -C(O)R 410b , -C(O)N(R 410b ) 2 , -N(R 410b ) C(O)R 410b , -N(R 410b ) C(O)N(R 410b ) 2 , -OC(O)N(R 410b ) 2 , -N(R 410b ) C(O)OR 410b , -C(O)OR 410b , -OC(O)R 410b , -S(O)R 410b , -S(O) 2 R 410b , -NO 2 , =O, =S, =N(R 410b ), -N 3 ,-CN,C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 A five-membered heteroaryl substituted as needed with one or more substituents independently selected from the alkynyl, where C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl has one or more R 49a The compound or salt according to any one of claims 59 to 72, wherein each is substituted as necessary.
74. R J However, halogen, -OR 410b , -N(R 410b ) 2 , -C(O)R 410b , -C(O)N(R 410b ) 2 , -N(R 410b ) C(O)R 410b , -OC(O)N(R 410b ) 2 , -C(O)OR 410b , -OC(O)R 410b , =O, =S, =N(R 410b ), -CN, C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Thiophenes, thiazoles, thiadiazoles, furans, isoxazoles, oxazoles, oxadiazoles, pyrroles, pyrazoles, imidazoles, or triazoles, which are optionally substituted with one or more substituents independently selected from alkynyl, where C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl has one or more R 49a The compound or salt according to any one of claims 59 to 73, wherein each is substituted as necessary.
75. R J However, halogen, -OR 410b , -N(R 410b ) 2 , -C(O)R 410b , -C(O)N(R 410b ) 2 , -N(R 410b ) C(O)R 410b , -OC(O)N(R 410b ) 2 , -C(O)OR 410b , -OC(O)R 410b , =O, =S, =N(R 410b ), -CN, C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 A thiophene, thiazole, or oxazole optionally substituted with one or more substituents independently selected from the alkynyl, where C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl has one or more R 49a The compound or salt according to any one of claims 59 to 74, wherein each is substituted as necessary.
76. R 47 A compound or salt according to any one of claims 59 to 75, wherein is hydrogen.
77. R 43 ga: Hydrogen, -F, -Cl, -OH, -NHMe, -CN, C 1~3 Selected from alkyl and cyclopropyl, where C 1~3 The compound or salt according to any one of claims 59 to 76, wherein the alkyl and cyclopropyl groups are each optionally substituted with one or more -F groups.
78. R 43 ga: hydrogen, -CH 3 , cyclopropyl, -F, -Cl, -CN, and CF 3 A compound or salt according to any one of claims 59 to 77, selected from the above.
79. R 43 ga: hydrogen, and CH 3 A compound or salt according to any one of claims 59 to 78, selected from the above.
80. R 48 a: A compound or salt according to any one of claims 59 to 79, selected from hydrogen and methyl.
81. R 48 a: A compound or salt according to any one of claims 59 to 80, selected from hydrogen.
82. R 45 but: Hydrogen, halogens, and halogens, -OR 410d , and -CN, C 3~10 A carbon ring and a carbon ring, optionally substituted with one or more substituents independently selected from 3-membered to 10-membered heterocycles. 1~6 Selected from alkyl, where C 3~10 Carbon rings and 3- to 10-membered heterocycles have one or more R 49d Each is replaced as needed; R 46 but: Hydrogen, halogens, and halogens, -OR 410d , and -CN, C 3~10 A carbon ring and a carbon ring, optionally substituted with one or more substituents independently selected from 3-membered to 10-membered heterocycles. 1~6 Selected from alkyl, where C 3~10 Carbon rings and 3- to 10-membered heterocycles have one or more R 49d And each is replaced as needed; Or R 45 R 46 Together with it, a 3-membered to 10-membered hetero ring or C 3~10 A carbon ring is formed, where the 3-membered to 10-membered heterocycle or C 3~10 A carbon ring has one or more R 49d It is replaced as needed. The compound or salt according to any one of claims 59 to 81. 【Request Item 83】 【Chemistry 292】 but: 【Chemistry 293】 A compound or salt according to any one of claims 59 to 82, selected from the above.
84. 1、2、3、4、5、6、7、8、9、10、11、12、13、14、15、16、17、18、19、20、21、22、23、24、25、26、27、28、29、30、31、32、33、34、35、36、37、38、39、40、41、42、43、44、45、46、47、48、49、50、51、52、53、54、55、56、57、58、59、60、61、62、63、64、65、66、67、68、69、70、71、72、73、74、75、76、77、78、79、80、81、82、83、84、85、86、87、88、89、90、91、92、93、94、95、96、97、98、99、100、101、102、103、104、105、106、107、108、109、110、111、112、113、114、115、116、117、118、119、120、121、122、123、124、125、126、127、128、129、130、131、132、133、134、135、136、137、1038、1039、1040、1041、1042、1043、1044、1045、1046、1047、1048、1049、1050、1051、1052、1053、1054、1055、1056、1057、1058、1059、1060、1061、1062、1063、1064、1065、1066、1067、1068、1069、1070、1071、1072、1073、1074、1075、1076、1077、1078、1079、1080、1081、1082、1083、1084、1085、1086、1087、1088、1089、1090、1091、1092、1093、1094、1095、1096、1097、1098、1099、1100、1101、1102、1103、1104、1105、1106、1107、1108、1109、1110、1111、1112、1113、1114、1115、1116、1117、1118、1119、1120、1121、1122、1123、1124、1125、1126、1127、1128、1129、1130、1131、1132、1133、1134、1135、1136、1137、1138、1139、1140、1141、1142、1143、1144、1145、1146、1147、1148、1149、1150、1151、1152、1153、2001、2002、2009、2010、2011、2012、2013、2014、2015、2016、2017、2018、2019、2020、2021、2022、2023、2024、2025、2026、2027、2028、2029、2030、2033、2034、2035、2036、2037、2038、2039、2040、2041、2042、2043、2044、2045、2046、2047、2048、2049、2050、2051、2052、2053、2054、2055、2056、2057、2058、2059、2060、2061、2062、2063、2064、2065、2066、2067、2068、2069、2070、2071、2072、2073、2074、2075、2076、2077、2078、2079、1153、2501、2502、2503、2504、2505、2506、2507、2508、2509、2510、2511、2512、2513、2514、2515、2516、2517、2518、2519、2520、2521、2522、2523、2524、2527、2528、2529、2530、2531、2532、2533、2534、2535、2536、2537、2538、2539、2540、2541、2542、2543、2544、2545、2546、2547、2548、2549、2550、2551、2552、2553、2554、2555、2556、2557、2558、2559、2560、2561、2562、2563、2564、2565、2566、2567、2568、2569、2570、2571、2572、2573、2574、2575、2576、2577、2578、2579、2580、2581、2582、2583、2584、2585、2586、2587、2588、2590、2591、2592、2593、2594、2595、2596、2597、2598、2599、2600、2601、2602、2603、2604、2605、2606、2607、2608、4502、4503、4504、4505、138、139、140、141、142、143、144、145、146、147、148、149、150、151、152、153、154、155、156、157、158、159、160、161、162、163、164、165、166、167、168、169、170、171、172、173、174、175、176、177、178、179、180、181、182、183、184、185、186、187、188、189、190、191、192、193、194、195、196、197、198、199、200、201、202、203、204、205、206、207、208、209、210、211、212、213、214、215、216、217、218、219、220、221、222、223、224、225、226、227、228、229、230、231、232、233、234、235、236、237、238、239、240、241、242、243、244、245、246、247、248、249、250、251、252、253、254、255、256、257、258、259、260、261、262、263、264、265、266、267、268、269、270、271、272、273、274、275、276、277、278、279、280、281、282、283、284、285、286、287、288、289、290、291、292、293、294、295、296、297、298、299、300、301、302、303、304、305、306、307、308、309、310、311、312、313、314、315、316、317、318、319、320、321、322、323、324、325、326、327、328、329、330、331、332、333、334、335、336、337、338、339、340、341、342、343、344、345、346、347、348、349、350、351、352、353、354、355、356、357、358、359、360、361、362、363、364、365、366、367、368、369、370、371、372、373、374、375、376、377、378、379、380、381、382、383、384、385、386、387、388、389、390、391、392、393、394、395、396、397、398、399、400、401、402、403、404、405、406、407、408、409、410、411、412、413、414、415、416、417、418、419、420、421、422、423、424、425、426、427、428、429、430、431、432、433、434、435、436、437、438、439、440、441、442、443、444、445、446、447、448、449、450、451、452、453、454、455、456、457、458、459、460、461、462、463、464、465、466、467、468、469、470、471、472、473、474、475、476、477、478、479、480、481、482、483、484、485、486、487、488、489、490、491、492、493、494、495、496、497、498、499、500、501、3001、3002、3003、3004、3005、3006、3007、3008、3009、3010、3011、3012、3013、3502、3503、3504、3505、3506、3507、3508、3509、3510、3511、3512、3513、3514、3515、3516、3517、3518、3519、4001、4002、4003、4004、4005、4006、4007、4008、4009、4010、7001、7002、7003、7004、7005、7006、7007、7008、7009、7010、7011、7012、7013、7014、7015、7016、7017、7018、7019、7020、7021、7022、7023、7024、7025、7026、7027、7028、7029、7030、7031、7032、7033、7034、7035、7036、7037、7038、7039、7040、7041、7042、7043、7044、7045、7046、7047、7048、7049、7050、7051、7052、7053、7054、7055、7056、7057、7058、7059、7060、7061、7062、7063、7064、7065、7066、7067、7068、7069、7070、7071、7072、7073、7074、7075、7076、7077、7078、7079、7080、7081、7082、7083、7084, 7085, 7086, 7087, 7088, 7089, 7090, 7091, 7092, 7093, 7094, 4801, 4802, 4803, 4804, 4805, 4806, 4807, 4808, 4809, 4810, 4811, 4812, 4813, 4814, 4815, 4816, 4817, 4818, 4819, 4820, 4821, 4822, 4823, 4 A compound selected from the group consisting of 824, 4825, 4826, 4827, 4828, 4829, 4830, 4831, 4832, 4833, 4834, 4835, 4836, 4837, 4838, 4839, 4840, 4841, 4842, 4843, 4844, 4845, 4846, 4847, 4848, 4849, 4850, 3520, 3521, 3522, and 3523.
85. A method for treating a cardiovascular disease or related condition, comprising the step of administering a compound or salt according to any one of claims 1 to 84 to a subject in need thereof.
86. A method for treating a diastolic dysfunction or related condition, comprising the step of administering a compound or salt according to any one of claims 1 to 84 to a subject in need thereof.
87. Hypertrophic cardiomyopathy (HCM); Heart failure with preserved ejection fraction (HFpEF); Heart failure with mildly reduced ejection fraction Disorders of relaxation; Impaired ventricular stiffness (diabetic HFpEF); Dilated cardiomyopathy (DCM); Ischemic cardiomyopathy; Heart transplant allograft vascular disease; Restrictive cardiomyopathy; Heart valve disease (e.g., aortic stenosis – including post-AVR / TAVR and congenital forms in the elderly); Left ventricular (LV) hypertrophy; Right ventricular (RV) hypertrophy; Acute myocardial infarction; acute vascular regeneration; ischemia; and Anguina; A method for treating a condition selected from, the method comprising the step of administering a compound or salt according to any one of claims 1 to 84 to a subject in need of such treatment.
88. The method according to claim 87, wherein the ejection fraction-preserved heart failure (HFpEF) comprises one or more disorders selected from impaired relaxation and impaired ventricular stiffness (diabetic HFpEF).
89. The method according to claim 87, wherein the left ventricular (LV) hypertrophy is malignant left ventricular (LV) hypertrophy.
90. The method according to claim 87, wherein the restrictive cardiomyopathy comprises one or more subgroups selected from the inflammatory subgroup, the infiltrative subgroup, the storage subgroup, the idiopathic / hereditary subgroup, and the congenital heart disease subgroup.
91. The method according to claim 90, wherein the inflammatory subgroup comprises one or more subgroups selected from refrel and EMF.
92. The method according to claim 90, wherein the inflammatory subgroup comprises one or more subgroups selected from amyloid, sarcoid, and XRT.
93. The method according to claim 90, wherein the storage subgroup comprises one or more subgroups selected from hemochromatosis, Fabri, and glycogen disease.
94. The method according to claim 90, wherein the idiopathic / hereditary subgroup comprises one or more subgroups selected from the subgroups related to Trop I (betamyosin HC), Trop T (alpha cardiac actin), and desmin.
95. The method according to claim 90, wherein the subgroup of congenital heart disease comprises one or more subgroups selected from pressure overload RV, Tetralogy of Fallot, and pulmonary valve stenosis.
96. A method for treating hypertrophic cardiomyopathy or a related condition, comprising the step of administering a compound or salt according to any one of claims 1 to 84 to a subject in need of such treatment.
97. A method for treating obstructive hypertrophic cardiomyopathy, comprising the step of administering a compound or salt according to any one of claims 1 to 84 to a subject in need of such treatment.
98. A method for treating non-obstructive hypertrophic cardiomyopathy, comprising the step of administering a compound or salt according to any one of claims 1 to 84 to a subject in need of such treatment.
99. A method for treating heart failure with preserved ejection fraction, comprising the step of administering a compound or salt according to any one of claims 1 to 84 to a subject in need of such treatment.
100. A method for treating left ventricular stiffness, comprising the step of administering a compound or salt according to any one of claims 1 to 84 to a subject in need of such treatment.
101. A pharmaceutical composition comprising a compound or salt according to any one of claims 1 to 84, and a pharmaceutically acceptable additive.
102. A method for treating heart disease in individuals in need, wherein the effective therapeutic dose is given by formula (III): 【Chemistry 294】 The process includes administering a compound or a salt thereof, in formula (III): X 1 , X 2 , X 3 , and X 4 These are independently selected from C(R) and N, where X 1 , X 2 , X 3 , and X 4 N is two or fewer of these; Each R is independent: Hydrogen, halogen, -NO 2 -CN, -N 3 , -OR 28 , -SR 28 , -N(R 28 ) 2 , -C(O)R 28 , -C(O)N(R 28 ) 2 , -N(R 28 ) C(O)R 28 , -N(R 28 ) C(O)N(R 28 ) 2 , -OC(O)N(R 28 ) 2 , -N(R 28 ) C(O)OR 28 , -C(O)OR 28 , -OC(O)R 28 , -S(O)R 28 , and -S(O) 2 R 28 ; C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkynnyl, each of which is a halogen, -OR 28 , -SR 28 , -N(R 28 ) 2 , -C(O)R 28 , -C(O)N(R 28 ) 2 , -N(R 28 ) C(O)R 28 , -C(O)OR 28 , -OC(O)R 28 , -N(R 28 ) C(O)N(R 28 ) 2 , -OC(O)N(R 28 ) 2 , -N(R 28 ) C(O)OR 28 , -S(O)R 28 , -S(O) 2 R 28 , -NO 2 , =O, =S, =N(R 28 ), -CN, C 3~10 The carbon ring is optionally substituted with one or more substituents independently selected from a carbon ring and a 3-membered to 10-membered heterocycle, where the C 3~10 Carbon rings and 3- to 10-membered heterocycles are R 27 Each of which is substituted as necessary with one or more substituents independently selected from; and C 3~10 Carbon rings and 3- to 10-membered heterorings, each of which is a halogen, -OR 28 , -SR 28 , -N(R 28 ) 2 , -C(O)R 28 , -C(O)N(R 28 ) 2 , -N(R 28 ) C(O)R 28 , -N(R 28 ) C(O)N(R 28 ) 2 , -OC(O)N(R 28 ) 2 , -N(R 28 ) C(O)OR 28 , -C(O)OR 28 , -OC(O)R 28 , -S(O)R 28 , -S(O) 2 R 28 , -NO 2 , =O-, =S, =N(R 28 ), -CN, C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 It is optionally substituted with one or more substituents independently selected from the alkynyl, where C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl is R 27 Each of which is substituted as needed by one or more substituents independently selected from the original. Selected from; R 21 teeth: Hydrogen, C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkynnyl, each of which is a halogen, -OR 28a , -SR 28a , -N(R 28a ) 2 , -C(O)R 28a , -C(O)N(R 28a ) 2 , -N(R 28a ) C(O)R 28a , -C(O)OR 28a , -OC(O)R 28a , -N(R 28a ) C(O)N(R 28a ) 2 , -OC(O)N(R 28a ) 2 , -N(R 28a ) C(O)OR 28a , -S(O)R 28a , -S(O) 2 R 28a , -NO 2 , =O, =S, =N(R 28a ), -CN, C 3~10 The carbon ring is optionally substituted with one or more substituents independently selected from 3-membered to 10-membered heterocycles, where the C 3~10 Carbon rings and 3- to 10-membered heterocycles are R 27a Each of which is substituted as necessary with one or more substituents independently selected from; and C 3~10 Carbon rings and 3- to 10-membered heterorings, each of which is a halogen, -OR 28a , -SR 28a , -N(R 28a ) 2 , -C(O)R 28a , -C(O)N(R 28a ) 2 , -N(R 28a ) C(O)R 28a , -N(R 28a ) C(O)N(R 28a ) 2 , -OC(O)N(R 28a ) 2 , -N(R 28a ) C(O)OR 28a , -C(O)OR 28a , -OC(O)R 28a , -S(O)R 28a , -S(O) 2 R 28a , -NO 2 , =O-, =S, =N(R 28a ), -CN, C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 It is optionally substituted with one or more substituents independently selected from the alkynyl, where C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl is R 27a Each of which is substituted as needed by one or more substituents independently selected from the original. Selected from; R 22 teeth: Hydrogen, C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkynnyl, each of which is a halogen, -OR 28b , -SR 28b , -C(O)R 28b , -C(O)N(R 28b ) 2 , -N(R 28b ) C(O)R 28b , -C(O)OR 28b , -OC(O)R 28b , -N(R 28b ) C(O)N(R 28b ) 2 , -OC(O)N(R 28b ) 2 , -N(R 28b ) C(O)OR 28b , -S(O)R 28b , -S(O) 2 R 28b , -NO 2 , =O, =S, =N(R 28b ), -CN, C 3~10 The carbon ring is optionally substituted with one or more substituents independently selected from 3-membered to 10-membered heterocycles, where the C 3~10 Carbon rings and 3- to 10-membered heterocycles are R 27b Each of which is substituted as necessary with one or more substituents independently selected from; and C 3~10 Carbon rings and 3- to 10-membered heterorings, each of which is a halogen, -OR 28b , -SR 28b , -N(R 28b ) 2 , -C(O)R 28b , -C(O)N(R 28b ) 2 , -N(R 28b ) C(O)R 28b , -N(R 28b ) C(O)N(R 28b ) 2 , -OC(O)N(R 28b ) 2 , -N(R 28b ) C(O)OR 28b , -C(O)OR 28b , -OC(O)R 28b , -S(O)R 28b , -S(O) 2 R 28b , -NO 2 , =O-, =S, =N(R 28b ), -CN, C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 It is optionally substituted with one or more substituents independently selected from the alkynyl, where C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl is R 27b Each of which is substituted as needed by one or more substituents independently selected from the original. Selected from; or R 21 is R 22 Together with C 3~10 They form a carbon ring, or a 3- to 10-membered heteroring, each of which is a halogen, -OR 28a , -SR 28a , -N(R 28a ) 2 , -C(O)R 28a , -C(O)N(R 28a ) 2 , -N(R 28a ) C(O)R 28a , -N(R 28a ) C(O)N(R 28a ) 2 , -OC(O)N(R 28a ) 2 , -N(R 28a ) C(O)OR 28a , -C(O)OR 28a , -OC(O)R 28a , -S(O)R 28a , -S(O) 2 R 28a , -NO 2 , =O-, =S, =N(R 28a ), -CN, C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 It is optionally substituted with one or more substituents independently selected from the alkynyl, where C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl is R 27b Each substituent is substituted as needed by one or more substituents selected independently of the original; R 23 teeth: Hydrogen, halogen, -OR 28c , -SR 28c , -N(R 28c ) 2 , -NO 2 , and -CN; and R 27c C as needed, substituted with one or more substituents independently selected from 1~6 Alkyl Selected from; or R 21 is R 23 Together with these, they form 3- to 10-membered heterocycles, which are halogens, -OR 28a , -SR 28a , -N(R 28a ) 2 , -C(O)R 28a , -C(O)N(R 28a ) 2 , -N(R 28a ) C(O)R 28a , -N(R 28a ) C(O)N(R 28a ) 2 , -OC(O)N(R 28a ) 2 , -N(R 28a ) C(O)OR 28a , -C(O)OR 28a , -OC(O)R 28a , -S(O)R 28a , -S(O) 2 R 28a , -NO 2 , =O-, =S, =N(R 28a ), -CN, C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 It is optionally substituted with one or more substituents independently selected from the alkynyl, where C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl is R 27c Each substituent is substituted as needed by one or more substituents selected independently of the other; or R 22 is R 23 Together with C 3~10 They form a carbon ring, or a 3- to 10-membered heteroring, each of which is a halogen, -OR 28a , -SR 28a , -N(R 28a ) 2 , -C(O)R 28a , -C(O)N(R 28a ) 2 , -N(R 28a ) C(O)R 28a , -N(R 28a ) C(O)N(R 28a ) 2 , -OC(O)N(R 28a ) 2 , -N(R 28a ) C(O)OR 28a , -C(O)OR 28a , -OC(O)R 28a , -S(O)R 28a , -S(O) 2 R 28a , -NO 2 , =O-, =S, =N(R 28a ), -CN, C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 It is optionally substituted with one or more substituents independently selected from the alkynyl, where C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl is R 27c Each substituent is substituted as needed by one or more substituents independently selected from the original; Or R 21 , R 22 , and R 23 Together they form a bicyclic heterocycle, which consists of halogens, -OR 28a , -SR 28a , -N(R 28a ) 2 , -C(O)R 28a , -C(O)N(R 28a ) 2 , -N(R 28a ) C(O)R 28a , -N(R 28a ) C(O)N(R 28a ) 2 , -OC(O)N(R 28a ) 2 , -N(R 28a ) C(O)OR 28a , -C(O)OR 28a , -OC(O)R 28a , -S(O)R 28a , -S(O) 2 R 28a , -NO 2 , =O-, =S, =N(R 28a ), -CN, C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 It is optionally substituted with one or more substituents independently selected from the alkynyl, where C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl is R 27c Each substituent is substituted as needed by one or more substituents selected independently of the original; R 24 teeth: Hydrogen, halogen, -OR 28d , -SR 28d , -N(R 28d ) 2 , -NO 2 , and -CN; and Halogen, -OR 28d , -SR 28d , -N(R 28d ) 2 , -NO 2 , and -CN, C 3~10 A carbon ring and a carbon ring, optionally substituted with one or more substituents independently selected from 3-membered to 10-membered heterocycles. 1~6 Alkyl, where C 3~10 Carbon rings and 3- to 10-membered heterocycles are R 27d Each of which is substituted as needed by one or more substituents independently selected from the original. Selected from; R 24’ teeth: Hydrogen, halogen, -OR 28d , -SR 28d , -N(R 28d ) 2 , -NO 2 , and -CN; and Halogen, -OR 28d , -SR 28d , -N(R 28d ) 2 , -NO 2 , and -CN, C 3~10 A carbon ring and a carbon ring, optionally substituted with one or more substituents independently selected from 3-membered to 10-membered heterocycles. 1~6 Alkyl, where C 3~10 Carbon rings and 3- to 10-membered heterocycles are R 27d Each of which is substituted as needed by one or more substituents independently selected from the original. Selected from; Or R 24 and R 24 'together with C 3~10 A carbon ring or a 3-membered to 10-membered heterocycle is formed, where the C 3~10 A carbon ring, or a 3- to 10-membered heterocycle, is R 27d It is optionally substituted with one or more substituents selected independently of it; R 25 teeth: Hydrogen, halogen, -OR 28e , -SR 28e , -N(R 28e ) 2 , -NO 2 ,-CN,C 1~6 Alkyl, C 3~10 Selected from carbon rings and 3-membered to 10-membered heterocycles, where the C 1~6 Alkyl, C 3~10 Carbon rings and 3- to 10-membered heterocycles have one or more R 27e Each is replaced as needed; R 26 teeth: Hydrogen, halogen, -OR 28f , -SR 28f , -N(R 28f ) 2 , -NO 2 , and -CN; and R 27f C as needed, substituted with one or more substituents independently selected from 1~6 Alkyl Selected from; Each R 27 , R 27a , R 27b , R 27c , R 27d , R 27e , and R 27f Independently: Halogen, -OR 28g , -SR 28g , -N(R 28g ) 2 , -C(O)R 28g , -C(O)N(R 28g ) 2 , -N(R 28g ) C(O)R 28g , -N(R 28g ) C(O)N(R 28g ) 2 , -OC(O)N(R 28g ) 2 , -N(R 28g ) C(O)OR 28g , -C(O)OR 28g , -OC(O)R 28g , -S(O)R 28g , -S(O) 2 R 28g , -NO 2 , =O, =S, =N(R 28g ), and -CN; and C 1~3 Alkyl, C 2~3 Alkenyl and C 2~3 Alkynnyl, each of which is a halogen, -OR 28g , -SR 28g , -N(R 28g ) 2 , -C(O)R 28g , -C(O)N(R 28g ) 2 , -N(R 28g ) C(O)R 28g , -N(R 28g ) C(O)N(R 28g ) 2 , -OC(O)N(R 28g ) 2 , -N(R 28g ) C(O)OR 28g , -C(O)OR 28g , -OC(O)R 28g , -S(O)R 28g , -S(O) 2 R 28g , -NO 2 , =O, =S, =N(R 28g ), and as needed, substituted with one or more substituents independently selected from -CN. Selected from; Each R 28 , R 28a , R 28b , R 28c , R 28d , R 28e , R 28f , and R 28g Independently: Hydrogen and halogens; and C 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl and C 3~10 A carbon ring, each of which is a halogen, -CN, -OH, -SH, -NO 2 , -NH 2 , =O, =S, -OC 1~6 Alkyl, -S-C 1~6 Alkyl, -N(C) 1~6 Alkyl) 2 ,-NH(C 1~6 Alkyl), C 3~10 Carbocyclic rings, or those optionally substituted with one or more substituents independently selected from 3-membered to 10-membered heterocycles; and C 3~10 Carbon rings and 3- to 10-membered heterocycles, each of which is a halogen, -CN, -OH, -SH, -NO 2 , -NH 2 , =O, =S, -OC 1~6 Alkyl, -S-C 1~6 Alkyl, -SO 2 -C 1~6 Alkyl, -N(C) 1~6 Alkyl) 2 ,-NH(C 1~6 Alkyl), C 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkinyl, C 3~10 Carbon rings, 3-membered to 10-membered heterocycles, and C 1~6 Substituted as needed with one or more substituents independently selected from the haloalkyl group. Selected from, method.
103. The compound of formula (III) is 【Chemistry 295】 The method according to claim 102, not the method described in claim 102.
104. R 21 but: Hydrogen, C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkynnyl, each of which is a halogen, -OR 28a , -SR 28a , -C(O)R 28a , -C(O)N(R 28a ) 2 , -N(R 28a ) C(O)R 28a , -C(O)OR 28a , -OC(O)R 28a , -N(R 28a ) C(O)N(R 28a ) 2 , -OC(O)N(R 28a ) 2 , -N(R 28a ) C(O)OR 28a , -S(O)R 28a , -S(O) 2 R 28a , -NO 2 , =O, =S, =N(R 28a ), -CN, C 3~10 The carbon ring is optionally substituted with one or more substituents independently selected from 3-membered to 10-membered heterocycles, where the C 3~10 Carbon rings and 3- to 10-membered heterocycles are R 27a Each of which is substituted as necessary with one or more substituents independently selected from; and C 3~10 Carbon rings and 3- to 10-membered heterorings, each of which is a halogen, -OR 28a , -SR 28a , -N(R 28a ) 2 , -C(O)R 28a , -C(O)N(R 28a ) 2 , -N(R 28a ) C(O)R 28a , -N(R 28a ) C(O)N(R 28a ) 2 , -OC(O)N(R 28a ) 2 , -N(R 28a ) C(O)OR 28a , -C(O)OR 28a , -OC(O)R 28a , -S(O)R 28a , -S(O) 2 R 28a , -NO 2 , =O-, =S, =N(R 28a ), -CN, C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 It is optionally substituted with one or more substituents independently selected from the alkynyl, where C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl is R 27a Each of which is substituted as needed by one or more substituents independently selected from the original. Selected from; R 22 but: Hydrogen, C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkynnyl, each of which is a halogen, -OR 28b , -SR 28b , -C(O)R 28b , -C(O)N(R 28b ) 2 , -N(R 28b ) C(O)R 28b , -C(O)OR 28b , -OC(O)R 28b , -N(R 28b ) C(O)N(R 28b ) 2 , -OC(O)N(R 28b ) 2 , -N(R 28b ) C(O)OR 28b , -S(O)R 28b , -S(O) 2 R 28b , -NO 2 , =O, =S, =N(R 28b ), -CN, C 3~10 The carbon ring is optionally substituted with one or more substituents independently selected from 3-membered to 10-membered heterocycles, where the C 3~10 Carbon rings and 3- to 10-membered heterocycles are R 27b Each of which is substituted as necessary with one or more substituents independently selected from; and C 3~10 Carbon rings and 3- to 10-membered heterorings, each of which is a halogen, -OR 28b , -SR 28b , -N(R 28b ) 2 , -C(O)R 28b , -C(O)N(R 28b ) 2 , -N(R 28b ) C(O)R 28b , -N(R 28b ) C(O)N(R 28b ) 2 , -OC(O)N(R 28b ) 2 , -N(R 28b ) C(O)OR 28b , -C(O)OR 28b , -OC(O)R 28b , -S(O)R 28b , -S(O) 2 R 28b , -NO 2 , =O-, =S, =N(R 28b ), -CN, C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 It is optionally substituted with one or more substituents independently selected from the alkynyl, where C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl is R 27b Each of which is substituted as needed by one or more substituents independently selected from the original. Selected from; or R 21 R 22 Together with C 3~10 They form a carbon ring, or a 3- to 10-membered heteroring, each of which is a halogen, -OR 28a , -SR 28a , -N(R 28a ) 2 , -C(O)R 28a , -C(O)N(R 28a ) 2 , -N(R 28a ) C(O)R 28a , -N(R 28a ) C(O)N(R 28a ) 2 , -OC(O)N(R 28a ) 2 , -N(R 28a ) C(O)OR 28a , -C(O)OR 28a , -OC(O)R 28a , -S(O)R 28a , -S(O) 2 R 28a , -NO 2 , =O-, =S, =N(R 28a ), -CN, C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 It is optionally substituted with one or more substituents independently selected from the alkynyl, where C 1~6 Alkyl, C 2~6 Alkenyl and C 2~6 Alkinyl is R 27b Each substituent is substituted as needed by one or more substituents selected independently of the original, The method according to claim 102.
105. R 25 but: Hydrogen, halogen, -OR 28e , -SR 28e , -N(R 28e ) 2 , -NO 2 , -CN, and C 1~6 Selected from alkyl, where C 1~6 Alkyl is one or more R 27e The method according to claim 102, wherein the substitutions are made as necessary.
106. The aforementioned cardiovascular disease or related condition: Hypertrophic cardiomyopathy (HCM); Heart failure with preserved ejection fraction (HFpEF); Heart failure with mildly reduced ejection fraction Disorders of relaxation; Impaired ventricular stiffness (diabetic HFpEF); Dilated cardiomyopathy (DCM); Ischemic cardiomyopathy; Heart transplant allograft vascular disease; Restrictive cardiomyopathy; Heart valve disease (e.g., aortic stenosis – including post-AVR / TAVR and congenital forms in the elderly); Left ventricular (LV) hypertrophy; Right ventricular (RV) hypertrophy; Acute myocardial infarction; acute vascular regeneration; ischemia; and Angina The method according to any one of claims 102 to 105, selected from the following.
107. The method according to claim 106, wherein the ejection fraction-preserved heart failure (HFpEF) comprises one or more disorders selected from impaired relaxation and impaired ventricular stiffness (diabetic HFpEF).
108. The method according to claim 106, wherein the left ventricular (LV) hypertrophy is malignant left ventricular (LV) hypertrophy.
109. The method according to claim 106, wherein the restrictive cardiomyopathy comprises one or more subgroups selected from the inflammatory subgroup, the infiltrative subgroup, the storage subgroup, the idiopathic / hereditary subgroup, and the congenital heart disease subgroup.
110. The method according to claim 106, wherein the inflammatory subgroup comprises one or more subgroups selected from refrel and EMF.
111. The method according to claim 106, wherein the inflammatory subgroup comprises one or more subgroups selected from amyloid, sarcoid, and XRT.
112. The method according to claim 106, wherein the storage subgroup comprises one or more subgroups selected from hemochromatosis, Fabry, and glycogen disease.
113. The method according to claim 106, wherein the idiopathic / hereditary subgroup comprises one or more subgroups selected from the subgroups related to Top I (betamyosin HC), Top T (alpha cardiac actin), and desmin.
114. The method according to claim 106, wherein the subgroup of congenital heart disease comprises one or more subgroups selected from pressure overload RV, Tetralogy of Fallot, and pulmonary valve stenosis.
115. The method according to any one of claims 106 to 114, wherein the cardiovascular disease or related condition is hypertrophic cardiomyopathy.
116. The method according to any one of claims 106 to 114, wherein the cardiovascular disease or related condition is obstructive hypertrophic cardiomyopathy.
117. The method according to any one of claims 106 to 114, wherein the cardiovascular disease or related condition is non-obstructive hypertrophic cardiomyopathy.
118. The method according to any one of claims 106 to 114, wherein the cardiovascular disease or related condition is heart failure with preserved ejection fraction.
119. The method according to any one of claims 106 to 114, wherein the cardiovascular disease or related condition is left ventricular stiffness.