Muscarinic acetylcholine M1 receptor antagonist

Abstract

To provide compounds which are useful as antagonists of the muscarinic acetylcholine receptor M1 (mAChR M1), and methods for preparing the compounds.SOLUTION: The present invention provides a compound having the structure of formula (IA) or (IB), or a pharmaceutically acceptable salt or solvate thereof.SELECTED DRAWING: None

Description

[Background technology]

[0001] Cross-reference of related applications This application is a result of U.S. Provisional Application No. 62 / 911,807, filed on October 7, 2019. Claiming priority, incorporated herein by reference in whole and for all purposes. ru.

[0002] Human muscarinic acetylcholine receptor M1 (mAChR M1) is a CHRM1 gene. It is a 479-amino acid protein encoded by mAChR M1. One of the five members of the carinic acetylcholine receptor (M1-M5) family. These receptors are widely expressed throughout the body and are involved in cognitive, sensory, motor, and autonomic nervous systems. It plays various roles in function. M1mAChR is involved in both the central and peripheral nervous systems. It is particularly observed in the cerebral cortex and sympathetic ganglia. mAChR in seizure activity and motor control. Based on the potential role of M1, highly selective mAChR M1 antagonists are, In addition to certain movement disorders including Parkinson's disease, dystonia, and fragile X syndrome, It may also have potential usefulness in the treatment of epileptic disorders in the body. [Overview of the Initiative]

[0003] This disclosure relates, for example, to the muscarinic acetylcholine M1 receptor (mAChR M1). Compounds and compositions that are antagonists, as well as their use as pharmaceuticals, and their Preparation method, and pharmaceutical composition containing the disclosed compound as at least one active ingredient. This disclosure also provides information on muscarinic acetylcholine M1 receptor activity in patients. The disclosed compounds as pharmaceuticals for inhibition and / or in the manufacture of pharmaceuticals are provided for use.

[0004] In one aspect, a compound, or a pharmaceutically acceptable salt or solvate thereof, having the structure of formula (IA-1) or (IB-1),

Chemical formula

Chemical formula

[0005] In one embodiment, a compound of formula (IA) or (IB), [ka] During the ceremony, X is bonded, -C(R 9 )(R 10 )-,-N(R 11 )-, -O-, -S(O) n - -CH2N(R 11 )-, or -CH2O-, Y is -CH2-, -CH2CH2-, -CH=CH-, or -CH2OCH2- can be, R 1 but, [ka] In the formula, ring A is either a 5-membered or 6-membered heteroaryl ring, or optionally, Rogen, Cyano, -N(R) 14 )(R 15 ), C 1-6 Alkyl, C 1-6 Alkoxy, C 1-6 Haloalkyl, C 1-6 Haloalkoxy, C 3-6 Cycloalkyl, C 3-6 C Chloalkoxy, C 3-6 Halocycloalkyl, C 3-6 Halocycloalkoxy, hetero Cycloalkyl, aryl, heteroaryl, S(O) n (R 16 ), or -SF5 a 5- or 6-membered heterocycloalkyl ring replaced by, wherein the heteroaryl or hetero cycloalkyl ring contains 1, 2, or 3 heteroatoms selected from the group consisting of O, N, or S ; R 2 is hydrogen, deuterium, halogen, hydroxyl, C 1-6 alkyl, C 1-6 alko xy, C 1-6 haloalkyl, C 1-6 haloalkoxy, C 3-6 cycloalkyl, C3 -6 cycloalkoxy, C 3-6 halocycloalkyl, C 3-6 halocycloalkoxy, C 1-6 alkylhydroxyl, heterocycloalkyl, aryl, or heteroaryl ; R 3 is halogen, C 1-6 alkyl, C 1-6 ​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​ Selected, or R 3 and R 4 They are connected, and optionally, halogen, C 1-6 Alkyl, also or C 3-6 Cycloalkyl or heterocycloalkyl Forming a ring, or R 4 and R 5 They are connected, and optionally, halogen, C 1-6 Alkyl , or C 3-6 Cycloalkyl or heterocycloalkyl substituted Forms a Kill ring, R 6 and R 7 These independently produce hydrogen, deuterium, halogens, and C 1-3 Selected from alkyl groups Selected, or R 3 and R 7 They are connected, and optionally, halogen, C 1-6 Alkyl, also or C 3-6 Cycloalkyl or heterocycloalkyl Forming a ring, or R 4 and R 6 They are connected, and optionally, halogen, C 1-6 Alkyl , or C 3-6 Cycloalkyl or heterocycloalkyl substituted It forms a kill ring, or R 5 and R 7 They connect to form a bond, R 8 but, [ka] And, R 9 and R 10 These independently produce hydrogen, deuterium, halogens, and C 1-6 Alkyl, C 1-6 Alkoxy, C 1-6Haloalkyl, C 1-6 Haloalkoxy, C 3-6 Cycloalkyl , C 3-6 Cycloalkoxy, C 3-6 Halocycloalkyl, C 3-6 Halocycloalco Selected from xy, heterocycloalkyl, aryl, or heteroaryl, is R 3 and R 10 They are connected, and optionally, halogen, C 1-6 Alkyl, or C 3- Forming a cycloalkyl or heterocycloalkyl ring substituted with a 6-cycloalkyl group, Or R 4 and R 10 They are connected, and optionally, halogen, C 1-6 Alkyl, or C 3-6 A cycloalkyl or heterocycloalkyl ring substituted with a cycloalkyl group accomplish, or R 6 and R 10 They are connected, and optionally, halogen, C 1-6 Alkyl, also or C 3-6 Cycloalkyl or heterocycloalkyl Forming a ring, or R 9 and R 10 They are connected, and optionally, halogen, C 1-6 Alki Ru, or C 3-6 Cycloalkyl or heterocycloalkyl substituted Forms a lucyl ring, R 11 However, hydrogen, C 1-6 Alkyl, C 1-6 Haloalkyl, C 3-6 Cycloalkyl , C 3-6 Halocycloalkyl, heterocycloalkylaryl, or heteroaryl It is R 3 and R11 They are connected, and optionally, halogen, C 1-6 Alkyl, Or C 3-6 Forms a heteroalkyl ring substituted with a cycloalkyl group, or R 4 oh Call R 11 They are connected, and optionally, halogen, C 1-6 Alkyl, or C 3-6 Cyclo Forms a heteroalkyl ring substituted with alkyl, or R 6 and R 11 They are connected, Optionally, halogen, C 1-6 Alkyl, or C 3-6 cycloalkyl substituted Forms a teloalkyl ring, Each R 12 These independently consist of hydroxyl, halogen, cyano, and -N(R) 14 )(R 15 ), C 1-6 Alkyl, C 1-6 Alkoxy, C 1-6 Haloalkyl, C 1-6 Haloalcochry C 3-6 Cycloalkyl, C 3-6 Cycloalkoxy, C 3-6 Halocycloalkyl , C 3-6 Halocycloalkoxy, C 1-6 Alkylhydroxyl, heterocycloalkyl Ru, aryl, heteroaryl, S(O) n (R 16 ), or selected from SF5, Or R 3 and one R 12 They are connected, and optionally, halogen, C 1-6 Alkyl, also or C 3-6 A cycloalkyl or heteroalkyl ring substituted with a cycloalkyl group accomplish, or R 10 and one R 12They are connected, and optionally, halogen, C 1-6 Al Kill, or C 3-6 Cycloalkyl or heteroalkyl substituted Forms a ring, or R 11 and one R 12 They are connected, and optionally, halogen, C1 -6 Alkyl, or C 3-6 Forms a heteroalkyl ring substituted with a cycloalkyl group. , R 13 However, hydrogen, C 1-6 Alkyl, C 1-6 Haloalkyl, C 3-6 Cycloalkyl , C 3-6 Halocycloalkyl, heterocycloalkyl, aryl, or heteroaryl It is R 14 and R 15 Hydrogen, C 1-6 Alkyl, C 1-6 Haloalkyl, C 3-6 Cycloalkyl, C 3-6 Halocycloalkyl, heterocycloalkyl, aryl , or selected from heteroaryls, or R 14 and R 15 They are linked together, arbitrarily , halogen, C 1-6 Alkyl, or C 3-6 Heterocyclic substituted Forms a chloroalkyl ring, R 16 However, C 1-6 Alkyl, C 1-6 Haloalkyl, C 3-6 Cycloalkyl, C3 -6 Halocycloalkyl, heterocycloalkyl, aryl, or heteroaryl the law of nature, m is 0 or 1, n is 0, 1, or 2, Compounds where o is 0, 1, 2, or 3. Or, provided that the aforementioned combination does not infringe upon the rules of valence which are readily apparent to those skilled in the art, A pharmaceutically acceptable salt or solvate thereof is provided.

[0006] In one embodiment, a compound of formula (IIA) or (IIB), [ka] During the ceremony, X is bonded, -C(R 9 )(R 10 )-,-N(R 11 )-, -O-, -S(O) n - -CH2N(R 11 )-, or -CH2O-, Y is -CH2-, -CH2CH2-, -CH=CH-, or -CH2OCH2- can be, R 1 but, [ka] In the formula, ring A is either a 5-membered or 6-membered heteroaryl ring, or optionally, Rogen, Cyano, -N(R) 14 )(R 15 ), C 1-6 Alkyl, C 1-6 Alkoxy, C 1-6 Haloalkyl, C 1-6 Haloalkoxy, C 3-6 Cycloalkyl, C 3-6 C Chloalkoxy, C 3-6 Halocycloalkyl, C 3-6 Halocycloalkoxy, hetero Cycloalkyl, aryl, heteroaryl, S(O) n (R 16 ), or -SF5 A 5-membered or 6-membered heterocycloalkyl ring substituted with a heteroaryl or hete The rocycloalkyl ring consists of 1, 2, or 3 elements selected from the group consisting of O, N, or S. It contains heteroatoms, R 2 However, hydrogen, deuterium, halogen, hydroxyl, C 1-6 Alkyl, C 1-6 Arco Kishi, C 1-6 Haloalkyl, C 1-6 Haloalkoxy, C 3-6 Cycloalkyl, C3 -6 Cycloalkoxy, C 3-6 Halocycloalkyl, C 3-6 Halocycloalkoxy, C 1-6 Alkylhydroxyl, heterocycloalkyl, aryl, or heteroaryl It is R 3 However, halogen, C 1-6 Alkyl, C 1-6 Alkoxy, C 1-6 Haloalkyl, C 1-6 Haloalkoxy, C 3-6 Cycloalkyl, C 3-6 Cycloalkoxy, C 3- 6-halocycloalkyl, C 3-6 Halocycloalkoxy, C 1-6 Alkylhydroxyl , heterocycloalkyl, aryl, or heteroaryl, or R 2 and R 3 They are connected, and optionally, halogen, C 1-6 Alkyl, or C 3-6 Cycloalkyl Forms a cycloalkyl or heterocycloalkyl ring substituted with , R 8 but, [ka] And, R 9 and R 10 These independently produce hydrogen, deuterium, halogens, and C 1-6 Alkyl, C 1-6 Alkoxy, C 1-6 Haloalkyl, C 1-6 Haloalkoxy, C 3-6 Cycloalkyl , C 3-6 Cycloalkoxy, C 3-6 Halocycloalkyl, C 3-6 Halocycloalco Selected from xy, heterocycloalkyl, aryl, or heteroaryl, is R 3 and R 10 They are connected, and optionally, halogen, C 1-6 Alkyl, or C 3- Forming a cycloalkyl or heterocycloalkyl ring substituted with a 6-cycloalkyl group, Or R 9 and R 10 They are connected, and optionally, halogen, C 1-6 Alkyl, or C 3-6 A cycloalkyl or heterocycloalkyl ring substituted with a cycloalkyl group accomplish, R 11 However, hydrogen, C 1-6 Alkyl, C 1-6 Haloalkyl, C 3-6 Cycloalkyl , C 3-6 Halocycloalkyl, heterocycloalkylaryl, or heteroaryl It is R 3 and R 11 They are connected, and optionally, halogen, C 1-6 Alkyl, Or C 3-6 Forms a heteroalkyl ring substituted with a cycloalkyl group, Each R 12 These independently consist of hydroxyl, halogen, cyano, and -N(R) 14)(R 15 ), C 1-6 Alkyl, C 1-6 Alkoxy, C 1-6 Haloalkyl, C 1-6 Haloalcochry C 3-6 Cycloalkyl, C 3-6 Cycloalkoxy, C 3-6 Halocycloalkyl , C 3-6 Halocycloalkoxy, C 1-6 Alkylhydroxyl, heterocycloalkyl Ru, aryl, heteroaryl, S(O) n (R 16 ), or selected from SF5, Or R 3 and one R 12 They are connected, and optionally, halogen, C 1-6 Alkyl, also or C 3-6 A cycloalkyl or heteroalkyl ring substituted with a cycloalkyl group accomplish, or R 10 and one R 12 They are connected, and optionally, halogen, C 1-6 Al Kill, or C 3-6 Cycloalkyl or heteroalkyl substituted Forms a ring, or R 11 and one R 12 They are connected, and optionally, halogen, C1 -6 Alkyl, or C 3-6 Forms a heteroalkyl ring substituted with a cycloalkyl group. , R 13 However, hydrogen, C 1-6 Alkyl, C 1-6 Haloalkyl, C 3-6 Cycloalkyl , C 3-6 Halocycloalkyl, heterocycloalkyl, aryl, or heteroaryl It is R14 and R 15 Hydrogen, C 1-6 Alkyl, C 1-6 Haloalkyl, C 3-6 Cycloalkyl, C 3-6 Halocycloalkyl, heterocycloalkyl, aryl , or selected from heteroaryls, or R 14 and R 15 They are linked together, arbitrarily , halogen, C 1-6 Alkyl, or C 3-6 Heterocyclic substituted Forms a chloroalkyl ring, R 16 However, C 1-6 Alkyl, C 1-6 Haloalkyl, C 3-6 Cycloalkyl, C3 -6 Halocycloalkyl, heterocycloalkyl, aryl, or heteroaryl the law of nature, m is 0 or 1, n is 0, 1, or 2, Compounds where o is 0, 1, 2, or 3. Or, on the condition that the aforementioned combination does not violate the rules of valence which are readily known to those skilled in the art. A pharmaceutically acceptable salt or solvate thereof is provided.

[0007] In another embodiment, the compound of formula (III) is, [ka] During the ceremony, X is bonded, -C(R 9 )(R 10 )-,-N(R 11 )-, -O-, -S(O) n - -CH2N(R 11 )-, or -CH2O-, R 1 but, [ka] In the formula, ring A is either a 5-membered or 6-membered heteroaryl ring, or optionally, Rogen, Cyano, -N(R) 14 )(R 15 ), C 1-6 Alkyl, C 1-6 Alkoxy, C 1-6 Haloalkyl, C 1-6 Haloalkoxy, C 3-6 Cycloalkyl, C 3-6 C Chloalkoxy, C 3-6 Halocycloalkyl, C 3-6 Halocycloalkoxy, hetero Cycloalkyl, aryl, heteroaryl, S(O) n (R 16 ), or -SF5 A 5-membered or 6-membered heterocycloalkyl ring substituted with a heteroaryl or hete The rocycloalkyl ring consists of 1, 2, or 3 elements selected from the group consisting of O, N, or S. It contains heteroatoms, R 2 However, hydrogen, deuterium, halogen, hydroxyl, C 1-6 Alkyl, C 1-6 Arco Kishi, C 1-6 Haloalkyl, C 1-6 Haloalkoxy, C 3-6 Cycloalkyl, C3 -6 Cycloalkoxy, C 3-6 Halocycloalkyl, C 3-6 Halocycloalkoxy, C 1-6 Alkylhydroxyl, heterocycloalkyl, aryl, or heteroaryl It is R 3 However, halogen, C 1-6 Alkyl, C 1-6 Alkoxy, C 1-6 Haloalkyl, C1-6 Haloalkoxy, C 3-6 Cycloalkyl, C 3-6 Cycloalkoxy, C 3- 6-halocycloalkyl, C 3-6 Halocycloalkoxy, C 1-6 Alkylhydroxyl , heterocycloalkyl, aryl, or heteroaryl, or R 2 and R 3 They are connected, and optionally, halogen, C 1-6 Alkyl, or C 3-6 Cycloalkyl Forms a cycloalkyl or heterocycloalkyl ring substituted with , R 8 but, [ka] And, R 9 and R 10 These independently produce hydrogen, deuterium, halogens, and C 1-6 Alkyl, C 1-6 Alkoxy, C 1-6 Haloalkyl, C 1-6 Haloalkoxy, C 3-6 Cycloalkyl , C 3-6 Cycloalkoxy, C 3-6 Halocycloalkyl, C 3-6 Halocycloalco Selected from xy, heterocycloalkyl, aryl, or heteroaryl, is R 3 and R 10 They are connected, and optionally, halogen, C 1-6 Alkyl, or C 3- Forming a cycloalkyl or heterocycloalkyl ring substituted with a 6-cycloalkyl group, Or R 9 and R 10 They are connected, and optionally, halogen, C 1-6 Alkyl, or C 3-6 A cycloalkyl or heterocycloalkyl ring substituted with a cycloalkyl group accomplish, R 11 However, hydrogen, C 1-6 Alkyl, C 1-6 Haloalkyl, C 3-6 Cycloalkyl , C 3-6 Halocycloalkyl, heterocycloalkylaryl, or heteroaryl It is R 3 and R 11 They are connected, and optionally, halogen, C 1-6 Alkyl, Or C 3-6 Forms a heteroalkyl ring substituted with a cycloalkyl group, Each R 12 These independently consist of hydroxyl, halogen, cyano, and -N(R) 14 )(R 15 ), C 1-6 Alkyl, C 1-6 Alkoxy, C 1-6 Haloalkyl, C 1-6 Haloalcochry C 3-6 Cycloalkyl, C 3-6 Cycloalkoxy, C 3-6 Halocycloalkyl , C 3-6 Halocycloalkoxy, C 1-6 Alkylhydroxyl, heterocycloalkyl Ru, aryl, heteroaryl, S(O) n (R 16 ), or selected from SF5, Or R 3 and one R 12 They are connected, and optionally, halogen, C 1-6 Alkyl, also or C 3-6 A cycloalkyl or heteroalkyl ring substituted with a cycloalkyl group accomplish, or R 10 and one R 12They are connected, and optionally, halogen, C 1-6 Al Kill, or C 3-6 Cycloalkyl or heteroalkyl substituted Forms a ring, or R 11 and one R 12 They are connected, and optionally, halogen, C1 -6 Alkyl, or C 3-6 Forms a heteroalkyl ring substituted with a cycloalkyl group. , R 13 However, hydrogen, C 1-6 Alkyl, C 1-6 Haloalkyl, C 3-6 Cycloalkyl , C 3-6 Halocycloalkyl, heterocycloalkyl, aryl, or heteroaryl It is R 14 and R 15 Hydrogen, C 1-6 Alkyl, C 1-6 Haloalkyl, C 3-6 Cycloalkyl, C 3-6 Halocycloalkyl, heterocycloalkyl, aryl , or selected from heteroaryls, or R 14 and R 15 They are linked together, arbitrarily , halogen, C 1-6 Alkyl, or C 3-6 Heterocyclic substituted Forms a chloroalkyl ring, R 16 However, C 1-6 Alkyl, C 1-6 Haloalkyl, C 3-6 Cycloalkyl, C3 -6 Halocycloalkyl, heterocycloalkyl, aryl, or heteroaryl the law of nature, m is 0 or 1, n is 0, 1, or 2, Compounds where o is 0, 1, 2, or 3. Or, provided that the aforementioned combination does not infringe upon the rules of valence which are readily apparent to those skilled in the art, A pharmaceutically acceptable salt or solvate thereof is provided.

[0008] Compounds of formula (IA), (IB), (IIA), (IIB), or (III), In some embodiments of those pharmaceutically acceptable salts or solvates, X is bonded. -C(R 9 )(R 10 )-,-N(R 11 )-, or -O-. Some real In the application form, X is bonded, -N(R 11 )-, or -O-.

[0009] Compounds of formula (IA), (IB), (IIA), (IIB), or (III), In some embodiments of those pharmaceutically acceptable salts or solvates, R 1 but, [ka] In some embodiments, R 1 but, [ka] That is the case.

[0010] Compounds of formula (IA), (IB), (IIA), (IIB), or (III), In some embodiments of those pharmaceutically acceptable salts or solvates, R 8 but, [ka] In some embodiments, R 8 but, [ka] That is the case.

[0011] Any combination of the groups described above or below for various variable parts is this This specification is intended to be used in this specification. Throughout this specification, these groups and substituents are safe. Selected by those skilled in the art to provide specific parts and compounds.

[0012] In another embodiment, formulas (IA), (IB), (IIA), (IIB), or (III) A compound, its pharmaceutically acceptable salt or solvate, and at least one pharmaceutically acceptable It is a pharmaceutical composition containing an excipient.

[0013] Another aspect is a method of doing so in a subject who requires treatment for a neurodegenerative disorder. There are formulas for the effective therapeutic dose, such as (IA), (IB), (IIA), (IIB), or (II I) administering the compound, or a pharmaceutically acceptable salt or solvate thereof, to the target. This method includes [something].

[0014] Another aspect was a method of doing so in a subject who required treatment for a neurological disorder. The formula for the effective therapeutic dose is (IA), (IB), (IIA), (IIB), or (III). This includes administering the compound, or a pharmaceutically acceptable salt or solvate thereof, to the target. Yes, it is a method. Some embodiments are for subjects who require treatment of neurological disorders. The method for doing so is the formula for the effective therapeutic dose (IA), (IB), (IIA), (II B) or (III) compounds, or their pharmaceutically acceptable salts or solvates The method involves administering the drug to the target, and the nerve damage is peripheral neuropathy. The embodiment was a method for treating neurological disorders in subjects who required treatment. The formula for the effective therapeutic dose is (IA), (IB), (IIA), (IIB), or (III). This includes administering the compound, or a pharmaceutically acceptable salt or solvate thereof, to the target. Therefore, the nerve damage is diabetic neuropathy.

[0015] Another aspect is a method of doing so in a subject who requires treatment for a demyelinating disease. That is, the formula for the effective therapeutic dose is (IA), (IB), (IIA), (IIB), or (III The administration of the compound of ) or a pharmaceutically acceptable salt or solvate thereof to the target This includes methods. Some embodiments are subjects that require treatment of demyelinating diseases. A method for doing so in which the formula for the effective therapeutic dose is (IA), (IB), (IIA), ( Compounds of type IIB, or type (III), or their pharmaceutically acceptable salts or solvents. The method involves administering a Japanese substance to a target, and the demyelinating disease is a demyelinating disease of the central nervous system. Some embodiments describe a subject that requires treatment for demyelinating diseases. A method for performing this, wherein the formulas for the effective therapeutic dose are (IA), (IB), (IIA), (IIB), Alternatively, the compound(III), or a pharmaceutically acceptable salt or solvate thereof. The method involves administering to a demyelinating disease, which is multiple sclerosis. The method of administration is a method of performing treatment in a patient who requires treatment for a demyelinating disease. The formula for the effective therapeutic dose is (IA), (IB), (IIA), (IIB), or (III) This includes administering the compound, or a pharmaceutically acceptable salt or solvate thereof, to the target. Demyelinating diseases are demyelinating diseases of the peripheral nervous system.

[0016] In some embodiments of the methods described herein, the method involves administering one or more immunomodulators The invention further includes the administration of an immunomodulator. In some embodiments, one or more immunomodulators are used to provide an IFN-β1 molecule. etc.; corticosteroids, etc.; polymers of glutamic acid, lysine, alanine, and tyrosine. or glatiramers, etc.; antibodies against alpha-4 integrin or fragments thereof. Examples include natalizumab; anthracendione molecules or mitoxantrone; and S1P1 devices. Potential modifiers or fingolimods, etc.; NRF2 functional modifiers or dimethyl fumare Antibodies against the alpha subunit of the IL-2 receptor (CD25) on T cells, etc. or daclizumab, etc.; antibodies against CD52 or alemtuzumab, etc.; against CD20 Antibodies or ocrelizumab, etc.; and inhibition of dihydroorote dehydrogenase. The agent is selected from teriflunomide, etc.

[0017] Another aspect is a method for modulating muscarinic acetylcholine receptor M1 activity in a subject. and the combination of formulas (IA), (IB), (IIA), (IIB), or (III) This includes administering a substance, or a pharmaceutically acceptable salt or solvate thereof, to a target. , a method. In some embodiments, formulas (IA), (IB), (IIA), (IIB ), or compounds of (III), or their pharmaceutically acceptable salts or solvations The substance acts as a selective M1 antagonist. [Modes for carrying out the invention]

[0018] This disclosure describes, at least in part, the inhibition of the muscarinic acetylcholine M1 receptor. This study focuses on compounds that can perform this action.

[0019] As used herein and in the appended claims, the singular forms "a", "an", and The pronoun "the" refers to multiple objects unless otherwise specified in the context. For example, a reference to "drugs" includes multiple such drugs, and a reference to "cells" means... Includes references to one or more cells (or more cells) and their equivalents. (e.g., molecular weight) Where the scope of a physiological property or a chemical property such as a chemical formula is used herein, All combinations and partial combinations of the range, as well as specific embodiments within them It is intended to be included. The term "approximately" when referring to a number or range of numbers. This means that the mentioned numerical value or range of values ​​is close to the experimental variability (or within the statistical experimental error). Similar values, and consequently, a numerical value or range of numerical values ​​is 1% of the stated numerical value or range of numerical values. This means it will vary by 15%. In embodiments, approximately is generally acceptable in the art. This means within the standard deviation used for the measurement. In embodiments, this is approximately + / - 10% of the specific value. It means a range that extends to. In embodiments, approximately includes a specific value. The term "ing)" (and "comprise" or "compr") Related terms such as "ises" or "to have" or "to include" The term refers to other specific embodiments, for example, any substance composition, composition, or method described herein. An embodiment of a law or process, etc., consisting of the described features or described features It is not intended to exclude the idea of ​​"becoming essentially from" a sign.

[0020] I. Definition When used in the specification and attached claims, unless otherwise specified, The following terms have the meanings set forth below.

[0021] When used herein, C1-C x C1-C2, C1-C3...C1-C x Includes C1-C x This refers to the number of carbon atoms that make up the part it specifies (any substitution). (excluding the base). Similarly, C1- x C1-2, C1-3...C1- x Includes C1-C x This refers to the number of carbon atoms that make up the part it specifies (excluding any substituents).

[0022] "Amino" refers to the -NH2 radical.

[0023] "Cyano" refers to the -CN radical.

[0024] "Hydroxyl" refers to the -OH radical.

[0025] "Nitro" refers to the -NO2 radical.

[0026] "Oxa" refers to the -O- radical.

[0027] "Oxo" refers to the =O radical.

[0028] "Thioxo" refers to the S group.

[0029] "Imino" refers to the NH radical.

[0030] "Oxymo" refers to the =N-OH radical.

[0031] "Alkyl" or "alkylene" consists only of carbon and hydrogen atoms and does not contain unsaturated atoms. First, 1 to 15 carbon atoms (for example, C1-C 15 Alkyl or C1-C 15 Alki Refers to linear or branched hydrocarbon chain radicals having (a) A carbon atom contains 1 to 13 carbon atoms (for example, C1-C 13 Alkyl or C1-C 13 Alkyl). In certain embodiments, the alkyl group contains 1 to 8 carbon atoms (e.g., C (1-C8 alkyl or C1-C8 alkyl). In other embodiments, alkyl is 1-6 Contains one carbon atom (e.g., C1-C6 alkyl or C1-C6 alkyl). Other In application, alkyl groups contain 1 to 5 carbon atoms (for example, C1-C5 alkyl groups). (C1-C5 alkyl). In other embodiments, the alkyl contains 1 to 4 carbon atoms. For example, C1-C4 alkyl or C1-C4 alkyl). In other embodiments, alkyl This includes 1 to 3 carbon atoms (for example, C1-C3 alkyl or C1-C3 alkyl ). In other embodiments, the alkyl group contains 1 to 2 carbon atoms (for example, C1-C2 alkyl group). (Lucyl or C1-C2 alkyl). In other embodiments, alkyl is one carbon atom Includes (e.g., C1 alkyl). In other embodiments, alkyl is composed of 5 to 15 carbon atoms. (For example, C5-C) 15 Alkyl or C5-C 15 Alkyl). In other embodiments Alkyls contain 5 to 8 carbon atoms (for example, C5-C8 alkyl or C5- C8 alkyl). In other embodiments, the alkyl contains 2 to 5 carbon atoms (for example, C2-C5 alkyl or C2-C5 alkyl). In other embodiments, alkyl is 3- Contains 5 carbon atoms (e.g., C3-C5 alkyl or C3-C5 alkyl). Other In the embodiment, the alkyl group is methyl, ethyl, 1-propyl (n-propyl), 1-methyl Isopropyl ethyl 1-butyl (n-butyl), methylpropyl 1-methylpropyl (se c-butyl), 2-methylpropyl (isobutyl), 1,1-dimethylethyl (ter Selected from t-butyl and 1-pentyl (n-pentyl). The alkyl is single-bonded. It is bonded to the rest of the molecule by bonding. Unless otherwise specified herein, A The lucyl group can optionally be halogen, cyano, nitro, oxo, thioxo, imino, or oxymo. , trimethylsilyl, -OR a , -SR a -OC(O)R a , -N(R a )2, -C( O)R a , -C(O)OR a ,-C(O)N(R a )2, -N(R a )C(O)OR f , -OC(O)-NR a R f , -N(R a )C(O)R f , -N(R a )S(O) t R f ( t is 1 or 2), -S(O) t Ure a (t is 1 or 2), -S(O) t R f (t is 1 or 2) and -S(O) t N(R a )2(t is 1 or 2 ) and in the formula, each R a These independently consist of hydrogen, alkyl, haloalkyl, and cycloalkyl aryl, aralkyl, heterocycloalkyl, heteroaryl, or heteroaryl It is an alkyl group, and each R f These are independently alkyl, haloalkyl, and cycloalkyl. Aryl, aralkyl, heterocycloalkyl, heteroaryl, or heteroaryl It is substituted with one or more substituents less than or equal to alkyl. Therefore, alkyl groups are substituted Alternatively, it may be unsubstituted. In the embodiment, the alkyl group is substituted with at least one substituent. Furthermore, when an alkyl group is substituted with multiple substituents, each substituent can be arbitrarily different. In form, the alkyl group is substituted with at least one size-restricted substituent, and the alkyl group When substituted with multiple size-restricting substituents, each size-restricting substituent can be arbitrarily different. In the application form, the alkyl group is substituted with at least one lower substituent, and multiple alkyl groups When substituted with lower substituents, each lower substituent can be arbitrarily different.

[0032] "Alkoxy" refers to a group bonded via the oxygen atom of the formula -O-alkyl, and alkyl This is the alkyl chain defined above.

[0033] "Alkenyl" consists only of carbon atoms and hydrogen atoms, and at least one carbon-carbon This refers to a branched hydrocarbon chain radical group that contains an elementary double bond and has 2 to 12 carbon atoms. In certain embodiments, the alkenyl contains 2 to 8 carbon atoms. In other embodiments, Lukenyl contains 2 to 4 carbon atoms. Alkenyl contains a single bond, for example, ethenyl ( (i.e., vinyl), prop-1-enyl (i.e., allyl), buta-1-enyl, pen The rest of the molecule is bonded to by ter-1-enyl, penta-1,4-dienyl, etc. Unless otherwise specified herein, alkenyl groups may optionally be halogens, cyanoacrylates, etc. Nitro, oxo, thioxo, imino, oxymo, trimethylsilyl, -OR a , -SR a -OC(O)-R f , -N(R a )2, -C(O)R a , -C(O)OR a , -C( O)N(R a )2, -N(R a )C(O)OR f -OC(O)-NR a R f , -N(R a )C(O)R f , -N(R a )S(O) t R f (t is 1 or 2), -S(O) t Ure a (t is 1 or 2), -S(O) t R f (t is 1 or 2) and -S(O) t N(R a )2(t is 1 or 2), where each R a It is independent Hydrogen, alkyl, haloalkyl, cycloalkyl, aryl, aralkyl, heteroalkyl It is a chloroalkyl, heteroaryl, or heteroarylalkyl, and each R f Independent And alkyl, haloalkyl, cycloalkyl, aryl, aralkyl, heterocyclo Alkyl, heteroaryl, or heteroarylalkyl - one of the following substituents Substitution occurs above. Therefore, the alkenyl group can be substituted or unsubstituted. Embodiments In this case, the alkenyl group is substituted with at least one substituent, and the alkenyl group is substituted with multiple substituents. When substituted with a group, each substituent can be arbitrarily different. In this embodiment, the alkenyl group is few At the very least, it is substituted with one size-restricting substituent, and the alkenyl group is substituted with multiple size-restricting substituents. If substituted, each size-limiting substituent can be arbitrarily different. In this embodiment, an alkenyl group is substituted with at least one lower substituent, and the alkenyl group is substituted with multiple lower substituents. In this case, each lower substituent can be arbitrarily different.

[0034] "Alkynnyl" consists only of carbon and hydrogen atoms, and at least one carbon-carbon This refers to a branched hydrocarbon chain radical group that contains a primary triple bond and has 2 to 12 carbon atoms. In certain embodiments, the alkynyl contains 2 to 8 carbon atoms. In other embodiments, Lukinyl has 2 to 4 carbon atoms. Alkinyl has a single bond, for example, ethynyl. The rest of the molecule is bonded by propynyl, butynyl, pentynyl, hexynyl, etc. Unless otherwise specified herein, the alkynyl group may optionally contain halogens, cyanoacrylates, and sylamines. Ano, nitro, oxo, thioxo, imino, oxymo, trimethylsilyl, -OR a ,- SR a -OC(O)R a , -N(R a )2, -C(O)R a , -C(O)OR a , -C (O)N(R a )2, -N(R a )C(O)OR f -OC(O)-NR a R f , -N( R a )C(O)R f , -N(R a )S(O) t R f (t is 1 or 2), -S(O )t Ure a (t is 1 or 2), -S(O) t R f (t is 1 or 2) bi-S(O) t N(R a )2(t is 1 or 2), where each R a Independent And hydrogen, alkyl, haloalkyl, cycloalkyl, aryl, aralkyl, hetero A cycloalkyl, heteroaryl, or heteroarylalkyl, where each R f German Alkyl, haloalkyl, cycloalkyl, aryl, aralkyl, heteroalkyl Roalkyl, heteroaryl, or one of the following substituents: heteroarylalkyl or less The above substitutions are achieved. Therefore, the alkynyl group can be substituted or unsubstituted. (Implementation) In this state, the alkynyl group is substituted with at least one substituent, and the alkynyl group has multiple substituents. When substitution occurs, each substituent can be arbitrarily different. In this embodiment, the alkynyl group is Substituted with at least one size-restricting substituent, and the alkynyl group has multiple size-restricting substituents. When substituted, each size-limiting substituent can be arbitrarily different. In this embodiment, alkynyl The group is substituted with at least one lower substituent, and the alkynyl group is substituted with multiple lower substituents. If so, each lower substituent can be arbitrarily different.

[0035] The term "heteroalkyl" may be used alone or in combination with other terms, as specified separately. Unless otherwise specified, at least one carbon atom and at least one heteroatom (for example, Stable linear or branched chains containing O, N, P, Si, and S, or combinations thereof. It means a combination, where the nitrogen atom and sulfur atom can be oxidized as desired, and the nitrogen heteroatom can be oxidized as desired. Intentionally, it can be quaternized and does not contain unsaturated compounds. Heteroatoms (plural possible) (e.g., O, N, S, Si, or P) is any internal position of the heteroalkyl group or alkyl group of the remainder of the molecule It may be positioned at a location where it is partially bonded. The heteroalkyl is an acyclic chain. Examples include -CH2-CH2-O-CH3, -CH2-CH2-NH-CH3, and -CH2- CH2-N(CH3)-CH3, -CH2-S-CH2-CH3, -CH2-S-CH2 , -S(O)-CH3, -CH2-CH2-S(O)2-CH3, -Si(CH3)3, This includes, but is not limited to, -O-CH3, -O-CH2-CH3, and -CN. For example, the most common -CH2-NH-OCH3 and -CH2-O-Si(CH3)3 There may be two or three heteroatoms in a row. The heteroalkyl portion consists of one heteroatom. It may contain a heteroalkyl atom (e.g., O, N, S, Si, or P). It contains two arbitrarily selected different heteroatoms (e.g., O, N, S, Si, or P). But that's fine too. The heteroalkyl portion consists of three arbitrarily selected different heteroatoms (e.g., O, N). It may contain S, Si, or P. The heteroalkyl moiety consists of four optionally different elements. It may also contain heteroatoms (e.g., O, N, S, Si, or P). Heteroalkyl The part consists of five arbitrarily selected different heteroatoms (e.g., O, N, S, Si, or P). It may contain. The heteroalkyl portion may contain up to 8 different heteroatoms of any choice (e.g., It may contain O, N, S, Si, or P. Heteroalkyl groups may be substituted or unsubstituted. It may be substituted. In the embodiment, the heteroalkyl group is substituted with at least one substituent. When a heteroalkyl group is substituted with multiple substituents, each substituent can be arbitrarily different. In the application form, the heteroalkyl group is substituted with at least one size-restricting substituent, and the heteroalkyl group When a loalkyl group is substituted with multiple size-restricting substituents, each size-restricting substituent is optional. It may differ. In the embodiment, the heteroalkyl group is substituted with at least one lower substituent. Furthermore, when a heteroalkyl group is substituted with multiple lower substituents, each lower substituent may be arbitrarily different. It is possible.

[0036] "Heteroalkenyl" is a compound of at least one carbon-carbon double bond and at least one Stable linear or branched chains containing heteroatoms (e.g., O, N, P, Si, and S) This refers to a chain, or a combination thereof, where nitrogen and sulfur atoms may be optionally oxidized. Nitrogen heteroatoms can optionally be quaternized. Heteroalkenyl groups can be substituted or unsubstituted. This is possible. In embodiments, the heteroalkenyl group is substituted with at least one substituent. When a heteroalkenyl group is substituted with multiple substituents, each substituent can be arbitrarily different. In the embodiment, the heteroalkenyl group is substituted with at least one size-restricting substituent. When a heteroalkenyl group is substituted with multiple size-restricting substituents, each size-restricting substituent is They can vary as needed. In the embodiment, the heteroalkenyl group is at least one lower substituent. When substituted, and the heteroalkenyl group is substituted with multiple lower substituents, each lower substituent is It can vary arbitrarily.

[0037] "Heteroalkynyl" is a compound of at least one carbon-carbon triple bond and at least one Stable linear or branched chains containing heteroatoms (e.g., O, N, P, Si, and S) This refers to a chain, or a combination thereof, where nitrogen and sulfur atoms may be optionally oxidized. The nitrogen heteroatom can optionally be quaternized. The heteroalkynyl group can be substituted or unsubstituted. This is possible. In embodiments, the heteroalkynyl group is substituted with at least one substituent. When a heteroalkynyl group is substituted with multiple substituents, each substituent can be arbitrarily different. In the embodiment, the heteroalkynyl group is substituted with at least one size-restricting substituent. When a heteroalkynyl group is substituted with multiple size-restricting substituents, each size-restricting substituent is They can vary as needed. In the embodiment, the heteroalkynyl group is at least one lower substituent. When substituted, and the heteroalkynyl group is substituted with multiple lower substituents, each lower substituent is It can vary arbitrarily.

[0038] The term "heteroalkylene" is used in particular when referring to a heteroalkylene, either by itself or as part of another substituent. Unless otherwise specified, it means, but is not limited to, a divalent radical derived from a heteroalkyl group. -CH2-CH2-S-CH2-CH2- and -CH2-S-CH2-CH2-NH As exemplified by -CH2-, for heteroalkylene groups, the heteroatom is also a chain. It may occupy either or both of the ends (e.g., alkylene oxy, alkylene dioxy (Xylamine, alkyleneamino, alkylenediamino, etc.). Furthermore, alkylene and he In the case of teloalkylene linking groups, the orientation of the linking group is implied by the direction in which the formula of the linking group is written. It is not. For example, the formula -C(O)2R'- is -C(O)2R'- and -R'C(O) 2- represents both. As stated above, heteroalkyl groups used herein are -C(O )R', -C(O)NR', ​​-NR'R'', -OR', -SR', and / or -S It contains groups such as O2R' that are bonded to the rest of the molecule via heteroatoms. After the list of alkyl groups, specific heteroalkyl groups, such as -NR'R'', are listed. If cited, the terms heteroalkyl and -NR'R'' are redundant but mutually exclusive. It will be understood that this is not the case. Rather, specific heteroalkyl groups are listed for clarification. Therefore, the term "heteroalkyl" in this specification refers to a specific heteroalkyl This should not be interpreted as excluding luquill groups, such as -NR'R''.

[0039] The term "heteroalkenylene" can refer to a compound, either by itself or as part of another substituent. Unless otherwise specified, this refers to divalent radicals derived from heteroalkenyls.

[0040] The term "heteroalkylylene" can refer to a compound, either by itself or as part of another substituent. Unless otherwise specified, this refers to divalent radicals derived from heteroalkylenes.

[0041] "Aryl" is formed by removing a hydrogen atom from a ring carbon atom, resulting in an aromatic monocyclic or This refers to radicals derived from polycyclic hydrocarbon ring systems. Aromatic monocyclic or polycyclic hydrocarbons. The ring system contains only hydrogen and carbon atoms from 6 to 18 carbon atoms, and a small portion of the rings in the ring system At least one of them is completely unsaturated, that is, it is a cyclic delocalization according to Hückel's theory. It contains a (4n+2)π electron system. Ring systems derived from the aryl group include benzene and fluorescein. It contains groups such as n, indan, indene, tetralin and naphthalene, but these Not limited to. Unless otherwise specified herein, the term "aryl" or "aryl" The prefix "ar-" (for example, "aralkyl") can optionally be alkyl, alkenyl, or alkini. Halogens, haloalkyls, cyano, nitro, aryl, aralkyl, aralkenyl, Aralkyl, cycloalkyl, heterocycloalkyl, heteroaryl, heteroaryl Alkyl, -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 (t is 1 or 2), -R b -S(O) t Ure a (t is 1 or 2), -R b -S(O) t R a (t is 1 or 2), o B-R b -S(O) t N(R a )2 (where t is 1 or 2), and each R a Independent And hydrogen, alkyl, haloalkyl, cycloalkyl, cycloalkylalkyl, ali AL (optionally substituted with one or more halogen groups), aralkyl, heterocycloalkyl , heteroaryl, or heteroarylalkyl, and each R b They are independent and directly connected A compound, linear, or branched alkylene or alkenylene chain, R c is a linear chain Alternatively, one or more branched alkylene or alkenylene chains selected from those. This means that it contains an aryl group substituted by a substituent. The group may be substituted or unsubstituted. In this embodiment, the aryl group may be at least one substituted When a group is substituted with an aryl group, and the aryl group is substituted with multiple substituents, each substituent can be arbitrarily different. In the embodiment, the aryl group is substituted with at least one size-restricting substituent, When a group is substituted with multiple size-restricting substituents, each size-restricting substituent is arbitrarily different. In this embodiment, the aryl group is substituted with at least one lower substituent, and aryl When a group is substituted with multiple lower substituents, each lower substituent can be arbitrarily different.

[0042] "Aryloxy" refers to a radical bonded via the oxygen atom of the formula -O-aryl. aryl is as defined above.

[0043] "Aralkyr" is formula -R c It refers to the aryl radical, R c This is defined as A above. The alkylene chain is, for example, methylene, ethylene, etc. The alkylene chain portion of the aralkyl group. The alkylene chain is optionally substituted as described above. The aryl portion can be optionally substituted with the aryl group as described above.

[0044] "Aralkyloxy" refers to a radical bonded via an oxygen atom in the formula -O-aralkyl. This refers to the term, and the term "alarkil" is as defined above.

[0045] "Aralkenyl" is derived from formula -R d - Refers to the aryl radical, R d is defined above This is an alkenylene chain. The aryl portion of the aralkenyl group can be optionally attached to the aryl group. The alkene chain portion of the aralkenyl group is optional. The alkenylene group is substituted as defined above.

[0046] "Aralkynyl" is represented by formula -R e - Refers to the aryl radical, R e This is defined above It is an alkylylene chain. The aryl portion of the aralkyl group can be arbitrarily attached to the aryl group. The substitution is as described above. The alkynylene chain portion of the aralkyl group can be optionally replaced. The alkynylene group is substituted as defined above.

[0047] "Cycloalkyl" refers to a stable, non-aromatic monocyclic compound consisting only of carbon and hydrogen atoms. This refers to polycyclic hydrocarbon radicals, which include condensation and ligation, which have 3 to 15 carbon atoms. Bridges or spirocycle systems are included. In certain embodiments, cycloalkyl groups number from 3 to 10. It contains carbon atoms. In other embodiments, the cycloalkyl contains 5 to 7 carbon atoms. Cycloalkyls are bonded to the rest of the molecule by single bonds. , saturated (i.e., containing only a single CC bond), or partially unsaturated (i.e., 1 It contains one or more double or triple bonds. Examples of monocyclic cycloalkyls include, for example, For example, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl , and cyclooctyl are included. In certain embodiments, the cycloalkyl group comprises 3 to 8 units. Contains carbon atoms (for example, C3-C8 cycloalkyl or C3-C8 cycloalkyl In other embodiments, the cycloalkyl group contains 3 to 7 carbon atoms (e.g., C3- (C7 cycloalkyl or C3-C7 cycloalkyl). In other embodiments, cycloalkyl Kill contains 3 to 6 carbon atoms (e.g., C3-C6 cycloalkyl or C3-C 6. Cycloalkyl. In other embodiments, the cycloalkyl comprises 3 to 5 carbon atoms. (For example, C3-C5 cycloalkyl or C3-C5 cycloalkyl). Other embodiments So, cycloalkyls contain 3 to 4 carbon atoms (for example, C3-C4 cycloalkyls). (C3-C4 cycloalkyl). Partially unsaturated cycloalkyls are called "cycloalkyl". Also called "kenyl". Examples of monocyclic cycloalkenyls include, for example, cyclopentenyl. This includes cyclohexenyl, cycloheptenyl, and cyclooctenyl. Examples of alkyl radicals include adamantyl, norbornyl (i.e., bicyclo[ 2.2.1] Heptanyl, norborneyl, dekalinyl, 7,7-dimethyl-bicyclo [2.2.1]heptanil, bicyclo[1.1.1]pentanil, spiro[3.3]heptanil This includes tanyl, spiro[4.4]nonanil, etc. Unless otherwise specified herein, The term "cycloalkyl" can optionally include alkyl, alkenyl, alkynyl, and ha Rogen, Haloalkyl, Cyano, Nitro, Aryl, Aralkyl, Aralkenyl, Aral Quinyl, cycloalkyl, heterocycloalkyl, heteroaryl, heteroaryl Kill, -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 (t is 1 or 2), -R b -S(O) t Ure a (t (is 1 or 2), -R b -S(O) t R a (t is 1 or 2), and -R b -S(O) t N(R a )2 (where t is 1 or 2), and each R a Independently, Hydrogen, alkyl, haloalkyl, cycloalkyl, cycloalkylalkyl, aryl ( (Optionally substituted with one or more halogen groups), aralkyl, heterocycloalkyl, hetero It is a loaryl or heteroarylalkyl, and each R bThey are independent, directly connected or R is a linear or branched alkylene or alkenylene chain, c is a linear or is one or more substitutions selected from branched alkylene or alkenylene chains. This means that it contains a cycloalkyl group substituted with a group. Therefore, cycloal The kill group may be substituted or unsubstituted. In the embodiment, the cycloalkyl group is at least If the cycloalkyl group is substituted with multiple substituents, each substitution The groups can be arbitrarily different. In the embodiment, the cycloalkyl group is at least one size-based When substituted with size-restricting substituents, and when a cycloalkyl group is substituted with multiple size-restricting substituents, each The size-restricting substituents can vary as desired. In this embodiment, the cycloalkyl group is at least When a cycloalkyl group is substituted with one lower substituent, and the cycloalkyl group is substituted with multiple lower substituents, Each lower substituent can be arbitrarily different.

[0048] "Cycloalkoxy" is a compound of -O-cycloalkyl groups bonded via the oxygen atom. The term refers to cycloalkyl, and cycloalkyl is defined as described above.

[0049] "Halo" or "halogen" refers to bromo, chloro, fluoro, or iodo substituents. vinegar.

[0050] "Haloalkyl" is defined as a group of one or more halogen radicals as described above. This refers to the alkyl radical defined above that is substituted.

[0051] "Haloalkoxy" is defined as a compound formed by one or more halogen radicals, as described above. This refers to the alkoxy radical defined above, which is substituted.

[0052] "Halocycloalkyl" is defined as one or more halogen radicals, as described above. This refers to the cycloalkyl radical defined above, which is substituted by [the specified term].

[0053] "Halocycloalkoxy" is defined as one or more halogenated radiocarbons as described above. This refers to the alkoxy radical defined above, which is substituted by the radical.

[0054] "Alkylhydroxyl" is defined as having one or more hydroxyl atoms as described above. This refers to the alkyl radical defined above, which is substituted by a dikal.

[0055] "Heterocycloalkyl" is a compound consisting of 2 to 12 carbon atoms, nitrogen, oxygen, and sulfur. This refers to a stable 3-18 member non-aromatic ring radical containing 1-6 selected heteroatoms. Unless otherwise specified herein, heterocycloalkyl groups are monocyclic, bicyclic, and These are tricyclic or tetracyclic ring systems, including fused ring systems, spirocyclic ring systems, or bridging ring systems. It contains. The heteroatoms in the heterocycloalkyl group are optionally oxidized. In this case, one or more nitrogen atoms are arbitrarily quaternized. Heterocycloalkyl groups are part Partially or completely saturated. In some embodiments, the heterocycloalkyl group is ring It is bonded to the rest of the molecule via any (or multiple) atoms of such heterozygotes. Examples of chloroalkyl groups include dioxolanil, thienyl[1,3]dithianil, and decahy. Droisoquinolyl, imidazolinyl, imidazolidinyl, isothiazolidinyl, isoxa Zolidinyl, Morpholinyl, Octahydroindolyl, Octahydroisoindolyl, 2 -Oxopiperazinil, 2-Oxopiperidinil, 2-Oxopyrrolidinil, Oxazoli Dinyl, piperidinyl, piperazinyl, 4-piperidonyl, pyrrolidinyl, pyrazolidinyl Luquinuclidinyl, thiazolidinyl, tetrahydrofuryl, trithianil, tetrahydrofuryl Dropyranil, thiomorpholinil, thiamorpholinil, 1-oxo-thiomorpholinil, This includes, but is not limited to, 1,1-dioxo-thiomorpholinyl. Unless otherwise specified in the details, the term "heterocycloalkyl" may optionally mean "a Lukyl, Alkenyl, Alkinyl, Halogen, Haloalkyl, Oxo, Thioxo, Cyano nitro, aryl, aralkyl, aralkenyl, aralkyl, cycloalkyl, hete Rocycloalkyl, heteroaryl, heteroarylalkyl, -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 ( t is 1 or 2), -R b -S(O) t Ure a (t is 1 or 2), -R b -S( O) t R a (t is 1 or 2) and -R b -S(O) t N(R a )2(t is 1 (and is 2), R a These are independently hydrogen, alkyl, haloalkyl, and cycloalkyl. Lukyl, cycloalkylalkyl, aryl, aralkyl, heterocycloalkyl, hetero It is a loaryl or heteroarylalkyl, and each R b They are independent, directly connected or is a linear or branched alkylene or alkenylene chain, and R c Also, linear chains or one or more selected from branched alkylene or alkenylene chains. This includes heterocycloalkyl radicals defined above that are substituted by substituents. This means that, in the embodiment, the heterocycloalkyl group may be substituted or unsubstituted. In the application form, the heterocycloalkyl group is substituted with at least one substituent, and the heterocycloalkyl group When a chloroalkyl group is substituted with multiple substituents, each substituent can be arbitrarily different. In this state, the heterocycloalkyl group is substituted with at least one size-restricting substituent, When a telocycloalkyl group is substituted with multiple size-restricting substituents, each size-restricting substituent These can vary as needed. In the embodiment, the heterocycloalkyl group is at least one lower Substituting with substituents, and when a heterocycloalkyl group is substituted with multiple lower substituents, each lower The tertiary substituents may vary as appropriate. In the embodiments used herein, the "heteroalkyl ring" The term "heterocycloalkyl ring" refers to a heterocycloalkyl ring.

[0056] A "heteroaryl" is a compound consisting of 1 to 17 carbon atoms and selected nitrogen, oxygen, and sulfur. Radicals derived from aromatic ring radicals with 5 to 18 members, containing 1 to 6 heteroatoms. This refers to a heteroaryl radical. As used herein, heteroaryl radicals are monocyclic, bicyclic, A tricyclic or tetracyclic ring system in which at least one of the rings in the ring system is completely unsaturated. This means that it includes a cyclic delocalized (4n+2)π-electron system according to Hückel's theory. Heteroaryls include fused ring systems or bridging ring systems. Heteroaryl groups The nitrogen atoms (or multiple atoms) are optionally oxidized. If present, one or more nitrogen atoms are optional. It is quaternized. Heteroaryls are the remainder of the molecule through any atom of the ring(s) It is bonded to the part. Unless otherwise specified herein, "heteroaryl" The terms used are, arbitrarily, alkyl, alkenyl, alkynyl, halo, haloalkyl, oxo, Thioxo, cyano, nitro, aryl, aralkyl, aralkenyl, aralkynyl, sic Roalkyl, heterocycloalkyl, heteroaryl, heteroarylalkyl, -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)O R 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 (t is 1 or 2), -R b -S(O) t Ure a (t is 1 or 2) ), -R b -S(O) t R a (t is 1 or 2) and -R b -S(O) t N(R a )2 (t is 1 or 2), R a These are independently hydrogen, alkyl, and halo Lukyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, heteroalkyl Each R is a r-alkyl, heteroaryl, or heteroarylalkyl, b It is independent These are directly bonded, linear, or branched alkylene or alkenylene chains, TsuR c The selected material is a linear or branched alkylene or alkenylene chain. The heteroaryl radical defined above is substituted by one or more substituents. It means "to include." Therefore, the heteroaryl group can be substituted or unsubstituted. In the embodiment, the heteroaryl group is substituted with at least one substituent, and the heteroaryl When the group is substituted with multiple substituents, each substituent can be arbitrarily different. In this embodiment, The teloaryl group is substituted with at least one size-restricted substituent, and the heteroaryl group When substituted with multiple size-restricting substituents, each size-restricting substituent can be arbitrarily different. In the application form, the heteroaryl group is substituted with at least one lower substituent, and the heteroaryl group is substituted with at least one lower substituent. When a rib group is substituted with multiple lower substituents, each lower substituent can be arbitrarily different.

[0057] "N heteroaryl" refers to a heteroaryl compound containing at least one nitrogen atom as defined above. A heteroaryl radical, where the bond site of the heteroaryl radical to the rest of the molecule is heteroaryl. This refers to the nitrogen atom-mediated structure within a loaryl radical. N-heteroaryl radicals are... Optionally, the heteroaryl radical is substituted as described above.

[0058] "C-heteroaryl" is a heteroaryl radical as defined above, and The binding site of the heteroaryl radical to the rest of the child is the carbon in the heteroaryl radical. This refers to structures mediated by elementary atoms. C-heteroaryl radicals are, arbitrarily, heteroaryl radicals. The term "Jical" will be replaced as described above.

[0059] "Heteroaryloxy" refers to a compound formed by bonding via the oxygen atom of the formula -O-heteroaryl. Radicals are defined as such, while heteroaryls are defined above.

[0060] "Heteroarylalkyl" is a compound of the formula -R c - Refers to a heteroaryl radical, R c teeth , an alkylene chain as defined above. The heteroaryl is a nitrogen-containing heteroaryl. In this case, the heteroaryl is optionally bonded to an alkyl radical by a nitrogen atom. The alkylene chain of the loarylalkyl group may optionally be defined above for the alkylene chain. As shown above, it can be arbitrarily substituted. The heteroaryl portion of a heteroarylalkyl group is hetero The aryl group can be substituted as arbitrarily as defined above.

[0061] "Heteroarylalkoxy" is a formula -OR c - Via the oxygen atom of the heteroaryl group This refers to the radical that is bound, where R is the alkylene chain as defined above. Heterozygous If the compound is a nitrogen-containing heteroaryl, the heteroaryl may optionally contain an alkyl group at the nitrogen atom. It is bonded to a radical. The alkylene chain of the heteroarylalkoxy group is optionally a The lucilene chain can be optionally substituted as defined above. Heteroaryl alcohols The heteroaryl portion of the cy group can be any as defined above for heteroaryl groups. It will be replaced with.

[0062] "Optional" or "optional" means the possibility that the following event or situation may occur. This may or may not occur, and this statement is intended to indicate whether the event or situation may or may not occur. It means that the aryl group is included. For example, "arbitrarily substituted" means that the aryl group is placed Whether replaced or not, this statement refers to the substituted aryl group and the substituted This means that it includes both aryl groups that do not have a group and those that do not.

[0063] In the embodiment, the above terms (for example, "alkyl", "alkenyl", "alkynyl") "heteroalkyl", "heteroalkenyl", "heteroalkyl", "cycloalkyl" Each of the following is: "heterocycloalkyl", "aryl", and "heteroaryl" This includes both substituted and unsubstituted forms of the radicals shown. The substituents are provided below.

[0064] As used herein, “substituent” means a group selected from the following parts: (A) Oxo, halogen, -CCl3, -CBr3, -CF3, -CI3, -CHCl 2, -CHBr2, -CHF2, -CHI2, -CH2Cl, -CH2Br, -CH2F , -CH2I, -OCCl3, -OCF3, -OCBr3, -OCI3, -OCHCl2 , -OCHBr2, -OCHI2, -OCHF2, -CN, -OH, -NH2, -COO H, -CONH2, -NO2, -SH, -SO3H, -OSO3H, -SO2NH2, - NHNH2, -ONH2, -NHC(O)NHNH2, -NHC(O)NH2, -NHS O2H, -NHC(O)H, -NHC(O)OH, -NHOH, -N3, unsubstituted alkyl (For example, C1-C8 alkyl, C1-C6 alkyl, or C1-C4 alkyl), non Substitutive alkenyls (e.g., C2-C8 alkenyls, C2-C6 alkenyls, or C2- C4 alkenyls), unsubstituted alkynyls (e.g., C2-C8 alkynyls, C2-C6 alkynyls) Quinyl (or C2-C4 alkynyl), unsubstituted heteroalkyl (e.g., 2-8 member heteroalkyl) (Roalkyl, 2-6 member heteroalkyl, or 2-4 member heteroalkyl), unsubstituted hetero Alkenyls (e.g., 3-8 member heteroalkenyls, 3-6 member heteroalkenyls, or 3 ~4-member heteroalkenyls), unsubstituted heteroalkynyls (e.g., 3-8 member heteroalkynyls) (Nyl, 3-6 member heteroalkynyl, or 3-4 member heteroalkynyl), unsubstituted cyclo Lukyl (for example, C3-C8 cycloalkyl, C3-C6 cycloalkyl, or C5- C6 cycloalkyl), unsubstituted heterocycloalkyl (e.g., 3-8 member heterocycloalkyl) Lukyl, 3-6 member heterocycloalkyl, or 5-6 member heterocycloalkyl), non-position Replacement aryl (e.g., C6-C) 10 Ariel, C 10 (aryl, or phenyl), also These are unsubstituted heteroaryls (e.g., 5-10 member heteroaryls, 5-9 member heteroaryls) , or 5-6 member heteroaryls), and (B) Alkyl (e.g., C) substituted with at least one substituent selected from the following 1-C 20 , C1-C 12 (C1-C8, C1-C6, C1-C4, or C1-C2) , alkenyl (for example, C2-C 20 , C2-C 12 , C2-C8, C2-C6, or C2-C4), alkynyl (e.g., C2-C 20 , C2-C 12 , C2-C8, C2- C6, or C2-C4), heteroalkyl (e.g., 2-20 member, 2-12 member, 2-8 member) (1 member, 2-6 members, 4-6 members, 2-3 members, or 4-5 members), heteroalkenyl (e.g., 3 (~20 members, 3~12 members, 3~8 members, 3~6 members, 4~6 members, or 4~5 members), heterogeneous Kinil (for example, 3-20 members, 3-12 members, 3-8 members, 3-6 members, 4-6 members, or 4- 5 members), cycloalkyl (e.g., C3-C 10 , C3-C8, C3-C6, C4-C6 , or C5-C6), heterocycloalkyl (e.g., 3-10 member, 3-8 member, 3-6 member) (member, 4-6 member, 4-5 member, or 5-6 member), aryl (e.g., C6-C) 12 , C6- C10 , or phenyl), or heteroaryl (e.g., 5-12 member, 5-10 member, (5-9 members, or 5-6 members) (i) Oxo, halogen, -CCl3, -CBr3, -CF3, -CI3, -CHC l2, -CHBr2, -CHF2, -CHI2, -CH2Cl, -CH2Br, -CH2 F, -CH2I, -OCCl3, -OCF3, -OCBr3, -OCI3, -OCHCl 2, -OCHBr2, -OCHI2, -OCHF2, -CN, -OH, -NH2, -CO OH, -CONH2, -NO2, -SH, -SO3H, -OSO3H, -SO2NH2, -NHNH2, -ONH2, -NHC(O)NHNH2, -NHC(O)NH2, -NH SO2H, -NHC(O)H, -NHC(O)OH, -NHOH, -N3, unsubstituted alkyl (For example, C1-C8 alkyl, C1-C6 alkyl, or C1-C4 alkyl), Unsubstituted alkenyls (e.g., C2-C8 alkenyls, C2-C6 alkenyls, or C2 -C4 alkenyls), unsubstituted alkynyls (e.g., C2-C8 alkynyls, C2-C6 alkynyls) Lukinyl (or C2-C4 alkynyl), unsubstituted heteroalkyl (e.g., 2-8 membered he) (Teloalkyl, 2-6 member heteroalkyl, or 2-4 member heteroalkyl), unsubstituted heteroalkyl Roalkenils (e.g., 3-8 member heteroalkenils, 3-6 member heteroalkenils, or 3-4 member heteroalkenyls, unsubstituted heteroalkynyls (e.g., 3-8 member heteroalkenyls) (Quinyl, 3-6 member heteroalkynyl, or 3-4 member heteroalkynyl), unsubstituted cyclo Alkyl (e.g., C3-C8 cycloalkyl, C3-C6 cycloalkyl, or C5 -C6 cycloalkyl), unsubstituted heterocycloalkyl (e.g., 3-8 member heterocyclo) Alkyl, 3-6 member heterocycloalkyl, or 5-6 member heterocycloalkyl), non Substitutive aryl (e.g., C6-C) 10 Ariel, C 10 (aryl or phenyl), or unsubstituted heteroaryls (e.g., 5-10 member heteroaryls, 5-9 member heteroaryls) (or 5-6 member heteroaryls), and (ii) an alkyl group substituted with at least one substituent selected from the following (e.g.) , C1-C 20 , C1-C 12 , C1-C8, C1-C6, C1-C4, or C1-C 2) Alkenyl (e.g., C2-C 20 , C2-C 12 , C2-C8, C2-C6, (C2-C4), alkynyl (for example, C2-C 20 , C2-C 12 , C2-C8, C 2-C6, or C2-C4), heteroalkyl (e.g., 2-20 member, 2-12 member, 2 (~8 members, 2~6 members, 4~6 members, 2~3 members, or 4~5 members), heteroalkenyl (e.g.) (3-20 members, 3-12 members, 3-8 members, 3-6 members, 4-6 members, or 4-5 members), heterozygous Alkinyl (for example, 3-20 members, 3-12 members, 3-8 members, 3-6 members, 4-6 members, or 4-5 member), cycloalkyl (e.g., C3-C 10 , C3-C8, C3-C6, C4- C6, or C5-C6), heterocycloalkyl (e.g., 3-10 member, 3-8 member, 3 (~6 members, 4~6 members, 4~5 members, or 5~6 members), aryl (e.g., C6-C) 12 , C 6-C 10 , or phenyl), or heteroaryl (e.g., 5-12 member, 5-10 (1 person, 5-9 people, or 5-6 people) (a) Oxo, halogen, -CCl3, -CBr3, -CF3, -CI3, -CH Cl2, -CHBr2, -CHF2, -CHI2, -CH2Cl, -CH2Br, -CH 2F, -CH2I, -OCCl3, -OCF3, -OCBr3, -OCI3, -OCHC l2, -OCHBr2, -OCHI2, -OCHF2, -CN, -OH, -NH2, -C OOH, -CONH2, -NO2, -SH, -SO3H, -OSO3H, -SO2NH2 , -NHNH2, -ONH2, -NHC(O)NHNH2, -NHC(O)NH2, -N HSO2H, -NHC(O)H, -NHC(O)OH, -NHOH, -N3, unsubstituted alcohol Kill (e.g., C1-C8 alkyl, C1-C6 alkyl, or C1-C4 alkyl) , unsubstituted alkenyls (e.g., C2-C8 alkenyls, C2-C6 alkenyls, or C 2-C4 alkenyls), unsubstituted alkynyls (e.g., C2-C8 alkynyls, C2-C6 Alkynyl (or C2-C4 alkynyl), unsubstituted heteroalkyl (e.g., 2-8 member) Heteroalkyl groups, 2-6 member heteroalkyl groups, or 2-4 member heteroalkyl groups), unsubstituted heteroalkyl groups Telalkenyls (for example, 3-8 member heteroalkenyls, 3-6 member heteroalkenyls, and (3-4 member heteroalkenyls), unsubstituted heteroalkenyls (e.g., 3-8 member heteroalkenyls) Lukinyl (3-6 member heteroalkynyl, or 3-4 member heteroalkynyl), unsubstituted cyclo cycloalkyl (e.g., C3-C8 cycloalkyl, C3-C6 cycloalkyl, or C 5-C6 cycloalkyl, unsubstituted heterocycloalkyl (e.g., 3-8 member heterocycloalkyl) (Roalkyl, 3-6 member heterocycloalkyl, or 5-6 member heterocycloalkyl), Unsubstituted aryls (e.g., C6-C) 10 Ariel, C 10(aryl or phenyl), Or unsubstituted heteroaryls (e.g., 5-10 member heteroaryls, 5-9 member heteroaryls) (or 5-6 member heteroaryls), and (b) an alkyl group substituted with at least one substituent selected from the following (e.g.) , C1-C 20 , C1-C 12 , C1-C8, C1-C6, C1-C4, or C1-C 2) Alkenyl (e.g., C2-C 20 , C2-C 12 , C2-C8, C2-C6, (C2-C4), alkynyl (for example, C2-C 20 , C2-C 12 , C2-C8, C 2-C6, or C2-C4), heteroalkyl (e.g., 2-20 member, 2-12 member, 2 (~8 members, 2~6 members, 4~6 members, 2~3 members, or 4~5 members), heteroalkenyl (e.g.) (3-20 members, 3-12 members, 3-8 members, 3-6 members, 4-6 members, or 4-5 members), heterozygous Alkinyl (for example, 3-20 members, 3-12 members, 3-8 members, 3-6 members, 4-6 members, or 4-5 member), cycloalkyl (e.g., C3-C 10 , C3-C8, C3-C6, C4- C6, or C5-C6), heterocycloalkyl (e.g., 3-10 member, 3-8 member, 3 (~6 members, 4~6 members, 4~5 members, or 5~6 members), aryl (e.g., C6-C) 12 , C 6-C 10 , or phenyl), or heteroaryl (e.g., 5-12 member, 5-10 (Member, 5-9 member, or 5-6 member): Oxo, Halogen, -CCl3, -CBr3, -CF 3, -CI3, -CHCl2, -CHBr2, -CHF2, -CHI2, -CH2Cl, -CH2Br, -CH2F, -CH2I, -OCCl3, -OCF3, -OCBr3, - OCI3, -OCHCl2, -OCHBr2, -OCHI2, -OCHF2, -CN, - OH, -NH2, -COOH, -CONH2, -NO2, -SH, -SO3H, -OSO 3H, -SO2NH2, -NHNH2, -ONH2, -NHC(O)NHNH2, -NH C(O)NH2, -NHSO2H, -NHC(O)H, -NHC(O)OH, -NHOH , -N3, unsubstituted alkyl (e.g., C1-C8 alkyl, C1-C6 alkyl, or C1-C4 alkyls), unsubstituted alkenyls (e.g., C2-C8 alkenyls, C2-C6 Alkenyls (or C2-C4 alkenyls), unsubstituted alkynyls (e.g., C2-C8 alkenyls), Lukinyl, C2-C6 alkynyl, or C2-C4 alkynyl), unsubstituted heteroalkyl (For example, 2-8 member heteroalkyl, 2-6 member heteroalkyl, or 2-4 member heteroalkyl) Alkyl), unsubstituted heteroalkenyl (e.g., 3-8 member heteroalkenyl, 3-6 member heteroalkenyl) Telalkenyls, or 3-4 member heteroalkenyls, unsubstituted heteroalkynyls (for example) For example, 3-8 member heteroalkynyl, 3-6 member heteroalkynyl, or 3-4 member heteroalkynyl Quinyl), unsubstituted cycloalkyl (e.g., C3-C8 cycloalkyl, C3-C6 cycloalkyl) (C5-C6 cycloalkyl, or C5-C6 cycloalkyl), unsubstituted heterocycloalkyl (e.g.) , 3-8 member heterocycloalkyl, 3-6 member heterocycloalkyl, or 5-6 member hetero Rocycloalkyl), unsubstituted aryl (e.g., C6-C 10 Ariel, C 10 Ariel , or phenyl), or unsubstituted heteroaryls (e.g., 5-10 member heteroaryls) (5-9 member heteroaryl, or 5-6 member heteroaryl).

[0065] The term "size-limited substituent" as used herein refers to a size-limited substituent. "subent)" or "size-limited substituent" The substituent group is selected from all substituents mentioned above. It means a group, and each substituted or unsubstituted alkyl is a substituted or unsubstituted C1-C 20 Alkyl Each substituted or unsubstituted alkenyl is a substituted or unsubstituted C2-C 20 In Alkenil Yes, each substituted or unsubstituted alkynyl is a substituted or unsubstituted C2-C 20 Alkinyl Each substituted or unsubstituted heteroalkyl group is a substituted or unsubstituted 2-20 member heteroalkyl group. Each substituted or unsubstituted heteroalkenyl is a substituted or unsubstituted 3-20 member heteroalkenyl. Each lucenyl is a substituted or unsubstituted heteroalkynyl with 3 to 20 members. It is a heteroalkynyl, and each substituted or unsubstituted cycloalkyl is a substituted or unsubstituted C3 -C8 cycloalkyl, and each substituted or unsubstituted heterocycloalkyl is either substituted or It is an unsubstituted 3- to 8-membered heterocycloalkyl, and each substituted or unsubstituted aryl is either substituted or is unsubstituted C6-C 10 It is an aryl, and each substituted or unsubstituted heteroaryl is substituted or These are unsubstituted 5-10 member heteroaryls.

[0066] "lower substituent" or "low substituent (low When used herein, "(er substituent group)" is used as "substituting The term "group" refers to a group selected from all the substituents described above, and each substituted or unsubstituted group is... Alkyls are substituted or unsubstituted C1-C8 alkyls, and each substituted or unsubstituted alkeni Alkenyl is a substituted or unsubstituted C2-C8 alkenyl, and each substituted or unsubstituted alkenyl is , substituted or unsubstituted C2-C8 alkynyl, and each substituted or unsubstituted heteroalkyl is , substituted or unsubstituted 2-8 member heteroalkyl, each substituted or unsubstituted heteroalkyl The 'L' is a substituted or unsubstituted 3- to 8-membered heteroalkenyl, and each substituted or unsubstituted heteroalkenyl Lukinyl is a substituted or unsubstituted 3- to 8-membered heteroalkynyl, and each substituted or unsubstituted sy Cloalkyls are substituted or unsubstituted C3-C7 cycloalkyls, each substituted or unsubstituted. Substituting heterocycloalkyls are substituted or unsubstituted 3- to 7-membered heterocycloalkyls, each Substituted or unsubstituted aryls are substituted or unsubstituted phenyls, and each substituted or unsubstituted he Terroraryls are substituted or unsubstituted 5- to 6-membered heteroaryls.

[0067] In some embodiments, each substituent described herein is at least It is substituted with one substituent. More specifically, in some embodiments, the compounds described herein Each substituted alkyl, substituted alkenyl, substituted alkynyl, and substituted heteroalkyl compound described in the product substituted heteroalkenyl, substituted heteroalkynyl, substituted cycloalkyl, substituted heterocyclic Roalkyl, substituted aryl, substituted heteroaryl, substituted alkylene, substituted alkenylene, Substituted alkylene, substituted heteroalkylene, substituted heteroalkene, substituted heteroalk Nylene, substituted cycloalkylene, substituted heterocycloalkyl, substituted arylene, and / Alternatively, the substituted heteroarylene is substituted with at least one substituent. In other embodiments, At least one or all of these bases is at least one size limiting Substituted with alternative groups. In other embodiments, at least one or all of these groups. However, it is substituted with at least one lower substituent.

[0068] In the embodiments of other compounds specified herein, each substituted or unsubstituted alkyl is substituted or unsubstituted. Substitution C1-C 20 It can be an alkyl group, and each substituted or unsubstituted alkenyl is substituted or unsubstituted. Exchange C1-C 20 It can be an alkenyl, and each substituted or unsubstituted alkenyl is substituted or unsubstituted. Exchange C1-C 20 It can be an alkynyl, and each substituted or unsubstituted heteroalkyl is substituted or These are unsubstituted 2-20 member heteroalkyls, and each substituted or unsubstituted heteroalkenyl is a substituted Alternatively, they are unsubstituted 3-20 member heteroalkenyls, each being a substituted or unsubstituted heteroalkenyl. These are substituted or unsubstituted 3-20 member heteroalkynyls, and each substituted or unsubstituted cyclo Lukyl is a substituted or unsubstituted C3-C8 cycloalkyl, and each substituted or unsubstituted hetero Rocycloalkyls are substituted or unsubstituted 3- to 8-membered heterocycloalkyls, and each substitution is Or non-substituted aryls, substituted or non-substituted C6-C 10 It is aryl and / or Each substituted or unsubstituted heteroaryl is a substituted or unsubstituted 5- to 10-membered heteroaryl. In some embodiments of the compounds described herein, each substituted or unsubstituted alkylene is placed Replacement or non-replacement C1-C 20 It is an alkylene, and each substituted or unsubstituted alkenylene is posed Replacement or non-replacement C1-C 20 It is an alkenylene, and each substituted or unsubstituted alkenylene is Substitute or non-substitute C1-C 20 Each alkynylene is a substituted or unsubstituted heteroalkylene. The compound is a substituted or unsubstituted 2-20 member heteroalkylene, and each substituted or unsubstituted heteroalkylene is a heteroalkylene. Alkenylenes are substituted or unsubstituted 3-20 member heteroalkenylenes, and each substitution or Unsubstituted heteroalkylenes are substituted or unsubstituted 3-20 member heteroalkylenes. Each substituted or unsubstituted cycloalkylene is a substituted or unsubstituted C3-C8 cycloalkylene. Each substituted or unsubstituted heterocycloalkyl is a substituted or unsubstituted 3- to 8-membered heterocycloalkyl. It is a cycloalkyl group, and each substituted or unsubstituted allylene is a substituted or unsubstituted C6-C 10 It is allylene, and / or each substituted or unsubstituted heteroalylene is substituted or unsubstituted. It is a 5-10 member heteroalylene.

[0069] In some embodiments, each substituted or unsubstituted alkyl is a substituted or unsubstituted C1-C It is an 8-alkyl group, and each substituted or unsubstituted alkenyl is a substituted or unsubstituted C2-C8 alkyl group. Each alkynyl is a substituted or unsubstituted C2-C8 alkynyl. Each substituted or unsubstituted heteroalkyl is a substituted or unsubstituted 2-8 member heteroalkyl. Each substituted or unsubstituted heteroalkenyl is a substituted or unsubstituted 3- to 8-member heteroalkenyl. Each is an alkenyl, and each substituted or unsubstituted heteroalkynyl has 3 to 8 members, either substituted or unsubstituted. It is a heteroalkynyl, and each substituted or unsubstituted cycloalkyl is a substituted or unsubstituted C3 -C7 cycloalkyl, and each substituted or unsubstituted heterocycloalkyl is either substituted or It is an unsubstituted 3- to 7-membered heterocycloalkyl, and each substituted or unsubstituted aryl is either substituted or is unsubstituted C6-C 10 It is an aryl and / or each substituted or unsubstituted heteroaryl The aryl is a substituted or unsubstituted 5- to 9-membered heteroaryl. In some embodiments, each aryl Substitutive or unsubstituted alkylenes are substituted or unsubstituted C1-C8 alkylenes, and each substitution or Unsubstituted alkenylenes are substituted or unsubstituted C1-C8 alkenylenes, and each substituted or Unsubstituted alkynylenes are substituted or unsubstituted C2-C8 alkynylenes, and each substituted or Unsubstituted heteroalkylenes are substituted or unsubstituted 2- to 8-membered heteroalkylenes, and each substitution Alternatively, unsubstituted heteroalkenylenes are substituted or unsubstituted 3- to 8-membered heteroalkenylenes. Each substituted or unsubstituted heteroalkylene is a substituted or unsubstituted 3-8 member heteroalkylene. It is nilen, and each substituted or unsubstituted cycloalkylene is substituted or unsubstituted C3-C7 cycloalkylene Each substituted or unsubstituted heterocycloalkyl is a roalkylene, and each substituted or unsubstituted heterocycloalkyl is substituted or unsubstituted 3 It is a ~7-membered heterocycloalkyl, and each substituted or unsubstituted arylene is substituted or unsubstituted. It is a substituted phenylene, and / or each substituted or unsubstituted heteroarylene is a substituted or The compound is an unsubstituted 5-6 member heteroarylene. In some embodiments, the compound is as described in this application. These are the chemical species described in (for example, the Examples section, figures, or tables below).

[0070] In the embodiment, substituted or unsubstituted moieties (e.g., substituted or unsubstituted alkyl, substituted or These are unsubstituted alkenyls, substituted or unsubstituted alkynyls, substituted or unsubstituted heteroalkyls, Substituted or unsubstituted heteroalkenyl, substituted or unsubstituted heteroalkynyl, substituted or non Substituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted ally , substituted or unsubstituted heteroaryls, substituted or unsubstituted alkylenes, substituted or unsubstituted alkylenes, substituted or unsubstituted Alkenylenes, substituted or unsubstituted alkylenes, substituted or unsubstituted heteroalkylenes, Substituted or unsubstituted heteroalkynylenes, substituted or unsubstituted heteroalkynylenes, substituted or Unsubstituted cycloalkylene, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted a Liylene and / or substituted or unsubstituted heteroalylenes are unsubstituted (for example, These are unsubstituted alkyl, unsubstituted alkenyl, unsubstituted alkynyl, and unsubstituted heteroalkyl, respectively. Unsubstituted heteroalkenyl, unsubstituted heteroalkynyl, unsubstituted cycloalkyl, unsubstituted Heterocycloalkyl, unsubstituted aryl, unsubstituted heteroaryl, unsubstituted alkylene, non Substituted alkenylenes, unsubstituted alkynylenes, unsubstituted heteroalkylenes, unsubstituted heteroalk Nylene, unsubstituted heteroalkylnylene, unsubstituted cycloalkylene, unsubstituted heterocycloalkyl (These are kill, unsubstituted allylene, and / or unsubstituted heteroalylene). In embodiments, Substituted or unsubstituted moieties (e.g., substituted or unsubstituted alkyl groups, substituted or unsubstituted alkenes) alkynyl, substituted or unsubstituted alkynyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted Heteroalkenyls, substituted or unsubstituted heteroalkynyls, substituted or unsubstituted cycloalkynyls aryl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, substituted or non Substituted heteroaryls, substituted or unsubstituted alkylenes, substituted or unsubstituted alkenylenes, Substitutable or unsubstituted alkylenes, substituted or unsubstituted heteroalkylenes, substituted or unsubstituted he Telalkenylenes, substituted or unsubstituted heteroalkylynylenes, substituted or unsubstituted cycloalkylynylenes Chelen, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted allylene, and / (or substituted or unsubstituted heteroalylenes) are substituted (for example, substituted a, respectively) Kill, substituted alkenyl, substituted alkynyl, substituted heteroalkyl, substituted heteroalkenyl, Substituted heteroalkynyl, substituted cycloalkyl, substituted heterocycloalkyl, substituted aryl substituted heteroaryl, substituted alkylene, substituted alkenylene, substituted alkylene, substituted he Teloalkylene, substituted heteroalkene, substituted heteroalkynylene, substituted cycloalkyl Len, substituted heterocycloalkyl, substituted allylene, and / or substituted heteroalylene be).

[0071] In the embodiment, the substituted portion (for example, substituted alkyl, substituted alkenyl, substituted alkynyl, Substituted heteroalkyl, substituted heteroalkenyl, substituted heteroalkynyl, substituted cycloalkyl , substituted heterocycloalkyl, substituted aryl, substituted heteroaryl, substituted alkylene, Substituted alkenylene, substituted alkylylene, substituted heteroalkylene, substituted heteroalkenylene substituted heteroalkylene, substituted cycloalkylene, substituted heterocycloalkyl, substituted a Leerene (and / or substituted heteroalylene) is substituted with at least one substituent. If the substitution is performed by multiple substituents, each substituent may be arbitrarily different. In the embodiment, if the substituted portion is replaced by multiple substituents, each substituent is different.

[0072] In the embodiment, the substituted portion (for example, substituted alkyl, substituted alkenyl, substituted alkynyl, Substituted heteroalkyl, substituted heteroalkenyl, substituted heteroalkynyl, substituted cycloalkyl , substituted heterocycloalkyl, substituted aryl, substituted heteroaryl, substituted alkylene, Substituted alkenylene, substituted alkylylene, substituted heteroalkylene, substituted heteroalkenylene substituted heteroalkylene, substituted cycloalkylene, substituted heterocycloalkyl, substituted a Leerene (and / or substituted heteroalylene) has at least one size-restricting substituent When substituted, and the substituted portion is replaced by multiple size-restricting substituents, each size-restricting substitution The groups may be arbitrarily different. In this embodiment, the substitution portion consists of multiple size-limiting substituents. If substituted, each size-restricting substituent will be different.

[0073] In the embodiment, the substituted portion (for example, substituted alkyl, substituted alkenyl, substituted alkynyl, Substituted heteroalkyl, substituted heteroalkenyl, substituted heteroalkynyl, substituted cycloalkyl , substituted heterocycloalkyl, substituted aryl, substituted heteroaryl, substituted alkylene, Substituted alkenylene, substituted alkylylene, substituted heteroalkylene, substituted heteroalkenylene substituted heteroalkylene, substituted cycloalkylene, substituted heterocycloalkyl, substituted a Leerenes (and / or substituted heteroalylenes) are substituted with at least one lower substituent. Furthermore, when the substitution is performed by multiple lower substituents, each lower substituent is arbitrarily different. This may also be the case. In the embodiment, if the substituted portion is substituted with multiple lower substituents, each lower substituent The substitution basis is different.

[0074] In the embodiment, the substituted portion (for example, substituted alkyl, substituted alkenyl, substituted alkynyl, Substituted heteroalkyl, substituted heteroalkenyl, substituted heteroalkynyl, substituted cycloalkyl , substituted heterocycloalkyl, substituted aryl, substituted heteroaryl, substituted alkylene, Substituted alkenylene, substituted alkylylene, substituted heteroalkylene, substituted heteroalkenylene substituted heteroalkylene, substituted cycloalkylene, substituted heterocycloalkyl, substituted a Lylene and / or substituted heteroalylene) have at least one substituent, size limitations Substituting with a substituent or lower substituent, the substituted portion is a substituent, a size-limiting substituent, and If substituted with multiple groups selected from lower substituents, each substituent, size limiting substituent , and / or lower substituents may be arbitrarily different. In the embodiment, the substitution portion The site is substituted with multiple groups selected from substituents, size-limiting substituents, and lower substituents. In combination, each substituent, size-limiting substituent, and / or lower substituent are different.

[0075] A "tautomer" is a molecule in which a proton shift occurs from one atom to another atom within the same molecule. This refers to molecules that can perform tautomerization. In certain embodiments, the compounds presented herein are tautomers. It exists. In situations where tautomerism is possible, a chemical equilibrium of tautomers exists. The exact body ratio depends on several factors, including physical conditions, temperature, solvent, and pH. Some examples of tautomeristic equilibrium include: [ka]

[0076] "Pharmacologically acceptable salts" include both acid and base addition salts. Any pharmaceutically acceptable salt of any of the listed compounds may be any pharmaceutically appropriate salt form. It is intended to include the preferred pharmaceutically acceptable compounds described herein. Salts are pharmaceutically acceptable acid addition salts and pharmaceutically acceptable base addition salts.

[0077] A "pharmaceutically acceptable acid addition salt" is one that retains the biological effects and properties of a free base. It is salt, and is not biologically undesirable or otherwise undesirable. Furthermore, hydrochloric acid, hydrobromic acid, sulfuric acid, nitric acid, phosphoric acid, hydroiodic acid, hydrofluoric acid, phosphorus phosphate. This refers to salts formed from inorganic acids such as acids. These include aliphatic mono-dicarboxylic acids and phenyl-substituted aliphatic acids. Alkanic acid, hydroxyalkanoic acid, alkanedioic acid, aromatic acid, aliphatic and aromatic sulfoacid. This also includes salts formed from organic acids such as acetic acid, trifluoroacetic acid, pro-acetic acid, etc. Pionic acid, glycolic acid, pyruvic acid, oxalic acid, maleic acid, malonic acid, succinic acid, f Maric acid, tartaric acid, citric acid, benzoic acid, cinnamic acid, mandelic acid, methanesulfonic acid, ethanol This includes sulfonic acid, p-toluenesulfonic acid, salicylic acid, etc. Therefore, examples Typical salts include sulfates, pyrosulfates, bicarbonates, sulfites, bisulfites, nitrates, and nitrates. Phosphates, monophosphates, diphosphates, metaphosphates, pyrophosphates, chlorides, bromides Substances, iodide, acetate, trifluoroacetate, propionate, caprylate, isobutyric acid Salt, oxalate, malonate, succinate, suberinate, sebacinate, fumarate, Maleate, mandelate, benzoate, chlorobenzoate, methylbenzoate, dinitrate Torobenzoate, phthalate, benzenesulfonate, toluenesulfonate, phenyl Examples include acetates, citrates, lactates, malates, tartrates, and methanesulfonates. It is also intended for use with salts of amino acids such as alginates, glucons, and galacturons. (For example, Berge S. et al., “Pharmaceutical al Salts,”Journal of Pharmaceutical Science See nce, 66:1-19 (1997). Acid addition salts of basic compounds are free. It is prepared by contacting a base form with a sufficient amount of the desired acid to produce a salt.

[0078] "Pharmacologically acceptable base addition salts" are those that are not biologically undesirable, or This refers to salts that retain the biological effects and properties of free acids, which are not other undesirable. These salts are prepared by adding an inorganic or organic base to a free acid. In terms of application, pharmaceutically acceptable base addition salts are metals or amines, such as alkali metals. and are formed from alkaline earth metals or organic amines. As salts derived from inorganic bases Sodium, potassium, lithium, ammonium, calcium, magnesium, iron, ammonium Examples include, but are not limited to, lead, copper, manganese, and aluminum salts. The salts derived from the group include salts of primary, secondary, and tertiary amines, and naturally occurring compounds. Substituted amines including substituted amines, cyclic amines, and basic ion exchange resins, such as isopropyl alcohol. Pyramine, trimethylamine, diethylamine, triethylamine, tripropylamine Ethanolamine, diethanolamine, 2--dimethylaminoethanol, 2-- Diethylaminoethanol, dicyclohexylamine, lysine, arginine, histidine caffeine, procaine, N,N-dibenzylethylenediamine, chloroprocaine, Hydrabamine, choline, betaine, ethylenediamine, ethylenedianiline, N-methyl Glucamine, glucosamine, methylglucamine, theobromine, purine, piperazine, pi This includes, but is not limited to, peridine, N-ethylpiperidine, and polyamine resins. No. See Berge et al. above.

[0079] In some embodiments, a "prodrug" is defined as a substance that, under physiological conditions or as a solvent. The solution indicates that the compound is converted into the biologically active compound described herein. It means that. Therefore, the term "prodrug" is pharmaceutically acceptable biologically. This refers to a precursor of an active compound. A prodrug is typically a precursor of an active compound. Although inactive, it can be converted to an active compound in vivo, for example, by hydrolysis. Lugg compounds often exhibit solubility, tissue compatibility, or delayed release properties in mammalian organisms. It offers advantages (for example, Bundgard, H., Design of Prodru See gs, Amsterdam: Elsevier, 1985.) Prodra The discussion also includes Higuchi, T. et al., “Pro-drugs as Novel Delivery Systems,”ACSSymposium Series, Vol. 14, and Roche, EB, ed. Biorevers ible Carriers in Drug Design,Oxford:Perg. It can also be found in Amon Press, 1987.

[0080] The term "prodrug" also refers to the administration of such prodrugs to mammalian subjects. This means that it sometimes contains any covalently bonded carrier that releases an active compound in vivo. As described herein, the prodrug of the active compound is present in the active compound. When modifying a functional group, the modification is performed either by a predetermined procedure or in vivo to make the functional group more reactivity. It can be prepared in a way that the compound is cleaved into its components. Prodrugs include prodrugs of the active compound. When administered to mammals, the hydroxyl group, amino group, or mercapto group is of any They bond to the base, forming a free hydroxyl group, a free amino group, or a free mercapto group, respectively. It contains compounds that cleave in a certain way. Examples of prodrugs include active compounds and other compounds containing alcohol. This includes, but is not limited to, kohl acetate, formate, and benzoate derivatives. It is not determined.

[0081] "Pharmacologically acceptable solvates" refer to substance compositions in a solvent-added form. In that embodiment, the solvate comprises either a stoichiometric or non-stoichiometric amount of solvent. It is formed during the manufacturing process using pharmaceutically acceptable solvents such as water and ethanol. When the medium is water, a "hydrate" is formed, or when the solvent is an alcoholic, an alcohol is formed. Salts are formed. The solvates of the compounds described herein are formed during the process described herein. The compounds provided herein are prepared or formed as appropriate. It can exist in any of the Japanese forms.

[0082] The terms "allosteric site" and "allosteric connection site" are used in reference to orthosteology. A LIC binding site refers to a locally distinct ligand binding site.

[0083] The terms "orthosteric site" and "orthosteric binding site" refer to receptors. This refers to the primary binding site of a receptor recognized by its endogenous ligand or agonist. For example, the orthosteric site of the muscarinic acetylcholine M1 receptor is acetylcholine This is the site where the n connects.

[0084] The term "ligand" refers to a substance that binds to or associates with a receptor to form a complex and exerts a biological effect. Ligands are natural or synthetic molecules that can mediate, prevent, or modify the fruit. The term "allosteric modifier" refers to an allosteric modifier, inhibitor, activator, or agonist. This means including antagonists, natural substrates, and analogues of natural substrates.

[0085] The terms "natural ligand" and "endogenous ligand" refer to naturally occurring ligands that bind to a receptor. It refers to the ligand present.

[0086] In the embodiment, the terms "inhibitor," "inhibition," and "inhibiting" are used in relation to protein-inhibitor interactions. Terms such as "inhibit" and "suppress" are used to compare the activity or function of a protein in the absence of an inhibitor. This means that it negatively affects (e.g., reduces) the activity or function of a protein. In the embodiment, inhibition is defined as the protein concentration or level compared to the protein concentration or level in the absence of the inhibitor. to have a negative effect on protein concentration or level (for example, to reduce it) This means (to reduce). In embodiments, inhibition refers to the reduction of a disease or the symptoms of a disease. In terms of application, inhibition refers to a reduction in the activity of a specific protein target. Therefore, inhibition is , at least partially, partially or completely blocking the stimulus, signaling or To reduce, inhibit, or delay the activation of enzyme activity or protein levels. This includes causing, inactivating, desensitizing, or downregulating the substance. In this embodiment, inhibition refers to a reduction in the activity of the target protein due to direct interaction. (For example, the inhibitor binds to the target protein.) In this embodiment, inhibition is an indirect phase. This refers to a reduction in the activity of a target protein due to interaction (for example, an inhibitor reduces the activity of the target protein). (It binds to proteins that activate proteins, thereby inhibiting the activation of the target protein.) .

[0087] In the embodiment, the terms "inhibitor," "suppressor," "antagonist," or "downregulator" may be used. The term "child" refers to a given gene or protein whose expression or activity is detected to be reduced. It is synonymous with any substance that can be used to kill. An antagonist is a substance that can kill in the absence of an antagonist. Compared to the control, expression or activity was increased by 10%, 20%, 30%, 40%, 50%, and 60%. It can be reduced by 70%, 80%, 90%, or more. In certain cases... Expression or activity is 1.5 times higher than expression or activity in the absence of the antagonist. Two times, three times, four times, five times, ten times, or even lower.

[0088] In the embodiments, the term “expression” includes transcription, post-transcriptional modification, translation, post-translational modification, and This includes any steps involved in polypeptide production, including but not limited to secretion. Expression is detected using conventional techniques for detecting proteins (e.g., ELISA, Western blot). Detected using methods such as immunofluorescence, flow cytometry, immunofluorescence, and immunohistochemistry. obtain.

[0089] The term "mAChR M1 receptor antagonist" refers to the mAChR M1 receptor... It partially or completely inhibits the effect of the opposing agonist (e.g., acetylcholine). It refers to any exogenously administered compound or drug that can reverse or reverse the effects of the drug. This term refers to an antagonist, a partial antagonist, and a negative allosteric modifier. It includes compounds or drugs characterized as or described as children. For example, m AChR M1 receptor antagonists target orthosteric or allosteric regions. They can mediate those effects by binding to the receptor site, or by the receptor's activity. It can interact at unique binding sites that are not normally involved in the biological regulation of [unclear text]. Therefore, mAChR M1 receptor antagonists are found in animals, especially mammals, such as humans. In the presence or absence of acetylcholine or another agonist, mACh It directly or indirectly inhibits the activity of the RM1 receptor. In various embodiments, mAChR M1 receptor antagonists are activated in the presence of extracellular acetylcholine in intracellular mAChR M It reduces the activity of receptor 1. In some embodiments, "mAChR M1 receptor annealing Compounds that are "tagonists" are "mAChR M1 receptor competitive antagonists," and "m AChR M1 receptor non-competitive antagonist, mAChR M1 receptor partial antagonist It is a "tagonist," or a "negative allosteric modifier of the mAChR M1 receptor." Contains compounds.

[0090] The term "mAChR M1 receptor competitive antagonist" refers to an antagonist that activates the receptor. Any This refers to compounds or drugs administered exogenously. Therefore, competitive antagonists are m It interacts with the AChR M1 receptor and has an endogenous ligand, acetamine, for binding to the receptor. A receptor that competes with chilcholine and transmits intracellular signals in response to the binding of endogenous ligands. It can reduce their abilities.

[0091] The term "mAChR M1 receptor non-competitive antagonist" refers to mAChR M1 Any exogenously administered substance that binds to a site other than the orthosteric binding site of the receptor This refers to a compound or drug, such as an agonist (e.g., acetyl) targeting the mAChR M1 receptor. It can partially or completely inhibit or reverse the effects of choline. Therefore, non-competitive antagonists interact with the mAChR M1 receptor and endogenous rigor It reduces the binding of the ligand acetylcholine to its receptor and / or the endogenous ligand It can reduce the ability of receptors to transmit intracellular signals in response to binding.

[0092] The term "mAChR M1 partial antagonist" is an orthosteric or atypical term. It can bind to the rosteric site, but the effect of binding is that of an agonist, such as acetyl A choice that partially blocks the effect of the mAChR M1 receptor response to lucorine. This refers to a compound or drug administered exogenously. Therefore, a partial antagonist is It can interact with the mAChR M1 receptor, but not with agonists such as acetylcholine. It is not possible to completely inhibit the response of the mAChR M1 receptor.

[0093] The term "negative allosteric modifier of mAChR M1" is used in animals, particularly mammals. In substances, such as humans, in the presence of acetylcholine or another agonist, mACh The role of binding to allosteric sites that directly or indirectly inhibit the activity of the RM1 receptor. This refers to compounds or drugs administered exogenously. For example, intended to limit this disclosure to the present. Although it does not do so, the negative allosteric modifier of selective muscarinic M1 is muscarinic. By preferentially binding to the phospho M1 receptor and acting as a non-competitive antagonist, This can reduce muscarinic M1 signaling. In one embodiment, mAChR Negative allosteric modifiers of the M1 receptor are present in the intracellular space in the presence of extracellular acetylcholine. It reduces the activity of the mAChR M1 receptor.

[0094] In the embodiments, terms such as "selective" or "selectivity" relating to a compound or drug are specific The activity of a molecular target (e.g., protein, enzyme, etc.) is superior to that of one or more different molecular targets. This refers to the ability of a compound or drug to increase or decrease (for example, muscarinic a Compounds that exhibit selectivity for the cetylcholine M1 receptor (mAChR M1) are other compounds. (Preferentially inhibits mAChR M1 over scarinic receptors). In embodiments, "Mus "Carinic acetylcholine M1 receptor selective compound" or "mAChR M1 selective compound" The substance exhibits selectivity for muscarinic acetylcholine M1 receptors (mAChR M1). This refers to a compound that possesses (for example, a compound described herein). In embodiments, a compound (for example) If the compounds described herein contain one or more mAChR M2, M3, M4, or M Approximately 5 receptors are more effective than the muscarinic acetylcholine M1 receptor (mAChR M1) It is 5 times, 10 times, 20 times, 30 times, 40 times, 50 times, or approximately 100 times more selective. In terms of form, a compound (for example, the compounds described herein) is one or more mAChR M2 , muscarinic acetylcholine M1 receptor (mAC) rather than M3, M4, or M5 receptors At least 5 times, 10 times, 20 times, 30 times, 40 times, 50 times compared to hR M1), and It is at least 100 times more selective.

[0095] The terms "subject" or "patient" include mammals. Examples of mammals include: Any member of the mammal class: humans, non-human primates such as chimpanzees, and others Great apes and primates; farm animals such as cattle, horses, sheep, goats, and pigs; rabbits, dogs, and domestic animals such as cats; experimental animals including rodents such as rats, mice, and guinea pigs. Examples include objects, but are not limited to these. In one aspect, the subject is a human being.

[0096] As used herein, “treatment” or “to treat” or “alleviate” or “improve” These terms are used interchangeably herein. These terms refer to therapeutic benefits and / or Apps for obtaining beneficial or desired results, including but not limited to preventive benefits. This refers to a roach. "Therapeutic benefit" means the eradication or improvement of the underlying disease being treated. Furthermore, the therapeutic benefits are even though the patient still suffers from the underlying disease. Furthermore, to observe improvement in the patient, the eradication of one or more physiological symptoms associated with the underlying disease. Or achieved by mitigation. For preventive benefit, the composition prevents the development of certain diseases. Patients at risk of developing this disease, or those who have not been diagnosed with this disease but have one or more symptoms of the disease It is administered to patients who report physical symptoms.

[0097] When used herein, "EC 50 " is a biological process, or protein, 50% utilization of process components including subunits, organelles, and ribonucleoproteins. This refers to the concentration of a substance (e.g., a compound or drug) necessary for sexualization or enhancement. This is intended. For example, EC 50 In in vitro assays, baseline and latest This can refer to the concentration of an agonist that elicits an intermediate response between a large response and several others. In this embodiment, the in vitro assay system either endogenously expresses the target of interest or This refers to cell lines transfected with an appropriate expression vector that directs the recombinant expression of the target. Use it.

[0098] When used herein, "IC 50 " is a biological process, or protein, It inhibits process components, including subunits, organelles, and ribonucleoproteins, by 50%. It is intended to refer to the concentration of a substance (e.g., a compound or drug) necessary to cause harm. For example, IC 50 This is half (50%) of the maximum amount of the substance determined by the appropriate assay. This refers to the inhibitory concentration (IC). For example, the IC of the mAChR M1 receptor. 50 is in vitro It can be determined by the Issei system.

[0099] II. Compounds This disclosure relates to the antagonist of the muscarinic acetylcholine M1 receptor (mAChR M1). The present invention provides compounds that are a stock. These compounds, and compositions containing these compounds, It is useful for the treatment or prevention of neurological disorders. In some embodiments, as described herein These compounds are useful for treating multiple sclerosis.

[0100] In one embodiment, a compound, or a pharmaceutically acceptable salt or solvate thereof, is of the formula Having the structure of (IA-1) or (IB-1), [ka] During the ceremony, X is bonded, -C(R 9 )(R 10 )-,-N(R 11 )-, -O-, -S(O) n- -CH2N(R 11 )-, substituted or unsubstituted alkylenes (e.g., C1-C8, C1 -C6, C1-C4, or C1-C2), substituted or unsubstituted alkenylenes (e.g., C2-C8, C2-C6, or C2-C4), substituted or unsubstituted alkynylenes (for example) (For example, C2-C8, C2-C6, or C2-C4), substituted or unsubstituted heteroalkylates (For example, 2-8 members, 2-6 members, 4-6 members, or 2-3 members), substitution or non-substitution. Telalkenylenes (e.g., 3-8 member, 3-6 member, or 4-6 member), or substitution or These are unsubstituted heteroalkylenes (e.g., 3-8 member, 3-6 member, or 4-6 member), Y is a substituted or unsubstituted alkylene (e.g., C1-C8, C1-C6, C1-C4) , or C1-C2), substituted or unsubstituted alkenylenes (e.g., C2-C8, C2- C6, or C2-C4), or substituted or unsubstituted heteroalkylenes (e.g., 2- (8 members, 2-6 members, 4-6 members, or 2-3 members) R 1 but, [ka] In the formula, ring A can optionally be hydroxyl, halogen, cyano, or -N(R 14 )(R 15 ), substituted or unsubstituted alkyl (C1-C8, C1-C6, C1-C4 or C1 -C2), substituted or unsubstituted alkoxys (e.g., C1-C8, C1-C6, C1-C) 4, or C1-C2), substituted or unsubstituted haloalkyl (e.g., C1-C8, C1 -C6, C1-C4, or C1-C2), substituted or unsubstituted haloalkoxy (e.g.) (C1-C8, C1-C6, C1-C4, or C1-C2), substitution or non-substitution Rhalkyl (e.g., C3-C8, C3-C6, C4-C6, or C5-C6), substitution Or unsubstituted cycloalkoxys (e.g., C3-C8, C3-C6, C4-C6, and (C5-C6), substituted or unsubstituted halocycloalkyl (e.g., C3-C8, C3- C6, C4-C6, or C5-C6), substituted or unsubstituted halocycloalkoxy (e.g.) For example, C3-C8, C3-C6, C4-C6, or C5-C6), substituted or not substituted. Heterocycloalkyl groups (e.g., 3-8 member, 3-6 member, 4-6 member, 4-5 member, or 5- 6-membered aryls), substituted or unsubstituted aryls (e.g., C6-C 10 (or phenyl), substitutions also Alternatively, unsubstituted heteroaryls (e.g., 5-10 member, 5-9 member, or 5-6 member), -S (O) n (R 16 ), or heteroaryl rings or heterocyclic rings substituted with -SF5 It is a chloroalkyl ring, and the heteroaryl or heterocycloalkyl ring is O, N, or It contains one, two, or three heteroatoms selected from the group consisting of S, R 2 However, hydrogen, deuterium, halogen, hydroxyl, substituted or unsubstituted alkyl (C1 -C8, C1-C6, C1-C4 or C1-C2), substituted or unsubstituted alkoxy( For example, C1-C8, C1-C6, C1-C4, or C1-C2), substitution or non-placement. Conversion haloalkyls (e.g., C1-C8, C1-C6, C1-C4, or C1-C2), Substituted or unsubstituted haloalkoxys (e.g., C1-C8, C1-C6, C1-C4, etc.) (C1-C2), substituted or unsubstituted cycloalkyl (e.g., C3-C8, C3-C) 6, C4-C6, or C5-C6), substituted or unsubstituted cycloalkoxys (e.g., C3-C8, C3-C6, C4-C6, or C5-C6), substituted or unsubstituted haloth Chloalkyl (e.g., C3-C8, C3-C6, C4-C6, or C5-C6), Substitutable or unsubstituted halocycloalkoxys (e.g., C3-C8, C3-C6, C4-C6) , or C5-C6), substituted or unsubstituted alkylhydroxyl (e.g., C1-C8) (C1-C6, C1-C6, or C1-C2), substituted or unsubstituted heterocycloal Kill (for example, 3-8 members, 3-6 members, 4-6 members, 4-5 members, or 5-6 members), replace k is an unsubstituted aryl (for example, C6-C 10 (or phenyl), or substituted or unsubstituted. These are heteroaryl compounds (e.g., 5-10 member, 5-9 member, or 5-6 member), R 3 However, halogens, substituted or unsubstituted alkyl (C1-C8, C1-C6, C1-C 4 or C1-C2), substituted or unsubstituted alkoxy (e.g., C1-C8, C1-C) 6, C1-C4, or C1-C2), substituted or unsubstituted haloalkyl (e.g., C1 -C8, C1-C6, C1-C4, or C1-C2), substituted or unsubstituted haloalcohols Xy (for example, C1-C8, C1-C6, C1-C4, or C1-C2), substitution or This refers to unsubstituted cycloalkyl groups (e.g., C3-C8, C3-C6, C4-C6, or C5- C6), substituted or unsubstituted cycloalkoxys (e.g., C3-C8, C3-C6, C4) -C6, or C5-C6), substituted or unsubstituted halocycloalkyl (e.g., C3- C8, C3-C6, C4-C6, or C5-C6), substituted or unsubstituted halocycloa Lucoxylation (e.g., C3-C8, C3-C6, C4-C6, or C5-C6), substitutions are also possible. or unsubstituted alkylhydroxyl (for example, C1-C8, C1-C6, C1-C6, (C1-C2), substituted or unsubstituted heterocycloalkyl (e.g., 3-8 member, 3- 6-membered, 4-6-membered, 4-5-membered, or 5-6-membered), substituted or unsubstituted aryls (for example, C6-C 10 (or phenyl), or substituted or unsubstituted heteroaryls (e.g., 5) (~10 members, 5-9 members, or 5-6 members), or R 2 and R 3 They are connected, In particular, halogens, substituted or unsubstituted alkyls (e.g., C1-C8, C1-C6, C1 -C4, or C1-C2), or substituted or unsubstituted cycloalkyl (e.g., C3 Cycloalkyls substituted with -C8, C3-C6, C4-C6, or C5-C6 (e.g.) For example, C3-C8, C3-C6, C4-C6, or C5-C6) or heterocyclo Alkyl (e.g., 3-8 member, 3-6 member, 4-6 member, 4-5 member, or 5-6 member) rings form accomplish, R 4 and R 5 These independently consist of hydrogen, deuterium, halogens, and substituted or unsubstituted alkyl groups. Selected from (for example, C1-C8, C1-C6, C1-C4, or C1-C2), Or R 3 and R 4 These are linked together, and optionally, halogens, substituted or unsubstituted alkyl groups ( For example, C1-C8, C1-C6, C1-C4, or C1-C2), or substitution or This refers to unsubstituted cycloalkyl groups (e.g., C3-C8, C3-C6, C4-C6, or C5- Cycloalkyls substituted with C6 (e.g., C3-C8, C3-C6, C4-C6, (C5-C6) or heterocycloalkyl (e.g., 3-8 member, 3-6 member, 4-6 member) Forming a ring (with 4-5 members, or 5-6 members), or R 4 and R 5 They are linked together, any in addition, halogens, substituted or unsubstituted alkyls (e.g., C1-C8, C1-C6, C1- C4, or C1-C2), or substituted or unsubstituted cycloalkyl (e.g., C3- Cycloalkyls substituted with C8, C3-C6, C4-C6, or C5-C6 (for example) (C3-C8, C3-C6, C4-C6, or C5-C6) or heterocycloa Lukil (for example, 3-8 members, 3-6 members, 4-6 members, 4-5 members, or 5-6 members) forms rings. death, R 6 and R 7 These independently consist of hydrogen, deuterium, halogens, and substituted or unsubstituted alkyl groups. Selected from (for example, C1-C8, C1-C6, C1-C4, or C1-C2), Or R 3 and R 7 These are linked together, and optionally, halogens, substituted or unsubstituted alkyl groups ( For example, C1-C8, C1-C6, C1-C4, or C1-C2), or substitution or This refers to unsubstituted cycloalkyl groups (e.g., C3-C8, C3-C6, C4-C6, or C5- Cycloalkyls substituted with C6 (e.g., C4-C8, C4-C6, or C5-C) 6) Or heterocycloalkyl (e.g., 4-8 member, 4-6 member, 4-5 member, or 5 Forms a ring (~6 members), or R 4 and R 6 They are linked together, and optionally, halogens can be substituted. or unsubstituted alkyl (e.g., C1-C8, C1-C6, C1-C4, or C1-C2) ), or substituted or unsubstituted cycloalkyls (e.g., C3-C8, C3-C6, C4 Cycloalkyls substituted with -C6 or C5-C6 (e.g., C4-C8, C4- C6, or C5-C6) or heterocycloalkyl (e.g., 4-8 member, 4-6 member) , forming a ring (4-5 members, or 5-6 members), or R 5 and R 7 They are linked, and the combination form, R 8 but, [ka] And, R 9 and R 10 These independently consist of hydrogen, deuterium, halogen, substituted or unsubstituted alkyl groups. (For example, C1-C8, C1-C6, C1-C4, or C1-C2), substitution or non Substitutive alkoxys (e.g., C1-C8, C1-C6, C1-C4, or C1-C2), Substituted or unsubstituted haloalkyls (e.g., C1-C8, C1-C6, C1-C4, and (C1-C2), substituted or unsubstituted haloalkoxys (e.g., C1-C8, C1-C6) , C1-C4, or C1-C2), substituted or unsubstituted cycloalkyl (e.g., C3 -C8, C3-C6, C4-C6, or C5-C6), substituted or unsubstituted cycloal Coxylation (e.g., C3-C8, C3-C6, C4-C6, or C5-C6), substitution also or unsubstituted halocycloalkyl (e.g., C3-C8, C3-C6, C4-C6, or C5-C6), substituted or unsubstituted halocycloalkoxy (e.g., C3-C8, C3- C6, C4-C6, or C5-C6), substituted or unsubstituted heterocycloalkyl (e.g.) For example, 3-8 members, 3-6 members, 4-6 members, 4-5 members, or 5-6 members), substitution or non-placement. Replacement aryl (e.g., C6-C) 10(or phenyl), or substituted or unsubstituted heterozygotes Selected from reels (e.g., 5-10 members, 5-9 members, or 5-6 members), or R 3 and R 10 These are linked together, and optionally, halogens, substituted or unsubstituted alkyl groups (for example, C 1-C8, C1-C6, C1-C4, or C1-C2), or substituted or unsubstituted cells Placed in a chloroalkyl group (e.g., C3-C8, C3-C6, C4-C6, or C5-C6). The cycloalkyl group to be replaced (e.g., C4-C8, C4-C6, or C5-C6) or A heterocycloalkyl (e.g., 4-8 member, 4-6 member, 4-5 member, or 5-6 member) ring form, or R 4 and R 10 These are linked together, and optionally, halogen, substituted, or unsubstituted. Alkyl (e.g., C1-C8, C1-C6, C1-C4, or C1-C2), or Substituted or unsubstituted cycloalkyls (e.g., C3-C8, C3-C6, C4-C6, etc.) or cycloalkyls substituted with C5-C6 (for example, C4-C8, C4-C6, and (C5-C6) or heterocycloalkyl (e.g., 4-8 member, 4-6 member, 4-5 member) Alternatively, it forms a ring (5-6 members), or R 6 and R 10 They are connected, and optionally, halogen , substituted or unsubstituted alkyl (e.g., C1-C8, C1-C6, C1-C4, or C1-C2), or substituted or unsubstituted cycloalkyl (e.g., C3-C8, C3- Cycloalkyls substituted with C6, C4-C6, or C5-C6 (e.g., C4-C 8, C4-C6, or C5-C6) or heterocycloalkyl (e.g., 4-8 member, Forms a ring with 4-6 members, 4-5 members, or 5-6 members, or R 9 and R10 Connect Optionally, halogens, substituted or unsubstituted alkyls (e.g., C1-C8, C1-C6, C1-C4, or C1-C2), or substituted or unsubstituted cycloalkyl (e.g., Cycloalkyl (substituted with C3-C8, C3-C6, C4-C6, or C5-C6) (For example, C3-C8, C3-C6, C4-C6, or C5-C6) or heterozygous Chloalkyl rings (e.g., 3-8 member, 3-6 member, 4-6 member, 4-5 member, or 5-6 member) Forming, R 11 However, hydrogen, substituted or unsubstituted alkyl (e.g., C1-C8, C1-C6, C) 1-C4, or C1-C2), substituted or unsubstituted haloalkyl (e.g., C1-C8) , C1-C6, C1-C4, or C1-C2), substituted or unsubstituted cycloalkyl ( For example, C3-C8, C3-C6, C4-C6, or C5-C6), substitution or non-position. Conversion halocycloalkyl (e.g., C3-C8, C3-C6, C4-C6, or C5-C) 6) Substituted or unsubstituted heterocycloalkyl (e.g., 3-8 member, 3-6 member, 4-6 member) (4-5 member, or 5-6 member), substituted or unsubstituted aryl (e.g., C6-C) 10 (or phenyl), or substituted or unsubstituted heteroaryls (e.g., 5-10 member, 5 (~9 members, or 5-6 members), or R 3 and R 11 They are connected, and optionally, halogen, Substituted or unsubstituted alkyl groups (e.g., C1-C8, C1-C6, C1-C4, or C 1-C2), or substituted or unsubstituted cycloalkyl (e.g., C3-C8, C3-C Heterocycloalkyls (e.g., 3-C6) substituted with C4-C6 or C5-C6 Forming rings (8 members, 3-6 members, 4-6 members, 4-5 members, or 5-6 members), or R 4 Oh biR 11 These are linked together, and optionally, halogens, substituted or unsubstituted alkyl groups (e.g., C1- C8, C1-C6, C1-C4, or C1-C2), or substituted or unsubstituted cyclo Substituted with alkyl (e.g., C3-C8, C3-C6, C4-C6, or C5-C6) Heterocycloalkyl groups (for example, 3-8 members, 3-6 members, 4-6 members, 4-5 members, or Forms a 5-6 member ring, or R 6 and R 11 These are linked together, and optionally, halogen, substitute Or unsubstituted alkyl (e.g., C1-C8, C1-C6, C1-C4, or C1- C2), or substituted or unsubstituted cycloalkyl (e.g., C3-C8, C3-C6, Heterocycloalkyls (e.g., 3-8 member) substituted with C4-C6 or C5-C6 , forming a ring (3-6 members, 4-6 members, 4-5 members, or 5-6 members), Each R 12 These independently consist of hydroxyl, halogen, cyano, and -N(R) 14 )(R 15 ), Substituted or unsubstituted alkyl groups (e.g., C1-C8, C1-C6, C1-C4, or C 1-C2), substituted or unsubstituted alkoxy (e.g., C1-C8, C1-C6, C1- C4, or C1-C2), substituted or unsubstituted haloalkyls (e.g., C1-C8, C) 1-C6, C1-C4, or C1-C2), substituted or unsubstituted haloalkoxy (e.g.) (For example, C1-C8, C1-C6, C1-C4, or C1-C2), substitution or non-substitution. Chloalkyl (e.g., C3-C8, C3-C6, C4-C6, or C5-C6), Substitutable or unsubstituted cycloalkoxys (e.g., C3-C8, C3-C6, C4-C6, etc.) (e.g., C5-C6), substituted or unsubstituted halocycloalkyl (e.g., C3-C8, C3) -C6, C4-C6, or C5-C6), substituted or unsubstituted halocycloalkoxy( For example, C3-C8, C3-C6, C4-C6, or C5-C6), substitution or non-position. Conversion alkylhydroxyl (e.g., C1-C8, C1-C6, C1-C4, or C1- C2), substituted or unsubstituted heterocycloalkyl (e.g., 3-8 member, 3-6 member, 4-) 6-membered, 4-5 membered, or 5-6 membered, substituted or unsubstituted aryl (e.g., C6-C1) 0 or phenyl), or substituted or unsubstituted heteroaryls (e.g., 5-10 member, 5-9 members, or 5-6 members), -S(O) n (R 16 ), or -SF5, selected Or R 3 and one R 12 These are linked together, optionally with halogen, substituted or unsubstituted halogen. Kill (e.g., C1-C8, C1-C6, C1-C4, or C1-C2), or replace. Or unsubstituted cycloalkyl (e.g., C3-C8, C3-C6, C4-C6, or Cycloalkyls substituted with C5-C6 (e.g., C3-C8, C3-C6, C4-C) 6, or C5-C6) or heterocycloalkyl (e.g., 3-8 member, 3-6 member, Forms a ring with 4-6 members, 4-5 members, or 5-6 members, or R 10 and one R 12 These are linked together, optionally with halogens, substituted or unsubstituted alkyl groups (e.g., C1-C8, C1 -C6, C1-C4, or C1-C2), or substituted or unsubstituted cycloalkyl ( For example, cyclo(C3-C8, C3-C6, C4-C6, or C5-C6) Alkyl (e.g., C3-C8, C3-C6, C4-C6, or C5-C6) or Heterocycloalkyl groups (e.g., 3-8 member, 3-6 member, 4-6 member, 4-5 member, or 5- 6-membered ring, or R 110 and one R 12 They are connected, and optionally, halogen , substituted or unsubstituted alkyl (e.g., C1-C8, C1-C6, C1-C4, or C1-C2), or substituted or unsubstituted cycloalkyl (e.g., C3-C8, C3- Heterocycloalkyls substituted with C6, C4-C6, or C5-C6 (e.g., 3 (8 members, 3-6 members, 4-6 members, 4-5 members, or 5-6 members) forming a ring, R 13 However, hydrogen, substituted or unsubstituted alkyl (e.g., C1-C8, C1-C6, C) 1-C4, or C1-C2), substituted or unsubstituted haloalkyl (e.g., C1-C8) , C1-C6, C1-C4, or C1-C2), substituted or unsubstituted cycloalkyl ( For example, C3-C8, C3-C6, C4-C6, or C5-C6), substitution or non-position. Conversion halocycloalkyl (e.g., C3-C8, C3-C6, C4-C6, or C5-C) 6) Substituted or unsubstituted heterocycloalkyl (e.g., 3-8 member, 3-6 member, 4-6 member) (4-5 member, or 5-6 member), substituted or unsubstituted aryl (e.g., C6-C) 10 (or phenyl), or substituted or unsubstituted heteroaryls (e.g., 5-10 member, 5- It consists of 9 members, or 5-6 members. R 14 and R 15 These independently consist of hydrogen, substituted or unsubstituted alkyl (e.g., C1- C8, C1-C6, C1-C4, or C1-C2), substituted or unsubstituted haloalkyl groups (For example, C1-C8, C1-C6, C1-C4, or C1-C2), substitution or non Substitutive cycloalkyl groups (e.g., C3-C8, C3-C6, C4-C6, or C5-C6) ), substituted or unsubstituted halocycloalkyls (e.g., C3-C8, C3-C6, C4- C6, or C5-C6), substituted or unsubstituted heterocycloalkyl (e.g., 3-8) (member, 3-6 member, 4-6 member, 4-5 member, or 5-6 member), substituted or unsubstituted aryl ( For example, C6-C 10 (or phenyl), or substituted or unsubstituted heteroaryls (e.g.) For example, the number of members can be selected from 5-10, 5-9, or 5-6, or R 14 and R 15 These are linked together, and optionally include halogens, substituted or unsubstituted alkyl groups (e.g., C1-C8 , C1-C6, C1-C4, or C1-C2), or substituted or unsubstituted cycloal Replaced by a kill (e.g., C3-C8, C3-C6, C4-C6, or C5-C6) Heterocycloalkyl groups (e.g., 3-8 member, 3-6 member, 4-6 member, 4-5 member, or 5- Forms a 6-member ring, R 16 However, substituted or unsubstituted alkyl (e.g., C1-C8, C1-C6, C1-C) 4, or C1-C2), substituted or unsubstituted haloalkyl (e.g., C1-C8, C1 -C6, C1-C4, or C1-C2), substituted or unsubstituted cycloalkyl (e.g.) , C3-C8, C3-C6, C4-C6, or C5-C6), substitution or non-substitution halo Cycloalkyl (e.g., C3-C8, C3-C6, C4-C6, or C5-C6), Substituted or unsubstituted heterocycloalkyl groups (e.g., 3-8 member, 3-6 member, 4-6 member, 4 ~5 members, or 5-6 members), substituted or unsubstituted aryls (e.g., C6-C) 10 or Phenyl), or substituted or unsubstituted heteroaryls (e.g., 5-10 member, 5-9 member, (or 5-6 members) m is 0 or 1, n is 0, 1, or 2, o is 0, 1, 2, or 3, A compound, or a pharmaceutically acceptable salt or solvate thereof, in which p is 0 or 1. It will be provided.

[0101] In one embodiment, a compound of formula (IA) or (IB), [ka] During the ceremony, X is bonded, -C(R 9 )(R 10 )-,-N(R 11 )-, -O-, -S(O) n - -CH2N(R 11 )-, or -CH2O-, Y is -CH2-, -CH2CH2-, -CH=CH-, or -CH2OCH2- can be, R 1 but, [ka] In the formula, ring A is either a 5-membered or 6-membered heteroaryl ring, or optionally, Rogen, Cyano, -N(R) 14 )(R 15 ), C 1-6 Alkyl, C 1-6 Alkoxy, C 1-6 Haloalkyl, C 1-6 Haloalkoxy, C 3-6 Cycloalkyl, C3-6 C Chloalkoxy, C 3-6 Halocycloalkyl, C 3-6 Halocycloalkoxy, hetero Cycloalkyl, aryl, heteroaryl, S(O) n (R 16 ), or -SF5 A 5-membered or 6-membered heterocycloalkyl ring substituted with a heteroaryl or hete The rocycloalkyl ring consists of 1, 2, or 3 elements selected from the group consisting of O, N, or S. It contains heteroatoms, R 2 However, hydrogen, deuterium, halogen, hydroxyl, C 1-6 Alkyl, C 1-6 Arco Kishi, C 1-6 Haloalkyl, C 1-6 Haloalkoxy, C 3-6 Cycloalkyl, C3 -6 Cycloalkoxy, C 3-6 Halocycloalkyl, C 3-6 Halocycloalkoxy, C 1-6 Alkylhydroxyl, heterocycloalkyl, aryl, or heteroaryl It is R 3 However, halogen, C 1-6 Alkyl, C 1-6 Alkoxy, C 1-6 Haloalkyl, C 1-6 Haloalkoxy, C 3-6 Cycloalkyl, C 3-6 Cycloalkoxy, C 3- 6-halocycloalkyl, C 3-6 Halocycloalkoxy, C 1-6 Alkylhydroxyl , heterocycloalkyl, aryl, or heteroaryl, or R 2 and R 3 They are connected, and optionally, halogen, C1-6 alkyl, or C 3-6 ycloalkyl forms a cycloalkyl or heterocycloalkyl ring substituted with cycloalkyl, R 4 and R 5 are independently selected from hydrogen, deuterium, halogen, and C 1-3 alkyl, or R and R 3 are linked to optionally form a cycloalkyl or heterocycloalkyl ring substituted with halogen, C 4 alkyl, or C 1-6 ycloalkyl, or R and R 3-6 are linked to optionally form a cycloalkyl or heterocycloalkyl ring substituted with cycloalkyl, or R 4 and R 5 are linked to optionally form a cycloalkyl or heterocycloalkyl ring substituted with halogen, C 1-6 alkyl or C 3-6 ycloalkyl, or R and R are independently selected from hydrogen, deuterium, halogen, and C 6 alkyl, or R 7 and R 1-3 are linked to optionally form a cycloalkyl or heterocycloalkyl ring substituted with halogen, C alkyl, or C 3 and R​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​​[ka] And, R 9 and R 10 These independently produce hydrogen, deuterium, halogens, and C 1-6 Alkyl, C 1-6 Alkoxy, C 1-6 Haloalkyl, C 1-6 Haloalkoxy, C 3-6 Cycloalkyl , C 3-6 Cycloalkoxy, C 3-6 Halocycloalkyl, C 3-6 Halocycloalco Selected from xy, heterocycloalkyl, aryl, or heteroaryl, is R 3 and R 10 They are connected, and optionally, halogen, C 1-6 Alkyl, or C 3- Forming a cycloalkyl or heterocycloalkyl ring substituted with a 6-cycloalkyl group, Or R 4 and R 10 They are connected, and optionally, halogen, C 1-6 Alkyl, or C 3-6 A cycloalkyl or heterocycloalkyl ring substituted with a cycloalkyl group accomplish, or R 6 and R 10 They are connected, and optionally, halogen, C 1-6 Alkyl, also or C 3-6 Cycloalkyl or heterocycloalkyl Forming a ring, or R 9 and R 10 They are connected, and optionally, halogen, C 1-6 Alki Ru, or C 3-6 Cycloalkyl or heterocycloalkyl substituted Forms a lucyl ring, R11 However, hydrogen, C 1-6 Alkyl, C 1-6 Haloalkyl, C 3-6 Cycloalkyl , C 3-6 Halocycloalkyl, heterocycloalkylaryl, or heteroaryl It is R 3 and R 11 They are connected, and optionally, halogen, C 1-6 Alkyl, Or C 3-6 Forms a heteroalkyl ring substituted with a cycloalkyl group, or R 4 oh Call R 11 They are connected, and optionally, halogen, C 1-6 Alkyl, or C 3-6 Cyclo Forms a heteroalkyl ring substituted with alkyl, or R 6 and R 11 They are connected, Optionally, halogen, C 1-6 Alkyl, or C 3-6 cycloalkyl substituted Forms a teloalkyl ring, Each R 12 These independently consist of hydroxyl, halogen, cyano, and -N(R) 14 )(R 15 ), C 1-6 Alkyl, C 1-6 Alkoxy, C 1-6 Haloalkyl, C 1-6 Haloalcochry C 3-6 Cycloalkyl, C 3-6 Cycloalkoxy, C 3-6 Halocycloalkyl , C 3-6 Halocycloalkoxy, C 1-6 Alkylhydroxyl, heterocycloalkyl Ru, aryl, heteroaryl, S(O) n (R 16 ), or selected from SF5, Or R 3and one R 12 are linked to optionally form a cycloalkyl or heteroalkyl ring substituted with halogen, C 1-6 alkyl, or C cycloalkyl, 3-6 or R and one R 10 are linked to optionally form a cycloalkyl or heteroalkyl ring substituted with halogen, C 12 alkyl, or C 1-6 cycloalkyl, or R 3-6 and one R are linked to optionally form a heteroalkyl ring substituted with halogen, C1 11 -6 12 alkyl, or C -6 cycloalkyl, 3-6 or R and form a heteroalkyl ring substituted with halogen, C alkyl, or C 13 cycloalkyl, 1-6 R 1-6 is hydrogen, C 3-6 alkyl, C haloalkyl, C 3-6 cycloalkyl, C halocycloalkyl, heterocycloalkyl, aryl, or heteroaryl, and R 14 and R 15 are independently selected from hydrogen, C 1-6 alkyl, C 1-6 haloalkyl, C 3-6 cycloalkyl, C 3-6 halocycloalkyl, heterocycloalkyl, aryl or heteroaryl, or R 14 and R 15 are linked to optionally form a heterocycloalkyl ring substituted with halogen, C 1-6 alkyl, or C 3-6 cycloalkyl, or R is C 16 alkyl, C 1-6 alkyl,1-6 Haloalkyl, C 3-6 Cycloalkyl, C3 -6 Halocycloalkyl, heterocycloalkyl, aryl, or heteroaryl the law of nature, m is 0 or 1, n is 0, 1, or 2, Compounds where o is 0, 1, 2, or 3. Or, provided that the aforementioned combination does not infringe upon the rules of valence which are readily apparent to those skilled in the art, A pharmaceutically acceptable salt or solvate thereof is provided.

[0102] In one embodiment, a compound of formula (IIA) or (IIB), [ka] During the ceremony, X is bonded, -C(R 9 )(R 10 )-,-N(R 11 )-, -O-, -S(O) n - -CH2N(R 11 )-, or -CH2O-, Y is -CH2-, -CH2CH2-, -CH=CH-, or -CH2OCH2- can be, R 1 but, [ka] In the formula, ring A is either a 5-membered or 6-membered heteroaryl ring, or optionally, Rogen, Cyano, -N(R) 14 )(R 15 ), C 1-6 Alkyl, C 1-6 Alkoxy, C 1-6 Haloalkyl, C 1-6 Haloalkoxy, C 3-6 Cycloalkyl, C 3-6 C Chloalkoxy, C 3-6 Halocycloalkyl, C 3-6 Halocycloalkoxy, hetero Cycloalkyl, aryl, heteroaryl, S(O) n (R 16 ), or -SF5 A 5-membered or 6-membered heterocycloalkyl ring substituted with a heteroaryl or hete The rocycloalkyl ring consists of 1, 2, or 3 elements selected from the group consisting of O, N, or S. It contains heteroatoms, R 2 However, hydrogen, deuterium, halogen, hydroxyl, C 1-6 Alkyl, C 1-6 Arco Kishi, C 1-6 Haloalkyl, C 1-6 Haloalkoxy, C 3-6 Cycloalkyl, C3 -6 Cycloalkoxy, C 3-6 Halocycloalkyl, C 3-6 Halocycloalkoxy, C 1-6 Alkylhydroxyl, heterocycloalkyl, aryl, or heteroaryl It is R 3 However, halogen, C 1-6 Alkyl, C 1-6 Alkoxy, C 1-6 Haloalkyl, C 1-6 Haloalkoxy, C 3-6 Cycloalkyl, C 3-6 Cycloalkoxy, C 3- 6-halocycloalkyl, C 3-6 Halocycloalkoxy, C 1-6 Alkylhydroxyl , heterocycloalkyl, aryl, or heteroaryl, or R 2 and R 3 They are connected, and optionally, halogen, C 1-6 Alkyl, or C 3-6Cycloalkyl Forms a cycloalkyl or heterocycloalkyl ring substituted with , R 8 but, [ka] And, R 9 and R 10 These independently produce hydrogen, deuterium, halogens, and C 1-6 Alkyl, C 1-6 Alkoxy, C 1-6 Haloalkyl, C 1-6 Haloalkoxy, C 3-6 Cycloalkyl , C 3-6 Cycloalkoxy, C 3-6 Halocycloalkyl, C 3-6 Halocycloalco Selected from xy, heterocycloalkyl, aryl, or heteroaryl, is R 3 and R 10 They are connected, and optionally, halogen, C 1-6 Alkyl, or C 3- Forming a cycloalkyl or heterocycloalkyl ring substituted with a 6-cycloalkyl group, Or R 9 and R 10 They are connected, and optionally, halogen, C 1-6 Alkyl, or C 3-6 A cycloalkyl or heterocycloalkyl ring substituted with a cycloalkyl group accomplish, R 11 However, hydrogen, C 1-6 Alkyl, C 1-6 Haloalkyl, C 3-6 Cycloalkyl , C 3-6 Halocycloalkyl, heterocycloalkylaryl, or heteroaryl It is R 3 and R 11They are connected, and optionally, halogen, C 1-6 Alkyl, Or C 3-6 Forms a heteroalkyl ring substituted with a cycloalkyl group, Each R 12 These independently consist of hydroxyl, halogen, cyano, and -N(R) 14 )(R 15 ), C 1-6 Alkyl, C 1-6 Alkoxy, C 1-6 Haloalkyl, C 1-6 Haloalcochry C 3-6 Cycloalkyl, C 3-6 Cycloalkoxy, C 3-6 Halocycloalkyl , C 3-6 Halocycloalkoxy, C 1-6 Alkylhydroxyl, heterocycloalkyl Ru, aryl, heteroaryl, S(O) n (R 16 ), or selected from SF5, Or R 3 and one R 12 They are connected, and optionally, halogen, C 1-6 Alkyl, also or C 3-6 A cycloalkyl or heteroalkyl ring substituted with a cycloalkyl group accomplish, or R 10 and one R 12 They are connected, and optionally, halogen, C 1-6 Al Kill, or C 3-6 Cycloalkyl or heteroalkyl substituted Forms a ring, or R 11 and one R 12 They are connected, and optionally, halogen, C1 -6 Alkyl, or C 3-6 Forms a heteroalkyl ring substituted with a cycloalkyl group. , R 13 However, hydrogen, C1-6 Alkyl, C 1-6 Haloalkyl, C 3-6 Cycloalkyl , C 3-6 Halocycloalkyl, heterocycloalkyl, aryl, or heteroaryl It is R 14 and R 15 Hydrogen, C 1-6 Alkyl, C 1-6 Haloalkyl, C 3-6 Cycloalkyl, C 3-6 Halocycloalkyl, heterocycloalkyl, aryl , or selected from heteroaryls, or R 14 and R 15 They are linked together, arbitrarily , halogen, C 1-6 Alkyl, or C 3-6 Heterocyclic substituted Forms a chloroalkyl ring, R 16 However, C 1-6 Alkyl, C 1-6 Haloalkyl, C 3-6 Cycloalkyl, C3 -6 Halocycloalkyl, heterocycloalkyl, aryl, or heteroaryl the law of nature, m is 0 or 1, n is 0, 1, or 2, Compounds where o is 0, 1, 2, or 3. Or, provided that the aforementioned combination does not infringe upon the rules of valence which are readily apparent to those skilled in the art, A pharmaceutically acceptable salt or solvate thereof is provided.

[0103] In another embodiment, the compound of formula (III) is, [ka] During the ceremony, X is bonded, -C(R 9 )(R10 )-,-N(R 11 )-, -O-, -S(O) n - -CH2N(R 11 )-, or -CH2O-, R 1 but, [ka] In the formula, ring A is either a 5-membered or 6-membered heteroaryl ring, or optionally, Rogen, Cyano, -N(R) 14 )(R 15 ), C 1-6 Alkyl, C 1-6 Alkoxy, C 1-6 Haloalkyl, C 1-6 Haloalkoxy, C 3-6 Cycloalkyl, C 3-6 C Chloalkoxy, C 3-6 Halocycloalkyl, C 3-6 Halocycloalkoxy, hetero Cycloalkyl, aryl, heteroaryl, S(O) n (R 16 ), or -SF5 A 5-membered or 6-membered heterocycloalkyl ring substituted with a heteroaryl or hete The rocycloalkyl ring consists of 1, 2, or 3 elements selected from the group consisting of O, N, or S. It contains heteroatoms, R 2 However, hydrogen, deuterium, halogen, hydroxyl, C 1-6 Alkyl, C 1-6 Arco Kishi, C 1-6 Haloalkyl, C 1-6 Haloalkoxy, C 3-6 Cycloalkyl, C3 -6 Cycloalkoxy, C 3-6 Halocycloalkyl, C 3-6 Halocycloalkoxy, C 1-6Alkylhydroxyl, heterocycloalkyl, aryl, or heteroaryl It is R 3 However, halogen, C 1-6 Alkyl, C 1-6 Alkoxy, C 1-6 Haloalkyl, C 1-6 Haloalkoxy, C 3-6 Cycloalkyl, C 3-6 Cycloalkoxy, C 3- 6-halocycloalkyl, C 3-6 Halocycloalkoxy, C 1-6 Alkylhydroxyl , heterocycloalkyl, aryl, or heteroaryl, or R 2 and R 3 They are connected, and optionally, halogen, C 1-6 Alkyl, or C 3-6 Cycloalkyl Forms a cycloalkyl or heterocycloalkyl ring substituted with , R 8 but, [ka] And, R 9 and R 10 These independently produce hydrogen, deuterium, halogens, and C 1-6 Alkyl, C 1-6 Alkoxy, C 1-6 Haloalkyl, C 1-6 Haloalkoxy, C 3-6 Cycloalkyl , C 3-6 Cycloalkoxy, C 3-6 Halocycloalkyl, C 3-6 Halocycloalco Selected from xy, heterocycloalkyl, aryl, or heteroaryl, is R 3 and R 10 They are connected, and optionally, halogen, C 1-6Alkyl, or C 3- Forming a cycloalkyl or heterocycloalkyl ring substituted with a 6-cycloalkyl group, Or R 9 and R 10 They are connected, and optionally, halogen, C 1-6 Alkyl, or C 3-6 A cycloalkyl or heterocycloalkyl ring substituted with a cycloalkyl group accomplish, R 11 However, hydrogen, C 1-6 Alkyl, C 1-6 Haloalkyl, C 3-6 Cycloalkyl , C 3-6 Halocycloalkyl, heterocycloalkylaryl, or heteroaryl It is R 3 and R 11 They are connected, and optionally, halogen, C 1-6 Alkyl, Or C 3-6 Forms a heteroalkyl ring substituted with a cycloalkyl group, Each R 12 These independently consist of hydroxyl, halogen, cyano, and -N(R) 14 )(R 15 ), C 1-6 Alkyl, C 1-6 Alkoxy, C 1-6 Haloalkyl, C 1-6 Haloalcochry C 3-6 Cycloalkyl, C 3-6 Cycloalkoxy, C 3-6 Halocycloalkyl , C 3-6 Halocycloalkoxy, C 1-6 Alkylhydroxyl, heterocycloalkyl Ru, aryl, heteroaryl, S(O) n (R 16 ), or selected from SF5, Or R 3 and one R 12They are connected, and optionally, halogen, C 1-6 Alkyl, also or C 3-6 A cycloalkyl or heteroalkyl ring substituted with a cycloalkyl group accomplish, or R 10 and one R 12 They are connected, and optionally, halogen, C 1-6 Al Kill, or C 3-6 Cycloalkyl or heteroalkyl substituted Forms a ring, or R 11 and one R 12 They are connected, and optionally, halogen, C1 -6 Alkyl, or C 3-6 Forms a heteroalkyl ring substituted with a cycloalkyl group. , R 13 However, hydrogen, C 1-6 Alkyl, C 1-6 Haloalkyl, C 3-6 Cycloalkyl , C 3-6 Halocycloalkyl, heterocycloalkyl, aryl, or heteroaryl It is R 14 and R 15 Hydrogen, C 1-6 Alkyl, C 1-6 Haloalkyl, C 3-6 Cycloalkyl, C 3-6 Halocycloalkyl, heterocycloalkyl, aryl , or selected from heteroaryls, or R 14 and R 15 They are linked together, arbitrarily , halogen, C 1-6 Alkyl, or C 3-6 Heterocyclic substituted Forms a chloroalkyl ring, R 16 However, C 1-6 Alkyl, C 1-6 Haloalkyl, C3-6 Cycloalkyl, C3 -6 Halocycloalkyl, heterocycloalkyl, aryl, or heteroaryl the law of nature, m is 0 or 1, n is 0, 1, or 2, Compounds where o is 0, 1, 2, or 3. Or, provided that the aforementioned combination does not infringe upon the rules of valence which are readily apparent to those skilled in the art, A pharmaceutically acceptable salt or solvate thereof is provided.

[0104] Compounds described herein (e.g., formulas (IA-1), (IB-1), (IA), (IB) ), (IIA), (IIB), or (III)), or their pharmaceutically acceptable In embodiments of the salt or solvate, X is bonded to -C(R 9 )(R 10 )-,-N(R 11 )-, or -O-. In some embodiments, X is bonded, -N(R 11 ) -, or -O-.

[0105] Compounds of formula (IA), (IB), (IIA), (IIB), or (III), In some embodiments of those pharmaceutically acceptable salts or solvates, X is bonded. -C(R 9 )(R 10 )-,-N(R 11 )-, or -O-. Some real In the application form, X is bonded, -N(R 11 )-, or -O-.

[0106] In this embodiment, substituted X (for example, substituted alkylene, substituted alkenylene, substituted alkynylene) , substituted heteroalkylene, substituted heteroalkene, and / or substituted heteroalkyl Nylene is substituted with at least one substituent, size-limiting substituent, or lower substituent. , substitution X is provided by multiple groups selected from substituents, size-limiting substituents, and lower substituents. If replaced, each substituent, size-limiting substituent, and / or lower substituent may be optionally They may be different. In the embodiment, if X is substituted, it is substituted with at least one substituent. It is replaced. In the embodiment, when X is replaced, it is replaced with at least one size-limiting substituent. It is replaced. In the embodiment, when X is replaced, it is replaced with at least one lower substituent. ru.

[0107] In the embodiment, substituted Y (e.g., substituted alkylene, substituted alkenylene, and / or A substituted heteroalkylene may have at least one substituent, a size-restricting substituent, or a lower-order substituent. Substituting with a substitution group, where substitution Y is selected from substituents, size-restricting substituents, and lower substituents. If substituted with multiple groups, each substituent, size-limiting substituent, and / or lower substituent The substitution base may be arbitrarily different. In this embodiment, if Y is substituted, at least 1 It is substituted with one substituent. In the embodiment, if Y is substituted, at least one size It is substituted with a limiting substituent. In the embodiment, if Y is substituted, at least one lower substituent It is replaced by a substitution element.

[0108] In the embodiment, ring A may be substituted with hydroxyls in addition to the listed substituents.

[0109] Compounds described herein (e.g., formulas (IA-1), (IB-1), (IA), (IB) ), (IIA), (IIB), or (III)), or their pharmaceutically acceptable In embodiments of the salt or solvate, R 1 but, [ka] In some embodiments, R 1 but, [ka] That is the case.

[0110] Compounds of formula (IA), (IB), (IIA), (IIB), or (III), In some embodiments of those pharmaceutically acceptable salts or solvates, R 1 but, [ka] In some embodiments, R 1 but, [ka] That is the case.

[0111] In this embodiment, R 2 However, hydrogen, deuterium, halogens, hydroxyl, substituted or unsubstituted C 1-6 Alkyl, substituted, or unsubstituted C 1-6 alkoxy, substituted or unsubstituted C 1- 6-haloalkyl, substituted or unsubstituted C 1-6 Haloalkoxy, substituted or unsubstituted C1 -6 Cycloalkyl, substituted, or unsubstituted C 1-6 Cycloalkoxy, substituted or unsubstituted exchange C 1-6 Halocycloalkyl, substituted or unsubstituted C 1-6 Halocycloalkoxy, Substitution or non-substitution C 1-6 Alkylhydroxyl, substituted or unsubstituted heterocycloal It is a kill, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl.

[0112] In the embodiment, substitution R 2 (For example, substituted alkyl, substituted alkoxy, substituted haloalkyl) substituted haloalkoxy, substituted cycloalkyl, substituted cycloalkoxy, substituted halocyclo Lukyl, substituted halocycloalkoxy, substituted alkylhydroxyl, substituted heterocycloal Kill, substituted aryl, and / or substituted heteroaryl are at least one substituent , substituted with size-limited substituents or lower substituents, substituted R 2 However, substituents, size limitations If substituted with multiple groups selected from substitution groups and lower substituents, each substituent, The limited substituents and / or lower substituents may be different as appropriate. In the embodiment, , R 2 If R is replaced, 2 is substituted with at least one substituent. In the embodiment, , R 2 If it is substituted, it is substituted with at least one size-restricting substituent. In state, R 2 If substitution occurs, it is substituted with at least one lower substituent.

[0113] In the embodiment, substitution R 3 (For example, substituted alkyl, substituted alkoxy, substituted haloalkyl) substituted haloalkoxy, substituted cycloalkyl, substituted cycloalkoxy, substituted halocyclo Lukyl, substituted halocycloalkoxy, substituted alkylhydroxyl, substituted heterocycloal Kill, substituted aryl, and / or substituted heteroaryl are at least one substituent , substituted with size-limited substituents or lower substituents, substituted R 3 However, substituents, size limitations If substituted with multiple groups selected from substitution groups and lower substituents, each substituent, The limited substituents and / or lower substituents may be different as appropriate. In the embodiment, , R 3 If it is substituted, it is substituted with at least one substituent. In the embodiment, R 3 but If substituted, it is substituted with at least one size-restricting substituent. In the embodiment, R 3 If substitution occurs, it is substituted with at least one lower substituent.

[0114] In the embodiment, substitution R 4 (For example, a substituted alkyl) has at least one substituent, cy Substituted with a Z-restricting substituent or a lower substituent, substituted R 4 However, substituents, size-restricting substituents, And when substituted with multiple groups selected from lower substituents, each substituent, size-limited substitution The group and / or lower substituent may be different as appropriate. In this embodiment, R 4 Place If replaced, it is replaced with at least one substituent. In the embodiment, R 4 is replaced If present, it is substituted with at least one size-limiting substituent. In the embodiment, R 4 but If substitution occurs, it will be substituted with at least one lower substituent.

[0115] In the embodiment, substitution R 5 (For example, a substituted alkyl) has at least one substituent, cy Substituted with a Z-restricting substituent or a lower substituent, substituted R 5 However, substituents, size-restricting substituents, And when substituted with multiple groups selected from lower substituents, each substituent, size-limited substitution The group and / or lower substituent may be different as appropriate. In this embodiment, R 5 Place If replaced, it is replaced with at least one substituent. In the embodiment, R 5is replaced In this case, it is replaced with at least one size-limiting substituent. In the embodiment, R 5 is replaced If so, it is substituted with at least one lower substituent.

[0116] In the embodiment, substitution R 6 (For example, a substituted alkyl) has at least one substituent, cy Substituted with a Z-restricting substituent or a lower substituent, substituted R 6 However, substituents, size-restricting substituents, And when substituted with multiple groups selected from lower substituents, each substituent, size-limited substitution The group and / or lower substituent may be different as appropriate. In this embodiment, R 6 Place If replaced, it is replaced with at least one substituent. In the embodiment, R 6 is replaced In this case, it is replaced with at least one size-limiting substituent. In the embodiment, R 6 is replaced If so, it is substituted with at least one lower substituent.

[0117] In the embodiment, substitution R 7 (For example, a substituted alkyl) has at least one substituent, cy Substituted with a Z-restricting substituent or a lower substituent, substituted R 7 However, substituents, size-restricting substituents, And when substituted with multiple groups selected from lower substituents, each substituent, size-limited substitution The group and / or lower substituent may be different as appropriate. In this embodiment, R 7 Place If replaced, it is replaced with at least one substituent. In the embodiment, R 7 is replaced In this case, it is replaced with at least one size-limiting substituent. In the embodiment, R 7 is replaced If so, it is substituted with at least one lower substituent.

[0118] Compounds described herein (e.g., formulas (IA-1), (IB-1), (IA), (IB) ), (IIA), (IIB), or (III)), or their pharmaceutically acceptable In embodiments of the salt or solvate, R 8 but, [ka] In some embodiments, R 8 but, [ka] That is the case.

[0119] Compounds of formula (IA), (IB), (IIA), (IIB), or (III), In some embodiments of those pharmaceutically acceptable salts or solvates, R 8 but, [ka] In some embodiments, R 8 but, [ka] That is the case.

[0120] In the embodiment, substitution R 9 (For example, substituted alkyl, substituted alkoxy, substituted haloalkyl) substituted haloalkoxy, substituted cycloalkyl, substituted cycloalkoxy, substituted halocyclo Lukyl, substituted halocycloalkoxy, substituted heterocycloalkyl, substituted aryl, and / or substituted heteroaryls) have at least one substituent, a size-limited substituent, or Substituted with a lower substituent, substituted R 9 However, substituents, size-limited substituents, and lower substituents If substituted with multiple selected groups, each substituent, size-limited substituent, and / or The lower substituents may be arbitrarily different. In this embodiment, R 9 If it is replaced, It is substituted with at least one substituent. In the embodiment, R 9 If it is replaced, at least It is replaced with one size-limiting substituent. In the embodiment, R 9 If it is replaced, at least It is then substituted with another lower substituent.

[0121] In the embodiment, substitution R 10 (For example, substituted alkyl, substituted alkoxy, substituted haloalkyl , substituted haloalkoxy, substituted cycloalkyl, substituted cycloalkoxy, substituted halocyclo Alkyl, substituted halocycloalkoxy, substituted heterocycloalkyl, substituted aryl, and (and / or substituted heteroaryls) may have at least one substituent, a size-limited substituent, and is substituted with a lower substituent, and substituted R 10 However, substituents, size-limited substituents, and lower substituents If substituted with multiple groups selected from, each substituent, size-limited substituent, and / Alternatively, the lower substituents may be arbitrarily different. In this embodiment, R 10 The place where it is replaced In combination, it is substituted with at least one substituent. In the embodiment, R 10 If it is replaced, At the very least, it is replaced by one size-limiting substituent. In the embodiment, R 10 If it is replaced , substituted with at least one lower substituent.

[0122] In the embodiment, substitution R 11 (For example, substituted alkyl, substituted haloalkyl, substituted cycloalkyl Lukyl, substituted halocycloalkyl, substituted heterocycloalkyl, substituted aryl, and / (or substituted heteroaryl) has at least one substituent, a size-limited substituent, or low Substituted with a cubic substituent, substituted R 11 However, substituents, size-limited substituents, and lower substituents If substituted with multiple selected groups, each substituent, size-limited substituent, and / or The lower substituents may be arbitrarily different. In this embodiment, R 11 If it is replaced, It is substituted with at least one substituent. In the embodiment, R 11 If it is replaced, less Both are substituted with a single size-restricting substituent. In the embodiment, R 11 If it is replaced, At the very least, it is substituted with one lower substituent.

[0123] In the embodiment, substitution R 12 (For example, substituted alkyl, substituted alkoxy, substituted haloalkyl , substituted haloalkoxy, substituted cycloalkyl, substituted cycloalkoxy, substituted halocyclo Alkyl, substituted halocycloalkoxy, substituted alkylhydroxyl, substituted heterocycloalkoxy Lukyl, substituted aryl, and / or substituted heteroaryl) have at least one substitution Substituted with a group, size-limited substituent, or lower substituent, substituted R 12 However, substituents, size limits When substituted with multiple groups selected from constant substituents and lower substituents, each substituent, The size-restricted substituents and / or lower substituents may be different as appropriate. Embodiments So, R 12 If it is substituted, it is substituted with at least one substituent. In the embodiment, R 12 If it is substituted, it is substituted with at least one size-restricting substituent. In embodiments R 12 If substitution occurs, it is substituted with at least one lower substituent.

[0124] In the embodiment, substitution R 13 (For example, substituted alkyl, substituted haloalkyl, substituted cycloalkyl Lukyl, substituted halocycloalkyl, substituted heterocycloalkyl, substituted aryl, and / (or substituted heteroaryl) has at least one substituent, a size-limited substituent, or low Substituted with a cubic substituent, substituted R 13 However, substituents, size-limited substituents, and lower substituents If substituted with multiple selected groups, each substituent, size-limited substituent, and / or The lower substituents may be arbitrarily different. In this embodiment, R 13 If it is replaced, It is substituted with at least one substituent. In the embodiment, R 13 If it is replaced, less Both are substituted with a single size-restricting substituent. In the embodiment, R 13 If it is replaced, At the very least, it is substituted with one lower substituent.

[0125] In the embodiment, substitution R 14 (For example, substituted alkyl, substituted haloalkyl, substituted cycloalkyl Lukyl, substituted halocycloalkyl, substituted heterocycloalkyl, substituted aryl, and / (or substituted heteroaryl) has at least one substituent, a size-limited substituent, or low Substituted with a cubic substituent, substituted R 14 However, substituents, size-limited substituents, and lower substituents If substituted with multiple selected groups, each substituent, size-limited substituent, and / or The lower substituents may be arbitrarily different. In this embodiment, R 14 If it is replaced, It is substituted with at least one substituent. In the embodiment, R 14 If it is replaced, less Both are substituted with a single size-restricting substituent. In the embodiment, R 14 If it is replaced, At the very least, it is substituted with one lower substituent.

[0126] In the embodiment, substitution R 15 (For example, substituted alkyl, substituted haloalkyl, substituted cycloalkyl Lukyl, substituted halocycloalkyl, substituted heterocycloalkyl, substituted aryl, and / (or substituted heteroaryl) has at least one substituent, a size-limited substituent, or low Substituted with a cubic substituent, substituted R 15 However, substituents, size-limited substituents, and lower substituents If substituted with multiple selected groups, each substituent, size-limited substituent, and / or The lower substituents may be arbitrarily different. In this embodiment, R 15 If it is replaced, It is substituted with at least one substituent. In the embodiment, R 15 If it is replaced, less Both are substituted with a single size-restricting substituent. In the embodiment, R 15 If it is replaced, At the very least, it is substituted with one lower substituent.

[0127] In the embodiment, substitution R 16 (For example, substituted alkyl, substituted haloalkyl, substituted cycloalkyl Lukyl, substituted halocycloalkyl, substituted heterocycloalkyl, substituted aryl, and / (or substituted heteroaryl) has at least one substituent, a size-limited substituent, or low Substituted with a cubic substituent, substituted R 16 However, substituents, size-limited substituents, and lower substituents If substituted with multiple selected groups, each substituent, size-limited substituent, and / or The lower substituents may be arbitrarily different. In this embodiment, R 16 If it is replaced, It is substituted with at least one substituent. In the embodiment, R 16 If it is replaced, less Both are substituted with a single size-restricting substituent. In the embodiment, R 16 If it is replaced, At the very least, it is substituted with one lower substituent.

[0128] Any combination of the groups described above or below for various variable parts is this This specification is intended to be used in this specification. Throughout this specification, these groups and substituents are safe. Selected by those skilled in the art to provide specific parts and compounds.

[0129] In some embodiments, a compound selected from the following, or its pharmaceutically acceptable equivalent A salt or solvate is provided: [ka] [ka] [ka] [ka] [ka] [ka] [ka] [ka] [ka] [ka] [ka] [ka] or a pharmaceutically acceptable salt or solvate thereof. The list of compounds immediately preceding this text is as follows: This is referred to as "Compound List 1" below.

[0130] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] 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embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the compound is [ka] In this embodiment, the 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[0131] In the embodiment, the compound is useful as a comparative compound. , assays (for example, described in this specification, for example, in the Examples section, figures, or tables) It can be used to evaluate the activity of a test compound in assays such as the following.

[0132] In the embodiments, the compound is a compound described herein (for example, in the Compounds section). Examples, methods, or claims, tables, or figures as described in the Examples section, Methods section, or Claims section, tables, or figures. (ru).

[0133] III. Further Forms of Compounds isomer The compounds described herein are all possible tautomers within the range of the formulas described herein. This includes. Furthermore, in some embodiments, the compounds described herein are geometric isomers. In some embodiments, the compounds described herein contain one or more double bonds. The compounds presented herein include all cis, trans, syn, and an ti, entgegen(E), and zusammen(Z) isomers, and their It includes the corresponding mixture of the compounds. In some situations, the compounds exist as tautomers.

[0134] In some situations, the compounds described herein have one or more chiral centers, and each of them The heart exists in either the (R) configuration or the (S) configuration. All compounds described herein The diastereomer, enantiomer, and epimer forms of [the substance], and their corresponding forms. It includes a mixture. Additional embodiments of the compounds and methods provided herein include a single Enantiomers and / or dimorphs resulting from preparative steps, combinations, or interconversions Mixtures of astereoisomers are useful for the applications described herein. Several embodiments The compounds described herein are obtained by chiral chromatographic decomposition of racemic mixtures. , are prepared as optically pure enantiomers. In some embodiments, as specified herein The compounds described are obtained by reacting a racemic mixture of compounds with an optically active resolving agent to form a pair of dias Form a teleosomer compound, separate the diastereomer, and optically obtain an optically pure enantiomer. —These are recovered and prepared as their individual stereoisomers. Several implementations In terms of morphology, dissociable complexes are preferred (e.g., crystalline diastereomer salts). In that embodiment, the diastereomer has different physical properties (e.g., melting point, boiling point, dissolution). They have (degrees, reactivity, etc.) and are separated by utilizing these dissimilarity properties. Several embodiments The diastereomers are then analyzed by chiral chromatography, or preferably by dissolution. They are separated by separation / decomposition techniques based on the degree of separation. In some embodiments, then, Optically pure enantiomers can be extracted by any practical means that do not result in racemization. It is recovered along with the dividing agent.

[0135] The term "geometric isomer" refers to the E or Z geometric isomer of an alkene double bond (e.g., c This refers to iso or trans. The term "positional isomer" refers to structural isomers around a central ring. This refers to isomers, such as ortho-, meta-, and para-isomers around a benzene ring.

[0136] labeled compound The compounds disclosed herein, in some embodiments, are in different enriched isotopic forms, e.g. For example, 2 H, 3 H, 11 C, 13 C and / or 14 It is used in a concentrated form with a high C content. It is used. In one particular embodiment, the compound is deuterated at at least one position. Such deuterated forms are described in U.S. Patent Nos. 5,846,514 and 6,334. It can be manufactured by the procedure described in U.S. Patent No. 5,846,51 As described in No. 4 and No. 6,334,997, deuteration improves metabolic stability and It can improve efficacy and / or increase the duration of action of the drug. .

[0137] Unless otherwise specified, the structures shown herein are of one or more isotope-enriched atoms It is intended to include compounds that differ only in their existence. For example, compounds having this structure The substance is one in which hydrogen is replaced with deuterium or tritium, or carbon 13 C- or 1 4 Except for substitution with carbon-enriched carbon, this is within the scope of this disclosure.

[0138] The compounds disclosed herein are characterized by the non-absence of atomic isotopes in one or more atoms constituting such compounds. It contains any proportion of natural elements. For example, a compound may contain, for example, deuterium ( 2 H), tritium ( 3 H) , Iodine-125 ( 125 I) or carbon-14 ( 14 It can be labeled with isotopes such as C). . 2 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, 125 Isotope substitution in I is all part of the plan All isotopic variations of the compounds disclosed herein, whether radioactive or not, are subject to the disclosure. It is included within the scope of the indication.

[0139] In certain embodiments, the compounds disclosed herein are 1 Some or all of the H atoms 2 It is replaced by an H atom. The method for synthesizing deuterium-containing compounds is known in the art. In some embodiments, the deuterium-substituted compound is used in various ways, as described below. Synthesized using the method: Dean, DC; “Recent Advances i n the Synthesis and Applications of Radi olabeled Compounds for Drug Discovery an d Development,”Curr.Pharm.Des.,2000,6(10 );George W.;Varma, RS, “The Synthesis of Radiolabeled Compounds via Organometall ic Intermediates,”Tetrahedron,1989,45(21 ), 6601-21; and Evans, EA, “Synthesis of ra diolabeled compounds,”J.Radioanal.Chem., 1981, 64(1-2), 9-32.

[0140] In some embodiments, the compounds described herein are chromophores or fluorescent moieties, biological Marking by other means, including but not limited to the use of luminescent or chemiluminescent labels. To be recognized.

[0141] Pharmaceutically acceptable salts In some embodiments, the compounds described herein are used as pharmaceutically acceptable salts thereof. It exists. In some embodiments, the methods disclosed herein are such pharmaceutical The method includes treating a disease by administering a salt that is tolerable to the disease. Several embodiments The method disclosed herein involves using such pharmaceutically acceptable salts in a pharmaceutical composition. This includes methods of treating diseases by administering drugs.

[0142] In some embodiments, the compounds described herein have an acidic group or a basic group. Therefore, several inorganic bases or organic bases, as well as inorganic acids and organic acids It reacts with to form a pharmaceutically acceptable salt. In some embodiments, these salts During the final isolation and purification of the compounds of this disclosure, or the purified compounds, their release The salts are reacted separately with the appropriate acid or base in their morphology, and the resulting salts are then isolated. Therefore, it is prepared on the spot.

[0143] solvate In some embodiments, the compounds described herein exist as solvates. The present invention provides a method for treating a disease by administering such a solvate. The indication further suggests treating diseases by administering such solvates as pharmaceutical compositions. Provide a method.

[0144] A solvate contains either a stoichiometric or non-stoichiometric amount of solvent, and several practices In terms of form, during the crystallization process using pharmaceutically acceptable solvents such as water and ethanol... It is formed. When the solvent is water, a hydrate is formed, or when the solvent is alcohol, an alcohol is formed. Cholate salts are formed. The solvates of the compounds described herein are the prosandwich salts described herein. They are appropriately prepared or formed during the process. As just one example, the hydration of the compounds described herein The substances include, but are not limited to, dioxane, tetrahydrofuran, or methanol. It is appropriately prepared by recrystallizing an aqueous / organic solvent mixture using an organic solvent. Furthermore, the compounds provided herein are available not only in their unsolvated form, but also in solvents. It exists in a solvated form. Generally, the solvated form is the compound provided herein. For the purposes of the method, it is considered equivalent to the unsolvated form.

[0145] Prodrug In some embodiments, the compounds described herein exist in the form of prodrugs. This disclosure provides a method for treating a disease by administering such a prodrug. The disclosure further describes administering such prodrugs as a pharmaceutical composition. This provides a method to treat the disease.

[0146] In some embodiments, the prodrug consists of an amino acid residue, or two or more (for example, A polypeptide chain of 2, 3, or 4 amino acid residues is linked by an amide bond or ester. The free amino group, hydroxyl group, or carboxylic acid group of the compound of this disclosure is covalently linked via bonding. It contains the compound it is bound to. The amino acid residues include 20 naturally occurring amino acids. However, it is not limited to these, and also includes 4-hydroxyproline, hydroxylysine, Demosine, Isodemosine, 3-methylhistidine, Norvaline, Beta-alanine, Cancer M-aminobutyric acid, citrulline, homocysteine, homoserine, ornithine and methionine It contains a nucleotide sulfone. In other embodiments, the prodrug is a nucleic acid residue, or two or more. Oligonucleotides of nucleic acid residues (for example, 2, 3, or 4) are added to the compound of this disclosure. It contains covalently bonded compounds.

[0147] pharmaceutically acceptable prodrugs of the compounds described herein include esters, carbonates, etc. Tel, thiocarbonate, N-acyl derivative, N-acyloxyalkyl derivative, tertiary Quaternary derivatives of amines, N-Mannich bases, Schiff bases, amino acid conjugates, This also includes, but is not limited to, sulfonic acid esters, metal salts, and sulfonic acid esters. In some embodiments, free amino groups, amide groups, hydroxyl groups, or carboxylic acid groups are used. The compound containing the free carboxyl group is converted into a prodrug. For example, the free carboxyl group is converted into an amide or It is derivatized as an alkyl ester. In certain cases, these prodrug moieties All of these groups include, but are not limited to, ether, amine, and carboxylic acid functional groups. It's integrated.

[0148] Hydroxyprodrugs include esters, for example, but are not limited to the following: Aloxyalkyl (e.g., acyloxymethyl, acyloxyethyl) esters, Coxycarbonyloxyalkyl esters, alkyl esters, aryl esters, phosphorus Acid esters, sulfonic acid esters, sulfuric acid esters and disulfide-containing esters; A Thel, amide, carbamate, hemisuccinate, dimethylaminoacetate and phosphate It contains folyloxymethyloxycarbonyl, and these are from Fleisher, D. et al. al.,“Improved oral drug delivery:solubi lity limitations overcome by the use of prodrugs,”Advanced Drug Delivery Reviews This is outlined in 1996, 19, 115-130.

[0149] The following groups and combinations of amine-derived prodrugs are examples: [ka] This also includes, but is not limited to, sulfonamides and phosphoamides.

[0150] IV. Pharmaceutical Compositions In embodiments, compounds described herein (e.g., formula (IA-1), (IB-1), ( IA), (IB), (IIA), (IIB), or (III)) are pure chemical substances and It is administered as follows. In embodiments, compounds described herein (e.g., formula (IA-1), ( IB-1), (IA), (IB), (IIA), (IIB), or (III) are selected. Based on the selected route of administration and standard pharmacopoeia, the drug was selected to be pharmaceutically appropriate or acceptable. The carrier (in this specification, a pharmaceutically appropriate (or acceptable) pharmaceutical excipient, physiological A scientifically appropriate (or acceptable) pharmaceutical excipient, or a physiologically appropriate (or It is combined with an acceptable carrier (also called a carrier), which is, for example, Gennaro, A .R., “Remington: The Science and Practice of Pharmacy, 21 st Easton Lippincott (ed.) This is described in Williams & Wilkins, 2005.

[0151] In certain embodiments, formulas (IA), (IB), (IIA), (I) described herein Compounds IB), or (III), are administered as pure chemicals. In terms of application methods, the formulas (IA), (IB), (IIA), (IIB), and other formulas described herein are used. The compounds in (III) are selected based on the chosen route of administration and standard pharmacopoeia. A pharmaceutically appropriate or acceptable carrier (in this specification, a pharmaceutically appropriate (or acceptable) carrier) Pharmaceutical excipients that are acceptable, physiologically appropriate (or acceptable) pharmaceutical excipients, This is combined with a physiologically appropriate (or tolerable) carrier, which is For example, Gennaro, AR, “Remington: The Science and Practice of Pharmacy,”21 st ed., East On: Lippincott Williams & Wilkins, 2005. It will be done.

[0152] Therefore, what is provided herein is a combination of one or more pharmaceutically acceptable carriers Formulas (IA-1), (IB-1), (IA), (IB), (IIA) described herein, A pharmaceutical composition comprising at least one compound of (IIB) or (III), or A pharmaceutically acceptable salt or solvate of [the substance]. Carrier(s) (or pharmaceutical excipient) (Multiple options available)) indicates that the carrier is compatible with the other components of the composition and the recipient of the composition (i.e., If it is not harmful to the subject, it is permissible or appropriate.

[0153] Therefore, what is provided herein is a combination of one or more pharmaceutically acceptable carriers , formulas (IA), (IB), (IIA), (IIB), or (III) as described in this specification A pharmaceutical composition comprising at least one compound thereof, or a pharmaceutically acceptable salt thereof It is a solvate. The carrier(s) (or pharmaceutical excipient(s)) is a composition of the carrier. If the other components are compatible and not harmful to the recipient (i.e., subject) of the composition It is acceptable, permissible, or appropriate.

[0154] One embodiment involves a pharmaceutically acceptable pharmaceutical excipient and a compound of formula (IA-1), or The present invention provides a pharmaceutical composition comprising a pharmaceutically acceptable salt thereof.

[0155] One embodiment involves a pharmaceutically acceptable pharmaceutical excipient and a compound of formula (IB-1), or The present invention provides a pharmaceutical composition comprising a pharmaceutically acceptable salt thereof.

[0156] One embodiment involves a pharmaceutically acceptable pharmaceutical excipient and a compound of formula (IA), or the The present invention provides a pharmaceutical composition comprising a pharmaceutically acceptable salt.

[0157] One embodiment involves a pharmaceutically acceptable pharmaceutical excipient and a compound of formula (IB), or the same. The present invention provides a pharmaceutical composition comprising a pharmaceutically acceptable salt.

[0158] One embodiment involves a pharmaceutically acceptable pharmaceutical excipient and a compound of formula (IIA), or the same. The present invention provides a pharmaceutical composition comprising a pharmaceutically acceptable salt of [the substance].

[0159] One embodiment involves a pharmaceutically acceptable pharmaceutical excipient and a compound of formula (IIB), or the same. The present invention provides a pharmaceutical composition comprising a pharmaceutically acceptable salt of [the substance].

[0160] One embodiment involves a pharmaceutically acceptable pharmaceutical excipient and a compound of formula (III), or the same. The present invention provides a pharmaceutical composition comprising a pharmaceutically acceptable salt of [the substance].

[0161] In this embodiment, the pharmaceutical composition is a compound selected from compound list 1, or the drug thereof. It contains scientifically acceptable salts and pharmaceutically acceptable excipients.

[0162] In embodiments, compounds described herein (e.g., formula (IA-1), (IB-1), ( IA), (IB), (IIA), (IIB), or (III)) are those in which approximately 5% remain unaccounted for. Other organic small molecules, such as a synthesis method, present in amounts of less than 1%, less than 0.1%, or approximately 1% or less. In that it includes the contaminating intermediates or by-products generated in the above steps, it is substantially pure. That is the case.

[0163] In certain embodiments, formulas (IA), (IB), (IIA), (IIB) described herein are used. ), or (III) compounds, if it is less than about 5%, or less than about 1%, or about 0 Less than 0.1% of other small organic molecules, for example, contamination generated in one or more steps of the synthesis method. It is substantially pure in that it contains intermixtures or by-products.

[0164] These pharmaceutical compositions include oral administration, rectal administration, topical administration, oral administration, and parenteral administration. Administration (e.g., subcutaneous, intramuscular, intradermal, or intravenous), vaginal administration, eye drops This includes products suitable for administration or aerosol delivery.

[0165] Exemplary pharmaceutical compositions are, for example, in solid, semi-solid, or liquid form for external or enteral use. Alternatively, in a mixture with an organic or inorganic carrier or pharmaceutical additive suitable for parenteral use, It is used in the form of a pharmaceutical formulation containing one or more of the disclosed compounds as active ingredients. In that embodiment, the active ingredient is, for example, a tablet, pellet, capsule, suppository, solvent, Ordinary non-toxic pharmaceuticals for emulsions, suspensions, and any other form suitable for use. The compound is formulated using a suitably acceptable carrier. The active compound is applied to the disease process or state. It is included in the pharmaceutical composition in an amount sufficient to produce the desired effect.

[0166] In some embodiments for preparing solid compositions such as tablets, the main active ingredient is: A solid comprising a homogeneous mixture of the disclosed compound or a non-toxic, pharmaceutically acceptable salt thereof. To form a preformulation composition, a pharmaceutical carrier, for example, corn starch Lactose, sucrose, sorbitol, talc, stearic acid, magnesium stearate Conventional tablet ingredients such as calcium, dicalcium phosphate, or gum, and other pharmaceutical diluents, For example, it is mixed with water. It is mentioned that these pre-formulation compositions are homogeneous. If so, the composition can be easily put into equally effective unit dosage forms such as tablets, pills, and capsules. This means that the active ingredient is uniformly dispersed throughout the composition, allowing for further subdivision.

[0167] For solid dosage forms for oral administration (capsules, tablets, pills, sugar-coated preparations, powders, granules, etc.), The elephant composition contains one or more pharmaceutically acceptable ingredients such as sodium citrate or dicalcium phosphate. The acceptable carrier and / or the following to be mixed: (1) Filling Agents or fillers, such as starch, cellulose, microcrystalline cellulose, silicified microcrystalline cellulose Sucrose, lactose, sucrose, glucose, mannitol, and / or silicic acid; ( 2) Binders, for example, carboxymethylcellulose, hypromellose, alginate, ze (3) Moisturizers such as latin, polyvinylpyrrolidone, sucrose and / or acacia; (3) Moisturizers , for example, glycerol; (4) Disintegrants, for example, crospovidone, croscarmellose Aluminium, sodium starch glycolate, agar, calcium carbonate, potato starch Alternatively, tapioca starch, alginic acid, certain silicates, and sodium carbonate; (5 (6) Dissolution retarders, e.g., paraffin; (7) Absorption enhancers, e.g., quaternary ammonium compounds (7) Humectants, e.g., sodium doxate, cetyl alcohol and monostearyl (8) Absorbents such as glycerol phosphate and bentonite clay; 9) Lubricants, e.g., talc, calcium stearate, magnesium stearate, solid Polyethylene glycol, sodium lauryl sulfate, and mixtures thereof, as well as (1 0) Coloring agent. In the case of capsules, tablets and pills, in some embodiments the composition is loose. Contains a buffer. In some embodiments, similar types of solid compositions also contain lactose. or a soft material using pharmaceutical additives such as lactose and high molecular weight polyethylene glycol It is used as a filler for hard gelatin capsules.

[0168] In some embodiments, the tablet is compressed or molded using one or more auxiliary components as optional. It is made by. In some embodiments, the compressed tablets also contain a binder (e.g., gelatin). (or hydroxypropyl methylcellulose), lubricant, inert diluent, preservative, disintegrant (For example, sodium starch glycolate or cross-linked carboxymethylcellulose It is prepared using thorium, a surfactant, or a dispersant. In some embodiments, Molded tablets are formed by molding a mixture of the target composition moistened with an inert liquid diluent using an appropriate machine. It is made by the following. In some embodiments, tablets, as well as other solid preparations, such as sugar-coated tablets. The preparations, capsules, pills, and granules may have coatings and shells, such as enteric coatings. Scoring or preparation with a coating and other methods.

[0169] Compositions for inhalation or inhalation may include solutions in pharmaceutically acceptable aqueous or organic solvents. This includes suspensions, or mixtures thereof, as well as powders. Liquid dosage forms for oral administration include , pharmaceutically acceptable emulsions, microemulsions, solutions, suspensions, syrups and elixir are included. In addition to the target composition, in some embodiments, the liquid dosage form is , inert diluents such as water or other solvents, solubilizers and emulsifiers such as ethyl alcohol Alcohol, isopropyl alcohol, ethyl carbonate, ethyl acetate, benzyl alcohol, Benzyl furoseate, propylene glycol, 1,3-butylene glycol, oil (especially cottonseed oil) Oils (peanut oil, corn oil, wheat germ oil, olive oil, castor oil, sesame oil), glycerol Fatty acids of tetrahydrofuryl alcohol, polyethylene glycol, and sorbitan. It contains esters, cyclodextrins, and mixtures thereof.

[0170] In some embodiments, the suspension may contain, in addition to the target composition, for example, isoethoxylated iso Stearyl alcohol, polyoxyethylene sorbitol and sorbitan ester, fine Crystalline cellulose, aluminum metahydroxide, bentonite, agar, and tragacanth, Furthermore, it includes a suspension agent as a mixture of those.

[0171] In some embodiments, formulations for transrectal or transvaginal administration are presented as suppositories, This refers to the target composition, for example, cocoa butter, polyethylene glycol, suppository wax, Alternatively, mix with one or more suitable non-irritating pharmaceutical excipients or carriers containing salicylates. It is prepared by and is a solid at room temperature, but a liquid at body temperature, and therefore, It dissolves within the body cavity and releases the active drug.

[0172] The target composition can be administered in the following transdermal forms: powder, spray, ointment, paste, cream, etc. This includes stimulants, gels, solutions, patches, and inhalants. In some embodiments, active The ingredients are a pharmaceutically acceptable carrier under sterile conditions, and any preservatives and buffers as needed. , or mixed with propellant.

[0173] In some embodiments, ointments, pastes, creams, and gels are added to the composition in question. For example, pharmaceutical additives such as animal and vegetable fats, oils, waxes, paraffin, and densitic acid. Pun, tragacanth, cellulose derivative, polyethylene glycol, silicone, vent It contains kite, silica, talc, and zinc oxide, or mixtures thereof.

[0174] In some embodiments, the powder and spray are used as pharmaceutical additives in addition to the target composition. For example, lactose, talc, silicic acid, aluminum hydroxide, calcium silicate and porcine It comprises riamid powder or a mixture of these substances. In some embodiments, it is sprayed. Furthermore, conventional propellants, such as chlorofluorocarbons and volatile unsubstituted carbons, are also used. It contains hydrogen, such as butane and propane.

[0175] In some embodiments, the compounds described herein are formulated as eye drops for ophthalmic administration. It will be done.

[0176] Alternatively, the compositions and compounds disclosed herein may be administered by aerosol. This involves preparing aqueous aerosols, liposome formulations, or solid particles containing the compound. This is achieved by using non-aqueous (e.g., fluorocarbon propellant) materials. In some embodiments, this is achieved by using non-aqueous (e.g., fluorocarbon propellant) materials. A suspension of the drug is used. In some embodiments, an ultrasonic nebulizer is used. These substances are subjected to shearing, resulting in the decomposition of compounds contained in the target composition. This is because it minimizes the risk of contamination. Typically, aqueous aerosols are used in the aqueous solutions of the target composition. Formulation of a liquid or suspension with conventional pharmaceutically acceptable carriers and stabilizers. It is manufactured by [method]. The carrier and stabilizer vary depending on the requirements of the specific target composition, but [explanation follows]. In terms of type, nonionic surfactants (e.g., Tween, Pluronic, or Poly Ethylene glycol, serum albumin, sorbitan ester, oleic acid, lecithin, Harmless proteins such as amino acids like glycine, buffers, salts, sugars, or sugar alcohols It contains [unclear]. Aerosols are generally prepared from isotonic solutions.

[0177] Pharmaceutical compositions suitable for parenteral administration should be reconstituted into a sterile, injectable solution or dispersion immediately before use. It comprises one or more pharmaceutically acceptable sterile isotonic aqueous or non-aqueous solutions, dispersions, or suspensions. The target composition includes a liquid or emulsion, or a combination with a sterile powder, and these include: In some embodiments, antioxidants, buffers, bacteriostatic agents, and formulations are added to the blood of the target recipient. It contains a solute, suspending agent, or thickener to make it isotonic.

[0178] Examples of suitable aqueous and non-aqueous carriers used in pharmaceutical compositions include water, ethanol, Polyols (e.g., glycerol, propylene glycol, polyethylene glycol, etc.) ), and suitable mixtures thereof, vegetable oils, such as olive oil, and injectable organic Esters, such as ethyl oleate and cyclodextrin, are included. Appropriate fluidity. For example, this involves using coating materials such as lecithin, and maintaining the required particle size in the case of dispersions. , and maintained by the use of surfactants.

[0179] Enteral pharmaceutical preparations containing disclosed compounds and intestinal substances; and their pharmaceutically acceptable Carriers or pharmaceutical excipients are also being considered. Enteric-coated materials are those that are substantially resistant to the acidic environment of the stomach. This refers to polymers that are insoluble and primarily soluble in intestinal fluid at a specific pH. The small intestine is the stomach and large intestine. It is part of the digestive tract (intestines), and includes the duodenum, jejunum, and ileum. The pH of the duodenum is approximately 5.5, the pH of the jejunum is approximately 6.5, and the pH of the distal ileum is approximately It is 7.5. Therefore, enteric coated materials are, for example, about 5.0, about 5.2, about 5.4, about 5.6, approximately 5.8, approximately 6.0, approximately 6.2, approximately 6.4, approximately 6.6, approximately 6.8, approximately 7.0, approximately 7.2, approximately 7.4, approximately 7.6, approximately 7.8, approximately 8.0, approximately 8.2, approximately 8.4, approximately 8.6, approximately pH 8.8, approximately 9.0, approximately 9.2, approximately 9.4, approximately 9.6, approximately 9.8, or approximately 10.0 It is not soluble until [a certain point]. An example of an enteric-coated material is cellulose acetate phthalate (CA). P), hydroxypropyl methylcellulose phthalate (HPMCP), polyvinyl acetate Tetophthalate (PVAP), Hydroxypropyl Methylcellulose Acetate Suci Natate (HPMCAS), Cellulose acetate trimellitate, Hydroxypropyl Meth Chill cellulose succinate, cellulose acetate succinate, cellulose acetate Tohexahydrophthalate, cellulose propionate phthalate, cellulose acetate Tomalate, cellulose acetate butyrate, cellulose acetate propionate , copolymer of methyl methacrylate and methyl methacrylate, methyl acrylate and methyl Copolymer of methacrylate and methacrylic acid, methyl vinyl ether and maleic anhydride Copolymer of substances (Gantrez ES series), ethyl methyl acrylate-methyl Methacrylate-chlorotrimethylammonium ethyl acrylate copolymer, natural tree Fats, such as zein, shellac and copal colophorum, as well as some commercially available Enteric-coated dispersion systems (e.g., Eudragit L30D55, Eudragit F S30D, Eudragit L100, Eudragit S100, Kollico at EMM30D, Estacryl 30D, Coateric, and Aquat This includes eric). The solubility of each of the above materials is known or can be measured in vitro. It can be easily determined.

[0180] At least one compound described herein (e.g., formula (IA-1), (IB-1), Dosage of a composition containing (IA), (IB), (IIA), (IIB), or (III)) This refers to the patient's (e.g., human) condition, i.e., the stage of the disease, general health status, age, It varies depending on other factors as well.

[0181] Formulas (IA), (IB), (IIA), (IIB), or (III) as described herein The dose of a composition containing at least one of the compounds is determined by the patient's (e.g., human) condition, that is, However, this varies depending on the stage of the disease, general health status, age, and other factors.

[0182] Pharmaceutical compositions are administered in a manner appropriate to the disease being treated (or prevented). The appropriate dosage, duration, and frequency of administration depend on the patient's condition, the type and severity of the patient's disease, and It is determined by factors such as the specific form of the active ingredient and the method of administration. Generally, appropriate Dosage and treatment regimens should be determined based on the therapeutic and / or prophylactic benefits (e.g., more frequent complete Total or partial remission, or longer disease-free survival and / or overall survival, A sufficient amount of the composition to provide improved clinical outcomes (such as reduced symptom severity). Provides (multiple options available). The optimal dose is generally determined using experimental models and / or clinical trials. The optimal dose is determined by the patient's body mass, weight, and It depends on blood volume.

[0183] Oral doses are typically in the range of approximately 1.0 mg to 1000 mg, once daily. ~4 times or more.

[0184] The disclosed compounds, at doses that provide optimal efficacy, are intended for subjects requiring such treatment. Or it is administered to patients (animals and humans). The dose required for any specific use is , not only the specific compound or composition selected, but also the route of administration, the nature of the condition being treated, The patient's age and condition, concomitant medications or special diets and subsequent patient adherence to them, and other factors. It is understood that the appropriate dosage varies from patient to patient depending on the factors, and ultimately the appropriate dosage should be determined by the attending physician. It is left to discretion. Disclosed herein for the treatment of the aforementioned clinical conditions and diseases. The intended compounds are conventional non-toxic, pharmaceutically acceptable carriers, adjuvants, and excipients. In drug formulations containing the agent, administered orally, subcutaneously, topically, parenterally, or by inhalation spray. It is administered rectally. Parenteral administration can be done by subcutaneous injection, intravenous injection, or intramuscular injection. This includes injection methods.

[0185] V. Methods using compounds and compositions mAChR M1 Antagonist Muscarinic acetylcholine receptor M1 (mAChR M1) is involved in the central nervous system and peripheral nerves. It is found in both the cerebral cortex and sympathetic ganglia. In particular, M1 is an oligodendrocyte of the central nervous system. It is expressed in endoplasmic progenitor cells (OPCs). Over time, OPCs produce myelin. It differentiates into living oligodendrocytes. Myelin is essential for action potential conduction along the axon. The loss is attributed to neurodegenerative disorders, particularly multiple sclerosis. In some embodiments, Selective mAChR M1 antagonists promote OPC differentiation into oligodendrocytes. To promote. In some embodiments, selective mAChR M1 antagonists promote multiple occurrences. It is useful in the treatment of demyelinating disorders such as sclerosis. In some embodiments, selective mACh R M1 antagonists are associated with epilepsy, as well as Parkinson's disease, dystonia, and other conditions. It is useful in treating certain movement disorders, including fragile X syndrome.

[0186] In one embodiment, the compounds disclosed herein are muscarinic acetylcholine M1 receptors. It is a selective antagonist of (mAChR M1). In some embodiments, this specification The compounds disclosed herein are one or more mAChR M2, M3, M4, or M5 receptors. Selective antagonistization of muscarinic acetylcholine M1 receptor (mAChR M1) It is a stent. In some embodiments, the compounds disclosed herein are mAChR M1 response IC 50 This shows that it is about one-fifth, or about 10 times, that of the mAChR M2. 1 / 1, approximately 1 / 20, approximately 1 / 30, approximately 1 / 50, approximately 1 / 100, or approximately 1 / 100 It is 1 / 1 or more. In some embodiments, the compounds disclosed herein are mACh R M1 response IC 50 This shows that this is about one-fifth of that of the mAChR M3, approximately 1 / 10, approximately 1 / 20, approximately 1 / 30, approximately 1 / 50, approximately 1 / 100, or approximately 1 It is 1 / 00 ​​or more. In some embodiments, the compounds disclosed herein are mA ChR M1 response IC 50 This shows that this is about one-fifth of that of the mAChR M4. Approximately 1 / 10, 1 / 20, 1 / 30, 1 / 50, 1 / 100, or It is approximately 1 / 100 or more. In some embodiments, the compounds disclosed herein are mAChR M1 response IC 50 This indicates that it takes about 5 minutes longer than the mAChR M5. 1 / 10, 1 / 20, 1 / 30, 1 / 50, 1 / 100, The ratio is approximately 1 / 100 or more. In some embodiments, the compounds disclosed herein This is an IC with mAChR M1 response. 50This indicates that mAChR M2, M3, M4, Alternatively, it's about 1 / 5, 1 / 10, or 2 times less than M5 or a combination of those. 1 / 0, approximately 1 / 30, approximately 1 / 50, approximately 1 / 100, or more than approximately 1 / 100 be.

[0187] treatment The compounds disclosed herein are intended for the treatment, prevention, improvement, control, or risk reduction of various disorders. It is useful for reduction, and here the patient or subject is muscarinic acetylcholine M1 receptor They will benefit from the antagonistic effect.

[0188] In one embodiment, the treatment selectively targets M1 receptors to an extent that is effective in influencing cholinergic activity. It may include antagonistic effects. Therefore, the hindrances for which the compounds disclosed herein are useful are Phosphoric activity may be associated with, for example, enhanced cholinergic function. In some embodiments, as described herein Provided are doses and amounts effective for treating the target disorder, as disclosed herein. A compound, or a pharmaceutically acceptable salt or solvate thereof, or a drug as described herein. A method for treating or preventing a disorder of a subject, comprising administering a scientific composition to the subject.

[0189] This specification provides for the inhibition of muscarinic acetylcholine receptors in the subject. A method for treating one or more disorders in which the treatment is expected to be beneficial, wherein the disorder in question is In doses and amounts effective for treatment, the compounds disclosed herein, or their pharmaceutically appropriate Administer an acceptable salt or solvate, or a pharmaceutical composition as described herein. This is a method that includes the following.

[0190] Some embodiments provided herein require the treatment of neurodegenerative disorders. A method for doing so in a target, wherein a therapeutically effective amount of the compound described herein (e.g.) , equations (IA-1), (IB-1), (IA), (IB), (IIA), (IIB), also (III)) or a pharmaceutically acceptable salt or solvate thereof may be administered to the target. This method includes the following:

[0191] Some embodiments provided herein require the treatment of neurodegenerative disorders. A method for performing this in a target, wherein the formula for the effective therapeutic dose is (IA), (IB), (IIA ), (IIB), or (III) compounds, or pharmaceutically acceptable salts thereof This method involves administering a solvate to the target.

[0192] In one embodiment, a method for treating neurodegenerative disorders in a subject who requires treatment. This also includes an effective amount of a compound selected from compound list 1, or a pharmaceutically acceptable salt thereof. This includes administering a solvate.

[0193] Some embodiments provided herein describe the treatment of neurological disorders A method for doing so in an elephant, wherein a therapeutically effective amount of the compound described herein (e.g., formula (IA-1), (IB-1), (IA), (IB), (IIA), (IIB), or ( III)) administration of a pharmaceutically acceptable salt or solvate thereof to the target This includes methods. Some embodiments are for subjects requiring treatment of neurological disorders. A method for doing so, wherein a therapeutically effective amount of the compound described herein (for example, formula (I A-1), (IB-1), (IA), (IB), (IIA), (IIB), or (II I)) including administration of a pharmaceutically acceptable salt or solvate thereof to the target. The method involves treating nerve damage, specifically peripheral nerve damage. Several embodiments describe how to treat nerve damage. A method for providing medical treatment to an object that requires medical treatment, wherein the therapeutically effective amount is specified herein The compounds listed (e.g., formulas (IA-1), (IB-1), (IA), (IB), (IIA) ), (IIB), or (III), or a pharmaceutically acceptable salt or solvation thereof. This method involves administering a substance to a target, and the nerve damage is diabetic neuropathy.

[0194] Some embodiments provided herein describe the treatment of neurological disorders A method for doing so in elephants, with the formulas for the effective therapeutic dose (IA), (IB), (IIA), Compounds of type (IIB) or (III), or their pharmaceutically acceptable salts or solutions. The method involves administering a mediator to the target. Some embodiments treat neurological disorders. A method for providing treatment to a person who requires treatment, and the formula for the effective therapeutic dose (IA) Compounds of (IB), (IIA), (IIB), or (III), or their pharmaceutical properties This includes administering a salt or solvate that is acceptable to the target, and the nerve damage is peripheral neuropathy. It is harmful, it is a method. Some embodiments require the treatment of neurological disorders. A method for doing so in elephants, with the formulas for the effective therapeutic dose (IA), (IB), (IIA), Compounds of type (IIB) or (III), or their pharmaceutically acceptable salts or solutions. A method that includes administering a mediator to the target, wherein the neuropathy is diabetic neuropathy. .

[0195] In one embodiment, a method for treating a neurological disorder in a subject requiring treatment is: An effective amount of a compound selected from compound list 1, or a pharmaceutically acceptable salt thereof, This includes administering a solvate.

[0196] Some embodiments perform this in subjects who require treatment for demyelinating diseases. A method wherein a therapeutically effective amount of the compound described herein (e.g., formula (IA-1), (I B-1), (IA), (IB), (IIA), (IIB), or (III), or The method involves administering a pharmaceutically acceptable salt or solvate to the subject. Some embodiments do so in subjects who require treatment for demyelinating diseases. A method comprising a therapeutically effective amount of a compound described herein (e.g., formula (IA-1), (IB) -1), (IA), (IB), (IIA), (IIB), or (III), or so This includes administering a pharmaceutically acceptable salt or solvate of to the target of demyelinating diseases, This describes a method for treating demyelinating diseases of the central nervous system. Several embodiments describe methods for treating demyelinating diseases. A method for doing so in a subject where it is necessary, and the therapeutically effective amount described herein The listed compounds (for example, formulas (IA-1), (IB-1), (IA), (IB), (IIA)) , (IIB), or (III)), or a pharmaceutically acceptable salt or solvate thereof The method involves administering the drug to the target, and the demyelinating disease is multiple sclerosis. That embodiment is a method for treating a demyelinating disease in a subject that requires treatment. There is a therapeutically effective amount of the compounds described herein (e.g., formula (IA-1), (IB-1) , (IA), (IB), (IIA), (IIB), or (III)), or its pharmaceutical This includes administering a moderately tolerable salt or solvate to a target, and is used for demyelinating diseases, including peripheral nerves. This is a method for treating demyelinating diseases of the circulatory system.

[0197] Some embodiments perform this in subjects who require treatment for demyelinating diseases. The method involves formulas for the effective therapeutic dose (IA), (IB), (IIA), (IIB), or (III) is administered as a compound, or a pharmaceutically acceptable salt or solvate thereof. This is a method that includes doing so. Some embodiments require the treatment of demyelinating diseases. A method for performing this in a subject, wherein the formula for the effective therapeutic dose is (IA), (IB), (I Compounds of type IA), (IIB), or (III), or their pharmaceutically acceptable salts. This includes administering a solvate to a demyelinating disease, or a demyelinating disease of the central nervous system. There is a method. Some embodiments describe subjects that require treatment for demyelinating diseases. A method for doing so in which the formula for the effective therapeutic dose is (IA), (IB), (IIA), ( Compounds of type IIB, or type (III), or their pharmaceutically acceptable salts or solvents. This method involves administering a Japanese drug to a target, where the demyelinating disease is multiple sclerosis. Several embodiments describe how to perform treatment in subjects who require treatment for demyelinating diseases. The law is defined by the formula (IA), (IB), (IIA), (IIB), or ( III) The compound, or a pharmaceutically acceptable salt or solvate thereof, is administered to the target. This includes the definition of demyelinating diseases as demyelinating diseases of the peripheral nervous system.

[0198] In one embodiment, a method for treating a demyelinating disease in a subject that requires treatment is described. , an effective amount of the compound selected from compound list 1, or a pharmaceutically acceptable salt thereof. This includes administering a solvate.

[0199] Some embodiments describe the adjustment of muscarinic acetylcholine receptor M1 activity in a subject. A method relating to the compounds described herein (e.g., formulas (IA-1), (IB-1)) , (IA), (IB), (IIA), (IIB), or (III)), or those This method involves administering a pharmaceutically acceptable salt or solvate to the target. In some embodiments, compounds described herein (e.g., formula (IA-1), (IB-1) , (IA), (IB), (IIA), (IIB), or (III)), or those Pharmacologically acceptable salts or solvates act as selective M1 antagonists.

[0200] Some embodiments describe the adjustment of muscarinic acetylcholine receptor M1 activity in a subject. A method of constructing a clause, using formulas (IA), (IB), (IIA), (IIB), or (II The compounds in I), or their pharmaceutically acceptable salts or solvates, are administered to the target. This method includes the following: In some embodiments, formulas (IA), (IB), (IIA) Compounds of (IIB), or (III), or their pharmaceutically acceptable salts. The solvates act as selective M1 antagonists.

[0201] In this embodiment, a method for regulating muscarinic acetylcholine receptor M1 activity in a subject is described. The law applies to compounds selected from compound list 1, or pharmaceutically acceptable salts thereof or This includes administering a solvate.

[0202] VI. Combination Therapy Furthermore, this specification aims to provide beneficial effects from the interactions of these therapeutic agents. As part of a specific treatment regimen, for example, the disclosed compounds and additional active agents Combination therapy involving the simultaneous administration of the agents is also being considered. In some embodiments, as described herein. The compound is administered in combination with one or more immunomodulators. In some embodiments, The compounds described herein are administered in combination with one or more immunomodulators, and one or more The immunomodulators include IFN-β1 molecules; corticosteroids; glutamic acid, lysine, and ara. Polymers or glutillamers of nin, tyrosine; antibodies against alpha-4 integrin or fragments thereof or natalizumab; anthracendione molecule or mitoxantrone ;Fingolimod or other S1Pl functional modifiers;Dimethyl fumarate or other N RF2 functional modifier; the alpha subunit of the IL-2 receptor (CD25) on T cells. Antibodies against or daclizumab; antibodies against CD52 or alemtuzumab; CD20 Antibodies or ocrelizumab against dihydroorote dehydrogenase; and inhibition of dihydroorote dehydrogenase. Selected from an agent or teriflunomide. In some embodiments, the immunomodulator is IF It is an N-β1 molecule. In some embodiments, the immunomodulator is a corticosteroid. In some embodiments, the immunomodulators include glutamic acid, lysine, alanine, and The immunomodulator is a polymer or glatiramer of tyrosine. In some embodiments, the immunomodulator is This is an antibody against alpha-4 integrin, a fragment thereof, or natalizumab. In some embodiments, the immunomodulator is an anthracendione molecule or mitoxanthrone. In some embodiments, the immunomodulator is fingolimod or other S1P1 It is a functional modifier. In some embodiments, the immunomodulator is dimethyl fumarate. or other NRF2 functional modifiers. In some embodiments, immunomodulators are T-cells Antibodies or dacrisps against the alpha subunit of the IL-2 receptor (CD25) in cells In some embodiments, the immunomodulator is an antibody against CD52 or an allele. It is tuzumab. In some embodiments, the immunomodulator is an antibody against CD20 or In some embodiments, the immunomodulator is dihydroorotate dehyphenate. It is an inhibitor of dragenase or teriflunomide.

[0203] The beneficial effects of combinations include pharmacokinetic or therapeutic effects resulting from the combination of therapeutic agents. This includes, but is not limited to, chemical interactions. These interactions may occur in combinations of these therapeutic agents. Administration typically lasts for a predetermined period (usually several weeks or months, depending on the chosen combination). It is carried out over a period of several years. Combination therapy involves administering multiple therapeutic agents in succession. In other words, not only is it necessary to administer each therapeutic agent at different times, but these therapeutic agents, or the This is intended to include administering at least two of the therapeutic agents substantially simultaneously. Yes, they are.

[0204] Substantially simultaneous administration is, for example, a single formulation or composition (e.g., a fixed ratio of each therapeutic agent). Tablets or capsules having a specific dosage, or multiple single formulations of each therapeutic agent (e.g., This is achieved by administering capsules to the target. Each therapeutic agent is sequential or substantial Simultaneous administration is possible via oral, intravenous, intramuscular, and mucosal tissue routes. This is carried out by any suitable route, including but not limited to the direct absorption route. The medication is administered via the same route or different routes. For example, the first of the selected combinations The treatment agent is administered by intravenous injection, while the other treatment agents in the combination are administered orally. Alternatively, for example, all therapeutic agents may be administered orally, or all therapeutic agents may be It is administered by intravenous injection.

[0205] Combination therapy also involves further combinations with other biologically active ingredients and non-pharmacological therapies. This includes the administration of the above-mentioned therapeutic agents. Non-pharmacological treatments achieve beneficial effects from the interaction of combinations of therapeutic and non-pharmacological treatments. It is performed at any appropriate time, as long as it is possible. For example, if appropriate, non-pharmacological treatment may be performed. Even when the administration is temporarily discontinued, perhaps for a few days or weeks, the beneficial effect may persist. The result is achieved.

[0206] The combined components are administered to the patient simultaneously or sequentially. The components are pharmaceutically similar. It will be understood that they are present in an acceptable carrier and therefore administered simultaneously. Alternatively, the active ingredient may be administered simultaneously or consecutively in a separate medication such as a conventional oral dosage form. It is present in the drug carrier.

[0207] The following examples are provided merely as illustrations of various embodiments, and the present invention is not intended to be used in any way. It should not be interpreted as something that limits the meaning.

[0208] The examples and embodiments described herein are for illustrative purposes only and should not be taken into consideration. Various modifications or changes are suggested to those skilled in the art, and the intent of this application and the attached claims is... All publications, patents, and patents cited herein should be included within the scope of: all publications, patents, and patents cited herein. The patent application is incorporated herein by reference in its entirety for all purposes.

[0209] VII. Preparation of Compounds The compounds used in the reactions described herein are commercially available chemicals and / or chemical literature. Starting from the compounds described, they are prepared according to known organic synthesis techniques. "Chemical materials" include Acros Organics (Geel, Belgium) and Aldri. ch Chemical(Milwaukee,WI,Sigma Chemical (including Fluka), Apin Chemicals Ltd. (Milton Park, UK), Ark Pharm, Inc. (Libertyville, IL) ), Avocado Research (Lancashire, UK), BDH Inc. (Toronto, Canada), Bionet (Cornwall, UK) .), Chemservice Inc. (West Chester, PA), Com bi-blocks (San Diego, CA), Crescent Chemica l Co. (Hauppauge, NY), eMolecules (San Diego) , CA), Fisher Scientific Co. (Pittsburgh, PA) ), Fisons Chemicals (Leicestershire, UK), Fr. ontier Scientific (Logan, UT), ICN Biomedic als, Inc. (Costa Mesa, CA), Key Organics (Cor nwall,UK), Lancaster Synthesis(Windham, NH), Matrix Scientific, (Columbia, SC), Mayb ridge Chemical Co. Ltd. (Cornwall, UK), Pa. rish Chemical Co. (Orem, UT), Pfaltz & Baue r, Inc. (Waterbury, CN), Polyorganix (Houston , TX), Pierce Chemical Co. (Rockford, IL), Ri edel de Haen AG (Hanover, Germany), Ryan Sc. ientific, Inc. (Mount Pleasant, SC), Spectru m Chemicals (Gardena, CA), Sundia Meditech, (Shanghai,China), TCI America(Portland,OR) ), Trans World Chemicals, Inc. (Rockville, M. D), and standard commercial suppliers including WuXi (Shanghai, China) I obtained it.

[0210] This specification details the synthesis of reactants useful for the preparation of the compounds described herein, or the preparation of reactants. Appropriate reference books and papers that provide references to the articles mentioned include, for example, “ Synthetic Organic Chemistry,”New York:Jo hn Wiley & Sons, Inc.,1982;Sandler SRet al.,“Organic Functional Group Preparati ons,”2 nded., New York: Academic Press, 198. 3;House,HO,“Modern Synthetic Reactions "2 nd ed.,Menlo Park:WABenjamin,Inc.,1 972;Gilchrist,TL,“Heterocyclic Chemist ry,”2 nd ed., New York: Wiley, 1992; March, J. ,“Advanced Organic Chemistry:Reactions,M "Echanisms and Structure," 4 th ed., New York k: Wiley, 1992 is included. Reactants useful for the preparation of the compounds described herein Additional references to articles that detail the synthesis or describe the preparation. Suitable reference books and articles include, for example, Fuhrhop, J., Penzlin, G. , “Organic Synthesis: Concepts, Methods, Sta. rting materials, 2 nd ed., New York: Wiley, 1994;Hoffman,RV,“Organic Chemistry,An Intermediate Text,”Oxford:Oxford Univers ity Press, 1996; Larock, RC, “Comprehensiv. e Organic Transformations: A Guide to Fun ctional Group Preparations,”2 nd ed., New York: Wiley, 1999; Otera, J., “Modern Carbony l Chemistry,”New York:Wiley,2000;Solomon s,TWG,“Organic Chemistry,”7 th ed., New York: Wiley, 2000; Stowell, JC, “Intermedi ate Organic Chemistry, 2 nd ed., New York: Wiley,1993;“Industrial Organic Chemicals :Starting Materials and Intermediates:An Ullmann's Encyclopedia,”New York:Wiley, 8 volumes;“Organic Reactions,”New York:W iley, 55 volumes; and “Chemistry of Function "nal Groups," New York: Wiley, includes 73 volumes. It can be done.

[0211] Furthermore, specific reactants and similar reactants can be found in the American Chemical Society's chemical information retrieval service. An index of known chemical substances was thus created (this is available in most public libraries and (Available in university libraries), and identified by online databases (details For further details, please contact the American Chemical Society (Washington, D.C.). Known However, chemicals not listed in the catalog can be synthesized at will by custom chemical companies. It is prepared and many standard chemical suppliers (e.g., the companies listed above) use it. We provide stam synthesis services. Preparation and selection of pharmaceutical salts of the compounds described herein. References related to this can be found in Stahl, PH, Wermuth, CG, “Handb ook of Pharmaceutical Salts,”Zurich:Verl ag Helvetica Chimica Acta, 2002.

[0212] List of abbreviations As used above and throughout this disclosure, the following abbreviations are not specifically indicated. Unless otherwise specified, it should be understood to have the following meaning: [Table 1-1] [Table 1-2]

[0213] General synthesis scheme Compounds of formula (IA) or (IB) in this disclosure include, for example, HATU, CDI, T3, etc. In the presence of a suitable coupling reagent and a suitable base such as TEA, DIEA, etc., (1a) or (1b), or the corresponding ammonium salt thereof, and carboxylic acid ( 2) can be prepared from (Scheme 1). Alternatively, the acid can be thionyl chloride, or o Pre-activation is performed by using drugs such as xalil to convert them into the corresponding acid chlorides. This can be done. The resulting amide (3a) or (3b) is itself formula (IA). It could be a compound of formula (IB), and to deliver another compound of formula (IA) or (IB) Furthermore, it can be further functionalized using a synthesis methodology readily known to those skilled in the art. Examples of such conversions include, but are not limited to, the following: (a) Catalysts such as Pd / C and Pd(OH)2, and reductions such as hydrogen gas and deuterium gas. Reduction of alkenes or alkynes in the presence of an agent. (b) Methylene sources such as trimethylsulfonium iodide and diazomethane, and potassium In the presence of accelerators such as um tert-butoxide and palladium(II) acetate, Converting Luken to cyclopropane. (c) Oxidation of sulfides in the presence of oxidizing agents such as oxone and mCPBA. (d) Methyl sources such as iodomethane and dimethyl sulfate, and sodium iodide , in the presence of accelerators such as potassium iodide, appropriately functionalized 2- or 4-methyl The corresponding cypyridine is 1-methylpyridine-2(1H)-one or 1-methylpyridine. Conversion to zinc-4(1H)-one. (e) Suitable palladium ligand complexes as catalysts and cyanide as a cyanide source In the presence of zinc, etc., the corresponding (hetero)aryl halides of appropriately functionalized (hetero)aryl halides Conversion to hetero)aryl cyanide. (f) Use an appropriate chiral column such as chiral PAK OD or chiral PAK AD. , separation of a mixture of stereoisomers into its stereochemically concentrated component. [ka]

[0214] Alternatively, use a suitable protective amine (4a) or (4b) and a carboxylic acid (2) The first coupling, followed by the amide (5a) using conditions readily apparent to those skilled in the art. Or (5b) removing the protecting group (PG) in (i.e., N-PG is tert-butyl In the case of carbamates, treatment with HCl, TFA, etc. is performed to obtain the final result. The amine (6a) or (6b) is subjected, for example, to standard aromatic electrophilic substitution conditions (i.e., (Also, by heating the reactants in a polar aprotic solvent in the presence of a suitable base.) The Buchwald-Hartwig coupling conditions (i.e., the appropriate catalyst) Coupling in the presence of palladium ligand complexes and metal alkoxides as bases 3) involves reacting with an appropriate functionalized (hetero)aryl halide using ( ). Prepare the compound of formula (IA) or (IB) via a step sequence (Scheme 2). Doing so may be more advantageous. [ka]

[0215] In certain embodiments, those skilled in the art will also refer to the provisions described in the reference books and papers previously highlighted. Using this, via direct nucleophilic substitution of the leaving group (LG) in (8a) or (8b) , through the bond between electrophile (9) and electrophile (8a) or (8b), formula (IA) or It is also possible to access compounds of (IB) (Scheme 3). In certain cases, especially sought If the electron agent (9) is an amine, then (9) is the chloride of isopropylmagnesium chloride. Pre-treatment with a chemical such as a thium complex may be beneficial for initial activation. The electrophile (8a) or (8b) itself is an appropriate one, such as TEA, DIEA, etc. It can be easily synthesized from an amine (1a) or (1b) and an acid chloride (7) in the presence of a base. It is possible. [ka]

[0216] In certain embodiments, the direct nucleophilic substitution described above uses an amide (11a) or an electrophile. This can be optimally achieved by using (11b), which itself is amine (1 a) or (1b) and acid (10), for example, a two-step amide coupling-decompression It is easily prepared by a protection sequence and appropriately functionalized as an electrophile (12) Scheme 4). [ka]

[0217] Regarding specific embodiments of formula (IA) or (IB) where X is NH, well known to those skilled in the art Under dehydration conditions, use ketones (14) and amines (13a) or (13b) as needed. It can be proven that forming a bond is more advantageous (Scheme 5). The ff base (15a) or (15b) is lithium borohydride, nanoborohydride. Reduction can be performed using reagents such as thorium, or Grignard reagent, (hetero) Ally. It can be captured with organometallic compounds such as lithium reagents. Organometallic compounds can capture organometallic compounds. In the case of an i-based reagent, fluoride activators such as TBAF and cesium fluoride may be added. It could be beneficial. [ka]

[0218] The general synthesis schemes described above are illustrative and not limited to... It is intended to have the properties described. Many of the reagents provided in the following examples are other It should also be understood that it can be replaced with an appropriate reagent (for example, Fieser, L). .,et al.,“Encyclopedia of Reagents for O rganic Synthesis,2 nd ed., New York: Wiley (See 2009). In addition, solvent selection, reaction temperature, volume and reaction time, etc. It will be understood that these conditions can still be changed while producing the desired compound. The chemical structures, substituents, derivatives, intermediates and / or related to the synthesis provided in the specification Such changes and modifications, including but not limited to those mentioned above, shall not be in any spirit or scope. It can be done without deviation.

[0219] VIII. Embodiments Embodiment P1. A compound, or a pharmaceutically acceptable salt or solvate thereof, Having the structure of formula (IA) or (IB), [ka] During the ceremony, X is bonded, -C(R 9 )(R 10 )-,-N(R 11 )-, -O-, -S(O) n - -CH2N(R 11 )-, or -CH2O-, Y is -CH2-, -CH2CH2-, -CH=CH-, or -CH2OCH2- can be, R 1 but, [ka] In the formula, ring A is either a 5-membered or 6-membered heteroaryl ring, or optionally, Rogen, Cyano, -N(R) 14 )(R 15 ), C 1-6 Alkyl, C 1-6 Alkoxy, C 1-6 Haloalkyl, C 1-6 Haloalkoxy, C 3-6 Cycloalkyl, C 3-6 C Chloalkoxy, C3-6 Halocycloalkyl, C 3-6 Halocycloalkoxy, hetero Cycloalkyl, aryl, heteroaryl, S(O) n (R 16 ), or -SF5 A 5-membered or 6-membered heterocycloalkyl ring substituted with a heteroaryl or hete The rocycloalkyl ring consists of 1, 2, or 3 elements selected from the group consisting of O, N, or S. It contains heteroatoms, R 2 However, hydrogen, deuterium, halogen, hydroxyl, C 1-6 Alkyl, C 1-6 Arco Kishi, C 1-6 Haloalkyl, C 1-6 Haloalkoxy, C 3-6 Cycloalkyl, C3 -6 Cycloalkoxy, C 3-6 Halocycloalkyl, C 3-6 Halocycloalkoxy, C 1-6 Alkylhydroxyl, heterocycloalkyl, aryl, or heteroaryl It is R 3 However, halogen, C 1-6 Alkyl, C 1-6 Alkoxy, C 1-6 Haloalkyl, C 1-6 Haloalkoxy, C 3-6 Cycloalkyl, C 3-6 Cycloalkoxy, C 3- 6-halocycloalkyl, C 3-6 Halocycloalkoxy, C 1-6 Alkylhydroxyl , heterocycloalkyl, aryl, or heteroaryl, or R 2 and R 3 They are connected, and optionally, halogen, C 1-6 Alkyl, or C 3-6 Cycloalkyl Forms a cycloalkyl or heterocycloalkyl ring substituted with , R 4 and R 5 These independently produce hydrogen, deuterium, halogens, and C 1-3 Selected from alkyl groups Selected, or R 3 and R 4 They are connected, and optionally, halogen, C 1-6 Alkyl, also or C 3-6 Cycloalkyl or heterocycloalkyl Forming a ring, or R 4 and R 5 They are connected, and optionally, halogen, C 1-6 Alkyl , or C 3-6 Cycloalkyl or heterocycloalkyl substituted Forms a Kill ring, R 6 and R 7 These independently produce hydrogen, deuterium, halogens, and C 1-3 Selected from alkyl groups Selected, or R 3 and R 7 They are connected, and optionally, halogen, C 1-6 Alkyl, also or C 3-6 Cycloalkyl or heterocycloalkyl Forming a ring, or R 4 and R 6 They are connected, and optionally, halogen, C 1-6 Alkyl , or C 3-6 Cycloalkyl or heterocycloalkyl substituted It forms a kill ring, or R 5 and R 7 They connect to form a bond, R 8 but, [ka] And, R 9 and R 10 These independently produce hydrogen, deuterium, halogens, and C 1-6 Alkyl, C 1-6 Alkoxy, C 1-6 Haloalkyl, C 1-6 Haloalkoxy, C 3-6 Cycloalkyl , C 3-6 Cycloalkoxy, C 3-6 Halocycloalkyl, C 3-6 Halocycloalco Selected from xy, heterocycloalkyl, aryl, or heteroaryl, is R 3 and R 10 They are connected, and optionally, halogen, C 1-6 Alkyl, or C 3- Forming a cycloalkyl or heterocycloalkyl ring substituted with a 6-cycloalkyl group, Or R 4 and R 10 They are connected, and optionally, halogen, C 1-6 Alkyl, or C 3-6 A cycloalkyl or heterocycloalkyl ring substituted with a cycloalkyl group accomplish, or R 6 and R 10 They are connected, and optionally, halogen, C 1-6 Alkyl, also or C 3-6 Cycloalkyl or heterocycloalkyl Forming a ring, or R 9 and R 10 They are connected, and optionally, halogen, C 1-6 Alki Ru, or C 3-6 Cycloalkyl or heterocycloalkyl substituted Forms a lucyl ring, R 11 However, hydrogen, C 1-6 Alkyl, C 1-6Haloalkyl, C 3-6 Cycloalkyl , C 3-6 Halocycloalkyl, heterocycloalkylaryl, or heteroaryl It is R 3 and R 11 They are connected, and optionally, halogen, C 1-6 Alkyl, Or C 3-6 Forms a heteroalkyl ring substituted with a cycloalkyl group, or R 4 oh Call R 11 They are connected, and optionally, halogen, C 1-6 Alkyl, or C 3-6 Cyclo Forms a heteroalkyl ring substituted with alkyl, or R 6 and R 11 They are connected, Optionally, halogen, C 1-6 Alkyl, or C 3-6 cycloalkyl substituted Forms a teloalkyl ring, Each R 12 These independently consist of hydroxyl, halogen, cyano, and -N(R) 14 )(R 15 ), C 1-6 Alkyl, C 1-6 Alkoxy, C 1-6 Haloalkyl, C 1-6 Haloalcochry C 3-6 Cycloalkyl, C 3-6 Cycloalkoxy, C 3-6 Halocycloalkyl , C 3-6 Halocycloalkoxy, C 1-6 Alkylhydroxyl, heterocycloalkyl Ru, aryl, heteroaryl, S(O) n (R 16 ), or selected from SF5, Or R 3 and one R 12 They are connected, and optionally, halogen, C 1-6Alkyl, also or C 3-6 A cycloalkyl or heteroalkyl ring substituted with a cycloalkyl group accomplish, or R 10 and one R 12 They are connected, and optionally, halogen, C 1-6 Al Kill, or C 3-6 Cycloalkyl or heteroalkyl substituted Forms a ring, or R 11 and one R 12 They are connected, and optionally, halogen, C1 -6 Alkyl, or C 3-6 Forms a heteroalkyl ring substituted with a cycloalkyl group. , R 13 However, hydrogen, C 1-6 Alkyl, C 1-6 Haloalkyl, C 3-6 Cycloalkyl , C 3-6 Halocycloalkyl, heterocycloalkyl, aryl, or heteroaryl It is R 14 and R 15 Hydrogen, C 1-6 Alkyl, C 1-6 Haloalkyl, C 3-6 Cycloalkyl, C 3-6 Halocycloalkyl, heterocycloalkyl, aryl , or selected from heteroaryls, or R 14 and R 15 They are linked together, arbitrarily , halogen, C 1-6 Alkyl, or C 3-6 Heterocyclic substituted Forms a chloroalkyl ring, R 16 However, C 1-6 Alkyl, C 1-6 Haloalkyl, C 3-6 Cycloalkyl, C3 -6 Halocycloalkyl, heterocycloalkyl, aryl, or heteroaryl the law of nature, m is 0 or 1, n is 0, 1, or 2, A compound, or a pharmaceutically acceptable salt thereof, in which o is 0, 1, 2, or 3 It is a solvate. Embodiment P2. Having the structure of formula (IIA) or (IIB), [ka] During the ceremony, X is bonded, -C(R 9 )(R 10 )-,-N(R 11 )-, -O-, -S(O) n - -CH2N(R 11 )-, or -CH2O-, Y is -CH2-, -CH2CH2-, -CH=CH-, or -CH2OCH2- can be, R 1 but, [ka] In the formula, ring A is either a 5-membered or 6-membered heteroaryl ring, or optionally, Rogen, Cyano, -N(R) 14 )(R 15 ), C 1-6 Alkyl, C 1-6 Alkoxy, C 1-6 Haloalkyl, C 1-6 Haloalkoxy, C 3-6 Cycloalkyl, C 3-6 C Chloalkoxy, C 3-6 Halocycloalkyl, C 3-6 Halocycloalkoxy, hetero Cycloalkyl, aryl, heteroaryl, S(O) n (R 16 ), or -SF5 A 5-membered or 6-membered heterocycloalkyl ring substituted with a heteroaryl or hete The rocycloalkyl ring consists of 1, 2, or 3 elements selected from the group consisting of O, N, or S. It contains heteroatoms, R 2 However, hydrogen, deuterium, halogen, hydroxyl, C 1-6 Alkyl, C 1-6 Arco Kishi, C 1-6 Haloalkyl, C 1-6 Haloalkoxy, C 3-6 Cycloalkyl, C3 -6 Cycloalkoxy, C 3-6 Halocycloalkyl, C 3-6 Halocycloalkoxy, C 1-6 Alkylhydroxyl, heterocycloalkyl, aryl, or heteroaryl It is R 3 However, halogen, C 1-6 Alkyl, C 1-6 Alkoxy, C 1-6 Haloalkyl, C 1-6 Haloalkoxy, C 3-6 Cycloalkyl, C 3-6 Cycloalkoxy, C 3- 6-halocycloalkyl, C 3-6 Halocycloalkoxy, C 1-6 Alkylhydroxyl , heterocycloalkyl, aryl, or heteroaryl, or R 2 and R 3 They are connected, and optionally, halogen, C 1-6 Alkyl, or C 3-6 Cycloalkyl Forms a cycloalkyl or heterocycloalkyl ring substituted with , R 8 but, [ka] And, R 9 and R 10 These independently produce hydrogen, deuterium, halogens, and C 1-6 Alkyl, C 1-6 Alkoxy, C 1-6 Haloalkyl, C 1-6 Haloalkoxy, C 3-6 Cycloalkyl , C 3-6 Cycloalkoxy, C 3-6 Halocycloalkyl, C 3-6 Halocycloalco Selected from xy, heterocycloalkyl, aryl, or heteroaryl, is R 3 and R 10 They are connected, and optionally, halogen, C 1-6 Alkyl, or C 3- Forming a cycloalkyl or heterocycloalkyl ring substituted with a 6-cycloalkyl group, Or R 9 and R 10 They are connected, and optionally, halogen, C 1-6 Alkyl, or C 3-6 A cycloalkyl or heterocycloalkyl ring substituted with a cycloalkyl group accomplish, R 11 However, hydrogen, C 1-6 Alkyl, C 1-6 Haloalkyl, C 3-6 Cycloalkyl , C 3-6 Halocycloalkyl, heterocycloalkylaryl, or heteroaryl It is R 3 and R 11 They are connected, and optionally, halogen, C 1-6 Alkyl, Or C 3-6 Forms a heteroalkyl ring substituted with a cycloalkyl group, Each R 12 These independently consist of hydroxyl, halogen, cyano, and -N(R) 14)(R 15 ), C 1-6 Alkyl, C 1-6 Alkoxy, C 1-6 Haloalkyl, C 1-6 Haloalcochry C 3-6 Cycloalkyl, C 3-6 Cycloalkoxy, C 3-6 Halocycloalkyl , C 3-6 Halocycloalkoxy, C 1-6 Alkylhydroxyl, heterocycloalkyl Ru, aryl, heteroaryl, S(O) n (R 16 ), or selected from SF5, Or R 3 and one R 12 They are connected, and optionally, halogen, C 1-6 Alkyl, also or C 3-6 A cycloalkyl or heteroalkyl ring substituted with a cycloalkyl group accomplish, or R 10 and one R 12 They are connected, and optionally, halogen, C 1-6 Al Kill, or C 3-6 Cycloalkyl or heteroalkyl substituted Forms a ring, or R 11 and one R 12 They are connected, and optionally, halogen, C1 -6 Alkyl, or C 3-6 Forms a heteroalkyl ring substituted with a cycloalkyl group. , R 13 However, hydrogen, C 1-6 Alkyl, C 1-6 Haloalkyl, C 3-6 Cycloalkyl , C 3-6 Halocycloalkyl, heterocycloalkyl, aryl, or heteroaryl It is R14 and R 15 Hydrogen, C 1-6 Alkyl, C 1-6 Haloalkyl, C 3-6 Cycloalkyl, C 3-6 Halocycloalkyl, heterocycloalkyl, aryl , or selected from heteroaryls, or R 14 and R 15 They are linked together, arbitrarily , halogen, C 1-6 Alkyl, or C 3-6 Heterocyclic substituted Forms a chloroalkyl ring, R 16 However, C 1-6 Alkyl, C 1-6 Haloalkyl, C 3-6 Cycloalkyl, C3 -6 Halocycloalkyl, heterocycloalkyl, aryl, or heteroaryl the law of nature, m is 0 or 1, n is 0, 1, or 2, The compound according to Embodiment P1, or its pharmaceutically acceptable form, wherein o is 0, 1, 2, or 3. A salt or solvate that is acceptable. Embodiment P3. Having the structure of formula (III), [ka] During the ceremony, X is bonded, -C(R 9 )(R 10 )-,-N(R 11 )-, -O-, -S(O) n - -CH2N(R 11 )-, or -CH2O-, R 1 but, [ka] In the formula, ring A is either a 5-membered or 6-membered heteroaryl ring, or optionally, Rogen, Cyano, -N(R) 14 )(R 15 ), C 1-6 Alkyl, C 1-6 Alkoxy, C 1-6 Haloalkyl, C 1-6 Haloalkoxy, C 3-6 Cycloalkyl, C 3-6 C Chloalkoxy, C 3-6 Halocycloalkyl, C 3-6 Halocycloalkoxy, hetero Cycloalkyl, aryl, heteroaryl, S(O) n (R 16 ), or -SF5 A 5-membered or 6-membered heterocycloalkyl ring substituted with a heteroaryl or hete The rocycloalkyl ring consists of 1, 2, or 3 elements selected from the group consisting of O, N, or S. It contains heteroatoms, R 2 However, hydrogen, deuterium, halogen, hydroxyl, C 1-6 Alkyl, C 1-6 Arco Kishi, C 1-6 Haloalkyl, C 1-6 Haloalkoxy, C 3-6 Cycloalkyl, C3 -6 Cycloalkoxy, C 3-6 Halocycloalkyl, C 3-6 Halocycloalkoxy, C 1-6 Alkylhydroxyl, heterocycloalkyl, aryl, or heteroaryl It is R 3 However, halogen, C 1-6 Alkyl, C 1-6 Alkoxy, C 1-6 Haloalkyl, C 1-6 Haloalkoxy, C 3-6 Cycloalkyl, C 3-6Cycloalkoxy, C 3- 6-halocycloalkyl, C 3-6 Halocycloalkoxy, C 1-6 Alkylhydroxyl , heterocycloalkyl, aryl, or heteroaryl, or R 2 and R 3 They are connected, and optionally, halogen, C 1-6 Alkyl, or C 3-6 Cycloalkyl Forms a cycloalkyl or heterocycloalkyl ring substituted with , R 8 but, [ka] And, R 9 and R 10 These independently produce hydrogen, deuterium, halogens, and C 1-6 Alkyl, C 1-6 Alkoxy, C 1-6 Haloalkyl, C 1-6 Haloalkoxy, C 3-6 Cycloalkyl , C 3-6 Cycloalkoxy, C 3-6 Halocycloalkyl, C 3-6 Halocycloalco Selected from xy, heterocycloalkyl, aryl, or heteroaryl, is R 3 and R 10 They are connected, and optionally, halogen, C 1-6 Alkyl, or C 3- Forming a cycloalkyl or heterocycloalkyl ring substituted with a 6-cycloalkyl group, Or R 9 and R 10 They are connected, and optionally, halogen, C 1-6 Alkyl, or C 3-6Form a cycloalkyl or heterocycloalkyl ring substituted with cycloalkyl and R 11 is hydrogen, C 1-6 alkyl, C 1-6 haloalkyl, C 3-6 cycloalkyl or C 3-6 halocycloalkyl, heterocycloalkylaryl, or heteroaryl or R 3 and R 11 are linked to optionally form a heteroalkyl ring substituted with halogen, C 1-6 alkyl, or C 3-6 cycloalkyl to form a heteroalkyl ring substituted with cycloalkyl, each R 12 is independently hydroxyl, halogen, cyano, -N(R 14 )(R 15 ), C 1-6 alkyl, C 1-6 alkoxy, C 1-6 haloalkyl, C 1-6 haloalkoxy , C 3-6 cycloalkyl, C 3-6 cycloalkoxy, C 3-6 halocycloalkyl or C 3-6 halocycloalkoxy, C 1-6 alkylhydroxyl, heterocycloalkyl aryl, heteroaryl, S(O) n (R 16 ), or SF5, and alternatively, R 3 and one R​​​​​​​​​​​​​​​​ Kill, or C 3-6 Cycloalkyl or heteroalkyl substituted Forms a ring, or R 11 and one R 12 They are connected, and optionally, halogen, C1 -6 Alkyl, or C 3-6 Forms a heteroalkyl ring substituted with a cycloalkyl group. , R 13 However, hydrogen, C 1-6 Alkyl, C 1-6 Haloalkyl, C 3-6 Cycloalkyl , C 3-6 Halocycloalkyl, heterocycloalkyl, aryl, or heteroaryl It is R 14 and R 15 Hydrogen, C 1-6 Alkyl, C 1-6 Haloalkyl, C 3-6 Cycloalkyl, C 3-6 Halocycloalkyl, heterocycloalkyl, aryl , or selected from heteroaryls, or R 14 and R 15 They are linked together, arbitrarily , halogen, C 1-6 Alkyl, or C 3-6 Heterocyclic substituted Forms a chloroalkyl ring, R 16 However, C 1-6 Alkyl, C 1-6 Haloalkyl, C 3-6 Cycloalkyl, C3 -6 Halocycloalkyl, heterocycloalkyl, aryl, or heteroaryl the law of nature, m is 0 or 1, n is 0, 1, or 2, The compound according to Embodiment P1, or its pharmaceutically acceptable form, wherein o is 0, 1, 2, or 3. A salt or solvate that is acceptable. Embodiment P4.X is a compound according to any one of Embodiments P1 to P3, wherein Embodiment P4.X is a bond. or a pharmaceutically acceptable salt or solvate thereof. Embodiment P5.X is -C(R 9 )(R 10 )- any of embodiments P1 to P3 The compound described in one of the above, or a pharmaceutically acceptable salt or solvate thereof. Embodiment P6.X is -N(R 11 )- which is one of the embodiments P1 to P3 The compound described, or a pharmaceutically acceptable salt or solvate thereof. Embodiment P7.X is -O-, the compound according to any one of Embodiments P1 to P3 A substance, or a pharmaceutically acceptable salt or solvate thereof. Embodiment P8.X is -S-, the compound according to any one of Embodiments P1 to P3 A substance, or a pharmaceutically acceptable salt or solvate thereof. Embodiment P9.X is described in any one of Embodiments P1 to P3, where -S(O)- A compound thereof, or a pharmaceutically acceptable salt or solvate thereof. Embodiment P10.X is -S(O)2- in any one of Embodiments P1 to P3 The compound described, or a pharmaceutically acceptable salt or solvate thereof. Embodiment P11.R 1 but, [ka] The compound described in any one of embodiments P1 to P10, or its pharmaceutically acceptable A salt or solvate that is produced. Embodiment P12.R 2 However, hydrogen, -F, -CH3, -CH2CH3, -CF2H, -C F3, -CH2OH, -C(CH3)2OH, phenyl, or cyclopropyl A compound described in any one of embodiments P1 to P11, or a pharmaceutically acceptable salt thereof. Or a solvate. Embodiment P13.R 3 However, -F, -CH3, -CH2CH3, -CF2H, -CF3, -CH2OH, -C(CH3)2OH, phenyl, or cyclopropyl, in action form A compound described in any one of P1 to P12, or a pharmaceutically acceptable salt thereof It is a solvate. Embodiment P14.R 2 and R 3 These are linked together to form cyclopropyl, cyclobutyl, or A compound according to any one of embodiments P1 to P11 that forms a cyclopentyl ring, or its pharmaceutically acceptable salt or solvate. Embodiment P15.R 2 and R 3 These are linked together, forming oxetanil or tetrahydrofuran. A compound according to any one of embodiments P1 to P11 that forms a ring, or its pharmaceutically acceptable properties A salt or solvate that is acceptable. Embodiment P16.m is 0, the compound according to any one of Embodiments P1 to P15 A substance, or a pharmaceutically acceptable salt or solvate thereof. Embodiment P17.m is 1, the compound according to any one of Embodiments P1 to P15 A substance, or a pharmaceutically acceptable salt or solvate thereof. Embodiment P18.o is 0, the compound according to any one of Embodiments P1 to P17 A substance, or a pharmaceutically acceptable salt or solvate thereof. Embodiment P19.o is 1, the compound according to any one of Embodiments P1 to P17 A substance, or a pharmaceutically acceptable salt or solvate thereof. Embodiment P20.o is 2, according to any one of Embodiments P1 to P17 A substance, or a pharmaceutically acceptable salt or solvate thereof. Embodiment P21.o is 3, according to any one of Embodiments P1 to P17 A substance, or a pharmaceutically acceptable salt or solvate thereof. Embodiment P22.R 8 but, [ka] The compound described in any one of embodiments P1 to P21, or the pharmaceutically acceptable compound thereof. A salt or solvate that is produced. Embodiment P23. A compound selected from compound list 1, or a pharmaceutically acceptable compound thereof. Salt. Embodiment P24. The compound or drug according to any one of Embodiments P1 to P23. A pharmaceutically acceptable salt or solvate and at least one pharmaceutically acceptable excipient A pharmaceutical composition containing , Embodiment P25. A person who performs treatment for neurodegenerative disorders in a person who needs to be treated. A law relating to a compound described in any one of the embodiments P1 to P23 of the therapeutically effective amount, or A method comprising administering the pharmaceutically acceptable salt or solvate thereof to a subject. Embodiment P26. A method for treating a demyelinating disease in a subject that requires treatment. and the compound described in any one of the embodiments P1 to P23 of the therapeutically effective amount, or A method comprising administering a pharmaceutically acceptable salt or solvate of to a subject. Embodiment P27. The demyelinating disease is a demyelinating disease of the central nervous system, as described in Embodiment P26. Method of loading. Embodiment P28. The method according to Embodiment P27, wherein the disease is multiple sclerosis. Embodiment P29. The demyelinating disease is a demyelinating disease of the peripheral nervous system, as described in Embodiment P26. Method of loading. Embodiment P30. A method for treating neuropathic diseases, optionally peripheral neuropathy, and For subjects requiring this, it is described in any one of the embodiments P1 to P23 of the therapeutically effective dose. This includes administering the compound, or a pharmaceutically acceptable salt or solvate thereof, to the target. Hmm, a method. Embodiment P31. The neuropathic disease is diabetic neuropathy, as described in Embodiment P30. The method. Embodiment P32. Embodiments P25-P31 further comprising the administration of one or more immunomodulators. The method described in any one of the following ways. Embodiment P33. One or more immunomodulators include IFN-β1 molecules; corticosteroids; Polymers or glutillamers of glutamic acid, lysine, alanine, and tyrosine; alpha- Antibodies or fragments thereof against 4-integrin or natalizumab; anthracendion Molecules or mitoxantrone; fingolimod or FTY720 or other S1P1 devices Potential modifiers; dimethyl fumarate or other NRF2 functional modifiers; IL- T cells Antibodies or daclizumab against the alpha subunit of the CD25 receptor; CD5 Antibodies against 2 or alemtuzumab; antibodies against CD20 or ocrelizumab; Selected from dihydroorotate dehydrogenase inhibitors or teriflunomide. The method described in embodiment P32. Embodiment P34. Modulation of muscarinic acetylcholine receptor M1 activity in the subject. A method relating to the compound described in any one of embodiments P1 to P23, or its pharmaceutically acceptable properties. A method comprising administering an acceptable salt or solvate to a target. Embodiment P35. Embodiment P3, in which the compound acts as a selective M1 antagonist. The method described in 4.

[0220] IX. Additional Embodiments Embodiment PP1. A compound, or a pharmaceutically acceptable salt or solvate thereof , having the structure of formula (IA-1) or (IB-1), [ka] During the ceremony, X is bonded, -C(R 9 )(R 10 )-,-N(R 11 )-, -O-, -S(O) n - -CH2N(R 11 )-, substituted or unsubstituted alkylene, substituted or unsubstituted alke Nylene, substituted or unsubstituted alkylylene, substituted or unsubstituted heteroalkylene, substituted Alternatively, an unsubstituted heteroalkynylene, or a substituted or unsubstituted heteroalkynylene. the law of nature, Y is a substituted or unsubstituted alkylene, a substituted or unsubstituted alkenylene, or a substituted alkenylene. Alternatively, it is an unsubstituted heteroalkylene. R 1 but, [ka] In the formula, ring A can optionally be hydroxyl, halogen, cyano, or -N(R 14 )(R 1 5 ), substituted or unsubstituted alkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted alkoxy, substituted or unsubstituted Substituting haloalkyls, substituted or unsubstituted haloalkoxys, substituted or unsubstituted cycloalkyls , substituted or unsubstituted cycloalkoxy, substituted or unsubstituted halocycloalkyl, Substituted or unsubstituted halocycloalkoxy, substituted or unsubstituted heterocycloalkyl, Substitutable or unsubstituted aryl, substituted or unsubstituted heteroaryl, -S(O) n (R 16 ), or a heteroaryl ring or heterocycloalkyl ring substituted with -SF5 Furthermore, the heteroaryl or heterocycloalkyl ring is selected from the group consisting of O, N, or S. It contains one, two, or three selected heteroatoms, R 2 However, hydrogen, deuterium, halogen, hydroxyl, substituted or unsubstituted alkyl, substituted Or unsubstituted alkoxy, substituted or unsubstituted haloalkyl, substituted or unsubstituted halo Alkoxy, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkoxy , substituted or unsubstituted halocycloalkyl, substituted or unsubstituted halocycloalkoxy, Substituted or unsubstituted alkylhydroxyl, substituted or unsubstituted heterocycloalkyl, A substituted or unsubstituted aryl, or a substituted or unsubstituted heteroaryl, R 3 However, halogens, substituted or unsubstituted alkyls, substituted or unsubstituted alkoxides, Substituted or unsubstituted haloalkyl, substituted or unsubstituted haloalkoxy, substituted or unsubstituted Substituting cycloalkyl, substituted or unsubstituted cycloalkoxy, substituted or unsubstituted haloalkyl Haloalkyl, substituted or unsubstituted halocycloalkoxy, substituted or unsubstituted alkylhybrid Droxyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or it is a substituted or unsubstituted heteroaryl, or R 2 and R 3 They are connected, Optionally, halogens, substituted or unsubstituted alkyls, or substituted or unsubstituted cycloal groups. The cycloalkyl or heterocycloalkyl ring is substituted by Kill, R 4 and R 5 These independently consist of hydrogen, deuterium, halogens, and substituted or unsubstituted alkyl groups. Selected from R 3 and R 4 These are linked together, and optionally, halogen, substituted or unsubstituted A cycloalkyl, or cycloalkyl or cycloalkyl substituted with substituted or unsubstituted cycloalkyl Forms a heterocycloalkyl ring, or R 4 and R 5 They are connected, and arbitrarily, Haroge Substituted with substituted or unsubstituted alkyl, or substituted or unsubstituted cycloalkyl Forms a cycloalkyl or heterocycloalkyl ring, R 6 and R 7 These independently consist of hydrogen, deuterium, halogens, and substituted or unsubstituted alkyl groups. Selected from R 3 and R 7 These are linked together, and optionally, halogen, substituted or unsubstituted A cycloalkyl, or cycloalkyl or cycloalkyl substituted with substituted or unsubstituted cycloalkyl Forming a heterocycloalkyl ring, R 4 and R 6 These are linked together, and optionally, halogen, substitute Alternatively, cycloalkyls substituted with unsubstituted alkyl groups, or substituted or unsubstituted cycloalkyl groups. Forms an alkyl or heterocycloalkyl ring, or R 5 and R 7 They are connected , forming a bond, R 8 but, [ka] And, R 9 and R 10 These independently consist of hydrogen, deuterium, halogen, substituted or unsubstituted alkyl groups. substituted or unsubstituted alkoxy, substituted or unsubstituted haloalkyl, substituted or unsubstituted Converted haloalkoxy, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkyl Coxy, substituted or unsubstituted halocycloalkyl, substituted or unsubstituted halocycloalco xy, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or Selected from substituted or unsubstituted heteroaryls, or R 3 and R 10 They are connected , optionally halogens, substituted or unsubstituted alkyls, or substituted or unsubstituted cycloal groups. Kill forms a cycloalkyl or heterocycloalkyl ring, or R 4 and R 10 These are linked together, and optionally a halogen, substituted or unsubstituted alkyl, or substituted Alternatively, cycloalkyl or heterocycloalkyl that is substituted with an unsubstituted cycloalkyl. Forms a ring, or R 6 and R 10 These are linked together, and optionally halogen, substituted, or non Cycloalkyls substituted with substituted or unsubstituted cycloalkyls Alternatively, it forms a heterocycloalkyl ring, or R 9 and R 10 They are connected, and arbitrarily Substituted with rogens, substituted or unsubstituted alkyl groups, or substituted or unsubstituted cycloalkyl groups. Forms a cycloalkyl or heterocycloalkyl ring, R 11 However, hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted haloalkyl, Substituted or unsubstituted cycloalkyl, substituted or unsubstituted halocycloalkyl, substituted or is an unsubstituted heterocycloalkyl, a substituted or unsubstituted aryl, or a substituted or unsubstituted aryl. Conversion heteroaryl, or R 3 and R 11 They are linked together, and optionally, halogens can be substituted. or an unsubstituted alkyl, or a heteroalkyl substituted with a substituted or unsubstituted cycloalkyl It forms a kill ring, or R 4 and R 11 They are linked together, and optionally, halogen, substitution or is an unsubstituted alkyl, or a heterocycloalkyl that is substituted with a substituted or unsubstituted cycloalkyl. Forms an alkyl ring, or R 6 and R 11 They are linked together, and optionally, halogens and substitutions are also possible. Alternatively, heterosymmetric alkyl groups substituted with substituted or unsubstituted cycloalkyl groups. Forms a chloroalkyl ring, Each R 12 These independently consist of hydroxyl, halogen, cyano, and -N(R) 14 )(R 15 ), Substituted or unsubstituted alkyl groups, substituted or unsubstituted alkoxy groups, substituted or unsubstituted halos Alkyl, substituted or unsubstituted haloalkoxy, substituted or unsubstituted cycloalkyl, Substituted or unsubstituted cycloalkoxy, substituted or unsubstituted halocycloalkyl, substituted or unsubstituted halocycloalkyl, substituted or unsubstituted halocycloalkoxy, substituted or unsubstituted alkylhydroxyl, substituted or k is an unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted he Terroraryl, -S(O) n (R 16 ), or selected from -SF5, or R 3 oh One R 12These are linked together, optionally with halogens, substituted or unsubstituted alkyl groups, or Cycloalkyl or heterocycloalkyl that is substituted or unsubstituted with substituted or unsubstituted cycloalkyls Forms a lukyl ring, or R 10 and one R 12 They are connected, and optionally, halogen, Substituted or unsubstituted alkyl, or substituted or unsubstituted cycloalkyl Forms a chloroalkyl or heterocycloalkyl ring, or R 11 and one R 12 These are linked together, optionally with halogens, substituted or unsubstituted alkyls, or substituted or A heterocycloalkyl ring is formed by substituted unsubstituted cycloalkyl groups. R 13 However, hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted haloalkyl, Substituted or unsubstituted cycloalkyl, substituted or unsubstituted halocycloalkyl, substituted or is an unsubstituted heterocycloalkyl, a substituted or unsubstituted aryl, or a substituted or unsubstituted aryl. It is a heteroaryl compound, R 14 and R 15 These independently consist of hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkyl. Substituted haloalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted halocyclo Alkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or selected from substituted or unsubstituted heteroaryls, or R 14 and R 15 ga In addition, optionally, halogens, substituted or unsubstituted alkyls, or substituted or unsubstituted alkyls Forms a heterocycloalkyl ring substituted with a chloroalkyl group, R 16 However, substituted or unsubstituted alkyl, substituted or unsubstituted haloalkyl, substituted k is an unsubstituted cycloalkyl, halocycloalkyl, substituted or unsubstituted heterocycloalkyl Kill, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl, m is 0 or 1, n is 0, 1, or 2, o is 0, 1, 2, or 3, A compound, or a pharmaceutically acceptable salt or solvate thereof, in which p is 0 or 1. . Embodiment PP2. Having the structure of formula (IA) or (IB), [ka] During the ceremony, X is bonded, -C(R 9 )(R 10 )-,-N(R 11 )-, -O-, -S(O) n - -CH2N(R 11 )-, or -CH2O-, Y is -CH2-, -CH2CH2-, -CH=CH-, or -CH2OCH2- can be, R 1 but, [ka] In the formula, ring A is either a 5-membered or 6-membered heteroaryl ring, or optionally, Rogen, Cyano, -N(R) 14 )(R 15 ), C 1-6 Alkyl, C 1-6 Alkoxy, C 1-6 Haloalkyl, C 1-6 Haloalkoxy, C 3-6 Cycloalkyl, C 3-6 C Chloalkoxy, C 3-6 Halocycloalkyl, C 3-6 Halocycloalkoxy, hetero Cycloalkyl, aryl, heteroaryl, S(O) n (R 16 ), or -SF5 A 5-membered or 6-membered heterocycloalkyl ring substituted with a heteroaryl or hete The rocycloalkyl ring consists of 1, 2, or 3 elements selected from the group consisting of O, N, or S. It contains heteroatoms, R 2 However, hydrogen, deuterium, halogen, hydroxyl, C 1-6 Alkyl, C 1-6 Arco Kishi, C 1-6 Haloalkyl, C 1-6 Haloalkoxy, C 3-6 Cycloalkyl, C3 -6 Cycloalkoxy, C 3-6 Halocycloalkyl, C 3-6 Halocycloalkoxy, C 1-6 Alkylhydroxyl, heterocycloalkyl, aryl, or heteroaryl It is R 3 However, halogen, C 1-6 Alkyl, C 1-6 Alkoxy, C 1-6 Haloalkyl, C 1-6 Haloalkoxy, C 3-6 Cycloalkyl, C 3-6 Cycloalkoxy, C 3- 6-halocycloalkyl, C 3-6 Halocycloalkoxy, C 1-6 Alkylhydroxyl , heterocycloalkyl, aryl, or heteroaryl, or R 2 and R 3 They are connected, and optionally, halogen, C 1-6 Alkyl, or C 3-6 Cycloalkyl Forms a cycloalkyl or heterocycloalkyl ring substituted with , R4 and R 5 These independently produce hydrogen, deuterium, halogens, and C 1-3 Selected from alkyl groups Selected, or R 3 and R 4 They are connected, and optionally, halogen, C 1-6 Alkyl, also or C 3-6 Cycloalkyl or heterocycloalkyl Forming a ring, or R 4 and R 5 They are connected, and optionally, halogen, C 1-6 Alkyl , or C 3-6 Cycloalkyl or heterocycloalkyl substituted Forms a Kill ring, R 6 and R 7 These independently produce hydrogen, deuterium, halogens, and C 1-3 Selected from alkyl groups Selected, or R 3 and R 7 They are connected, and optionally, halogen, C 1-6 Alkyl, also or C 3-6 Cycloalkyl or heterocycloalkyl Forming a ring, or R 4 and R 6 They are connected, and optionally, halogen, C 1-6 Alkyl , or C 3-6 Cycloalkyl or heterocycloalkyl substituted It forms a kill ring, or R 5 and R 7 They connect to form a bond, R 8 but, [ka] And, R 9 and R 10These independently produce hydrogen, deuterium, halogens, and C 1-6 Alkyl, C 1-6 Alkoxy, C 1-6 Haloalkyl, C 1-6 Haloalkoxy, C 3-6 Cycloalkyl , C 3-6 Cycloalkoxy, C 3-6 Halocycloalkyl, C 3-6 Halocycloalco Selected from xy, heterocycloalkyl, aryl, or heteroaryl, is R 3 and R 10 They are connected, and optionally, halogen, C 1-6 Alkyl, or C 3- Forming a cycloalkyl or heterocycloalkyl ring substituted with a 6-cycloalkyl group, Or R 4 and R 10 They are connected, and optionally, halogen, C 1-6 Alkyl, or C 3-6 A cycloalkyl or heterocycloalkyl ring substituted with a cycloalkyl group accomplish, or R 6 and R 10 They are connected, and optionally, halogen, C 1-6 Alkyl, also or C 3-6 Cycloalkyl or heterocycloalkyl Forming a ring, or R 9 and R 10 They are connected, and optionally, halogen, C 1-6 Alki Ru, or C 3-6 Cycloalkyl or heterocycloalkyl substituted Forms a lucyl ring, R 11 However, hydrogen, C 1-6 Alkyl, C 1-6 Haloalkyl, C 3-6 Cycloalkyl , C3-6 Halocycloalkyl, heterocycloalkylaryl, or heteroaryl It is R 3 and R 11 They are connected, and optionally, halogen, C 1-6 Alkyl, Or C 3-6 Forms a heteroalkyl ring substituted with a cycloalkyl group, or R 4 oh Call R 11 They are connected, and optionally, halogen, C 1-6 Alkyl, or C 3-6 Cyclo Forms a heterocycloalkyl ring substituted with alkyl, or R 6 and R 11 is connected Then, optionally, halogen, C 1-6 Alkyl, or C 3-6 Substituted with cycloalkyl Forms a heterocycloalkyl ring, Each R 12 These independently consist of hydroxyl, halogen, cyano, and -N(R) 14 )(R 15 ), C 1-6 Alkyl, C 1-6 Alkoxy, C 1-6 Haloalkyl, C 1-6 Haloalcochry C 3-6 Cycloalkyl, C 3-6 Cycloalkoxy, C 3-6 Halocycloalkyl , C 3-6 Halocycloalkoxy, C 1-6 Alkylhydroxyl, heterocycloalkyl Ru, aryl, heteroaryl, S(O) n (R 16 ), or selected from SF5, Or R 3 and one R 12 They are connected, and optionally, halogen, C 1-6 Alkyl, also or C 3-6Cycloalkyl or heterocycloalkyl Forming a ring, or R 10 and one R 12 They are connected, and optionally, halogen, C 1- 6 alkyl, or C 3-6 Cycloalkyl or hetero Forms a cycloalkyl ring, or R 11 and one R 12 They are connected, and arbitrarily, Rogen, C 1-6 Alkyl, or C 3-6 Heterocyclo substituted with cycloalkyl Forming an alkyl ring, R 13 However, hydrogen, C 1-6 Alkyl, C 1-6 Haloalkyl, C 3-6 Cycloalkyl , C 3-6 Halocycloalkyl, heterocycloalkyl, aryl, or heteroaryl It is R 14 and R 15 Hydrogen, C 1-6 Alkyl, C 1-6 Haloalkyl, C 3-6 Cycloalkyl, C 3-6 Halocycloalkyl, heterocycloalkyl, aryl , or selected from heteroaryls, or R 14 and R 15 They are linked together, arbitrarily , halogen, C 1-6 Alkyl, or C 3-6 Heterocyclic substituted Forms a chloroalkyl ring, R 16 However, C 1-6 Alkyl, C 1-6 Haloalkyl, C 3-6 Cycloalkyl, C3 -6Halocycloalkyl, heterocycloalkyl, aryl, or heteroaryl the law of nature, m is 0 or 1, n is 0, 1, or 2, The compound according to Embodiment PP1, or its pharmaceutically acceptable form, wherein o is 0, 1, 2, or 3. A generally acceptable salt or solvate. Embodiment PP3. Having the structure of formula (IIA) or (IIB), [ka] During the ceremony, X is bonded, -C(R 9 )(R 10 )-,-N(R 11 )-, -O-, -S(O) n - -CH2N(R 11 )-, or -CH2O-, Y is -CH2-, -CH2CH2-, -CH=CH-, or -CH2OCH2- can be, R 1 but, [ka] In the formula, ring A is either a 5-membered or 6-membered heteroaryl ring, or optionally, Rogen, Cyano, -N(R) 14 )(R 15 ), C 1-6 Alkyl, C 1-6 Alkoxy, C 1-6 Haloalkyl, C 1-6 Haloalkoxy, C 3-6 Cycloalkyl, C 3-6 C Chloalkoxy, C 3-6 Halocycloalkyl, C 3-6 Halocycloalkoxy, hetero Cycloalkyl, aryl, heteroaryl, S(O) n (R 16 ), or -SF5 A 5-membered or 6-membered heterocycloalkyl ring substituted with a heteroaryl or hete The rocycloalkyl ring consists of 1, 2, or 3 elements selected from the group consisting of O, N, or S. It contains heteroatoms, R 2 However, hydrogen, deuterium, halogen, hydroxyl, C 1-6 Alkyl, C 1-6 Arco Kishi, C 1-6 Haloalkyl, C 1-6 Haloalkoxy, C 3-6 Cycloalkyl, C3 -6 Cycloalkoxy, C 3-6 Halocycloalkyl, C 3-6 Halocycloalkoxy, C 1-6 Alkylhydroxyl, heterocycloalkyl, aryl, or heteroaryl It is R 3 However, halogen, C 1-6 Alkyl, C 1-6 Alkoxy, C 1-6 Haloalkyl, C 1-6 Haloalkoxy, C 3-6 Cycloalkyl, C 3-6 Cycloalkoxy, C 3- 6-halocycloalkyl, C 3-6 Halocycloalkoxy, C 1-6 Alkylhydroxyl , heterocycloalkyl, aryl, or heteroaryl, or R 2 and R 3 They are connected, and optionally, halogen, C 1-6 Alkyl, or C 3-6 Cycloalkyl Forms a cycloalkyl or heterocycloalkyl ring substituted with , R 8 but, [ka] And, R 9 and R 10 These independently produce hydrogen, deuterium, halogens, and C 1-6 Alkyl, C 1-6 Alkoxy, C 1-6 Haloalkyl, C 1-6 Haloalkoxy, C 3-6 Cycloalkyl , C 3-6 Cycloalkoxy, C 3-6 Halocycloalkyl, C 3-6 Halocycloalco Selected from xy, heterocycloalkyl, aryl, or heteroaryl, is R 3 and R 10 They are connected, and optionally, halogen, C 1-6 Alkyl, or C 3- Forming a cycloalkyl or heterocycloalkyl ring substituted with a 6-cycloalkyl group, Or R 9 and R 10 They are connected, and optionally, halogen, C 1-6 Alkyl, or C 3-6 A cycloalkyl or heterocycloalkyl ring substituted with a cycloalkyl group accomplish, R 11 However, hydrogen, C 1-6 Alkyl, C 1-6 Haloalkyl, C 3-6 Cycloalkyl , C 3-6 Halocycloalkyl, heterocycloalkylaryl, or heteroaryl It is R 3 and R 11 They are connected, and optionally, halogen, C 1-6 Alkyl, Or C 3-6 Forming a heterocycloalkyl ring substituted with a cycloalkyl group, Each R 12 These independently consist of hydroxyl, halogen, cyano, and -N(R)14 )(R 15 ), C 1-6 Alkyl, C 1-6 Alkoxy, C 1-6 Haloalkyl, C 1-6 Haloalcochry C 3-6 Cycloalkyl, C 3-6 Cycloalkoxy, C 3-6 Halocycloalkyl , C 3-6 Halocycloalkoxy, C 1-6 Alkylhydroxyl, heterocycloalkyl Ru, aryl, heteroaryl, S(O) n (R 16 ), or selected from SF5, Or R 3 and one R 12 They are connected, and optionally, halogen, C 1-6 Alkyl, also or C 3-6 Cycloalkyl or heterocycloalkyl Forming a ring, or R 10 and one R 12 They are connected, and optionally, halogen, C 1- 6 alkyl, or C 3-6 Cycloalkyl or hetero Forms a cycloalkyl ring, or R 11 and one R 12 They are connected, and arbitrarily, Rogen, C 1-6 Alkyl, or C 3-6 Heterocyclo substituted with cycloalkyl Forming an alkyl ring, R 13 However, hydrogen, C 1-6 Alkyl, C 1-6 Haloalkyl, C 3-6 Cycloalkyl , C 3-6 Halocycloalkyl, heterocycloalkyl, aryl, or heteroaryl It is R 14 and R 15 Hydrogen, C 1-6 Alkyl, C 1-6 Haloalkyl, C 3-6 Cycloalkyl, C 3-6 Halocycloalkyl, heterocycloalkyl, aryl , or selected from heteroaryls, or R 14 and R 15 They are linked together, arbitrarily , halogen, C 1-6 Alkyl, or C 3-6 Heterocyclic substituted Forms a chloroalkyl ring, R 16 However, C 1-6 Alkyl, C 1-6 Haloalkyl, C 3-6 Cycloalkyl, C3 -6 Halocycloalkyl, heterocycloalkyl, aryl, or heteroaryl the law of nature, m is 0 or 1, n is 0, 1, or 2, The embodiment described in any one of Embodiments PP1 to PP2, wherein o is 0, 1, 2, or 3. A compound, or a pharmaceutically acceptable salt or solvate thereof. Embodiment PP4. Having the structure of formula (III), [ka] During the ceremony, X is bonded, -C(R 9 )(R 10 )-,-N(R 11 )-, -O-, -S(O) n - -CH2N(R 11 )-, or -CH2O-, R 1 but, [ka] In the formula, ring A is either a 5-membered or 6-membered heteroaryl ring, or optionally, Rogen, Cyano, -N(R) 14 )(R 15 ), C 1-6 Alkyl, C 1-6 Alkoxy, C 1-6 Haloalkyl, C 1-6 Haloalkoxy, C 3-6 Cycloalkyl, C 3-6 C Chloalkoxy, C 3-6 Halocycloalkyl, C 3-6 Halocycloalkoxy, hetero Cycloalkyl, aryl, heteroaryl, S(O) n (R 16 ), or -SF5 A 5-membered or 6-membered heterocycloalkyl ring substituted with a heteroaryl or hete The rocycloalkyl ring consists of 1, 2, or 3 elements selected from the group consisting of O, N, or S. It contains heteroatoms, R 2 However, hydrogen, deuterium, halogen, hydroxyl, C 1-6 Alkyl, C 1-6 Arco Kishi, C 1-6 Haloalkyl, C 1-6 Haloalkoxy, C 3-6 Cycloalkyl, C3 -6 Cycloalkoxy, C 3-6 Halocycloalkyl, C 3-6 Halocycloalkoxy, C 1-6 Alkylhydroxyl, heterocycloalkyl, aryl, or heteroaryl It is R 3 However, halogen, C 1-6 Alkyl, C 1-6 Alkoxy, C 1-6 Haloalkyl, C 1-6 Haloalkoxy, C 3-6 Cycloalkyl, C3-6 Cycloalkoxy, C 3- 6-halocycloalkyl, C 3-6 Halocycloalkoxy, C 1-6 Alkylhydroxyl , heterocycloalkyl, aryl, or heteroaryl, or R 2 and R 3 They are connected, and optionally, halogen, C 1-6 Alkyl, or C 3-6 Cycloalkyl Forms a cycloalkyl or heterocycloalkyl ring substituted with , R 8 but, [ka] And, R 9 and R 10 These independently produce hydrogen, deuterium, halogens, and C 1-6 Alkyl, C 1-6 Alkoxy, C 1-6 Haloalkyl, C 1-6 Haloalkoxy, C 3-6 Cycloalkyl , C 3-6 Cycloalkoxy, C 3-6 Halocycloalkyl, C 3-6 Halocycloalco Selected from xy, heterocycloalkyl, aryl, or heteroaryl, is R 3 and R 10 They are connected, and optionally, halogen, C 1-6 Alkyl, or C 3- Forming a cycloalkyl or heterocycloalkyl ring substituted with a 6-cycloalkyl group, Or R 9 and R 10 They are connected, and optionally, halogen, C 1-6 Alkyl, or C 3-6A cycloalkyl or heterocycloalkyl ring substituted with a cycloalkyl group accomplish, R 11 However, hydrogen, C 1-6 Alkyl, C 1-6 Haloalkyl, C 3-6 Cycloalkyl , C 3-6 Halocycloalkyl, heterocycloalkylaryl, or heteroaryl It is R 3 and R 11 They are connected, and optionally, halogen, C 1-6 Alkyl, Or C 3-6 Forming a heterocycloalkyl ring substituted with a cycloalkyl group, Each R 12 These independently consist of hydroxyl, halogen, cyano, and -N(R) 14 )(R 15 ), C 1-6 Alkyl, C 1-6 Alkoxy, C 1-6 Haloalkyl, C 1-6 Haloalcochry C 3-6 Cycloalkyl, C 3-6 Cycloalkoxy, C 3-6 Halocycloalkyl , C 3-6 Halocycloalkoxy, C 1-6 Alkylhydroxyl, heterocycloalkyl Ru, aryl, heteroaryl, S(O) n (R 16 ), or selected from SF5, Or R 3 and one R 12 They are connected, and optionally, halogen, C 1-6 Alkyl, also or C 3-6 Cycloalkyl or heterocycloalkyl Forming a ring, or R 10 and one R 12 They are connected, and optionally, halogen, C 1- 6 alkyl, or C 3-6 Cycloalkyl or hetero Forms a cycloalkyl ring, or R 11 and one R 12 They are connected, and arbitrarily, Rogen, C 1-6 Alkyl, or C 3-6 Heterocyclo substituted with cycloalkyl Forming an alkyl ring, R 13 However, hydrogen, C 1-6 Alkyl, C 1-6 Haloalkyl, C 3-6 Cycloalkyl , C 3-6 Halocycloalkyl, heterocycloalkyl, aryl, or heteroaryl It is R 14 and R 15 Hydrogen, C 1-6 Alkyl, C 1-6 Haloalkyl, C 3-6 Cycloalkyl, C 3-6 Halocycloalkyl, heterocycloalkyl, aryl , or selected from heteroaryls, or R 14 and R 15 They are linked together, arbitrarily , halogen, C 1-6 Alkyl, or C 3-6 Heterocyclic substituted Forms a chloroalkyl ring, R 16 However, C 1-6 Alkyl, C 1-6 Haloalkyl, C 3-6 Cycloalkyl, C3 -6 Halocycloalkyl, heterocycloalkyl, aryl, or heteroaryl the law of nature, m is 0 or 1, n is 0, 1, or 2, The embodiment described in any one of Embodiments PP1 to PP2, wherein o is 0, 1, 2, or 3. A compound, or a pharmaceutically acceptable salt or solvate thereof. Embodiment PP5.X is a combination of any one of Embodiments PP1 to PP4. A compound, or a pharmaceutically acceptable salt or solvate thereof. Embodiment PP6.X is -C(R 9 )(R 10 )-The embodiments PP1 to PP4 are Any one of the compounds listed, or a pharmaceutically acceptable salt or solvate thereof. Embodiment PP7.X is -N(R 11 )- one of the embodiments PP1 to PP4 One of the compounds described herein, or a pharmaceutically acceptable salt or solvate thereof. Embodiment PP8.X is described in any one of Embodiments PP1 to PP4, where -O- A compound thereof, or a pharmaceutically acceptable salt or solvate thereof. Embodiment PP9.X is described in any one of Embodiments PP1 to PP4, where -S- A compound thereof, or a pharmaceutically acceptable salt or solvate thereof. Embodiment PP10.X is -S(O)-, one of Embodiments PP1 to PP4 The compounds described above, or their pharmaceutically acceptable salts or solvates. Embodiment PP11.X is -S(O)2-, one of Embodiments PP1 to PP4. One of the compounds described herein, or a pharmaceutically acceptable salt or solvate thereof. Embodiment PP12.R 1 but, [ka] The compound described in any one of embodiments PP1 to PP11, or the pharmaceutically effective compound thereof. Acceptable salts or solvates. Embodiment PP13.R2 However, hydrogen, -F, -CH3, -CH2CH3, -CF2H, - It is CF3, -CH2OH, -C(CH3)2OH, phenyl, or cyclopropyl. , the compound described in any one of embodiments PP1 to PP12, or the pharmaceutically acceptable compound thereof A salt or solvate of a compound. Embodiment PP14.R 3 However, -F, -CH3, -CH2CH3, -CF2H, -CF3 The expression is -CH2OH, -C(CH3)2OH, phenyl, or cyclopropyl. A compound described in any one of forms PP1 to PP13, or a pharmaceutically acceptable salt thereof. Or a solvate. Embodiment PP15.R 2 and R 3 These are linked together to form cyclopropyl, cyclobutyl, and The compound described in any one of embodiments PP1 to PP12 forms a cyclopentyl ring. A substance, or a pharmaceutically acceptable salt or solvate thereof. Embodiment PP16.R 2 and R 3 These are linked together, forming oxetanyl or tetrahydrofur. A compound according to any one of embodiments PP1 to PP12 that forms a ring, or A pharmaceutically acceptable salt or solvate. Embodiment PP17.m is described in any one of Embodiments PP1 to PP16, where the value is 0. A compound thereof, or a pharmaceutically acceptable salt or solvate thereof. Embodiment PP18.m is described in any one of Embodiments PP1 to PP16, where PP18.m is 1. A compound thereof, or a pharmaceutically acceptable salt or solvate thereof. Embodiment PP19.o is described in any one of Embodiments PP1 to PP18, where the value is 0. A compound thereof, or a pharmaceutically acceptable salt or solvate thereof. Embodiment PP20.o is described in any one of Embodiments PP1 to PP18, where Embodiment PP20.o is 1. A compound thereof, or a pharmaceutically acceptable salt or solvate thereof. Embodiment PP21.o is described in any one of Embodiments PP1 to PP18, where PP21.o is 2. A compound thereof, or a pharmaceutically acceptable salt or solvate thereof. Embodiment PP22.o is described in any one of Embodiments PP1 to PP18, where 3 is the embodiment. A compound thereof, or a pharmaceutically acceptable salt or solvate thereof. Embodiment PP23.R 8 but, [ka] The compound described in any one of embodiments PP1 to PP22, or the pharmaceutically effective Acceptable salts or solvates. Embodiment PP24. Compounds selected from compound list 1, or their pharmaceutically acceptable Salt. Embodiment PP25. A compound described in any one of Embodiments PP1 to PP24, or The pharmaceutically acceptable salt or solvate and at least one pharmaceutically acceptable excipient A pharmaceutical composition comprising a modifier. Embodiment PP26. Performing the procedure in a subject who requires treatment for neurodegenerative disorders. A method comprising a compound described in any one of the embodiments PP1 to PP24 of the therapeutically effective amount, A method comprising administering to a subject a pharmaceutically acceptable salt or solvate thereof. Embodiment PP27. Persons who perform treatment for demyelinating diseases in subjects who require such treatment. A law relating to a compound described in any one of the embodiments PP1 to PP24 of the therapeutically effective amount, A method comprising administering a pharmaceutically acceptable salt or solvate thereof to a subject. Embodiment PP28. Embodiment PP27, in which the demyelinating disease is a demyelinating disease of the central nervous system. Methods used. Embodiment PP29. The method according to Embodiment PP28, wherein the disease is multiple sclerosis. Embodiment PP30. The demyelinating disease is a demyelinating disease of the peripheral nervous system, Embodiment PP27 Methods used. Embodiment PP31. A method for treating neuropathic diseases, optionally peripheral neuropathy, For subjects requiring it, one of the embodiments PP1 to PP24 of the therapeutically effective dose The compounds described, or their pharmaceutically acceptable salts or solvates, are administered to the target. A method that includes [this]. Embodiment PP32. The neuropathic disease is diabetic neuropathy, as in Embodiment PP31. Method of description. Embodiment PP33. Embodiments PP26-P further comprising the administration of one or more immunomodulators. The method described in any one of the methods on page 32. Embodiment PP34. One or more immunomodulators are IFN-β1 molecules; corticosteroids ; Polymers or glutillamers of glutamic acid, lysine, alanine, and tyrosine; alpha -4 Antibodies or fragments thereof against integrin, or natalizumab; anthracenzio N molecule or mitoxantrone; fingolimod or FTY720 or other S1P1 Functional modifiers; dimethyl fumarate or other NRF2 functional modifiers; IL in T cells Antibodies or daclizumab against the alpha subunit of the CD2 receptor (CD25); CD Antibodies against 52 or alemtuzumab; antibodies against CD20 or ocrelizumab; and selected from dihydroorotate dehydrogenase inhibitors or teriflunomide The method described in embodiment PP33. Embodiment PP35. In the subject, muscarinic acetylcholine receptor M1 activity is regulated. A method for which a compound described in any one of embodiments PP1 to PP24, or the A method comprising administering a pharmaceutically acceptable salt or solvate to a subject. Embodiment PP36. Embodiment P in which the compound acts as a selective M1 antagonist. The method described on page 35.

[0221] X. Further Embodiments Embodiment 1. A compound, or a pharmaceutically acceptable salt or solvate thereof, wherein the formula Having the structure of (IA) or (IB), [ka] During the ceremony, X is bonded, -C(R 9 )(R 10 )-,-N(R 11 )-, -O-, -S(O) n - -CH2N(R 11 )-, or -CH2O-, Y is -CH2-, -CH2CH2-, -CH=CH-, or -CH2OCH2- can be, R 1 but, [ka] In the formula, ring A is either a 5-membered or 6-membered heteroaryl ring, or optionally, Rogen, Cyano, -N(R) 14 )(R 15 ), C 1-6 Alkyl, C 1-6 Alkoxy, C 1-6 Haloalkyl, C 1-6 Haloalkoxy, C 3-6 Cycloalkyl, C 3-6 C Chloalkoxy, C 3-6Halocycloalkyl, C 3-6 Halocycloalkoxy, hetero Cycloalkyl, aryl, heteroaryl, -S(O) n (R 16 ), or -SF A 5-membered or 6-membered heterocycloalkyl ring substituted with 5, and heteroaryl or he The telocycloalkyl ring is selected from the group consisting of O, N, or S, 1, 2, or 3 It contains a number of heteroatoms, R 2 However, hydrogen, deuterium, halogen, hydroxyl, C 1-6 Alkyl, C 1-6 Arco Kishi, C 1-6 Haloalkyl, C 1-6 Haloalkoxy, C 3-6 Cycloalkyl, C3 -6 Cycloalkoxy, C 3-6 Halocycloalkyl, C 3-6 Halocycloalkoxy, C 1-6 Alkylhydroxyl, heterocycloalkyl, aryl, or heteroaryl It is R 3 However, halogen, C 1-6 Alkyl, C 1-6 Alkoxy, C 1-6 Haloalkyl, C 1-6 Haloalkoxy, C 3-6 Cycloalkyl, C 3-6 Cycloalkoxy, C 3- 6-halocycloalkyl, C 3-6 Halocycloalkoxy, C 1-6 Alkylhydroxyl , heterocycloalkyl, aryl, or heteroaryl, or R 2 and R 3 They are connected, and optionally, halogen, C 1-6 Alkyl, or C 3-6 Cycloalkyl Forms a cycloalkyl or heterocycloalkyl ring substituted with , R 4 and R 5 These independently produce hydrogen, deuterium, halogens, and C 1-3 Selected from alkyl groups Selected, or R 3 and R 4 They are connected, and optionally, halogen, C 1-6 Alkyl, also or C 3-6 Cycloalkyl or heterocycloalkyl Forming a ring, or R 4 and R 5 They are connected, and optionally, halogen, C 1-6 Alkyl , or C 3-6 Cycloalkyl or heterocycloalkyl substituted Forms a Kill ring, R 6 and R 7 These independently produce hydrogen, deuterium, halogens, and C 1-3 Selected from alkyl groups Selected, or R 3 and R 7 They are connected, and optionally, halogen, C 1-6 Alkyl, also or C 3-6 Cycloalkyl or heterocycloalkyl Forming a ring, or R 4 and R 6 They are connected, and optionally, halogen, C 1-6 Alkyl , or C 3-6 Cycloalkyl or heterocycloalkyl substituted It forms a kill ring, or R 5 and R 7 They connect to form a bond, R 8 but, [ka] And, R 9 and R 10 These independently produce hydrogen, deuterium, halogens, and C 1-6 Alkyl, C 1-6 Alkoxy, C 1-6 Haloalkyl, C 1-6 Haloalkoxy, C 3-6 Cycloalkyl , C 3-6 Cycloalkoxy, C 3-6 Halocycloalkyl, C 3-6 Halocycloalco Selected from xy, heterocycloalkyl, aryl, or heteroaryl, is R 3 and R 10 They are connected, and optionally, halogen, C 1-6 Alkyl, or C 3- Forming a cycloalkyl or heterocycloalkyl ring substituted with a 6-cycloalkyl group, Or R 4 and R 10 They are connected, and optionally, halogen, C 1-6 Alkyl, or C 3-6 A cycloalkyl or heterocycloalkyl ring substituted with a cycloalkyl group accomplish, or R 6 and R 10 They are connected, and optionally, halogen, C 1-6 Alkyl, also or C 3-6 Cycloalkyl or heterocycloalkyl Forming a ring, or R 9 and R 10 They are connected, and optionally, halogen, C 1-6 Alki Ru, or C 3-6 Cycloalkyl or heterocycloalkyl substituted Forms a lucyl ring, R 11 However, hydrogen, C 1-6 Alkyl, C 1-6Haloalkyl, C 3-6 Cycloalkyl , C 3-6 Halocycloalkyl, heterocycloalkylaryl, or heteroaryl It is R 3 and R 11 They are connected, and optionally, halogen, C 1-6 Alkyl, Or C 3-6 Forms a heterocycloalkyl ring substituted with a cycloalkyl group, or R 4 and R 11 They are connected, and optionally, halogen, C 1-6 Alkyl, or C 3-6 Forms a heterocycloalkyl ring substituted with a cycloalkyl group, or R 6 and R 11 They are connected, and optionally, halogen, C 1-6 Alkyl, or C 3-6 Cycloalkyl Forms a substituted heterocycloalkyl ring, Each R 12 These independently consist of hydroxyl, halogen, cyano, and -N(R) 14 )(R 15 ), C 1-6 Alkyl, C 1-6 Alkoxy, C 1-6 Haloalkyl, C 1-6 Haloalcochry C 3-6 Cycloalkyl, C 3-6 Cycloalkoxy, C 3-6 Halocycloalkyl , C 3-6 Halocycloalkoxy, C 1-6 Alkylhydroxyl, heterocycloalkyl Lu, aryl, heteroaryl, -S(O) n (R 16 ), or select from -SF5 re, or R 3 and one R 12 They are connected, and optionally, halogen, C1-6 Alkyl , or C 3-6 Cycloalkyl or heterocycloalkyl substituted It forms a kill ring, or R 10 and one R 12 They are connected, and optionally, halogen, C 1-6 Alkyl, or C 3-6 Cycloalkyl or cycloalkyl substituted Forms a telocycloalkyl ring, or R 11 and one R 12 They are linked together, arbitrarily , halogen, C 1-6 Alkyl, or C 3-6 Heterocyclic substituted Forms a chloroalkyl ring, R 13 However, hydrogen, C 1-6 Alkyl, C 1-6 Haloalkyl, C 3-6 Cycloalkyl , C 3-6 Halocycloalkyl, heterocycloalkyl, aryl, or heteroaryl It is R 14 and R 15 Hydrogen, C 1-6 Alkyl, C 1-6 Haloalkyl, C 3-6 Cycloalkyl, C 3-6 Halocycloalkyl, heterocycloalkyl, aryl , or selected from heteroaryls, or R 14 and R 15 They are linked together, arbitrarily , halogen, C 1-6 Alkyl, or C 3-6 Heterocyclic substituted Forms a chloroalkyl ring, R 16 However, C 1-6 Alkyl, C 1-6 Haloalkyl, C 3-6Cycloalkyl, C3 -6 Halocycloalkyl, heterocycloalkyl, aryl, or heteroaryl the law of nature, m is 0 or 1, n is 0, 1, or 2, A compound, or a pharmaceutically acceptable salt thereof, in which o is 0, 1, 2, or 3 It is a solvate. Embodiment 2. Having the structure of formula (IIA) or (IIB), [ka] During the ceremony, X is bonded, -C(R 9 )(R 10 )-,-N(R 11 )-, -O-, -S(O) n - -CH2N(R 11 )-, or -CH2O-, Y is -CH2-, -CH2CH2-, -CH=CH-, or -CH2OCH2- can be, R 1 but, [ka] In the formula, ring A is either a 5-membered or 6-membered heteroaryl ring, or optionally, Rogen, Cyano, -N(R) 14 )(R 15 ), C 1-6 Alkyl, C 1-6 Alkoxy, C 1-6 Haloalkyl, C 1-6 Haloalkoxy, C 3-6 Cycloalkyl, C 3-6 C Chloalkoxy, C 3-6 Halocycloalkyl, C 3-6 Halocycloalkoxy, hetero Cycloalkyl, aryl, heteroaryl, -S(O) n (R16 ), or -SF A 5-membered or 6-membered heterocycloalkyl ring substituted with 5, and heteroaryl or he The telocycloalkyl ring is selected from the group consisting of O, N, or S, 1, 2, or 3 It contains a number of heteroatoms, R 2 However, hydrogen, deuterium, halogen, hydroxyl, C 1-6 Alkyl, C 1-6 Arco Kishi, C 1-6 Haloalkyl, C 1-6 Haloalkoxy, C 3-6 Cycloalkyl, C3 -6 Cycloalkoxy, C 3-6 Halocycloalkyl, C 3-6 Halocycloalkoxy, C 1-6 Alkylhydroxyl, heterocycloalkyl, aryl, or heteroaryl It is R 3 However, halogen, C 1-6 Alkyl, C 1-6 Alkoxy, C 1-6 Haloalkyl, C 1-6 Haloalkoxy, C 3-6 Cycloalkyl, C 3-6 Cycloalkoxy, C 3- 6-halocycloalkyl, C 3-6 Halocycloalkoxy, C 1-6 Alkylhydroxyl , heterocycloalkyl, aryl, or heteroaryl, or R 2 and R 3 They are connected, and optionally, halogen, C 1-6 Alkyl, or C 3-6 Cycloalkyl Forms a cycloalkyl or heterocycloalkyl ring substituted with , R 8 but, [ka] And, R 9 and R 10 These independently produce hydrogen, deuterium, halogens, and C 1-6 Alkyl, C 1-6 Alkoxy, C 1-6 Haloalkyl, C 1-6 Haloalkoxy, C 3-6 Cycloalkyl , C 3-6 Cycloalkoxy, C 3-6 Halocycloalkyl, C 3-6 Halocycloalco Selected from xy, heterocycloalkyl, aryl, or heteroaryl, is R 3 and R 10 They are connected, and optionally, halogen, C 1-6 Alkyl, or C 3- Forming a cycloalkyl or heterocycloalkyl ring substituted with a 6-cycloalkyl group, Or R 9 and R 10 They are connected, and optionally, halogen, C 1-6 Alkyl, or C 3-6 A cycloalkyl or heterocycloalkyl ring substituted with a cycloalkyl group accomplish, R 11 However, hydrogen, C 1-6 Alkyl, C 1-6 Haloalkyl, C 3-6 Cycloalkyl , C 3-6 Halocycloalkyl, heterocycloalkylaryl, or heteroaryl It is R 3 and R 11 They are connected, and optionally, halogen, C 1-6 Alkyl, Or C 3-6 Forming a heterocycloalkyl ring substituted with a cycloalkyl group, Each R 12These independently consist of hydroxyl, halogen, cyano, and -N(R) 14 )(R 15 ), C 1-6 Alkyl, C 1-6 Alkoxy, C 1-6 Haloalkyl, C 1-6 Haloalcochry C 3-6 Cycloalkyl, C 3-6 Cycloalkoxy, C 3-6 Halocycloalkyl , C 3-6 Halocycloalkoxy, C 1-6 Alkylhydroxyl, heterocycloalkyl Lu, aryl, heteroaryl, -S(O) n (R 16 ), or select from -SF5 re, or R 3 and one R 12 They are connected, and optionally, halogen, C 1-6 Alkyl , or C 3-6 Cycloalkyl or heterocycloalkyl substituted It forms a kill ring, or R 10 and one R 12 They are conne...

Claims

1. Formula (IA) or (IB): 【Chemistry 1】 [In the formula, X is a bond, -C(R9)(R10)-, -N(R11)-, -O-, -S(O)n-, -CH2N(R11)-, or -CH2O-, Y is -CH₂-, -CH₂CH₂-, -CH=CH-, or -CH₂OCH₂-, R 1 is, 【Chemistry 2】 In the formula, ring A is a 5-membered or 6-membered heteroaryl ring, or a 5-membered or 6-membered heterocycloalkyl ring optionally substituted with halogen, cyano, -N(R14)(R15), C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkyl, C1-6 haloalkoxy, C3-6 cycloalkyl, C3-6 cycloalkoxy, C3-6 halocycloalkyl, C3-6 halocycloalkoxy, heterocycloalkyl, aryl, heteroaryl, -S(O)n(R16), or -SF5, wherein the heteroaryl or heterocycloalkyl ring contains 1, 2, or 3 heteroatoms selected from the group consisting of O, N, or S. R2 is hydrogen, deuterium, halogen, hydroxyl, C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkyl, C1-6 haloalkoxy, C3-6 cycloalkyl, C3-6 cycloalkoxy, C3-6 halocycloalkyl, C3-6 halocycloalkoxy, C1-6 alkylhydroxyl, heterocycloalkyl, aryl, or heteroaryl. R3 is a halogen, C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkyl, C1-6 haloalkoxy, C3-6 cycloalkyl, C3-6 cycloalkoxy, C3-6 halocycloalkyl, C3-6 halocycloalkoxy, C1-6 alkylhydroxyl, heterocycloalkyl, aryl, or heteroaryl, or R2 and R3 are linked to optionally form a cycloalkyl or heterocycloalkyl ring substituted with a halogen, C1-6 alkyl, or C3-6 cycloalkyl, R4 and R5 are independently selected from hydrogen, deuterium, halogen, and C1-3 alkyl, or R3 and R4 are linked to form a cycloalkyl or heterocycloalkyl ring optionally substituted with halogen, C1-6 alkyl, or C3-6 cycloalkyl, or R4 and R5 are linked to form a cycloalkyl or heterocycloalkyl ring optionally substituted with halogen, C1-6 alkyl, or C3-6 cycloalkyl, R6 and R7 are independently selected from hydrogen, deuterium, halogen, and C1-3 alkyl, or R3 and R7 are linked to form a cycloalkyl or heterocycloalkyl ring optionally substituted with halogen, C1-6 alkyl, or C3-6 cycloalkyl, or R4 and R6 are linked to form a cycloalkyl or heterocycloalkyl ring optionally substituted with halogen, C1-6 alkyl, or C3-6 cycloalkyl, or R5 and R7 are linked to form a bond, R8, 【Transformation 3】 And, R9 and R10 are independently selected from hydrogen, deuterium, halogen, C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkyl, C1-6 haloalkoxy, C3-6 cycloalkyl, C3-6 cycloalkoxy, C3-6 halocycloalkyl, C3-6 halocycloalkoxy, heterocycloalkyl, aryl, or heteroaryl, or R3 and R10 are linked to optionally form a cycloalkyl or heterocycloalkyl ring substituted with halogen, C1-6 alkyl, or C3-6 cycloalkyl, Alternatively, R 4 and R 10 may be linked to form a cycloalkyl or heterocycloalkyl ring optionally substituted with a halogen, C 1-6 alkyl, or C 3-6 cycloalkyl, or R 6 and R 10 may be linked to form a cycloalkyl or heterocycloalkyl ring optionally substituted with a halogen, C 1-6 alkyl, or C 3-6 cycloalkyl, or R 9 and R 10 may be linked to form a cycloalkyl or heterocycloalkyl ring optionally substituted with a halogen, C 1-6 alkyl, or C 3-6 cycloalkyl, R11 is hydrogen, C1-6 alkyl, C1-6 haloalkyl, C3-6 cycloalkyl, C3-6 halocycloalkyl, heterocycloalkylaryl, or heteroaryl, or R3 and R11 are linked to form a heterocycloalkyl ring optionally substituted with a halogen, C1-6 alkyl, or C3-6 cycloalkyl, or R4 and R11 are linked to form a heterocycloalkyl ring optionally substituted with a halogen, C1-6 alkyl, or C3-6 cycloalkyl, or R6 and R11 are linked to form a heterocycloalkyl ring optionally substituted with a halogen, C1-6 alkyl, or C3-6 cycloalkyl, Each R12 is independently selected from hydroxyl, halogen, cyano, -N(R14)(R15), C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkyl, C1-6 haloalkoxy, C3-6 cycloalkyl, C3-6 cycloalkoxy, C3-6 halocycloalkyl, C3-6 halocycloalkoxy, C1-6 alkylhydroxyl, heterocycloalkyl, aryl, heteroaryl, -S(O)n(R16), or -SF5, or R3 and one R12 are linked to optionally form a cycloalkyl or heterocycloalkyl ring substituted with halogen, C1-6 alkyl, or C3-6 cycloalkyl, or R10 and one R12 are linked to optionally form a halogen, C1-6 alkyl, or C3-6 A cycloalkyl or heterocycloalkyl ring is formed by substituted cycloalkyl groups, or R11 and one R12 are linked to optionally form a heterocycloalkyl ring substituted with a halogen, C1-6 alkyl, or C3-6 cycloalkyl group. R13 is hydrogen, C1-6 alkyl, C1-6 haloalkyl, C3-6 cycloalkyl, C3-6 halocycloalkyl, heterocycloalkyl, aryl, or heteroaryl. R14 and R15 are independently selected from hydrogen, C1-6 alkyl, C1-6 haloalkyl, C3-6 cycloalkyl, C3-6 halocycloalkyl, heterocycloalkyl, aryl, or heteroaryl, or R14 and R15 are linked to form a heterocycloalkyl ring optionally substituted with halogen, C1-6 alkyl, or C3-6 cycloalkyl. R16 is a C1-6 alkyl, C1-6 haloalkyl, C3-6 cycloalkyl, C3-6 halocycloalkyl, heterocycloalkyl, aryl, or heteroaryl. m is 0 or 1, n is 0, 1, or 2, [where o is 0, 1, 2, or 3] A method for preparing a compound of the same, or a pharmaceutically acceptable salt or solvate thereof, The aforementioned method, (i) In the presence of a suitable coupling reagent and base, formula (1a) or (1b) 【Chemistry 2A】 The compound or its corresponding ammonium salt is given by formula (2) 【Chemistry 3A】 Reacting with a carboxylic acid, formula (3a) or (3b) [Chemistry 4A] The step of generating the amide, And optionally, (ii) Below: (a) Reduction of alkenes or alkynes, (b) Cyclopropane conversion of alkenes, (c) Oxidation of sulfides, (d) Conversion of appropriately functionalized 2- or 4-methoxypyridine to its corresponding 1-methylpyridine-2(1H)-one or 1-methylpyridine-4(1H)-one, (e) Conversion of appropriately functionalized (hetero)aryl halides to their corresponding (hetero)aryl cyanides, and (f) Separation of a mixture of stereoisomers into its stereochemically concentrated component. A step of further functionalizing by at least one transformation selected from, Methods that include...

2. Formula (IA) or (IB): 【Chemistry 1】 [In the formula, X, Y, R1, R2, R3, R4, R5, R6, R7, R8, and m are as defined in claim 1.] A method for preparing a compound of the same, or a pharmaceutically acceptable salt or solvate thereof, The aforementioned method, (i) Equation (1a) or (1b) 【Chemistry 2A】 Formula (2) shows the compound being pre-activated into the corresponding acid chloride. 【Chemistry 3A】 Reacting with a carboxylic acid, formula (3a) or (3b) [Chemistry 4A] The step of generating the amide, And optionally, (ii) Below: (a) Reduction of alkenes or alkynes, (b) Cyclopropane conversion of alkenes, (c) Oxidation of sulfides, (d) Conversion of appropriately functionalized 2- or 4-methoxypyridine to its corresponding 1-methylpyridine-2(1H)-one or 1-methylpyridine-4(1H)-one, (e) Conversion of appropriately functionalized (hetero)aryl halides to their corresponding (hetero)aryl cyanides, and (f) Separation of a mixture of stereoisomers into its stereochemically concentrated component. A step of further functionalizing by at least one transformation selected from, Methods that include...

3. Formula (IA) or (IB): 【Chemistry 1】 [In the formula, X, Y, R1, R2, R3, R4, R5, R6, R7, R8, and m are as defined in claim 1.] A method for preparing a compound of the same, or a pharmaceutically acceptable salt or solvate thereof, The aforementioned method, (i) Equation (4a) or (4b) [Chemical 5A] (In the formula, PG is a protecting group.) The compound is given by formula (2) 【Chemical Engineering 6A】 By coupling with a carboxylic acid, formula (5a) or (5b) 【Chemical 7A】 The step of generating the compound, (ii) Remove the protecting group (PG) to form formula (6a) or (6b) 【Chemical Engineering 8A】 The steps of generating the compound, (iii) The step of reacting the obtained amine (6a) or (6b) with a (hetero)aryl halide represented by R8 to produce a compound of formula (IA) or (IB), Methods that include...

4. Formula (IA) or (IB): 【Chemistry 1】 [In the formula, X, Y, R1, R2, R3, R4, R5, R6, R7, R8, and m are as defined in claim 1.] A method for preparing a compound of the same, or a pharmaceutically acceptable salt or solvate thereof, The aforementioned method, (i) Equation (9) 【Chemical Engineering 9A】 The compound of formula (8a) or (8b) 【Chemical Engineering 10A】 (In the formula, LG is a leaving group.) The step of reacting the compound with the leaving group (LG) via direct nucleophilic substitution, And optionally, (ii) If the compound of formula (9) is an amine, a step including a prior step of activating the compound; or Methods that include...

5. Formula (IA) or (IB): 【Chemistry 1】 [In the formula, X, Y, R1, R2, R3, R4, R5, R6, R7, R8, and m are as defined in claim 1.] A method for preparing a compound of the same, or a pharmaceutically acceptable salt or solvate thereof, The aforementioned method, Formula (11a) or (11b) 【Chemical Engineering 11A】 The compound is given by formula (12) 【Chemical Engineering 12A】 (In the formula, LG is a leaving group.) step of reacting with the compound Methods that include...

6. The method according to claim 4, wherein the method is (i) Equation (9) 【Chemical 14A】 The compound of formula (8a) or (8b) 【Chemical Engineering 15A】 (In the formula, LG is a leaving group.) A step of reacting the compound with the compound via direct nucleophilic substitution of a leaving group (LG), and optionally, if the compound of formula (9) is an amine, a step of activating the compound; And optionally, (ii) Furthermore, equation (8a) or (8b) 【Chemical Engineering 16A】 (In the formula, LG is a leaving group.) A step of preparing a compound of formula (1a) or (1b) in the presence of a suitable base 【Chemical Engineering 17A】 The compound is given by formula (7) 【Chemical 18A】 A step including reacting with the compound; Methods that include...

7. The method according to claim 5, wherein the method is (i) Equation (11a) or (11b) 【Chemical Engineering 19A】 The compound is given by formula (12) 【Chemical Engineering 20A】 (In the formula, LG is a leaving group.) A step of reacting with the compound; And optionally, (ii) Furthermore, equation (11a) or (11b) 【Chemical Engineering 21A】 A step of preparing a compound of formula (1a) or (1b) 【Chemical Engineering 22A】 The compound is given by formula (10) 【Chemical Engineering 23A】 A step comprising reacting with and further removing the protecting group (PG); Methods that include...

8. Formula (IA) or (IB): 【Chemistry 1】 [wherein X is NH, and Y, R1, R2, R3, R4, R5, R6, R7, R8, and m are as defined in claim 1.] A method for preparing a compound of the same, or a pharmaceutically acceptable salt or solvate thereof, wherein the method is: (i) Equation (15a) or (15b) 【Chemical 24A】 The compound can be reduced using an appropriate reagent, or formula R ２ - A step of supplementing with an organometallic compound of M; And optionally, (ii) Furthermore, equation (15a) or (15b) 【Chemical 25A】 A step of preparing a compound of formula (13a) or (13b) 【Chemical Engineering 26A】 The compound is given by formula (14) 【Chemical Engineering 27A】 A step comprising reacting the compound with the compound under dehydration conditions; Methods that include... 【Request Item 9】 【Chemical 28A】 A compound of formula (2), or a salt thereof.

10. formula 【Chemistry 29A】 A compound or salt thereof.

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