B0AT1 inhibitor

Description

COMPOUND, PHARMACEUTICAL COMPOSITION, USES THEREOF, B0AT1 INHIBITOR AND KIT TECHNICAL FIELD

[001] The present invention relates to a new compound with inhibitory action on the neutral amino acid transporter B0AT1. BACKGROUND OF THE TECHNIQUE

[002] SLC6A19, the gene causing Hartnup disease, is located at 5p15.33 and consists of 12 exons. Its gene product, the neutral amino acid transporter B0AT1, consists of 634 amino acids and has 12 transmembrane sites (Unpatented Documents 1 and 2). B0AT1 is an important transporter of neutral amino acids in the small intestine and kidneys, being responsible for the absorption of glycine, leucine, phenylalanine, etc. in the small intestine and their reabsorption in the kidneys (Unpatented Documents 3 to 5). B0AT1 knockout mice exhibit elevated urinary levels of amino acids (Unpatented Document 6), and clinically, B0AT1 dysfunction also results in severe neutral aminoaciduria, known as Hartnup disease (Unpatented Document 7). Therefore, it is believed that inhibiting B0AT1 may improve (alleviate) various diseases or conditions involving neutral amino acids, which are transport substrates.

[003] In addition, specific examples of therapeutic effects in diseases by inhibiting B0AT1 function have also been reported. For example, phenylketonuria pathology in model mice is improved by congenital B0AT1 deficiency or by inducing acquired inhibition of expression through administration of a nucleic acid compound that binds to mRNA (Unpatented Document 4).

[004] In this context, compounds that inhibit B0AT1 have attracted attention as drugs for prophylaxis and / or treatment of Petition 870250102069, dated 07 / 11 / 2025, pp. 443 / 861 2 / 389 various diseases or conditions involving neutral amino acids as transport substrates, specifically, disorders of amino acid metabolism.

[005] Examples of amino acid metabolism disorders include designated intractable diseases such as phenylketonuria, urea cycle disorder, hypertyrosinemia (types 1-3), hypermethioninemia, maple syrup urine disease, homocystinuria, nonketotic hyperglycinemia, propionic acidemia, methylmalonic acidemia, isovaleric acidemia and the like.

[006] As a treatment method for this, continuous dietary therapy is primarily known. In addition to dietary therapy, the administration of drugs that increase coenzymes and enzymes and treatment methods based on enzyme injection are also known, but none of them is a fundamental treatment (e.g., Non-Patented Document 8, etc.).

[007] Therefore, there is a need to develop agents to prevent and / or treat diseases, specifically, disorders of amino acid metabolism that can be alleviated by normalizing neutral amino acid metabolism through the inhibition of B0AT1.

[008] To date, compounds with inhibitory activity of For example, nucleic acids with sequences that partially or completely correspond to B0AT1 RNA are known (Unpatented Document 4), nimesulide and its derivatives (Unpatented Documents 9 and 10), which are commercially available products, sinromide (Unpatented Document 11), which is a publicly known compound, and basic compounds found in library screenings (Unpatented Documents 12, 13), and similar compounds. Furthermore, cinnamic acid glycineamide and compounds are also known (Patent Literature 1). Petition 870250102069, dated 07 / 11 / 2025, pp. 444 / 861 3 / 389 LIST OF CITATIONS PATENTED LITERATURE Patented Literature 1 WO 2023 / 145804 Non-Patented Literature Non-Patented Literature 1 Nat. Genet., 2004; 36: p.999-1002 Non-Patented Literature 2 Nat. Genet., 2004; 36: p.1003-w07 Non-Patented Literature 3 The Journal of Biological Chemistry 2004; 279: p.24467-24476 Non-Patented Literature 4 JCI Insight., 2018; 3(14): p.e121762 Non-Patented Literature 5 IUBMB Life, 2009; 61(6): p.591-599 Non-Patented Literature 6 MOLECULAR METABOLISM, 2015: p.406-417 Non-Patented Literature 7 Biochem. J., 2005; 389: p.745-751 Non-Patented Literature 8 Intractable Disease Information Center, Phenylketonuria (designated intractable disease 240)(http: / / www.nanbyou.or.jp / entry / 4747) Non-Patented Literature 9 Biochemical Pharmacology, 2014; 89: p.422-430 Non-Patented Literature 10 Letters on Bioorganic and Medicinal Chemistry, 2021; 53: p. 128421 Non-Patented Literature 11 SLAS Discovery, 2019; 24(2): p. 111-120 Non-Patented Literature 12 British Journal of Pharmacology, 2017; 174: p.468-482 Petition 870250102069, dated 07 / 11 / 2025, pp. 445 / 861 4 / 389 Non-Patented Literature 13 Frontiers in Pharmacology, 2020; 11: p. 140 SUMMARY OF THE INVENTION TECHNICAL PROBLEM

[009] The present invention provides a new compound with superior inhibitory action on B0AT1 and a drug containing the same as an active ingredient. SOLUTION TO THE PROBLEM

[0010] Intensive studies were conducted and found that a compound represented by the following formula (I): (l) in which R is an optionally substituted Ce-waryl-ethenyl group; R1 is a carboxy group or a group biologically equivalent to a carboxy group; L is a divalent organic group comprising a group selected from the group consisting of a C1-6 alkylene group, a C1-6 arylene group, a C3-4 cycloalkylene group, a C2-6 alkenylene group, a C2-6 alkynylene group and a divalent non-aromatic heterocyclic group of 3 to 14 members, each of which is optionally also substituted, and A is a heterocyclic group containing divalent nitrogen that is optionally also substituted (hereinafter sometimes abbreviated as “compound (I)”), and a pharmaceutically acceptable salt thereof has a superior inhibitory action on the neutral amino acid transporter B0AT1, and concludes the present invention.

[0011] In other words, the present invention provides the following.

[0012] [1] A compound represented by formula (I): Petition 870250102069, dated 07 / 11 / 2025, pp. 446 / 861 5 / 389 O (1) in which R is an optionally substituted Ce-waryl-ethenyl group; R1 is a carboxy group, or a group biologically equivalent to a carboxy group; L is a divalent organic group comprising a group selected from the group consisting of a C1-6 alkylene group, a C1-6 arylene group, a C3-4 cycloalkylene group, a C2-6 alkenylene group, a C2-6 alkynylene group and a divalent non-aromatic heterocyclic group of 3 to 14 members, each of which is optionally substituted; and A is a heterocyclic group containing divalent nitrogen, optionally also substituted, or a pharmaceutically acceptable salt thereof.

[0013] [2] The compound described in [1] above or a pharmaceutically acceptable salt thereof, wherein, in formula (I), R is a 2-phenylthenyl group optionally substituted by 1 to 3 substituents selected from the group consisting of a halogen atom, an optionally substituted C1-6 alkyl group, an optionally substituted C3-8 cycloalkyl group, an optionally substituted C1-6 alkoxy group, an optionally substituted C3-8 cycloalkoxy group, an optionally substituted C1-6 alkylsulfanyl group, an optionally substituted C3-8 cycloalkylsulfanyl group, and a pentafluorosulfanyl group; R1 is a carboxy group, or a group biologically equivalent to a carboxy group; L is a C1-6 alkylene group, a Ce-wararylene group, a C3-14 cycloalkylene group, a C2-6 alkenylene group, a C2-6 Petition 870250102069, dated 07 / 11 / 2025, pp. 447 / 861 6 / 389 alkynylene, or a divalent non-aromatic heterocyclic group of 3 to 14 members, each of which optionally has, in the interior or at the end, one or more divalent groups selected from the group consisting of -NR2- (where R2 is a hydrogen atom or a C1-6 alkyl group), -O-, -S-, -C(=O)-, a C1-6 alkylene group, a Ce-warrylene group, a C3-4 cycloalkylene group, a C2-6 alkenylene group, a C2-6 alkynylene group and a divalent non-aromatic heterocyclic group of 3 to 14 members, and each of which is optionally also substituted by 1 to 3 substituents selected from substituent group a; and A is a non-aromatic heterocyclic group containing divalent nitrogen, represented by the following formula: where ** is a carbonyl group binding site, *** is an L group binding site, and ring A1 is a 3- to 10-membered monocycle, an 8- to 14-membered fused cycle, a 6- to 16-membered spiro cycle, or a 6- to 14-membered bridging cycle, and optionally has, as a ring constituent atom in addition to a nitrogen atom and a carbon atom, heteroatoms selected from the group consisting of a nitrogen atom, an oxygen atom, and a sulfur atom, which is optionally also substituted by 1 to 3 substituents selected from the substituent group a (Substituent Group a): a halogen atom; a hydroxyl group; a cyan group; an oxo group; a C1-6 alkyl group optionally substituted by Petition 870250102069, dated 07 / 11 / 2025, pp. 448 / 861 7 / 389 substituents selected from the group consisting of a halogen atom, a hydroxyl group, a cyano group, a C1-6 alkoxy, a C6-14 aryl group, a carboxy group, a C1-6 alkoxy-carbonyl group, a carbamoyl group optionally substituted by 1 or 2 C1-6 alkyl groups, and a C6-14 aryloxy group; a C1-6 alkoxy optionally substituted with halogen atoms; a C1-6 alkylsulfonyl group optionally substituted with halogen atoms; a C1-6 alkyl-carbonyl group; a C1-6 alkoxy-carbonyl group; a carbamoyl group optionally substituted by 1 or 2 C1-6 alkyl groups optionally substituted by substituents selected from the group consisting of a halogen atom, a hydroxyl group, a di-C1-6 alkylamino group, and a C1-6 alkoxy group; a di-C1-6 alkylamino group; a trisubstituted silyl group; a trisubstituted silyl oxy group; a C6-14 hydrocarbocyclic group optionally substituted by 1 to 3 substituents selected from substituent group b or substituent group b'; an aromatic heterocyclic group of 5 to 14 members optionally substituted by 1 to 3 substituents selected from substituent group b or substituent group b'; and a non-aromatic heterocyclic group of 3 to 14 members optionally substituted by 1 to 3 substituents selected from substituent group b or substituent group b' (Substituent Group b): a halogen atom; a hydroxyl group; Petition 870250102069, dated 07 / 11 / 2025, pp. 449 / 861 8 / 389 a cyan group; an oxo group; a carboxy group; a C1-6 alkyl group optionally substituted by substituents selected from the group consisting of a halogen atom, a hydroxyl group, a cyano group, and a C1-6 alkoxy; a C3-8 cycloalkyl group optionally substituted by substituents selected from the group consisting of a halogen atom, a hydroxyl group, a cyano group, and a C1-6 alkoxy; an optionally substituted C6-10 aryl group with substituents selected from the group consisting of a halogen atom, a hydroxyl group, a cyano group, a C1-6 alkyl group, and a C1-6 alkoxy group; an aromatic heterocyclic group of 5 to 14 members optionally substituted with substituents selected from the group consisting of a halogen atom, a hydroxyl group, a cyano group, a C1-6 alkyl group, and a C1-6 alkoxy group; a non-aromatic heterocyclic group of 3 to 14 members optionally substituted with substituents selected from the group consisting of a halogen atom, a hydroxyl group, a cyano group, a C1-6 alkyl group, and a C1-6 alkoxy group; a C1-6 alkoxy optionally substituted by substituents selected from the group consisting of a halogen atom, a hydroxyl group, a cyano group, and a C1-6 alkoxy; a C1-6 alkylsulfanyl group optionally substituted by substituents selected from the group consisting of a halogen atom, a hydroxyl group, a cyano group, and a C1-6 alkoxy; a C3-8 cycloalkyloxy group optionally substituted by substituents selected from the group consisting of a halogen atom, a hydroxyl group, a cyano group, and a C1-6 alkoxy; Petition 870250102069, dated 07 / 11 / 2025, pp. 450 / 861 9 / 389 a C1-6 alkylsulfonyl group optionally substituted by halogen atoms; a C1-6 alkyl-carbonyl group optionally substituted with halogen atoms; a C1-6 alkoxy-carbonyl group; a carbamoyl group optionally substituted by 1 or 2 C1-6 alkyl groups optionally substituted by substituents selected from the group consisting of a halogen atom, a hydroxyl group, a di-C1-6 alkylamino group, and a C1-6 alkoxy group; a sulfamoyl group substituted by a substituent selected from the group consisting of a C1-6 alkyl group, a C3-8 cycloalkyl group, and a non-aromatic heterocyclic group, each of which is optionally substituted by 1 to 3 substituents selected from the group consisting of a halogen atom, a hydroxyl group, a cyano group, and a C1-6 alkoxy group; and a pentafluorosulfanyl group (Substituent Group b'): a halogen atom; a hydroxyl group; a cyan group; an oxo group; a carboxy group; a C1-6 alkyl group optionally substituted by substituents selected from the group consisting of a halogen atom, a hydroxyl group, a cyano group, and a C1-6 alkoxy; a C3-8 cycloalkyl group optionally substituted by substituents selected from the group consisting of a halogen atom, a hydroxyl group, a cyano group, and a C1-6 alkoxy; an optionally substituted C1-6 alkoxy with substituents selected from the group consisting of a halogen atom, a Petition 870250102069, dated 07 / 11 / 2025, pp. 451 / 861 10 / 389 hydroxyl group, a cyano group, and a C1-6 alkoxy group; a C1-6 alkylsulfonyl group optionally substituted by substituents selected from the group consisting of a halogen atom, a hydroxyl group, a cyano group, and a C1-6 alkoxy; a C3-8 cycloalkyloxy group optionally substituted by substituents selected from the group consisting of a halogen atom, a hydroxyl group, a cyano group, and a C1-6 alkoxy; a C1-6 alkylsulfonyl group optionally substituted with halogen atoms; a C1-6 alkyl-carbonyl group optionally substituted with halogen atoms; a C1-6 alkoxy-carbonyl group; a carbamoyl group optionally substituted by 1 or 2 C1-6 alkyl groups optionally substituted by substituents selected from the group consisting of a halogen atom, a hydroxyl group, a di-C1-6 alkylamino group, and a C1-6 alkoxy group; a sulfamoyl group substituted by a substituent selected from the group consisting of a C1-6 alkyl group, a C3-8 cycloalkyl group and a non-aromatic heterocyclic group, each of which is optionally substituted by 1 to 3 substituents selected from the group consisting of a halogen atom, a hydroxyl group, a cyano group, and a C1-6 alkoxy group; and a pentafluorosulfanyl group.

[0014] [3] The compound described in [1] above or a pharmaceutically acceptable salt thereof, wherein, in formula (I), R is a 2-(E)-phenylthenyl group optionally substituted by 1 to 3 substituents selected from the group consisting of a halogen atom, a C1-6 alkyl group optionally substituted by halogen atoms, and a pentafluorosulfanyl group; R1 is a carboxy group or a biologically Petition 870250102069, dated 07 / 11 / 2025, pp. 452 / 861 11 / 389 equivalent to a carboxy group; L is a C1-6 alkylene group optionally having, in the interior or at the end, one or more divalent groups selected from the group consisting of -NR2- (where R2 is a hydrogen atom or a C16 alkyl group), -O-, -S-, -C(=O)-, a Ce-10 arylene group, a C3-10 cycloalkylene group, a C2-6 alkynylene group, and a 3- to 8-membered divalent non-aromatic heterocyclic group, optionally also substituted by 1 to 3 substituents selected from the previously mentioned substituent group, a Ce-10 arylene group optionally also substituted by 1 to 3 substituents selected from the previously mentioned substituent group, a C3-10 cycloalkylene group optionally also substituted by 1 to 3 substituents selected from the previously mentioned substituent group, a C2-4 alkynylene group optionally also substituted by 1 to 3 substituents selected from the previously mentioned substituent group, or a 3- to 8-membered divalent non-aromatic heterocyclic group optionally also substituted by 1 to 3 substituents selected from the previously mentioned substituent group a; and A is a non-aromatic heterocyclic group containing divalent nitrogen, represented by the following formula: Petition 870250102069, dated 07 / 11 / 2025, pp. 453 / 861 12 / 389 uww wherein a wavy line is a bonding site of the group represented by the chemical formula mentioned above, a bond represented by is a single bond or a double bond, each Y is independently a nitrogen atom or CR3 (wherein R3 is a hydrogen atom or a C1-6 alkyl group), Z is an oxygen atom, a sulfur atom, NR4 or CR5R6 (wherein R4, R5 and R6 are each independently a hydrogen atom or a C1-6 alkyl group), n is an integer from 0 to 2, m is an integer from Petition 870250102069, dated 07 / 11 / 2025, pp. 454 / 861 13 / 389 a 2, n1 and n2 are, each independently, an integer from 0 to 2, m1 and m2 are, each independently, an integer from 0 to 2, **is a binding site with a carbonyl group, and ***is a binding site with the L group, whose non-aromatic heterocyclic group is optionally also replaced by 1 to 3 substituents selected from the previously mentioned substituent group.

[0015] [3'] The compound described in [1] mentioned above or a pharmaceutically acceptable salt thereof, wherein, in formula (I), R is a 2-(E)-phenyl-ethenyl group optionally substituted by 1 to 3 substituents selected from the group consisting of a halogen atom, a C1-6 alkyl group optionally substituted by halogen atoms, and a pentafluorosulfanyl group; R1 is a carboxy group or a group biologically equivalent to a carboxy group; L is a C1-6 alkylene group optionally having, in the interior or at the end, one or more divalent groups selected from the group consisting of -NR2- (where R2 is a hydrogen atom or a C16 alkyl group), -O-, -S-, -C(=O)-, a C10 arylene group, a C3-10 cycloalkylene group, a C2-6 alkynylene group, and a divalent non-aromatic heterocyclic group of 3 to 8 members, and optionally also substituted by 1 to 3 substituents selected from the previously mentioned substituent group, a C10 arylene group optionally also substituted by 1 to 3 substituents selected from the previously mentioned substituent group, a C3-10 cycloalkylene group optionally also substituted by 1 to 3 substituents selected from the previously mentioned substituent group, Petition 870250102069, dated 07 / 11 / 2025, pp. 455 / 861 14 / 389 a C2-4 alkynylene group optionally also substituted by 1 to 3 substituents selected from the aforementioned substituent group, or a divalent non-aromatic heterocyclic group of 3 to 8 members optionally also substituted by 1 to 3 substituents selected from the aforementioned substituent group; and A is a non-aromatic heterocyclic group containing divalent nitrogen, represented by the following formula: where a wavy line is a binding site of the group represented by the chemical formula mentioned above, a bond represented by Petition 870250102069, dated 07 / 11 / 2025, pp. 456 / 861 15 / 389 is a single bond or a double bond, each Y is independently a nitrogen atom or CR3 (where R3 is a hydrogen atom or a C1-6 alkyl group), Z is an oxygen atom, a sulfur atom, NR4 or CR5R6 (where R4, R5 and R6 are each independently a hydrogen atom or a C1-6 alkyl group), n is an integer from 0 to 2, m is an integer from 0 to 2, n1 and n2 are each independently an integer from 0 to 2, m1 and m2 are each independently an integer from 0 to 2, ** is a bonding site with a carbonyl group, and *** is a bonding site with the L group, whose non-aromatic heterocyclic group is optionally also substituted by 1 to 3 substituents selected from the previously mentioned substituent group.

[0016] [4] The compound described in [3] or [3'] above or a pharmaceutically acceptable salt thereof, wherein, in formula (I), L is a C1-6 alkylene group optionally having, in the interior or at the end, one or more divalent groups selected from the group consisting of -NR2- (where R2 is a hydrogen atom or a C16 alkyl group), -O-, -S-, a C3-10 cycloalkylene group, and a 3- to 8-membered divalent non-aromatic heterocyclic group, and optionally also substituted by 1 to 3 substituents selected from the previously mentioned substituent group, a C3-10 cycloalkylene group optionally also substituted by 1 to 3 substituents selected from the previously mentioned substituent group, or a 3- to 8-membered divalent non-aromatic heterocyclic group optionally also substituted by 1 to 3 substituents selected from the previously mentioned substituent group.

[0017] [5] The compound described in [3] or [3'] above or Petition 870250102069, dated 07 / 11 / 2025, pp. 457 / 861 16 / 389 a pharmaceutically acceptable salt thereof, wherein, in formula (I), L is a C1-6 alkylene group optionally also substituted by 1 to 3 substituents selected from the previously mentioned substituent group.

[0018] [6] The compound described in [5] above or a pharmaceutically acceptable salt thereof, wherein, in formula (I), A is a non-aromatic heterocyclic group containing divalent nitrogen, represented by the following formula: (where each symbol is as defined above), and optionally also replaced by 1 to 3 substituents selected from the previously mentioned substituent group.

[0019] [7] The compound described in [5] above or a pharmaceutically acceptable salt thereof, wherein, in formula (I), A is a non-aromatic heterocyclic group containing divalent nitrogen, represented by the following formula: Petition 870250102069, dated 07 / 11 / 2025, pp. 458 / 861 17 / 389 (where each symbol is as defined above, provided that when Z is CR5R6, the optionally substituted substituent is selected from the group consisting of, among the substituents in the aforementioned substituent group a, a Ce-14 hydrocarbocyclic group optionally substituted by 1 to 3 substituents selected from substituent group b or substituent group b'; an aromatic heterocyclic group of 5 to 14 members optionally substituted by 1 to 3 substituents selected from substituent group b or substituent group b'; and a non-aromatic heterocyclic group of 3 to 14 members optionally substituted by 1 to 3 substituents selected from substituent group b or substituent group b'), and optionally also substituted by 1 to 3 substituents selected from the aforementioned substituent group a.

[0020] [8] The compound described in [5] above or a pharmaceutically acceptable salt thereof, wherein, in formula (I), A is a non-aromatic heterocyclic group containing divalent nitrogen, represented by the following formula: (where each symbol is as defined above), and optionally also replaced by 1 to 3 substituents selected from the previously mentioned substituent group.

[0021] [9] The compound described in [5] above or a pharmaceutically acceptable salt thereof, wherein, in formula (I), Petition 870250102069, dated 07 / 11 / 2025, pp. 459 / 861 18 / 389 A is a non-aromatic heterocyclic group containing divalent nitrogen, represented by the following formula: (where each symbol is as defined above), and optionally also replaced by 1 to 3 substituents selected from the previously mentioned substituent group.

[0022] [9'] The compound described in [5] above or a pharmaceutically acceptable salt thereof, wherein, in formula (I), A is a non-aromatic heterocyclic group containing divalent nitrogen, represented by the following formula: (where each symbol is as defined above), and optionally also replaced by 1 to 3 substituents selected from the previously mentioned substituent group.

[0023]

[10] The compound described in any of the [1] to [9], [3'], and [9'] mentioned above, or a pharmaceutically acceptable salt thereof, wherein, in formula (I), R1 is a carboxy group, an optionally substituted C1-6 alkoxy-carbonyl group, or an optionally substituted carbamoyl group.

[0024]

[11] A compound selected from the group consisting of 2-[2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]3,4-dihydro-1H-isoquinolin-6-yl]acetic acid; 3-[2-[2-[[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]3,4-dihydro-1H-isoquinolin-6-yl]propanoic acid; N,N-dimethyl-3-[5-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] Petition 870250102069, dated 07 / 11 / 2025, p. 460 / 861 19 / 389 acetyl]-6,7-di-hydro-4H-pyrazolo[1,5-a]pyrazine-3-yl]propanamide; Acid 1 -[7-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]6,8-di-hydro-5H-2,7-naphthyridine-3-yl]piperidine-4-carboxylic; Acid 3-[3-bromo-5-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-6,7-di-hydro-4H-pyrazolo[1,5-a]pyrazine-2-yl]propanoic; Acid 2-[[2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]3,4-di-hydro-1H-isoquinolin-6-yl]oxy]acetic acid; Acid 2-[2-[2-[[(E)-3-3-[4-(pentafluoro-À6-sulfanyl)phenyl]prop-2-enoyl]amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid (1R*,2R*)-2-[2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2enoyl]amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]cyclopropane-1carboxylic enantiomer and both os Acid 2-[2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]3,4-di-hydro-1H-isoquinolin-6-yl]propanoic acid; Acid 2-[7-fluoro-2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid 2-[8-fluoro-2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; 2-[7-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-6,8-dihydro-5H- 2,7-naphthyridine-3-yl]acetic acid; 3-[3-bromo-5-[2-[[(E)-3-[4-(pentafluoro-À6-sulfanyl)phenyl]prop-2enoyl]amino] acetyl]-6,7-di-hydro-4H-pyrazolo[1,5-a]pyrazine-2yl]propanoic; Acid 2-[2-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid 2-[[2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]3,4-di-hydro-1H-isoquinolin-6-yl]amino]acetic acid; Acid 2-[2-[2-[[(E)-3-(4-iodophenyl)prop-2-enoyl]amino] acetyl]-3,4-di-hydro1H-isoquinolin-6-yl]acetic acid; Acid 2-[5-fluoro-2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] Petition 870250102069, dated 07 / 11 / 2025, p. 461 / 861 20 / 389 acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid 2-[8-chloro-2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid 2-[8-fluoro-2-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2enoyl]amino]acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid 2-[8-cyano-2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid 2-[8-fluoro-2-[2-[[(E)-3-(2-fluoro-4-iodophenyl)prop-2-enoyl]amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid 2-[8-fluoro-2-[2-[[(E)-3-(4-iodophenyl)prop-2-enoyl]amino] acetyl]-3,4di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid 2-[8-chloro-2-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2enoyl]amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid 2-[[5-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]6,7-di-hydro-4H-[1,3]thiazolo[5,4-c]pyridin-2-yl]sulfanyl]acetic acid; Acid 2-[7-chloro-2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid 2-[8-cyano-2-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2enoyl]amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid 2-[5-chloro-2-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2enoyl]amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid (E)-N-[2-[6-(2-amino-2-oxoethyl)-3,4-di-hydro-1H-isoquinolin-2-yl]-2oxoethyl]-3-[4-(trifluoromethyl)phenyl]prop-2-enamide; Acid 2-[5-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]6,7-di-hydro-4H-[1,3]thiazolo[4,5-c]pyridin-2-yl]acetic acid; (E)-N-[2-[6-[2-(methylamino)-2-oxoethyl]-3,4-di-hydro-1H-isoquinolin-2-yl]-2oxoethyl]-3-[4-(trifluoromethyl)phenyl]prop-2-enamide; 4-[4-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-3-phenylpiperazine-1-yl]butanoic acid and both enantiomers of the same; Petition 870250102069, dated 07 / 11 / 2025, p. 462 / 861 21 / 389 Acid 2-[[1-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]2,3-di-hydroindol-4-yl]oxy]acetic acid; Acid 1 -[1-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2enoyl]amino]acetyl]piperidin-3-yl]bicyclo[2.1.1]hexane-5-carboxylic; Acid 2-[[8-fluoro-2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]oxy]-2-methylpropanoic; 3-[[8-fluoro-2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-3,4-di-hidro-1H-isoquinolin-6-yl]óxi]-2,2-dimethylpropanoic acid; 4-[4-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-2-methylpiperazin-1-yl]butanoic acid; 4-[(3S)-3-(4-bromophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid; 4-[3-(3-bromophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid; 4-[3-(4-chlorophenyl)-4-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid; 3-[[3-(4-chlorophenyl)-4-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop2-enoyl]amino]acetyl]piperazin-1-yl]methyl]cyclobutane-1-carboxylic acid and both enantiômeros do mesmo; 4-[3-(4-chlorophenyl)-4-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop2-enoyl]amino]acetyl]piperazin-1-yl]-2,2-dimethylbutanoic acid; 4-[3-(3-cyclopropylphenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid; 4-[3-(4-chlorophenyl)-4-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid and both enantiômeros do mesmo; 4-[(2R,5S)-4-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2enoyl]amino]acetyl]-2-methyl-5-phenylpiperazin-1-yl]butanoic acid; 4-[(3S)-3-(4-cyclopropylphenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid; Petition 870250102069, 07 / 11 / 2025, pág. 463 / 861 22 / 389 4-[3-(4-chloro-3-fluorophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid; 4-[(2R,5S)-5-(3,4-difluorophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-2-methylpiperazin-1yl]butanoic acid; 4-[(2R,5S)-5-(3,4-difluorophenyl)-2-methyl-4-[2-[[(E)-3-[4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid; 4-[(2R,5S)-5-(4-chlorophenyl)-4-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop2-enoyl]amino]acetyl]-2-methylpiperazin-1-yl]butanoic acid; 3-[(2R,5S)-5-(4-chlorophenyl)-4-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop2-enoyl]amino]acetyl]-2-methylpiperazin-1-yl]propanoic acid; 4-[(2R,5S)-5-(4-chlorophenyl)—4—[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-2-methylpiperazin-1yl]butanoic acid; 4-[(2R,5S)-5-(4-fluorophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-2-methylpiperazin-1yl]butanoic acid; 3-[(2R,5S)-5-(4-chlorophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]-2-methylpiperazin-1yl]propanoic acid; 4-[(2R,5S)-5-(3-fluorophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]-2-methylpiperazin-1yl]butanoic acid; 4-[(2R,5S)-2-ethyl-4-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop2-enoyl]amino]acetyl]-5-phenylpiperazin-1-yl]butanoic acid; and 4-[(2R,5S)-4-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]-2-methyl-5-phenylpiperazin-1-yl]-2,2-dimethylbutanoic acid or a pharmaceutically acceptable salt thereof.

[12] A compound selected from the group consisting of Petition 870250102069, dated 07 / 11 / 2025, pp. 464 / 861 23 / 389 2-[2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]3,4-dihydro-1H-isoquinolin-6-yl]acetic acid; Acid 3-[2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]3,4-di-hydro-1H-isoquinolin-6-yl]propanoic acid; N,N-dimethyl-3-[5-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-6,7-di-hydro-4H-pyrazolo[1,5-a]pyrazine-3-yl]propanamide; Acid 2-[2-[2-[[(E)-3-3-[4-(pentafluoro-À6-sulfanyl)phenyl]prop-2-enoyl]amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid (1R*,2R*)-2-[2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]cyclopropane-1-enantiome ambiome doxoid; Acid 2-[2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]3,4-di-hydro-1H-isoquinolin-6-yl]propanoic acid; Acid 2-[7-fluoro-2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid 2-[8-fluoro-2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid 2-[2-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid 2-[2-[2-[[(E)-3-(4-iodophenyl)prop-2-enoyl]amino] acetyl]-3,4-di-hydro1H-isoquinolin-6-yl]acetic acid; Acid 2-[5-fluoro-2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid 2-[8-chloro-2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid 2-[8-fluoro-2-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2enoyl]amino]acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid 2-[8-cyano-2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid 2-[8-fluoro-2-[2-[[(E)-3-(2-fluoro-4-iodophenyl)prop-2-enoyl]amino] Petition 870250102069, dated 07 / 11 / 2025, p. 465 / 861 24 / 389 acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid 2-[8-chloro-2-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2-enoyl] amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid 2-[7-chloro-2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid 2-[5-chloro-2-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2-enoyl] amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid 2-[5-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]6,7-di-hydro-4H-[1,3]thiazolo[4,5-c]pyridin-2-yl]acetic acid; Acid 4-[(3S)-4-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2-enoyl] amino] acetyl]-3-phenylpiperazine-1-yl]butanoic; 1-[1-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperidin-3-yl]bicyclo[2.1.1]hexane-5-carboxylic acid; 4-[(3S)-3-(4-bromophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid; 4-[3-(3-Bromophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid; 4-[3-(4-Chlorophenyl)-4-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid; 3-[[3-(4-chlorophenyl)-4-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop2-enoyl]amino]acetyl]piperazin-1-yl]methyl]cyclobutane-1-carboxylic acid and both enantiomers thereof; 4-[3-(4-chlorophenyl)-4-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid and both enantiomers thereof; 4-[(2R,5S)-4-[2-[[(E)-3-[2-fluoro-4-(trifluorometil)feml]prop-2enoyl]amino] acetyl]-2-methyl-5-phenylpiperazin-1-yl]butanoic acid; 4-[(3S)-3-(4-cyclopropylphenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid; Acid 4-[3-(4-chloro-3-fluorophenyl)-4-[2-[[(E)-3-[2-fluoro-4Petition 870250102069, dated 07 / 11 / 2025, pág. 466 / 861 25 / 389 (trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid; 4-[(2R,5S)-5-(3,4-difluorophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]-2-methylpiperazin-1yl]butanoic acid; 4-[(2R,5S)-5-(3,4-difluorophenyl)-2-methyl-4-[2-[[(E)-3-[4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid; 4-[(2R,5S)-5-(4-chlorophenyl)-4-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop2-enoyl]amino]acetyl]-2-methylpiperazin-1-yl]butanoic acid; 3-[(2R,5S)-5-(4-chlorophenyl)-4-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop2-enoyl]amino]acetyl]-2-methylpiperazin-1-yl]propanoic acid; 4-[(2R,5S)-5-(4-chlorophenyl)—4—[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]-2-methylpiperazin-1yl]butanoic acid; 4-[(2R,5S)-5-(4-fluorophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]-2-methylpiperazin-1yl]butanoic acid; 3-[(2R,5S)-5-(4-chlorophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]-2-methylpiperazin-1yl]propanoic acid; 4-[(2R,5S)-5-(3-fluorophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]-2-methylpiperazin-1yl]butanoic acid; 4-[(2R,5S)-2-ethyl-4-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop2-enoyl]amino]acetyl]-5-phenylpiperazin-1-yl]butanoic acid; and Acid 4-[(2R,5S)-4-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2enoyl]amino] acetyl]-2-methyl-5-phenylpiperazine-1-yl]-2,2-dimethylbutanoe pharmaceutical mesamente salt.

[13] A selected compound from the group consisting of em Acid 2-[7-fluoro-2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Petition 870250102069, dated 07 / 11 / 2025, p. 467 / 861 26 / 389 Acid 2-[8-fluoro-2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid 2-[2-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid 2-[2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]- 3,4-d hydro-1H-isoquinolin-6-yl]propanoic; Acid 2-[2-[2-[[(E)-3-(4-iodophenyl)prop-2-enoyl]amino] acetyl]-3,4-di-hydro1H-isoquinolin-6-yl]acetic acid; Acid 2-[5-fluoro-2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid 2-[8-chloro-2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid 2-[8-fluoro-2-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2enoyl]amino]acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid 2-[8-chloro-2-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2enoyl]amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid 2-[7-chloro-2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid 2-[5-chloro-2-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2enoyl]amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; 4-[(3S)-4-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2enoyl]amino] acetyl]-3-phenylpiperazin-1-yl]butanoic acid; 1-[1-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2enoyl]amino]acetyl]piperidin-3-yl]biciclo[2.1.1]hexano-5-carboxylic acid; 4-[(3S)-3-(4-bromophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid; 4-[3-(3-bromophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid; 4-[3-(4-chlorophenyl)-4-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid; Petition 870250102069, 07 / 11 / 2025, pág. 468 / 861 27 / 389 4-[(2R,5S)-4-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2enoyl]amino]acetyl]-2-methyl-5-phenylpiperazin-1-yl]butanoic acid; 4-[(3S)-3-(4-cyclopropylphenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid; 4-[(2R,5S)-5-(3,4-difluorophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-2-methylpiperazin-1yl]butanoic acid; 4-[(2R,5S)-5-(3,4-difluorophenyl)-2-methyl-4-[2-[[(E)-3-[4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid; 4-[(2R,5S)-5-(4-chlorophenyl)-4-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop2-enoyl]amino]acetyl]-2-methylpiperazin-1-yl]butanoic acid; 3-[(2R,5S)-5-(4-chlorophenyl)-4-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop2-enoyl]amino]acetyl]-2-methylpiperazin-1-yl]propanoic acid; 4-[(2R,5S)-5-(4-chlorophenyl)—4—[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-2-methylpiperazin-1yl]butanoic acid; 4-[(2R,5S)-5-(4-fluorophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]-2-methylpiperazin-1yl]butanoic acid; 3-[(2R,5S)-5-(4-chlorophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]-2-methylpiperazin-1yl]propanoic acid; 4-[(2R,5S)-5-(3-fluorophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]-2-methylpiperazin-1yl]butanoic acid; 4-[(2R,5S)-2-ethyl-4-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop2-enoyl]amino]acetyl]-5-phenylpiperazin-1-yl]butanoic acid; and 4-[(2R,5S)-4-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]-2-methyl-5-phenylpiperazin-1-yl]-2,2-dimethylbutanoic acid, or a pharmaceutically acceptable salt thereof. Petition 870250102069, dated 07 / 11 / 2025, pp. 469 / 861 28 / 389

[14] A selected compound from the group consisting of Acid 2-[2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]- 3,4- di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid 3-[2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]- 3,4- dihydro-1H-isoquinolin-6-yl]propanoic; Acid N,N-dimethyl-3-[5-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2enoyl]amino] acetyl]-6,7-di-hydro-4H-pyrazolo[1,5-a]pyrazine-3yl]propanamide; Acid 2-[2-[2-[[(E)-3-3-[4-(pentafluoro-À6-sulfanyl)phenyl]prop-2-enoyl]amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid 2-[2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]- 3,4- dihydro-1H-isoquinolin-6-yl]propanoic; Acid 2-[8-fluoro-2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; 2-[2-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; 2-[8-chloro-2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-3,4-di-hidro-1H-isoquinolin-6-yl]acetic acid; Ácido 2-[8-cloro-2-[2-[[(E)-3-[2-fluoro-4-(trifluorometil)fenil]prop-2enoyl]amino] acetil]-3,4-di-hidro-1H-isoquinolin-6-il]acético; 4-[(3R)-3-(4-chlorophenyl)-4-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid; 4-[(2R,5S)-4-[2-[[(E)-3-[2-fluoro-4-(trifluorometil)feml]prop-2enoyl]amino] acetyl]-2-methyl-5-phenylpiperazin-1-yl]butanoic acid; 3-[(2R,5S)-5-(4-chloropheml)-4-[2-[[(E)-3-[4-(trifluoromethyl)feml]prop2-enoyl]amino] acetyl]-2-methylpiperazin-1-yl]propanoic acid; 3-[(2R,5S)-5-(4-chlorophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-2-methylpiperazin-1yl]propanoic acid; 4-[(2R,5S)-5-(3-fluorophenyl)-4-[2-[[(E)-3-[2-fluoro-4-]] Petition 870250102069, dated 07 / 11 / 2025, page 470 / 861 29 / 389 (trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]-2-methylpiperazin-1yl]butanoic acid; 4-[(2R,5S)-2-ethyl-4-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop2-enoyl]amino]acetyl]-5-phenylpiperazin-1-yl]butanoic acid; and 4-[(3S)-3-(4-cyclopropylphenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid, or a pharmaceutically acceptable salt thereof.

[0025]

[15] A B0AT1 inhibitor comprising a compound described in any of the [1] to

[14] , [3'] and [9'] above or a pharmaceutically acceptable salt thereof.

[0026] [15'] The B0AT1 inhibitor described in

[15] above, which is an agent for the prophylaxis and / or treatment of a disorder of amino acid metabolism.

[0027] [15''] The B0AT1 inhibitor described above [15'], in which the amino acid metabolism disorder is phenylketonuria, urea cycle disorder, hypertyrosinemia (types 1-3), hypermethioninemia, maple syrup urine disease, homocystinuria, nonketotic hyperglycinemia, propionic acidemia, methylmalonic acidemia or isovaleric acidemia.

[0028]

[16] A pharmaceutical composition comprising a compound described in any of the [1] to

[14] , [3'] and [9'] above or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.

[0029]

[17] The pharmaceutical composition described in

[16] above, for the prophylaxis and / or treatment of a disease whose symptoms can be relieved by the inhibitory action of B0AT1.

[0030]

[18] The pharmaceutical composition described in

[17] above, in which the disease whose symptoms can be relieved by the inhibitory action of B0AT1 is a disorder of amino acid metabolism. Petition 870250102069, dated 07 / 11 / 2025, pp. 471 / 861 30 / 389

[0031]

[19] The pharmaceutical composition described in

[18] above, in which the amino acid metabolism disorder is phenylketonuria, urea cycle disorder, hypertyrosinemia (types 1-3), hypermethioninemia, maple syrup urine disease, homocystinuria, nonketotic hyperglycinemia, propionic acidemia, methylmalonic acidemia or isovaleric acidemia.

[0032]

[20] The pharmaceutical composition described in

[18] above, in which the amino acid metabolism disorder is phenylketonuria.

[0033]

[21] The pharmaceutical composition described in any of the

[16] to

[20] mentioned above, which is administered in combination with another drug.

[0034]

[22] The pharmaceutical composition described in

[21] above, wherein the other drug is a B0AT1 inhibitor.

[0035]

[23] The pharmaceutical composition described in

[21] above, wherein the other drug is a vitamin, a drug to relieve various symptoms of amino acid metabolism disorders, an antidepressant, an anxiolytic drug or a therapeutic drug for ADHD.

[0036]

[24] The pharmaceutical composition of any of the

[21] a

[23] mentioned above, including a pharmaceutical composition of any of the

[16] to

[20] mentioned above and the other drugs are administered separately.

[0037]

[25] The pharmaceutical composition of any of the

[21] a

[23] mentioned above, in which the pharmaceutical composition in any of the

[16] to

[20] mentioned above and the other drugs are administered simultaneously or sequentially.

[0038]

[26] A method for the prophylaxis or treatment of a disorder of amino acid metabolism in a mammal, comprising administering an effective amount of a Petition 870250102069, dated 07 / 11 / 2025, pp. 472 / 861 31 / 389 compound described in any of the [1] to

[14] , [3'] and [9'] mentioned above or a pharmaceutically acceptable salt thereof to mammals.

[0039]

[27] A method for the prophylaxis or treatment of a selected disease from the group consisting of phenylketonuria, urea cycle disorder, hypertyrosinemia (types 1-3), hypermethioninemia, maple syrup urine disease, homocystinuria, nonketotic hyperglycinemia, propionic acidemia, methylmalonic acidemia and isovaleric acidemia in a mammal, comprising administering an effective amount of a compound described in any of the [1] to

[14] , [3'] and [9'] mentioned above or a pharmaceutically acceptable salt thereof to mammals.

[0040]

[28] A method for the prophylaxis or treatment of a disorder of amino acid metabolism in a mammal, comprising administering an effective amount of a pharmaceutical composition described in any of the

[16] to

[20] above and other drugs simultaneously or sequentially to the mammal.

[0041]

[29] A method for the prophylaxis or treatment of a selected disease from the group consisting of phenylketonuria, urea cycle disorder, hypertyrosinemia (types 1-3), hypermethioninemia, maple syrup urine disease, homocystinuria, nonketotic hyperglycinemia, propionic acidemia, methylmalonic acidemia and isovaleric acidemia in a mammal, comprising administering an effective amount of a pharmaceutical composition described in any of the

[16] to

[20] above mentioned and other drugs simultaneously or sequentially to the mammal.

[0042]

[30] Use of a compound described in any of the [1] to

[14] , [3'] and [9'] mentioned above or a pharmaceutically acceptable salt thereof in the production of a therapeutic agent or a prophylactic agent for a disorder of amino acid metabolism. Petition 870250102069, dated 07 / 11 / 2025, pp. 473 / 861 32 / 389

[0043]

[31] Use of a compound described in any of the [1] to

[14] , [3'] and [9'] mentioned above or a pharmaceutically acceptable salt thereof in the production of a therapeutic agent or a prophylactic agent for a disease selected from the group consisting of phenylketonuria, urea cycle disorder, hypertyrosinemia (types 13), hypermethioninemia, maple syrup urine disease, homocystinuria, nonketotic hyperglycinemia, propionic acidemia, methylmalonic acidemia and isovaleric acidemia.

[0044]

[32] A compound described in any of [1] to

[14] , [3'] and [9'] mentioned above or a pharmaceutically acceptable salt thereof for use in the prophylaxis or treatment of an amino acid metabolism disorder.

[0045]

[33] A compound described in any of [1] to

[14] , [3'] and [9'] mentioned above or a pharmaceutically acceptable salt thereof for use in the prophylaxis or treatment of a disease selected from the group consisting of phenylketonuria, urea cycle disorder, hypertyrosinemia (types 1-3), hypermethioninemia, maple syrup urine disease, homocystinuria, nonketotic hyperglycinemia, propionic acidemia, methylmalonic acidemia and isovaleric acidemia.

[0046]

[34] A method for producing a compound described in any of [1] to

[14] , [3'] and [9'] mentioned above or a pharmaceutically acceptable salt thereof.

[0047]

[35] A prodrug of a compound described in any of the [1] to

[14] , [3'] and [9'] above or a pharmaceutically acceptable salt thereof. ADVANTAGEOUS EFFECTS OF THE INVENTION

[0048] Compound (I) of the present invention, or a pharmaceutically acceptable salt thereof, has superior inhibitory activity against B0AT1. Therefore, a pharmaceutical composition containing said compound is useful for the treatment and / or prophylaxis of Petition 870250102069, dated 07 / 11 / 2025, pp. 474 / 861 33 / 389 diseases whose symptoms can be relieved by an inhibitory action of B0AT1. DESCRIPTION OF THE MODALITIES

[0049] The definitions of the terms and symbols used in this descriptive report are explained below.

[0050] In this descriptive report, "halogen atom" means a fluorine atom, a chlorine atom, a bromine atom, or an iodine atom.

[0051] In this descriptive report, the alkyl group means a monovalent linear or branched chain group with one or more carbon atoms, excluding a hydrogen atom from any carbon atom of an alkane. Although the number of carbon atoms is not particularly limited, it is a C1-20 alkyl group, preferably a C1-6 alkyl group.

[0052] In this descriptive report, the “C1-20 alkyl group” means an alkyl group with 1 to 20 carbon atoms and, for example, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, sec-butyl, tert-butyl, pentyl, isopentyl, neopentyl, 1-ethylpropyl, hexyl, isohexyl, 1,1-dimethylbutyl, 2,2-dimethylbutyl, 3,3-dimethylbutyl, 2-ethylbutyl, heptyl, octyl, nonyl, decyl, undecyl, dodecyl, tridecyl, eicosyl and the like may be mentioned.

[0053] In this descriptive report, the “C1-6 alkyl group” means an alkyl group with 1 to 6 carbon atoms and, for example, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, sec-butyl, tert-butyl, pentyl, isopentyl, neopentyl, sec-pentyl (pentan-2-yl), 3-pentyl (pentan-3-yl), tert-pentyl (1,1-dimethylpropyl), hexyl, isohexyl, 1,1-dimethylbutyl, 2,2-dimethylbutyl, 3,3-dimethylbutyl, 2-ethylbutyl and the like may be mentioned.

[0054] In this descriptive report, the “C1-4 alkyl group” means an alkyl group with 1 to 4 carbon atoms and, for example, Petition 870250102069, dated 07 / 11 / 2025, pp. 475 / 861 34 / 389 Methyl, ethyl, propyl, isopropyl, butyl, isobutyl, sec-butyl, tert-butyl and similar compounds may be mentioned.

[0055] In this descriptive report, the “C1-4 alkyl group” means an alkyl group with 1 to 4 carbon atoms and, for example, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, sec-butyl, tert-butyl and the like may be mentioned.

[0056] In this descriptive report, the “C1-6 alkyl group optionally substituted by halogen atom(s)” means the unsubstituted C1-6 alkyl group mentioned above, or a C1-6 alkyl group in which one or more (preferably 1 to 6, more preferably 1 to 3) hydrogen atoms in the C1-6 alkyl group mentioned above are substituted by halogen. Specifically, for example, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, pentyl, neopentyl, hexyl, fluoromethyl, difluoromethyl, trifluoromethyl, 2-chloroethyl, 2-bromoethyl, 2-iodoethyl, 2-fluoroethyl, 2,2-difluoroethyl, 2,2,2-trifluoroethyl, pentafluoroethyl, 2,2,3,3-tetrafluoropropyl, 3,3,3-trifluoropropyl, 4,4,4-trifluorobutyl, 5,5,5-trifluoropentyl, 6,6,6-trifluorohexyl and the like may be mentioned. Among these, a “C1-4 alkyl group optionally substituted by halogen atom(s)” is most preferred.

[0057] In this descriptive report, the “optionally substituted C1-6 alkyl group with substituent(s) selected from the group” means the aforementioned unsubstituted C1-6 alkyl group, or a C1-6 alkyl group in which one or more (preferably 1 to 6, more preferably 1 to 3) hydrogen atoms in the aforementioned C1-6 alkyl group are substituted with the same or a different substituent selected from the substituent group. Among these, an “optionally substituted C14 alkyl group with the same or a different substituent selected from the substituent group” is most preferred.

[0058] In the present description, the cycloalkyl group means a cyclic alkyl group. When the number of carbon atoms is not Petition 870250102069, dated 07 / 11 / 2025, pp. 476 / 861 35 / 389 particularly limited, this is preferably a C3-14 cycloalkyl group, more preferably a C3-8 cycloalkyl group.

[0059] In this descriptive report, the “C3-14 cycloalkyl group” means a cyclic alkyl group with 3 to 14 carbon atoms, which may be monocyclic, fused cyclic, spirocyclic and bridging cyclic. Specific examples of “C3-14 cycloalkyl groups” include monocyclic C3-14 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl and the like; fused cyclic C5-14 cycloalkyl, such as 1-decalynyl, 2-decalynyl and the like; spirocyclic C6-14 cycloalkyl, such as spiro[3,4]octyl, spiro[4,5]decyl, spiro[3,6]decyl and the like; bridged cyclic C5-14 cycloalkyl, such as bicyclo[1.1.1]pentyl, bicyclo[2.2.1]heptyl, bicyclo[2.2.2]octyl and the like, among others. Among these, a C3-8 cycloalkyl group is preferred.

[0060] In the present description, the C3-8 cycloalkyl group means a cyclic alkyl group with 3 to 8 carbon atoms, and may include, for example, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl and the like. Among these, a C36 cycloalkyl group is preferred.

[0061] In this descriptive report, the “optionally substituted C3-8 cycloalkyl group with substituent(s) selected from the group” means the unsubstituted C3-8 cycloalkyl group mentioned above or the C3-8 cycloalkyl group mentioned above in which one or more (preferably 1 to 6, more preferably 1 to 3) hydrogen atoms are substituted with the same or a different substituent selected from the substituent group.

[0062] In this descriptive report, the “C3-8 cycloalkyloxy group” means a group resulting from the linkage of the aforementioned C3-8 cycloalkyl group to an oxygen atom and specifically, for example, cyclopropyloxy, cyclobutyloxy, cyclopentyloxy, cyclohexyloxy, cycloheptyloxy, cyclooctyloxy and the like may be mentioned. Petition 870250102069, dated 07 / 11 / 2025, pp. 477 / 861 36 / 389

[0063] In this descriptive report, the “optionally substituted C3-8 cycloalkyloxy group with substituent(s) selected from the group” means the unsubstituted C3-8 cycloalkyloxy group mentioned above, or the C3-8 cycloalkyloxy group mentioned above in which one or more (preferably 1 to 6, more preferably 1 to 3) hydrogen atoms are substituted with the same or a different substituent selected from the substituent group.

[0064] In this descriptive report, the “C3-8 cycloalkylsulfanyl group” means a group resulting from the linkage of the aforementioned C38 cycloalkyl group to a sulfur atom and specifically, for example, cyclopropylsulfanyl, cyclobutylsulfanyl, cyclopentylsulfanyl, cyclohexylsulfanyl, cycloheptylsulfanyl, cyclooctylsulfanyl and the like may be mentioned.

[0065] In this descriptive report, “alkoxy (group)” means a group resulting from the attachment of a linear or branched chain alkyl group to an oxygen atom. Although the number of carbon atoms is not particularly limited, it is a C1-20 alkoxy group, preferably a C1-6 alkoxy group.

[0066] In the present description, the C1-6 alkoxy group means an alkoxy group with 1 to 6 carbon atoms, such as, for example, methoxy, ethoxy, propoxy, isopropoxy, butoxy, isobutoxy, sec-butoxy, tert-butoxy, pentyloxy, isopentyloxy, neopentyloxy, hexyloxy and the like. Among these, a C1-4 alkoxy group is preferred.

[0067] In this descriptive report, the “C1-6 alkoxy (group) optionally substituted by halogen atom(s)” is the unsubstituted C1-6 alkoxy group mentioned, or the C1-6 alkoxy group mentioned above in which one or more hydrogen atoms are substituted by halogen. Specifically, for example, methoxy, ethoxy, propoxy, isopropoxy, butoxy, pentyloxy, hexyloxy, fluoromethoxy, difluoromethoxy, trifluoromethoxy, 2-chloroethoxy, 2-bromoethoxy, 2-iodoethoxy, 2-fluoroethoxy, Petition 870250102069, dated 07 / 11 / 2025, pp. 478 / 861 37 / 389 2,2-difluoroethoxy, 2,2,2-trifluoroethoxy, pentafluoroethoxy, 2,2,3,3-tetrafluoropropoxy, 3,3,3-trifluoropropoxy, 4,4,4-trifluorobutoxy, 5,5,5-trifluoropentyloxy, 6,6,6-trifluorohexyloxy and the like may be mentioned. Among these, a “C1-4 alkoxy (group) optionally substituted by halogen atom(s)” is most preferred.

[0068] In this descriptive report, the “C1-6 alkoxy (group) optionally substituted by substituent(s) selected from the group” means the unsubstituted C1-6 alkoxy group mentioned above, or the C1-6 alkoxy group mentioned above in which one or more (preferably from 1 to 6, more preferably from 1 to 3) hydrogen atoms are substituted by the same substituent or by a different substituent selected from the group of substituents. Among these, a “C1-4 alkoxy (group) optionally substituted by the same or by a different substituent selected from the group” is more preferred.

[0069] In this descriptive report, the “alkylsulfanyl group” means a group resulting from the attachment of a straight or branched chain alkyl group to a sulfur atom, and a C1-6 alkylsulfanyl group is preferred.

[0070] In this descriptive report, the “C1-6 alkylsulfanyl group” means an alkylsulfanyl group with 1 to 6 carbon atoms and, for example, methylsulfanyl, ethylsulfanyl, propylsulfanyl, isopropylsulfanyl, butylsulfanyl, isobutylsulfanyl, c-butylsulfanyl, tert-butylsulfanyl, pentylsulfanyl, isopentylsulfanyl, neopentylsulfanyl, hexylsulfanyl and the like may be mentioned.

[0071] In this descriptive report, the “optionally substituted C1-6 alkylsulfanyl group with substituent(s) selected from the group” means the unsubstituted C1-6 alkylsulfanyl group mentioned above, or the C1-6 alkylsulfanyl group mentioned above in which one or more (preferably 1 to 6, more preferably 1 to 3) hydrogen atoms are substituted by the same or a different substituent. Petition 870250102069, dated 07 / 11 / 2025, pp. 479 / 861 38 / 389 selected from the replacement group.

[0072] In this descriptive report, the “C1-6 alkylsulfonyl group” means a group resulting from the linkage of the aforementioned “C1-6 alkyl” group to the sulfur atom of a sulfonyl group (-S(=O)2-), that is, a linear or branched chain alkylsulfonyl group with 1 to 6 carbon atoms. Examples of C1-6 alkylsulfonyl groups include methylsulfonyl, ethylsulfonyl, propylsulfonyl, isopropylsulfonyl, butylsulfonyl, isobutylsulfonyl, sec-butylsulfonyl, tert-butylsulfonyl, pentylsulfonyl, isopentylsulfonyl, neopentylsulfonyl, 1-ethylpropylsulfonyl, hexylsulfonyl, and similar groups.

[0073] In this descriptive report, the “C1-6 alkylsulfonyl group optionally substituted by halogen atom(s)” is the unsubstituted C1-6 alkylsulfonyl group mentioned, or the C1-6 alkylsulfonyl group mentioned in which one or more (preferably 1 to 6, more preferably 1 to 3) hydrogen atoms are substituted by halogen. Specifically, for example, methylsulfonyl, ethylsulfonyl, propylsulfonyl, butylsulfonyl, pentylsulfonyl, hexylsulfonyl, fluoromethylsulfonyl, difluoromethylsulfonyl, trifluoromethylsulfonyl, 2-chloroethylsulfonyl, 2-bromoethylsulfonyl, 2-iodoethylsulfonyl, 2-fluoroethylsulfonyl, 2,2-difluoroethylsulfonyl, 2,2,2-trifluoroethylsulfonyl, pentafluoroethylsulfonyl, 2,2,3,3-tetrafluoropropylsulfonyl, 3,3,3-trifluoropropylsulfonyl, 4,4,4-trifluorobutylsulfonyl, 5,5,5-trifluoropentylsulfonyl, 6,6,6-trifluorohexylsulfonyl and the like may be mentioned.

[0074] In this descriptive report, the “C1-6 alkylcarbonyl group” means a group in which the aforementioned C1-6 alkyl group is attached to a carbonyl group. Specifically, for example, acetyl, ethylcarbonyl, propylcarbonyl, butylcarbonyl, pentylcarbonyl, hexylcarbonyl and the like may be mentioned.

[0075] In this descriptive report, the “C1-6 alkyl-carbonyl group Petition 870250102069, dated 07 / 11 / 2025, pp. 480 / 861 39 / 389 optionally substituted by halogen atom(s)” is the unsubstituted C1-6 alkyl-carbonyl group mentioned above, or the C1-6 alkyl-carbonyl group mentioned above in which one or more (preferably 1 to 6, more preferably 1 to 3) hydrogen atoms are substituted by halogen. Specifically, for example, acetyl, ethylcarbonyl, propylcarbonyl, butylcarbonyl, pentylcarbonyl, hexylcarbonyl, fluoromethylcarbonyl, difluoromethylcarbonyl, trifluoromethylcarbonyl, 2-chloroethylcarbonyl, 2-bromoethylcarbonyl, 2-iodoethylcarbonyl, 2-fluoroethylcarbonyl, 2,2-difluoroethylcarbonyl, 2,2,2-trifluoroethylcarbonyl, pentafluoroethylcarbonyl, 2,2,3,3-tetrafluoropropylcarbonyl, 3,3,3-trifluoropropylcarbonyl, 4,4,4-trifluorobutylcarbonyl, 5,5,5-trifluoropentylcarbonyl, 6,6,6-trifluorohexylcarbonyl and similar compounds may be mentioned.

[0076] In this descriptive report, the “C1-6 alkoxycarbonyl group” means a group in which the aforementioned C1-6 alkoxy group is attached to a carbonyl group. Specifically, for example, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, butoxycarbonyl, pentyloxycarbonyl, hexyloxycarbonyl and the like may be mentioned.

[0077] In this descriptive report, the “optionally substituted carbamoyl group” means a group (mono- or disubstituted carbamoyl group) in which 1 or 2 hydrogen atoms of the carbamoyl group (-CONH2) are, each independently, optionally substituted by other substituents. The disubstituted carbamoyl group includes the 1-pyrrolidinylcarbonyl group and the 1-piperidylcarbonyl group.

[0078] In this descriptive report, the “carbamoyl group optionally substituted by 1 or 2 C1-6 alkyl groups optionally substituted by substituent(s) selected from the group consisting of a halogen atom, a hydroxyl group, a C1-6 alkylamino group Petition 870250102069, dated 07 / 11 / 2025, pp. 481 / 861 40 / 389 and a C1-6 alkoxy group” means a group in which 1 or 2 hydrogen atoms of the carbamoyl group (-CONH2) are each independently optionally substituted by 1 or 2 C1-6 alkyl groups optionally substituted by substituent(s) selected from the group consisting of a halogen atom, a hydroxyl group, a C1-6 alkylamino group and a C1-6 alkoxy group, and a C1-6 mono- or di-alkyl-carbamoyl group are preferred.

[0079] In this descriptive report, the “C2-6 alkenyl group” means a linear or branched monovalent group with 2 to 6 carbon atoms, in which a hydrogen atom is removed from any carbon atom of the C2-6 alkene. Specifically, for example, vinyl, 1-propenyl, allyl, isopropenyl, butenyl, 1-isobutenyl and the like may be mentioned.

[0080] In this descriptive report, the “C2-6 alkylnyl group” means a linear or branched monovalent group with 2 to 6 carbon atoms, in which a hydrogen atom is removed from any carbon atom of a C2-6 alkyl. Specifically, for example, ethinyl, propargyl, 3-butynyl, 2-butynyl, 2-pentynyl, 3-pentynyl, 4-pentynyl and the like may be mentioned.

[0081] In the present description, the aryl group means a monocyclic or polycyclic (fused) aromatic hydrocarbon group. Among these, the C6-14 aryl group is the most preferred, and the C6-10 aryl group is the most preferred.

[0082] In this descriptive report, the terms “C6-14 aryl group” may include phenyl, 1-naphthyl, 2-naphthyl, biphenyl, phenantrile, 2-antrile, fluorenyl and similar compounds.

[0083] In the present description, phenyl, 1-naphthyl and 2-naphthyl may be mentioned as C6-10 aryl groups. Of these, phenyl is preferred.

[0084] In the present description, the aryl-carbonyl group means a Petition 870250102069, dated 07 / 11 / 2025, pp. 482 / 861 41 / 389 group resulting from the bonding of the aforementioned aryl group to a carbonyl group.

[0085] Although the number of carbon atoms is not particularly limited, it is preferably a C6-14 arylcarbonyl group.

[0086] In the present description, the C6-14 aryloxy group means a group resulting from the attachment of the aforementioned C6-14 aryl group to an oxygen atom, and specifically, for example, phenyloxy, 1-naphthyloxy, 2-naphthyloxy, biphenyloxy, phenantriloxy, 2-antriloxy and the like may be mentioned. Among these, a C6-10 aryloxy group is preferred and a phenyloxy group is particularly preferred.

[0087] In this descriptive report, the “C6-14 group “hydrocarbocycle” means a monovalent aliphatic hydrocarbocycle, saturated or partially unsaturated (group) with 6 to 14 carbon atoms, or a monovalent aromatic hydrocarbocycle (group) with 6 to 14 carbon atoms.

[0088] In this descriptive report, the “C6-14 arylsulfonyl group” means a group resulting from the linkage of the aforementioned C6-14 aryl group to a sulfur atom of a sulfonyl group (-S(=O)2-) and, for example, phenylsulfonyl, 1-naphthylsulfonyl, 2-naphthylsulfonyl and the like may be mentioned.

[0089] In this descriptive report, the “C6-14 arylsulfonyloxy group” means a group resulting from the linkage of the aforementioned C6-14 aryl group to a sulfur atom of a sulfonyloxy group (-S(=O)2O-) and, for example, phenylsulfonyloxy, 1-naphthylsulfonyloxy, 2-naphthylsulfonyloxy and the like may be mentioned.

[0090] In this descriptive report, the aryl-ethenyl group means a group in which the terminal hydrogen atom of an ethenyl group (-CH=CH2) is replaced by the C6-10 aryl group mentioned above. Among these, the 2-phenylethenyl group is preferred, and the group Petition 870250102069, dated 07 / 11 / 2025, pp. 483 / 861 42 / 389 2-(E)-phenylenyl is particularly preferred.

[0091] In this descriptive report, “(E)” in the chemical formula of each example compound or “(E)-” in the compound name indicates that the double bond is in the E configuration.

[0092] In the present description, the C7-18 aralkyl group means a group resulting from the linkage of the C6-14 aryl group mentioned above to the C1-4 alkyl group mentioned above, and specifically, for example, benzyl, phenethyl, naphthylmethyl, biphenylmethyl and the like may be mentioned. Among these, a C7-10 aralkyl group is preferred, and a benzyl group is particularly preferred.

[0093] In this descriptive report, the C7-18 aralkyloxy group means a group resulting from the linkage of the aforementioned C7-18 aralkyl group to an oxygen atom, and specifically, for example, benzyloxy, phenethyloxy, naphthylmethyloxy, biphenylylmethyloxy and the like may be mentioned. Among these, a benzyloxy group is particularly preferred.

[0094] In this descriptive report, the acyl group means a formyl group, a linear or branched chain alkylcarbonyl group, or an arylcarbonyl group. Although the number of carbon atoms is not particularly limited, it is preferably a formyl group, a C1-6 alkylcarbonyl group, or a C6-14 arylcarbonyl group. Specific preferred examples of the acyl group include formyl, acetyl, propionyl, butyryl, isobutyryl, pentanoyl, tert-butylcarbonyl (pivaloyl), hexanoyl, heptanoyl, benzoyl, 1-naphthoyl, 2-naphthoyl, and the like.

[0095] In this descriptive report, the “acyloxy group” means a group resulting from the attachment of the aforementioned acyl group to an oxygen atom, and is preferably a C1-6 alkylcarbonyloxy group or a C6-14 arylcarbonyloxy group.

[0096] In this descriptive report, the “C1-6 dialkylamino” Petition 870250102069, dated 07 / 11 / 2025, pp. 484 / 861 43 / 389 means a group in which two hydrogen atoms of the amino group are replaced by the same or different C1-6 alkyl groups mentioned.

[0097] In this descriptive report, the “C1-6 alkylene group” means a divalent group in which a hydrogen atom is removed from the C1-6 alkyl group mentioned above. As a C1-6 alkylene group, specifically, for example, methylene, dimethylene, methylmethylene, dimethylmethylene, trimethylene, propane-1,2-di-yl, tetramethylene, pentamethylene, isopentane-2,4-di-yl, hexamethylene and the like may be mentioned.

[0098] In this descriptive report, the “C6-10 arylene group” means a divalent group in which a hydrogen atom is removed from the aforementioned “C6-10 aryl group”. Specifically, for example, 1,2-phenylene, 1,3-phenylene, 1,4-phenylene, 1,2-naphthylene, 1,3-naphthylene, 1,4-naphthylene, 2,6-naphthylene and the like may be mentioned as C6-10 arylene groups.

[0099] In this descriptive report, the “C2-6 alkenylene group” means a divalent group in which a hydrogen atom is removed from the aforementioned “C2-6 alkenyl group”. Among them, the C2-3 alkenylene is preferred. As the C2-3 alkenylene group, specifically, for example, ethenylene (-CH=CH-), propenylene (-CH=CHCH2-) and the like may be mentioned.

[00100] In this descriptive report, the “C2-6 alkynylene group” means a divalent group in which a hydrogen atom is removed from the aforementioned “C2-6 alkynyl group”. Among them, the C2-3 alkynylene is preferred. As C2-3 alkynylene groups, specifically, for example, ethynylene (-C^C-), propynylene (-C^C-CH-) and the like may be mentioned.

[00101] In this descriptive report, the “C3-14 cycloalkylene group” means a divalent group in which a hydrogen atom is removed. Petition 870250102069, dated 07 / 11 / 2025, pp. 485 / 861 44 / 389 of the aforementioned “C3-14 cycloalkyl group”. Among them, C3-8 cycloalkylene is preferred. As C3-8 cycloalkylene groups may be mentioned, specifically, for example, cyclopropane-1,1-di-yl, cyclopropane-1,2-di-yl, cyclobutane-1,3-di-yl, bicyclo[2.1.1]hexane-1,2di-yl, bicyclo[1.1.1]pentane-1,3-di-yl and the like.

[00102] In this descriptive report, the 3- to 14-membered divalent non-aromatic heterocycle group means a divalent group in which a hydrogen atom is removed from the 3- to 14-membered non-aromatic heterocycle group mentioned below. Among them, the 3- to 8-membered divalent non-aromatic heterocycle is preferred. As the 3- to 8-membered divalent non-aromatic heterocycle group, specifically, for example, aziridine-1,2-di-yl, oxetano-2,4-di-yl, azetidine-1,3-di-yl, pyrrolidine-1,3-di-yl, piperidine-1,2-di-yl, piperidine-1,3-di-yl, piperidine-1,4-di-yl and the like may be mentioned.

[00103] In this descriptive report, the “divalent organic group including a C1-6 alkylene group, a C6-10 arylene group, a C314 cycloalkylene group, a C2-6 alkenylene group, a C2-6 alkynylene group or a divalent non-aromatic heterocyclic group of 3 to 14 members” means a divalent group having the aforementioned “C1-6 alkylene group, C6-10 arylene group, C3-14 cycloalkylene group, C2-6 alkenylene group, C2-6 alkynylene group or divalent non-aromatic heterocyclic group of 3 to 14 members” and the portion other than the “C1-6 alkylene group, C6-10 arylene group, C3-14 cycloalkylene group, C2-6 alkenylene group, C26 alkynylene group or divalent non-aromatic heterocyclic group of 3 to 14 members” "14 members".A 14-membered divalent non-aromatic heterocyclic group” in the “organic group with a C1-6 alkylene group, a C6-10 arylene group, a C3-14 cycloalkylene group, a C2-6 alkenylene group, a C2-6 alkynylene group, or a 3- to 14-membered divalent non-aromatic heterocyclic group can be determined. Reference examples of the “divalent organic group including a C1-6 group. Petition 870250102069, dated 07 / 11 / 2025, pp. 486 / 861 45 / 389 alkylene, a Ce-10 arylene group, a C3-14 cycloalkylene group, a C2-e alkenylene group, a C2-e alkynylene group or a divalent non-aromatic heterocyclic group of 3 to 14 members” include a C1-e alkylene group, a Ce-10 arylene group, a C3-14 cycloalkylene group, a C2-e alkenylene group, a C2-e alkynylene group or a divalent non-aromatic heterocyclic group of 3 to 14 members, each of which optionally has, in the interior or at the end, one or more divalent groups selected from the group consisting of -NR2- (where R2 is a hydrogen atom or a C1-e alkyl group), -O-, -S-, -C(=O)-, a C1-e alkylene group, a Ce-10 arylene group, a group C3-14 cycloalkylene, a C2-e alkenylene group, a C2-e alkynylene group, and a divalent non-aromatic heterocyclic group of 3 to 14 members, each of which is optionally substituted by 1 to 3 substituents selected from the aforementioned substituent group.Here, the two bonds of the divalent (organic) group can originate from the same carbon atom or from different carbon atoms in the (organic) group, or from the heteroatom that constitutes the (organic) group. In this descriptive report, the “C3-10 cycloalkylene group”, “C2-4 alkenylene group” and “C2-4 alkynylene group” are respectively the same as the “C3-14 cycloalkylene group”, “C2-e alkenylene group” and “C2-e alkynylene group” mentioned above, except that the carbon number range is different.

[00104] In the present descriptive report, the “heterocycle (group)” is (i) an aromatic heterocyclic group or (ii) a non-aromatic heterocyclic group, each of which contains from 1 to 4 heteroatoms selected from a nitrogen atom, a sulfur atom and an oxygen atom as a ring constituent atom, in addition to the carbon atom, and (i) an included aromatic heterocyclic group is a 5- or 8-membered monocyclic aromatic heterocyclic group and a fused aromatic heterocyclic group of 8 to 14 members, and (ii) a non-aromatic heterocyclic group Petition 870250102069, dated 07 / 11 / 2025, pp. 487 / 861 46 / 389 aromatic included non-aromatic monocyclic heterocyclic groups of 3 to 10 members, fused non-aromatic heterocyclic groups of 9 to 14 members, bridging non-aromatic heterocyclic groups of 6 to 14 members, and spirocyclic non-aromatic heterocyclic groups of 6 to 16 members.

[00105] In this descriptive report, the term “aromatic heterocyclic group” may refer to an aromatic heterocyclic group of 5 to 14 members containing 1 to 4 heteroatoms selected from among a nitrogen atom, a sulfur atom, and an oxygen atom as ring constituent atoms, in addition to the carbon atom.

[00106] Preferred examples of “aromatic heterocyclic groups” include 5- or 6-membered monocyclic aromatic heterocyclic groups, such as thienyl, furyl, pyrrolyl, imidazolyl, pyrazolyl, thiazolyl, isothiazolyl, oxazolyl, isoxazolyl, pyridyl, pyrazinyl, pyrimidinyl, pyridazinyl, 1,2,4-oxadiazolyl, 1,3,4-oxadiazolyl, 1,2,4-thiadiazolyl, 1,3,4-thiadiazolyl, triazolyl, tetrazolyl, triazinyl and the like; and Fused aromatic heterocyclic groups of 8 to 14 members (fused polycyclic aromatic heterocyclic groups (preferably bi- or tricyclic)), such as benzothiophenyl, benzofuranyl, benzoimidazolyl, benzoxazolyl, benzisoxazolyl, benzothiazolyl, benzisothiazolyl, benzotriazolyl, imidazopyridyl, thienopyridyl, furopyridyl, pyrrolopyridyl, pyrazolopyridyl, oxazolopyridyl, thiazolopyridyl, imidazopyrazinyl, imidazopyrimidinyl, thienopyrimidinyl, furopyrimidinyl, pyrrolopyrimidinyl, pyrazolopyrimidinyl, oxazolopyrimidinyl, thiazolopyrimidinyl, pyrazolotriazinyl, naphtho[2,3b]thienyl, fenoxati-inyl, indolyl, isoindolyl, 1H-indazolyl, purinyl, isoquinolyl, quinolyl, phthalazinyl, naphthyridinyl, quinoxalinyl, quinazolinyl, cinolinyl, carbazolyl, β-carbolinyl, phenanthridinyl, acridinyl, phenazinyl, phenothiazinyl, phenoxazinyl and the like.

[00107] No descriptive report, such as “heterocyclic group” Petition 870250102069, dated 07 / 11 / 2025, pp. 488 / 861 47 / 389 non-aromatic”, a non-aromatic heterocyclic group of 3 to 14 members containing 1 to 4 heteroatoms selected from among a nitrogen atom, a sulfur atom and an oxygen atom as ring constituent atoms, in addition to the carbon atom, can be mentioned.

[00108] Preferred examples of “non-aromatic heterocyclic groups” include 3- to 10-membered monocyclic non-aromatic heterocyclic groups (preferably 5- to 8-membered monocyclic non-aromatic heterocyclic groups), such as aziridinyl, oxiranyl, thiiranyl, azetidinyl, oxetanyl, thietanyl, tetrahydrothienyl, tetrahydrofuryl, pyrrolinyl, pyrrolidinyl, imidazolinyl, imidazolidinyl, oxazolinyl, oxazolidinyl, pyrazolinyl, pyrazolidinyl, thiazolinyl, thiazolidinyl, tetrahydroisothiazolyl, tetrahydrooxazolyl, tetrahydroisoxazolyl, piperidyl, piperazinyl, tetrahydropyridyl, dihydropyridyl, dihydrothiopyranyl, tetrahydropyrimidinyl, tetrahydropyridazinyl, dihydropyranyl, tetrahydropyranyl, tetrahydrothiopyranyl, morpholinyl, thiomorpholinyl, azepanil, diazepanil, azepinyl, oxepanil, azocanyl, diazocanil and the like;and fused non-aromatic heterocyclic groups of 8 to 14 members (fused polycyclic non-aromatic heterocyclic groups (preferably bicyclic)), such as tetra-hydrotriazolopyridyl, tetrahydrotriazolopyrazinyl, tetra-hydropyrazolopyrazinyl, dihydropyrazolopyrrolyl, di-hydropyrazolopyrazinyl, tetrahydropyrazolopyridyl, tetra-hydroimidazolopyridyl, dihydroimidazolopyridyl, di-hydroimidazolopyridyl, tetrahydroimidazolopyrazinyl, di-hydropyrimidopyrrolyl, di-hydropyridopyrrolyl, tetra-hydropyridopyridyl, tetra-hydro-oxazolopyrazinyl, tetrahydropyridopyridyl, tetra-hydrotriazolodiazepinyl, octa-hydro-1,4-oxazinopyrazinyl, dihydrobenzofuranyl, di-hydrobenzimidazolyl, dihydrobenzoxazolyl, di-hydrobenzothiazolyl, di-hydrobenzisothiazolyl, dihydronaphtho[2,3-b]thienyl, tetra-hydroisoquinolyl, di-hydroisoquinolyl, tetraPetição 870250102069, dated 07 / 11 / 2025, p. 489 / 861; 48 / 389 hydroquinolile, 4H-quinolizine, indolinyl, isoindolinyl, tetrahydrothiene[2,3-c]pyridyl, dihydrothiazolo[4,5-c]pyridyl, dihydrothiazolo[5,4-c]pyridyl, tetrahydrobenzoazepinyl, tetrahydroquinoxalinyl, tetrahydrophenanthridinyl, hexahydrophenothiazinyl, hexahydrophenoxazinyl, tetrahydrophthalazinyl, tetrahydronaphthiridinyl, dihydronaphthiridinyl, tetrahydroquinazoliniyl, tetrahydrocinolinyl, tetrahydrocarbazolyl, tetrahydro-βcarboliniyl, tetrahydroacridiniyl, tetrahydrophenazinyl, tetrahydrothioxanthenyl, octahydroisoquinolilyl and the like.

[00109] More preferred examples of “heterocyclic non-aromatic group” include pyrrolidinyl, piperidyl, tetra-hidrotriazolopyrazinyl (for example, 5,6,7,8-tetra-hidro-[1,2,4]triazolo[4,3-a]pirazinyl, 5,6,7,8tetra-hidro-[1,2,4]triazolo[1,5-a]pirazinyl), tetra-hydropyrazolopyrazinyl (for example, e.g., 4,5,6,7-tetra-hidropyrazolo[1,5-a]pirazinila), tetrahydroisoquinolila (for e.g., 1,2,3,4-tetra-hidroisoquinolila), tetrahydronaftiridinila (for e.g., 5,6,7,8-tetra-hidro-1,6-naftiridinila, 1,2,3,4-tetra-hidro-2,6-naftiridinila, 1,2,3,4-tetra-hidro-2,7-naftiridinila), di-hidropirazolopirazinila (por example, di-hidro-4H-pirazolo[1,5a]pirazinila), di-hidronaftiridinila (por example, 6,8-di-hidro-5H-2,7naftiridinila), di-hidroisoquinolila (por example, 3,4-di-hidro-1Hisoquinolila), di-hidrotiazol [5,4-c]piridila (por example, 6,7-di-hidro-4H[1,3]tiazol[5,4-c]piridila), di-hidrotiazol [4,5-c]pyridyl (for example, 6,7-dihidro-4H-[1,3]thiazol[4,5-c]pyridyl), indolinyl (for example, 2,3-dihydroindolyl) and the like.,

[00110] Other preferable examples of “non-aromatic heterocyclic groups” include cyclic non-aromatic heterocyclic groups of 6 to 14 members in bridging configuration, such as 3,8-diazabicyclo[3.2.1]octyl, 2,5-diazabicyclo[2.2.2]octyl, 7-azabicyclo[2.2.1]heptanil, quinuclidinyl and the like; and spirocyclic non-aromatic heterocyclic groups of 6 to 16 members, such as 2,8-diazaspiro[4.5]decyl, 2,7-diazaspiro[3.5]nonyl, 2,6-diazaspiro[3.3]heptyl and the like. Petition 870250102069, dated 07 / 11 / 2025, pp. 490 / 861 49 / 389

[00111] In this descriptive report, the term "nitrogen-containing heterocyclic group" may refer to both nitrogen-containing aromatic heterocyclic groups and nitrogen-containing non-aromatic heterocyclic groups.

[00112] In this descriptive report, the “nitrogen-containing aromatic heterocyclic group” or “nitrogen-containing non-aromatic heterocyclic group” means the aforementioned aromatic heterocyclic group or non-aromatic heterocyclic group that has at least one nitrogen atom as a ring constituent atom.

[00113] In this descriptive report, the “divalent nitrogen-containing aromatic heterocyclic group” means a divalent group in which a hydrogen atom has been removed from the aforementioned “nitrogen-containing aromatic heterocyclic group”.

[00114] In this descriptive report, the “non-aromatic heterocyclic group containing divalent nitrogen” means a divalent group in which a hydrogen atom is removed from the aforementioned “non-aromatic heterocyclic group containing nitrogen”.

[00115] In this descriptive report, being “optionally additionally replaced by 1 to 3 substituents selected from substituent group a (or substituent group b)” means that, in addition to the two bonds in the divalent group, 1 to 3 hydrogen atoms are each independently optionally additionally replaced by 1 to 3 substituents selected from substituent group a (or substituent group b). When substituent group a' (or substituent group b') is adopted instead of substituent group a, this definition applies similarly by replacing substituent group a (or substituent group b) with substituent group a' (or substituent group b').

[00116] In this descriptive report, trisubstituted silyl group means a silyl group substituted by the same or by three different substituents (e.g., C1-6 alkyl group, C1-10 aryl group, etc.). Petition 870250102069, dated 07 / 11 / 2025, pp. 491 / 861 50 / 389 Examples of these include trialkylsilyl groups, such as trimethylsilyl group, triethylsilyl group, tri-isopropylsilyl group, tert-butyldimethylsilyl group and the like (preferably, C1-6 trialkylsilyl group), tert-butyldiphenylsilyl group, triphenylsilyl group and the like.

[00117] In this descriptive report, the “trisubstituted silylox group” means a group in which a trisubstituted silyl group is bonded to an oxygen atom. Examples of these include trialkylsilyloxy groups, such as trimethylsilyloxy groups, triethylsilyloxy groups, triisopropylsilyloxy groups, tert-butyldimethylsilyloxy groups and the like (preferably, C1-6 trialkylsilyloxy groups), tert-butyldiphenylsilyloxy groups, triphenylsilyloxy groups and the like.

[00118] In this descriptive report, a biologically equivalent group means a functional group that exhibits broadly similar biological effects and possesses chemical and physical similarities, as proposed by Thornberg in 1979 in the area of ​​drug discovery chemistry. Examples of a biologically equivalent group to a carboxyl group include the optionally substituted C1-6 alkoxycarbonyl group, the optionally substituted carbamoyl group, the cyano group, and the selected group consisting of the following formulas: Petition 870250102069, dated 07 / 11 / 2025, pp. 492 / 861 51 / 389 where a wavy line is a binding site of the group represented by the chemical formula mentioned above, and * shows a binding position with L, tautomeric groups thereof, or similar. Among these, the optionally substituted C1-alkoxycarbonyl group or the optionally substituted carbamoyl group is preferred.

[00119] In this descriptive report, optionally substituted means not substituted or substituted by a specific substituent at any substituteable position (any hydrogen atom is substituted by a substituent). The substituent is not particularly limited and may be a substituent selected from the following: (Substituent group a), (Substituent group a'), (Substituent group b) and (Substituent group b'). When the substituent group is not Petition 870250102069, dated 07 / 11 / 2025, pp. 493 / 861 52 / 389, as specifically specified, means optionally being replaced by one or more substituents selected from the following: (substituent group c) or (substituent group c'). Although the number of substituents is not particularly limited, provided it is a replaceable number, it is generally from 1 to 5, preferably from 1 to 3. When multiple substituents are present, the respective substituents may be the same or different. (Replacement Group a): a halogen atom; a hydroxyl group; a cyan group; an oxo group; a C1-6 alkyl group optionally substituted by substituents selected from the group consisting of a halogen atom, a hydroxyl group, a cyano group, a C1-6 alkoxy, a C6-14 aryl group, a carboxy group, a C1-6 alkoxy-carbonyl group, a carbamoyl group optionally substituted by 1 or 2 C1-6 alkyl groups, and a C6-14 aryloxy group; an optionally substituted C1-6 alkoxy with halogen atoms; a C1-6 alkylsulfonyl group optionally substituted with halogen atoms; a C1-6 alkyl-carbonyl group; a C1-6 alkoxy-carbonyl group; a carbamoyl group optionally substituted by 1 or 2 C1-6 alkyl groups optionally substituted by substituents selected from the group consisting of a halogen atom, a hydroxyl group, a di-C1-6 alkylamino group, and a C1-6 alkoxy group; a di-C1-6 alkylamino group; a trisubstituted silyl group; Petition 870250102069, dated 07 / 11 / 2025, pp. 494 / 861 53 / 389 a trisubstituted silyl oxy group; a C6-14 hydrocarbocyclic group optionally substituted by 1 to 3 substituents selected from substituent group b or substituent group b'; an aromatic heterocyclic group of 5 to 14 members optionally substituted by 1 to 3 substituents selected from substituent group b or substituent group b'; and a non-aromatic heterocyclic group of 3 to 14 members optionally substituted by 1 to 3 substituents selected from substituent group b or substituent group b' (Substituent Group a'): a halogen atom; a hydroxyl group; a cyan group; an oxo group; a C1-6 alkyl group optionally substituted by substituents selected from the group consisting of a halogen atom, a hydroxyl group, a cyano group, a C1-6 alkoxy, a C6-14 aryl group, and a C6-14 aryloxy group; an optionally substituted C1-6 alkoxy with halogen atoms; a C1-6 alkylsulfonyl group optionally substituted with halogen atoms; a C1-6 alkyl-carbonyl group; a C1-6 alkoxy-carbonyl group; carbamoyl group optionally substituted by 1 or 2 C1-6 alkyl groups optionally substituted by substituents selected from the group consisting of a halogen atom, a hydroxyl group, a di-C1-6 alkylamino group, and a C1-6 alkoxy group; a di-C1-6 alkylamino group; Petition 870250102069, dated 07 / 11 / 2025, pp. 495 / 861 54 / 389 a trisubstituted silyl group; a trisubstituted silyl oxy group; a C6-14 hydrocarbocyclic group optionally substituted by 1 to 3 substituents selected from substituent group b or substituent group b'; an aromatic heterocyclic group of 5 to 14 members optionally substituted by 1 to 3 substituents selected from substituent group b or substituent group b'; and a non-aromatic heterocyclic group of 3 to 14 members optionally substituted by 1 to 3 substituents selected from substituent group b or substituent group b'. (Substituent Group b): a halogen atom; a hydroxyl group; a cyan group; an oxo group; a carboxy group; a C1-6 alkyl group optionally substituted by substituents selected from the group consisting of a halogen atom, a hydroxyl group, a cyano group, and a C1-6 alkoxy; a C3-8 cycloalkyl group optionally substituted by substituents selected from the group consisting of a halogen atom, a hydroxyl group, a cyano group, and a C1-6 alkoxy; an optionally substituted C6-10 aryl group with substituents selected from the group consisting of a halogen atom, a hydroxyl group, a cyano group, a C1-6 alkyl group, and a C1-6 alkoxy group; an aromatic heterocyclic group of 5 to 14 members optionally substituted with substituents selected from the group consisting of a halogen atom, a hydroxyl group, a cyano group, Petition 870250102069, dated 07 / 11 / 2025, pp. 496 / 861 55 / 389 a C1-6 alkyl group, and a C1-6 alkoxy group; a non-aromatic heterocyclic group of 3 to 14 members optionally substituted with substituents selected from the group consisting of a halogen atom, a hydroxyl group, a cyano group, a C1-6 alkyl group, and a C1-6 alkoxy group; a C1-6 alkoxy optionally substituted by substituents selected from the group consisting of a halogen atom, a hydroxyl group, a cyano group, and a C1-6 alkoxy; a C1-6 alkylsulfonyl group optionally substituted by substituents selected from the group consisting of a halogen atom, a hydroxyl group, a cyano group, and a C1-6 alkoxy; a C3-8 cycloalkyloxy group optionally substituted by substituents selected from the group consisting of a halogen atom, a hydroxyl group, a cyano group, and a C1-6 alkoxy; a C1-6 alkylsulfonyl group optionally substituted with halogen atoms; a C1-6 alkyl-carbonyl group optionally substituted with halogen atoms; a C1-6 alkoxy-carbonyl group; a carbamoyl group optionally substituted by 1 or 2 C1-6 alkyl groups optionally substituted by substituents selected from the group consisting of a halogen atom, a hydroxyl group, a di-C1-6 alkylamino group, and a C1-6 alkoxy group; a sulfamoyl group substituted by a substituent selected from the group consisting of a C1-6 alkyl group, a C3-8 cycloalkyl group, and a non-aromatic heterocyclic group, each of which is optionally substituted by 1 to 3 substituents selected from the group consisting of a halogen atom, a hydroxyl group, a cyano group, and a C1-6 alkoxy group; and a pentafluorosulfanyl group. Petition 870250102069, dated 07 / 11 / 2025, pp. 497 / 861 56 / 389 (Substituent Group b'): a halogen atom; a hydroxyl group; a cyan group; an oxo group; a carboxy group; a C1-6 alkyl group optionally substituted by substituents selected from the group consisting of a halogen atom, a hydroxyl group, a cyano group, and a C1-6 alkoxy; a C3-8 cycloalkyl group optionally substituted by substituents selected from the group consisting of a halogen atom, a hydroxyl group, a cyano group, and a C1-6 alkoxy; a C1-6 alkoxy optionally substituted by substituents selected from the group consisting of a halogen atom, a hydroxyl group, a cyano group, and a C1-6 alkoxy; a C1-6 alkylsulfonyl group optionally substituted by substituents selected from the group consisting of a halogen atom, a hydroxyl group, a cyano group, and a C1-6 alkoxy; a C3-8 cycloalkyloxy group optionally substituted by substituents selected from the group consisting of a halogen atom, a hydroxyl group, a cyano group, and a C1-6 alkoxy; a C1-6 alkylsulfonyl group optionally substituted with halogen atoms; a C1-6 alkyl-carbonyl group optionally substituted with halogen atoms; a C1-6 alkoxy-carbonyl group; a carbamoyl group optionally substituted by 1 or 2 C1-6 alkyl groups optionally substituted by substituents selected from the group consisting of a halogen atom, a hydroxyl group, a di-C1-6 alkylamino group, and a C1-6 alkoxy group; Petition 870250102069, dated 07 / 11 / 2025, pp. 498 / 861 57 / 389 a sulfamoyl group substituted by a substituent selected from the group consisting of a C1-6 alkyl group, a C3-8 cycloalkyl group and a non-aromatic heterocyclic group, each of which is optionally substituted by 1 to 3 substituents selected from the group consisting of a halogen atom, a hydroxyl group, a cyano group, and a C1-6 alkoxy group; and a pentafluorosulfanyl group. (Substituent Group c): a halogen atom; a hydroxyl group; a carboxy group; a nitro group; a cyan group; an amino group optionally substituted by one or two substituents selected from the group consisting of a C1-6 alkyl group and a C1-6 alkoxy-carbonyl group; a C1-6 alkyl group optionally substituted by 1 to 3 substituents selected from substituent group a or substituent group a'; an optionally substituted C1-6 alkoxy with 1 to 3 substituents selected from the substituent group a or substituent group a'; a C1-6 alkoxy-carbonyl group; a C1-6 alkylsulfonyl group optionally substituted by 1 to 3 substituents selected from the substituent group a or substituent group a'; a C3-8 cycloalkyl group optionally substituted by 1 to 3 substituents selected from substituent group a or substituent group a'; an acyl group optionally replaced by 1 to 3 Petition 870250102069, dated 07 / 11 / 2025, pp. 499 / 861 58 / 389 selected substituents from substituent group a or substituent group a'; an acyloxy group optionally substituted by 1 to 3 substituents selected from substituent group a or substituent group a'; an optional C6-14 aryl group replaced by 1 to 3 substituents selected from substituent group b; an optionally substituted C6-14 aryloxy group with 1 to 3 substituents selected from substituent group b; a C6-14 arylsulfonyl optionally substituted by 1 to 3 substituents selected from substituent group b; an optionally substituted C6-14 arylsulfonyloxy group with 1 to 3 substituents selected from substituent group b; a C7-18aralkyl group optionally substituted by 1 to 3 substituents selected from substituent group b; a C7-18 aralkyloxy group optionally substituted by 1 to 3 substituents selected from substituent group b; a carbamoyl group optionally substituted by 1 or 2 C1-6 alkyl groups optionally substituted by substituents selected from the group consisting of a hydroxy group, a diC1-6 alkylamino group, and a C1-6 alkoxy group; a carbamoyloxy group optionally substituted by 1 or 2 C1-6 alkyl groups optionally substituted by substituents selected from the group consisting of a hydroxy group, a diC1-6 alkylamino group, and a C1-6 alkoxy group; an oxo group; a tioxo group; a mono- or di-C1-6 alkylamino group; an azide group; a trisubstituted silyl group; Petition 870250102069, dated 07 / 11 / 2025, pp. 500 / 861 59 / 389 a trisubstituted silyloxy group; an aromatic heterocycle optionally substituted by 1 to 3 substituents selected from substituent group b; and a non-aromatic heterocycle optionally substituted by 1 to 3 substituents selected from substituent group b. (Substituent Group c'): a halogen atom; a hydroxyl group; a carboxy group; a nitro group; a cyan group; an amino group optionally substituted by one or two substituents selected from the group consisting of a C1-6 alkyl group and a C1-6 alkoxy-carbonyl group; a C1-6 alkyl group optionally substituted by 1 to 3 substituents selected from substituent group a or substituent group a'; an optionally substituted C1-6 alkoxy with 1 to 3 substituents selected from the substituent group a or substituent group a'; a C1-6 alkoxy-carbonyl group; a C1-6 alkylsulfonyl group optionally substituted by 1 to 3 substituents selected from the substituent group a or substituent group a'; a C3-8 cycloalkyl group optionally substituted by 1 to 3 substituents selected from substituent group a or substituent group a'; an acyl group optionally replaced by 1 to 3 substituents selected from substituent group a or substituent group a'; Petition 870250102069, dated 07 / 11 / 2025, pp. 501 / 861 60 / 389 an acyloxy group optionally substituted by 1 to 3 substituents selected from substituent group a or substituent group a'; C6-14 aryl group optionally replaced by 1 to 3 substituents selected from substituent group b; an optionally substituted C6-14 aryloxy group with 1 to 3 substituents selected from the b' substituent group; an optionally substituted C6-14 arylsulfonyl group with 1 to 3 substituents selected from the b' substituent group; an optionally substituted C6-14 arylsulfonyloxy group with 1 to 3 substituents selected from the b' substituent group; a C7-18aralkyl group optionally substituted by 1 to 3 substituents selected from substituent group b'; a C7-18 aralkyloxy group optionally substituted by 1 to 3 substituents selected from the b' substituent group; a carbamoyl group optionally substituted by 1 or 2 C1-6 alkyl groups optionally substituted by substituents selected from the group consisting of a hydroxy group, a diC1-6 alkylamino group, and a C1-6 alkoxy group; a carbamoyloxy group optionally substituted by 1 or 2 C1-6 alkyl groups optionally substituted by substituents selected from the group consisting of a hydroxy group, a diC1-6 alkylamino group, and a C1-6 alkoxy group; an oxo group; a tioxo group; a mono- or di-C1-6 alkylamino group; an azide group; a trisubstituted silyl group; a trisubstituted silyloxy group; an aromatic heterocycle optionally substituted by 1 Petition 870250102069, dated 07 / 11 / 2025, pp. 502 / 861 61 / 389 to 3 substituents selected from substituent group b'; and a non-aromatic heterocyclic group optionally substituted by 1 to 3 substituents selected from substituent group b'.

[00120] In the present description, the pharmaceutically acceptable salt thereof means a salt that can be used as a drug. When compound (I) of the present invention has an acidic group or a basic group, it indicates a basic salt or an acidic salt that can be obtained by reaction with a base or an acid. A water-soluble salt is preferred.

[00121] Examples of the pharmaceutically acceptable basic salt of compound (I) of the present invention include alkali metal salts, such as sodium salt, potassium salt, lithium salt and the like; alkaline earth metal salts, such as magnesium salt, calcium salt and the like; ammonium salts, such as ammonium salt, tetramethylammonium salt and the like; organic-based salts, such as N-methylmorpholine salt, triethylamine salt, tributylamine salt, diisopropylethylamine salt, dicyclohexylamine salt, N-methylpiperidinium salt, pyridinium salt, 4-pyrrolidinopyridinium salt, picolinium salt and the like; basic amino acid salts, such as lysine salt, arginine salt and the like. Preferably, it is an alkali metal salt (particularly sodium salt or potassium salt) or a basic amino acid salt.

[00122] Examples of pharmaceutically acceptable acid salts of compound (I) of the present invention include salts of inorganic acids, such as hydrohalides (e.g., fluoride, hydrochloride, hydrobromide, iodide and the like), nitride, perchloride, sulfate, phosphate and the like; salts of organic acids, such as lower alkanesulfonates (e.g., methanesulfonate, trifluoromethanesulfonate, ethanesulfonate and the like), arylsulfonates (e.g., benzenesulfonate, ptoluenesulfonate and the like), acetate, malate, fumarate, succinate, citrate, ascorbate, tartrate, oxalate, maleate and the like. A hydro Petition 870250102069, dated 07 / 11 / 2025, pp. 503 / 861 62 / 389 halide (particularly hydrochloride) is preferred.

[00123] In this descriptive report, “salt of the same” means all salts, including the “pharmaceutically acceptable salt of the same” mentioned above.

[00124] In this descriptive report, prophylaxis includes prevention of disease onset, delay of disease onset, and prevention of pathogenesis. The prophylactically effective amount refers to a dose of the active ingredient sufficient to achieve the prophylactic objectives.

[00125] In this descriptive report, “treatment” includes curing a disease, improving the pathology of a disease (e.g., one or more symptoms), and inhibiting disease progression (disease severity). The “therapeutically effective amount” is a dose of the active ingredient sufficient to achieve the therapeutic goal. Thus, “improvement” is a concept encompassed by “treatment.”

[00126] In this descriptive report, the individual means an object to which a drug (pharmaceutical composition) containing an effective amount of an active ingredient is administered to prevent and / or treat (or improve) a disease or pathological condition. The individual may be a human or non-human animal, particularly a mammal (e.g., human, mouse, rat, guinea pig, hamster, rabbit, cat, dog, bovine, sheep, monkey, etc.).

[00127] In this descriptive report, the B0AT1 inhibitor means an agent containing a compound that has the ability to inhibit B0AT1, a transporter responsible for the reabsorption of neutral amino acids, such as phenylalanine, in the kidney. In particular, compound (I) of the present invention, or a pharmaceutically acceptable salt thereof, exhibits excellent inhibitory activity against B0AT1. The inhibitory activity against B0AT1 can be measured, for example, by Petition 870250102069, dated 07 / 11 / 2025, pp. 504 / 861 63 / 389 method described in Unpatented Document 11 (SLAS Discovery, 2019; 24(2): p.111-120) and by the method described in the Examples Experiments described below.

[00128] In this descriptive report, diseases whose symptoms can be alleviated by B0AT1 inhibition mean diseases caused by an increased level of neutral amino acids in the blood due to a mutation in a gene related to an amino acid metabolic pathway or similar. Specific examples of the disease include amino acid metabolism disorders such as phenylketonuria, urea cycle disorder, hypertyrosinemia (types 1-3), hypermethioninemia, maple syrup urine disease, homocystinuria, nonketotic hyperglycinemia, propionic acidemia, methylmalonic acidemia, isovaleric acidemia, and similar disorders.

[00129] (The compound of the present invention (compound (I)))

[00130] Each group in the above-mentioned formula (I) of compound (I) is explained below.

[00131] R1 is a carboxyl group or a group biologically equivalent to a carboxyl group.

[00132] R1 is preferably a carboxyl group, an optionally substituted C1-6 alkoxycarbonyl group, an optionally substituted carbamoyl group, a cyano group, or a group selected from the group consisting of the following formulas: Petition 870250102069, dated 07 / 11 / 2025, pp. 505 / 861 64 / 389 wherein a wavy line is a binding site of the group represented by the chemical formula mentioned above, and * is a binding position with L, or a tautomeric group thereof, more preferably a carboxyl group, an optionally substituted C1-6 alkoxycarbonyl group or an optionally substituted carbamoyl group.

[00133] L is a divalent organic group comprising a group consisting of a C1-6 alkylene group, a Ce-w arylene group, a C3-14 cycloalkylene group, a C2-6 alkenylene group, a C2-6 alkynylene group and a divalent non-aromatic heterocyclic group of 3 to 14 members, each of which is optionally further substituted. Petition 870250102069, dated 07 / 11 / 2025, pp. 506 / 861 65 / 389

[00134] L is preferably a C1-6 alkylene group, a C6-10 arylene group, a C3-14 cycloalkylene group, a C2-6 alkenylene group, a C2-6 alkynylene group, or a 3- to 14-membered divalent non-aromatic heterocyclic group, each of which optionally has, internally or at the end, one or more divalent groups selected from the group consisting of -NR2- (where R2 is a hydrogen atom or a C1-6 alkyl group), -O-, -S-, -C(=O)-, a C1-6 alkylene group, a C6-10 arylene group, a C3-14 cycloalkylene group, a C2-6 alkenylene group, a C2-6 alkynylene group, and a 3- to 14-membered divalent non-aromatic heterocyclic group, each of which is optionally further substituted by 1 three substituents selected from the aforementioned substituent group a or substituent group a', more preferably a C1-6 alkylene group optionally having, in the interior or at the end,one or more divalent groups selected from the group consisting of -NR2- (where R2 is a hydrogen atom or a C1-6 alkyl group), -O-, -S-, -C(=O)-, a C610 arylene group (for example, 1,2-phenylene, 1,3-phenylene, 1,4-phenylene), a C3-10 cycloalkylene group (for example, cyclobutane-1,3-di-yl, cyclopropane-1,2-di-yl, cyclopropane-1,1-di-yl, cyclopentane-1,2-di-yl, cyclohexane-1,2-di-yl, bicyclo[2.1.1]hexane-1,2-di-yl), a C2-6 alkylene group, and a 3- to 8-membered divalent non-aromatic heterocyclic group (for example, azetidine-1,3-di-yl, pyrrolidine-1,3-di-yl, pyrrolidine-1,2-di-yl, piperidine-1,2-di-yl, piperidine-1,4-di-yl, azepane-1,2-di-yl), and optionally also substituted by 1 to 3 substituents selected from the previously mentioned substituent group a or substituent group a' a C6-10 arylene group (e.g., 1,2-phenylene, 1,3-phenylene, 1,4-phenylene) optionally also replaced by 1 to 3 substituents selected from the substituent group or substituent group, Petition 870250102069, dated 07 / 11 / 2025, pp. 507 / 861 66 / 389 a' previously mentioned a C3-10 cycloalkylene group (for example, cyclobutane-1,3-di-yl, cyclopropane-1,2-di-yl, cyclopropane-1,1-di-yl, cyclopentane-1,2-di-yl, cyclohexane-1,2-di-yl, bicyclo[2.1.1]hexane-1,2-di-yl) optionally also substituted by 1 to 3 substituents selected from the previously mentioned substituent group a or substituent group a' a C2-4 alkynylene group optionally also substituted by 1 to 3 substituents selected from the previously mentioned substituent group a or substituent group a' or a divalent non-aromatic heterocyclic group of 3 to 8 members (for example, azetidine-1,3-di-yl, pyrrolidine-1,3-di-yl, pyrrolidine-1,2-di-yl, piperidine-1,2-di-yl, piperidine-1,4-di-yl, azepane-1,2-di-yl) optionally also substituted by 1 to 3 substituents selected from the previously mentioned substituent group a or substituent group a', also preferably a C1-6 alkylene group optionally having,within or at the end, one or more divalent groups selected from the group consisting of -NR2 (where R2 is a hydrogen atom or a C1-6 alkyl group), -O-, S-, a C3-10 cycloalkylene group (for example, cyclobutane-1,3-diyl, cyclopropane-1,2-diyl, cyclopropane-1,1-diyl, cyclopentane-1,2-diyl, cyclohexane-1,2-diyl, bicyclo[2.1.1]hexane-1,2-diyl), and a divalent non-aromatic heterocyclic group of 3 to 8 members (for example, azetidine-1,3-diyl, pyrrolidine-1,3-diyl, pyrrolidine-1,2-diyl, piperidine-1,2-diyl, piperidine-1,4-diyl, azepane-1,2-diyl), and optionally also replaced by 1 to 3 substituents selected from the previously mentioned substituent group a or substituent group a' a C3-10 cycloalkylene group (for example, cyclobutane-1,3-di-yl, cyclopropane-1,2-di-yl, cyclopropane-1,1-di-yl, cyclopentane-1,2-di-yl, cyclohexane-1,2-di-yl, bicyclo[2.1.1]hexane-1,2-di-yl), Petition 870250102069, dated 07 / 11 / 2025, pp. 508 / 861 67 / 389 optionally also substituted by 1 to 3 substituents selected from the aforementioned substituent group a or substituent group a' or a divalent non-aromatic heterocyclic group of 3 to 8 members (for example, azetidine-1,3-di-yl, pyrrolidine-1,3-di-yl, pyrrolidine-1,2-di-yl, piperidine-1,2-di-yl, piperidine-1,4-di-yl, azepane-1,2-di-yl) optionally also substituted by 1 to 3 substituents selected from the aforementioned substituent group a or substituent group a', in particular, preferably, a C1-6 alkylene group optionally also substituted by 1 to 3 substituents selected from the aforementioned substituent group a or substituent group a', A is a heterocyclic group containing divalent nitrogen that can also be substituted.

[00135] A is preferably a non-aromatic heterocyclic group containing divalent nitrogen represented by the following formula: where ** is a carbonyl group bonding site, *** is an L group bonding site, and ring A1 is a 3- to 10-membered monocycle, an 8- to 14-membered fused cycle, a 6- to 16-membered spiro cycle, or a 6- to 14-membered bridging cycle, and optionally has, as a ring constituent atom in addition to a nitrogen atom and a carbon atom, heteroatoms selected from the group consisting of a nitrogen atom, an oxygen atom, and a sulfur atom, which is optionally also substituted by 1 to 3 substituents selected from the previously mentioned substituent group a or substituent group a'; a more preferred embodiment is a non-aromatic heterocyclic group containing divalent nitrogen represented by the following Petition 870250102069, dated 07 / 11 / 2025, pp. 509 / 861 68 / 389 formula: or or wherein a wavy line is a binding site to the group represented by the chemical formula mentioned above, a bond represented by is a single bond or a double bond, each Y is independently a nitrogen atom or CR3 (wherein R3 is a hydrogen atom or a C1-6 alkyl group), Z is an oxygen atom, a sulfur atom, NR4 or CR5R6 (wherein R4, R5 and R6 are each independently a hydrogen atom or a C1-6 alkyl group), n is an integer from 0 to 2, m is an integer from Petition 870250102069, dated 07 / 11 / 2025, pp. 510 / 861 69 / 389 a 2, n1 and n2 are, each independently, an integer from 0 to 2, m1 and m2 are, each independently, an integer from 0 to 2, “ is a carbonyl group binding site, and *** is an L group binding site, and optionally also substituted by 1 to 3 substituents selected from the substituent group a or substituent group a' mentioned above (for example, a non-aromatic heterocyclic group containing divalent nitrogen represented by the following formula: or ( / f] where each symbol is as defined above, and optionally also replaced by 1 to 3 substituents selected from the substituent group a or substituent group a' mentioned previously), another more preferred embodiment is a non-aromatic heterocyclic group containing divalent nitrogen represented by the following formula: Petition 870250102069, dated 07 / 11 / 2025, pp. 511 / 861 70 / 389 or wherein a wavy line is a bonding site of the group represented by the chemical formula mentioned above, a bond represented by is a single bond or a double bond, each Y is independently a nitrogen atom or CR3 (wherein R3 is a hydrogen atom or a C1-6 alkyl group), Z is an oxygen atom, a sulfur atom, NR4 or CR5R6 (wherein R4, R5 and R6 are each independently a hydrogen atom or a C1-6 alkyl group), n is an integer from 0 to 2, m is an integer from 0 to 2, n1 and n2 are each independently an integer of Petition 870250102069, dated 07 / 11 / 2025, pp. 512 / 861 71 / 389 a 2, m1e m2são, each independently, is an integer from 0 to 2, “ is a carbonyl group binding site, and *** is an L group binding site, and optionally also substituted by 1 to 3 substituents selected from the previously mentioned substituent group a or substituent group a' (for example, a non-aromatic heterocyclic group containing divalent nitrogen represented by the following formula: VWL where each symbol is as defined above, and optionally also replaced by 1 to 3 substituents selected from the substituent group a or substituent group a' mentioned previously), also preferably a non-aromatic heterocyclic group containing divalent nitrogen represented by the following formula: Petition 870250102069, dated 07 / 11 / 2025, pp. 513 / 861 72 / 389 wherein each symbol is as defined above, and optionally also replaced by 1 to 3 substituents selected from the previously mentioned substituent group a or substituent group a' (for example, a non-aromatic heterocyclic group containing divalent nitrogen represented by the following formula: or Petition 870250102069, dated 07 / 11 / 2025, pp. 514 / 861 73 / 389 where each symbol is as defined above, and optionally also replaced by 1 to 3 substituents selected from the substituent group a or substituent group a' previously mentioned), even more preferably, a non-aromatic heterocyclic group containing divalent nitrogen represented by the following formula: wherein each symbol is as defined above, and optionally also replaced by 1 to 3 substituents selected from the previously mentioned substituent group a or substituent group a' (for example, a non-aromatic heterocyclic group containing divalent nitrogen represented by the following formula: wherein each symbol is as defined above, and optionally also substituted by 1 to 3 substituents selected from the substituent group a or substituent group a' previously mentioned, provided that when Z is CR5R6, the optionally substituted substituent is selected from the group consisting of, among the substituents in the substituent group a or substituent group a' previously mentioned, a Ce-14 hydrocarbocyclic group optionally substituted by 1 to 3 substituents selected from the substituent group b or substituent group b'; an aromatic heterocyclic group of 5 to 14 members optionally substituted by 1 to 3 substituents selected from the substituent group b or substituent group b'; and a non-aromatic heterocyclic group of 3 to Petition 870250102069, dated 07 / 11 / 2025, pp. 515 / 861 74 / 389 members optionally replaced by 1 to 3 substituents selected from substituent group b or substituent group b'), in particular, preferably, a non-aromatic heterocyclic group containing divalent nitrogen represented by the following formula: wherein each symbol is as defined above, and optionally also replaced by 1 to 3 substituents selected from the previously mentioned substituent group a or substituent group a' (in particular, preferably, a non-aromatic heterocyclic group containing divalent nitrogen represented by the following formula: where each symbol is as defined above, and optionally also replaced by 1 to 3 substituents selected from the substituent group a or substituent group a' mentioned above).

[00136] R is an optionally substituted Ce-waryl-ethenyl group.

[00137] R is preferably a 2-phenylthenyl group optionally substituted by 1 to 3 substituents selected from the group consisting of a halogen atom, an optionally substituted C1-6 alkyl group, an optionally substituted C3-8 cycloalkyl group, an optionally substituted C1-6 alkoxy group, an optionally substituted C3-8 cycloalkoxy group, an optionally substituted C1-6 alkylsulfanyl group, an optionally substituted C3-8 cycloalkylsulfanyl group, and a pentafluorosulfanyl group, most preferably a 2-(E)-phenylthenyl group Petition 870250102069, dated 07 / 11 / 2025, pp. 516 / 861 75 / 389 optionally substituted by 1 to 3 substituents selected from the group consisting of a halogen atom, a C1-6 alkyl group optionally substituted by halogen atoms, and a pentafluorosulfanyl group.

[00138] Like compound (I), the following compounds are preferred. [Compound (IA)1

[00139] Compound (I), wherein R1 is a carboxy group, an optionally substituted C1-6 alkoxy-carbonyl group, an optionally substituted carbamoyl group, a cyano group, or a group selected from the group consisting of the following formulas: where a wavy line is a connecting site of the represented group. Petition 870250102069, dated 07 / 11 / 2025, p. 517 / 861 76 / 389 by the chemical formula mentioned above, and * is a bonding position with L, or a tautomeric group thereof; L is a C1-6 alkylene group, a Ce-warylene group, a C3-14 cycloalkylene group, a C2-6 alkenylene group, a C2-6 alkynylene group, or a divalent non-aromatic heterocyclic group of 3 to 14 members, each of which optionally has, in the interior or at the end, one or more divalent groups selected from the group consisting of -NR2- (where R2 is a hydrogen atom or a C1-6 alkyl group), -O-, -S-, -C(=O)-, a C1-6 alkylene group, a Ce-warylene group, a C3-4 cycloalkylene group, a C2-6 alkenylene group, a C2-6 alkynylene group and a divalent non-aromatic heterocyclic group of 3 to 14 members, and each of which is optionally also substituted by 1 to 3 substituents selected from the substituent group or substituent group a' previously mentioned; A is a non-aromatic heterocyclic group containing divalent nitrogen, represented by the following formula: wherein ** is a carbonyl group binding site, *** is an L group binding site, and ring A1 is a 3- to 10-membered monocycle, an 8- to 14-membered fused cycle, a 6- to 16-membered spiro cycle, or a 6- to 14-membered bridging cycle, and optionally contains, as a ring constituent atom in addition to a nitrogen atom and a carbon atom, heteroatoms selected from the group consisting of a nitrogen atom, an oxygen atom, and a sulfur atom, and optionally also substituted by 1 to 3 substituents selected from the previously mentioned substituent group a or substituent group a'; and Petition 870250102069, dated 07 / 11 / 2025, pp. 518 / 861 77 / 389 R is a 2-phenylthenyl group optionally substituted by 1 to 3 substituents selected from the group consisting of a halogen atom, an optionally substituted C1-6 alkyl group, an optionally substituted C3-8 cycloalkyl group, an optionally substituted C1-6 alkoxy group, an optionally substituted C3-8 cycloalkoxy group, an optionally substituted C1-6 alkylsulfanyl group, an optionally substituted C3-8 cycloalkylsulfanyl group, and a pentafluorosulfanyl group, or a pharmaceutically acceptable salt thereof. Compound (IB)

[00140] Compound (I), where R1 is a carboxy group, an optionally substituted C1-6 alkoxy-carbonyl group, or an optionally substituted carbamoyl group; L is a C1-6 alkylene group, a Ce-warylene group, a C3-14 cycloalkylene group, a C2-6 alkenylene group, a C2-6 alkynylene group, or a divalent non-aromatic heterocyclic group of 3 to 14 members, each of which optionally has, in the interior or at the end, one or more divalent groups selected from the group consisting of -NR2- (where R2 is a hydrogen atom or a C1-6 alkyl group), -O-, -S-, -C(=O)-, a C1-6 alkylene group, a Ce-warylene group, a C3-4 cycloalkylene group, a C2-6 alkenylene group, a C2-6 alkynylene group and a divalent non-aromatic heterocyclic group of 3 to 14 members, and each of which is optionally also substituted by 1 to 3 substituents selected from the substituent group or substituent group a' mentioned earlier; A is a non-aromatic heterocyclic group containing divalent nitrogen, represented by the following formula: Petition 870250102069, dated 07 / 11 / 2025, p. 519 / 861 78 / 389 where ** is a carbonyl group bonding site, *** is an L group bonding site, and ring A1 is a 3- to 10-membered monocycle, an 8- to 14-membered fused cycle, a 6- to 16-membered spiro cycle, or a 6- to 14-membered bridging cycle, and optionally contains, as a ring constituent atom in addition to a nitrogen atom and a carbon atom, heteroatoms selected from the group consisting of a nitrogen atom, an oxygen atom, and a sulfur atom, and optionally also substituted by 1 to 3 substituents selected from the previously mentioned substituent group a or substituent group a'; and R is a 2-phenylthenyl group optionally substituted by 1 to 3 substituents selected from the group consisting of a halogen atom, an optionally substituted C1-6 alkyl group, an optionally substituted C3-8 cycloalkyl group, an optionally substituted C1-6 alkoxy group, an optionally substituted C3-8 cycloalkoxy group, an optionally substituted C1-6 alkylsulfanyl group, an optionally substituted C3-8 cycloalkylsulfanyl group, and a pentafluorosulfanyl group, or a pharmaceutically acceptable salt thereof. [Compound (IC)]

[00141] Compound (I), in which R1 is a carboxy group, an optionally substituted C1-6 alkoxy-carbonyl group, an optionally substituted carbamoyl group, a cyano group, or a group selected from the group consisting of the following formulas: Petition 870250102069, dated 07 / 11 / 2025, pp. 520 / 861 79 / 389 where a wavy line is a binding site of the group represented by the chemical formula mentioned above, and * is a binding position with L, or a tautomeric group thereof; L is a C1-6 alkylene group optionally having, in the interior or at the end, one or more divalent groups selected from the group consisting of -NR2- (wherein R2 is a hydrogen atom or a C1-6 alkyl group), -O-, -S-, -C(=O)-, a C3-10 arylene group (e.g., 1,2-phenylene, 1,3-phenylene, 1,4-phenylene), a C3-10 cycloalkylene group (e.g., cyclobutane-1,3-di-yl, cyclopropane-1,2-di-yl, cyclopropane-1,1-di-yl, cyclopentane-1,2-di-yl, cyclohexane-1,2-di Petition 870250102069, dated 07 / 11 / 2025, pp. 521 / 861 80 / 389 ila, bicyclo[2.1.1]hexane-1,2-di-yl), C2-6 alkylene group, and a 3- to 8-membered divalent non-aromatic heterocyclic group (e.g., azetidine-1,3-di-yl, pyrrolidine-1,3-di-yl, pyrrolidine-1,2-di-yl, piperidine-1,2-di-yl, piperidine-1,4-di-yl, azepane-1,2-di-yl), and optionally also substituted by 1 to 3 substituents selected from the aforementioned substituent group a or substituent group a'; a C3-10 cycloalkylene group (e.g., cyclobutane-1,3di-yl, cyclopropane-1,2-di-yl, cyclopropane-1,1-di-yl, cyclopentane-1,2di-yl, cyclohexane-1,2-di-yl, bicyclo[2.1.1 ]hexane-1,2-di-yl) optionally also substituted by 1 to 3 substituents selected from the substituent group a or substituent group a' mentioned above; a C2-4 alkynylene group optionally also substituted by 1 to 3 substituents selected from the substituent group a or substituent group a' mentioned above; or a divalent non-aromatic heterocyclic group of 3 to 8 members (e.g., azetidine-1,3-di-yl, pyrrolidine-1,3-di-yl, pyrrolidine-1,2-di-yl, piperidine-1,2-di-yl, piperidine-1,4-di-yl, azepane-1,2-di-yl) optionally also substituted by 1 to 3 substituents selected from the substituent group a or substituent group a' mentioned above. A is a non-aromatic heterocyclic group containing divalent nitrogen, represented by the following formula: where ** is a binding site with a carbonyl group, *** is a binding site Petition 870250102069, dated 07 / 11 / 2025, pp. 522 / 861 81 / 389 linkage with the L group, and ring A1 is a 3- to 10-membered monocycle, an 8- to 14-membered fused cycle, a 6- to 16-membered spiro cycle, or a 6- to 14-membered bridging cycle, and optionally has, as a constituent atom of the ring in addition to a nitrogen atom and a carbon atom, heteroatoms selected from the group consisting of a nitrogen atom, an oxygen atom, and a sulfur atom, which is optionally also substituted by 1 to 3 substituents selected from the substituent group a or substituent group a' mentioned above; and R is a 2-phenylthenyl group optionally substituted by 1 to 3 substituents selected from the group consisting of a halogen atom, an optionally substituted C1-6 alkyl group, an optionally substituted C3-8 cycloalkyl group, an optionally substituted C1-6 alkoxy group, an optionally substituted C3-8 cycloalkoxy group, an optionally substituted C1-6 alkylsulfanyl group, an optionally substituted C3-8 cycloalkylsulfanyl group, and a pentafluorosulfanyl group, or a pharmaceutically acceptable salt thereof. [Compound (ID)]

[00142] Compound (I), in which R1 is a carboxy group, an optionally substituted C1-6 alkoxy-carbonyl group, an optionally substituted carbamoyl group, a cyano group, or a group selected from the group consisting of the following formulas: Petition 870250102069, dated 07 / 11 / 2025, pp. 523 / 861 82 / 389 where a wavy line is a binding site of the group represented by the chemical formula mentioned above, and * is a binding position with L, or a tautomeric group thereof; L is a C1-6 alkylene group optionally having, in the interior or at the end, one or more divalent groups selected from the group consisting of -NR2- (wherein R2 is a hydrogen atom or a C1-6 alkyl group), -O-, -S-, a C3-10 cycloalkylene group (for example, cyclobutane-1,3-di-yl, cyclopropane-1,2-di-yl, cyclopropane-1,1-di-yl, cyclopentane-1,2-di-yl, cyclohexane-1,2-di-yl, bicyclo[2.1.1]hexane-1,2-di-yl), and a 3- to 8-membered divalent non-aromatic heterocyclic group (for example, azetidine-1,3-di-yl, pyrrolidyne-1,3-di-yl, pyrrolidyne-1,2-di-yl, piperidyne-1,2-di-yl, piperidine-1,4-di-yl, azepane-1,2-di-yl), and optionally also Petition 870250102069, dated 07 / 11 / 2025, pp. 524 / 861 83 / 389 substituted by 1 to 3 substituents selected from the previously mentioned substituent group a or substituent group a' or a C3-10 cycloalkylene group (e.g., cyclobutane-1,3-di-yl, cyclopropane-1,2-di-yl, cyclopropane-1,1-di-yl, cyclopentane-1,2-di-yl, cyclohexane-1,2-di-yl, bicyclo[2.1.1]hexane-1,2-di-yl) optionally also substituted by 1 to 3 substituents selected from the previously mentioned substituent group a or substituent group a' or a 3 to 8 membered divalent non-aromatic heterocyclic group (e.g., azetidine-1,3-di-yl, pyrrolidine-1,3-di-yl, pyrrolidine-1,2-di-yl, piperidine-1,2-di-yl, piperidine-1,4-di-yl, azepane-1,2-di-yl) optionally also replaced by 1 to 3 substituents selected from the previously mentioned substituent group a or substituent group a'; A is a non-aromatic heterocyclic group containing divalent nitrogen, represented by the following formula: wherein ** is a carbonyl group binding site, *** is an L group binding site, and ring A1 is a 3- to 10-membered monocycle, an 8- to 14-membered fused cycle, a 6- to 16-membered spiro cycle, or a 6- to 14-membered bridging cycle, and optionally has, as a ring constituent atom in addition to a nitrogen atom and a carbon atom, heteroatoms selected from the group consisting of a nitrogen atom, an oxygen atom, and a sulfur atom, which is optionally also substituted by 1 to 3 substituents selected from the previously mentioned substituent group a or substituent group a'; and R is a 2-phenylthenyl group optionally substituted by 1 to 3 substituents selected from the group consisting of an atom of Petition 870250102069, dated 07 / 11 / 2025, pp. 525 / 861 84 / 389 halogen, an optionally substituted C1-6 alkyl group, an optionally substituted C3-8 cycloalkyl group, an optionally substituted C1-6 alkoxy group, an optionally substituted C3-8 cycloalkoxy group, an optionally substituted C1-6 alkylsulfanyl group, an optionally substituted C3-8 cycloalkylsulfanyl group, and a pentafluorosulfanyl group, or a pharmaceutically acceptable salt thereof. [Compound (IE)1

[00143] Compound (I), in which R1 is a carboxy group, an optionally substituted C1-6 alkoxy-carbonyl group, an optionally substituted carbamoyl group, a cyano group, or a group selected from the group consisting of the following formulas: Petition 870250102069, dated 07 / 11 / 2025, pp. 526 / 861 85 / 389 where a wavy line is a binding site of the group represented by the chemical formula mentioned above, and * is a binding position with L, or a tautomeric group thereof; L is a C1-6 alkylene group optionally also substituted by 1 to 3 substituents selected from the substituent group a or substituent group a' mentioned above; A is a non-aromatic heterocyclic group containing divalent nitrogen, represented by the following formula: where ** is a carbonyl group binding site, *** is an L group binding site, and ring A1 is a 3- to 10-membered monocycle, an 8- to 14-membered fused cycle, a 6- to 16-membered spiro cycle, or a 6- to 14-membered bridging cycle, and optionally has, as a ring constituent atom in addition to a nitrogen atom and a Petition 870250102069, dated 07 / 11 / 2025, pp. 527 / 861 86 / 389 carbon atom, heteroatoms selected from the group consisting of one nitrogen atom, one oxygen atom, and one sulfur atom, which is optionally also replaced by 1 to 3 substituents selected from the previously mentioned substituent group a or substituent group a'; and R is a 2-phenylthenyl group optionally substituted by 1 to 3 substituents selected from the group consisting of a halogen atom, an optionally substituted C1-6 alkyl group, an optionally substituted C3-8 cycloalkyl group, an optionally substituted C1-6 alkoxy group, an optionally substituted C3-8 cycloalkoxy group, an optionally substituted C1-6 alkylsulfanyl group, an optionally substituted C3-8 cycloalkylsulfanyl group, and a pentafluorosulfanyl group, or a pharmaceutically acceptable salt thereof. [Compound (IF)1

[00144] Compound (I), in which R1 is a carboxy group, an optionally substituted C1-6 alkoxy-carbonyl group, an optionally substituted carbamoyl group, a cyano group, or a group selected from the group consisting of the following formulas: Petition 870250102069, dated 07 / 11 / 2025, pp. 528 / 861 87 / 389 where a wavy line is a binding site of the group represented by the chemical formula mentioned above, and * is a binding position with L, or a tautomeric group thereof; L is a C1-6 alkylene group, a Ce-warylene group, a C3-14 cycloalkylene group, a C2-6 alkenylene group, a C2-6 alkynylene group, or a divalent non-aromatic heterocyclic group of 3 to 14 members, each of which optionally has, in the interior or at the end, one or more divalent groups selected from the group consisting of -NR2- (where R2 is a hydrogen atom or a C1-6 alkyl group), -O-, -S-, -C(=O)-, a C1-6 alkylene group, a Ce-warylene group, a C3-4 cycloalkylene group, a C2-6 alkenylene group, a C2-6 alkynylene group and a divalent non-aromatic heterocyclic group of 3 to 14 members, and each of which is optionally also substituted by 1 to 3 substituents selected from the substituent group or substituent group a' mentioned earlier; A is a non-aromatic heterocyclic group containing divalent nitrogen, represented by the following formula: Petition 870250102069, dated 07 / 11 / 2025, pp. 529 / 861 88 / 389 wherein a wavy line is a bonding site of the group represented by the chemical formula mentioned above, a bond represented by is a single bond or a double bond, each Y is independently a nitrogen atom or CR3 (wherein R3 is a hydrogen atom or a C1-6 alkyl group), Z is an oxygen atom, a sulfur atom, NR4 or CR5R6 (wherein R4, R5 and R6 are each independently a hydrogen atom or a C1-6 alkyl group), n is an integer from 0 to 2, m is an integer from 0 to 2, n1 and n2 are each independently an integer from 0 to 2, m1 and m2 are each independently an integer Petition 870250102069, dated 07 / 11 / 2025, pp. 530 / 861 89 / 389 from 0 to 2, “ is a carbonyl group binding site, and *** is an L group binding site, and optionally also substituted by 1 to 3 substituents selected from the substituent group a or substituent group a' mentioned above (for example, a non-aromatic heterocyclic group containing divalent nitrogen represented by the following formula: or ó Ϊ 1, ** N where each symbol is as defined above, and optionally also replaced by 1 to 3 substituents selected from the substituent group a or substituent group a' mentioned previously); and R is a 2-phenylthenyl group optionally substituted by 1 to 3 substituents selected from the group consisting of a halogen atom, an optionally substituted C1-6 alkyl group, a group Petition 870250102069, dated 07 / 11 / 2025, pp. 531 / 861 90 / 389 Optionally substituted C3-8 cycloalkyl, an optionally substituted C1-6 alkoxy group, an optionally substituted C3-8 cycloalkoxy group, an optionally substituted C1-6 alkylsulfanyl group, an optionally substituted C3-8 cycloalkylsulfanyl group, and a pentafluorosulfanyl group, or a pharmaceutically acceptable salt thereof. [Compound (IF')1

[00145] Compound (I), in which A is a non-aromatic heterocyclic group containing divalent nitrogen, represented by the following formula: where a wavy line is a connecting site of the represented group. Petition 870250102069, dated 07 / 11 / 2025, pp. 532 / 861 91 / 389 by the chemical formula mentioned above, a bond represented by is a single bond or a double bond, each Y is independently a nitrogen atom or CR3 (where R3 is a hydrogen atom or a C1-6 alkyl group), Z is an oxygen atom, a sulfur atom, NR4 or CR5R6 (where R4, R5 and R6 are each independently a hydrogen atom or a C1-6 alkyl group), n is an integer from 0 to 2, m is an integer from 0 to 2, n1 and n2 are each independently an integer from 0 to 2, m1 and m2 are each independently an integer from 0 to 2, ** is a bonding site with a carbonyl group, and *** is a bonding site with the L group, and optionally also substituted by 1 to 3 substituents selected from the substituent group a or substituent group a' mentioned above (for example, a non-aromatic heterocyclic group containing divalent nitrogen is represented by the following formula: Petition 870250102069, dated 07 / 11 / 2025, pp. 533 / 861 92 / 389 ALA? where each symbol is as defined above, and optionally also replaced by 1 to 3 substituents selected from the substituent group a or substituent group a' mentioned above); and other symbols are as defined for the [compound (IF)] mentioned above, or a pharmaceutically acceptable salt thereof. [Compound (IG)1

[00146] Compound (I), in which R1 is a carboxy group, an optionally substituted C1-6 alkoxy-carbonyl group, an optionally substituted carbamoyl group, a cyano group, or a group selected from the group consisting of the following formulas: Petition 870250102069, dated 07 / 11 / 2025, pp. 534 / 861 93 / 389 where a wavy line is a binding site of the group represented by the chemical formula mentioned above, and * is a binding position with L, or a tautomeric group thereof; L is a C1-6 alkylene group, a Ce-warylene group, a C3-14 cycloalkylene group, a C2-6 alkenylene group, a C2-6 alkynylene group, or a divalent non-aromatic heterocyclic group of 3 to 14 members, each of which optionally has, in the interior or at the end, one or more divalent groups selected from the group consisting of -NR2- (where R2 is a hydrogen atom or a C1-6 alkyl group), -O-, -S-, -C(=O)-, a C1-6 alkylene group, a Ce-warylene group, a C3-4 cycloalkylene group, a C2-6 alkenylene group, a Petition 870250102069, dated 07 / 11 / 2025, pp. 535 / 861 94 / 389 C2-6 alkynylene group and a divalent non-aromatic heterocyclic group of 3 to 14 members, each of which is optionally also substituted by 1 to 3 substituents selected from the previously mentioned substituent group a or substituent group a'; A is a non-aromatic heterocyclic group containing divalent nitrogen, represented by the following formula: wherein ** is a carbonyl group binding site, *** is an L group binding site, and ring A1 is a 3- to 10-membered monocycle, an 8- to 14-membered fused cycle, a 6- to 16-membered spiro cycle, or a 6- to 14-membered bridging cycle, and optionally has, as a ring constituent atom in addition to a nitrogen atom and a carbon atom, heteroatoms selected from the group consisting of a nitrogen atom, an oxygen atom, and a sulfur atom, which is optionally also substituted by 1 to 3 substituents selected from the previously mentioned substituent group a or substituent group a'; and R is a 2-(E)-phenylthenyl group optionally substituted by 1 to 3 substituents selected from the group consisting of a halogen atom, a C1-6 alkyl group optionally substituted by halogen atoms, and a pentafluorosulfanyl group, or a pharmaceutically acceptable salt thereof. [Compound (IH)1

[00147] Compound (I), in which R1 is a carboxy group, an optionally substituted C1-6 alkoxy-carbonyl group, or an optionally substituted carbamoyl group; L is a C1-6 alkylene group optionally having, within Petition 870250102069, dated 07 / 11 / 2025, pp. 536 / 861 95 / 389 or at the end, one or more divalent groups selected from the group consisting of -NR2- (where R2 is a hydrogen atom or a C1-6 alkyl group), -O-, -S-, -C(=O)-, a C6-10 arylene group (for example, 1,2-phenylene, 1,3-phenylene, 1,4-phenylene), a C3-10 cycloalkylene group (for example, cyclobutane-1,3-di-yl, cyclopropane-1,2-di-yl, cyclopropane-1,1-di-yl, cyclopentane-1,2-di-yl, cyclohexane-1,2-diyl, bicyclo[2.1.[1]hexane-1,2-di-yl), C2-6 alkylene group, and a 3- to 8-membered divalent non-aromatic heterocyclic group (e.g., azetidine-1,3-di-yl, pyrrolidine-1,3-di-yl, pyrrolidine-1,2-di-yl, piperidine-1,2-di-yl, piperidine-1,4-di-yl, azepane-1,2-di-yl), and optionally also substituted by 1 to 3 substituents selected from the aforementioned substituent group a or substituent group a'; a C6-10 arylene group (e.g., 1,2-phenylene, 1,3-phenylene, 1,4-phenylene) optionally also substituted by 1 to 3 substituents selected from the previously mentioned substituent group a or substituent group a'; a C3-10 cycloalkylene group (e.g., cyclobutane-1,3-di-yl, cyclopropane-1,2-di-yl, cyclopropane-1,1-di-yl, cyclopentane-1,2-di-yl, cyclohexane-1,2-di-yl, bicyclo[2.1.[1]hexane-1,2-di-yl) optionally also substituted by 1 to 3 substituents selected from the previously mentioned substituent group a or substituent group a'; a C2-4 alkynylene group optionally also substituted by 1 to 3 substituents selected from the previously mentioned substituent group a or substituent group a'; or a divalent non-aromatic heterocyclic group of 3 to 8 members (e.g., azetidine-1,3-di-yl, pyrrolidine-1,3-di-yl, pyrrolidine-1,2-di-yl, piperidine-1,2-di-yl, piperidine-1,4-di-yl, azepane-1,2-di-yl) optionally also substituted by 1 to 3 substituents selected from the previously mentioned substituent group a or substituent group a'. Petition 870250102069, dated 07 / 11 / 2025, pp. 537 / 861 96 / 389 A is a non-aromatic heterocyclic group containing divalent nitrogen, represented by the following formula: wherein a wavy line is a bonding site of the group represented by the chemical formula mentioned above, a bond represented by is a single bond or a double bond, each Y is independently a nitrogen atom or CR3 (wherein R3 is a hydrogen atom or a C1-6 alkyl group), Z is an oxygen atom, a sulfur atom, NR4 or CR5R6 (wherein R4, R5 and R6 are each independently a hydrogen atom or a C1-6 alkyl group), n is an integer from 0 to 2, m is an integer from 0 to 2, n1 and n2 are each independently an integer of Petition 870250102069, dated 07 / 11 / 2025, pp. 538 / 861 97 / 389 a 2, m1e m2são, each independently, is an integer from 0 to 2, “ is a binding site with a carbonyl group, and *** is a binding site with the L group, and optionally also substituted by 1 to 3 substituents selected from the previously mentioned substituent group a or substituent group a' (for example, a non-aromatic heterocyclic group containing divalent nitrogen represented by the following formula: where each symbol is as defined above, and optionally also replaced by 1 to 3 substituents selected from the substituent group a or substituent group a' mentioned previously); and R is a 2-(E)-phenylthenyl group optionally substituted by 1 to 3 substituents selected from the group consisting of a halogen atom, a C1-6 alkyl group optionally substituted by halogen atoms, and a pentafluorosulfanyl group, or a pharmaceutically acceptable salt thereof. [Compound (IH')1 Petition 870250102069, dated 07 / 11 / 2025, pp. 539 / 861 98 / 389

[00148] Compound (I), where A is a non-aromatic heterocyclic group containing divalent nitrogen, represented by the following formula: wherein a wavy line is a bonding site of the group represented by the chemical formula mentioned above, a bond represented by is a single bond or a double bond, each Y is independently a nitrogen atom or CR3 (wherein R3 is a hydrogen atom or a C1-6 alkyl group), Z is an oxygen atom, a sulfur atom, NR4 or CR5R6 (wherein R4, R5 and R6 are each independently a hydrogen atom or a C1-6 alkyl group), n is an integer from 0 to 2, m is an integer from 0 to 2, n1 and n2 are each independently an integer of Petition 870250102069, dated 07 / 11 / 2025, pp. 540 / 861 99 / 389 a 2, m1e m2são, each independently, is an integer from 0 to 2, “ is a carbonyl group binding site, and *** is an L group binding site, and optionally also substituted by 1 to 3 substituents selected from the previously mentioned substituent group a or substituent group a' (for example, a non-aromatic heterocyclic group containing divalent nitrogen represented by the following formula: where each symbol is as defined above, and optionally also replaced by 1 to 3 substituents selected from the substituent group a or substituent group a' mentioned above); and other symbols are as defined for the aforementioned [compound (IH)], or a pharmaceutically acceptable salt thereof. [Compound (IJ)1

[00149] Compound (I), in which R1 is a carboxy group, a C1-6 alkoxy-carbonyl group. Petition 870250102069, dated 07 / 11 / 2025, pp. 541 / 861 100 / 389 optionally substituted, or a carbamoyl group optionally substituted; L is a C1-6 alkylene group optionally having, in the interior or at the end, one or more divalent groups selected from the group consisting of -NR2- (wherein R2 is a hydrogen atom or a C1-6 alkyl group), -O-, -S-, a C3-10 cycloalkylene group (for example, cyclobutane-1,3-diyl, cyclopropane-1,2-diyl, cyclopropane-1,1-diyl, cyclopentane-1,2-diyl, cyclohexane-1,2-diyl, bicyclo[2.1.1]hexane-1,2-diyl), and a 3- to 8-membered divalent non-aromatic heterocyclic group (for example, azetidine-1,3-diyl, pyrrolidine-1,3-diyl, pyrrolidine-1,2-diyl, piperidine-1,2-diyl, piperidine-1,4-diyl, azepane-1,2-di-yl), and optionally also substituted by 1 to 3 substituents selected from the previously mentioned substituent group a or substituent group a' a C3-10 cycloalkylene group (for example, cyclobutane-1,3-di-yl, cyclopropane-1,2-di-yl, cyclopropane-1,1-di-yl, cyclopentane-1,2-di-yl, cyclohexane-1,2-di-yl, bicyclo[2.1.[1]hexane-1,2-di-yl) optionally also substituted by 1 to 3 substituents selected from the previously mentioned substituent group a or substituent group a' or a divalent non-aromatic heterocyclic group of 3 to 8 members (e.g., azetidine-1,3-di-yl, pyrrolidine-1,3-di-yl, pyrrolidine-1,2-di-yl, piperidine-1,2-di-yl, piperidine-1,4-di-yl, azepane-1,2-di-yl) optionally also substituted by 1 to 3 substituents selected from the previously mentioned substituent group a or substituent group a'; A is a non-aromatic heterocyclic group containing divalent nitrogen, represented by the following formula: Petition 870250102069, dated 07 / 11 / 2025, pp. 542 / 861 101 / 389 wherein a wavy line is a bonding site of the group represented by the chemical formula mentioned above, a bond represented by is a single bond or a double bond, each Y is independently a nitrogen atom or CR3 (wherein R3 is a hydrogen atom or a C1-6 alkyl group), Z is an oxygen atom, a sulfur atom, NR4 or CR5R6 (wherein R4, R5 and R6 are each independently a hydrogen atom or a C1-6 alkyl group), n is an integer from 0 to 2, m is an integer from Petition 870250102069, dated 07 / 11 / 2025, pp. 543 / 861 102 / 389 a 2, n1 and n2 are, each independently, an integer from 0 to 2, m1 and m2 are, each independently, an integer from 0 to 2, “ is a binding site with a carbonyl group, and *** is a binding site with the L group, and optionally also substituted by 1 to 3 substituents selected from the substituent group a or substituent group a' mentioned above (for example, a non-aromatic heterocyclic group containing divalent nitrogen represented by the following formula: or where each symbol is as defined above, and optionally also replaced by 1 to 3 substituents selected from the substituent group a or substituent group a' mentioned previously); and R is a 2-(E)-phenylthenyl group optionally substituted by 1 to 3 substituents selected from the group consisting of a halogen atom, a C1-6 alkyl group optionally substituted by Petition 870250102069, dated 07 / 11 / 2025, pp. 544 / 861 103 / 389 halogen atoms, and a pentafluorosulfanyl group, or a pharmaceutically acceptable salt thereof. [Compound (IJ')]

[00150] Compound (I), where A is a non-aromatic heterocyclic group containing divalent nitrogen, represented by the following formula: where a wavy line is a binding site of the group represented by the chemical formula mentioned above, a bond represented by is a single bond or a double bond, each Y is Petition 870250102069, dated 07 / 11 / 2025, pp. 545 / 861 104 / 389 independently a nitrogen atom or CR3 (where R3 is a hydrogen atom or a C1-6 alkyl group), Z is an oxygen atom, a sulfur atom, NR4 or CR5R6 (where R4, R5 and R6 are each independently a hydrogen atom or a C1-6 alkyl group), n is an integer from 0 to 2, m is an integer from 0 to 2, n1 and n2 are each independently an integer from 0 to 2, m1 and m2 are each independently an integer from 0 to 2, “ is a carbonyl group bonding site, and *** is an L group bonding site, and optionally also substituted by 1 to 3 substituents selected from the previously mentioned substituent group a or substituent group a' (for example, a non-aromatic heterocyclic group containing divalent nitrogen represented by the following formula: where each symbol is as defined above, and optionally also replaced by 1 to 3 substituents selected from the substituent group a or substituent group a' mentioned previously); and Petition 870250102069, dated 07 / 11 / 2025, pp. 546 / 861 105 / 389 other symbols are as defined for the aforementioned [compound (IJ)]> or a pharmaceutically acceptable salt thereof. [Compound (IK)]

[00151] Compound (I), in which R1 is a carboxy group, an optionally substituted C1-6 alkoxy-carbonyl group, or an optionally substituted carbamoyl group; L is a C1-6 alkylene group optionally also substituted by 1 to 3 substituents selected from the substituent group a or substituent group a' mentioned above; A is a non-aromatic heterocyclic group containing divalent nitrogen, represented by the following formula: where a wavy line is a binding site of the group represented by the chemical formula mentioned above, a bond represented by Petition 870250102069, dated 07 / 11 / 2025, pp. 547 / 861 106 / 389 is a single bond or a double bond, each Y is independently a nitrogen atom or CR3 (where R3 is a hydrogen atom or a C1-6 alkyl group), Z is an oxygen atom, a sulfur atom, NR4 or CR5R6 (where R4, R5 and R6 are each independently a hydrogen atom or a C1-6 alkyl group), n is an integer from 0 to 2, m is an integer from 0 to 2, n1 and n2 are each independently an integer from 0 to 2, m1 and m2 are each independently an integer from 0 to 2, “ is a bonding site with a carbonyl group, and *** is a bonding site with the L group, and optionally also substituted by 1 to 3 substituents selected from the previously mentioned substituent group a or substituent group a' (for example, a non-aromatic heterocyclic group containing divalent nitrogen represented by the following formula: where each symbol is as defined above, and optionally also replaced by 1 to 3 substituents selected from the substituent group to be Petition 870250102069, dated 07 / 11 / 2025, pp. 548 / 861 107 / 389 or the substitute group ' mentioned above); and R is a 2-(E)-phenylthenyl group optionally substituted by 1 to 3 substituents selected from the group consisting of a halogen atom, a C1-6 alkyl group optionally substituted by halogen atoms, and a pentafluorosulfanyl group, or a pharmaceutically acceptable salt thereof. [Compound (IK')]

[00152] Compound (I), in which A is a non-aromatic heterocyclic group containing divalent nitrogen, represented by the following formula: where a wavy line is a binding site of the group represented by the chemical formula mentioned above, a bond represented by Petition 870250102069, dated 07 / 11 / 2025, pp. 549 / 861 108 / 389 is a single bond or a double bond, each Y is independently a nitrogen atom or CR3 (where R3 is a hydrogen atom or a C1-6 alkyl group), Z is an oxygen atom, a sulfur atom, NR4 or CR5R6 (where R4, R5 and R6 are each independently a hydrogen atom or a C1-6 alkyl group), n is an integer from 0 to 2, m is an integer from 0 to 2, n1 and n2 are each independently an integer from 0 to 2, m1 and m2 are each independently an integer from 0 to 2, “ is a bonding site with a carbonyl group, and *** is a bonding site with the L group, and optionally also substituted by 1 to 3 substituents selected from the previously mentioned substituent group a or substituent group a' (for example, a non-aromatic heterocyclic group containing divalent nitrogen represented by the following formula: where each symbol is as defined above, and optionally also replaced by 1 to 3 substituents selected from the substituent group to be Petition 870250102069, dated 07 / 11 / 2025, pp. 550 / 861 109 / 389 or substituent group a' mentioned above); and other symbols are as defined for the above-mentioned [compound (IK)], or a pharmaceutically acceptable salt thereof. [Compound (IL)]

[00153] Compound (I), in which R1 is a carboxy group, an optionally substituted C1-6 alkoxy-carbonyl group, or an optionally substituted carbamoyl group; L is a C1-6 alkylene group optionally having, in the interior or at the end, one or more divalent groups selected from the group consisting of -NR2- (wherein R2 is a hydrogen atom or a C1-6 alkyl group), -O-, -S-, -C(=O)-, a C6-10 arylene group (for example, 1,2-phenylene, 1,3-phenylene, 1,4-phenylene), a C3-10 cycloalkylene group (for example, cyclobutane-1,3-di-yl, cyclopropane-1,2-di-yl, cyclopropane-1,1-di-yl, cyclopentane-1,2-di-yl, cyclohexane-1,2-di-yl, bicyclo[2.1.[1]hexane-1,2-di-yl), C2-6 alkylene group, and a 3- to 8-membered divalent non-aromatic heterocyclic group (e.g., azetidine-1,3-di-yl, pyrrolidine-1,3-di-yl, pyrrolidine-1,2-di-yl, piperidine-1,2-di-yl, piperidine-1,4-di-yl, azepane-1,2-di-yl), and optionally also substituted by 1 to 3 substituents selected from the aforementioned substituent group a or substituent group a'; a C6-10 arylene group (e.g., 1,2-phenylene, 1,3-phenylene, 1,4-phenylene) optionally also substituted by 1 to 3 substituents selected from the previously mentioned substituent group a or substituent group a'; a C3-10 cycloalkylene group (e.g., cyclobutane-1,3-di-yl, cyclopropane-1,2-di-yl, cyclopropane-1,1-di-yl, cyclopentane-1,2-di-yl, cyclohexane-1,2-di-yl, bicyclo[2.1.1]hexane-1,2-di-yl) optionally also replaced by 1 to 3 substituents selected from the group. Petition 870250102069, dated 07 / 11 / 2025, pp. 551 / 861 110 / 389 substituent a or substituent group a' previously mentioned a C2-4 alkynylene group optionally also substituted by 1 to 3 substituents selected from the substituent group a or substituent group a' previously mentioned or a divalent non-aromatic heterocyclic group of 3 to 8 members (for example, azetidine-1,3-di-yl, pyrrolidine-1,3-di-yl, pyrrolidine-1,2-di-yl, piperidine-1,2-di-yl, piperidine-1,4-di-yl, azepane-1,2-di-yl) optionally also substituted by 1 to 3 substituents selected from the substituent group a or substituent group a' previously mentioned; A is a non-aromatic heterocyclic group containing divalent nitrogen, represented by the following formula: wherein each symbol is as defined above, and optionally also replaced by 1 to 3 substituents selected from the previously mentioned substituent group a or substituent group a' (for example, a non-aromatic heterocyclic group containing divalent nitrogen represented by the following formula: Petition 870250102069, dated 07 / 11 / 2025, pp. 552 / 861 111 / 389 where each symbol is as defined above, and optionally also replaced by 1 to 3 substituents selected from the substituent group a or substituent group a' previously mentioned); and R is a 2-(E)-phenylthenyl group optionally substituted by 1 to 3 substituents selected from the group consisting of a halogen atom, a C1-6 alkyl group optionally substituted by halogen atoms, and a pentafluorosulfanyl group, or a pharmaceutically acceptable salt thereof. [Compound (IM)]

[00154] Compound (I), wherein R1 is a carboxy group, an optionally substituted C1-6 alkoxy-carbonyl group, or an optionally substituted carbamoyl group; L is a C1-6 alkylene group optionally having, within or at the end, one or more divalent groups selected from the group consisting of -NR2- (wherein R2 is a hydrogen atom or a C1-6 alkyl group), -O-, -S-, a C3-10 cycloalkylene group (for example, cyclobutane-1,3-di-yl, cyclopropane-1,2-di-yl, cyclopropane). Petition 870250102069, dated 07 / 11 / 2025, page. 112 / 389 1,1-di-yl, cyclopentane-1,2-di-yl, cyclohexane-1,2-di-yl, bicyclo[2.1.1]hexane-1,2-di-yl), and a divalent non-aromatic heterocyclic group of 3 to 8 members (for example, azetidine-1,3-di-yl, pyrrolidyne-1,3-di-yl, pyrrolidyne-1,2-di-yl, piperidyne-1,2-di-yl, piperidine-1,4-di-yl, azepane-1,2-di-yl), and optionally also substituted by 1 to 3 substituents selected from the previously mentioned substituent group a or substituent group a' a C3-10 cycloalkylene group (for example, cyclobutane-1,3-di-yl, cyclopropane-1,2-di-yl, cyclopropane-1,1-di-yl, cyclopentane-1,2-di-yl, cyclohexane-1,2-diyl, bicyclo[2.1.1 ]hexane-1,2-di-yl) optionally also substituted by 1 to 3 substituents selected from the previously mentioned substituent group a or substituent group a' or a divalent non-aromatic heterocyclic group of 3 to 8 members (e.g., azetidine-1,3-di-yl, pyrrolidine-1,3-di-yl, pyrrolidine-1,2-di-yl, piperidine-1,2-di-yl, piperidine-1,4-di-yl, azepane-1,2-di-yl) optionally also substituted by 1 to 3 substituents selected from the previously mentioned substituent group a or substituent group a'; A is a non-aromatic heterocyclic group containing divalent nitrogen, represented by the following formula: Petition 870250102069, dated 07 / 11 / 2025, pp. 554 / 861 113 / 389 where each symbol is as defined above, and optionally also replaced by 1 to 3 substituents selected from the previously mentioned substituent group a or substituent group a' (for example, a non-aromatic heterocyclic group containing divalent nitrogen represented by the following formula: ( / ] or where each symbol is as defined above, and optionally also replaced by 1 to 3 substituents selected from the substituent group a or substituent group a' mentioned above); and R is a 2-(E)-phenylthenyl group optionally substituted by 1 to 3 substituents selected from the group consisting of a halogen atom, a C1-6 alkyl group optionally substituted by halogen atoms, and a pentafluorosulfanyl group, or a pharmaceutically acceptable salt thereof. [Compound (IN)]

[00155] Compound (I), where R1 is a carboxy group, an optionally substituted C1-6 alkoxy-carbonyl group, or an optionally substituted carbamoyl group; L is a C1-6 alkylene group optionally also Petition 870250102069, dated 07 / 11 / 2025, pp. 555 / 861 114 / 389 replaced by 1 to 3 substituents selected from substituent group a or substituent group a' previously mentioned; A is a non-aromatic heterocyclic group containing divalent nitrogen, represented by the following formula: wherein each symbol is as defined above, and optionally also replaced by 1 to 3 substituents selected from the previously mentioned substituent group a or substituent group a' (for example, a non-aromatic heterocyclic group containing divalent nitrogen represented by the following formula: Petition 870250102069, dated 07 / 11 / 2025, pp. 556 / 861 115 / 389 ( / Y ] OR where each symbol is as defined above, and optionally also replaced by 1 to 3 substituents selected from the substituent group a or substituent group a' mentioned previously); and R is a 2-(E)-phenylthenyl group optionally substituted by 1 to 3 substituents selected from the group consisting of a halogen atom, a C1-6 alkyl group optionally substituted by halogen atoms, and a pentafluorosulfanyl group, or a pharmaceutically acceptable salt thereof. [Composite (IP)]

[00156] Compound (I), in which R1 is a carboxy group, an optionally substituted C1-6 alkoxy-carbonyl group, or an optionally substituted carbamoyl group; L is a C1-6 alkylene group, a Ce-w arylene group, a C3-14 cycloalkylene group, a C2-6 alkenylene group, a C2-6 alkynylene group, or a divalent non-aromatic heterocyclic group of 3 to 14 members, each of which optionally has, in the interior or at the end, one or more divalent groups selected from the group consisting of -NR2- (where R2 is a hydrogen atom or a C1-6 alkyl group), -O-, -S-, -C(=O)-, a C1-6 alkylene group, a Ce-w group Petition 870250102069, dated 07 / 11 / 2025, pp. 557 / 861 116 / 389 arylene, a C3-4 cycloalkylene group, a C2-6 alkenylene group, a C2-6 alkynylene group and a divalent non-aromatic heterocyclic group of 3 to 14 members, each of which is optionally also substituted by 1 to 3 substituents selected from the substituent group a or substituent group a' mentioned above; A is a non-aromatic heterocyclic group containing divalent nitrogen, represented by the following formula: wherein each symbol is as defined above, and optionally also replaced by 1 to 3 substituents selected from the previously mentioned substituent group a or substituent group a' (for example, a non-aromatic heterocyclic group containing divalent nitrogen represented by the following formula: wherein each symbol is as defined above, and optionally also substituted by 1 to 3 substituents selected from the substituent group a or substituent group a' previously mentioned, provided that when Z is CR5R6, the optionally substituted substituent is selected from the group consisting of, among the substituents in the substituent group a or substituent group a' previously mentioned, a Ce-14 hydrocarbocyclic group optionally substituted by 1 to 3 substituents selected from the substituent group b or substituent group b'; an aromatic heterocyclic group of 5 to 14 members optionally substituted by 1 to 3 substituents selected from the substituent group b or substituent group b'; and a non-aromatic heterocyclic group of 3 to Petition 870250102069, dated 07 / 11 / 2025, pp. 558 / 861 117 / 389 members optionally replaced by 1 to 3 substitutes selected from substitute group b or substitute group b'); and R is a 2-(E)-phenylthenyl group optionally substituted by 1 to 3 substituents selected from the group consisting of a halogen atom, a C1-6 alkyl group optionally substituted by halogen atoms, and a pentafluorosulfanyl group, or a pharmaceutically acceptable salt thereof. [Compound (IQ)]

[00157] Compound (I), in which R1 is a carboxy group, an optionally substituted C1-6 alkoxy-carbonyl group, or an optionally substituted carbamoyl group; L is a C1-6 alkylene group optionally having, in the interior or at the end, one or more divalent groups selected from the group consisting of -NR2- (wherein R2 is a hydrogen atom or a C1-6 alkyl group), -O-, -S-, a C3-10 cycloalkylene group (for example, cyclobutane-1,3-diyl, cyclopropane-1,2-diyl, cyclopropane-1,1-diyl, cyclopentane-1,2-diyl, cyclohexane-1,2-diyl, bicyclo[2.1.1]hexane-1,2-diyl), and a divalent non-aromatic heterocyclic group of 3 to 8 members (for example, azetidine-1,3-diyl, pyrrolidine-1,3-diyl, pyrrolidine-1,2-diyl, piperidine-1,2-diyl, piperidine-1,4-diyl, azepane-1,2-di-yl), and optionally also substituted by 1 to 3 substituents selected from the previously mentioned substituent group a or substituent group a' a C3-10 cycloalkylene group (for example, cyclobutane-1,3-di-yl, cyclopropane-1,2-di-yl, cyclopropane-1,1-di-yl, cyclopentane-1,2-di-yl, cyclohexane-1,2-di-yl, bicyclo[2.1.1]hexane-1,2-di-yl) optionally also substituted by 1 to 3 substituents selected from the previously mentioned substituent group a or substituent group a' or a divalent non-aromatic heterocyclic group of 3 to 8 members (e.g. Petition 870250102069, dated 07 / 11 / 2025, pp. 559 / 861 118 / 389 example, azetidine-1,3-di-yl, pyrrolidine-1,3-di-yl, pyrrolidine-1,2-di-yl, piperidin-1,2-di-yl, piperidin-1,4-di-yl, azepane-1,2-di-yl) optionally also substituted by 1 to 3 substituents selected from the previously mentioned substituent group a or substituent group a'; A is a non-aromatic heterocyclic group containing divalent nitrogen, represented by the following formula: wherein each symbol is as defined above, and optionally also replaced by 1 to 3 substituents selected from the previously mentioned substituent group a or substituent group a' (for example, a non-aromatic heterocyclic group containing divalent nitrogen represented by the following formula: wherein each symbol is as defined above, and optionally also substituted by 1 to 3 substituents selected from the substituent group a or substituent group a' previously mentioned, provided that when Z is CR5R6, the optionally substituted substituent is selected from the group consisting of, among the substituents in the substituent group a or substituent group a' previously mentioned, a Ce-14 hydrocarbocyclic group optionally substituted by 1 to 3 substituents selected from the substituent group b or substituent group b'; an aromatic heterocyclic group of 5 to 14 members optionally substituted by 1 to 3 substituents selected from the substituent group b Petition 870250102069, dated 07 / 11 / 2025, pages 560 / 861 119 / 389 or substituent group b'; and a non-aromatic heterocyclic group of 3 to 14 members optionally substituted by 1 to 3 substituents selected from substituent group b or substituent group b'); and R is a 2-(E)-phenylthenyl group optionally substituted by 1 to 3 substituents selected from the group consisting of a halogen atom, a C1-6 alkyl group optionally substituted by halogen atoms, and a pentafluorosulfanyl group, or a pharmaceutically acceptable salt thereof. [Compound (IR)]

[00158] Compound (I), in which R1 is a carboxy group, an optionally substituted C1-6 alkoxy-carbonyl group, or an optionally substituted carbamoyl group; L is a C1-6 alkylene group optionally having, in the interior or at the end, one or more divalent groups selected from the group consisting of -NR2- (wherein R2 is a hydrogen atom or a C1-6 alkyl group), -O-, -S-, a C3-10 cycloalkylene group (for example, cyclobutane-1,3-diyl, cyclopropane-1,2-diyl, cyclopropane-1,1-diyl, cyclopentane-1,2-diyl, cyclohexane-1,2-diyl, bicyclo[2.1.1]hexane-1,2-diyl), and a divalent non-aromatic heterocyclic group of 3 to 8 members (for example, azetidine-1,3-diyl, pyrrolidine-1,3-diyl, pyrrolidine-1,2-diyl, piperidine-1,2-diyl, piperidine-1,4-diyl, azepane-1,2-di-yl), and optionally also substituted by 1 to 3 substituents selected from the previously mentioned substituent group a or substituent group a' a C3-10 cycloalkylene group (for example, cyclobutane-1,3-di-yl, cyclopropane-1,2-di-yl, cyclopropane-1,1-di-yl, cyclopentane-1,2-di-yl, cyclohexane-1,2-di-yl, bicyclo[2.1.1]hexane-1,2-di-yl) optionally also replaced by 1 to 3 substituents selected from the previously mentioned substituent group a or substituent group a'. Petition 870250102069, dated 07 / 11 / 2025, pages 561 / 861 120 / 389 a divalent non-aromatic heterocyclic group of 3 to 8 members (for example, azetidine-1,3-di-yl, pyrrolidine-1,3-di-yl, pyrrolidine-1,2-di-yl, piperidyne-1,2-di-yl, piperidyne-1,4-di-yl, azepane-1,2-di-yl) optionally also substituted by 1 to 3 substituents selected from the previously mentioned substituent group a or substituent group a'; A is a non-aromatic heterocyclic group containing divalent nitrogen, represented by the following formula: wherein each symbol is as defined above, and optionally also replaced by 1 to 3 substituents selected from the substituent group a or substituent group a' previously mentioned; and R is a 2-(E)-phenylthenyl group optionally substituted by 1 to 3 substituents selected from the group consisting of a halogen atom, a C1-6 alkyl group optionally substituted by halogen atoms, and a pentafluorosulfanyl group, or a pharmaceutically acceptable salt thereof. [Compound (IS)]

[00159] Compound (I), in which R1 is a carboxy group, an optionally substituted C1-6 alkoxy-carbonyl group, or an optionally substituted carbamoyl group; L is a C1-6 alkylene group optionally also substituted by 1 to 3 substituents selected from the substituent group a or substituent group a' mentioned above; A is a non-aromatic heterocyclic group containing divalent nitrogen, represented by the following formula: Petition 870250102069, dated 07 / 11 / 2025, pp. 562 / 861 121 / 389 where each symbol is as defined above, and optionally also replaced by 1 to 3 substituents selected from the substituent group a or substituent group a' mentioned previously; and R is a 2-(E)-phenylthenyl group optionally substituted by 1 to 3 substituents selected from the group consisting of a halogen atom, a C1-6 alkyl group optionally substituted by halogen atoms, and a pentafluorosulfanyl group, or a pharmaceutically acceptable salt thereof. [Compound (IT)]

[00160] Compound (I), in which R1 is a carboxy group, an optionally substituted C1-6 alkoxy-carbonyl group, or an optionally substituted carbamoyl group; L is a C1-6 alkylene group optionally having, in the interior or at the end, one or more divalent groups selected from the group consisting of -NR2- (wherein R2 is a hydrogen atom or a C1-6 alkyl group), -O-, -S-, a C3-10 cycloalkylene group (for example, cyclobutane-1,3-diyl, cyclopropane-1,2-diyl, cyclopropane-1,1-diyl, cyclopentane-1,2-diyl, cyclohexane-1,2-diyl, bicyclo[2.1.1]hexane-1,2-diyl), and a divalent non-aromatic heterocyclic group of 3 to 8 members (for example, azetidine-1,3-diyl, pyrrolidine-1,3-diyl, pyrrolidine-1,2-diyl, piperidine-1,2-diyl, piperidine-1,4-diyl, azepane-1,2-di-yl), and optionally also substituted by 1 to 3 substituents selected from the previously mentioned substituent group a or substituent group a' a C3-10 cycloalkylene group (for example, cyclobutane-1,3-di-yl, cyclopropane-1,2-di-yl, cyclopropane-1,1-di-yl, cyclopentane-1,2-di-yl, cyclohexane-1,2-di-yl, bicyclo[2.1.1 ]hexane-1,2-di-yl) optionally also replaced by 1 to 3 substituents selected from the group. Petition 870250102069, dated 07 / 11 / 2025, pp. 563 / 861 122 / 389 substituent a or substituent group a' previously mentioned or a divalent non-aromatic heterocyclic group of 3 to 8 members (for example, azetidine-1,3-di-yl, pyrrolidine-1,3-di-yl, pyrrolidine-1,2-di-yl, piperidyne-1,2-di-yl, piperidyne-1,4-di-yl, azepane-1,2-di-yl) optionally also substituted by 1 to 3 substituents selected from the substituent group a or substituent group a' previously mentioned; A is a non-aromatic heterocyclic group containing divalent nitrogen, represented by the following formula: wherein each symbol is as defined above, and optionally also replaced by 1 to 3 substituents selected from the substituent group a or substituent group a' previously mentioned; and R is a 2-(E)-phenylthenyl group optionally substituted by 1 to 3 substituents selected from the group consisting of a halogen atom, a C1-6 alkyl group optionally substituted by halogen atoms, and a pentafluorosulfanyl group, or a pharmaceutically acceptable salt thereof. [Compound (IU)]

[00161] Compound (I), in which R1 is a carboxy group, an optionally substituted C1-6 alkoxy-carbonyl group, or an optionally substituted carbamoyl group; L is a C1-6 alkylene group optionally also substituted by 1 to 3 substituents selected from the substituent group a or substituent group a' mentioned above; A is a non-aromatic heterocyclic group containing divalent nitrogen, represented by the following formula: Petition 870250102069, dated 07 / 11 / 2025, pp. 564 / 861 123 / 389 where each symbol is as defined above, and optionally also replaced by 1 to 3 substituents selected from the substituent group a or substituent group a' mentioned previously; and R is a 2-(E)-phenylthenyl group optionally substituted by 1 to 3 substituents selected from the group consisting of a halogen atom, a C1-6 alkyl group optionally substituted by halogen atoms, and a pentafluorosulfanyl group, or a pharmaceutically acceptable salt thereof. [Compound (IV)]

[00162] Compound (I), in which R1 is a carboxy group, an optionally substituted C1-6 alkoxy-carbonyl group, or an optionally substituted carbamoyl group; L is a C1-6 alkylene group optionally having, in the interior or at the end, one or more divalent groups selected from the group consisting of -NR2- (wherein R2 is a hydrogen atom or a C1-6 alkyl group), -O-, -S-, a C3-10 cycloalkylene group (for example, cyclobutane-1,3-di-yl, cyclopropane-1,2-di-yl, cyclopropane-1,1-di-yl, cyclopentane-1,2-di-yl, cyclohexane-1,2-di-yl, bicyclo[2.1.1]hexane-1,2-di-yl), and a 3- to 8-membered divalent non-aromatic heterocyclic group (for example, azetidine-1,3-di-yl, pyrrolidyne-1,3-di-yl, pyrrolidyne-1,2-di-yl, piperidyne-1,2-di-yl, piperidine-1,4-di-yl, azepane-1,2-di-yl), and optionally also substituted by 1 to 3 substituents selected from the previously mentioned substituent group a or substituent group a' a C3-10 cycloalkylene group (e.g., cyclobutane-1,3-di-yl, Petition 870250102069, dated 07 / 11 / 2025, pages 565 / 861 124 / 389 cyclopropane-1,2-di-yl, cyclopropane-1,1-di-yl, cyclopentane-1,2-di-yl, cyclohexane-1,2-di-yl, bicyclo[2.1.1]hexane-1,2-di-yl) optionally also substituted by 1 to 3 substituents selected from the substituent group a or substituent group a' previously mentioned or a divalent non-aromatic heterocyclic group of 3 to 8 members (for example, azetidine-1,3-di-yl, pyrrolidine-1,3-di-yl, pyrrolidine-1,2-di-yl, piperidinate-1,2-di-yl, piperidinate-1,4-di-yl, azepane-1,2-di-yl) optionally also substituted by 1 to 3 substituents selected from the substituent group a or substituent group a' previously mentioned; A is a non-aromatic heterocyclic group containing divalent nitrogen, represented by the following formula: wherein each symbol is as defined above, and optionally also replaced by 1 to 3 substituents selected from the substituent group a or substituent group a' previously mentioned; and R is a 2-(E)-phenylthenyl group optionally substituted by 1 to 3 substituents selected from the group consisting of a halogen atom, a C1-6 alkyl group optionally substituted by halogen atoms, and a pentafluorosulfanyl group, or a pharmaceutically acceptable salt thereof. [Compound (IW)]

[00163] Compound (I), in which R1 is a carboxy group, an optionally substituted C1-6 alkoxy-carbonyl group, or an optionally substituted carbamoyl group; L is a C1-6 alkylene group optionally also substituted by 1 to 3 substituents selected from the substituent group. Petition 870250102069, dated 07 / 11 / 2025, pp. 566 / 861 125 / 389 or the substitute group 'a' mentioned above; A is a non-aromatic heterocyclic group containing divalent nitrogen, represented by the following formula: wherein each symbol is as defined above, and optionally also replaced by 1 to 3 substituents selected from the substituent group a or substituent group a' previously mentioned; and R is a 2-(E)-phenylthenyl group optionally substituted by 1 to 3 substituents selected from the group consisting of a halogen atom, a C1-6 alkyl group optionally substituted by halogen atoms, and a pentafluorosulfanyl group, or a pharmaceutically acceptable salt thereof.

[00164] Preferred specific examples of compound (I) are the compounds of Examples 1 to 403 mentioned below (compound (1-1) to compound (I-403)), or pharmaceutically acceptable salts thereof.

[00165] Among them, a compound selected from the group consisting of 2-[2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]-3,4-dihydro-1H-isoquinolin-6-yl]acetic acid; acid 3-[2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]3,4-di-hydro-1H-isoquinolin-6-yl]propanoic acid; / V, / V-dimethyl-3-[5-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-6,7-di-hydro-4H-pyrazolo[1,5-a]pyrazine-3-yl]propanamide; Acid 1 -[7-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]6,8-di-hydro-5H-2,7-naphthyridine-3-yl]piperidine-4-carboxylic; acid 3-[3-bromo-5-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-6,7-di-hydro-4H-pyrazolo[1,5-a]pyrazine-2-yl]propanoic; acid 2-[[2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]Petition 870250102069, dated 07 / 11 / 2025, p. 567 / 861 126 / 389 3,4-di-hydro-1H-isoquinolin-6-yl]oxy]acetic acid; acid 2-[2-[2-[[(E)-3-[4-(pentafluoro-À6-sulfanyl)phenyl]prop-2-enoyl]amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid (1R*,2R*)-2-[2-[2-[[(E)-3-[4-(trifluoromethyl)feml]prop-2enoyl]amino] acetyl]-3,4-di-hydro-1H-isoquinoline-6-yl]cyclopropane-1carboxylic dosmores mesomers and both 2-[2-[2-[[(E)-3-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]3,4-di-hydro-1H-isoquinolin-6-yl]propanoic acid; acid 2-[7-fluoro-2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; acid 2-[8-fluoro-2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; acid 2-[7-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]6,8-di-hydro-5H-2,7-naphthyridine-3-yl]acetic acid; acid 3-[3-bromo-5-[2-[[(E)-3-[4-(pentafluoro-À6-sulfanyl)phenyl]prop-2enoyl]amino] acetyl]-6,7-di-hydro-4H-pyrazolo[1,5-a]pyrazin-2yl]propanoic; acid 2-[2-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; acid 2-[[2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]3,4-di-hydro -1H-isoquinolin-6-yl]amino]acetic; Acid 2-[2-[2-[[(E)-3-(4-iodophenyl)prop-2-enoyl]amino] acetyl]-3,4-di-hydro1H-isoquinolin-6-yl]acetic acid; acid 2-[5-fluoro-2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; acid 2-[8-chloro-2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; acid 2-[8-fluoro-2-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2enoyl]amino]acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl] acetic acid; acid 2-[8-cyano-2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] Petition 870250102069, dated 07 / 11 / 2025, p. 568 / 861 127 / 389 acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid 2-[8-fluoro-2-[2-[[(E)-3-(2-fluoro-4-iodophenyl)prop-2-enoyl]amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid 2-[8-fluoro-2-[2-[[(E)-3-(4-iodophenyl)prop-2-enoyl]amino] acetyl]-3,4di-hydro-1H-isoquinolin-6-yl]acetic acid; acid 2-[8-chloro-2-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2enoyl]amino]acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl] acetic acid; acid 2-[[5-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]6,7-di-hydro-4H-[1,3]thiazolo[5,4-c]pyridin-2-yl]sulfanyl] acetic acid; acid 2-[7-chloro-2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; acid 2-[8-cyano-2-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2enoyl]amino]acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; ácido 2-[5-cloro-2-[2-[[(E)-3-[2-fluoro-4-(trifluorometil)fenil]prop-2enoil]amino] acetil]-3,4-di-hidro-1H-isoquinolin-6-il] acetic acid; (E)-N-[2-[6-(2-amino-2-oxoethyl)-3,4-di-hidro-1H-isoquinolin-2-yl]-2oxoethyl]-3-[4-(trifluoromethyl)phenyl]prop-2-enamide; ácido 2-[5-[2-[[(E)-3-[4-(trifluorometil)fenil]prop-2-enoyl]amino] acetil]6,7-di-hidro-4H-[1,3]thiazolo[4,5-c]piridin-2-il] acetic acid; (E)-N-[2-[6-[2-(methylamino)-2-oxoethyl]-3,4-di-hidro-1H-isoquinolin-2-yl]-2oxoethyl]-3-[4-(trifluoromethyl)phenyl]prop-2-enamida; 4-[4-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-3-phenylpiperazin-1-yl]butanoic acid and both enantiômeros dos mesmos; 2-[[1-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]2,3-di-hidroindol-4-yl]óxi]acetic acid; 1-[1-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2enoyl]amino]acetyl]piperidin-3-yl]biciclo[2.1.1]hexano-5-carboxylic acid; 2-[[8-fluoro-2-[2-[[(E)-3-[4-(trifluorometil)fenil]prop-2-enoyl]amino] acetyl]-3,4-di-hidro-1H-isoquinolin-6-yl]óxi]-2- metilpropanoico acid; Petition 870250102069, 07 / 11 / 2025, pág. 569 / 861 128 / 389 3-[[8-fluoro-2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-3,4-di-hidro-1H-isoquinolin-6-yl]óxi]-2,2-dimethylpropanoic acid; 4-[4-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-2-methylpiperazin-1-yl]butanoic acid; 4-[(3S)-3-(4-bromophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop- 2- enoyl]amino]acetyl]piperazin-1-yl]butanoic acid; 4-[3-(3-bromophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid; 4-[3-(4-chlorophenyl)-4-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid; 3-[[3-(4-chlorophenyl)-4-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop2-enoyl]amino]acetyl]piperazin-1-yl]methyl]cyclobutane-1-carboxylic acid and both enantiômeros dos mesmos; 4-[3-(4-chlorophenyl)-4-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop2-enoyl]amino]acetyl]piperazin-1-yl]-2,2-dimethylbutanoic acid; 4-[3-(3-cyclopropylphenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid; 4-[3-(4-chlorophenyl)-4-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid and both enantiômeros dos mesmos; 4-[(2R,5S)-4-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2enoyl]amino]acetyl]-2-methyl-5-phenylpiperazin-1-yl]butanoic acid; 4-[(3S)-3-(4-cyclopropylphenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid; 4-[3-(4-chloro-3-fluorophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid; 4-[(2R,5S)-5-(3,4-difluorophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-2-methylpiperazin-1yl]butanoic acid; ácido 4-[(2R,5S)-5-(3,4-difluorophenyl)-2-methyl-4-[2-[[(E)-3-[4Petition 870250102069, dated 07 / 11 / 2025, pág. 570 / 861 129 / 389 (trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid; 4-[(2R,5S)-5-(4-chlorophenyl)-4-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop2-enoyl]amino]acetyl]-2-methylpiperazin-1-yl]butanoic acid; 3-[(2R,5S)-5-(4-chlorophenyl)-4-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop2-enoyl]amino] acetyl]-2-methylpiperazin-1-yl] propanoic acid; 4-[(2R,5S)-5-(4-chlorophenyl)—4—[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-2-methylpiperazin-1yl]butanoic acid; 4-[(2R,5S)-5-(4-fluorophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]-2-methylpiperazin-1yl]butanoic acid; 3-[(2R,5S)-5-(4-chlorophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]-2-methylpiperazin-1-yl]propanoic acid; 4-[(2R,5S)-5-(3-fluorophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]-2-methylpiperazin-1yl]butanoic acid; 4-[(2R,5S)-2-ethyl-4-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop2-enoyl]amino]acetyl]-5-phenylpiperazin-1-yl]butanoic acid; and 4-[(2R,5S)-4-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]-2-methyl-5-phenylpiperazin-1-yl]-2,2-dimethylbutanoic acid, or a pharmaceutically acceptable salt thereof, of which a compound selected from the group consisting of 2-[2-[2-[[(E)3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]-3,4-dihydro-1-Hisoquinolin-6-yl]acetic acid is preferred; acid 3-[2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]3,4-di-hydro-1H-isoquinolin-6-yl]propanoic acid; N,N-dimethyl-3-[5-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-6,7-di-hydro-4H-pyrazolo[1,5-a]pyrazine-3-yl]propanamide; acid 2-[2-[2-[[(E)-3-[4-(pentafluoro-A6-sulfanyl)phenyl]prop-2-enoyl]amino] Petition 870250102069, dated 07 / 11 / 2025, p. 571 / 861 130 / 389 acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid (1R*,2R*)-2-[2-[2-[[(E)-3-[4-(trifluoromethyl)feml]prop-2enoyl]amino] acetyl]-3,4-di-hydro-1H-isoquinoline-6-yl]cyclopropane-1carboxylic dosmores mesomers and both 2-[2-[2-[[(E)-3-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]3,4-di-hydro-1H-isoquinolin-6-yl]propanoic acid; acid 2-[7-fluoro-2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; acid 2-[8-fluoro-2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; acid 2-[2-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid 2-[2-[2-[[(E)-3-(4-iodophenyl)prop-2-enoyl]amino] acetyl]-3,4-di-hydro1H-isoquinolin-6-yl]acetic acid; acid 2-[5-fluoro-2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; acid 2-[8-chloro-2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; acid 2-[8-fluoro-2-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2enoyl]amino]acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl] acetic acid; acid 2-[8-cyano-2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid 2-[8-fluoro-2-[2-[[(E)-3-(2-fluoro-4-iodophenyl)prop-2-enoyl]amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; acid 2-[8-chloro-2-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2enoyl]amino]acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl] acetic acid; acid 2-[7-chloro-2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; acid 2-[5-chloro-2-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2enoyl]amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl] acetic acid; Petition 870250102069, dated 07 / 11 / 2025, p. 572 / 861 131 / 389 acid 2-[5-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]6,7-di-hydro-4H-[1,3]thiazolo[4,5-c]pyridin-2-yl] acetic acid; Acid 4-[(3S)-4-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2enoyl]amino]acetyl]-3-phenylpiperazine-1-yl]butanoic; 1-[1-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2enoyl]amino]acetyl]piperidin-3-yl]biciclo[2.1.1]hexano-5-carboxylic acid; 4-[(3S)-3-(4-bromophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid; 4-[3-(3-bromophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid; 4-[3-(4-chlorophenyl)-4-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid; 3-[[3-(4-chlorophenyl)-4-[2-[[rac-(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperazin-1yl]methyl]cyclobutane-1-carboxylic acid and both enantiômeros dos mesmos; 4-[3-(4-chlorophenyl)-4-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid and both enantiômeros dos mesmos; 4-[(2R,5S)-4-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2enoyl]amino]acetyl]-2-methyl-5-phenylpiperazin-1-yl]butanoic acid; 4-[(3S)-3-(4-cyclopropylphenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid; 4-[3-(4-chloro-3-fluorophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid; 4-[(2R,5S)-5-(3,4-difluorophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-2-methylpiperazin-1yl]butanoic acid; 4-[(2R,5S)-5-(3,4-difluorophenyl)-2-methyl-4-[2-[[(E)-3-[4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid; Ácido 4-[(2R,5S)-5-(4-chlorophenyl)-4-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]propPetição 870250102069, de 07 / 11 / 2025, pág. 573 / 861 132 / 389 2-enoyl]amino]acetyl]-2-methylpiperazine-1-yl]butanoic acid; 3-[(2R,5S)-5-(4-chlorophenyl)-4-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop2-enoyl]amino]acetyl]-2-methylpiperazin-1-yl]propanoic acid; 4-[(2R,5S)-5-(4-chlorophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]-2-methylpiperazin-1yl]butanoic acid; 4-[(2R,5S)-5-(4-fluorophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]-2-methylpiperazin-1yl]butanoic acid; 3-[(2R,5S)-5-(4-chlorophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]-2-methylpiperazin-1-yl]propanoic acid; 4-[(2R,5S)-5-(3-fluorophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]-2-methylpiperazin-1yl]butanoic acid; 4-[(2R,5S)-2-ethyl-4-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)pheml]prop2-enoyl]amino]acetyl]-5-phenylpiperazin-1-yl]butanoic acid; and Acid 4-[(2R,5S)-4-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)feml]prop-2enoyl]amino] acetyl]-2-methyl-5-phenylpiperazin-1-yl]-2,2-dimethyl acetyl pharmaceutical preferentio, or umethylbutanoic, or selected compound from the group consisting of acid 2-[7-fluoro2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-3,4-dihydro-1H-isoquinolin-6-yl]acetic acid; acid 2-[8-fluoro-2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; acid 2-[2-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; 2-[2-[2-[[(E)-3-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]3,4-di-hydro-1H-isoquinolin-6-yl]propanoic acid; Acid 2-[2-[2-[[(E)-3-(4-iodophenyl)prop-2-enoyl]amino] acetyl]-3,4-di-hydroPetition 870250102069, dated 07 / 11 / 2025, p. 574 / 861 133 / 389 1H-isoquinolin-6-yl]acetic acid; acid 2-[5-fluoro-2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; acid 2-[8-chloro-2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; acid 2-[8-fluoro-2-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2enoyl]amino]acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl] acetic acid; acid 2-[8-chloro-2-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2enoyl]amino]acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl] acetic acid; acid 2-[7-chloro-2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid 2-[5-chloro-2-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2enoyl]amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid 4-[(3S)-4-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2enoyl]amino]acetyl]-3-phenylpiperazine-1-yl]butanoic; 1 -[1-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2enoyl]amino]acetyl]piperidin-3-yl]biciclo[2.1.1]hexano-5-carboxylic acid; 4-[(3S)-3-(4-bromophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid; 4-[3-(3-bromophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid; 4-[3-(4-chlorophenyl)-4-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid; 4-[(2R,5S)-4-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2enoyl]amino]acetyl]-2-methyl-5-phenylpiperazin-1-yl]butanoic acid; 4-[(3S)-3-(4-cyclopropylphenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid; 4-[(2R,5S)-5-(3,4-difluorophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-2-methylpiperazin-1yl]butanoic acid; Petition 870250102069, dated 07 / 11 / 2025, pp. 575 / 861 134 / 389 4-[(2R,5S)-5-(3,4-difluorophenyl)-2-methyl-4-[2-[[(E)-3-[4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid; 4-[(2R,5S)-5-(4-chlorophenyl)-4-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop2-enoyl]amino]acetyl]-2-methylpiperazin-1-yl]butanoic acid; 3-[(2R,5S)-5-(4-chlorophenyl)-4-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop2-enoyl]amino]acetyl]-2-methylpiperazin-1-yl]propanoic acid; 4-[(2R,5S)-5-(4-chlorophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]-2-methylpiperazin-1yl]butanoic acid; 4-[(2R,5S)-5-(4-fluorophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]-2-methylpiperazin-1yl]butanoic acid; 3-[(2R,5S)-5-(4-chlorophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]-2-methylpiperazin-1-yl]propanoic acid; 4-[(2R,5S)-5-(3-fluorophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]-2-methylpiperazin-1yl]butanoic acid; 4-[(2R,5S)-2-ethyl-4-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop2-enoyl]amino]acetyl]-5-phenylpiperazin-1-yl]butanoic acid; and 4-[(2R,5S)-4-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]-2-methyl-5-phenylpiperazin-1-yl]-2,2-dimethylbutanoic acid, or a pharmaceutically acceptable salt of which is even more preferred, and a compound selected from the group consisting of 2-[2-[2-[[(E)3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]-3,4-dihydro-1-Hisoquinolin-6-yl]acetic acid; 3-[2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]3,4-dihydro-1H-isoquinolin-6-yl]propanoic acid; N,N-dimethyl-3-[5-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] Petition 870250102069, dated 07 / 11 / 2025, pp. 576 / 861 135 / 389 acetyl]-6,7-di-hydro-4H-pyrazolo[1,5-a]pyrazine-3-yl]propanamide; acid 2-[2-[2-[[(E)-3-[4-(pentafluoro-À6-sulfanyl)phenyl]prop-2-enoyl]amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; 2-[2-[2-[[(E)-3-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]3,4-di-hydro-1H-isoquinolin-6-yl]propanoic acid; acid 2-[8-fluoro-2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; acid 2-[2-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; acid 2-[8-chloro-2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; acid 2-[8-chloro-2-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2enoyl]amino]acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; 4-[(3R)-3-(4-chlorophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid; 4-[(2R,5S)-4-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2enoyl]amino] acetyl]-2-methyl-5-phenylpiperazin-1-yl]butanoic acid; 3-[(2R,5S)-5-(4-chlorophenyl)-4-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2enoyl]amino]acetyl]-2-methylpiperazin-1-yl]propanoic acid; 3-[(2R,5S)-5-(4-chlorophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-2-methylpiperazin-1yl]propanoic acid; 4-[(2R,5S)-5-(3-fluorophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino] acetyl]-2-methylpiperazin-1yl]butanoic acid; 4-[(2R,5S)-2-ethyl-4-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]-5-phenylpiperazin-1-yl]butanoic acid; and 4-[(3S)-3-(4-cyclopropylphenyl)-4-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid, or a pharmaceutically acceptable salt of which is particularly Petition 870250102069, dated 07 / 11 / 2025, pp. 577 / 861 136 / 389 preferred.

[00166] When compound (I) of the present invention has asymmetric carbon atom(s) in the molecule, it can exist as multiple stereoisomers (i.e., diastereomeric isomers, optical isomers) based on said asymmetric carbon atom(s), and the present invention includes any of these stereoisomers and mixtures containing these multiple stereoisomers in any ratio. Isomers due to conformation or tautomerism can also be formed, and such isomers or mixtures thereof are also included in compound (I) of the present invention.

[00167] The compound (I) of the present invention can be labeled or substituted with isotopes (e.g., 2H, 3H, 13C, 14C, 15N, 18F, 32P, 35S, 123I, 125I, i3i|, etc.). Isotope-labeled or isotopically substituted compounds can be used as tracers (PET tracers) for, for example, Single Photon Emission Computed Tomography (SPECT) and Positron Emission Tomography (PET) and are useful in the field of medical diagnosis and similar applications.

[00168] The compound (I) of the present invention or a pharmaceutically acceptable salt thereof can be crystalline and can have a single crystal form or a mixture of several crystal forms.

[00169] The compound (I) of the present invention or a pharmaceutically acceptable salt thereof may also include intramolecular or adducted salts thereof and their solvates. Its solvates are those in which a solvent molecule is coordinated to compound (I) or to a salt thereof, and hydrates are also included. For example, hydrates, ethanol solvates or dimethyl sulfoxide solvates of compound (I) or of a salt thereof are included.

[00170] Compound (I) of the present invention can be a prodrug.

[00171] The prodrugs of compound (I) of the present invention are Petition 870250102069, dated 07 / 11 / 2025, pp. 578 / 861 137 / 389 compounds that are converted into compound (I) in vivo by reactions with enzymes or stomach acid. As a prodrug of compound (I), phosphate group monoesters or diesters may be considered, preferably whose ester functional groups have structures that are easily hydrolyzed or metabolized after administration to a patient.

[00172] A prodrug of compound (I) may be a monoester or diester of a phosphate group, whose ester functional group preferably has a structure that is readily hydrolyzed or metabolized after administration to the patient. Examples of ester functional groups of such prodrugs include optionally substituted C1-6 alkyl esters with acyloxy groups, phenyl esters, benzyl esters, and the like (see, Bioorganic Chemistry, 1984; 12: p. 118-129). In addition, as prodrugs other than the above monoesters or diesters of phosphate groups, see, for example, compounds with groups derived from phosphate groups, etc., as described in Current opinion in investigational drugs, 2006; 7: p. 109-117, J. Med. Chem. 1994; 37: p. 1857-1864, and J. Med. Chem. 2000; 43: pp. 4570-4574.

[00173] As another form of a prodrug of compound (I), for example, when compound (I) has an amino group, a compound in which the amino group is acylated, alkylated or phosphorylated (for example, the amino group of compound (I) is eicosanoylated, alanylated, pentylaminocarbonylated, (5-methyl-2-oxo-1,3-dioxolen-4yl)methoxycarbonylated, tetrahydrofurylated, pyrrolidylmethylated, pivaloyloxymethylated, acetoxymethylated, tert-butylated, etc.); when compound (I) has a hydroxyl group, a compound in which the hydroxyl group is acylated, alkylated, phosphorylated, borylated (for example, the hydroxyl group of compound (I) is acetylated, palmitoylated, propanoylated, pivaloylated, succinylated, fumarylated, alanylated, dimethylaminomethylcarbonylated, etc.); when compound (I) has a Petition 870250102069, dated 07 / 11 / 2025, pp. 579 / 861 138 / 389 carboxyl group, a compound in which the carboxyl group is esterified or amidated (for example, the carboxyl group of compound (I) is ethyl esterified, phenyl esterified, carboxymethyl esterified, dimethylaminomethyl esterified, pivaloyloxymethyl esterified, 1{(ethoxycarbonyl)oxy}ethyl esterified, phthalidyl esterified, (5-methyl-2-oxo-1,3-dioxolen-4-yl)methyl esterified, 1-{[(cyclohexyloxy)carbonyl]oxy}ethyl esterified, methylamidated, etc.). These compounds can be produced by methods known per se. Furthermore, the prodrugs of compound (I) can be hydrated or non-hydrated. The prodrugs of compound (I) can also be those that transform into compound (I) under physiological conditions, as described in “Molecular Design”, pp. 163-198 in “Development of Pharmaceuticals”, Vol. 7, published by Hirokawa Shoten 1990. Production methods for compound (I) of the present invention

[00174] The methods for producing compound (I) of the present invention or a pharmaceutically acceptable salt thereof are explained below.

[00175] As an example of the production method for compound (I), representative production methods (A) to (F) are described below. However, the production method is not limited to these. In addition, the following production methods and steps can be combined with each other.

[00176] Compound (I) (for example, compound (I-1) to compound (I403) described in the Examples mentioned below) can be produced by the following production methods (A) to (F), the Reference Examples mentioned below, Examples or a method analogous to them and similar.

[00177] Each starting material compound can form a salt if the reaction is not inhibited, and such salts are the same as compound (I). If a specific manufacturing method is not described, the compounds of Petition 870250102069, dated 07 / 11 / 2025, pages 580 / 861 139 / 389 starting materials can be readily obtained and used commercially, or can be manufactured according to known methods per se or analogous methods. The intermediates produced in the following manufacturing process can be isolated and purified by column chromatography, recrystallization, distillation or similar methods, or can be used in the following process without isolation.

[00178] The contents of all patent documents, non-patented documents or reference documents expressly cited may be incorporated herein by reference. Production method (A)

[00179] In this production method, compound (1-1) and compound (2-1) are condensed to give compound (3-1), and the protecting group (P1) is removed to give compound (Ia).

[00180] Compound (1-1) synthesized by a method known per se (e.g., U.S. Patent No. 10,836,736, etc.) may preferably be used. Production method (A) ------R\ Step A-2 ΤΪ ™ ° Where R1a-P1 is protected by R1 and other symbols are as defined above. (Stage A-1)

[00181] In this step, compound (1-1) and compound (2-1) are condensed in the presence of a condensing agent to produce Petition 870250102069, dated 07 / 11 / 2025, pp. 581 / 861 140 / 389 the compound (3-1).

[00182] The amount of compound (2-1) to be used is 0.8 mol to 5 mol, preferably 0.8 mol to 3 mol, per 1 mol of compound (1-1).

[00183] The condensing agent includes o-(7azabenzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate (HATU), 1-ethyl-3-(3'-dimethylaminopropyl)carbodiimide hydrochloride (EDC-HCl) (WSC hydrochloride), dicyclohexylcarbodiimide (DCC), diisopropylcarbodiimide (DIC), benzotriazol-1-yl-oxy-tris-pyrrolidinophosphonium hexafluorophosphate (PyBop), O-(benzotriazol-1-yl)-N,N',N'-tetramethyluronium tetrafluoroborate (TBTU), 1-[bis(dimethylamino)methylene]-5-chloro-1H-benzotriazolium 3-oxide hexafluorophosphate (HCTU), hexafluoroborate of O-benzotriazoleN,N,N',N'-tetramethyluronium (HBTU), propylphosphonic acid anhydride (T3P) solution and the like, preferably HATU or WSC hydrochloride.

[00184] The amount of condensing agent to be used is generally 1 mol to 10 mol, preferably 1 mol to 5 mol, per 1 mol of compound (1-1).

[00185] The reaction can be carried out in the co-presence of 1-hydroxybenzotriazole (HOBt), ethyl 1-hydroxy-1H-1,2,3-triazole-5-carboxylate (HOCt), 1-hydroxy-7-azabenzotriazole (HOAt) or similar as an additive.

[00186] The amount of additive to be used is generally 0 to 1.5 mol per 1 mol of compound (1-1).

[00187] Examples of the base include organic bases such as triethylamine, pyridine, N,N-diisopropylethylamine and the like. Among these, triethylamine or N,N-diisopropylethylamine is preferred.

[00188] The amount of base to be used is generally 1 mol to 5 mol, preferably 1.5 mol, per 1 mol of compound (1-1).

[00189] This reaction can be carried out in a solvent that does not affect the reaction. Examples of reaction solvents include, but are not particularly limited to, aromatic hydrocarbons, such as Petition 870250102069, dated 07 / 11 / 2025, pp. 582 / 861 141 / 389 Toluene, xylene and similar substances; amide solvents, such as N,N-dimethylformamide, N,N-dimethylacetamide and similar substances; ethers, such as diethyl ether, tetrahydrofuran, dioxane and similar substances; halogenated hydrocarbons, such as chloroform, dichloromethane and similar substances; nitriles, such as acetonitrile and similar substances, or a mixture thereof, may be mentioned.

[00190] The reaction temperature is generally -78 °C at room temperature, preferably 0 °C at room temperature, and the reaction time is generally 1 h 48 h. (Stage A-2)

[00191] In this step, the amino protecting group (P1) is removed to obtain compound (I a).

[00192] For the deprotection step of step A-2, the reaction conditions can be selected according to the type of protecting group (P1). The conditions for the deprotection reaction can be selected by known methods, such as Protective Groups in Organic Synthesis, 4th Ed., published by Wiley-Interscience in 2007 by Theodora W. Greene and Peter GM Wuts; Protective Groups in Organic Synthesis, 3rd Ed., 2004, Protecting Groups 3rd Ed., by PJ Kocienski, etc., or as described in the examples below. Production method (B)

[00193] In this production method, compound (1-1) and compound (4-1) are condensed to give compound (5-1), the compound is converted into compound (7-1) by a coupling reaction with compound (6-1), and the protecting group (P2) is removed to give compound (Ib).

[00194] Compound (1-1) synthesized by a method known per se (e.g., U.S. Patent No. 10,836,736, etc.) may preferably be used. Production method (B) Petition 870250102069, dated 07 / 11 / 2025, pp. 583 / 861 142 / 389 where X is an exit group, P2 and P3 are, each independently, protection groups, and other protection symbols are as defined above.

[00195] As the protecting group P3 in compound (6-1), a trisubstituted silyl group, such as a trimethylsilyl group, a triethylsilyl group, a tert-butyldimethylsilyl group, a tert-butyldiphenylsilyl group, a tri-isopropylsilyl group or similar is used. The protecting group P3 is removed by a reaction process in step B-2. (Stage B-1)

[00196] In this step, compound (1-1) and compound (4-1) are condensed in the presence of a condensing agent to produce compound (5-1).

[00197] The amount of compound (4 -1) to be used is 0.8 mol to 5 mol, preferably 0.8 mol to 3 mol, per 1 mol of compound (1-1).

[00198] In step B-1, the reaction can be carried out under the same conditions as step A-1 mentioned above, except that compound (41) is used instead of compound (2-1). (Stage B-2)

[00199] This step can be carried out by a cross-coupling reaction (Heck reaction) of compound (5-1) and compound (6-1) in a solvent that does not affect the reaction, in the presence of a metallic catalyst (e.g., palladium catalyst) and a base as needed.

[00200] The amount of compound (6 -1) to be used is 0.8 mol a Petition 870250102069, dated 07 / 11 / 2025, pp. 584 / 861 143 / 389 mol, preferably 0.8 mol to 3 mol, per 1 mol of compound (5-1).

[00201] Metallic catalysts include palladium catalysts, such as palladium(II) acetate, palladium(II) chloride, dichlorobis(tricyclohexylphosphine)palladium(II), tris(dibenzylideneacetone)dipalladium(0), bis(dibenzylideneacetone)palladium(0) (Pd2(dba)3), tetracis(triphenylphosphine)palladium(0), bis(tri-tert-butylphosphine)palladium(0), palladium(II) chloride and diphenylphosphineferrocene (PdCl2(dppf)), dichloromethane complex PdCl2(dppf), palladium(0) carbon, bis(triphenylphosphine)palladium dichloride, dichlorobis(tri-o-tolylphosphine)palladium(II), bis(tris(2-tolyl)phosphine)palladium(0) and similar substances; copper catalysts, such as copper(I) iodide, copper(I) bromide, copper(I) chloride, copper(II) chloride and similar substances; iron catalysts, such as iron(III) acetylacetonate and similar substances;Nickel catalysts, such as bis(1,5-cyclooctadiene)nickel(0), bis(acetylacetonate)nickel(II) and the like; ruthenium catalysts, such as dichloro(p-cimene)ruthenium(II) dimer, ruthenium alumina and the like. A palladium catalyst is preferred, among which dichlorobis(tricyclohexylphosphine)palladium(II), dichlorobis(tri-o-tolylphosphine)palladium(II) or bis(tritert-butylphosphine)palladium(0) are the most preferred.

[00202] When necessary, phosphine ligands, such as 1,1'bis(diphenylphosphino)ferrocene (dppf), 2-dicyclohexylphosphino-2',6'-dimethoxybiphenyl (SPhos), 2-dicyclohexylphosphino-2',4',6'-triisopropylbiphenyl (XPhos), 2-dicyclohexylphosphino-2',6'-diisopropoxybiphenyl (RuPhos), 3,6-dimethoxy-2-dicyclohexylphosphino-2',4',6'-triisopropylbiphenyl (BrettPhos), tri-t-butylphosphine, tricyclohexylphosphine, [4(N,N-dimethylamino)phenyl]di-tert-butylphosphine (AmPhos), (S)-1-[(RP)-2(dicyclohexylphosphino)ferrocenyl]ethyl di-tert-butylphosphine (JosiPhos), and similar substances; phenanthroline and similar substances may also be added.

[00203] The quantity of metallic catalyst to be used is Petition 870250102069, dated 07 / 11 / 2025, pp. 585 / 861 144 / 389 generally from 0.01 mol to 1 mol, preferably from 0.05 mol to 0.3 mol, per 1 mol of compound (5-1).

[00204] The amount of ligand to be used is generally from 0.05 mol to 1 mol, preferably from 0.1 mol to 0.4 mol, per 1 mol of compound (5-1).

[00205] The reaction can be carried out in the presence of zinc fluoride (ZnF2), copper fluoride (CuF2), lithium fluoride (LiF) or similar substances, as an additive.

[00206] The amount of additive to be used is generally 0 to 1.5 mol per 1 mol of compound (5-1).

[00207] Examples of the base include alkali metal amides, such as lithium diisopropylamide, sodium amide, lithium bis-trimethylsilylamide and the like; alkali metal carbonate salts, such as sodium carbonate, potassium carbonate, sodium bicarbonate, potassium bicarbonate and the like; alkali metal phosphate salts, such as sodium phosphate, potassium phosphate and the like; and amines, such as triethylamine, N,N-diisopropylethylamine, pyridine, N-methylmorpholine and the like.

[00208] The amount of base to be used is generally from 1 mol to 5 mol, preferably from 1 mol to 2.5 mol, per 1 mol of compound (5-1).

[00209] The reaction solvent is not particularly limited and includes, for example, amides such as N,N-dimethylformamide, N-methylpyrrolidone and the like; ethers such as tetrahydrofuran, 1,4-dioxane and the like; halogenated hydrocarbons such as chloroform, dichloromethane and the like; aromatic hydrocarbons such as toluene, xylene and the like; nitriles such as acetonitrile and the like; water; a mixture of these and the like.

[00210] The reaction temperature is generally from -78 °C to 200 °C, preferably from -78 °C to 120 °C.

[00211] The reaction time is generally from 0.5 h to 12 hours. Petition 870250102069, dated 07 / 11 / 2025, pp. 586 / 861 145 / 389 (Stage B-3)

[00212] In this step, compound (Ib) is obtained by removing the protecting group (P2).

[00213] For the deprotection process in step B-3, the reaction conditions can be selected according to the type of protecting group (P2). The conditions for the deprotection reaction can be selected by known methods, such as Protective Groups in Organic Synthesis, 4th Ed., published by Wiley-Interscience in 2007 by Theodora W. Greene and Peter GM Wuts; Protecting Groups, 3rd Ed., published by Thieme in 2004 by PJ Kocienski, etc., or as described in the Examples below. [Production method (C)]

[00214] In this production method, compound (1-1) and compound (8-1) are condensed to give compound (9-1), the protecting group (P4) is removed to give compound (10-1), compound (10-1) is converted into compound (12-1) by reaction with compound (11-1), and the protecting group (P5) is removed to obtain compound (Ic). Production method (C) Step (10-1) (12-1) Stage C-4 where R1b-P5 is a protected R1, X1 is an exit group, and P4 and P5 are, Petition 870250102069, dated 07 / 11 / 2025, pp. 587 / 861 146 / 389 each independently, protection groups and other protection symbols are as defined above. (Stage C-1)

[00215] In this step, compound (1-1) and compound (8-1) are condensed in the presence of a condensing agent to produce compound (9-1).

[00216] The amount of compound (8-1) to be used is 0.8 mol to 5 mol, preferably 0.8 mol to 3 mol, per 1 mol of compound (1-1).

[00217] In step C-1, the reaction can be carried out under conditions similar to those of step A-1 mentioned, except that compound (8-1) is used instead of compound (2-1). (Stage C-2)

[00218] In this step, the compound (1 0 -1) is obtained by removing the amino protecting group (P4).

[00219] For the deprotection process in step C-2, the reaction conditions can be selected according to the type of protecting group (P4). The conditions for the deprotection reaction can be determined by methods known per se, such as Protective Groups in Organic Synthesis, 4th Ed., published by Wiley-Interscience in 2007 by Theodora W. Greene and Peter GM Wuts; Protecting Groups, 3rd Ed., published by Thieme in 2004 by PJ Kocienski, etc., or as described in the Examples below. (Stage C-3)

[00220] In this step, compound (10-1) and compound (11-1) react in the presence of a base to produce compound (12-1).

[00221] The amount of compound (11-1) to be used is 1 mol to 5 mol, preferably 1 mol to 3 mol, per 1 mol of compound (1 0 -1).

[00222] As bases, organic bases such as triethylamine, pyridine, N,N-diisopropylethylamine and the like may be mentioned; and inorganic bases such as sodium carbonate, potassium carbonate, Petition 870250102069, dated 07 / 11 / 2025, pp. 588 / 861 147 / 389 Cesium carbonate and similar substances. Among these, triethylamine or N,N-diisopropylethylamine is preferred.

[00223] The amount of base to be used is generally 1 mol to 5 mol, preferably 1.5 mol, per 1 mol of compound (10-1).

[00224] The reaction can be carried out in the presence of tetrabutylammonium iodide (TBAI), sodium iodide, silver trifluoromethanesulfonate or similar as an additive.

[00225] The amount of additive to be used is generally 0 to 1.5 mol per 1 mol of compound (10-1).

[00226] This reaction can be carried out in a solvent that does not affect the reaction. The reaction solvent is not particularly limited and, for example, aromatic hydrocarbons such as toluene, xylene and the like; amide solvents such as N,N-dimethylformamide, N,N-dimethylacetamide and the like; ethers such as diethyl ether, tetrahydrofuran, dioxane and the like; halogenated hydrocarbons such as chloroform, dichloromethane and the like; nitriles such as acetonitrile and the like, and a mixture thereof may be mentioned.

[00227] The reaction temperature is generally from 0 °C to 100 °C, preferably from 0 °C to 50 °C, and the reaction time is generally from 1 h to 48 h.

[00228] When the resulting product obtained by this reaction contains a halogen, the halo group can be converted into an alkyl group or a cycloalkyl group by the subsequent coupling reaction. (Step C-4)

[00229] In this step, compound (Ic) is obtained by removing the amino protecting group (P5).

[00230] For the deprotection process in step C-4, the reaction conditions can be selected according to the type of protection group (P5). The conditions for the deprotection reaction can be Petition 870250102069, dated 07 / 11 / 2025, pp. 589 / 861 148 / 389 selected by methods known per se, such as Protective Groups in Organic Synthesis, 4th Ed., published by Wiley-Interscience in 2007 by Theodora W. Greene and Peter GM Wuts; Protecting Groups, 3rd Ed., published by Thieme in 2004 by PJ Kocienski, etc., or as described in the Examples below.

[00231] When the resulting product obtained by this reaction contains a halogen, the halo group can be converted into an alkyl group or a cycloalkyl group by the subsequent coupling reaction. Production method (D)

[00232] In this production method, compound (14-1) is obtained by a reductive alkylation reaction of compound (10-1) and compound (131), and the protecting group (P6) is moved to obtain compound (I d). Production method (D) where R1c-P6 is a protected R1, P6 is a protection group, La is a divalent organic group, and other symbols are as defined above. (Step D-1)

[00233] In this step, compound (10-1) reacts with a reducing agent and compound (13-1) (reductive alkylation reaction) in a solvent that does not affect the reaction to obtain compound (14-1).

[00234] The amount of compound (13-1) to be used is 1 mol to 3 mol, preferably 1 mol to 2 mol, per 1 mol of compound (1 0 -1). Petition 870250102069, dated 07 / 11 / 2025, pp. 590 / 861 149 / 389

[00235] The reducing agent is not particularly limited and, for example, sodium triacetoxyborohydride, sodium borohydride and the like may be mentioned.

[00236] The amount of reducing agent to be used is 1 mol to 10 mol, preferably 1 mol to 3 mol, per 1 mol of compound (1 0 -1).

[00237] As an additive, the reaction can be carried out in the presence of, for example, organic acids, such as acetic acid and the like; Lewis acids, such as titanium (IV) tetrachloride, titanium tetraisopropoxide and the like, and the like.

[00238] The amount of additive to be used is 1 mol to 10 mol, preferably 1 mol to 3 mol, per 1 mol of compound (10-1).

[00239] The reaction solvent is not particularly limited and, for example, aromatic hydrocarbons such as benzene, toluene, xylene and the like; alcohols such as methanol, ethanol and the like; ethers such as tetrahydrofuran and the like; halogenated hydrocarbons such as chloroform, dichloromethane and the like, and a mixture thereof may be mentioned.

[00240] The reaction temperature is generally from -10 °C to 100 °C, preferably from 10 °C to 50 °C, and the reaction time is generally from 1 h to 48 h. (Stage D-2)

[00241] In this step, compound (Id) is obtained by removing the amino protecting group (P6).

[00242] For the deprotection process in step D-2, the reaction conditions can be selected according to the type of protecting group (P6). The conditions for the deprotection reaction can be selected by methods known per se, such as Protective Groups in Organic Synthesis, 4th Ed., published by Wiley-Interscience in 2007 by Theodora W. Greene and Peter GM Wuts; Protecting Groups, 3rd Ed., published by Thieme in 2004 by PJ Kocienski, etc., or as Petition 870250102069, dated 07 / 11 / 2025, pp. 591 / 861 150 / 389 described in the examples below. [Production method (E)1

[00243] In this production method, compound (8-1) and compound (11-1) react to give compound (15-1), the protecting group (P4) is removed to give compound (16-1), compound (16-1) is converted into compound (12-1) by condensation with compound (1-1) and the protecting group (P5) is moved to obtain compound (Ic).

[00244] Compound (1-1) synthesized by a method known per se (e.g., U.S. Patent No. 10,836,736, etc.) may preferably be used. Production method (E) P4-N A1NH (8-1) P R1bP Ί-—X1R1b\ (11-1) \-N A1N-P4 Stage El Stage E-2P R\bχ LN A1NH Stage E-4R\ Λλ LN A1N OH(Ic) (where each symbol is as defined above.) (Step E-1)

[00245] In this step, compound (8-1) and compound (11-1) react in the presence of a base to produce compound (15-1).

[00246] The amount of compound (11 -1) to be used is 1 mol to 5 mol, preferably 1 mol to 3 mol, per 1 mol of compound (8 -1). Petition 870250102069, dated 07 / 11 / 2025, pp. 592 / 861 151 / 389

[00247] In step E-1, the reaction can be carried out under conditions similar to those of step C-3 mentioned, except that compound (8-1) is used instead of compound (10-1). (Stage E-2)

[00248] In this step, compound (16-1) is obtained by removing the amino protecting group (P4).

[00249] For the deprotection process in step E-2, the reaction conditions can be selected according to the type of protecting group (P4). The conditions for the deprotection reaction can be selected by known methods, such as Protective Groups in Organic Synthesis, 4th Ed., published by Wiley-Interscience in 2007 by Theodora W. Greene and Peter GM Wuts; Protecting Groups, 3rd Ed., published by Thieme in 2004 by PJ Kocienski, etc., or as described in the Examples below. (Stage E-3)

[00250] In this step, compound (16-1) and compound (1-1) are condensed in the presence of a condensing agent to produce compound (12-1).

[00251] The amount of compound (16-1) to be used is from 0.8 mol to 5 mol, preferably from 0.8 mol to 3 mol, per 1 mol of compound (1-1).

[00252] In step E-3, the reaction can be carried out under conditions similar to those of step A-1 mentioned, except that compound (16-1) is used instead of compound (2-1).

[00253] When the resulting product obtained by this reaction contains a halogen, the halo group can be converted into an alkyl group or a cycloalkyl group by the subsequent coupling reaction. (Stage E-4)

[00254] In this step, compound (Ic) is obtained by removing the amino protecting group (P5).

[00255] For the deprotection process in step E-4, the conditions Petition 870250102069, dated 07 / 11 / 2025, pp. 593 / 861 152 / 389 of the reaction can be selected according to the type of protecting group (P5). The conditions for the deprotection reaction can be selected by methods known per se, such as Protective Groups in Organic Synthesis, 4th Ed., published by Wiley-Interscience in 2007 by Theodora W. Greene and Peter GM Wuts; Protecting Groups, 3rd Ed. Ed., published by Thieme in 2004 by PJ Kocienski, etc., or as described in the Examples below.

[00256] When the resulting product obtained by this reaction contains a halogen, the halo group can be converted into an alkyl group or a cycloalkyl group by the subsequent coupling reaction. [Production method (F)]

[00257] In this production method, compound (8-1) and compound (13-1) react to give compound (17-1), the protecting group (P4) is removed to give compound (18-1), compound (18-1) is converted into compound (14-1) by reaction with compound (1-1), and the protecting group (P6) is removed to obtain compound (I d). Production method (F) p6 p6 Ia xo CHO Lap4-n A1NH N a1n-p4 Stage F Petition 870250102069, dated 07 / 11 / 2025, pp. 594 / 861 153 / 389 (where each symbol is as defined above.) (Step F-1)

[00258] In this step, compound (8-1) reacts with a reducing agent and compound (13-1) (reductive alkylation reaction) in a solvent that does not affect the reaction to obtain compound (17-1).

[00259] The amount of compound (13 -1) to be used is 1 mol to 3 mol, preferably 1 mol to 2 mol, per 1 mol of compound (8 -1).

[00260] In step F-1, the reaction can be carried out under conditions similar to those of step D-1 mentioned, except that compound (8-1) is used instead of compound (10-1). (Stage F-2)

[00261] In this step, the compound (1 8 -1) is obtained by removing the amino protecting group (P4).

[00262] For the deprotection process in step F-2, the reaction conditions can be selected according to the type of protecting group (P4). The conditions for the deprotection reaction can be selected by methods known per se, such as Protective Groups in Organic Synthesis, 4th Ed., published by Wiley-Interscience in 2007 by Theodora W. Greene and Peter GM Wuts; Protecting Groups, 3rd Ed., published by Thieme in 2004 by PJ Kocienski, etc., or as described in the Examples below. (Stage F-3)

[00263] In this step, compound (18-1) and compound (1-1) are condensed in the presence of a condensing agent to produce compound (14-1).

[00264] The amount of compound (18-1) to be used is 0.8 mol to 5 mol, preferably 0.8 mol to 3 mol, per 1 mol of compound (1-1).

[00265] In step F-3, the reaction can be carried out under conditions similar to those of step A-1 mentioned, except that compound (18-1) is used instead of compound (2-1). Petition 870250102069, dated 07 / 11 / 2025, pp. 595 / 861 154 / 389

[00266] When the resulting product obtained by this reaction contains a halogen, the halo group can be converted into an alkyl group or a cycloalkyl group by the subsequent coupling reaction. (Stage F-4)

[00267] In this step, compound (Id) is obtained by removing the amino protecting group (P6).

[00268] For the deprotection process in step F-4, the reaction conditions can be selected according to the type of protecting group (P6). The conditions for the deprotection reaction can be selected by methods known per se, such as Protective Groups in Organic Synthesis, 4th Ed., published by Wiley-Interscience in 2007 by Theodora W. Greene and Peter GM Wuts; Protecting Groups, 3rd Ed., published by Thieme in 2004 by PJ Kocienski, etc., or as described in the Examples below.

[00269] When the resulting product obtained by this reaction contains a halogen, the halo group can be converted into an alkyl group or a cycloalkyl group by the subsequent coupling reaction. [Production method (G)]

[00270] In this production method, compound (8-1) and compound (19-1) react to give compound (20-1), the protecting group (P4) is removed to give compound (21-1), compound (21-1) is converted into compound (22-1) by reaction with compound (11-1), the protecting group (P7) is moved to obtain compound (23-1), compound (23-1) is converted into compound (12-1) by reaction with compound (241), and the protecting group (P5) is moved to obtain compound (Ic). Production method (G) Petition 870250102069, dated 07 / 11 / 2025, pp. 596 / 861 155 / 389 (8-1) Stage Gl (20-1) Stage G-2 (21-1) R1b'L-X1(11·1) _ _vR-------► P5 Stage G-3 (22-1) Stage G-4 (23-1) THE Step G-6 (24-1) ---------*Step G-5 (where each symbol is as defined above.) (Step G-1)

[00271] In this step, compound (19-1) reacts with a halogen attenuating agent in a solvent that does not affect the reaction to form an acid halide, and the acid halide reacts with compound (8-1) to obtain compound (20-1).

[00272] The amount of compound (19 -1) to be used is 1 mol to 3 mol, preferably 1 mol to 2 mol, per 1 mol of compound (8-1).

[00273] The halogenating agent is not particularly limited and, for example, thionyl chloride, sulfuryl chloride, phosphorus trichloride, phosphorus pentachloride, phosphorus oxychloride, oxalyl chloride and the like may be mentioned.

[00274] The amount of halogenating agent to be used is 1 mol to 10 mol, preferably 1 mol to 3 mol, per 1 mol of compound (1 9-1). Petition 870250102069, dated 07 / 11 / 2025, pp. 597 / 861 156 / 389

[00275] As an additive, the reaction can be carried out in the presence of, for example, DMF and similar substances.

[00276] The amount of additive to be used is 0.05 mol to 1 mol, preferably 10.05 mol to 0.1 mol, per 1 mol of compound (19-1).

[00277] The reaction solvent is not particularly limited and, for example, aromatic hydrocarbons such as benzene, toluene, xylene and the like; ethers such as tetrahydrofuran and the like; halogenated hydrocarbons such as chloroform, dichloromethane and the like, and a mixture thereof may be mentioned.

[00278] The reaction temperature is generally from -10 °C to 100 °C, preferably from 10 °C to 50 °C, and the reaction time is generally from 1 h to 48 h. (Stage G-2) In this step, the compound (2 1-1) is obtained by removing the amino protecting group (P4).

[00279] For the deprotection process in step G-2, the reaction conditions can be selected according to the type of protecting group (P4). The conditions for the deprotection reaction can be selected by known methods, such as Protective Groups in Organic Synthesis, 4th Ed., published by Wiley-Interscience in 2007 by Theodora W. Greene and Peter GM Wuts; Protecting Groups, 3rd Ed., published by Thieme in 2004 by PJ Kocienski, etc., or as described in the Examples below. (Stage G-3)

[00280] In this step, compound (21-1) and compound (11-1) react in the presence of a base to produce compound (22-1).

[00281] The amount of compound (11-1) to be used is 1 mol to 5 mol, preferably 1 mol to 3 mol, per 1 mol of compound (21-1).

[00282] In step G-3, the reaction can be carried out under conditions similar to those of step C-3 mentioned, except that compound (21-1) Petition 870250102069, dated 07 / 11 / 2025, pp. 598 / 861 157 / 389 is used instead of compound (10-1). (Stage G-4)

[00283] In this step, compound (23-1) is obtained by removing the amino protecting group (P7).

[00284] For the deprotection process in step G-4, the reaction conditions can be selected according to the type of protecting group (P7). The conditions for the deprotection reaction can be selected by known methods, such as Protective Groups in Organic Synthesis, 4th Ed., published by Wiley-Interscience in 2007 by Theodora W. Greene and Peter GM Wuts; Protecting Groups, 3rd Ed., published by Thieme in 2004 by PJ Kocienski, etc., or as described in the Examples below. (Stage G-5)

[00285] In this step, compound (23-1) and compound (24-1) are condensed in the presence of a condensing agent to produce compound (12-1).

[00286] The amount of compound (23-1) to be used is 0.8 mol to 5 mol, preferably 0.8 mol to 3 mol, per 1 mol of compound (24-1).

[00287] In step G-5, the reaction can be carried out under conditions similar to those of step A-1 mentioned, except that compound (23-1) is used instead of compound (2-1). (Stage G-6)

[00288] In this step, compound (Ic) is obtained by removing the amino protecting group (P5).

[00289] For the deprotection process in step G-6, the reaction conditions can be selected according to the type of protecting group (P5). The conditions for the deprotection reaction can be selected by methods known per se, such as Protective Groups in Organic Synthesis, 4th Ed., published by Wiley-Interscience in 2007 by Theodora W. Greene and Peter GM Wuts; Protecting Groups, 3rd Ed. Petition 870250102069, dated 07 / 11 / 2025, pp. 599 / 861 158 / 389 Ed., published by Thieme in 2004 by PJ Kocienski, etc., or as described in the Examples below.

[00290] Compound (I) or a pharmaceutically acceptable salt thereof obtained by the above-mentioned production methods may be isolated and purified by a general separation method, for example, recrystallization, distillation, chromatography and the like.

[00291] When compound (I) of the present invention or a pharmaceutically acceptable salt thereof exists as an optical isomer based on an asymmetric carbon, it can be separated into individual optical isomers by conventional means of optical resolution (e.g., fractional crystallization method, resolution using a chiral column). Alternatively, the optical isomers can be synthesized using optically pure starting materials. Furthermore, the optical isomers can also be synthesized by carrying out each reaction stereoselectively using chiral auxiliary groups or asymmetric catalysts. Medication (pharmaceutical composition) of the present invention

[00292] The drug of the present invention is a drug for preventing and / or treating diseases whose symptoms can be relieved by the inhibitory action of B0AT1, containing compound (I), or a pharmaceutically acceptable salt thereof, as the active ingredient. Specifically, the drug of the present invention is at least one of a drug containing the aforementioned active ingredient for preventing the onset of a disease whose symptoms can be relieved by the inhibitory action of B0AT1, and a drug for improving the symptoms of the disease.

[00293] The medicament of the present invention may be a drug comprising only compound (I) or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising said compound (I) or a pharmaceutically acceptable salt. Petition 870250102069, dated 07 / 11 / 2025, pages 600 / 861 159 / 389 acceptable of it and a pharmaceutically acceptable vehicle, etc. The drug of the present invention can be administered to an individual (e.g., mouse, rat, hamster, rabbit, cat, dog, bovine, sheep, monkey, human, etc.) in a prophylactically effective amount or in a therapeutically effective amount.

[00294] Examples of pharmaceutically acceptable vehicles include excipients (e.g., starch, lactose, sugar, calcium carbonate, calcium phosphate, etc.), binders (e.g., starch, gum arabic, carboxymethylcellulose, hydroxypropylcellulose, crystalline cellulose, etc.), lubricants (e.g., magnesium stearate, talc, etc.), disintegrants (e.g., carboxymethylcellulose, talc, etc.), solvents (e.g., water for injection, physiological saline, Ringer's solution, alcohol, propylene glycol, polyethylene glycol, sesame oil, corn oil, olive oil, cottonseed oil, etc.), solubilizing agents (e.g., polyethylene glycol, propylene glycol, D-mannitol, trehalose, benzyl benzoate, ethanol, trisaminomethane, cholesterol, triethanolamine, sodium carbonate, sodium citrate, sodium salicylate, sodium acetate, etc.), suspending agent (e.g., surfactants such as stearyltriethanolamine, sodium lauryl sulfate, lauryl aminopropionate, lecithin, benzalkonium chloride, benzethonium chloride, glyceryl monostearate and the like; hydrophilic polymers such as poly(vinyl alcohol), polyvinylpyrrolidone, sodium carboxymethylcellulose, methylcellulose, hydroxymethylcellulose, hydroxyethylcellulose, hydroxypropylcellulose and the like; polysorbates, polyoxyethylene hydrogenated castor oil, etc.), isotonic agent (e.g., sodium chloride, glycerol, D-mannitol, D-sorbitol, glucose, etc.), buffering agent (e.g., buffers such as phosphate, acetate, carbonate, citrate and the like, etc.), soothing agent (e.g., benzyl alcohol, etc.), antiseptic (e.g., p-hydroxybenzoic acid esters, chlorobutanol, benzyl alcohol, phenethyl alcohol, dehydroacetic acid. Petition 870250102069, dated 07 / 11 / 2025, pages 601 / 861 160 / 389 sorbic acid, etc.), antioxidant (e.g., sulfite, ascorbate, etc.), colorant (e.g., water-soluble food tar colorant (e.g., food colorants such as food red colorant no. 2 and 3, food yellow colorant no. 4 and no. 5, food blue colorant no. 1 and 2 and the like), water-insoluble lake pigment (e.g., the above-mentioned aluminum salts of water-soluble food tar colorant), natural colorant (e.g., β-carotene, chlorophyll, red iron oxide), etc.), sweetener (e.g., sodium saccharin, dipotassium glycyrrhizinate, stevia, etc.) and the like.

[00295] The medicament (pharmaceutical composition) of the present invention is prepared by mixing the aforementioned ingredients and then preparing the mixture according to known means, for example, oral dosage forms such as tablets, fine granules, granules, capsules, dry syrups and the like, or parenteral dosage forms such as injections (e.g., subcutaneous injection, intravenous injection, intramuscular injection, intraperitoneal injection, intravenous infusion, etc.), topical formulations (e.g., transdermal, ointments, lotions, patches), suppositories (e.g., rectal suppositories, vaginal suppositories), lozenges, nasal agents, transpulmonary agents (inhalation agents), ophthalmic agents, implantable agents, microcapsules, liposomes and the like.

[00296] Among them, the drug of the present invention is preferably a preparation for oral administration, such as tablets and the like.

[00297] The content of compound (I) of the present invention, or of a pharmaceutically acceptable salt thereof, in the drug (pharmaceutical composition) of the present invention varies depending on the form of preparation. It is generally in the range of about 0.01 to 100% by weight, preferably about 0.1 to 50% by weight, and even more. Petition 870250102069, dated 07 / 11 / 2025, pp. 602 / 861 161 / 389 preferably about 0.5 to 20% by weight, based on the total preparation.

[00298] The dose of compound (I) of the present invention, or of a pharmaceutically acceptable salt thereof, may be selected according to the individual to be administered (age, weight, general health status, sex, disease grade, etc.), route of administration, type of disease, type of concomitant drug and the like. For example, in the case of a human being, when administered orally to an adult patient (weighing approximately 60 kg), the dose of compound (I), or of a pharmaceutically acceptable salt thereof, is generally from 0.001 mg to 1000 mg, preferably from 0.01 mg to 100 mg in terms of the active ingredient, once or several times a day. It may be administered before, after or between meals. The duration of administration is not limited.

[00299] Compound (I) of the present invention, or a pharmaceutically acceptable salt thereof, is useful for the prevention of the onset of diseases whose symptoms can be relieved by an inhibitory action of B0AT1 or for therapeutic use in the diseases. In particular, it is effective for prophylactic or therapeutic use in the aforementioned diseases, including disorders of amino acid metabolism such as phenylketonuria, urea cycle disorder, hypertyrosinemia (types 1-3), hypermethioninemia, maple syrup urine disease, homocystinuria, nonketotic hyperglycinemia, propionic acidemia, methylmalonic acidemia, isovaleric acidemia and the like.

[00300] Compound (I) of the present invention, or a pharmaceutically acceptable salt thereof, may be administered in combination with other drugs (concomitant drugs) (combined use), provided that its efficacy is not impaired. The concomitant drug is not particularly limited and, for example, one or more drugs known to be conventionally used for the treatment of Petition 870250102069, dated 07 / 11 / 2025, pp. 603 / 861 162 / 389 diseases whose symptoms can be relieved by the inhibitory action of B0AT1, as exemplified above, may be preferentially used.

[00301] Specifically, when compound (I) of the present invention or a pharmaceutically acceptable salt thereof is used for the treatment and / or prevention of amino acid metabolism disorders, such as phenylketonuria, urea cycle disorder, hypertyrosinemia (type 1-3), hypermethioninemia, maple syrup urine disease, homocystinuria, nonketotic hyperglycinemia, propionic acidemia, methylmalonic acidemia, isovaleric acidemia and the like, concomitant drugs to be used in combination include, for example, vitamins (e.g., folic acid (vitamin B9), nicotinamide (vitamin B3), thiamine (vitamin B1), pyridoxine (vitamin B6), etc.) and drugs to relieve various symptoms of amino acid metabolism disorders (e.g., L-dopa, LNAA, such as 5-hydroxytryptophan, sapropterin hydrochloride, pegvaliase, nicotinic acid, nitisinone, S-adenosylmethionine, betaine, aspirin, dipyridamole, sodium benzoate, sodium phenylbutyrate, dextromethorphan, ketamine, antidepressants, anxiolytics, ADHD drugs, etc.).

[00302] When a concomitant drug is used, the administration period is not limited and it can be administered simultaneously or with a time interval relative to the administration individual. In time-interrupted administration, the drug of the present invention can be administered first and the concomitant drug can be administered later, or the concomitant drug can be administered first and the drug of the present invention can be administered later. Each method of administration can be the same or different. Furthermore, a single preparation containing compound (I) of the present invention or a pharmaceutically acceptable salt thereof, and a concomitant drug in combination, can also be administered. Petition 870250102069, dated 07 / 11 / 2025, pp. 604 / 861 163 / 389

[00303] The dose of the concomitant drug can be appropriately selected, using the clinically used dose as a standard. The mixing ratio of the compound of the present invention, or of a pharmaceutically acceptable salt thereof, and the concomitant drug can be appropriately determined according to the individual of administration (age, body weight, general health status, sex, disease severity, etc.), route of administration, type of disease, type of concomitant drug and the like.

[00304] The mass ratio of compound (I) or of a pharmaceutically acceptable salt thereof and of the concomitant drug is not particularly limited.

[00305] The concomitant drug that complements and / or enhances the therapeutic effect of compound (I) or a pharmaceutically acceptable salt thereof includes not only those that have been found to date, but also those that will be found in the future based on the mechanism described above.

[00306] In addition, to complement and / or enhance the therapeutic effect of compound (I) or its pharmaceutically acceptable salt, it may also be useful in combination with dietary therapy or enzyme replacement therapy to avoid the intake of certain amino acids.

[00307] The drug or pharmaceutical composition of the present invention may be supplied in the form of a kit, together with instructions for administration. The drug in the kit is supplied in a container made of a material that will effectively maintain the activity of the components of the drug or pharmaceutical composition for a long period, will not adsorb to the inside of the container, and will not alter the components. For example, a sealed glass ampoule may contain buffer and similar sealed in the presence of a neutral and inert gas, such as nitrogen gas. Petition 870250102069, dated 07 / 11 / 2025, pp. 605 / 861 164 / 389

[00308] The kit may also be accompanied by instructions for use. The instructions for use of the kit may be printed on paper or other media, or may be stored on an electromagnetically readable medium, such as a CD-ROM or DVD-ROM, and provided to the user. EXAMPLES

[00309] The present invention is explained in more detail below by reference to Reference Examples, Examples, and Experimental Examples, which do not limit the present invention. The present invention may be modified without departing from the scope of the invention. The reagents, apparatus, materials and the like used in the present invention are commercially available unless particularly indicated.

[00310] % indicates mol / mol % for productions, and weight % for others, unless otherwise specified. Room temperature indicates a temperature of 15°C to 30°C, unless otherwise specified. * in the following structural formulas indicates racemic carbon. Other abbreviations used in the text show the following meanings. THF: tetrahydrofuran DMSO: dimethyl sulfoxide DMF: N,N-dimethylformamide HATU: O-(7-azabenzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate WSC: 1-ethyl-3-(3'-dimethylaminopropyl)carbodiimide HOBt: 1-hydroxybenzotriazole

[00311] The starting compounds used in the Examples of Reference and Examples are known compounds unless specifically indicated, and those synthesized and identified according to the methods of per se (e.g., US Patent No. Petition 870250102069, dated 07 / 11 / 2025, pp. 606 / 861 165 / 389 10,836,736; Bioorganic & Medicinal Chemistry Letters, 2017, 27(21), 4805-4811; J. Med. Chern., 2014, 57, 3687-3706; WO 2013 / 067274), or methods analogous to this were used. Example of Reference 1: Production of 6-bromo-4-methoxy-1,2,3,4-tetrahydroisoquinoline Me.o

[00312] (1) To a solution of 6-bromo-2-(2-nitrophenyl)sulfonyl-3,4-dihydro-1H-isoquinolin-4-ol (300 mg) in toluene (2 ml) were added tetrabutylammonium hydrogen sulfate (25 mg), iodomethane (206 mg), and potassium hydroxide (50% w / v, 2 ml), and the reaction mixture was stirred at 50°C for 1 h. Water was added to the reaction mixture, and the aqueous layer was extracted with ethyl acetate. The organic layer was washed with saturated brine, dried over anhydrous sodium sulfate, and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (solvent: n-hexane / ethyl acetate = 100 / 0 - 50 / 50) to give 6-bromo-4-methoxy-2-(2-nitrophenyl)sulfonyl-3,4-dihydro-1H-isoquinoline (295 mg; 95% yield) as a colorless viscous oil. EM(ESI) m / z: 397.1 / 399.1[M-OMe+H]+

[00313] (2) To a solution of 6-bromo-4-methoxy-2-(2-nitrophenyl)sulfonyl-3,4-dihydro-1H-isoquinoline (295 mg) obtained in (1) above mentioned in DMF (2 ml) were added potassium carbonate (191 mg) and phenylmethanethiol (172 mg), and the reaction mixture was stirred for 3 h at room temperature. Water was added to the reaction mixture, and the aqueous layer was extracted with ethyl acetate. The organic layer was washed with saturated brine, dried over anhydrous sodium sulfate, concentrated under reduced pressure, and dried under reduced pressure to give a crude product (167 mg; 99% yield) of the title compound as a brown viscous oil. Petition 870250102069, dated 07 / 11 / 2025, pp. 607 / 861 166 / 389 Example of Reference 2: Production of methyl 3-(1-methylpiperazin-2-yl)benzoate

[00314] (1) Benzyl 3-(3-bromophenyl)pipiperazine-1-carboxylate (1.4 g) was dissolved in THF (12 ml), acetic acid (2 ml), aqueous formalin solution (37%, 1.4 ml) and sodium triacetoxyborohydride (1.58 g) were added, and the reaction mixture was stirred at room temperature for 30 min. Aqueous sodium hydroxide solution (1 mol / l) and chloroform were added to the reaction mixture, the organic layer was separated, and the aqueous layer was extracted with chloroform. The organic layers were combined, dried over anhydrous magnesium sulfate, and filtered. The filtrate was evaporated under reduced pressure to give a crude product (1.47 g) of benzyl 3-(3-bromophenyl)-4-methylpipiperazine-1-carboxylate as a yellow oil.

[00315] (2) The crude product (350 mg) of benzyl 3-(3-bromophenyl)-4-methylpipiperazine-1-carboxylate obtained in (1) above was dissolved in acetonitrile (6 ml), methanol (3 ml), molybdenum hexacarbonyl (239 mg) and DBU (0.28 ml) were added to this, and the mixture was subjected to nitrogen substitution. Bis(tri-tert-butylphosphine)palladium(0) (46 mg) was added to the reaction mixture, and the mixture was stirred under microwave irradiation at 140°C for 30 min. The reaction mixture was allowed to cool to room temperature, diluted with ethyl acetate and filtered. The filtrate was concentrated under reduced pressure, and the residue obtained was purified by silica gel column chromatography (solvent: n-hexane / ethyl acetate = 50 / 50 - 25 / 75) to give benzyl 3-(3-methoxycarbonylphenyl)-4-methylpipiperazine-1-carboxylate (306 mg; 92.4% yield) as a yellow oil. Petition 870250102069, dated 07 / 11 / 2025, pp. 608 / 861 167 / 389 EM(ESI) m / z: 369.2 [M+H]+

[00316] (3) 3-(3-methoxycarbonylphenyl)-4-methylpipiperazine-1-carboxylate benzyl (306 mg) obtained in (2) above was dissolved in methanol (2.8 ml), palladium hydroxide (30 mg) was added, and the mixture was added to hydrogen substitution. The reaction mixture was stirred at 60°C for 4 h 30 min, allowed to cool to room temperature, filtered through Celite, and washed with methanol. The filtrate was concentrated under reduced pressure to give the title compound (265 mg; yield of 136.2%) as a yellow amorphous substance. EM(ESI) m / z: 235.2[M+H]+ Example of Reference 3: Production of 2-[2-(1,2,3,6-tetrahydropyridine-5iD-phenylmethylacetate hydrochloride]

[00317] (1) 5-(4,4,5,5-tetramethyl-1,3,2-dioxa borolan-2-yl)-3,6-dihydro2H-pyridine-1-carboxylate tert-butyl (1.0 g) was dissolved in 1,4-dioxane (40 ml), methyl 2-(2-bromophenyl)acetate (890 mg), tetracis(triphenylphosphine)palladium (380 mg), cesium carbonate (2.1 g) and water (10 ml) were added, and the reaction mixture was stirred at 90°C for 1 h. The reaction mixture was allowed to cool to room temperature, water was added to it, and the mixture was extracted with ethyl acetate. The organic layer was washed with saturated brine, dried over anhydrous magnesium sulfate, and filtered. The filtrate was concentrated under reduced pressure, and the residue obtained was purified by silica gel column chromatography (solvent: n-hexane / ethyl acetate = 80 / 20 - 50 / 50) to provide tert-butyl 5-[2-(2-methoxy-2-oxoethyl)phenyl]-3,6-dihydro-2H-pyridine-1-carboxylate (1.0 Petition 870250102069, dated 07 / 11 / 2025, pp. 609 / 861 168 / 389 g; 93.3% yield) as a colorless oil.

[00318] (2) 5-[2-(2-methoxy-2-oxoethyl)phenyl]-3,6-dihydro-2H-pyridine-1-tert-butylcarboxylate (300 mg) obtained in (1) above was dissolved in methanol (3 ml), and 1,4-dioxane hydrogen chloride solution (4 mol / l.3 ml) was added. The reaction mixture was stirred at room temperature for 1 h, and concentrated under reduced pressure at 40°C to give a crude product (242 mg) of the title compound as a colorless amorphous substance. Example of Reference 4: Production of methyl 2-(3-piperidin-3-ylphenyl)acetate hydrochloride

[00319] (1) 5-[2-(2-methoxy-2-oxoethyl)phenyl]-3,6-dihydro-2H-pyridine-1 tert-butyl carboxylate (700 mg) obtained in Reference Example 3, step (1), was dissolved in methanol (10 ml), and palladium-carbon (10%, 200 mg) was added. The reaction mixture was subjected to hydrogen substitution, and stirred at room temperature for 2 h. The reaction mixture was filtered through Celite, and the filtrate was concentrated under reduced pressure. The residue obtained was purified by silica gel column chromatography (solvent: n-hexane / ethyl acetate = 95 / 5 - 80 / 20) to give tert-butyl 3-[3-(2-methoxy-2-oxoethyl)phenyl]piperidine-1-carboxylate (580 mg; yield of 82.3%) as a colorless oil. EM(ESI) m / z: 334.1[M+H]+

[00320] (2) 3-[3-(2-methoxy-2-oxoethyl)phenyl]piperidine-1-tert-butyl carboxylate (580 mg) obtained in (1) above was dissolved in methanol (6 ml), and a solution of 1,4-dioxane hydrogen chloride (4 mol / l, 6 ml) was added to this. The reaction mixture was stirred in Petition 870250102069, dated 07 / 11 / 2025, pp. 610 / 861 169 / 389 room temperature for 1 h, and concentrated under reduced pressure at 40°C to give a crude product (469 mg) of the title compound as a colorless amorphous substance. Example of Reference 5: Production of tert-butyl 3-(5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-2-yl)propanoate

[00321] (1) To a solution of 2-chloro-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidine hydrochloride (400 mg), benzyloxycarbonyl chloride (0.48 ml), sodium hydrogen carbonate (326 mg) and 1,4-dioxane (6.4 ml) was added water (1.8 ml), and the mixture was stirred at room temperature for 18 h. Water was added to the reaction mixture. The organic layer was extracted with ethyl acetate, and the combined organic layer was successively washed with water and saturated brine, dried over anhydrous magnesium sulfate, and concentrated under reduced pressure. The residue obtained was purified by silica gel column chromatography (solvent: n-hexane / ethyl acetate = 100 / 0 - 30 / 70) to give benzyl 2-chloro-7,8-dihydro-5H-pyrido[4,3-d]pyrimidine-6-carboxylate (535 mg; 80% yield) as a colorless viscous oil. EM(ESI) m / z: 304.1 / 306.1[M+H]+

[00322] (2) To a solution of benzyl 2-chloro-7,8-dihydro-5H-pyrido[4,3d]pyrimidine-6-carboxylate (535 mg) obtained in (1) mentioned above, palladium(II) bis[4-(N,N-dimethylamino)phenyl]-di-tert-butylphosphine chloride (124 mg), tert-butyl (E)-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2yl)prop-2-enoate (538 mg), cesium carbonate (1.15 g) and 1,4-dioxane (3 ml) water (0.8 ml) was added, and the mixture was stirred under microwave irradiation at 140°C for 1 h. Water was added to the reaction mixture. The organic layer was extracted with acetate Petition 870250102069, dated 07 / 11 / 2025, pp. 611 / 861 170 / 389 ethyl, and the combined organic layer was successively washed with water and saturated brine, dried over anhydrous magnesium sulfate, and concentrated under reduced pressure. The residue obtained was purified by silica gel column chromatography (solvent: n-hexane / ethyl acetate = 100 / 0 - 30 / 70) to give 2-[(E)-3-[(2-methylpropan-2-yl)oxy]-3oxoprop-1-enyl]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidine-6-carboxylate benzyl (318 mg; 46% yield) as a yellow viscous oil. EM(ESI) m / z: 396.2[M+H]+

[00323] (3) To a solution of 2-[(E)-3-[(2-methylpropan-2-yl)oxy]-3oxoprop-1-enyl]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidine-6-benzyl carboxylate (52 mg) obtained in (2) above, palladium(II) hydroxide (20 mg) was added in ethanol (1.4 ml), and the mixture was stirred under a hydrogen atmosphere at room temperature for 3 h. The reaction mixture was filtered through Celite, and the filtrate was concentrated under reduced pressure to give a crude product (35 mg) of the title compound as a colorless viscous oil. Example of Reference 6: Production of methyl trifluoroacetate 3-(indolin-4-yl)propanoate

[00324] (1) tert-butyl 4-bromoindoline-1-carboxylate (500 mg) was dissolved in 1,4-dioxane (4.5 ml), and water (1 ml), cesium carbonate (1.1 g), ethyl (E)-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)prop-2-enoate (570 mg) and bis(4-di-tert-butylphosphanyl-N,N-dimethylaniline)dichloropalladium(II) (100 mg) were added to the reaction mixture. The reaction mixture was stirred under microwave irradiation at 110°C for 2 h 30 min. The reaction mixture was allowed to cool to room temperature and extracted with ethyl acetate. The organic layer was dried over sodium sulfate, filtered, and the filtrate was Petition 870250102069, dated 07 / 11 / 2025, pp. 612 / 861 171 / 389 concentrated under reduced pressure to provide a crude product (560 mg) of tert-butyl 4-[(E)-3-ethoxy-3-oxoprop-1-enyl]indoline-1-carboxylate as a brown solid.

[00325] (2) The crude product (560 mg) of tert-butyl 4-[(E)-3-ethoxy-3-oxoprop-1-enyl]indoline-1-carboxylate obtained in (1) above was dissolved in methanol (25 ml). Magnesium (500 mg) was added to this, and the mixture was stirred at room temperature for 14 h. The reaction mixture was washed with hydrochloric acid (1 mol / l), and the organic layer was dried over sodium sulfate, silica gel of NH2 was added, and the mixture was filtered. The filtrate was concentrated under reduced pressure to give a crude product (550 mg) of tert-butyl 4-(3-methoxy-3-oxopropyl)indoline-1-carboxylate as a yellow oil.

[00326] (3) The crude product (247 mg) of tert-butyl 4-(3-methoxy-3-oxopropyl)indoline-1-carboxylate obtained in (2) above was dissolved in dichloromethane (1 ml), trifluoroacetic acid (1.3 ml) was added to this, and the mixture was stirred at room temperature for 1 h. The solvent was evaporated under reduced pressure, 0 toluene was added to the residue, and the mixture was concentrated under reduced pressure again to provide a crude product (258.2 mg) of the title compound. Example of Reference 7: Production of tert-butyl 2-(5-cyano-1,2,3,4-tetrahydroisoquinolin-6-yl)acetate

[00327] (1) To a solution of 6-bromoisoquinoline (1 g) in sulfuric acid (10 ml) was added 1-chloropyrrolidine-2,5-dione (1.3 g), and the mixture was stirred at 50°C for 3 h. The 1-chloropyrrolidine-2,5-dione (1,3 Petition 870250102069, dated 07 / 11 / 2025, pp. 613 / 861 172 / 389 g) was added to this, and the mixture was also stirred at 50°C for 15 h. Water and sodium hydroxide were added to the reaction mixture, and the organic layer was extracted with ethyl acetate. The combined organic layer was washed with water and saturated brine, dried over anhydrous magnesium sulfate, and concentrated under reduced pressure. The residue obtained was purified by silica gel column chromatography (solvent: n-hexane / ethyl acetate = 100 / 0 - 30 / 70) to give 6-bromo-5-chloroisoquinoline (824 mg; 71% yield) as a white solid. MS(ESI) m / z: 242.0 / 244.0[M+H]+

[00328] (2) To a solution of 6-bromo-5-chloroisoquinoline (824 mg) obtained in (1) above in acetic acid (10 ml) sodium borohydride (141 mg) was added under freezing conditions, and the mixture was stirred at room temperature for 1 h. Under freezing conditions, sodium borohydride (71 mg) was added, and the mixture was stirred at room temperature for a further 2 h. The reaction mixture was neutralized with saturated aqueous sodium hydroxide solution, and the organic layer was extracted with ethyl acetate. The combined organic layer was washed with saturated brine, dried over anhydrous magnesium sulfate, and concentrated under reduced pressure to give a crude product (837 mg) of 6-bromo-5-chloro-1,2,3,4-tetrahydroisoquinoline as a white solid.

[00329] (3) To the crude product (837 mg) of 6-bromo-5-chloro-1,2,3,4-tetrahydroisoquinoline obtained in (2) above, ethyl acetate (4 ml) and hydrogen chloride (4 mol / l of 1,4-dioxane solution) (0.93 ml) were added, and the precipitated solution was collected by filtration to give 6-bromo-5-chloro-1,2,3,4-tetrahydroisoquinoline hydrochloride (766 mg; 80% yield) as a white solid. EM(ESI) m / z: 246.0 / 248.0[M+H]+

[00330] (4) To a solution of 6-bromo-5-chloro-1,2,3,4-tetrahydroisoquinoline hydrochloride (1 g) obtained in (3) mentioned above, pyridine (7 Petition 870250102069, dated 07 / 11 / 2025, pp. 614 / 861 To the reaction mixture, 173 / 389 ml) and N,N-dimethylpyridine-4-amine (43 mg), trifluoroacetic anhydride (1.5 g) was added under freezing conditions, and the mixture was stirred at room temperature for 2 h. Water and 1 mol / l hydrochloric acid were added to the reaction mixture, and the organic layer was extracted with ethyl acetate. The combined organic layer was successively washed with water and saturated brine, dried over anhydrous magnesium sulfate, and concentrated under reduced pressure. The residue obtained was purified by silica gel column chromatography (solvent: n-hexane / ethyl acetate = 100 / 0 - 80 / 20) to give 1-(6-bromo-5-chloro-3,4-dihydro-1H-isoquinolin-2-yl)-2,2,2-trifluoroethanone (1.05 g; 87% yield) as a white solid.

[00331] 1H-NMR (400 MHz, CDCh) δ ppm: 3.05(2H, t), 3.87(2H, t), 4.76(2H, s), 6.96(1H, d), 7.53(1H, d)(*rotamers were observed in the NMR integration ratio of approximately 2:1)

[00332] (5) 1-(6-Bromo-5-chloro-3,4-dihydro-1H-isoquinolin-2-yl)2,2,2-trifluoroethanone (1.05 g) obtained in (4) above, 1-tert-butoxyvinyloxy-tert-butyl-dimethylsilane (285 mg), potassium carbonate (114 mg) and bis(tri-tert-butylphosphine) palladium(0) (63 mg) were dissolved in DMF (7 ml), and the mixture was stirred under microwave irradiation at 120°C for 1 h. Water was added to the reaction mixture, and the organic layer was extracted with ethyl acetate. The combined organic layer was washed successively with water and saturated brine, dried over anhydrous magnesium sulfate, and concentrated under reduced pressure. The residue obtained was purified by silica gel column chromatography (solvent: n-hexane / ethyl acetate = 100 / 0 - 30 / 70) to give tert-butyl 2-[5-chloro-2-(2,2,2-trifluoroacetyl)-3,4-dihydro-1H-isoquinolin-6-yl]acetate (1.02 g; 76% yield) as a colorless viscous oil. EM(ESI) m / z: 322.1[M-C4H8+H]+

[00333] (6) tert-butyl 2-[5-chloro-2-(2,2,2-trifluoroacetyl)-3,4-dihydro-1Hisoquinolin-6-yl]acetate (1.02 g) obtained in (5) above Petition 870250102069, dated 07 / 11 / 2025, pp. 615 / 861 174 / 389 mentioned, potassium hexacyanoferrate(II) trihydrate (1.65 g), [2(2-aminophenyl)phenyl]-chloropalladium; 2-dicyclohexylphosphino-2',4',6'-triisopropylbiphenyl (212 mg) and potassium acetate (530 mg) were dissolved in 1,4-dioxane (50 ml), water (15 ml) was added and the mixture was stirred at 100°C for 2 h. The reaction mixture was filtered, water was added to the filtrate, and the organic layer was extracted with ethyl acetate. The combined organic layer was washed successively with water and saturated brine, dried over anhydrous magnesium sulfate, and concentrated under reduced pressure. The residue obtained was purified by silica gel column chromatography (solvent: n-hexane / ethyl acetate = 100 / 0 - 80 / 20) to give tert-butyl 2-[5-cyano-2(2,2,2-trifluoroacetyl)-3,4-dihydro-1H-isoquinolin-6-yl]acetate (551 mg; 55% yield) as a brown viscous oil.

[00334] 1H-NMR (400 MHz, CDCh) δ ppm: 1.47(9H, s), 3.18(2H, t), 3.79(2H, s), 3.91(2H, t), 4.81(2H, s), 7.29(1H, d), 7.34(1H, d). (*Rotamers were observed at an NMR integration ratio of approximately 2:1)

[00335] (7) 2-[5-cyano-2-(2,2,2-trifluoroacetyl)-3,4-dihydro-1-Hisoquinolin-6-yl] tert-butyl acetate (551 mg) obtained in the above-mentioned (6) was dissolved in ethanol (9 ml), 1 mol / l aqueous sodium hydroxide solution (5.4 ml) was added and the mixture was stirred at room temperature for 1 h. Water was added to the reaction mixture and the organic layer was extracted with ethyl acetate. The combined organic layer was washed successively with water and saturated brine, dried over anhydrous magnesium sulfate, and concentrated under reduced pressure. The residue obtained was purified by silica-gel column chromatography (solvent: n-hexane / ethyl acetate = 100 / 0 - 0 / 100) to give the title compound (172 mg; 42% yield) as a white solid. EM(ESI) m / z: 273.3 [M+H]+ Petition 870250102069, dated 07 / 11 / 2025, pp. 616 / 861 175 / 389 Example of Reference 8: Production of tert-butyl 2-(1,2,3,4-tetrahydroisoquinolin-6-yl)acetate

[00336] (1) Benzyl 6-bromo-3,4-dihydro-1H-isoquinoline-2-carboxylate (2 g), tert-butyl-(1-methoxyvinyloxy)-dimethylsilane (2.5 ml), potassium carbonate (1.6 g) and bis(tri-tert-butylphosphine)palladium(0) (886 mg) were dissolved in DMF (19 ml), and the mixture was stirred under microwave irradiation at 120°C for 2 h. Water was added to the reaction mixture, and the organic layer was extracted with ethyl acetate. The combined organic layer was successively washed with water and saturated brine, dried over anhydrous magnesium sulfate, and concentrated under reduced pressure. The residue obtained was purified by silica gel column chromatography (solvent: n-hexane / ethyl acetate = 100 / 0 - 70 / 30) to give benzyl 6-(2-methoxy-2-oxoethyl)-3,4-dihydro-1H-isoquinoline-2-carboxylate (978 mg; 48% yield) as a yellow viscous oil.

[00337] 1H-NMR (400 MHz, CDCh) δ ppm: 2.84(2H,br-s), 3.58(2H, s), 3.69(3H, s), 3.72(2H, s), 4.63(2H, s), 5.18(21-1, s), 7.01-7.12(3H, m), 7.29-7.42(5H, m). (2) 6-(2-methoxy-2-oxoethyl)-3,4-dihydro-1H-isoquinoline-2-carboxylate benzyl (1.41 g) obtained in (1) above was dissolved in methanol (31 ml), 4 mol / l aqueous lithium hydroxide solution (9.2 ml) was added and the mixture was stirred at room temperature for 3 h. The reaction mixture was neutralized, and the organic layer was extracted with ethyl acetate. The combined organic layer was washed with saturated brine, dried over anhydrous magnesium sulfate and concentrated under reduced pressure to give a crude product (1.33 g) of 2-(2-phenylmethoxycarbonyl-3,4-dihydro-1H-isoquinoline-6-yl)acetic acid as a yellow viscous oil.

[00338] (3) The crude product (1.33 g) of 2-(2) acid Petition 870250102069, dated 07 / 11 / 2025, page 617 / 861 176 / 389 phenylmethoxycarbonyl-3,4-dihydro-1H-isoquinolin-6-yl)acetic acid obtained in (2) mentioned above was dissolved in toluene (13.6 ml), 1,1-di-tert-butoxy-N,N-dimethylmethanamine (4 ml) was added and the mixture was stirred at 120°C for 3 h. The reaction mixture was allowed to cool, concentrated under reduced pressure, and the residue obtained was purified by silica gel column chromatography (solvent: n-hexane / ethyl acetate = 100 / 0 - 70 / 30) to give benzyl 6-[2-[(2-methylpropan-2-yl)oxy]-2oxoethyl]-3,4-dihydro-1H-isoquinoline-2-carboxylate (428 mg; 26% yield) as a colorless viscous oil. EM(ESI) m / z: 380.4[MH]-

[00339] (4) To a solution of benzyl 6-[2-[(2-methylpropan-2-yl)oxy]-2-oxoethyl]3,4-dihydro-1H-isoquinoline-2-carboxylate (400 mg) obtained in (3) above, palladium(II) hydroxide (40 mg) was added in ethanol (3.3 ml), and the mixture was stirred under a hydrogen atmosphere at room temperature for 3 h. The reaction mixture was filtered through a membrane filter, and the filtrate was concentrated under reduced pressure to give a crude product (244 mg) of the title compound as a white solid. Reference Examples 9 to 21:

[00340] The corresponding starting compounds were treated in the same manner as in Reference Example 8 to obtain the crude products of the compounds described in Tables 1-1 and 1-2 below. Petition 870250102069, dated 07 / 11 / 2025, pp. 618 / 861 177 / 389 Table 1-1 Example of structural formula of Reference No. Example of Reference No. 4 Structural Formula Me Me Me Me Petition 870250102069, dated 07 / 11 / 2025, pp. 619 / 861 178 / 389

[0470] Table 1-2 Example of Reference 22: Production of (2S)-1-(1,2,3,4-tetrahydroisoquinolin-6-yl)piperidine-2-

[00341] (1) To a solution of benzyl 6-bromo-3,4-dihydro-1H-isoquinoline-2-carboxylate (1.00 g), tert-butyl (2S)-piperidine-2-carboxylate (800 mg), bis(dibenzylideneacetone)palladium(0) (270 mg), 2-di Petition 870250102069, dated 07 / 11 / 2025, pp. 620 / 861 179 / 389 cyclohexylphosphino-2',6'-diisopropoxybiphenyl (135 mg) etoluene (30 ml) was added to sodium tert-butoxide (1.10 g) and the mixture was stirred at 120°C for 1 h. The reaction mixture was allowed to cool, water was added to it, and the organic layer was extracted with ethyl acetate. The combined organic layer was dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue obtained was purified by silica gel column chromatography (solvent: n-hexane / ethyl acetate = 90 / 10 - 60 / 40) to give 6-[(2S)-2-[(2-methylpropan-2-yl)oxycarbonyl]piperidin-1-yl]-3,4-dihydro-1H-isoquinoline-2-carboxylate (113 mg; 9% yield) as a brown viscous oil. EM(ESI) m / z: 451.4[M+H]+

[00342] (2) 6-[(2S)-2-[(2-methylpropan-2-yl)oxycarbonyl]piperidin-1-yl]3,4-dihydro-1H-isoquinoline-2-carboxylate benzyl (113 mg) obtained in (1) above was dissolved in methanol (5 ml), 10% palladium carbonate (100 mg) was added, and the mixture was stirred under a hydrogen atmosphere at room temperature for 3 h. The reaction mixture was filtered through Celite, and the filtrate was concentrated under reduced pressure to provide a crude product of the title compound as a brown solid. Example of Reference 23: Production of tert-butyl 1-(1,2,3,4-tetrahydroisoquinolin-6-yl)pyrrolidine-3-carboxylate

[00343] (1) To a solution of benzyl 6-bromo-3,4-dihydro-1H-isoquinoline-2-carboxylate (1.00 g), tert-butyl pyrrolidine-3-carboxylate (600 mg), bis(dibenzylideneacetone)palladium(0) (270 mg), 2-dicyclo Petition 870250102069, dated 07 / 11 / 2025, pp. 621 / 861 180 / 389 hexylphosphine-2',6'-diisopropoxybiphenyl (135 mg) and toluene (30 ml) were added to sodium tert-butoxide (1.10 g), and the mixture was stirred at 120°C for 1 h. The reaction mixture was allowed to cool, water was added, and the organic layer was extracted with ethyl acetate. The combined organic layer was dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue obtained was purified by silica gel column chromatography (solvent: n-hexane / ethyl acetate = 90 / 10 - 60 / 40) to give 6-[3-[(2-methylpropan-2-yl)oxycarbonyl]pyrrolidin-1-yl]-3,4-dihydro-1H-isoquinoline-2-carboxylate benzyl (517 mg; 41% yield) as a brown viscous oil. MS(ESI) m / z: 436.9 [M+H]+

[00344] (2) 6-[3-[(2-methylpropan-2-yl)oxycarbonyl]pyrrolidin-1-yl]-3,4-dihydro-1H-isoquinoline-2-carboxylate benzyl (517 mg) obtained in (1) above was dissolved in methanol (30 ml), 10% palladium-carbon (200 mg) was added, and the mixture was stirred under a hydrogen atmosphere at room temperature for 3 h. The reaction mixture was filtered through Celite, and the filtrate was concentrated under reduced pressure to give the title compound (311 mg; 87% yield) as a yellow solid. EM(ESI) m / z: 303.3 [M+H]+ Example of Reference 24: Production of tert-butyl 1-(1,2,3,4-tetrahydroisoquinolin-6-yl)piperidine-4-carboxylate

[00345] (1) To a solution of benzyl 6-bromo-3,4-dihydro-1H-isoquinoline-2-carboxylate (1.00 g), tert-butyl piperidine-4-carboxylate hydrochloride (770 mg), bis(dibenzylideneacetone)palladium(0) (270 mg), Petition 870250102069, dated 07 / 11 / 2025, pp. 622 / 861 181 / 389 2-dicyclohexylphosphino-2',6'-diisopropoxybiphenyl (135 mg) and toluene (30 ml) were added to N,N-diisopropylethylamine (0.6 ml) and sodium tert-butoxide (840 mg), and the mixture was stirred at 120°C for 1 h. The reaction mixture was allowed to cool, water was added, and the organic layer was extracted with ethyl acetate. The combined organic layer was dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The residue obtained was purified by silica-gel column chromatography (solvent: n-hexane / ethyl acetate = 90 / 10 - 60 / 40) to give benzyl 6-[4-[(2-methylpropan-2-yl)oxycarbonyl]piperidin-1-yl]-3,4-dihydro-1H-isoquinoline-2-carboxylate (1.11 g; 85% yield) as a brown viscous oil. EM(ESI) m / z: 450.9[M+H]+

[00346] (2) 6-[4-[(2-methylpropan-2-yl)oxycarbonyl]piperidin-1-yl]-3,4-dihydro-1H-isoquinoline-2-carboxylate benzyl (1.11 g) obtained in (1) above was dissolved in methanol (10 ml), 10% palladium carbonate (200 mg) was added, and the mixture was stirred under a hydrogen atmosphere at room temperature for 3 h. The reaction mixture was filtered through Celite, and the filtrate was concentrated under reduced pressure to give the title compound (707 mg; 91% yield) as a brown solid. EM(ESI) m / z: 317.3 [M+H]+ Example of Reference 25: Production of tert-butyl 2-methyl-3-(1,2,3,4-tetrahydroisoquinolin-6-yl)propanoate

[00347] (1) benzyl 6-bromo-3,4-dihydro-1H-isoquinoline-2-carboxylate (1 g), tert-butyl 2-methylprop-2-enoate (821 mg), potassium carbonate (567 mg) and [1,3-bis(2,6-diisopropyl phenyl)imidazole dichloride Petition 870250102069, dated 07 / 11 / 2025, pp. 623 / 861 182 / 389 2-ylidene(3-chloropyridyl)palladium(II) (394 mg) were dissolved in DMF (6 ml), and the mixture was stirred under microwave irradiation at 120°C for 2 h. Water was added to the reaction mixture, and the organic layer was extracted with ethyl acetate. The combined organic layer was washed successively with water and saturated brine, dried over anhydrous magnesium sulfate, and concentrated under reduced pressure. The residue obtained was purified by silica gel column chromatography (solvent: n-hexane / ethyl acetate = 100 / 0 - 30 / 70) to give benzyl 6-[2-methyl-3-[(2-methylpropan-2-yl)oxy]-3-oxoprop-1-enyl]-3,4-dihydro-1H-isoquinoline-2-carboxylate (1.06 g; yield of 32%) as a colorless viscous oil. MS(ESI) m / z: 352.2 [M-C4H8+H]+

[00348] (2) To a solution of benzyl 6-[2-methyl-3-[(2-methylpropan-2-yl)oxy]-3oxoprop-1-enyl]-3,4-dihydro-1H-isoquinoline-2-carboxylate (1.06 g) obtained in (1) above in ethanol (4 ml) was added palladium(II) hydroxide (48 mg), and the mixture was stirred under a hydrogen atmosphere at room temperature for 3 h. The reaction mixture was filtered through Celite, and the filtrate was concentrated under reduced pressure to give a crude product (1.04 g) of the title compound as a colorless viscous oil. Example of Reference 26: Production of tert-butyl 3-(1,2,3,4-tetrahydroisoquinolin-6-yl)butanoate

[00349] (1) Benzyl 6-bromo-3,4-dihydro-1H-isoquinoline-2-carboxylate (1 g), tributyl(1-ethoxyvinyl)tin (1.27 ml) and bis(tri-tert-butylphosphine)palladium(O) (74 mg) were dissolved in DMF (9 ml), and the mixture was stirred under microwave irradiation at 100°C for 1 h. Petition 870250102069, dated 07 / 11 / 2025, pp. 624 / 861 183 / 389 To the reaction mixture, 1 mol / L of hydrochloric acid was added, and the mixture was stirred at room temperature for 1 h. Water was added to the reaction mixture, and the organic layer was extracted with ethyl acetate. The combined organic layer was washed with saturated brine, dried over anhydrous magnesium sulfate, and concentrated under reduced pressure. The residue obtained was purified by silica gel column chromatography (solvent: n-hexane / ethyl acetate = 100 / 0 60 / 40) to give benzyl 6-acetyl-3,4-dihydro-1H-isoquinoline-2-carboxylate (67.1 mg; 8% yield) as a colorless viscous oil. 1H-NMR (400 MHz, CDCb) δ ppm: 2.58(3H, s),2.91(2H, br-s), 3.75(2H, t), 4.70(2H, s),5.19(2H, s), 7.20(1H, br-s), 7.29-7.45(5H, m), 7.74(1H, s), 7.77(1H, d).

[00350] (2) To a solution of tert-butyl 2-diethoxyphoryl acetate (109 mg) in THF (1.4 ml) was added sodium hydride (60%, 17 mg). To the reaction mixture was added a solution of benzyl 6-acetyl-3,4-dihydro-1H-isoquinoline-2-carboxylate (67.1 mg) obtained in (1) above in THF, and the mixture was stirred at room temperature for 18 h. Water was added to the reaction mixture, and the organic layer was extracted with ethyl acetate. The combined organic layer was washed with saturated brine, dried over anhydrous magnesium sulfate, and concentrated under reduced pressure. The residue obtained was purified by silica-gel column chromatography (solvent: n-hexane / ethyl acetate = 100 / 0 - 70 / 30) to give benzyl 6-[4-[(2-methylpropan-2-yl)oxy]-4-oxobut-2-en-2-yl]-3,4-dihydro-1H-isoquinoline-2-carboxylate (68.5 mg; 78% yield) as a colorless viscous oil.

[00351] 1H-NMR (400 MHz, CDCh) δ ppm: 1.52(9H, s), 2.51(3H, d), 2.86(2H, br-s), 3.73(2H, br-s), 4.66(2H, s), 5.18(2H, s), 6.03(1H, d), 6.94-7.16(2H, m), 7.20-7.43(6H, m). (*Isomeric mixture of approximately a 3:1 NMR integration ratio) Petition 870250102069, dated 07 / 11 / 2025, pp. 625 / 861 184 / 389

[00352] (3) To a solution of benzyl 6-[4-[(2-methylpropan-2-yl)oxy]-4-oxobut-2-en-2-yl]-3,4-dihydro-1H-isoquinoline-2-carboxylate (68.5 mg) obtained in (2) above in ethanol (1 ml) palladium(II) hydroxide (8 mg) was added, and the mixture was stirred under a hydrogen atmosphere at room temperature for 3 h. The reaction mixture was filtered through Celite, and the filtrate was concentrated under reduced pressure to give a crude product (46.3 mg) of the title compound as a colorless viscous oil. Example of Reference 27: Production of tert-butyl 1-(1,2,3,4-tetrahydroisoquinolin-6-yl)cyclopropane-1-carboxylate

[00353] (1) A mixture of benzyl 6-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-3,4-dihydro-1H-isoquinoline-2-carboxylate (2.2 g), tert-butyl 2-bromoacrylate (1.1 g), bis(di-tert-butyl(4-dimethylaminophenyl)phosphine)dichloropalladium(II) (190 mg), cesium carbonate (3.5 g), 1,4-dioxane (20 ml) and water (4 ml) was stirred in a microwave reactor at 140°C for 1 h. After cooling to room temperature, the reaction mixture was filtered and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (solvent: n-hexane / ethyl acetate = 100 / 0 - 70 / 30) to give 6[3-[(2-methylpropan-2-yl)oxy]-3-oxoprop-1-en-2-yl]-3,4-dihydro-1-Hisoquinoline-2-carboxylate benzyl (725 mg; yield of 31%) as a brown oil. EM(ESI) m / z: 338.1[M-C4H8+H]+

[00354] (2) To a DMSO solution (6 ml) of trimethylsulfoxonium iodide (810 mg) were added 60% sodium hydride (148 mg) at 0°C, and the mixture was stirred for 10 min. A DMSO solution of 6-[3-[(2-methylpropan-2-yl)oxy]-3-oxoprop-1-en-2-yl]-3,4-di Petition 870250102069, dated 07 / 11 / 2025, pp. 626 / 861 Benzyl 1H-isoquinoline-2-carboxylate (725 mg; 89 wt%) obtained in (1) above was added to this, and the mixture was stirred at room temperature for 18 h. Water was added to the reaction mixture, and the mixture was extracted with ethyl acetate. The organic layer was washed with saturated brine, dried over anhydrous magnesium sulfate, and concentrated under reduced pressure. The residue obtained was purified by silica gel column chromatography (solvent: n-hexane / ethyl acetate = 100 / 0 - 70 / 30) to give benzyl 6-[1-[(2-methylpropan-2-yl)oxycarbonyl]cyclopropyl]-3,4-dihydro-1H-isoquinoline-2-carboxylate (454 mg; 55% yield) as a yellow oil.

[00355] Ή-NMR (400 MHz, CDCb) δ ppm: 1.08-1.10(2H,m),1.38 (9H,s), 1.47-1.51(2H,m),3.71(2H,br),2.83(2H,br),4.62(2H,s),5.17 (2H,s), 7.00-7.15(3H,m),7.30-7.39(5H,m).

[00356] (3) To the benzyl 6-[1-[(2-methylpropan-2-yl)oxycarbonyl]cyclopropyl]-3,4-dihydro-1H-isoquinoline-2-carboxylate (454 mg) obtained in (2) above, ethanol (4 ml) and 20% palladium hydroxide (45 mg) were added, and the mixture was stirred under a hydrogen atmosphere at room temperature for 3 h. The reaction mixture was filtered through Celite, and the filtrate was concentrated under reduced pressure to give a crude product (277 mg) of the title compound as a colorless oil. Example of Reference 28: Production of tert-butyl 2-methyl-2-(1,2,3,4-tetrahydroisoquinolin-6-yl)propanoate Me Me

[00357] (1) 60% sodium hydride (25.6 mg) was added to DMSO (1.6 ml). Methyl iodide was added to the reaction mixture. Petition 870250102069, dated 07 / 11 / 2025, pp. 627 / 861 186 / 389 (90 mg) and a solution of 6-[2-[(2-methylpropan-2-yl)oxy]-2-oxoethyl]-3,4-dihydro-1H-isoquinoline-2-benzyl carboxylate (130 mg) in THF (1.6 ml) at 0°C, and the reaction mixture was stirred at room temperature for 4 h. Water was added to the reaction mixture, and the mixture was extracted with ethyl acetate. The organic layer was washed with saturated brine, dried over anhydrous magnesium sulfate, and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (solvent: n-hexane / ethyl acetate = 100 / 0 - 50 / 50) to give benzyl 6-[1-[(2-methylpropan-2-yl)oxy]-1-oxopropan-2-yl]-3,4-dihydro-1H-isoquinoline-2-carboxylate (79.7 mg; yield of 52%) as a colorless oil. EM(ESI) m / z: 340.1[M-C4H8+H]+

[00358] (2) 60% sodium hydride (26 mg) was added to DMSO (1.2 ml). Methyl iodide (91 mg) and a solution of benzyl 6-[1-[(2-methylpropan-2-yl)oxy]-1-oxopropan-2yl]-3,4-dihydro-1H-isoquinoline-2-carboxylate (79.7 mg) obtained in (1) above in THF (1.2 ml) at 0°C were added to the reaction mixture, and the reaction mixture was stirred at room temperature for 18 h. Water was added to the reaction mixture, and the mixture was extracted with ethyl acetate. The organic layer was washed with saturated brine, dried over anhydrous magnesium sulfate, and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (solvent: n-hexane / ethyl acetate = 100 / 0 - 85 / 15) to give 6-[2-methyl-1-[(2-methylpropan-2-yl)oxy]-1-oxopropan-2-yl]-3,4-dihydro-1-Hisoquinoline-2-carboxylate (22.4 mg; yield of 33%) as a colorless oil. EM(ESI) m / z: 354.2[M-C4H8+H]+

[00359] (3) To the benzyl 6-[2-methyl-1-[(2-methylpropan-2-yl)oxy]-1-oxopropan-2yl]-3,4-dihydro-1H-isoquinoline-2-carboxylate (22.4 mg) obtained in (2) above, ethanol (0.6 ml) and 20% of Petition 870250102069, dated 07 / 11 / 2025, pp. 628 / 861 187 / 389 palladium hydroxide (4 mg), and the mixture was stirred under a hydrogen atmosphere at room temperature for 3 h. The reaction mixture was filtered through Celite and concentrated under reduced pressure to give a crude product (15.1 mg) of the title compound as a colorless oil. Example of Reference 29: Production of tert-butyl 4-(1,2,3,4-tetrahydroisoquinolin-6-yl)butanoate

[00360] (1) To a solution of benzyl 6-bromo-3,4-dihydro-1H-isoquinoline-2-carboxylate (1 g) in 1,4-dioxane (10 ml) were added [1,3-bis(2,6-diisopropylphenyl)imidazol-2-ylidene](3-chloropyridyl)palladium(II) dichloride (197 mg) and 4-ethoxy-4-oxobutylzinc bromide (1 mol / L, 3.5 ml), and the mixture was stirred in a nitrogen atmosphere at room temperature for 3 h. Water was added to the reaction mixture, and the mixture was extracted with ethyl acetate. The organic layer was washed with saturated brine, dried over anhydrous magnesium sulfate, and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (solvent: n-hexane / ethyl acetate = 100 / 0 - 0 / 100) to give benzyl 6-(4-ethoxy-4-oxobutyl)-3,4-dihydro-1H-isoquinoline-2-carboxylate (183 mg; 17% yield) as a yellow oil.

[00361] Ή-NMR (400 MHz, CDCb) δ ppm: 1.25(3H,t), 1.89-1.94 (2H,m), 2.29-2.33(2H,m), 2.60-2.61(2H,m), 2.82(2H,br), 3.72(2H,br), 4.13 (2H,q), 4.62(2H,s), 5.18(2H,s), 6.95-7.00(3H,m), 7.30-7.40(5H,m).

[00362] (2) To a reaction mixture of benzyl 6-(4-ethoxy-4-oxobutyl)-3,4-dihydro-1H-isoquinoline-2-carboxylate (183 mg) obtained in (1) Petition 870250102069, dated 07 / 11 / 2025, pp. 629 / 861 188 / 389 mentioned above and methanol (1.6 ml) was added to 4N aqueous lithium hydroxide solution (0.48 ml), and the mixture was stirred at room temperature for 12 h. The reaction mixture was neutralized with 1N hydrochloric acid and extracted with ethyl acetate. The organic layer was washed with saturated brine, dried over anhydrous magnesium sulfate, and concentrated under reduced pressure to give a crude product (159 mg) of 4-(2-phenylmethoxycarbonyl-3,4-dihydro-1H-isoquinolin-6-yl)butanoic acid as a yellow oil.

[00363] (3) To a mixture solution of the crude product (159 mg) of 4-(2-phenylmethoxycarbonyl-3,4-dihydro-1H-isoquinolin-6-yl)butanoic acid obtained in (2) above and toluene (1.5 ml) was added N,N-dimethylformamide di-tert-butylacetal (0.3 ml), and the mixture was stirred at 120°C for 1 h. The reaction mixture was cooled to room temperature, and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (solvent: n-hexane / ethyl acetate = 100 / 0 - 70 / 30) to give benzyl 6-[4-[(2-methylpropan-2-yl)oxy]-4-oxobutyl]-3,4-dihydro-1H-isoquinoline-2-carboxylate (57 mg; 31% yield) as a colorless oil.

[00364] 1H-NMR (400 MHz, CDCh) δ ppm: 1.44(9H,s), 1.841.92(2H,m), 2.21-2.24(2H,m),2.56-1.61(2H,m), 2.82(2H,br), 3.71(2H,br), 4.62(2H,s), 5.18(2H,s), 6.95-7.03(3H,m), 7.36-7.40(5H,m).

[00365] (4) To the benzyl 6-[4-[(2-methylpropan-2-yl)oxy]-4-oxobutyl]-3,4-dihydro-1H-isoquinoline-2-carboxylate (57 mg) obtained in (3) above, ethanol (0.9 ml) and 20% palladium hydroxide (4 mg) were added, and the mixture was stirred under a hydrogen atmosphere at room temperature for 3 h. The reaction mixture was filtered through Celite and concentrated under reduced pressure to give a crude product (39 mg) of the title compound as a colorless oil. Example of Reference 30: Production of 2-(1,2,3,4-tetrahydroisoquinolin-6-yl)propanoate of tert-1-(1,2,3,4-tetrahydroisoquinolin-6-yl)propanoate. Petition 870250102069, dated 07 / 11 / 2025, pages 630 / 861 189 / 389 butyl Me

[00366] To benzyl 6-[1-[(2-methylpropan-2-yl)oxy]-1-oxopropan-2-yl]-3,4-dihydro-1H-isoquinoline-2-carboxylate (85.4 mg) obtained in Reference Example 28, (1), ethanol (1.4 ml) and 20% palladium hydroxide (10 mg) were added, and the mixture was stirred under a hydrogen atmosphere at room temperature for 3 h. The reaction mixture was filtered through Celite, and the filtrate was concentrated under reduced pressure to give a crude product (56.4 mg) of the title compound as a yellow oil. Example of Reference 31: Production of tert-butyl rac-(1R,2R)-2-(1,2,3,4-tetrahydroisoquinolin-6-yl)cyclopropane-1-carboxylate Me O

[00367] (1) A mixture of benzyl 6-bromo-3,4-dihydro-1H-isoquinoline-2-carboxylate (1.5 g), 4,4,5,5-tetramethyl-2-vinyl-1,3,2-dioxaborolane (800 mg), bis(di-tert-butyl(4-dimethylaminophenyl)phosphine)dichloropalladium(II) (155 mg), cesium carbonate (2.8 g), 1,4-dioxane (14 mL) and water (2 mL) was stirred in a microwave reactor at 140°C for 1 h. After cooling to room temperature, the reaction solution was concentrated under reduced pressure. The residue was purified by silica gel column chromatography (solvent: n-hexane / ethyl acetate = 100 / 0 - 80 / 20) to give benzyl 6-ethenyl-3,4-dihydro-1H-isoquinoline-2-carboxylate (734 mg; 55% yield) as a colorless oil. EM(ESI) m / z: 294.1[M+H]+ Petition 870250102069, dated 07 / 11 / 2025, pp. 631 / 861 190 / 389

[00368] (2) 6-ethenyl-3,4-dihydro-1H-isoquinoline-2-carboxylate benzyl (734 mg) obtained in (1) above was dissolved in 1,4-dioxane (8 ml), sodium periodate (1 g), 2,6-lutidine (0.56 ml) and 2.5 wt% osmium tert-butanol-tetraoxide solution (2.4 ml) were added and the mixture was stirred at room temperature for 18 h. The reaction solution was filtered and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (solvent: n-hexane / ethyl acetate = 100 / 0 - 70 / 30) to give benzyl 6-formyl-3,4-dihydro-1H-isoquinoline-2-carboxylate (565 mg; 74% yield) as a colorless oil. EM(ESI) m / z: 296.2[M+H]+

[00369] (3) A reaction mixture of benzyl 6-formyl-3,4-dihydro-1-Hisoquinoline-2-carboxylate (1.06 g) obtained in (2) above, tert-butyl dietoxyphosphoryl acetate (1.8 g), 1,1,3,3-tetramethylguanidine (830 mg) and THF (11 ml) was stirred at room temperature for 12 h. The reaction solution was concentrated under reduced pressure. The residue was purified by silica gel column chromatography (solvent: n-hexane / ethyl acetate = 100 / 0 - 70 / 30) to give benzyl 6-[(E)-3-[(2-methylpropan-2-yl)oxy]-3-oxoprop-1-enyl]-3,4-dihydro-1H-isoquinoline-2-carboxylate (698 mg; yield of 46%) as a white solid. EM(ESI) m / z: 392.4[MH]-

[00370] (4) To a DMSO solution (12 ml) of trimethylsulfoxonium iodide (1.6 g) were added 60% sodium hydride (288 mg) at 0°C, and the mixture was stirred for 10 min. To the reaction mixture was added a DMSO solution of 6-[(E)-3-[(2-methylpropan-2-yl)oxy]-3-oxoprop-1-enyl]-3,4-dihydro-1H-isoquinoline-2-carboxylate benzyl (698 mg) obtained in (3) above, and the mixture was stirred at room temperature for 18 h. Water was added to the reaction mixture, and the mixture was extracted with acetate. Petition 870250102069, dated 07 / 11 / 2025, pp. 632 / 861 191 / 389 ethyl. The organic layer was washed with saturated brine, dried over anhydrous magnesium sulfate, and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (solvent: n-hexane / ethyl acetate = 100 / 0 - 70 / 30) to give 6[rac-(1R,2R)-2-[(2-methylpropan-2-yl)oxycarbonyl]cyclopropyl]-3,4-dihydro1H-isoquinoline-2-carboxylate benzyl (129 mg; 19% yield) as a colorless oil.

[00371] 1H-NMR (400 MHz, CDCb) δ ppm: 1.18-1.21(1H,m),1.46 (9H,s),1.47-1.50(1 H,m),1.80-1.82(1 H,m), 2.38-2.41(1 H,m), 2.81 (br, 1H), 3.70(1H,br), 4.61 (2H,s), 5.17(2H,s), 6.87-7.02(3H,m), 7.33-7.39(5H,m).

[00372] (5) To the 6-[rac-(1R,2R)-2-[(2-methylpropan-2yl)oxycarbonyl]cyclopropyl]-3,4-dihydro-1H-isoquinoline-2-carboxylate benzyl (129 mg) obtained in (4) above, ethanol (1 ml) and 20% palladium hydroxide (12 mg) were added, and the mixture was stirred under a hydrogen atmosphere at room temperature for 3 h. The reaction mixture was filtered through Celite, and the filtrate was concentrated under reduced pressure to give the title compound (107 mg; 97% yield) as a grey oil. EM(ESI) m / z: 274.3[M+H]+ Example of Reference 32: Production of 1-(5,6,7,8-tetrahydro-2,7-naphthyridin-3-yl)piperidine-4-tert-butylcarboxylate

[00373] (1) A mixture of benzyl 6-chloro-3,4-dihydro-1H-2,7-naphthyridine-2-carboxylate (300 mg), DMSO (3 ml), diisopropylethylamine (0.33 ml) and tert-butyl piperidine-4-carboxylate hydrochloride (250 mg) was stirred in a microwave reactor at 180°C for 1 h. After Petition 870250102069, dated 07 / 11 / 2025, pp. 633 / 861 192 / 389 Cooling to room temperature, water was added to the reaction mixture, and the mixture was extracted with ethyl acetate. The organic layer was washed with saturated brine, dried over anhydrous magnesium sulfate, and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (solvent: nhexane / ethyl acetate = 100 / 0 - 40 / 60) to give 6-[4-[(2-methylpropan-2-yl)oxycarbonyl]piperidin-1-yl]-3,4-dihydro-1H-2,7-naphthyridine-2-benzyl carboxylate (117 mg; 22% yield) as a yellow oil. EM(ESI) m / z: 452.3[M+H]+

[00374] (2) To the benzyl 6-[4-[(2-methylpropan-2-yl)oxycarbonyl]piperidin-1-yl]-3,4-dihydro-1H-2,7-naphthyridine-2-carboxylate (117 mg) obtained in (1) above, ethanol (1 ml) and 20% palladium hydroxide (12 mg) were added, and the mixture was stirred under a hydrogen atmosphere at room temperature for 3 h. The reaction mixture was filtered through Celite, and the filtrate was concentrated under reduced pressure to give a crude product (65 mg) of the title compound as a yellow solid. Example of Reference 33: Production of tert-butyl 3-(1,2,3,4-tetrahydroisoquinolin-6-yl)propanoate

[00375] (1) 6-bromo-1,2,3,4-tetrahydroisoquinoline (12 g) was dissolved in pyridine (47 ml), N,N-dimethylpyridine-4-amine (172 mg), trifluoroacetic anhydride (6 g) were added, and the mixture was stirred at room temperature for 18 h. The reaction mixture was Petition 870250102069, dated 07 / 11 / 2025, pp. 634 / 861 Concentrated 193 / 389, ethyl acetate was added to the residue and the mixture was washed with 1N hydrochloric acid. The organic layer was dried and concentrated, and the residue was purified by silica gel column chromatography (solvent: n-hexane / ethyl acetate = 100 / 0 - 70 / 30) to give 1-(6-bromo-3,4-dihydro-1H-isoquinolin-2-yl)-2,2,2-trifluoroethanone (11.8 g; 68% yield) as a white solid. MS(ESI) m / z: 308.0 / 310.0[M+H]+

[00376] (2) 1-(6-Bromo-3,4-dihydro-1H-isoquinolin-2-yl)-2,2,2-trifluoroethanone (2.4 g) obtained in (1) above was dissolved in 1,4-dioxane (16 ml), water (4 ml), 4,4,5,5-tetramethyl-2-vinyl-1,3,2-dioxaborolane (1.16 g), bis[di-tert-butyl(4-dimethylaminophenyl)phosphine]dichloropalladium(II) (178 mg) and cesium carbonate (3.3 g) were mixed with it, and stirring using a microwave reactor at 140°C for 1 h. The reaction solution was filtered, and the filtrate was concentrated. The residue was purified by silica gel column chromatography (solvent: n-hexane / ethyl acetate = 100 / 0 - 80 / 20) to give 1-(6-ethenyl-3,4-dihydro-1H-isoquinolin-2-yl)-2,2,2-trifluoroethanone (903 mg; 44%) as a white solid. EM(ESI) m / z: 256.2[M+H]+

[00377] (3) 1-(6-ethenyl-3,4-dihydro-1H-isoquinolin-2-yl)-2,2,2-trifluoroethanone (903 mg) obtained in (2) above was dissolved in 1,4-dioxane (12 ml), water (3 ml), 2,6-lutidine (0.78 ml), 2.5 wt% osmium tert-butanol-tetraoxide solution (3.5 ml) and sodium periodate (1.4 g) were added, and the mixture was stirred at room temperature for 18 h. The reaction solution was filtered, and the filtrate was concentrated. The residue was purified by silica gel column chromatography (solvent: n-hexane / ethyl acetate = 80 / 20 - 50 / 50) to give 2-(2,2,2-trifluoroacetyl)-3,4-dihydro-1H-isoquinoline-6-carbaldehyde (573 mg; 66%) as a white solid. EM(ESI) m / z: 258.0[M+H]+. Petition 870250102069, dated 07 / 11 / 2025, pp. 635 / 861 194 / 389

[00378] (4) The 2-(2,2,2-trifluoroacetyl)-3,4-dihydro-1H-isoquinoline-6-carbaldehyde (573 mg) obtained in (3) above was dissolved in THF (7 ml), 1,1,3,3-tetramethylguanidine (513 mg) and 2-diethoxyphoryl tert-butyl acetate (843 mg) were added to this, and the mixture was stirred at room temperature for 3 h. The reaction solution was concentrated, and the residue was purified by silica-gel column chromatography (solvent: n-hexane / ethyl acetate = 100 / 0 - 70 / 30) to give tert-butyl (E)-3-[2-(2,2,2-trifluoroacetyl)-3,4-dihydro-1H-isoquinolin-6yl]prop-2-enoate (544 mg; 63%) as a colorless oil. 1H-NMR (400 MHz, CDCh) δ ppm: 1.56(9H,s), 2.99(2H,t), 3.88(2H,t), 4.82(2H,s), 6.38(1H,d), 7.19(1H,d), 7.32(1H,s), 7.41(1H,d), 7.56(1H,d). (*rotameric mixture of approximately 2:1 NMR integration ratio)

[00379] (5) tert-butyl (E)-3-[2-(2,2,2-trifluoroacetyl)-3,4-dihydro-1H-isoquinolin-6-yl]prop-2-enoate (544 mg) obtained in (4) above was dissolved in ethanol (6 ml), palladium hydroxide activated carbon (55 mg) was added, and the mixture was stirred under a hydrogen atmosphere at room temperature for 3 h. The reaction solution was filtered through a membrane filter, and the filtrate was concentrated under reduced pressure, a crude product (527 mg) of tert-butyl 3-[2-(2,2,2-trifluoroacetyl)-3,4-dihydro-1H-isoquinolin-6-yl]propanoate as a colorless oil.

[00380] 1H-NMR (400 MHz, CDCh) δ ppm: 1.35(9H,s), 2.45(2H,t), 2.80(2H,t), 2.85(2H,t), 3.76(2H,t), 4.69(2H,s), 7.01-6.92(3H,m). (*rotameric mixture of approximately 2:1 NMR integration ratio)

[00381] (6) The crude product (527 mg) of tert-butyl 3-[2-(2,2,2-trifluoroacetyl)3,4-dihydro-1H-isoquinolin-6-yl]propanoate obtained in (5) above was dissolved in ethanol (5 ml), aqueous sodium hydroxide solution (4 mol / l, 1.5 ml) was added, and the mixture was stirred at room temperature for 3 h. Water was added to the reaction mixture, and the mixture was extracted with ethyl acetate. The organic layer was washed with saturated brine, dried, and concentrated to provide Petition 870250102069, dated 07 / 11 / 2025, pp. 636 / 861 195 / 389 a crude product (377 mg) of the title compound as a colorless oil. Example of Reference 34: Production of 2-[(8-bromo-1,2,3,4-tetrahydroisoquinolin-6-yl)oxy] tert-butyl acetate

[00382] (1) A mixture of 8-bromo-6-methoxy-1,2,3,4-tetrahydroisoquinoline (180 mg) and 50% hydrobromic acid (4 ml) was stirred at 130°C for 8 h. After cooling to room temperature, the reaction mixture was concentrated under reduced pressure. To a solution of the residue obtained, 1,4-dioxane (1 ml) and water (1 ml) were added 1N aqueous sodium hydroxide solution (2 ml) and benzyl chloroformate (0.15 ml) under cooling in an ice bath, and the mixture was stirred for 1 h. Saturated aqueous ammonium chloride solution was added to the reaction mixture, and the mixture was extracted with ethyl acetate. The organic layer was washed with saturated brine, dried over anhydrous magnesium sulfate, and concentrated under reduced pressure.The residue was purified by silica gel column chromatography (solvent: n-hexane / ethyl acetate = 90 / 10 - 50 / 50) to give benzyl 8-bromo-6-hydroxy-3,4-dihydro-1H-isoquinoline-2-carboxylate (53 mg; 23% yield) as a colorless oil. EM(ESI) m / z: 360.1 / 362.1 [MH]'

[00383] (2) To a solution of benzyl 8-bromo-6-hydroxy-3,4-dihydro-1-Hisoquinoline-2-carboxylate (53 mg) obtained in (1) above, DMF (0.5 ml) and THF (0.1 ml) were added to 60% sodium hydride (9 mg) under ice bath cooling, and the mixture was stirred for 5 min. The mixture was heated to room temperature, tert-butyl bromoacetate (47 mg) was added, and the mixture was stirred for 1 h. Saturated aqueous ammonium chloride solution was added to the reaction mixture, and the mixture was extracted. Petition 870250102069, dated 07 / 11 / 2025, pp. 637 / 861 196 / 389 with chloroform. The organic layer was washed with saturated brine, dried over anhydrous magnesium sulfate, and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (solvent: n-hexane / ethyl acetate = 90 / 10 - 70 / 30) to give 8-bromo-6-[2-[(2-methylpropan-2-yl)oxy]-2-oxoethoxy]-3,4-dihydro-1-Hisoquinoline-2-carboxylate benzyl (64 mg; 92% yield) as a colorless oil. MS(ESI) m / z: 493.0 / 495.0 [M+NH4]+

[00384] (3) To a solution of palladium acetate (7 mg) and dichloromethane (1.0 ml) were added triethylamine (0.02 ml), triethylsilane (0.032 ml) and benzyl 8-bromo-6-[2-[(2-methylpropan-2-yl)oxy]-2oxoethoxy]-3,4-dihydro-1H-isoquinoline-2-carboxylate (64 mg) obtained in (2) above under a nitrogen atmosphere, and the mixture was stirred at room temperature for 30 min. The reaction mixture was filtered through Celite, and the filtrate was concentrated under reduced pressure to give a crude product of tert-butyl 2-[(8-bromo-1,2,3,4-tetrahydroisoquinoline-6-yl)oxy]acetate as a brown oil. EM(ESI) m / z: 342.1 / 344.1 [M+H]+ Example of Reference 35: Production of tert-butyl 2-[(8-fluoro-1,2,3,4-tetrahydroisoquinolin-6-yl)oxyl-2-methylpropanoate]

[00385] (1) Benzyl 8-fluoro-6-hydroxy-3,4-dihydro-1H-isoquinoline-2-carboxylate (101 mg) was dissolved in DMF (1 ml), potassium carbonate (52 mg) and tert-butyl 2-bromo-2-methylpropanoate (0.064 ml) were added, and the reaction mixture was stirred at room temperature for 5 h. Potassium carbonate (49 mg) and tert-butyl 2-bromo-2-methylpropanoate (0.064 ml) were added to the reaction mixture. Petition 870250102069, dated 07 / 11 / 2025, pp. 638 / 861 197 / 389 ml), and the mixture was stirred at room temperature for 15 h 30 min, at 50°C for 7 h, and also at 80°C for 1 h. Potassium carbonate (102 mg) and tert-butyl 2-bromo-2-methylpropanoate (0.128 ml) were added to the reaction mixture, and the mixture was stirred at 80°C for 15 h 30 min. The reaction mixture was cooled to room temperature, water was added, and the mixture was extracted with ethyl acetate. The organic layer was washed with saturated brine diluted twice, filtered through a phase separator (manufactured by Biotage AB), and the filtrate was concentrated under reduced pressure. The residue obtained was purified by silica-gel column chromatography (solvent: n-hexane / ethyl acetate = 91 / 9 - 70 / 30) to give 8-fluoro-6-[2-methyl-1-[(2-methylpropan-2-yl)oxy]-1-oxopropan-2-yl]oxy-3,4-dihydro-1-Hisoquinoline-2-carboxylate (97.2 mg; yield of 69.8%) as a colorless oil. EM(ESI) m / z: 444.4[M+H]+

[00386] (2) 8-fluoro-6-[2-methyl-1-[(2-methylpropan-2-yl)oxy]-1-oxopropan-2-yl]oxy-3,4-dihydro-1H-isoquinoline-2-carboxylate benzyl (97 mg) obtained in (1) above was dissolved in ethanol (1 ml), palladium carbonate (10%, 50 mg) was added, and the mixture was stirred under a hydrogen atmosphere at room temperature for 2 h 30 min. After nitrogen replacement, the reaction mixture was filtered through a membrane filter, and the filtrate was concentrated under reduced pressure and dried under vacuum to give the title compound (65.2 mg; yield of 96.2%) as a colorless oil. EM(ESI) m / z: 310.3[M+H]+ Example of Reference 36:

[00387] The corresponding starting compounds were treated in the same manner as in Reference Example 35 to obtain a crude product of the compound described in the following Table 2. Table 2 Petition 870250102069, dated 07 / 11 / 2025, pp. 639 / 861 198 / 389 Example of Reference 37: Production of tert-butyl 3-[(8-fluoro-1,2,3,4-tetrahydroisoquinolin-6-yl)oxy]-2,2-dimethylpropanoate

[00388] (1) Benzyl 8-fluoro-6-hydroxy-3,4-dihydro-1H-isoquinoline-2-carboxylate (108 mg) was dissolved in THF (1 ml), triphenyl phosphine (117 mg), tert-butyl 3-hydroxy-2,2-dimethylpropanoate (115 mg) and diethyl azodicarboxylate (2.2 mol / l toluene solution, 0.31 ml) were added to this, and the reaction mixture was stirred at 70°C for 21 h. Hereafter, the mixture was stirred for 4 days, while at the same time allowed to cool to room temperature. The reaction mixture was concentrated under reduced pressure, and the residue was diluted with diisopropyl ether. The precipitate was treated, and the filtrate was concentrated under reduced pressure. The residue obtained was purified by silica gel column chromatography (solvent: n-hexane / ethyl acetate = 95 / 5 - 75 / 25) to give benzyl 6-[2,2-dimethyl-3-[(2-methylpropan-2-yl)oxy]-3-oxopropoxy]-8-fluoro-3,4-dihydro-1H-isoquinoline-2-carboxylate (85.8 mg; yield of 44.4%) as a colorless oil. EM(ESI) m / z: 402.3[M-C4H8+H]+

[00389] (2) Benzyl 6-[2,2-dimethyl-3-[(2-methylpropan-2-yl)oxy]-3-oxopropoxy]-8fluoro-3,4-dihydro-1H-isoquinoline-2-carboxylate (85.8 mg) Petition 870250102069, dated 07 / 11 / 2025, pp. 640 / 861 199 / 389 obtained in (1) mentioned above was dissolved in ethanol (2 ml), palladium carbonate (10%, 23 mg) was added, and the mixture was stirred under a hydrogen atmosphere at room temperature for 30 min. After nitrogen replacement, the reaction mixture was filtered through a membrane filter, and the filtrate was concentrated under reduced pressure and dried under vacuum to give the title compound (57.1 mg; 104% yield) as a colorless oil. EM(ESI) m / z: 324.3[M+H]+ Example of Reference 38: Production of tert-butyl 3-(4,5,6,7-tetrahydropyrazolo[1,5-alpyrazin-2-yl)propanoate Me Me-)—O Me NH

[00390] (1) To a solution of ethyl 3-(4,5,6,7-tetrahydropyrazolo[1,5a]pyrazin-2-yl)propanoate (1.0 g) and dichloromethane (13 ml) were added triethylamine (1.8 ml) and benzyl chloroformate (0.6 ml), and the mixture was stirred at room temperature for 3 h. Saturated aqueous ammonium chloride solution was added to the reaction mixture, and the mixture was extracted with chloroform. The organic layer was dried over anhydrous magnesium sulfate, and concentrated under reduced pressure to give benzyl 2-(3-ethoxy-3-oxopropyl)-6,7-dihydro-4Hpyrazolo[1,5a]pyrazine-5-carboxylate (1.4 g; yield of 102%) as a white solid. EM(ESI) m / z: 358.2[M+H]+

[00391] (2) To a solution of 2-(3-ethoxy-3-oxopropyl)-6,7-dihydro-4H-pyrazolo[1,5-a]pyrazine-5-carboxylate benzyl (1.4 g) obtained in (1) above and ethanol (13 ml) was added 4N aqueous sodium hydroxide solution (1.6 ml), and the mixture was stirred at 50°C for 1 h. The reaction mixture was neutralized with hydrochloric acid. Petition 870250102069, dated 07 / 11 / 2025, pp. 641 / 861 200 / 389 at 1N and extracted with ethyl acetate. The organic layer was washed with saturated brine, dried over anhydrous magnesium sulfate, and concentrated under reduced pressure to give 3-(5-phenylmethoxycarbonyl-6,7-dihydro-4H-pyrazolo[1,5-a]pyrazin-2yl)propanoic acid (940 mg; 73% yield) as a colorless oil. EM(ESI) m / z: 328.1[MH]-

[00392] (3) To a mixed solution of 3-(5-phenylmethoxycarbonyl-6,7-dihydro-4H-pyrazolo[1,5-a]pyrazin-2-yl)propanoic acid (940 mg) obtained in (2) above and toluene (10 ml) was added N,N-dimethylformamide di-tert-butylacetal (2.2 ml), and the mixture was stirred under a nitrogen atmosphere at 120°C for 30 min. The reaction mixture was cooled to room temperature and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (solvent: n-hexane / ethyl acetate = 60 / 40 - 40 / 60) to give benzyl 2-[3-[(2-methylpropan-2-yl)oxy]-3oxopropyl]-6,7-dihydro-4H-pyrazolo[1,5-a]pyrazine-5-carboxylate (611 mg; yield of 56%) as a colorless oil. EM(ESI) m / z: 386.1[M+H]+

[00393] (4) To a solution of 2-[3-[(2-methylpropan-2-yl)oxy]-3oxopropyl]-6,7-dihydro-4H-pyrazolo[1,5-a]pyrazine-5-carboxylate benzyl (95 mg) obtained in (3) above and methanol (1 ml) were added 20% palladium hydroxide (15 mg), and the mixture was stirred under a hydrogen atmosphere at 60°C for 2 h. The reaction mixture was filtered through Celite, and the filtrate was concentrated under reduced pressure to give a crude product (62 mg) of the title compound as a grey oil. Example of Reference 39: Production of 2-(4,5,6,7-tetrahydro-[1,3]thiazolo[5,4-c]pyridin-2-yl)acetate methyl trifluoroacetate Petition 870250102069, dated 07 / 11 / 2025, pp. 642 / 861 201 / 389

[00394] (1) To a mixed solution of tert-butyl 4-oxopiperidine-1-carboxylate (15 g) and toluene (70 ml) were added pyrrolidine (6.6 L) and p-toluenesulfonic acid monohydrate (5 mg), and the mixture was heated under reflux for 8 h using a Dean-Stark apparatus. The reaction mixture was cooled to room temperature and concentrated under reduced pressure. Methanol (30 ml) and sulfur (2.41 g) were added to the residue, and a solution of cyanamide (3.17 g) in methanol (10 ml) was added dropwise under ice-bath cooling. After completion of dropwise addition, the mixture was stirred under ice-bath cooling for 5 h. The precipitated solid was collected by filtration, washed with ethyl acetate, and dried under reduced pressure to give tert-butyl 2-amino-6,7-dihydro-4H[1,3]thiazolo[5,4-c]pyridine-5-carboxylate (11.6 g; 60% yield) as a yellow solid. MS(APCI)m / z:256.1[M+H]+

[00395] (2) To a solution of copper(II) bromide (11.9 g) and DMF (40 ml) was added hexyl nitrite (6.83 g), and the mixture was stirred at 50°C for 5 min. To the reaction mixture was added tert-butyl 2-amino-6,7-dihydro-4H-[1,3]thiazolo[5,4-c]pyridine-5-carboxylate (11.3 g) obtained in (1) mentioned above, and the mixture was stirred at 50°C for 2 h. The reaction mixture was cooled to room temperature and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (solvent: n-hexane / ethyl acetate =83 / 17) to give tert-butyl 2-bromo-6,7-dihydro-4H-[1,3]thiazolo[5,4c]pyridine-5-carboxylate (4.1 g; yield of 24%) as a yellow solid. Petition 870250102069, dated 07 / 11 / 2025, pp. 643 / 861 202 / 389 MS(APCI)m / z:319.0 / 321.0[M+H]+

[00396] (3) A mixture of tert-butyl 2-bromo-6,7-dihydro-4H-[1,3]thiazolo[5,4c]pyridine-5-carboxylate (150 mg) obtained in (2) above, 1-(tert-butyldimethylsiloxy)-1-methoxyethene (266 mg), potassium carbonate (130 mg), bis(tri-tert-butylphosphine)palladium(0) (72 mg) and DMF (1 ml) was stirred in a microwave reactor at 120°C for 1 h. The reaction mixture was cooled to room temperature, saturated aqueous ammonium chloride solution was added, and the mixture was extracted with ethyl acetate. The organic layer was washed with saturated brine, dried over anhydrous magnesium sulfate, and concentrated under reduced pressure. The residue was purified by reversed-phase HPLC (10 mmol / l aqueous ammonium carbonate / acetonitrile solution = 60 / 40 - 30 / 70) to give tert-butyl 2-(2-methoxy-2-oxoethyl)-6,7-dihydro-4H-[1,3]thiazolo[5,4-c]pyridine-5-carboxylate (36 mg; 25% yield) as a yellow amorphous substance. EM(ESI) m / z: 313.2[M+H]+

[00397] (4) To a solution of tert-butyl 2-(2-methoxy-2-oxoethyl)-6,7-dihydro-4H[1,3]thiazolo[5,4-c]pyridine-5-carboxylate (34 mg) obtained in (3) above and dichloromethane (0.5 ml) was added trifluoroacetic acid (0.1 ml), and the mixture was stirred at room temperature for 1 h. The reaction mixture was concentrated under reduced pressure to give a crude product (36 mg) of the title compound as a colorless amorphous substance. Exam...

Claims

1. Compound, characterized in that it is represented by formula (I): wherein R is a substituted aryl-ethenyl Ce-w group; R1 is a carboxylic group, or a group biologically equivalent to a carboxylic group, provided that a sulfonamide group is excluded;L is a C1-6 alkylene group, a C1-6 arylene group, a C3-14 cycloalkylene group, a C2-6 alkenylene group, a C2-6 alkynylene group, or a 3- to 14-membered divalent non-aromatic heterocyclic group, each of which optionally has, in the interior or at the end, one or more divalent groups selected from the group consisting of -NR2- (where R2 is a hydrogen atom or a C1-6 alkyl group), -O-, -S-, -C(=O)-, a C1-6 alkylene group, a C1-6 arylene group, a C3-14 cycloalkylene group, a C2-6 alkenylene group, a C2-6 alkynylene group, and a 3- to 14-membered divalent non-aromatic heterocyclic group, each of which is optionally further substituted by 1 to 3 substituents selected from the group of Substituents a; and A is a divalent heterocyclic group containing nitrogen that is optionally further substituted, or a pharmaceutically acceptable salt thereof (Substituent group a): a halogen atom; a hydroxyl group; a cyano group;Petition 870250102069, dated 07 / 11 / 2025, p. 832 / 861 2 / 26 an oxo group; a C1-6 alkyl group optionally substituted by substituent(s) selected from the group consisting of a halogen atom, a hydroxyl group, a cyano group, a C1-6 alkoxy group, a C6-14 aryl group, a carboxyl group, a C16 alkoxy-carbonyl group, a carbamoyl group optionally substituted by 1 or 2 C1-6 alkyl groups, and a C6-14 aryloxy group; a C1-6 alkoxy group optionally substituted by halogen atom(s); a C1-6 alkylsulfonyl group optionally substituted by halogen atom(s); a C1-6 alkyl-carbonyl group; a C1-6 alkoxy-carbonyl group; a carbamoyl group optionally substituted by 1 or 2 C1-6 alkyl groups optionally substituted by substituent(s) selected from the group consisting of a halogen atom, a hydroxyl group, a C1-6 dialkylamino group and a C1-6 alkoxy group; a C1-6 dialkylamino group; a tri-substituted silyl group;a tri-substituted oxy silyl group; a C6-14 hydrocarbocyclic group optionally substituted by 1 to 3 substituents selected from substituent group b; a 5- to 14-membered aromatic heterocyclic group optionally substituted by 1 to 3 substituents selected from substituent group b; and a 3- to 14-membered non-aromatic heterocyclic group optionally substituted by 1 to 3 substituents selected from substituent group b (Substituent group b): a halogen atom; Petition 870250102069, dated 07 / 11 / 2025, page 833 / 861 3 / 26 a hydroxyl group; a cyano group; an oxo group; a carboxylic group; an optionally substituted C1-6 alkyl group with substituent(s) selected from the group consisting of a halogen atom, a hydroxyl group, a cyano group and a C16 alkoxy group; an optionally substituted C3-8 cycloalkyl group with substituent(s) selected from the group consisting of a halogen atom, a hydroxyl group, a cyano group and a C16 alkoxy group;an aryl C6-10 group optionally substituted with substituent(s) selected from the group consisting of a halogen atom, a hydroxyl group, a cyano group, a C1-6 alkyl group and a C1-6 alkoxy group; an aromatic heterocyclic group of 5 to 14 members optionally substituted with substituent(s) selected from the group consisting of a halogen atom, a hydroxyl group, a cyano group, a C1-6 alkyl group and a C1-6 alkoxy group; a non-aromatic heterocyclic group of 3 to 14 members optionally substituted with substituent(s) selected from the group consisting of a halogen atom, a hydroxyl group, a cyano group, a C1-6 alkyl group and a C1-6 alkoxy group; an optionally substituted C1-6 alkoxy group with substituent(s) selected from the group consisting of a halogen atom, a hydroxyl group, a cyano group and a C16 alkoxy group;an alkylsulfanyl group C1-6 optionally substituted with substituent(s) selected from the group consisting of a halogen atom, a hydroxyl group, a cyano group and a C1-6 alkoxy group; a cycloalkyloxy group C3-8 optionally substituted with substituent(s) selected from the group consisting of a halogen atom, a hydroxyl group, a cyano group and a C1-6 alkoxy group; an alkylsulfonyl group C1-6 optionally substituted with halogen atom(s); an alkylcarbonyl group C1-6 optionally substituted with halogen atom(s); a C1-6 alkoxycarbonyl group; a carbamoyl group optionally substituted by 1 or 2 C1-6 alkyl groups optionally substituted by substituent(s) selected from the group consisting of a halogen atom, a hydroxyl group, a C1-6 dialkylamino group and a C1-6 alkoxy group;a sulfamoyl group substituted by a substituent selected from the group consisting of a C1-6 alkyl group, a C3-8 cycloalkyl group and a non-aromatic heterocyclic group, each of which is optionally substituted by 1 to 3 substituents selected from the group consisting of a halogen atom, a hydroxyl group, a cyano group and a C1-6 alkoxy group; and a pentafluorosulfanyl group.

2. Compound according to claim 1, or a pharmaceutically acceptable salt thereof, characterized in that, in formula (I), R is a 2-phenylthenyl group substituted by 1 to 3 substituents selected from the group consisting of a halogen atom, an optionally substituted C1-6 alkyl group, an optionally substituted C3-8 cycloalkyl group, an optionally substituted C1-6 alkoxy group, an optionally substituted C3-8 cycloalkyloxy group. Petition 870250102069, dated 07 / 11 / 2025, p.835 / 861 5 / 26 substituted, an optionally substituted C1-6 alkylsulfanyl group, an optionally substituted C3-8 cycloalkylsulfanyl group and a pentafluorosulfanyl group; R1 is a carboxyl group, or a group biologically equivalent to a carboxyl group, provided that a sulfonamide group is excluded; and A is a non-aromatic heterocyclic group containing divalent nitrogen represented by the following formula: where “ is a bonding site with a carbonyl group, *** is a bonding site with the L group, and the A ring is a 3- to 10-membered monocycle, an 8- to 14-membered fused cycle, a 6- to 16-membered spiro cycle, or a 6- to 14-membered bridging cycle and optionally has, as a constituent atom of the ring, in addition to a nitrogen atom and a carbon atom, heteroatom(s) selected from the group consisting of a nitrogen atom, an oxygen atom, and a sulfur atom, which is optionally replaced by 1 to 3 substituents selected from the a group of substituents.

3. Compound according to claim 1 or a pharmaceutically acceptable salt thereof, characterized in that, in formula (I), R is a 2-(E)-phenylethenyl group substituted by 1 to 3 substituents selected from the group consisting of a halogen atom, a C1-6 alkyl group optionally substituted by halogen atoms, and a pentafluorosulfanyl group; R1 is a carboxy group or a group biologically equivalent to a carboxy group; provided that a sulfonamide group is excluded; L is a C1-6 alkylene group optionally having, within or at the end, one or more divalent groups selected from the group consisting of -NR2- (where R2 is a hydrogen atom or a C1-6 alkyl group), -O-, -S-, -C(=O)-, a C6-10 arylene group, a C3-10 cycloalkylene group, a C2-6 alkynylene group, and a divalent non-aromatic heterocyclic group of 3 to 8 members.and optionally also substituted by 1 to 3 substituents selected from substituent group a, a C6-10 arylene group optionally also substituted by 1 to 3 substituents selected from substituent group a, a C3-10 cycloalkylene group optionally also substituted by 1 to 3 substituents selected from substituent group a, a C2-4 alkynylene group optionally also substituted by 1 to 3 substituents selected from substituent group a, or a divalent non-aromatic heterocyclic group of 3 to 8 members optionally also substituted by 1 to 3 substituents selected from substituent group a; and A is a divalent non-aromatic heterocyclic group containing nitrogen represented by the following formula: Petition 870250102069, dated 07 / 11 / 2025, page 837 / 861 7 / 26 where a wavy line is a site represented by the chemical formula, a bond represented by is a single bond or a double bond,each Y is independently a nitrogen atom or CR3 (where R3 is a hydrogen atom or a C1-6 alkyl group), Z is an oxygen atom, a sulfur atom, NR4 or CR5R6 (where R4, R5 and R6 are each independently a hydrogen atom or a C1-6 alkyl group), n is an integer from 0 to 2, m is an integer from 0 to 2, n1 and n2 are each independently a Petition 870250102069, dated 07 / 11 / 2025, p. 838 / 861 8 / 26 integer from 0 to 2, m1 and m2 are each independently an integer from 0 to 2, ** is a binding site with a carbonyl group, and *** is a binding site with the L group, whose non-aromatic heterocyclic group is optionally also replaced by 1 to 3 substituents selected from the substituent group a.

4. Compound according to claim 3 or a pharmaceutically acceptable salt thereof, characterized in that, in formula (I), L is a C1-6 alkylene group optionally having, in the interior or at the end, one or more divalent groups selected from the group consisting of -N R2- (wherein R2 is a hydrogen atom or a C1-6 alkyl group), -O-, -S-, a C3-10 cycloalkylene group, and a divalent non-aromatic heterocyclic group of 3 to 8 members, and optionally also substituted by 1 to 3 substituents selected from the substituent group a, a C3-10 cycloalkylene group optionally also substituted by 1 to 3 substituents selected from the substituent group a, or a divalent non-aromatic heterocyclic group of 3 to 8 members optionally also substituted by 1 to 3 substituents selected from the substituent group a.

5. Compound according to claim 3 or a pharmaceutically acceptable salt thereof, characterized in that, in formula (I), L is a C1-6 alkylene group optionally also substituted by 1 to 3 substituents selected from substituent group a.

6. Compound according to claim 5 or a pharmaceutically acceptable salt thereof, characterized in that, in formula (I), A is a non-aromatic heterocyclic group containing divalent nitrogen represented by the following formula: (where each symbol is as defined above), and optionally also substituted by 1 to 3 substituents selected from substituent group a.

7. Compound according to claim 5 or a pharmaceutically acceptable salt thereof, characterized in that, in formula (I), A is a non-aromatic heterocyclic group containing divalent nitrogen represented by the following formula: (where each symbol is as defined above, and the non-aromatic heterocyclic group represented is optionally replaced by 1 to 3 Petition 870250102069, dated 07 / 11 / 2025, page.840 / 861 10 / 26 substituents selected from substituent group a, provided that when Z is CR5R6, the optionally substituted substituent is selected from the group consisting of, among the substituents in substituent group a, a Ce-14 hydrocarbocyclic group optionally substituted by 1 to 3 substituents selected from substituent group b; an aromatic heterocyclic group of 5 to 14 members optionally substituted by 1 to 3 substituents selected from substituent group b; and a non-aromatic heterocyclic group of 3 to 14 members optionally substituted by 1 to 3 substituents selected from substituent group b).

8. Compound according to claim 5 or a pharmaceutically acceptable salt thereof, characterized in that, in formula (I), A is a non-aromatic heterocyclic group containing divalent nitrogen represented by the following formula: (wherein each symbol is as defined above), and optionally also substituted by 1 to 3 substituents selected from substituent group a.

9. Compound according to claim 5 or a pharmaceutically acceptable salt thereof, characterized in that, in formula (I), A is a non-aromatic heterocyclic group containing divalent nitrogen represented by the following formula: Petition 870250102069, dated 07 / 11 / 2025, page 841 / 861 11 / 26 (wherein each symbol is as defined above), and optionally also substituted by 1 to 3 substituents selected from substituent group a.

10. Compound according to claim 5 or a pharmaceutically acceptable salt thereof, characterized in that, in formula (I), A is a non-aromatic heterocyclic group containing divalent nitrogen represented by the following formula: (wherein each symbol is as defined above), and optionally also substituted by 1 to 3 substituents selected from substituent group a.

11. Compound according to any one of claims 1 to 10, or a pharmaceutically acceptable salt thereof, characterized in that, in formula (I), R1 is a carboxy group, an optionally substituted C1-6 alkoxy-carbonyl group, or an optionally substituted carbamoyl group.

12. Compound, characterized by the fact that it is selected from the group consisting of 2-[2-[2-[[(E)-3-[4(trifluoromethyl)phenyl]prop-2-enoyl] amino] acetyl]-3,4-d ih hydro-1Hisoquinolin-6-yl]acetic acid; 3-[2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl] amino]acetyl]3,4-di-hidro-1H-isoquinolin-6-yl]propanoic acid; / V, / V-dimethyl-3-[5-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl] amino] acetyl]-6,7-di-hidro-4H-pyrazolo[1,5-a]pyrazin-3-yl]propanamida; 1-[7-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl] amino]acetyl]6,8-di-hydro-5H-2,7-naftiridin-3-yl]piperidine-4-carboxylic acid; Petition 870250102069, 07 / 11 / 2025, pág. 842 / 861 12 / 26 Ácido 3-[3-bromo-5-[2-[[(E)-3-[4-(trifluorometil)fenil]prop-2-enoyl] amino] acetil]-6,7-di-hidro-4H-pyrazolo[1,5-a]pyrazin-2-yl]propanoic; 2-[[2-[2-[[(E)-3-[4-(trifluorometil)fenil]prop-2-enoyl] amino] acetil]-3,4di-hidro-1H-isoquinolin-6-yl]óxi]acético;Acid 2-[2-[2-[[(E)-3-[4-(pentafluoro-À6-sulfanyl)phenyl]prop-2-enoyl] amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid (1R*,2R*)-2-[2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl] amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]cyclopropane-1carboxylic dosmores mesomers;both Acid 2-[2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl] amino] acetyl]3,4-di-hydro-1H-isoquinolin-6-yl]propanoic acid; Acid 2-[7-fluoro-2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl] amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid 2-[8-fluoro-2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl] amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid 2-[7-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl] amino] acetyl]6,8-di-hydro-5H-2,7-naphthyridine-3-yl]acetic acid; Acid 3-[3-bromo-5-[2-[[(E)-3-[4-(pentafluoro-À6-sulfanyl)phenyl]prop-2enoyl] amino] acetyl]-6,7-di-hydro-4H-pyrazolo[1,5-a]pyrazin-2yl]propanoic;Acid 2-[2-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2-enoyl] amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid 2-[[2-[2-[[(E)-3-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl] amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]amino]acetic acid; Acid 2-[2-[2-[[(E)-3-(4-iodophenyl)prop-2-enoyl] amino] acetyl]-3,4-dihydro-1H-isoquinolin-6-yl]acetic acid; Acid 2-[5-fluoro-2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl] amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid 2-[8-chloro-2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl] amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Petition 870250102069, dated 07 / 11 / 2025, p. 843 / 861 13 / 26 Acid 2-[8-fluoro-2-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2enoyl] amino] acetyl]-3,4-di-hydro-1H-isoquinolinetic-;6-yl]yl] Acid 2-[8-cyano-2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl] amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid;Acid 2-[8-fluoro-2-[2-[[(E)-3-(2-fluoro-4-iodophenyl)prop-2-enoyl] amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid 2-[8-fluoro-2-[2-[[(E)-3-(4-iodophenyl)prop-2-enoyl] amino] acetyl]3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid 2-[8-chloro-2-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2enoyl] amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid 2-[[5-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl] amino] acetyl]-6,7-di-hydro-4H-[1,3]thiazolo[5,4-c]pyridin-2-yl]sulfanyl]acetic acid; Acid 2-[7-chloro-2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl] amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid 2-[8-cyano-2-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2enoyl] amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid 2-[5-chloro-2-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2enoyl] amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid;(E)-N-[2-[6-(2-amino-2-oxoethyl)-3,4-di-hydro-1H-isoquinolin-2-yl]-2oxoethyl]-3-[4-(trifluoromethyl)phenyl]prop-2-enamide; Acid 2-[5-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl] amino] acetyl]6,7-di-hydro-4H-[1,3]thiazolo[4,5-c]pyridin-2-yl]acetic acid; (E)-N-[2-[6-[2-(methylamino)-2-oxoethyl]-3,4-di-hydro-1H-isoquinolin-2-yl]2-oxoethyl]-3-[4-(trifluoromethyl)phenyl]prop-2-enamide; Acid 4-[4-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2-enoyl] amino] acetyl]-3-phenylpiperazine-1-yl]butanoic and both enantiomers of the same; Acid 2-[[1-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl] amino] acetyl]-2,3-di-hydroindol-4-yl]oxy]acetic acid; Acid 1 -[1-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2Petition 870250102069, dated 07 / 11 / 2025, p. 844 / 861 14 / 26 enoyl]amino]acetyl]piperidin-3-yl]bicycle[2.1.1 ]hexane-5-carboxylic; Acid 2-[[8-fluoro-2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl] amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]oxy]-2-methylpropanoic;3-[[8-fluoro-2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]-3,4-dihydro-1H-isoquinolin-6-yl]óxy]-2,2dimethylpropanoic acid; 4-[4-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]-2-methylpiperazin-1-yl]butanoic acid; 4-[(3S)-3-(4-bromophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid; 4-[3-(3-bromophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid; 4-[3-(4-chlorophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid; 3-[[3-(4-chlorophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperazin-1yl]methyl]cyclobutane-1-carboxylic acid and both enantiômeros dos mesmos; 4-[3-(4-chlorophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperazin-1-yl]-2,2dimethylbutanoic acid;Ácido 4-[3-(3-cyclopropylphenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid; Ácido 4-[3-(4-clorophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid e ambos enantiômeros dos mesmos; 4-[(2R,5S)-4-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2enoyl] amino]acetyl]-2-methyl-5-phenylpiperazin-1-yl]butanoic acid; 4-[(3S)-3-(4-cyclopropylphenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid; Acid 4-[3-(4-chloro-3-fluorophenyl)-4-[2-[[(E)-3-[2-fluoro-4Petition 870250102069, dated 07 / 11 / 2025, pág. 845 / 861 15 / 26 (trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid; 4-[(2R,5S)-5-(3,4-difluorophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]-2-methylpiperazin-1 yl]butanoic acid;4-[(2R,5S)-5-(3,4-difluorophenyl)-2-methyl-4-[2-[[(E)-3-[4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid; 4-[(2R,5S)-5-(4-chlorophenyl)-4-[2-[[(E)-3-[4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]-2-methylpiperazin-1yl]butanoic acid; 3-[(2R,5S)-5-(4-chlorophenyl)-4-[2-[[(E)-3-[4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]-2-methylpiperazin-1yl]propanoic acid; 4-[(2R,5S)-5-(4-chlorophenyl)—4—[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]-2-methylpiperazin-1-yl]butanoic acid; 4-[(2R,5S)-5-(4-fluorophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]-2-methylpiperazin-1-yl]butanoic acid; 3-[(2R,5S)-5-(4-chlorophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]-2-methylpiperazin-1-yl]propanoic acid; 4-[(2R,5S)-5-(3-fluorophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]-2-methylpiperazin-1yl]butanoic acid;4-[(2R,5S)-2-ethyl-4-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]-5-phenylpiperazin-1-yl]butanoic acid; and 4-[(2R,5S)-4-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]-2-methyl-5-phenylpiperazin-1-yl]-2,2-dimethylbutanoic acid or a pharmaceutically acceptable salt thereof. Petition 870250102069, dated 07 / 11 / 2025, pp. 846 / 861 16 / 26; 13. Compound, characterized hair fact that is selected from the group consisting of: Acid 2-[2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl] amino] acetyl]3,4-di-hydro-1H-yl]isoquinolinete-6-acid; Acid 3-[2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl] amino] acetyl]3,4-di-hydro-1H-isoquinolin-6-yl]propanoic acid; N,N-dimethyl-3-[5-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl] amino] acetyl]-6,7-di-hydro-4H-pyrazolo[1,5-a]pyrazine-3-yl]propanamide; Acid 2-[2-[2-[[(E)-3-[4-(pentafluoro-À6-sulfanyl)phenyl]prop-2-enoyl] amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid (1R*,2R*)-2-[2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl] amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]cyclopropane-1carboxylic dosmores mesomers;both Acid 2-[2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl] amino] acetyl]3,4-di-hydro-1H-isoquinolin-6-yl]propanoic acid;Acid 2-[7-fluoro-2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl] amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid 2-[8-fluoro-2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl] amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid 2-[2-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2-enoyl] amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid 2-[2-[2-[[(E)-3-(4-iodophenyl)prop-2-enoyl] amino] acetyl]-3,4-dihydro-1H-isoquinolin-6-yl]acetic acid; Acid 2-[5-fluoro-2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl] amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid 2-[8-chloro-2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl] amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid 2-[8-fluoro-2-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2enyl] amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid;Acid 2-[8-cyano-2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl] Petition 870250102069, dated 07 / 11 / 2025, p. 847 / 861 17 / 26 amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic; Acid 2-[8-fluoro-2-[2-[[(E)-3-(2-fluoro-4-iodophenyl)prop-2-enoyl] amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid 2-[8-chloro-2-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2enoyl] amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid 2-[7-chloro-2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl] amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid 2-[5-chloro-2-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2enoyl] amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid 2-[5-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl] amino] acetyl]6,7-di-hydro-4H-[1,3]thiazolo[4,5-c]pyridin-2-yl]acetic acid; Acid 4-[(3S)-4-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2-enoyl] amino] acetyl]-3-phenylpiperazine-1-yl]butanoic;1-[1-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2enoyl]amino]acetyl]piperidin-3-yl]bicyclo[2.1.1 ]hexane-5-carboxylic acid; 4-[(3S)-3-(4-bromophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid; 4-[3-(3-bromophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid; 4-[3-(4-chlorophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid; 3-[[3-(4-chlorophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperazin-1yl]methyl]cyclobutane-1- carboxílico and both enantiômeros dos mesmos; 4-[3-(4-chlorophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid and both enantiômeros dos mesmos; 4-[(2R,5S)-4-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2enoyl] amino]acetyl]-2-methyl-5-phenylpiperazin-1-yl]butanoic acid;Petition 870250102069, 07 / 11 / 2025, pág. 848 / 861 18 / 26 4-[(3S)-3-(4-cyclopropylphenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid; 4-[3-(4-chloro-3-fluorophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid; 4-[(2R,5S)-5-(3,4-difluorophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]-2-methylpiperazin-1yl]butanoic acid; 4-[(2R,5S)-5-(3,4-difluorophenyl)-2-methyl-4-[2-[[(E)-3-[4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid; 4-[(2R,5S)-5-(4-chlorophenyl)-4-[2-[[(E)-3-[4(trifluoromethyl)phenyl]prop-2-enoyl] amino] acetyl]-2-methylpiperazin-1yl]butanoic acid; 3-[(2R,5S)-5-(4-chlorophenyl)-4-[2-[[(E)-3-[4(trifluoromethyl)phenyl]prop-2-enoyl] amino] acetyl]-2-methylpiperazin-1-yl] propanoic acid;4-[(2R,5S)-5-(4-chlorophenyl)—4—[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]-2-methylpiperazin-1-yl]butanoic acid; 4-[(2R,5S)-5-(4-fluorophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]-2-methylpiperazin-1-yl]butanoic acid; 3-[(2R,5S)-5-(4-chlorophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]-2-methylpiperazin-1-yl]propanoic acid; 4-[(2R,5S)-5-(3-fluorophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]-2-methylpiperazin-1-yl]butanoic acid; 4-[(2R,5S)-2-ethyl-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]-5-phenylpiperazin-1-yl]butanoic acid; and Petition 870250102069, dated 07 / 11 / 2025, page. 849 / 861 19 / 26 4-[(2R,5S)-4-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]-2-methyl-5-phenylpiperazin-1-yl]-2,2-dimethylbutanoic acid, or a pharmaceutically acceptable salt thereof.

14. The compound, characterized hair made is selected from the group consisting of Acid 2-[7-fluoro-2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl] amino] acetyl]-3,4-di-isohydroquinoacylene-1H-1H- Acid 2-[8-fluoro-2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl] amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid 2-[2-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2-enoyl] amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid 2-[2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl] amino] acetyl]3,4-di-hydro-1H-isoquinolin-6-yl]propanoic acid; Acid 2-[2-[2-[[(E)-3-(4-iodophenyl)prop-2-enoyl] amino] acetyl]-3,4-dihydro-1H-isoquinolin-6-yl]acetic acid; Acid 2-[5-fluoro-2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl] amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid 2-[8-chloro-2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl] amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid;2-[8-fluoro-2-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2enoyl] amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; 2-[8-chloro-2-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2enoyl] amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; 2-[7-chloro-2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl] amino] acetyl]-3,4-di-hidro-1H-isoquinolin-6-yl]acetic acid; 2-[5-chloro-2-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2enoyl] amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; 4-[(3S)-4-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2-enoyl] amino]acetyl]-3-phenylpiperazin-1-yl]butanoic acid; Petition 870250102069, 07 / 11 / 2025, pág. 850 / 861 20 / 26 1-[1-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2enoyl]amino]acetyl]piperidin-3-yl]bicyclo[2.1.1 ]hexane-5-carboxylic acid; 4-[(3S)-3-(4-bromophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid;4-[3-(3-bromophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid; 4-[3-(4-chlorophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid; 4-[(2R,5S)-4-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2enoyl]amino]acetyl]-2-methyl-5-phenylpiperazin-1-yl]butanoic acid; 4-[(3S)-3-(4-cyclopropylphenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid; 4-[(2R,5S)-5-(3,4-difluorophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]-2-methylpiperazin-1yl]butanoic acid; 4-[(2R,5S)-5-(3,4-difluorophenyl)-2-methyl-4-[2-[[(E)-3-[4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid; 4-[(2R,5S)-5-(4-chlorophenyl)-4-[2-[[(E)-3-[4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]-2-methylpiperazin-1yl]butanoic acid;3-[(2R,5S)-5-(4-chlorophenyl)-4-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]-2-methylpiperazin-1-yl]propanoic acid; 4-[(2R,5S)-5-(4-chlorophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]-2-methylpiperazin-1-yl]butanoic acid; 4-[(2R,5S)-5-(4-fluorophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]-2-methylpiperazin-1-yl]butanoic acid; 3-[(2R,5S)-5-(4-chlorophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]-2-methylpiperazin-1-yl]propanoic acid; 4-[(2R,5S)-5-(3-fluorophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]-2-methylpiperazin-1-yl]butanoic acid; 4-[(2R,5S)-2-ethyl-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]-5-phenylpiperazin-1yl]butanoic acid;and 4-[(2R,5S)-4-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]-2-methyl-5-phenylpiperazin-1-yl]-2,2-dimethylbutanoic acid, or a pharmaceutically acceptable salt thereof.

15. Compound, characterized hair made is selected from the group consisting of: Acid 2-[2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl] amino] acetyl]3,4-di-hydro-1H-ylisoquinoline]acetic-6; Acid 3-[2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl] amino] acetyl]3,4-di-hydro-1H-isoquinolin-6-yl]propanoic acid; N,N-dimethyl-3-[5-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl] amino] acetyl]-6,7-di-hydro-4H-pyrazolo[1,5-a]pyrazine-3-yl]propanamide; Acid 2-[2-[2-[[(E)-3-[4-(pentafluoro-A6-sulfanyl)phenyl]prop-2-enoyl] amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid 2-[2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl] amino] acetyl]3,4-di-hydro-1H-isoquinolin-6-yl]propanoic acid; Acid 2-[8-fluoro-2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl] amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid; Acid 2-[2-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2-enoyl] amino] acetyl]-3,4-di-hydro-1H-isoquinolin-6-yl]acetic acid;2-[8-chloro-2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl] amino]acetyl]-3,4-di-hidro-1H-isoquinolin-6-yl]acetic acid; Acid 2-[8-chloro-2-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2 Request 870250102069, dated 07 / 11 / 2025, pág. 852 / 861 22 / 26 enoyl] amino] acetyl]-3,4-di-hidro-1H-isoquinolin-6-yl]acético; 4-[(3R)-3-(4-chlorophenyl)-4-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid; 4-[(2R,5S)-4-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2enoyl]amino]acetyl]-2-methyl-5-phenylpiperazin-1-yl]butanoic acid; 3-[(2R,5S)-5-(4-chlorophenyl)-4-[2-[[(E)-3-[4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]-2-methylpiperazin-1-yl]propanoic acid; 3-[(2R,5S)-5-(4-chlorophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl] amino] acetyl]-2-methylpiperazin-1yl]propanoic acid; 4-[(2R,5S)-5-(3-fluorophenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl] amino] acetyl]-2-methylpiperazin-1yl]butanoic acid;4-[(2R,5S)-2-ethyl-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]-5-phenylpiperazin-1-yl]butanoic acid; and 4-[(3S)-3-(4-cyclopropylphenyl)-4-[2-[[(E)-3-[2-fluoro-4(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid, or a pharmaceutically acceptable salt thereof.

16. Compound, characterized in that it is 2-[8-chloro-2-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]-3,4-dihydro-1H-isoquinolin-6-yl]acetic acid, or a pharmaceutically acceptable salt thereof.

17. Compound, characterized in that it is 2-[2-[[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]3,4-dihydro-1H-isoquinolin-6-yl]acetic acid, or a pharmaceutically acceptable salt thereof.

18. Compound, characterized in that it is 2-[8-fluoro-2-[2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]- Petition 870250102069, dated 07 / 11 / 2025, page 853 / 861 23 / 26 3,4-dihydro-1H-isoquinolin-6-yl]acetic acid, or a pharmaceutically acceptable salt thereof.

19. Compound, characterized in that it is 4-[(3S)-3-(4-cyclopropylphenyl)-4-[2-[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid, or a pharmaceutically acceptable salt thereof.

20. Compound, characterized in that it is 4-[(3S, 6R)-3-phenyl-6-methyl-4-[2-[[[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid, or a pharmaceutically acceptable salt thereof.

21. Compound, characterized in that it is 4-[(3S, 6R)-3-(3-fluorophenyl)-6-methyl-4-[2-[[[[(E)-3-[2-fluoro-4-(trifluoromethyl)phenyl]prop-2-enoyl]amino]acetyl]piperazin-1-yl]butanoic acid, or a pharmaceutically acceptable salt thereof.

22. B0AT1 inhibitor, characterized in that it comprises a compound, as defined in any one of claims 1 to 21, or a pharmaceutically acceptable salt thereof.

23. Pharmaceutical composition, characterized in that it comprises a compound, as defined in any one of claims 1 to 21, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.

24. Use of the compound, as defined in any one of claims 1 to 21 or a pharmaceutically acceptable salt thereof, characterized in that it is used in the manufacture of a pharmaceutical composition for the prophylaxis and / or treatment of a disease whose symptoms can be relieved by the inhibitory action of B0AT1.

25. Use, according to claim 24, characterized in that the disease whose symptoms can be relieved by the inhibitory action of B0AT1 is a disorder of amino acid metabolism.

26. Use, according to claim 25, characterized in that the amino acid metabolism disorder is phenylketonuria, urea cycle disorder, hypertyrosinemia (types 1-3), hypermethioninemia, maple syrup urine disease, homocystinuria, nonketotic hyperglycinemia, propionic acidemia, methylmalonic acidemia or isovaleric acidemia.

27. Use, according to claim 25, characterized in that the amino acid metabolism disorder is phenylketonuria.

28. Invention, characterized by any form of its embodiment or any categories of claims applicable to claim, for example, a product or process or use encompassed by the matter initially described, disclosed or illustrated in the patent application, including: Compound represented by formula (I): The (I) or a pharmaceutically acceptable salt thereof; and / or Pharmaceutical composition comprising a compound as defined in any of the preceding claims or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier; and / or Single or separate pharmaceutical composition comprising a compound as defined in any of the preceding claims or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier and one or more drugs;and / or Use of the compound as defined in any of the preceding claims or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition as defined in any of the preceding claims, in the manufacture of a medicament, a pharmaceutical composition or a product for the prophylaxis and / or treatment of a disease, a disorder and / or a health condition; and / or Use of (i) the compound as defined in any of the preceding claims or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition as defined in any of the preceding claims, in combination with (ii) other medicament(s) or drug(s) in the manufacture of a kit or a product for the prophylaxis and / or treatment of a disease, a disorder and / or a health condition;and / or Use of (i) the compound as defined in any of the preceding claims or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition as defined in any of the preceding claims, in the manufacture of a kit or product in combination with (ii) other medicine(s) or drug(s) for the prophylaxis and / or treatment of a disease, disorder and / or health condition; and / or Kit comprising the compound as defined in any of the preceding claims or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition as defined in any of the preceding claims, in a first container; a package insert containing instructions for use;and, optionally, a second container containing other medicine(s) or drug(s), in which the package insert contains instructions for using the compound and / or pharmaceutical composition of the invention and the other medicine(s) or drug(s) separately, simultaneously, sequentially or concomitantly.