JPWO2020086504A5 - - Google Patents

Download PDF

Info

Publication number
JPWO2020086504A5
JPWO2020086504A5 JP2021520916A JP2021520916A JPWO2020086504A5 JP WO2020086504 A5 JPWO2020086504 A5 JP WO2020086504A5 JP 2021520916 A JP2021520916 A JP 2021520916A JP 2021520916 A JP2021520916 A JP 2021520916A JP WO2020086504 A5 JPWO2020086504 A5 JP WO2020086504A5
Authority
JP
Japan
Prior art keywords
group
acceptable salt
pharmacologically acceptable
substituted
alkylsulfonyl
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Granted
Application number
JP2021520916A
Other languages
Japanese (ja)
Other versions
JP2022506017A (en
JP7449283B2 (en
Publication date
Application filed filed Critical
Priority claimed from PCT/US2019/057314 external-priority patent/WO2020086504A1/en
Publication of JP2022506017A publication Critical patent/JP2022506017A/en
Publication of JPWO2020086504A5 publication Critical patent/JPWO2020086504A5/ja
Application granted granted Critical
Publication of JP7449283B2 publication Critical patent/JP7449283B2/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Claims (18)

下記式（Ｉ）：
Figure 2020086504000001
[式中、Ｘ１は窒素原子又はＣＲ９を示し、
Ｒ１は、水素原子、Ｃ１－Ｃ６アルキル基又はＣ１－Ｃ６アルコキシ基を示し、
Ｒ２は、ハロゲン原子を示し、
Ｒ３は、水素原子又はハロゲン原子を示し、
Ｒ４は、水素原子又はハロゲン原子を示し、
Ｒ５は、Ｃ１－Ｃ３アルキルスルホニル基、Ｃ１－Ｃ６アルキル基（該アルキル基は、Ｃ１－Ｃ３アルキルスルホニル基、カルボキシ基及びテトラゾリル基から選択される基で１つ置換されている）、Ｃ１－Ｃ６ハロアルキル基（該ハロアルキル基は、Ｃ１－Ｃ３アルキルスルホニル基、カルボキシ基及びテトラゾリル基から選択される基で１つ置換されていてもよい）、Ｃ１－Ｃ６アルコキシ基（該アルコキシ基は、Ｃ１－Ｃ３アルキルスルホニル基、カルボキシ基及びテトラゾリル基から選択される基で１つ置換されている）又はＣ１－Ｃ６アルキルアミノ基（該アルキルアミノ基は、Ｃ１－Ｃ３アルキルスルホニル基、カルボキシ基及びテトラゾリル基から選択される基で１つ置換されている）を示し、
Ｒ９は、水素原子、ハロゲン原子、Ｃ１－Ｃ３アルキルスルホニル基、Ｃ１－Ｃ６アルキル基又はＣ１－Ｃ６アルコキシ基を示す]
で表される化合物又はその薬理上許容される塩。 Formula (I) below:
Figure 2020086504000001
[Wherein, X 1 represents a nitrogen atom or CR 9 ,
R 1 represents a hydrogen atom, a C1-C6 alkyl group or a C1-C6 alkoxy group,
R 2 represents a halogen atom,
R 3 represents a hydrogen atom or a halogen atom,
R 4 represents a hydrogen atom or a halogen atom,
R 5 is a C1-C3 alkylsulfonyl group, a C1-C6 alkyl group (the alkyl group is substituted with one group selected from a C1-C3 alkylsulfonyl group, a carboxy group and a tetrazolyl group), C1- C6 haloalkyl group (the haloalkyl group may be substituted with one group selected from a C1-C3 alkylsulfonyl group, a carboxy group and a tetrazolyl group), a C1-C6 alkoxy group (the alkoxy group is a C1- one substituted with a group selected from a C3 alkylsulfonyl group, a carboxy group and a tetrazolyl group) or a C1-C6 alkylamino group (the alkylamino group is selected from a C1-C3 alkylsulfonyl group, a carboxy group and a tetrazolyl group substituted with one selected group),
R 9 represents a hydrogen atom, a halogen atom, a C1-C3 alkylsulfonyl group, a C1-C6 alkyl group or a C1-C6 alkoxy group]
A compound represented by or a pharmacologically acceptable salt thereof. 下記式（ＩＩ）：
Figure 2020086504000002
[式中、Ｒ１は、水素原子又はＣ１－Ｃ３アルキル基を示し、
Ｒ２は、ハロゲン原子を示し、
Ｒ３は、ハロゲン原子を示し、
Ｒ５は、Ｃ１－Ｃ６アルキル基（該アルキル基は、Ｃ１－Ｃ３アルキルスルホニル基、カルボキシ基及びテトラゾリル基から選択される基で１つ置換されている）、Ｃ１－Ｃ６アルコキシ基（該アルコキシ基は、Ｃ１－Ｃ３アルキルスルホニル基、カルボキシ基及びテトラゾリル基から選択される基で１つ置換されている）又はＣ１－Ｃ６アルキルアミノ基（該アルキルアミノ基は、Ｃ１－Ｃ３アルキルスルホニル基、カルボキシ基及びテトラゾリル基から選択される基で１つ置換されている）を示し、
Ｒ９は、Ｃ１－Ｃ３アルキル基又はＣ１－Ｃ３アルコキシ基を示す]
で表される化合物又はその薬理上許容される塩。 Formula (II) below:
Figure 2020086504000002
[Wherein, R 1 represents a hydrogen atom or a C1-C3 alkyl group,
R 2 represents a halogen atom,
R 3 represents a halogen atom,
R 5 is a C1-C6 alkyl group (the alkyl group is substituted with one group selected from a C1-C3 alkylsulfonyl group, a carboxy group and a tetrazolyl group), a C1-C6 alkoxy group (the alkoxy group is substituted with one group selected from a C1-C3 alkylsulfonyl group, a carboxy group and a tetrazolyl group) or a C1-C6 alkylamino group (the alkylamino group is a C1-C3 alkylsulfonyl group, a carboxy group and one substituted with a group selected from a tetrazolyl group),
R 9 represents a C1-C3 alkyl group or a C1-C3 alkoxy group]
A compound represented by or a pharmacologically acceptable salt thereof. 下記式（ＩＩＩ）：
Figure 2020086504000003
[式中、Ｒ１は、水素原子、メチル基又はエチル基を示し、
Ｒ２は、フッ素原子又は塩素原子を示し、
Ｒ３は、ハロゲン原子を示し、
Ｒ５は、カルボキシ基によって１つ置換されたＣ１－Ｃ６アルキル基又はカルボキシ基によって１つ置換されたＣ１－Ｃ６アルコキシ基を示す］
で表される化合物又はその薬理上許容される塩。 Formula (III) below:
Figure 2020086504000003
[Wherein, R 1 represents a hydrogen atom, a methyl group or an ethyl group,
R 2 represents a fluorine atom or a chlorine atom,
R 3 represents a halogen atom,
R 5 represents a C1-C6 alkyl group substituted with one carboxy group or a C1-C6 alkoxy group substituted with one carboxy group]
A compound represented by or a pharmacologically acceptable salt thereof.
Figure 2020086504000004
で表される化合物又はその薬理上許容される塩。
Figure 2020086504000004
A compound represented by or a pharmacologically acceptable salt thereof.
Figure 2020086504000005
で表される化合物又はその薬理上許容される塩。
Figure 2020086504000005
A compound represented by or a pharmacologically acceptable salt thereof.
Figure 2020086504000006
で表される化合物又はその薬理上許容される塩。
Figure 2020086504000006
A compound represented by or a pharmacologically acceptable salt thereof.
Figure 2020086504000007
で表される化合物又はその薬理上許容される塩。
Figure 2020086504000007
A compound represented by or a pharmacologically acceptable salt thereof. 前記薬理上許容される塩がナトリウム塩又はカリウム塩である、請求項１～７のいずれか一項に記載の化合物。 A compound according to any one of claims 1 to 7, wherein said pharmacologically acceptable salt is sodium or potassium salt. 請求項１～７のいずれか一項に記載の化合物又はその薬理上許容される塩を有効成分として含有する医薬組成物。 A pharmaceutical composition containing the compound according to any one of claims 1 to 7 or a pharmaceutically acceptable salt thereof as an active ingredient. 異所性石灰化の治療又は予防のための請求項９に記載の医薬組成物。 A pharmaceutical composition according to claim 9 for the treatment or prevention of ectopic calcification. 弾性線維性仮性黄色腫(PXE)、乳児全身性動脈石灰化(GACI)、関節と動脈の石灰化(CALJA)、CKD/ESRDにおける血管石灰化、カルシフィラキシス、後縦靱帯骨化症(OPLL)、黄色靭帯骨化症(OYLL)、又は大動脈弁狭窄症の治療又は予防のための請求項９に記載の医薬組成物。 Pseudoxanthoelastic fibrosis (PXE), infantile systemic arterial calcification (GACI), joint and arterial calcification (CALJA), vascular calcification in CKD/ESRD, calciphylaxis, posterior longitudinal ligament ossification (OPLL) ), ossification of the ligamentum flavum (OYLL), or aortic valve stenosis. 弾性線維性仮性黄色腫(PXE)の治療又は予防のための請求項９に記載の医薬組成物。 10. A pharmaceutical composition according to claim 9 for the treatment or prevention of pseudoxanthoma elastoma (PXE). 請求項１～７のいずれか一項に記載の化合物又はその薬理上許容される塩を有効成分として含有するTNAP阻害剤。 A TNAP inhibitor comprising the compound according to any one of claims 1 to 7 or a pharmacologically acceptable salt thereof as an active ingredient. 医薬組成物を製造するための、請求項１～７のいずれか一項に記載の化合物又はその薬理上許容される塩の使用。 Use of a compound according to any one of claims 1-7 or a pharmaceutically acceptable salt thereof for the manufacture of a pharmaceutical composition. 対象においてＴＮＡＰを阻害するための、請求項１～７のいずれか一項に記載の化合物又はその薬理上許容される塩。 A compound according to any one of claims 1 to 7, or a pharmaceutically acceptable salt thereof, for inhibiting TNAP in a subject. 異所性石灰化の治療又は予防に用いられる、請求項１～７のいずれか一項に記載の化合物又はその薬理上許容される塩。 A compound or a pharmacologically acceptable salt thereof according to any one of claims 1 to 7, which is used for the treatment or prevention of ectopic calcification. 弾性線維性仮性黄色腫(PXE)、乳児全身性動脈石灰化(GACI)、関節と動脈の石灰化(CALJA)、CKD/ESRDにおける血管石灰化、カルシフィラキシス、後縦靱帯骨化症(OPLL)、黄色靭帯骨化症(OYLL)、及び大動脈弁狭窄症からなる群より選ばれる疾病又は病態の治療又は予防に用いられる、請求項１～７のいずれか一項に記載の化合物又はその薬理上許容される塩。 Pseudoxanthoelastic fibrosis (PXE), infantile systemic arterial calcification (GACI), joint and arterial calcification (CALJA), vascular calcification in CKD/ESRD, calciphylaxis, posterior longitudinal ligament ossification (OPLL) ), ossification of the ligamentum flavum ( OYLL ), and aortic valve stenosis. Salt tolerable above. 弾性線維性仮性黄色腫(PXE)の治療又は予防に用いられる、請求項１～７のいずれか一項に記載の化合物又はその薬理上許容される塩。
8. The compound or a pharmacologically acceptable salt thereof according to any one of claims 1 to 7, which is used for the treatment or prevention of pseudoxanthoma elastoma (PXE).
JP2021520916A 2018-10-23 2019-10-22 biaryl derivative Active JP7449283B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862749590P 2018-10-23 2018-10-23
US62/749,590 2018-10-23
PCT/US2019/057314 WO2020086504A1 (en) 2018-10-23 2019-10-22 Biaryl derivative

Publications (3)

Publication Number Publication Date
JP2022506017A JP2022506017A (en) 2022-01-17
JPWO2020086504A5 true JPWO2020086504A5 (en) 2022-10-04
JP7449283B2 JP7449283B2 (en) 2024-03-13

Family

ID=68542774

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2021520916A Active JP7449283B2 (en) 2018-10-23 2019-10-22 biaryl derivative

Country Status (8)

Country Link
US (1) US11932600B2 (en)
EP (1) EP3870287A1 (en)
JP (1) JP7449283B2 (en)
KR (1) KR20210080416A (en)
BR (1) BR112021007261A2 (en)
CA (1) CA3113805C (en)
TW (1) TWI828783B (en)
WO (1) WO2020086504A1 (en)

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2164329A4 (en) 2007-05-08 2010-11-17 Burnham Inst Medical Research Tissue non-specific alkaline phosphatase inhibitors and uses thereof for treating vascular calcification
CN103619818A (en) 2011-06-20 2014-03-05 纳幕尔杜邦公司 Heterocyclic compounds for treating helminth infections
EP2817292B1 (en) 2012-02-22 2019-12-18 Sanford-Burnham Medical Research Institute Sulfonamide compounds and uses as tnap inhibitors
JP6563947B2 (en) 2013-12-02 2019-08-21 ケモセントリックス，インコーポレイティド CCR6 compound
RU2715704C2 (en) 2015-07-08 2020-03-03 Дайити Санкио Компани, Лимитед Pyridoxazinone derivatives as tnap inhibitors
CN108484584A (en) * 2018-05-22 2018-09-04 窦玉玲 A kind of sulfonic acid amide derivatives and its purposes in anti-antianemic object

Similar Documents

Publication Publication Date Title
JP2011504935A5 (en)
JP2006143737A5 (en)
MA29926B1 (en) PYRAZINE DERIVATIVES
RU2009110442A (en) CONDENSED IMIDAZOLE DERIVATIVES FOR TREATMENT OF DISORDERS MEDIATED BY ALDOSTEROSYNTHASE AND / OR 11-BETA-HYDROXYLASE, AND / OR AROMATASE
MY142807A (en) Benzimidazole derivative and use thereof.
CA2565813A1 (en) Substituted methyl aryl or heteroaryl amide compounds
JP2011527345A5 (en)
EA200700103A1 (en) NEW 2-SUBSTITUTED D-HOMO-ESTRA-1,3,5 (10) -TRIENES AS INHIBITORS OF 17β-HYDROXYSTEROID DEHYDROGENASE TYPE 1
RS20050182A (en) Derivatives of dioxane-2-alkyl carbamates,preparation method thereof and application of same in therapeutics
RU2007132179A (en) HIV INHIBITING DERIVATIVES 2- (4-CYANOPHENYLAMINO) PYRIMIDINE
NO20065863L (en) 3- [4- (6- (4,5-Dihydroisoxazol-3-yl) pyridin-3-yl) -3-phenyl] -5- (1H, 1,2,3-triazol-1-yl-methyl) ) -1,3-oxazolidin-2-ones as antibacterial agents
WO2019241213A1 (en) 2-naphthimidamides, analogues thereof, and methods of treatment using same
JP2008069182A5 (en)
JP2004525183A5 (en)
CA2690349A1 (en) Derivatives of 7-alkynyl-1,8-naphthyridones, preparation method thereof and use of same in therapeutics
RU2008128566A (en) ORGANIC COMPOUNDS
JP2019182865A5 (en)
JPWO2020086504A5 (en)
CY1109678T1 (en) NEW 3-PHYNYLPROPYNIC ACID PRODUCTS AND USE THESE AS PPAR-GAMMA RECEPTOR CONNECTORS
UA89807C2 (en) New 3-phenylpropionic acid derivatives for the treatment of diabetes
TW200635911A (en) Sulfanyl substituted phenyl methanones
PE20001596A1 (en) MORPHOLIN DERIVATIVES
JP2019529501A5 (en)
JP2008519001A5 (en)
MX2022011392A (en) Phd inhibitor compounds, compositions, and use.