TWI859303B - 受體作動活性的化合物的鹽及結晶形 - Google Patents

受體作動活性的化合物的鹽及結晶形 Download PDF

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Publication number
TWI859303B
TWI859303B TW109128245A TW109128245A TWI859303B TW I859303 B TWI859303 B TW I859303B TW 109128245 A TW109128245 A TW 109128245A TW 109128245 A TW109128245 A TW 109128245A TW I859303 B TWI859303 B TW I859303B
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Taiwan
Prior art keywords
powder
crystal
ray diffraction
crystals
methyl
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TW109128245A
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English (en)
Chinese (zh)
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TW202114984A (zh
Inventor
大谷修平
藤戸貴之
子
木嶋秀臣
史蒂芬Ｄ 帕瑞特
梅蘭妮 珍奈爾 畢菲
柯特尼Ｓ 強森
崔維斯 李 胡士頓
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日商小野藥品工業股份有限公司
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/04—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C55/00—Saturated compounds having more than one carboxyl group bound to acyclic carbon atoms
    • C07C55/02—Dicarboxylic acids
    • C07C55/10—Succinic acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C65/00—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C65/01—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing hydroxy or O-metal groups
    • C07C65/03—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing hydroxy or O-metal groups monocyclic and having all hydroxy or O-metal groups bound to the ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/18—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D209/20—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals substituted additionally by nitrogen atoms, e.g. tryptophane
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
TW109128245A 2019-08-20 2020-08-19 受體作動活性的化合物的鹽及結晶形 TWI859303B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201962889091P 2019-08-20 2019-08-20
US62/889,091 2019-08-20

Publications (2)

Publication Number Publication Date
TW202114984A TW202114984A (zh) 2021-04-16
TWI859303B true TWI859303B (zh) 2024-10-21

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TW109128245A TWI859303B (zh) 2019-08-20 2020-08-19 受體作動活性的化合物的鹽及結晶形

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US (1) US12459890B2 (https=)
EP (1) EP4019496B1 (https=)
JP (1) JP7409383B2 (https=)
KR (1) KR102930707B1 (https=)
CN (1) CN114302873A (https=)
AU (1) AU2020334489C1 (https=)
BR (1) BR112022002632A2 (https=)
CA (1) CA3150303A1 (https=)
ES (1) ES2983098T3 (https=)
IL (1) IL290432A (https=)
MX (1) MX2022001820A (https=)
MY (1) MY207001A (https=)
PH (1) PH12022550319A1 (https=)
TW (1) TWI859303B (https=)
WO (1) WO2021033729A1 (https=)
ZA (1) ZA202201784B (https=)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HUE068382T2 (hu) * 2018-02-22 2024-12-28 Ono Pharmaceutical Co SIP5-receptor-agonista aktivitással rendelkezõ 1[[(3S)-3-metil-6-(4(4,4-trifluorbutoxi)-3,4-dihidronaftalen-2-il]metil]azetidin-3-karbonsav neurodegeneratív rendellenességek és rák kezelésére
US11919879B2 (en) 2021-06-16 2024-03-05 Celgene Corporation Carboxylic acid containing azetidinyl compounds for the treatment of neurodegenerative diseases
KR20250114133A (ko) * 2022-12-16 2025-07-28 셀진 코포레이션 S1p5의 조정제로서의 헤테로시클릭 화합물
WO2025119254A1 (en) 2023-12-06 2025-06-12 Ono Pharmaceutical Co., Ltd. Method for preparing dihydronaphthalene derivative

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1826197A1 (en) * 2004-12-13 2007-08-29 Ono Pharmaceutical Co., Ltd. Aminocarboxylic acid derivative and medicinal use thereof
TW202114983A (zh) * 2019-08-20 2021-04-16 日商小野藥品工業股份有限公司 Ｓ１ｐ媒介疾病的預防及／或治療劑
TWI789495B (zh) * 2018-02-22 2023-01-11 日商小野藥品工業股份有限公司 具有ｓ1ｐ5受體作動活性的化合物

Family Cites Families (12)

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Publication number Priority date Publication date Assignee Title
NZ234564A (en) * 1986-11-21 1991-04-26 Haessle Ab 1-substituted benzimidazoles and pharmaceutical compositions
GB8725118D0 (en) * 1987-10-27 1987-12-02 Ciba Geigy Ag Rifamycin derivatives
JP2005020882A (ja) 2003-06-25 2005-01-20 Matsushita Electric Works Ltd モータアクチュエータ装置
CN1874991A (zh) 2003-08-29 2006-12-06 小野药品工业株式会社 能够结合s1p受体的化合物及其药物用途
EP1661881B1 (en) 2003-08-29 2014-12-17 Ono Pharmaceutical Co., Ltd. Compound capable of binding s1p receptor and pharmaceutical use thereof
JP2006064757A (ja) 2004-08-24 2006-03-09 Systec Kyowa:Kk ディスプレイ固定用スタンド
AU2007212193A1 (en) 2006-02-09 2007-08-16 University Of Virginia Patent Foundation Bicyclic sphingosine 1-phosphate analogs
EP2086930A2 (en) * 2006-06-12 2009-08-12 Novartis AG Polymorphs of n-hydroxy-3-[4-[[[2-(2-methyl-1h-indol-3-yl)ethyl]amino]methyl]phenyl]-2e-2-propenamide
UA107360C2 (en) 2009-08-05 2014-12-25 Biogen Idec Inc Bicyclic aryl sphingosine 1-phosphate analogs
UA113507C2 (xx) 2011-02-07 2017-02-10 Модулятори s1p
ES2852724T3 (es) 2014-12-04 2021-09-14 Ono Pharmaceutical Co Derivados de dihidronaftaleno útiles en el tratamiento de enfermedades mediadas por S1P5
ES2975689T3 (es) 2016-01-29 2024-07-11 Ono Pharmaceutical Co Derivado de tetrahidronaftaleno

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1826197A1 (en) * 2004-12-13 2007-08-29 Ono Pharmaceutical Co., Ltd. Aminocarboxylic acid derivative and medicinal use thereof
TWI789495B (zh) * 2018-02-22 2023-01-11 日商小野藥品工業股份有限公司 具有ｓ1ｐ5受體作動活性的化合物
TWI821061B (zh) * 2018-02-22 2023-11-01 日商小野藥品工業股份有限公司 介入性疾病之預防及/或治療劑
TW202114983A (zh) * 2019-08-20 2021-04-16 日商小野藥品工業股份有限公司 Ｓ１ｐ媒介疾病的預防及／或治療劑

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Publication number Publication date
IL290432A (en) 2022-04-01
CA3150303A1 (en) 2021-02-25
KR102930707B1 (ko) 2026-02-24
US20220289675A1 (en) 2022-09-15
EP4019496B1 (en) 2024-06-05
JP7409383B2 (ja) 2024-01-09
MX2022001820A (es) 2022-03-17
PH12022550319A1 (en) 2022-12-19
ES2983098T3 (es) 2024-10-22
AU2020334489A1 (en) 2022-03-03
AU2020334489B2 (en) 2025-10-30
AU2020334489C1 (en) 2026-03-26
US12459890B2 (en) 2025-11-04
NZ785003A (en) 2024-09-27
BR112022002632A2 (pt) 2022-05-03
JPWO2021033729A1 (https=) 2021-02-25
KR20220050886A (ko) 2022-04-25
ZA202201784B (en) 2024-02-28
MY207001A (en) 2025-01-23
CN114302873A (zh) 2022-04-08
EP4019496A4 (en) 2023-01-11
EP4019496A1 (en) 2022-06-29
TW202114984A (zh) 2021-04-16
WO2021033729A1 (ja) 2021-02-25

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