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)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (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=)
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
PT3757091T (pt) * 2018-02-22 2024-09-11 Ono Pharmaceutical Co Ácido 1-[[(3s)-3-metil-6-(4,4,4-trifluorobutoxi)-3,4-di-hidronaftalen-2-il]metil]azetidino-3-carboxílico com atividade agonista do recetor s1p5 para o tratamento de doenças neurodegenerativas e cancro
AU2022291768A1 (en) 2021-06-16 2023-11-30 Celgene Corporation Azetidinyl compounds comprising a carboxylic acid group for the treatment of neurodegenerative diseases
EP4633736A1 (en) * 2022-12-16 2025-10-22 Celgene Corporation Heterocyclic compounds as modulators of s1p5
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

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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
US7825109B2 (en) 2003-08-29 2010-11-02 Ono Pharmaceutical Co., Ltd. Compound capable of binding S1P receptor and pharmaceutical use thereof
KR20110140139A (ko) 2003-08-29 2011-12-30 오노 야꾸힝 고교 가부시키가이샤 Ｓ１ｐ 수용체 결합능을 갖는 화합물 및 그 의약 용도
JP2006064757A (ja) 2004-08-24 2006-03-09 Systec Kyowa:Kk ディスプレイ固定用スタンド
JP2009526073A (ja) 2006-02-09 2009-07-16 ユニバーシティ オブ バージニア パテント ファンデーション 二環式スフィンゴシン−１−リン酸受容体アナログ
ME00529B (me) * 2006-06-12 2011-10-10 Novartis Ag Polimorfi n-hidroksi-3-[4-[[[2-(-metil-1h-indol-3-il)etil]amino]fenil]-2e-2-propenamida
UA107360C2 (en) 2009-08-05 2014-12-25 Biogen Idec Inc Bicyclic aryl sphingosine 1-phosphate analogs
EA034451B1 (ru) 2011-02-07 2020-02-10 Байоджен Ма Инк. Модуляторы s1p
EP3228615B1 (en) * 2014-12-04 2021-01-20 ONO Pharmaceutical Co., Ltd. Dihydronaphthalene derivatives useful in the treatment of s1p5-mediated diseases
EP3409658B9 (en) 2016-01-29 2024-07-17 ONO Pharmaceutical Co., Ltd. Tetrahydronaphthalene derivative

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

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