JP6607780B2 - Ｌｆａ−１阻害剤およびその多形 - Google Patents

Ｌｆａ−１阻害剤およびその多形 Download PDF

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JP6607780B2
JP6607780B2 JP2015524447A JP2015524447A JP6607780B2 JP 6607780 B2 JP6607780 B2 JP 6607780B2 JP 2015524447 A JP2015524447 A JP 2015524447A JP 2015524447 A JP2015524447 A JP 2015524447A JP 6607780 B2 JP6607780 B2 JP 6607780B2
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compound
formula
various embodiments
acid
acetone
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JP2015523398A (ja
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ジェームズ・ロバート・ツェラー
スリパティ・ヴェンカトラマン
エリザベス・シー・エー・ブロット
スバシュリー・アイヤー
マイケル・ホール
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サルコード・バイオサイエンス・インコーポレイテッド
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/10—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
    • C07D407/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B63/00—Purification; Separation; Stabilisation; Use of additives

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
JP2015524447A 2012-07-25 2013-07-25 Ｌｆａ−１阻害剤およびその多形 Active JP6607780B2 (ja)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US201261675663P 2012-07-25 2012-07-25
US61/675,663 2012-07-25
US201261680099P 2012-08-06 2012-08-06
US61/680,099 2012-08-06
US201261729294P 2012-11-21 2012-11-21
US61/729,294 2012-11-21
PCT/US2013/052044 WO2014018748A1 (en) 2012-07-25 2013-07-25 Lfa-1 inhibitor and polymorph thereof

Related Child Applications (1)

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JP2018135758A Division JP2018162313A (ja) 2012-07-25 2018-07-19 Ｌｆａ−１阻害剤およびその多形

Publications (2)

Publication Number Publication Date
JP2015523398A JP2015523398A (ja) 2015-08-13
JP6607780B2 true JP6607780B2 (ja) 2019-11-20

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JP2015524447A Active JP6607780B2 (ja) 2012-07-25 2013-07-25 Ｌｆａ−１阻害剤およびその多形
JP2018135758A Pending JP2018162313A (ja) 2012-07-25 2018-07-19 Ｌｆａ−１阻害剤およびその多形
JP2020096854A Active JP7008750B2 (ja) 2012-07-25 2020-06-03 Ｌｆａ－１阻害剤およびその多形

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JP2020096854A Active JP7008750B2 (ja) 2012-07-25 2020-06-03 Ｌｆａ－１阻害剤およびその多形

Country Status (14)

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US (4) US9085553B2 (enExample)
EP (3) EP3715345B8 (enExample)
JP (3) JP6607780B2 (enExample)
KR (2) KR20200108932A (enExample)
CN (2) CN110922393A (enExample)
AU (5) AU2013295706A1 (enExample)
BR (1) BR112015001608B1 (enExample)
CA (1) CA2879982C (enExample)
HK (1) HK1210782A1 (enExample)
IN (1) IN2015DN00847A (enExample)
MX (2) MX2015001098A (enExample)
RU (1) RU2658015C2 (enExample)
SI (1) SI3715345T1 (enExample)
WO (1) WO2014018748A1 (enExample)

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AU2006247136C1 (en) * 2005-05-17 2020-01-16 Bausch + Lomb Ireland Limited Compositions and methods for treatment of eye disorders
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JP6607780B2 (ja) 2012-07-25 2019-11-20 サルコード・バイオサイエンス・インコーポレイテッド Ｌｆａ−１阻害剤およびその多形
CN106714801B (zh) 2014-09-25 2021-04-06 诺华股份有限公司 连续流羧基化反应
CN113230021A (zh) 2015-01-12 2021-08-10 科达莱昂治疗公司 微滴递送设备和方法
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WO2018019300A1 (zh) * 2016-07-29 2018-02-01 武汉朗来科技发展有限公司 一种口服固体制剂及其应用
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CN108084067B (zh) * 2016-11-22 2019-08-30 重庆圣华曦药业股份有限公司 一种立他司特中间体的制备方法
JP7768665B2 (ja) 2017-01-20 2025-11-12 ボシュ ＋ ロム アイルランド リミテッド 圧電流体ディスペンサ
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CN115784950B (zh) * 2022-12-08 2024-06-28 广东先强药业有限公司 一种立他司特中间体的制备方法
CN116239532B (zh) * 2022-12-19 2023-11-07 浙江博崤生物制药有限公司 一种二氯四氢异喹啉羧酸的中间体及其制备方法和应用
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