JP7110094B2 - 医薬化合物のアミンプロドラッグ - Google Patents

医薬化合物のアミンプロドラッグ Download PDF

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Publication number
JP7110094B2
JP7110094B2 JP2018526135A JP2018526135A JP7110094B2 JP 7110094 B2 JP7110094 B2 JP 7110094B2 JP 2018526135 A JP2018526135 A JP 2018526135A JP 2018526135 A JP2018526135 A JP 2018526135A JP 7110094 B2 JP7110094 B2 JP 7110094B2
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alkyl
aryl
substituted
heteroaryl
metal
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JP2019501877A (ja
JP2019501877A5 (enExample
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アンソニー・マーファット
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Biohaven Pharmaceutical Holding Co Ltd
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Biohaven Pharmaceutical Holding Co Ltd
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425Thiazoles
    • A61K31/428Thiazoles condensed with carbocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/16Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62Benzothiazoles
    • C07D277/68Benzothiazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
    • C07D277/82Nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6536Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having nitrogen and sulfur atoms with or without oxygen atoms, as the only ring hetero atoms
    • C07F9/6539Five-membered rings
    • C07F9/6541Five-membered rings condensed with carbocyclic rings or carbocyclic ring systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Indole Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
JP2018526135A 2015-11-19 2016-11-17 医薬化合物のアミンプロドラッグ Active JP7110094B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562257533P 2015-11-19 2015-11-19
US62/257,533 2015-11-19
PCT/US2016/062400 WO2017087594A1 (en) 2015-11-19 2016-11-17 Amine prodrugs of pharmaceutical compounds

Publications (3)

Publication Number Publication Date
JP2019501877A JP2019501877A (ja) 2019-01-24
JP2019501877A5 JP2019501877A5 (enExample) 2019-12-26
JP7110094B2 true JP7110094B2 (ja) 2022-08-01

Family

ID=58717793

Family Applications (1)

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JP2018526135A Active JP7110094B2 (ja) 2015-11-19 2016-11-17 医薬化合物のアミンプロドラッグ

Country Status (8)

Country Link
US (2) US20180318268A1 (enExample)
EP (1) EP3377111B1 (enExample)
JP (1) JP7110094B2 (enExample)
KR (1) KR20180084049A (enExample)
ES (1) ES2969792T3 (enExample)
IL (1) IL259394B (enExample)
SG (2) SG11201803645PA (enExample)
WO (1) WO2017087594A1 (enExample)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US12295942B2 (en) 2015-03-03 2025-05-13 Biohaven Therapeutics Ltd. Riluzole prodrugs and their use
BR112017018832B1 (pt) 2015-03-03 2023-12-26 Biohaven Pharmaceutical Holding Company Ltd Profármacos de riluzol e seu uso e composição
US12029731B2 (en) 2016-08-10 2024-07-09 Biohaven Therapeutics Ltd. Acyl benzo[d]thiazol-2-amine and their methods of use
US20250049748A1 (en) * 2021-12-16 2025-02-13 Terran Biosciences Inc. Analogs of 4-bromo-2,5-dimethoxyphenethylamine
WO2023141636A1 (en) * 2022-01-24 2023-07-27 Terran Biosciences Inc. Prodrugs of 2-bromo-lsd (2-bromolysergic acid diethylamide)

Citations (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2003534312A (ja) 2000-05-26 2003-11-18 ワーナー−ランバート・カンパニー、リミテッド、ライアビリティ、カンパニー 薬剤として有用な環状アミノ酸誘導体
WO2004052841A1 (en) 2002-12-06 2004-06-24 Xenoport, Inc. Carbidopa prodrugs and uses thereof
JP2006510618A (ja) 2002-11-18 2006-03-30 ヤウポン セラピューティクス,インコーポレーテッド ノルケタミンおよびケタミン/ノルケタミンプロドラッグの鎮痛的使用
JP2008518970A (ja) 2004-11-05 2008-06-05 メルク エンド カムパニー インコーポレーテッド {3−[2(r)−[(1r)−1−[3,5−ビス(トリフルオロメチル)フェニル]エトキシ]−3(s)−(4−フルオロフェニル)モルホリン−4−イル]メチル]−5−オキソ−4,5−ジヒドロ−[1,2,4]−トリアゾール−1−イル}ホスホン酸を調製する方法
JP2009504677A (ja) 2005-08-12 2009-02-05 メルク・エンド・カムパニー・インコーポレーテツド 新規2’−c−メチル及び4’−c−メチルヌクレオシド誘導体
JP2010539191A (ja) 2007-09-17 2010-12-16 エナンタ ファーマシューティカルズ インコーポレイテッド 6,11−架橋ビアリールマクロライド
JP2011522838A (ja) 2008-06-06 2011-08-04 アキリオン ファーマシューティカルズ,インコーポレーテッド 抗hcv活性を有する化合物の置換アミノチアゾールプロドラッグ
JP2014533718A (ja) 2011-12-15 2014-12-15 アルカーメス ファーマ アイルランド リミテッド 二級アミン化合物のプロドラッグ
US20150111932A1 (en) 2012-05-08 2015-04-23 Mahesh Kandula Compositions and methods for the treatment of neurological degenerative disorders
JP2015521598A (ja) 2012-06-11 2015-07-30 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company 5−[5−フェニル−4−(ピリジン−2−イルメチルアミノ)キナゾリン−2−イル]ピリジン−3−スルホンアミドのホスホロアミド酸プロドラッグ
JP2015524394A (ja) 2012-07-09 2015-08-24 オニキス セラピューティクス, インク.Onyx Therapeutics, Inc. ペプチドエポキシケトンプロテアーゼ阻害剤のプロドラッグ

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW354293B (en) * 1995-06-06 1999-03-11 Bristol Myers Squibb Co Prodrugs of paclitaxel derivatives
US20040176430A1 (en) * 2002-11-21 2004-09-09 Jeffrey Sterling Propargyl-trifluoromethoxy-amino-benzothiazole derivatives
US20130030359A1 (en) * 2010-01-22 2013-01-31 Ascendis Pharma A/S Dipeptide-based prodrug linkers for aromatic amine-containing drugs
US8937151B2 (en) * 2010-03-04 2015-01-20 University Of Notre Dame Du Lac Gelatinase inhibitors and prodrugs
WO2013138753A1 (en) 2012-03-16 2013-09-19 Fox Chase Chemical Diversity Center, Inc. Prodrugs of riluzole and their method of use

Patent Citations (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2003534312A (ja) 2000-05-26 2003-11-18 ワーナー−ランバート・カンパニー、リミテッド、ライアビリティ、カンパニー 薬剤として有用な環状アミノ酸誘導体
JP2006510618A (ja) 2002-11-18 2006-03-30 ヤウポン セラピューティクス,インコーポレーテッド ノルケタミンおよびケタミン/ノルケタミンプロドラッグの鎮痛的使用
WO2004052841A1 (en) 2002-12-06 2004-06-24 Xenoport, Inc. Carbidopa prodrugs and uses thereof
JP2008518970A (ja) 2004-11-05 2008-06-05 メルク エンド カムパニー インコーポレーテッド {3−[2(r)−[(1r)−1−[3,5−ビス(トリフルオロメチル)フェニル]エトキシ]−3(s)−(4−フルオロフェニル)モルホリン−4−イル]メチル]−5−オキソ−4,5−ジヒドロ−[1,2,4]−トリアゾール−1−イル}ホスホン酸を調製する方法
JP2009504677A (ja) 2005-08-12 2009-02-05 メルク・エンド・カムパニー・インコーポレーテツド 新規2’−c−メチル及び4’−c−メチルヌクレオシド誘導体
JP2010539191A (ja) 2007-09-17 2010-12-16 エナンタ ファーマシューティカルズ インコーポレイテッド 6,11−架橋ビアリールマクロライド
JP2011522838A (ja) 2008-06-06 2011-08-04 アキリオン ファーマシューティカルズ,インコーポレーテッド 抗hcv活性を有する化合物の置換アミノチアゾールプロドラッグ
JP2014533718A (ja) 2011-12-15 2014-12-15 アルカーメス ファーマ アイルランド リミテッド 二級アミン化合物のプロドラッグ
US20150111932A1 (en) 2012-05-08 2015-04-23 Mahesh Kandula Compositions and methods for the treatment of neurological degenerative disorders
JP2015521598A (ja) 2012-06-11 2015-07-30 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company 5−[5−フェニル−4−(ピリジン−2−イルメチルアミノ)キナゾリン−2−イル]ピリジン−3−スルホンアミドのホスホロアミド酸プロドラッグ
JP2015524394A (ja) 2012-07-09 2015-08-24 オニキス セラピューティクス, インク.Onyx Therapeutics, Inc. ペプチドエポキシケトンプロテアーゼ阻害剤のプロドラッグ

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Bioorg. Med. Chem. Lett.,2013年,23,3028-3033
HOLGER STARK,ENZYME-CATALYZED PRODRUG APPROACHES FOR THE HISTAMINE H3-RECEPTOR AGONIST (R)-α-METHYLHISTAMINE,BIOORGANIC & MEDICINAL CHEMISTRY,2000年12月15日,VOL:9,PAGE(S):191 - 198,https://www.sciencedirect.com/science/article/pii/S0968089600002376?via%3Dihub
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Also Published As

Publication number Publication date
EP3377111B1 (en) 2023-11-29
EP3377111A4 (en) 2019-11-13
IL259394B (en) 2022-04-01
US20180318268A1 (en) 2018-11-08
IL259394A (en) 2018-07-31
EP3377111A1 (en) 2018-09-26
US20190365721A1 (en) 2019-12-05
ES2969792T3 (es) 2024-05-22
SG10202112588PA (en) 2021-12-30
US11083711B2 (en) 2021-08-10
SG11201803645PA (en) 2018-06-28
KR20180084049A (ko) 2018-07-24
JP2019501877A (ja) 2019-01-24
WO2017087594A1 (en) 2017-05-26

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