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 PDFInfo
- 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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- JP
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- Prior art keywords
- alkyl
- aryl
- substituted
- heteroaryl
- metal
- 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.)
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Classifications
-
- 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
- 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
- A61K31/41—Heterocyclic 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
- A61K31/425—Thiazoles
- A61K31/428—Thiazoles condensed with carbocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/16—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular 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
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
-
- 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
-
- 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
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
- C07D277/62—Benzothiazoles
- C07D277/68—Benzothiazoles 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
- C07D277/82—Nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic 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
- C07D417/02—Heterocyclic 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
- C07D417/12—Heterocyclic 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6536—Heterocyclic 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
- C07F9/6539—Five-membered rings
- C07F9/6541—Five-membered rings condensed with carbocyclic rings or carbocyclic ring systems
Landscapes
- 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)
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)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| 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)
| 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)
| 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 |
Family Cites Families (5)
| 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 |
-
2016
- 2016-11-17 SG SG11201803645PA patent/SG11201803645PA/en unknown
- 2016-11-17 KR KR1020187013838A patent/KR20180084049A/ko not_active Ceased
- 2016-11-17 WO PCT/US2016/062400 patent/WO2017087594A1/en not_active Ceased
- 2016-11-17 ES ES16867091T patent/ES2969792T3/es active Active
- 2016-11-17 JP JP2018526135A patent/JP7110094B2/ja active Active
- 2016-11-17 US US15/775,897 patent/US20180318268A1/en not_active Abandoned
- 2016-11-17 EP EP16867091.7A patent/EP3377111B1/en active Active
- 2016-11-17 SG SG10202112588PA patent/SG10202112588PA/en unknown
-
2018
- 2018-05-16 IL IL259394A patent/IL259394B/en unknown
-
2019
- 2019-08-19 US US16/544,166 patent/US11083711B2/en active Active
Patent Citations (11)
| 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 |
Non-Patent Citations (7)
| Title |
|---|
| Bioorg. Med. Chem. Lett.,2005年,15,709-713 |
| 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 |
| J. Heterocyclic Chem.,1985年,22,429-432 |
| J. Med. Chem.,1988年,31,318-322 |
| JEFFREY J. HALE,PHOSPHORYLATED MORPHOLINE ACETAL HUMAN NEUROKININ-1 RECEPTOR ANTAGONISTS AS WATER-SOLUBLE PRODRUGS,JOURNAL OF MEDICINAL CHEMISTRY,2000年02月25日,VOL:43,PAGE(S):1234 - 1241,http://dx.doi.org/10.1021/jm990617v |
| Pharm. Res.,1993年,10,1350-1355 |
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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