CN108289905A - 用于癌症疗法的阿糖胞苷缀合物 - Google Patents
用于癌症疗法的阿糖胞苷缀合物 Download PDFInfo
- Publication number
- CN108289905A CN108289905A CN201680070972.5A CN201680070972A CN108289905A CN 108289905 A CN108289905 A CN 108289905A CN 201680070972 A CN201680070972 A CN 201680070972A CN 108289905 A CN108289905 A CN 108289905A
- Authority
- CN
- China
- Prior art keywords
- acid
- subject
- administered
- compound
- astarabine
- 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.)
- Pending
Links
Classifications
-
- 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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
- A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
- A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
-
- 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
- A61K47/50—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/54—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
- A61K47/542—Carboxylic acids, e.g. a fatty acid or an amino acid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Molecular Biology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Virology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Saccharide Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562262428P | 2015-12-03 | 2015-12-03 | |
| US62/262,428 | 2015-12-03 | ||
| PCT/IL2016/050077 WO2017093993A1 (en) | 2015-12-03 | 2016-01-25 | Cytarabine conjugates for cancer therapy |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN108289905A true CN108289905A (zh) | 2018-07-17 |
Family
ID=58796462
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201680070972.5A Pending CN108289905A (zh) | 2015-12-03 | 2016-01-25 | 用于癌症疗法的阿糖胞苷缀合物 |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US11058701B2 (https=) |
| EP (1) | EP3383407B1 (https=) |
| JP (3) | JP7149183B2 (https=) |
| CN (1) | CN108289905A (https=) |
| AU (2) | AU2016362830B2 (https=) |
| BR (1) | BR112018011177A2 (https=) |
| CA (1) | CA3007058C (https=) |
| IL (2) | IL259631B (https=) |
| RU (1) | RU2708672C1 (https=) |
| WO (1) | WO2017093993A1 (https=) |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110590862A (zh) * | 2019-11-01 | 2019-12-20 | 南京师范大学 | 阿糖胞苷4-n位氨基酸衍生物及其制备方法与应用 |
| CN112409431A (zh) * | 2020-12-07 | 2021-02-26 | 武汉伯瑞恒医药科技有限公司 | 阿糖胞苷结构类似物及其制备方法和用途 |
| CN115052607A (zh) * | 2020-02-04 | 2022-09-13 | 拜欧赛特有限公司 | 天冬阿糖胞苷药物组合物和其用途 |
| CN115461058A (zh) * | 2020-04-23 | 2022-12-09 | 拜欧赛特有限公司 | 用于治疗血液癌的方法和方案 |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US12071450B2 (en) | 2015-12-03 | 2024-08-27 | Biosight Ltd. | Salts of conjugates for cancer therapy |
| US12064445B2 (en) | 2015-12-03 | 2024-08-20 | Biosight Ltd. | Cytarabine conjugates for cancer therapy |
| US11104698B2 (en) | 2015-12-03 | 2021-08-31 | Biosight Ltd. | Salts of conjugates for cancer therapy |
| WO2019012328A1 (en) * | 2017-07-09 | 2019-01-17 | Biosight Pharma | ANTICANCER POLY THERAPY |
| KR20230074156A (ko) * | 2020-09-21 | 2023-05-26 | 바이오사이트 리미티드 | 아스파시타라빈의 결정질 형태 |
| JP2024540613A (ja) * | 2021-11-21 | 2024-10-31 | バイオサイト リミテッド | がんの治療のためのシタラビン-アミノ酸系プロドラッグ |
| WO2023175622A1 (en) * | 2022-03-17 | 2023-09-21 | Biosight Ltd. | Crystalline forms of aspacytarabine |
| WO2023228177A1 (en) * | 2022-05-22 | 2023-11-30 | Biosight Ltd. | Compositions comprising aspacytarabine and additional compounds, and use thereof |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20110275590A1 (en) * | 2004-02-02 | 2011-11-10 | BioSight Ltd., | Conjugates for cancer therapy and diagnosis |
| CN103781760A (zh) * | 2011-06-13 | 2014-05-07 | 株式会社Ihi | 金属salen络合物化合物、局部麻醉药剂及抗恶性肿瘤药剂 |
Family Cites Families (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2949451A (en) | 1959-04-21 | 1960-08-16 | Hoffmann La Roche | Preparation of thymidine and deoxyfluorouridine, and intermediates therefor |
| US3041335A (en) | 1959-04-21 | 1962-06-26 | Hoffmann La Roche | Mercury salts of nitrogen heterocyclics and preparation thereof |
| US4179337A (en) | 1973-07-20 | 1979-12-18 | Davis Frank F | Non-immunogenic polypeptides |
| US4296105A (en) | 1978-08-03 | 1981-10-20 | Institut International De Pathologie Cellulaire Et Moleculaire | Derivatives of doxorubicine, their preparation and use |
| US4348522A (en) | 1980-01-23 | 1982-09-07 | Starks Associates, Inc. | N-(phosphonacetyl)-L-aspartic acid salts with piperazine, cyclohexylamine and calcium |
| EP0329184A3 (en) | 1988-02-19 | 1990-05-23 | Neorx Corporation | Antimers and antimeric conjugation |
| RU2085557C1 (ru) | 1991-09-30 | 1997-07-27 | Санкио Компани Лимитед | Производные нуклеозидов пиримидина или их фармацевтически приемлемые соли и способ их получения |
| US5643957A (en) | 1993-04-22 | 1997-07-01 | Emisphere Technologies, Inc. | Compounds and compositions for delivering active agents |
| EP0737077A1 (en) * | 1994-01-11 | 1996-10-16 | Targetech, Inc. | Hepatocyte-targeted drug conjugates |
| JP4157600B2 (ja) | 1994-08-19 | 2008-10-01 | ラ レフィオン バロンネ | 化合物、製剤用組成物及びこれらを含む診断装置とこれらの利用 |
| JPH0859688A (ja) | 1994-08-25 | 1996-03-05 | Mitsui Toatsu Chem Inc | 5’−チオノエステル置換トリフルオロチミジン誘導体およびそれを有効成分とする制癌剤 |
| US6001347A (en) | 1995-03-31 | 1999-12-14 | Emisphere Technologies, Inc. | Compounds and compositions for delivering active agents |
| US5650386A (en) | 1995-03-31 | 1997-07-22 | Emisphere Technologies, Inc. | Compositions for oral delivery of active agents |
| SI9720025A (sl) | 1996-03-29 | 1999-08-31 | Emishphere Technologies, Inc. | Spojine in sestavki za prenos aktivne snovi |
| US6258774B1 (en) | 1998-03-19 | 2001-07-10 | University Of Medicine And Dentistry Of New Jersey | Carrier for in vivo delivery of a therapeutic agent |
| PT1144011E (pt) | 1998-12-11 | 2010-06-16 | Coulter Pharm Inc | Compostos pró-fármacos e processo para a sua preparação |
| JP5046219B2 (ja) | 2002-10-31 | 2012-10-10 | リガンド・ファーマシューティカルズ・インコーポレイテッド | 1,3−プロパン−1−アリールジオールの新規環状リン酸ジエステルおよびそのプロドラッグへの使用 |
| KR101442288B1 (ko) | 2006-12-13 | 2014-09-19 | 지보당 네덜란드 서비시즈 비.브이. | 카복실산과 퓨린, 피리미딘, 뉴클레오사이드 또는 뉴클레오타이드의 향미 조절 유도체 |
| CN101812105A (zh) | 2009-02-25 | 2010-08-25 | 沈阳药科大学 | 阿糖胞苷5’-o-氨基酸酯和其盐类及其制备方法 |
| KR20140079831A (ko) | 2011-10-18 | 2014-06-27 | 아지노모토 가부시키가이샤 | 췌장암 및/또는 담도암 치료약 |
| JP2016503005A (ja) * | 2012-12-18 | 2016-02-01 | ゴーダーヴァリ バイオリファイナリーズ リミテッド | 腫瘍始原細胞を除去するための薬剤 |
| WO2015178265A1 (ja) | 2014-05-23 | 2015-11-26 | 日本化薬株式会社 | 新規なグルタミン酸誘導体およびその用途 |
-
2016
- 2016-01-25 BR BR112018011177A patent/BR112018011177A2/pt not_active Application Discontinuation
- 2016-01-25 EP EP16870114.2A patent/EP3383407B1/en active Active
- 2016-01-25 CA CA3007058A patent/CA3007058C/en active Active
- 2016-01-25 US US15/780,732 patent/US11058701B2/en active Active - Reinstated
- 2016-01-25 CN CN201680070972.5A patent/CN108289905A/zh active Pending
- 2016-01-25 RU RU2018119319A patent/RU2708672C1/ru active
- 2016-01-25 JP JP2018527797A patent/JP7149183B2/ja active Active
- 2016-01-25 WO PCT/IL2016/050077 patent/WO2017093993A1/en not_active Ceased
- 2016-01-25 AU AU2016362830A patent/AU2016362830B2/en not_active Ceased
-
2018
- 2018-05-27 IL IL259631A patent/IL259631B/en unknown
-
2020
- 2020-07-17 JP JP2020122708A patent/JP2020183419A/ja active Pending
-
2021
- 2021-10-27 IL IL287644A patent/IL287644A/en unknown
-
2022
- 2022-05-10 JP JP2022077787A patent/JP7417658B2/ja active Active
- 2022-06-22 AU AU2022204373A patent/AU2022204373B2/en not_active Ceased
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20110275590A1 (en) * | 2004-02-02 | 2011-11-10 | BioSight Ltd., | Conjugates for cancer therapy and diagnosis |
| CN103781760A (zh) * | 2011-06-13 | 2014-05-07 | 株式会社Ihi | 金属salen络合物化合物、局部麻醉药剂及抗恶性肿瘤药剂 |
Non-Patent Citations (4)
| Title |
|---|
| CHEON EP, ET AL.: "Enhanced cellular uptake of ara-C via a peptidomimetic prodrug, L-valyl-ara-C in Caco-2 cells", 《JOURNAL OF PHARMACY AND PHARMACOLOGY》 * |
| CHHIKARA BS, ET AL.: "Development of cytarabine prodrugs and delivery systems for leukemia treatment", 《EXPERT OPINION ON DRUG DELIVERY》 * |
| FASINU P, ET AL.: "Diverse approaches for the enhancement of oral drug bioavailability", 《BIOPHARMACEUTICS DRUG DISPOSITION》 * |
| RENIS HE, ET AL.: "Antiviral activity of cytarabine in herpesvirus-infected rats", 《ANTIMICROBIAL AGENTS AND CHEMOTHERAPY》 * |
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110590862A (zh) * | 2019-11-01 | 2019-12-20 | 南京师范大学 | 阿糖胞苷4-n位氨基酸衍生物及其制备方法与应用 |
| CN115052607A (zh) * | 2020-02-04 | 2022-09-13 | 拜欧赛特有限公司 | 天冬阿糖胞苷药物组合物和其用途 |
| CN115461058A (zh) * | 2020-04-23 | 2022-12-09 | 拜欧赛特有限公司 | 用于治疗血液癌的方法和方案 |
| CN112409431A (zh) * | 2020-12-07 | 2021-02-26 | 武汉伯瑞恒医药科技有限公司 | 阿糖胞苷结构类似物及其制备方法和用途 |
| CN112409431B (zh) * | 2020-12-07 | 2023-04-21 | 武汉伯瑞恒医药科技有限公司 | 阿糖胞苷结构类似物及其制备方法和用途 |
Also Published As
| Publication number | Publication date |
|---|---|
| IL287644A (en) | 2021-12-01 |
| US20180369265A1 (en) | 2018-12-27 |
| JP7149183B2 (ja) | 2022-10-06 |
| JP7417658B2 (ja) | 2024-01-18 |
| AU2016362830A1 (en) | 2018-07-12 |
| AU2022204373B2 (en) | 2024-01-25 |
| WO2017093993A1 (en) | 2017-06-08 |
| IL259631A (en) | 2018-07-31 |
| JP2018535989A (ja) | 2018-12-06 |
| EP3383407A4 (en) | 2019-07-17 |
| JP2022097619A (ja) | 2022-06-30 |
| RU2708672C1 (ru) | 2019-12-11 |
| US11058701B2 (en) | 2021-07-13 |
| CA3007058C (en) | 2023-10-17 |
| CA3007058A1 (en) | 2017-06-08 |
| IL259631B (en) | 2021-10-31 |
| EP3383407B1 (en) | 2023-12-06 |
| AU2022204373A1 (en) | 2022-07-28 |
| EP3383407A1 (en) | 2018-10-10 |
| JP2020183419A (ja) | 2020-11-12 |
| AU2016362830B2 (en) | 2022-07-14 |
| BR112018011177A2 (pt) | 2018-11-21 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PB01 | Publication | ||
| PB01 | Publication | ||
| SE01 | Entry into force of request for substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| RJ01 | Rejection of invention patent application after publication | ||
| RJ01 | Rejection of invention patent application after publication |
Application publication date: 20180717 |