JP2013526577A - 葉酸を標的にする薬剤用の改善されたプロセス - Google Patents
葉酸を標的にする薬剤用の改善されたプロセス Download PDFInfo
- Publication number
- JP2013526577A JP2013526577A JP2013511354A JP2013511354A JP2013526577A JP 2013526577 A JP2013526577 A JP 2013526577A JP 2013511354 A JP2013511354 A JP 2013511354A JP 2013511354 A JP2013511354 A JP 2013511354A JP 2013526577 A JP2013526577 A JP 2013526577A
- Authority
- JP
- Japan
- Prior art keywords
- formula
- compound represented
- buffer
- acylating agent
- reaction mixture
- 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.)
- Withdrawn
Links
- 0 CCC(*)(C1)C*(CC2)=CC1C[C@](*)(C(C=C(C*1*)[C@@]3(CC4)C1(*I)C(*)(CC(**C(OCCN*)=O)=*)[C@](*)C1(CC)C=CC*4C31)=C(C*)*C)C(*1)=C2c2c1cccc2 Chemical compound CCC(*)(C1)C*(CC2)=CC1C[C@](*)(C(C=C(C*1*)[C@@]3(CC4)C1(*I)C(*)(CC(**C(OCCN*)=O)=*)[C@](*)C1(CC)C=CC*4C31)=C(C*)*C)C(*1)=C2c2c1cccc2 0.000 description 2
- VZEYMKJCJRJWAT-UHFFFAOYSA-N C(CSSc1ccccn1)OC1OC1 Chemical compound C(CSSc1ccccn1)OC1OC1 VZEYMKJCJRJWAT-UHFFFAOYSA-N 0.000 description 1
- ADEUBFAWQRMQQZ-UHFFFAOYSA-N N=C(OCCSSc1ncccc1)O[n]1nnc2ccccc12 Chemical compound N=C(OCCSSc1ncccc1)O[n]1nnc2ccccc12 ADEUBFAWQRMQQZ-UHFFFAOYSA-N 0.000 description 1
- KRPACOYLOTZHII-UHFFFAOYSA-N O=C(OCCSSc1ccccn1)O[n]1nnc2c1cccc2 Chemical compound O=C(OCCSSc1ccccn1)O[n]1nnc2c1cccc2 KRPACOYLOTZHII-UHFFFAOYSA-N 0.000 description 1
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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
- C07K7/02—Linear peptides containing at least one abnormal peptide link
-
- 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
- A61K47/55—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 the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
- A61K47/551—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 the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds one of the codrug's components being a vitamin, e.g. niacinamide, vitamin B3, cobalamin, vitamin B12, folate, vitamin A or retinoic acid
-
- 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)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Genetics & Genomics (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Molecular Biology (AREA)
- Biophysics (AREA)
- Biochemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US34644410P | 2010-05-19 | 2010-05-19 | |
| US61/346,444 | 2010-05-19 | ||
| US35102210P | 2010-06-03 | 2010-06-03 | |
| US61/351,022 | 2010-06-03 | ||
| PCT/US2011/037134 WO2011146707A1 (en) | 2010-05-19 | 2011-05-19 | Improved process for a folate-targeted agent |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2013526577A true JP2013526577A (ja) | 2013-06-24 |
| JP2013526577A5 JP2013526577A5 (enExample) | 2014-07-10 |
Family
ID=44992057
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013511354A Withdrawn JP2013526577A (ja) | 2010-05-19 | 2011-05-19 | 葉酸を標的にする薬剤用の改善されたプロセス |
Country Status (11)
| Country | Link |
|---|---|
| US (2) | US20130065841A1 (enExample) |
| JP (1) | JP2013526577A (enExample) |
| KR (1) | KR20130079431A (enExample) |
| CN (1) | CN102984943B (enExample) |
| BR (1) | BR112012029458A2 (enExample) |
| CA (1) | CA2799391A1 (enExample) |
| IL (1) | IL222964A0 (enExample) |
| MX (1) | MX2012013250A (enExample) |
| RU (1) | RU2012154914A (enExample) |
| SG (1) | SG185592A1 (enExample) |
| WO (1) | WO2011146707A1 (enExample) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2020515582A (ja) * | 2016-03-29 | 2020-05-28 | エンドサイト・インコーポレイテッドＥｎｄｏｃｙｔｅ， Ｉｎｃ． | 腫瘍関連マクロファージの治療における使用のための葉酸コンジュゲート |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6676650B2 (ja) | 2015-03-13 | 2020-04-08 | エンドサイト・インコーポレイテッドＥｎｄｏｃｙｔｅ， Ｉｎｃ． | 疾患を処置するためのコンジュゲート |
| WO2019196999A1 (en) | 2018-04-11 | 2019-10-17 | Radisurf Aps | Compositions for forming polymer brushes |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100381177C (zh) * | 2003-01-27 | 2008-04-16 | 恩多塞特公司 | 维生素受体结合递药缀合物 |
| CN100423778C (zh) * | 2003-11-25 | 2008-10-08 | 上海复旦张江生物医药股份有限公司 | 用于上载抗肿瘤药物的脂质体载体及其制备方法和应用 |
| JP2009504783A (ja) * | 2005-08-19 | 2009-02-05 | エンドサイト，インコーポレイテッド | ビンカアルカロイド、類似体および誘導体のリガンド結合体 |
-
2011
- 2011-05-19 US US13/698,215 patent/US20130065841A1/en not_active Abandoned
- 2011-05-19 WO PCT/US2011/037134 patent/WO2011146707A1/en not_active Ceased
- 2011-05-19 CN CN201180035630.7A patent/CN102984943B/zh not_active Expired - Fee Related
- 2011-05-19 SG SG2012084190A patent/SG185592A1/en unknown
- 2011-05-19 RU RU2012154914/13A patent/RU2012154914A/ru not_active Application Discontinuation
- 2011-05-19 BR BR112012029458A patent/BR112012029458A2/pt not_active IP Right Cessation
- 2011-05-19 KR KR1020127032401A patent/KR20130079431A/ko not_active Withdrawn
- 2011-05-19 CA CA2799391A patent/CA2799391A1/en not_active Abandoned
- 2011-05-19 MX MX2012013250A patent/MX2012013250A/es not_active Application Discontinuation
- 2011-05-19 JP JP2013511354A patent/JP2013526577A/ja not_active Withdrawn
-
2012
- 2012-11-11 IL IL222964A patent/IL222964A0/en unknown
-
2013
- 2013-03-14 US US13/803,150 patent/US20140066593A1/en not_active Abandoned
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2020515582A (ja) * | 2016-03-29 | 2020-05-28 | エンドサイト・インコーポレイテッドＥｎｄｏｃｙｔｅ， Ｉｎｃ． | 腫瘍関連マクロファージの治療における使用のための葉酸コンジュゲート |
Also Published As
| Publication number | Publication date |
|---|---|
| IL222964A0 (en) | 2013-02-03 |
| BR112012029458A2 (pt) | 2015-10-20 |
| US20140066593A1 (en) | 2014-03-06 |
| WO2011146707A1 (en) | 2011-11-24 |
| US20130065841A1 (en) | 2013-03-14 |
| CA2799391A1 (en) | 2011-12-04 |
| MX2012013250A (es) | 2013-03-05 |
| CN102984943A (zh) | 2013-03-20 |
| KR20130079431A (ko) | 2013-07-10 |
| SG185592A1 (en) | 2012-12-28 |
| CN102984943B (zh) | 2016-01-13 |
| RU2012154914A (ru) | 2014-06-27 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AU2024202618A1 (en) | Bicyclic peptide ligands specific for EphA2 | |
| AU2020214507B2 (en) | Bi-ligand drug conjugate and use thereof | |
| JP2024023291A (ja) | 多量体二環式ペプチドリガンド | |
| AU2020204250B2 (en) | One-pot process for preparing intermediate of antibody-drug conjugate | |
| CN109939242B (zh) | 抗体前药偶联物及其制备和应用 | |
| AU2018329066B2 (en) | Amanitin antibody conjugate | |
| JP2022515720A (ja) | Ｉｌ－１７に特異的な二環式ペプチドリガンド | |
| Tai et al. | A novel rapamycin-polymer conjugate based on a new poly (ethylene glycol) multiblock copolymer | |
| SA113340536B1 (ar) | معضدات مستقبل v1a | |
| JP2013526577A (ja) | 葉酸を標的にする薬剤用の改善されたプロセス | |
| CN111574592B (zh) | 一类具有拮抗pd-1/pd-l1相互作用的环肽类化合物及其应用 | |
| CN111909240B (zh) | 一种pd-1/pd-l1多肽类抑制剂及其医药用途 | |
| CA3085001C (en) | One-pot process for preparing intermediate of antibody-drug conjugate | |
| EP4201429A1 (en) | Antibody-drug conjugate intermediate comprising sn38 and preparation method therefor | |
| EP4417618A1 (en) | Epha2 bicyclic peptide ligand and conjugate thereof | |
| EP3950700A1 (en) | Peptide complex and production method therefor, and use of said peptide complex | |
| EP2571362A1 (en) | Improved process for a folate-targeted agent | |
| TWI905962B (zh) | 用於綴合之化合物、綴合物及包含其之醫藥組成物 | |
| Cao et al. | Peptide-drug conjugates with linker-dependent payload release coordinate dual antitumor efficacy: Intrinsic RGDS-mediated metastasis suppression synergizes with camptothecin cytotoxicity | |
| RU2798981C2 (ru) | Конъюгат антитела с аматоксином неприродного типа | |
| RU2809116C2 (ru) | Конъюгат амантина с антителом | |
| Le Roy et al. | Grafting a chromophore on AMD070 analogues for CXCR4 bioimaging: Chemical synthesis and in vitro assessment of the inhibition properties of the CXCR4 receptor | |
| EP4365184A1 (en) | Analysis method for peptide bound to carrier for liquid phase peptide synthesis | |
| RU2840926C2 (ru) | Конъюгат антитела с аматоксином неприродного типа | |
| ES2930177T3 (es) | Procedimiento optimizado para el conjugado péptido-fosfolípido dimérico |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20140519 |
|
| A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20140519 |
|
| A761 | Written withdrawal of application |
Free format text: JAPANESE INTERMEDIATE CODE: A761 Effective date: 20150223 |