CA2799391A1 - Improved process for a folate-targeted agent - Google Patents
Improved process for a folate-targeted agent Download PDFInfo
- Publication number
- CA2799391A1 CA2799391A1 CA2799391A CA2799391A CA2799391A1 CA 2799391 A1 CA2799391 A1 CA 2799391A1 CA 2799391 A CA2799391 A CA 2799391A CA 2799391 A CA2799391 A CA 2799391A CA 2799391 A1 CA2799391 A1 CA 2799391A1
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- Prior art keywords
- formula
- compound
- buffer
- treating
- reaction mixture
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- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 description 1
- 125000001624 naphthyl group Chemical group 0.000 description 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 description 1
- 239000012299 nitrogen atmosphere Substances 0.000 description 1
- 125000004433 nitrogen atom Chemical group N* 0.000 description 1
- 230000002611 ovarian Effects 0.000 description 1
- 210000003101 oviduct Anatomy 0.000 description 1
- 230000003647 oxidation Effects 0.000 description 1
- 238000007254 oxidation reaction Methods 0.000 description 1
- 238000007911 parenteral administration Methods 0.000 description 1
- 238000010647 peptide synthesis reaction Methods 0.000 description 1
- 201000002524 peritoneal carcinoma Diseases 0.000 description 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 description 1
- 239000010452 phosphate Substances 0.000 description 1
- 239000002953 phosphate buffered saline Substances 0.000 description 1
- 230000003389 potentiating effect Effects 0.000 description 1
- 238000001556 precipitation Methods 0.000 description 1
- 108090000765 processed proteins & peptides Proteins 0.000 description 1
- WHMDPDGBKYUEMW-UHFFFAOYSA-N pyridine-2-thiol Chemical compound SC1=CC=CC=N1 WHMDPDGBKYUEMW-UHFFFAOYSA-N 0.000 description 1
- 238000010791 quenching Methods 0.000 description 1
- 150000003254 radicals Chemical class 0.000 description 1
- 238000004366 reverse phase liquid chromatography Methods 0.000 description 1
- 238000013341 scale-up Methods 0.000 description 1
- 238000010898 silica gel chromatography Methods 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- 238000010532 solid phase synthesis reaction Methods 0.000 description 1
- 238000000638 solvent extraction Methods 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 229910052717 sulfur Inorganic materials 0.000 description 1
- 239000011593 sulfur Substances 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 238000003786 synthesis reaction Methods 0.000 description 1
- 230000008685 targeting Effects 0.000 description 1
- 150000003573 thiols Chemical class 0.000 description 1
- 125000002221 trityl group Chemical group [H]C1=C([H])C([H])=C([H])C([H])=C1C([*])(C1=C(C(=C(C(=C1[H])[H])[H])[H])[H])C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 description 1
- JXLYSJRDGCGARV-XQKSVPLYSA-N vincaleukoblastine Chemical class C([C@@H](C[C@]1(C(=O)OC)C=2C(=CC3=C([C@]45[C@H]([C@@]([C@H](OC(C)=O)[C@]6(CC)C=CCN([C@H]56)CC4)(O)C(=O)OC)N3C)C=2)OC)C[C@@](C2)(O)CC)N2CCC2=C1NC1=CC=CC=C21 JXLYSJRDGCGARV-XQKSVPLYSA-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 (1)
| Publication Number | Publication Date |
|---|---|
| CA2799391A1 true CA2799391A1 (en) | 2011-12-04 |
Family
ID=44992057
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2799391A Abandoned CA2799391A1 (en) | 2010-05-19 | 2011-05-19 | Improved process for a folate-targeted agent |
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) |
Families Citing this family (3)
| 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 |
| WO2017172930A1 (en) * | 2016-03-29 | 2017-10-05 | Endocyte, Inc. | Pbd conjugates for treating diseases |
| 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
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 |
| MX2012013250A (es) | 2013-03-05 |
| CN102984943A (zh) | 2013-03-20 |
| KR20130079431A (ko) | 2013-07-10 |
| SG185592A1 (en) | 2012-12-28 |
| JP2013526577A (ja) | 2013-06-24 |
| CN102984943B (zh) | 2016-01-13 |
| RU2012154914A (ru) | 2014-06-27 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FZDE | Discontinued |
Effective date: 20160519 |