CN112996778A - 制备微管溶素及其中间体的替代方法 - Google Patents
制备微管溶素及其中间体的替代方法 Download PDFInfo
- Publication number
- CN112996778A CN112996778A CN201980071734.XA CN201980071734A CN112996778A CN 112996778 A CN112996778 A CN 112996778A CN 201980071734 A CN201980071734 A CN 201980071734A CN 112996778 A CN112996778 A CN 112996778A
- Authority
- CN
- China
- Prior art keywords
- optionally substituted
- formula
- moiety
- compound
- alkyl
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
- C07K1/107—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides
- C07K1/1072—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides by covalent attachment of residues or functional groups
- C07K1/1077—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides by covalent attachment of residues or functional groups by covalent attachment of residues other than amino acids or peptide residues, e.g. sugars, polyols, fatty acids
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
- C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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 to ring carbon atoms
- C07D277/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
-
- 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
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
- C07H15/26—Acyclic or carbocyclic radicals, substituted by hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
- C07K5/021—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-(X)n-C(=0)-, n being 5 or 6; for n > 6, classification in C07K5/06 - C07K5/10, according to the moiety having normal peptide bonds
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/10—Tetrapeptides
- C07K5/1024—Tetrapeptides with the first amino acid being heterocyclic
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Biochemistry (AREA)
- Genetics & Genomics (AREA)
- Medicinal Chemistry (AREA)
- Molecular Biology (AREA)
- Biophysics (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Engineering & Computer Science (AREA)
- Analytical Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Biotechnology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Crystallography & Structural Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Peptides Or Proteins (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862728639P | 2018-09-07 | 2018-09-07 | |
| US62/728,639 | 2018-09-07 | ||
| PCT/US2019/050023 WO2020051503A1 (en) | 2018-09-07 | 2019-09-06 | Alternative processes for the preparation of tubulysins and intermediates thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN112996778A true CN112996778A (zh) | 2021-06-18 |
Family
ID=68000124
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201980071734.XA Pending CN112996778A (zh) | 2018-09-07 | 2019-09-06 | 制备微管溶素及其中间体的替代方法 |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US20230002440A1 (https=) |
| EP (1) | EP3847161A1 (https=) |
| JP (1) | JP7511543B2 (https=) |
| KR (1) | KR20210073525A (https=) |
| CN (1) | CN112996778A (https=) |
| AU (1) | AU2019336231A1 (https=) |
| BR (1) | BR112021004317A2 (https=) |
| CA (1) | CA3111149A1 (https=) |
| EA (1) | EA202190699A1 (https=) |
| IL (1) | IL281090A (https=) |
| MA (1) | MA53550A (https=) |
| MX (1) | MX2021002570A (https=) |
| SA (1) | SA521421375B1 (https=) |
| SG (1) | SG11202102126VA (https=) |
| TW (1) | TWI825169B (https=) |
| UA (1) | UA128730C2 (https=) |
| WO (1) | WO2020051503A1 (https=) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN115867283A (zh) * | 2020-12-23 | 2023-03-28 | 启德医药科技(苏州)有限公司 | 包含开环硫代琥珀酰亚胺基团、寡肽片段和手性部分的新型异构化合物 |
| BR112023018676A2 (pt) | 2021-03-18 | 2023-10-10 | Seagen Inc | Conjugado anticorpo-fármaco, composição farmacêutica, métodos de tratamento de uma doença ou condição e de um câncer, e, composição de conjugado ligante-fármaco |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008138561A1 (en) * | 2007-05-10 | 2008-11-20 | R & D Biopharmaceuticals Gmbh | Tubulysine derivatives |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IT1394860B1 (it) | 2009-07-22 | 2012-07-20 | Kemotech S R L | Composti farmaceutici |
| KR20180090290A (ko) | 2015-12-04 | 2018-08-10 | 시애틀 지네틱스, 인크. | 사차화 튜불리신 화합물들의 컨쥬게이트들 |
| KR20200051733A (ko) * | 2017-09-08 | 2020-05-13 | 시애틀 지네틱스, 인크. | 튜불리신 및 그 중간물의 제조 공정 |
-
2019
- 2019-09-06 US US17/273,693 patent/US20230002440A1/en not_active Abandoned
- 2019-09-06 CN CN201980071734.XA patent/CN112996778A/zh active Pending
- 2019-09-06 TW TW108132162A patent/TWI825169B/zh active
- 2019-09-06 EP EP19773284.5A patent/EP3847161A1/en active Pending
- 2019-09-06 MA MA053550A patent/MA53550A/fr unknown
- 2019-09-06 MX MX2021002570A patent/MX2021002570A/es unknown
- 2019-09-06 CA CA3111149A patent/CA3111149A1/en active Pending
- 2019-09-06 WO PCT/US2019/050023 patent/WO2020051503A1/en not_active Ceased
- 2019-09-06 EA EA202190699A patent/EA202190699A1/ru unknown
- 2019-09-06 SG SG11202102126VA patent/SG11202102126VA/en unknown
- 2019-09-06 JP JP2021512696A patent/JP7511543B2/ja active Active
- 2019-09-06 KR KR1020217010157A patent/KR20210073525A/ko not_active Withdrawn
- 2019-09-06 BR BR112021004317-9A patent/BR112021004317A2/pt unknown
- 2019-09-06 AU AU2019336231A patent/AU2019336231A1/en not_active Abandoned
- 2019-09-06 UA UAA202101737A patent/UA128730C2/uk unknown
-
2021
- 2021-02-24 IL IL281090A patent/IL281090A/en unknown
- 2021-03-03 SA SA521421375A patent/SA521421375B1/ar unknown
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008138561A1 (en) * | 2007-05-10 | 2008-11-20 | R & D Biopharmaceuticals Gmbh | Tubulysine derivatives |
Non-Patent Citations (2)
| Title |
|---|
| AZA-MICHAEL REACTIONS OF 2-ENOYLTHIAZOLES SREEJITH SHANKAR P. 等: "Studies towards a Novel Synthesis of Tubulysins: Highly Asymmetric Aza-Michael Reactions of 2-Enoylthiazoles with Metalated Chiral Oxazolidinones", SYNLETT * |
| MONICA SANI 等: "Total Synthesis of Tubulysins U and V", ANGEW. CHEM. INT. ED., pages 8 - 9 * |
Also Published As
| Publication number | Publication date |
|---|---|
| JP2021536475A (ja) | 2021-12-27 |
| JP7511543B2 (ja) | 2024-07-05 |
| IL281090A (en) | 2021-04-29 |
| MA53550A (fr) | 2021-12-15 |
| UA128730C2 (uk) | 2024-10-09 |
| WO2020051503A1 (en) | 2020-03-12 |
| TW202024043A (zh) | 2020-07-01 |
| TWI825169B (zh) | 2023-12-11 |
| CA3111149A1 (en) | 2020-03-12 |
| BR112021004317A2 (pt) | 2021-05-25 |
| SG11202102126VA (en) | 2021-04-29 |
| EA202190699A1 (ru) | 2021-06-08 |
| EP3847161A1 (en) | 2021-07-14 |
| US20230002440A1 (en) | 2023-01-05 |
| MX2021002570A (es) | 2021-06-08 |
| AU2019336231A1 (en) | 2021-03-18 |
| SA521421375B1 (ar) | 2024-02-11 |
| KR20210073525A (ko) | 2021-06-18 |
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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 | ||
| REG | Reference to a national code |
Ref country code: HK Ref legal event code: DE Ref document number: 40045709 Country of ref document: HK |
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| CB02 | Change of applicant information | ||
| CB02 | Change of applicant information |
Address after: Washington State Applicant after: Sijin Co. Address before: Washington State Applicant before: Xigen Co. |
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| WD01 | Invention patent application deemed withdrawn after publication | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20210618 |