SA521421375B1 - عمليات بديلة لتحضير مركبات تيوبولايسن ومركبات وسيطة منها - Google Patents
عمليات بديلة لتحضير مركبات تيوبولايسن ومركبات وسيطة منهاInfo
- Publication number
- SA521421375B1 SA521421375B1 SA521421375A SA521421375A SA521421375B1 SA 521421375 B1 SA521421375 B1 SA 521421375B1 SA 521421375 A SA521421375 A SA 521421375A SA 521421375 A SA521421375 A SA 521421375A SA 521421375 B1 SA521421375 B1 SA 521421375B1
- Authority
- SA
- Saudi Arabia
- Prior art keywords
- intermediates
- preparation
- tubulysins
- alternative processes
- tubulysin
- Prior art date
Links
- 239000000543 intermediate Substances 0.000 title abstract 2
- 229930184737 tubulysin Natural products 0.000 title abstract 2
- DLKUYSQUHXBYPB-NSSHGSRYSA-N (2s,4r)-4-[[2-[(1r,3r)-1-acetyloxy-4-methyl-3-[3-methylbutanoyloxymethyl-[(2s,3s)-3-methyl-2-[[(2r)-1-methylpiperidine-2-carbonyl]amino]pentanoyl]amino]pentyl]-1,3-thiazole-4-carbonyl]amino]-2-methyl-5-(4-methylphenyl)pentanoic acid Chemical class N([C@@H]([C@@H](C)CC)C(=O)N(COC(=O)CC(C)C)[C@H](C[C@@H](OC(C)=O)C=1SC=C(N=1)C(=O)N[C@H](C[C@H](C)C(O)=O)CC=1C=CC(C)=CC=1)C(C)C)C(=O)[C@H]1CCCCN1C DLKUYSQUHXBYPB-NSSHGSRYSA-N 0.000 abstract 2
- 239000003814 drug Substances 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
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)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
يتعلق الاختراع الحالي بالكشف عن عمليات مُحسَّنة لتحضير مركبات تيوبولايسن tubulysin ومركبات رابط عقار تيوبولايسن tubulysin drug linker والمركبات الوسيطة منها.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201862728639P | 2018-09-07 | 2018-09-07 |
Publications (1)
Publication Number | Publication Date |
---|---|
SA521421375B1 true SA521421375B1 (ar) | 2024-02-11 |
Family
ID=68000124
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
SA521421375A SA521421375B1 (ar) | 2018-09-07 | 2021-03-03 | عمليات بديلة لتحضير مركبات تيوبولايسن ومركبات وسيطة منها |
Country Status (16)
Country | Link |
---|---|
US (1) | US20230002440A1 (ar) |
EP (1) | EP3847161A1 (ar) |
JP (1) | JP7511543B2 (ar) |
KR (1) | KR20210073525A (ar) |
CN (1) | CN112996778A (ar) |
AU (1) | AU2019336231A1 (ar) |
BR (1) | BR112021004317A2 (ar) |
CA (1) | CA3111149A1 (ar) |
EA (1) | EA202190699A1 (ar) |
IL (1) | IL281090A (ar) |
MA (1) | MA53550A (ar) |
MX (1) | MX2021002570A (ar) |
SA (1) | SA521421375B1 (ar) |
SG (1) | SG11202102126VA (ar) |
TW (1) | TWI825169B (ar) |
WO (1) | WO2020051503A1 (ar) |
Families Citing this family (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US12036286B2 (en) | 2021-03-18 | 2024-07-16 | Seagen Inc. | Selective drug release from internalized conjugates of biologically active compounds |
Family Cites Families (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US8980833B2 (en) * | 2007-05-10 | 2015-03-17 | R&D-Biopharmaceuticals Gmbh | Tubulysine derivatives |
IT1394860B1 (it) * | 2009-07-22 | 2012-07-20 | Kemotech S R L | Composti farmaceutici |
CA3006000A1 (en) * | 2015-12-04 | 2017-06-08 | Seattle Genetics, Inc. | Conjugates of quaternized tubulysin compounds |
EA202090670A1 (ru) * | 2017-09-08 | 2020-07-28 | Сиэтл Дженетикс, Инк. | Способ получения тубулизинов и их промежуточных соединений |
-
2019
- 2019-09-06 SG SG11202102126VA patent/SG11202102126VA/en unknown
- 2019-09-06 EA EA202190699A patent/EA202190699A1/ru unknown
- 2019-09-06 US US17/273,693 patent/US20230002440A1/en active Pending
- 2019-09-06 KR KR1020217010157A patent/KR20210073525A/ko active Search and Examination
- 2019-09-06 CA CA3111149A patent/CA3111149A1/en active Pending
- 2019-09-06 CN CN201980071734.XA patent/CN112996778A/zh active Pending
- 2019-09-06 MA MA053550A patent/MA53550A/fr unknown
- 2019-09-06 AU AU2019336231A patent/AU2019336231A1/en active Pending
- 2019-09-06 EP EP19773284.5A patent/EP3847161A1/en active Pending
- 2019-09-06 BR BR112021004317-9A patent/BR112021004317A2/pt unknown
- 2019-09-06 MX MX2021002570A patent/MX2021002570A/es unknown
- 2019-09-06 WO PCT/US2019/050023 patent/WO2020051503A1/en active Application Filing
- 2019-09-06 TW TW108132162A patent/TWI825169B/zh active
- 2019-09-06 JP JP2021512696A patent/JP7511543B2/ja active Active
-
2021
- 2021-02-24 IL IL281090A patent/IL281090A/en unknown
- 2021-03-03 SA SA521421375A patent/SA521421375B1/ar unknown
Also Published As
Publication number | Publication date |
---|---|
IL281090A (en) | 2021-04-29 |
MX2021002570A (es) | 2021-06-08 |
BR112021004317A2 (pt) | 2021-05-25 |
WO2020051503A1 (en) | 2020-03-12 |
US20230002440A1 (en) | 2023-01-05 |
AU2019336231A1 (en) | 2021-03-18 |
EP3847161A1 (en) | 2021-07-14 |
CA3111149A1 (en) | 2020-03-12 |
CN112996778A (zh) | 2021-06-18 |
JP7511543B2 (ja) | 2024-07-05 |
KR20210073525A (ko) | 2021-06-18 |
SG11202102126VA (en) | 2021-04-29 |
TW202024043A (zh) | 2020-07-01 |
MA53550A (fr) | 2021-12-15 |
JP2021536475A (ja) | 2021-12-27 |
EA202190699A1 (ru) | 2021-06-08 |
TWI825169B (zh) | 2023-12-11 |
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