PL391695A1 - Pochodne 2',3'-didehydro-3'-deoksy-4'-etynylotymidyny do leczenia zakażeń wirusem ludzkiego nabytego niedoboru odporności (HIV) wykazujących oporność wielolekową, sposób ich wytwarzania oraz farmaceutycznie dopuszczalne formy leków - Google Patents
Pochodne 2',3'-didehydro-3'-deoksy-4'-etynylotymidyny do leczenia zakażeń wirusem ludzkiego nabytego niedoboru odporności (HIV) wykazujących oporność wielolekową, sposób ich wytwarzania oraz farmaceutycznie dopuszczalne formy lekówInfo
- Publication number
- PL391695A1 PL391695A1 PL391695A PL39169510A PL391695A1 PL 391695 A1 PL391695 A1 PL 391695A1 PL 391695 A PL391695 A PL 391695A PL 39169510 A PL39169510 A PL 39169510A PL 391695 A1 PL391695 A1 PL 391695A1
- Authority
- PL
- Poland
- Prior art keywords
- derivatives
- didehydro
- deoxy
- hiv
- ethynylthymidine
- Prior art date
Links
- OSYWBJSVKUFFSU-SKDRFNHKSA-N festinavir Chemical class O=C1NC(=O)C(C)=CN1[C@H]1C=C[C@](CO)(C#C)O1 OSYWBJSVKUFFSU-SKDRFNHKSA-N 0.000 title abstract 4
- 241000725303 Human immunodeficiency virus Species 0.000 title 2
- 239000003814 drug Substances 0.000 title 1
- 229940079593 drug Drugs 0.000 title 1
- 230000001747 exhibiting effect Effects 0.000 title 1
- 208000015181 infectious disease Diseases 0.000 title 1
- 230000036457 multidrug resistance Effects 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 2
- 208000030507 AIDS Diseases 0.000 abstract 1
- 210000004366 CD4-positive T-lymphocyte Anatomy 0.000 abstract 1
- 241000713772 Human immunodeficiency virus 1 Species 0.000 abstract 1
- 230000000840 anti-viral effect Effects 0.000 abstract 1
- 230000003013 cytotoxicity Effects 0.000 abstract 1
- 231100000135 cytotoxicity Toxicity 0.000 abstract 1
- 231100000053 low toxicity Toxicity 0.000 abstract 1
- 210000005259 peripheral blood Anatomy 0.000 abstract 1
- 239000011886 peripheral blood Substances 0.000 abstract 1
- 230000001225 therapeutic effect Effects 0.000 abstract 1
- 230000009466 transformation Effects 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
- C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
- C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
- C07H19/06—Pyrimidine radicals
-
- 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
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Virology (AREA)
- Molecular Biology (AREA)
- General Health & Medical Sciences (AREA)
- Communicable Diseases (AREA)
- General Chemical & Material Sciences (AREA)
- Biochemistry (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
- Engineering & Computer Science (AREA)
- Biotechnology (AREA)
- Oncology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Genetics & Genomics (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Ujawniono pochodne 4'-etynylostawudyny o wzorze ogólnym 1, które charakteryzują się bardzo wysoką aktywnością przeciwwirusową, zarówno w stosunku do szczepu dzikiego HIV-1, jak i jego szczepów opornych, przy całkowitym braku cytotoksyczności w stężeniach terapeutycznych, czyli nadzwyczaj wysokim indeksem selektywności. Ze względu na bardzo niską toksyczność związki te mogą być stosowane we wszystkich stadiach AIDS, również w fazie końcowej tj. w momencie, gdy ilość limfocytów T4 u pacjentów spada poniżej 200/µL krwi obwodowej. Pochodne 2',3'-didehydro-3'-deoksy-4'-etynylotymidyny, według wynalazku, wytwarza się poprzez transformację znanego związku 4'-etynylostawudyny.
Priority Applications (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PL391695A PL217133B1 (pl) | 2010-06-30 | 2010-06-30 | Pochodne 2',3'-didehydro-3'-deoksy-4'-etynylotymidyny do leczenia zakażeń wirusem ludzkiego nabytego niedoboru odporności (HIV) wykazujących oporność wielolekową, sposób ich wytwarzania oraz farmaceutycznie dopuszczalne formy leków |
| EP10172853A EP2402358A3 (en) | 2010-06-30 | 2010-08-15 | 2',3'-Didehydro-3'-deoxy-4'-ethynylothymidine derivatives for treatment infections caused by human immunodeficiency virus (HIV) multidrug resistant strains, method of their synthesis and pharmaceutically acceptable forms of drugs |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PL391695A PL217133B1 (pl) | 2010-06-30 | 2010-06-30 | Pochodne 2',3'-didehydro-3'-deoksy-4'-etynylotymidyny do leczenia zakażeń wirusem ludzkiego nabytego niedoboru odporności (HIV) wykazujących oporność wielolekową, sposób ich wytwarzania oraz farmaceutycznie dopuszczalne formy leków |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| PL391695A1 true PL391695A1 (pl) | 2012-01-02 |
| PL217133B1 PL217133B1 (pl) | 2014-06-30 |
Family
ID=44774212
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PL391695A PL217133B1 (pl) | 2010-06-30 | 2010-06-30 | Pochodne 2',3'-didehydro-3'-deoksy-4'-etynylotymidyny do leczenia zakażeń wirusem ludzkiego nabytego niedoboru odporności (HIV) wykazujących oporność wielolekową, sposób ich wytwarzania oraz farmaceutycznie dopuszczalne formy leków |
Country Status (2)
| Country | Link |
|---|---|
| EP (1) | EP2402358A3 (pl) |
| PL (1) | PL217133B1 (pl) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2021188959A1 (en) | 2020-03-20 | 2021-09-23 | Gilead Sciences, Inc. | Prodrugs of 4'-c-substituted-2-halo-2'-deoxyadenosine nucleosides and methods of making and using the same |
| AU2023255774A1 (en) * | 2022-04-22 | 2024-12-05 | Rome Therapeutics, Inc. | Didehydro-3'-deoxy-4'-ethynylthymidines and related compounds and their use in treating medical conditions |
-
2010
- 2010-06-30 PL PL391695A patent/PL217133B1/pl unknown
- 2010-08-15 EP EP10172853A patent/EP2402358A3/en not_active Withdrawn
Also Published As
| Publication number | Publication date |
|---|---|
| EP2402358A3 (en) | 2012-07-18 |
| PL217133B1 (pl) | 2014-06-30 |
| EP2402358A2 (en) | 2012-01-04 |
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