MD4625C1 - Derivaţi de 5-fenoxi-3H-pirimidin-4-onă şi utilizarea acestora ca inhibitori ai transcriptazei inverse a HIV - Google Patents
Derivaţi de 5-fenoxi-3H-pirimidin-4-onă şi utilizarea acestora ca inhibitori ai transcriptazei inverse a HIVInfo
- Publication number
- MD4625C1 MD4625C1 MD20150047A MD20150047A MD4625C1 MD 4625 C1 MD4625 C1 MD 4625C1 MD 20150047 A MD20150047 A MD 20150047A MD 20150047 A MD20150047 A MD 20150047A MD 4625 C1 MD4625 C1 MD 4625C1
- Authority
- MD
- Moldova
- Prior art keywords
- reverse transcriptase
- hiv reverse
- transcriptase inhibitors
- pyrimidin
- phenoxy
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- 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
- A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/52—Two oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/52—Two oxygen atoms
- C07D239/54—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/56—One oxygen atom and one sulfur atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Virology (AREA)
- Communicable Diseases (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Molecular Biology (AREA)
- Tropical Medicine & Parasitology (AREA)
- AIDS & HIV (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Enzymes And Modification Thereof (AREA)
Abstract
Compuşii cu formula I:în care R1, R2, R3, M şi Z au semnificaţiile definite în descriere, sunt inhibitori de transcriptază inversă a HIV. Compuşii cu formula I şi sărurile farmaceutic acceptabile ale acestora sunt utile în inhibarea transcriptazei inverse a HIV, profilaxia şi tratamentul infecţiei HIV şi în profilaxia, întârzierea debutului sau progresării şi tratamentul SIDA. Compuşii şi sărurile acestora pot fi utilizate ca ingrediente în compoziţii farmaceutice, opţional în combinaţie cu alte preparate antivirale, imunomodulatori, antibiotice sau vaccinuri.Revendicări: 51Figuri: 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2012001358 | 2012-10-08 | ||
| PCT/US2013/063612 WO2014058747A1 (en) | 2012-10-08 | 2013-10-07 | 5-phenoxy-3h-pyrimidin-4-one derivatives and their use as hiv reverse transcriptase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| MD20150047A2 MD20150047A2 (ro) | 2015-08-31 |
| MD4625B1 MD4625B1 (ro) | 2019-04-30 |
| MD4625C1 true MD4625C1 (ro) | 2019-11-30 |
Family
ID=49354986
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MD20150047A MD4625C1 (ro) | 2012-10-08 | 2013-10-07 | Derivaţi de 5-fenoxi-3H-pirimidin-4-onă şi utilizarea acestora ca inhibitori ai transcriptazei inverse a HIV |
Country Status (47)
Families Citing this family (44)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20140031250A1 (en) | 2010-10-07 | 2014-01-30 | David Tsai Ting | Biomarkers of Cancer |
| JO3470B1 (ar) * | 2012-10-08 | 2020-07-05 | Merck Sharp & Dohme | مشتقات 5- فينوكسي-3h-بيريميدين-4-أون واستخدامها كمثبطات ناسخ عكسي ل hiv |
| UY35735A (es) | 2013-09-16 | 2015-04-30 | Bayer Pharma AG | Trifluorometilpirimidinonas disustituidas y su uso |
| PT3125894T (pt) * | 2014-04-01 | 2020-11-05 | Merck Sharp & Dohme | Profármacos de inibidores da transcriptase reversa do vih |
| CA2959208C (en) | 2014-08-29 | 2023-09-19 | Tes Pharma S.R.L. | Pyrimidine derivatives and their use as inhibitors of alpha-amino-beta-carboxymuconate-epsilon-semialdehyde decarboxylase |
| FR3027901B1 (fr) * | 2014-10-31 | 2018-03-16 | Universite De Reims Champagne Ardenne | Nouveaux procedes appartenant a la famille des pyridazinones. |
| US10350165B2 (en) * | 2014-12-12 | 2019-07-16 | Ojai Energetics Pbc | Methods and systems for forming stable droplets |
| IL294014B2 (en) | 2015-10-23 | 2024-07-01 | Harvard College | Nucleobase editors and their uses |
| CA3032699A1 (en) | 2016-08-03 | 2018-02-08 | President And Fellows Of Harvard College | Adenosine nucleobase editors and uses thereof |
| AU2017308889B2 (en) | 2016-08-09 | 2023-11-09 | President And Fellows Of Harvard College | Programmable Cas9-recombinase fusion proteins and uses thereof |
| US11542509B2 (en) | 2016-08-24 | 2023-01-03 | President And Fellows Of Harvard College | Incorporation of unnatural amino acids into proteins using base editing |
| WO2018071868A1 (en) | 2016-10-14 | 2018-04-19 | President And Fellows Of Harvard College | Aav delivery of nucleobase editors |
| US10745677B2 (en) | 2016-12-23 | 2020-08-18 | President And Fellows Of Harvard College | Editing of CCR5 receptor gene to protect against HIV infection |
| EP3592853A1 (en) | 2017-03-09 | 2020-01-15 | President and Fellows of Harvard College | Suppression of pain by gene editing |
| JP2020510439A (ja) | 2017-03-10 | 2020-04-09 | プレジデント アンド フェローズ オブ ハーバード カレッジ | シトシンからグアニンへの塩基編集因子 |
| IL269458B2 (en) | 2017-03-23 | 2024-02-01 | Harvard College | Nucleic base editors that include nucleic acid programmable DNA binding proteins |
| WO2018209320A1 (en) | 2017-05-12 | 2018-11-15 | President And Fellows Of Harvard College | Aptazyme-embedded guide rnas for use with crispr-cas9 in genome editing and transcriptional activation |
| JP2020534795A (ja) | 2017-07-28 | 2020-12-03 | プレジデント アンド フェローズ オブ ハーバード カレッジ | ファージによって支援される連続的進化（ｐａｃｅ）を用いて塩基編集因子を進化させるための方法および組成物 |
| US11319532B2 (en) | 2017-08-30 | 2022-05-03 | President And Fellows Of Harvard College | High efficiency base editors comprising Gam |
| EP3684364A4 (en) * | 2017-09-18 | 2021-06-02 | Goldfinch Bio, Inc. | PYRIDAZINONE AND METHOD OF USE THEREOF |
| US11795443B2 (en) | 2017-10-16 | 2023-10-24 | The Broad Institute, Inc. | Uses of adenosine base editors |
| CA3090652A1 (en) | 2018-02-06 | 2019-08-15 | The General Hospital Corporation | Repeat rna as biomarkers of tumor immune response |
| CA3098585A1 (en) | 2018-04-30 | 2019-11-07 | Ribon Therapeutics Inc. | Pyridazinones as parp7 inhibitors |
| PE20211774A1 (es) | 2018-09-18 | 2021-09-08 | Goldfinch Bio Inc | Piridazinonas y sus metodos de uso |
| EP3898595B1 (en) * | 2018-12-18 | 2024-05-01 | Merck Sharp & Dohme LLC | Pyrimidone derivatives as selective cytotoxic agents against hiv infected cells |
| DE112020001342T5 (de) | 2019-03-19 | 2022-01-13 | President and Fellows of Harvard College | Verfahren und Zusammensetzungen zum Editing von Nukleotidsequenzen |
| BR112021023204A8 (pt) | 2019-05-22 | 2023-04-11 | Merck Sharp & Dohme | Composto, composição farmacêutica, métodos para tratar infecção por hiv, para induzir dimerização de gag-pol em células infectadas por hiv, para matar seletivamente células expressoras de gag-pol infectadas por hiv e para aumentar a supressão de viremia do hiv, e, uso de um composto |
| US20240091303A1 (en) * | 2019-10-04 | 2024-03-21 | Goldfinch Bio, Inc. | Biomarker-based treatment of focal segmental glomerulosclerosis and diabetic kidney disease |
| AU2020375821A1 (en) | 2019-10-30 | 2022-06-02 | Ribon Therapeutics, Inc. | Pyridazinones as PARP7 inhibitors |
| WO2021107066A1 (ja) | 2019-11-28 | 2021-06-03 | 塩野義製薬株式会社 | インテグラーゼ阻害剤及び抗ｈｉｖ薬を組み合わせることを特徴とするｈｉｖ感染症の予防及び治療用医薬 |
| TW202146416A (zh) | 2019-12-11 | 2021-12-16 | 德商拜耳廠股份有限公司 | 吡唑并三𠯤 |
| DE112021002672T5 (de) | 2020-05-08 | 2023-04-13 | President And Fellows Of Harvard College | Vefahren und zusammensetzungen zum gleichzeitigen editieren beider stränge einer doppelsträngigen nukleotid-zielsequenz |
| JP2023543803A (ja) | 2020-09-24 | 2023-10-18 | ザ ブロード インスティテュート，インコーポレーテッド | プライム編集ガイドｒｎａ、その組成物、及びその使用方法 |
| WO2022150790A2 (en) | 2021-01-11 | 2022-07-14 | The Broad Institute, Inc. | Prime editor variants, constructs, and methods for enhancing prime editing efficiency and precision |
| KR20240029027A (ko) * | 2021-07-01 | 2024-03-05 | 얀센 파마슈티카 엔브이 | 5-옥소-피리도[2,3-d]피리다진-6(5H)-일 아세트아미드 |
| EP4381057A2 (en) | 2021-08-06 | 2024-06-12 | The Broad Institute Inc. | Improved prime editors and methods of use |
| WO2023076898A1 (en) | 2021-10-25 | 2023-05-04 | The Broad Institute, Inc. | Methods and compositions for editing a genome with prime editing and a recombinase |
| GB202409668D0 (en) | 2021-12-03 | 2024-08-14 | Broad Inst Inc | Self-assembling virus-like particles for delivery of prime editors and methods of making and using same |
| WO2023205687A1 (en) | 2022-04-20 | 2023-10-26 | The Broad Institute, Inc. | Improved prime editing methods and compositions |
| WO2023240137A1 (en) | 2022-06-08 | 2023-12-14 | The Board Institute, Inc. | Evolved cas14a1 variants, compositions, and methods of making and using same in genome editing |
| WO2024077267A1 (en) | 2022-10-07 | 2024-04-11 | The Broad Institute, Inc. | Prime editing methods and compositions for treating triplet repeat disorders |
| WO2024108092A1 (en) | 2022-11-17 | 2024-05-23 | The Broad Institute, Inc. | Prime editor delivery by aav |
| WO2024168147A2 (en) | 2023-02-09 | 2024-08-15 | The Broad Institute, Inc. | Evolved recombinases for editing a genome in combination with prime editing |
| WO2024206125A1 (en) | 2023-03-24 | 2024-10-03 | The Broad Institute, Inc. | Use of prime editing for treating sickle cell disease |
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2013
- 2013-09-29 JO JOP/2013/0284A patent/JO3470B1/ar active
- 2013-10-02 AR ARP130103568A patent/AR092876A1/es active IP Right Grant
- 2013-10-07 HR HRP20220502TT patent/HRP20220502T1/hr unknown
- 2013-10-07 ES ES19210167T patent/ES2909190T3/es active Active
- 2013-10-07 SI SI201330835T patent/SI2903977T1/sl unknown
- 2013-10-07 PT PT171913072T patent/PT3295942T/pt unknown
- 2013-10-07 LT LTEP13776702.6T patent/LT2903977T/lt unknown
- 2013-10-07 NZ NZ706729A patent/NZ706729A/en unknown
- 2013-10-07 RS RS20220359A patent/RS63112B1/sr unknown
- 2013-10-07 EP EP19210167.3A patent/EP3656384B1/en active Active
- 2013-10-07 NO NO13776702A patent/NO2903977T3/no unknown
- 2013-10-07 EA EA201590674A patent/EA033436B1/ru not_active IP Right Cessation
- 2013-10-07 PT PT137767026T patent/PT2903977T/pt unknown
- 2013-10-07 CA CA2887312A patent/CA2887312C/en active Active
- 2013-10-07 BR BR112015007742A patent/BR112015007742B8/pt active IP Right Grant
- 2013-10-07 LT LTEP19210167.3T patent/LT3656384T/lt unknown
- 2013-10-07 ES ES17191307T patent/ES2770774T3/es active Active
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- 2013-10-07 HU HUE19210167A patent/HUE058903T2/hu unknown
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- 2013-10-07 AU AU2013329552A patent/AU2013329552B8/en active Active
- 2013-10-07 SI SI201331662T patent/SI3295942T1/sl unknown
- 2013-10-07 KR KR1020157011661A patent/KR101696128B1/ko active IP Right Grant
- 2013-10-07 PE PE2015001782A patent/PE20151787A1/es active IP Right Grant
- 2013-10-07 MY MYPI2015000836A patent/MY192716A/en unknown
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Owner name: MERCK SHARP & DOHME LLC, US126 EAST LINCOLN AVENUE, RAHWAY, NEW JERSEY 07065, STATELE UNITE ALE AMERICII Free format text: PREVIOUS NAME OF PROPRIETOR: MERCK SHARP & DOHME CORP, US126 EAST LINCOLN AVENUE, RAHWAY,NEW JERSEY 07065-0907, STATELE UNITE ALE AMERICII |