MD4625B1 - 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 HIV Download PDFInfo
- Publication number
- MD4625B1 MD4625B1 MDA20150047A MD20150047A MD4625B1 MD 4625 B1 MD4625 B1 MD 4625B1 MD A20150047 A MDA20150047 A MD A20150047A MD 20150047 A MD20150047 A MD 20150047A MD 4625 B1 MD4625 B1 MD 4625B1
- Authority
- MD
- Moldova
- Prior art keywords
- reverse transcriptase
- hiv reverse
- transcriptase inhibitors
- pyrimidin
- phenoxy
- Prior art date
Links
- 108010078851 HIV Reverse Transcriptase Proteins 0.000 title abstract 3
- 239000003419 rna directed dna polymerase inhibitor Substances 0.000 title abstract 2
- PRXCVXCFQYBCQL-UHFFFAOYSA-N 5-phenoxy-1h-pyrimidin-6-one Chemical class OC1=NC=NC=C1OC1=CC=CC=C1 PRXCVXCFQYBCQL-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- 238000011321 prophylaxis Methods 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 238000011282 treatment Methods 0.000 abstract 2
- 208000030507 AIDS Diseases 0.000 abstract 1
- 239000003242 anti bacterial agent Substances 0.000 abstract 1
- 229940088710 antibiotic agent Drugs 0.000 abstract 1
- 239000003443 antiviral agent Substances 0.000 abstract 1
- 239000002955 immunomodulating agent Substances 0.000 abstract 1
- 229940121354 immunomodulator Drugs 0.000 abstract 1
- 208000015181 infectious disease Diseases 0.000 abstract 1
- 239000004615 ingredient Substances 0.000 abstract 1
- 230000005764 inhibitory process Effects 0.000 abstract 1
- 229940042443 other antivirals in atc Drugs 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 229960005486 vaccine Drugs 0.000 abstract 1
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.
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 true MD4625B1 (ro) | 2019-04-30 |
| MD4625C1 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 (46)
Families Citing this family (58)
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| US9228207B2 (en) | 2013-09-06 | 2016-01-05 | President And Fellows Of Harvard College | Switchable gRNAs comprising aptamers |
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| TW200831085A (en) | 2006-12-13 | 2008-08-01 | Merck & Co Inc | Non-nucleoside reverse transcriptase inhibitors |
| AU2008326784B2 (en) * | 2007-11-20 | 2014-04-24 | Merck Sharp & Dohme Corp. | Non-nucleoside reverse transcriptase inhibitors |
| CN103254138A (zh) * | 2008-01-08 | 2013-08-21 | 默沙东公司 | 用于制备n-取代的羟基嘧啶酮羧酰胺类化合物的方法 |
| PL2552902T3 (pl) | 2010-03-30 | 2015-10-30 | Merck Canada Inc | Nienukleozydowe inhibitory odwrotnej transkryptazy |
| US20130040914A1 (en) | 2010-04-08 | 2013-02-14 | Samson M. Jolly | Prodrugs of an hiv reverse transcriptase inhibitor |
| JO3470B1 (ar) | 2012-10-08 | 2020-07-05 | Merck Sharp & Dohme | مشتقات 5- فينوكسي-3h-بيريميدين-4-أون واستخدامها كمثبطات ناسخ عكسي ل hiv |
| JP6342011B2 (ja) | 2014-04-01 | 2018-06-13 | メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． | Ｈｉｖ逆転写酵素阻害剤のプロドラッグ |
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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 |