ECSP15018618A - Inhibidores no nucleósidos de la transcriptasa inversa - Google Patents
Inhibidores no nucleósidos de la transcriptasa inversaInfo
- Publication number
- ECSP15018618A ECSP15018618A ECIEPI201518618A ECPI201518618A ECSP15018618A EC SP15018618 A ECSP15018618 A EC SP15018618A EC IEPI201518618 A ECIEPI201518618 A EC IEPI201518618A EC PI201518618 A ECPI201518618 A EC PI201518618A EC SP15018618 A ECSP15018618 A EC SP15018618A
- Authority
- EC
- Ecuador
- Prior art keywords
- reverse transcriptase
- inhibitors
- nucleosid
- compounds
- prophylaxis
- 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)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Virology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Molecular Biology (AREA)
- AIDS & HIV (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (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
Los compuestos de Fórmula I: son inhibidores de la transcriptasa inversa del VIH, en la que R1, R2, RE, L, M y Z se definen en el presente documento. Los compuestos de Fórmula I y sus sales farmacéuticamente aceptables son útiles en la inhibición de la transcriptasa inversa del VIH, la profilaxis y el tratamiento de infección por VIH y en la profilaxis, retraso de la aparición o el desarrollo, y tratamiento del SIDA. Los compuestos y sus sales se pueden emplear como ingredientes en composiciones
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CN2012001358 | 2012-10-08 |
Publications (1)
Publication Number | Publication Date |
---|---|
ECSP15018618A true ECSP15018618A (es) | 2019-06-30 |
Family
ID=49354986
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ECIEPI201518618A ECSP15018618A (es) | 2012-10-08 | 2015-05-12 | Inhibidores no nucleósidos de la transcriptasa inversa |
Country Status (47)
Families Citing this family (44)
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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 |
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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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US7803940B2 (en) | 2006-11-24 | 2010-09-28 | Takeda Pharmaceutical Company Limited | Heteromonocyclic compound or a salt thereof having strong antihypertensive action, insulin sensitizing activity and the like production thereof and use thereof for prophylaxis or treatment of cardiovascular diseases, metabolic diseases and/or central nervous system diseases |
TW200831085A (en) | 2006-12-13 | 2008-08-01 | Merck & Co Inc | Non-nucleoside reverse transcriptase inhibitors |
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EP2231621B1 (en) * | 2008-01-08 | 2016-11-02 | Merck Sharp & Dohme Corp. | Process for preparing n-substituted hydroxypyrimidinone carboxamides |
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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
- 2013-10-07 PT PT192101673T patent/PT3656384T/pt unknown
- 2013-10-07 HU HUE19210167A patent/HUE058903T2/hu unknown
- 2013-10-07 HU HUE13776702A patent/HUE037231T2/hu unknown
- 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
- 2013-10-07 EP EP17191307.2A patent/EP3295942B1/en active Active
- 2013-10-07 EP EP13776702.6A patent/EP2903977B1/en active Active
- 2013-10-07 AP AP2015008355A patent/AP2015008355A0/xx unknown
- 2013-10-07 JP JP2015535852A patent/JP5877281B2/ja active Active
- 2013-10-07 PL PL19210167T patent/PL3656384T3/pl unknown
- 2013-10-07 RS RS20200052A patent/RS59863B1/sr unknown
- 2013-10-07 MA MA37959A patent/MA37959A2/fr unknown
- 2013-10-07 TW TW102136225A patent/TWI538907B/zh active
- 2013-10-07 UA UAA201504486A patent/UA114006C2/uk unknown
- 2013-10-07 MX MX2015004448A patent/MX355040B/es active IP Right Grant
- 2013-10-07 MD MD20150047A patent/MD4625C1/ro active IP Right Grant
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