DOP2015000082A - Inhibidores no nucleósidos de la transcriptasa inversa - Google Patents
Inhibidores no nucleósidos de la transcriptasa inversaInfo
- Publication number
- DOP2015000082A DOP2015000082A DO2015000082A DO2015000082A DOP2015000082A DO P2015000082 A DOP2015000082 A DO P2015000082A DO 2015000082 A DO2015000082 A DO 2015000082A DO 2015000082 A DO2015000082 A DO 2015000082A DO P2015000082 A DOP2015000082 A DO P2015000082A
- Authority
- DO
- Dominican Republic
- Prior art keywords
- compounds
- nucleoside inhibitors
- reverse transcript
- prophylaxis
- formula
- 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
Abstract
Los compuestos de Fórmula I: (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 fabricación de medicamento útiles en el tratamiento del SIDA. Los compuestos y sus sales se pueden emplear como ingredientes en composiciones farmacéuticas, opcionalmente en combinación con otros antivirales, inmunomoduladores, antibióticos o vacunas.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2012001358 | 2012-10-08 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| DOP2015000082A true DOP2015000082A (es) | 2015-08-16 |
Family
ID=49354986
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DO2015000082A DOP2015000082A (es) | 2012-10-08 | 2015-04-08 | Inhibidores no nucleósidos de la transcriptasa inversa |
Country Status (47)
Families Citing this family (41)
| 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 |
| WO2015036563A1 (de) | 2013-09-16 | 2015-03-19 | Bayer Pharma Aktiengesellschaft | Disubstituierte trifluormethylpyrimidinone und ihre verwendung als ccr2 antagonisten |
| EP3125894B1 (en) * | 2014-04-01 | 2020-09-09 | Merck Sharp & Dohme Corp. | Prodrugs of hiv reverse transcriptase inhibitors |
| JP6769963B2 (ja) | 2014-08-29 | 2020-10-14 | ティエエッセ ファルマ ソチエタ レスポンサビリタ リミタータ | α−アミノ−β−カルボキシムコン酸セミアルデヒド脱炭酸酵素の阻害剤 |
| 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 |
| EP3365357B1 (en) | 2015-10-23 | 2024-02-14 | President and Fellows of Harvard College | Evolved cas9 proteins for gene editing |
| AU2017306676B2 (en) | 2016-08-03 | 2024-02-22 | 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 |
| SG11201903089RA (en) | 2016-10-14 | 2019-05-30 | Harvard College | Aav delivery of nucleobase editors |
| WO2018119359A1 (en) | 2016-12-23 | 2018-06-28 | President And Fellows Of Harvard College | Editing of ccr5 receptor gene to protect against hiv infection |
| WO2018165504A1 (en) | 2017-03-09 | 2018-09-13 | President And Fellows Of Harvard College | Suppression of pain by gene editing |
| US11542496B2 (en) | 2017-03-10 | 2023-01-03 | President And Fellows Of Harvard College | Cytosine to guanine base editor |
| IL306092A (en) | 2017-03-23 | 2023-11-01 | 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 |
| WO2019139645A2 (en) | 2017-08-30 | 2019-07-18 | President And Fellows Of Harvard College | High efficiency base editors comprising gam |
| CA3075727A1 (en) * | 2017-09-18 | 2019-03-21 | Goldfinch Bio, Inc. | Pyridazinones and methods of use thereof |
| US11795443B2 (en) | 2017-10-16 | 2023-10-24 | The Broad Institute, Inc. | Uses of adenosine base editors |
| WO2019157087A1 (en) | 2018-02-06 | 2019-08-15 | The General Hospital Corporation | Repeat rna as biomarkers of tumor immune response |
| HRP20230458T1 (hr) | 2018-04-30 | 2023-07-21 | Ribon Therapeutics Inc. | Piridazinoni kao inhibitori parp7 |
| KR20210069652A (ko) | 2018-09-18 | 2021-06-11 | 골드핀치 바이오 인코포레이티드 | 피리다지논 및 이의 사용 방법 |
| AU2019402998B2 (en) * | 2018-12-18 | 2022-12-15 | Merck Sharp & Dohme Llc | Pyrimidone derivatives as selective cytotoxic agents against HIV infected cells |
| JP2022526908A (ja) | 2019-03-19 | 2022-05-27 | ザ ブロード インスティテュート，インコーポレーテッド | 編集ヌクレオチド配列を編集するための方法および組成物 |
| US20220242847A1 (en) * | 2019-05-22 | 2022-08-04 | Merck Sharp & Dohme Corp. | Pyridinone derivatives as selective cytotoxic agents against hiv infected cells |
| JP2022551580A (ja) * | 2019-10-04 | 2022-12-12 | ゴールドフィンチ バイオ，インク． | 巣状分節性糸球体硬化症および糖尿病性腎症のバイオマーカーに基づく処置 |
| US11691969B2 (en) | 2019-10-30 | 2023-07-04 | Ribon Therapeutics, Inc. | Pyridazinones as PARP7 inhibtors |
| JPWO2021107066A1 (es) | 2019-11-28 | 2021-06-03 | ||
| TW202146416A (zh) | 2019-12-11 | 2021-12-16 | 德商拜耳廠股份有限公司 | 吡唑并三𠯤 |
| AU2021267940A1 (en) | 2020-05-08 | 2022-12-08 | President And Fellows Of Harvard College | Methods and compositions for simultaneous editing of both strands of a target double-stranded nucleotide sequence |
| 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 |
| JP2024503437A (ja) | 2021-01-11 | 2024-01-25 | ザ ブロード インスティテュート，インコーポレーテッド | プライム編集効率及び精度を向上させるためのプライム編集因子バリアント、構築物、及び方法 |
| KR20240029027A (ko) * | 2021-07-01 | 2024-03-05 | 얀센 파마슈티카 엔브이 | 5-옥소-피리도[2,3-d]피리다진-6(5H)-일 아세트아미드 |
| CA3227004A1 (en) | 2021-08-06 | 2023-02-09 | 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 |
| WO2023102538A1 (en) | 2021-12-03 | 2023-06-08 | The Broad Institute, 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 |
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| IT1305313B1 (it) | 1998-07-17 | 2001-05-04 | Colla Paolo | 3,4 - diidro- 6- benzil-4-oxopirimidine sostituite e relativo processodi produzione e impiego nella terapia delle infezioni da hiv-1. |
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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 |
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| WO2009088729A1 (en) * | 2008-01-08 | 2009-07-16 | Merck & Co., Inc. | Process for preparing n-substituted hydroxypyrimidinone carboxamides |
| EA024804B1 (ru) | 2010-03-30 | 2016-10-31 | Мерк Кэнэда Инк. | Ненуклеозидные ингибиторы обратной транскриптазы, композиции, их содержащие, и их применение |
| WO2011126969A1 (en) | 2010-04-08 | 2011-10-13 | Merck Sharp & Dohme Corp. | 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 |
| EP3125894B1 (en) | 2014-04-01 | 2020-09-09 | Merck Sharp & Dohme Corp. | Prodrugs of hiv reverse transcriptase inhibitors |
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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 WO PCT/US2013/063612 patent/WO2014058747A1/en active Application Filing
- 2013-10-07 PT PT171913072T patent/PT3295942T/pt unknown
- 2013-10-07 LT LTEP19210167.3T patent/LT3656384T/lt unknown
- 2013-10-07 UA UAA201504486A patent/UA114006C2/uk unknown
- 2013-10-07 MY MYPI2015000836A patent/MY192716A/en unknown
- 2013-10-07 MD MD20150047A patent/MD4625C1/ro active IP Right Grant
- 2013-10-07 ES ES17191307T patent/ES2770774T3/es active Active
- 2013-10-07 BR BR112015007742A patent/BR112015007742B8/pt active IP Right Grant
- 2013-10-07 AP AP2015008355A patent/AP2015008355A0/xx unknown
- 2013-10-07 TW TW102136225A patent/TWI538907B/zh active
- 2013-10-07 SG SG11201502620UA patent/SG11201502620UA/en unknown
- 2013-10-07 HU HUE19210167A patent/HUE058903T2/hu unknown
- 2013-10-07 NO NO13776702A patent/NO2903977T3/no unknown
- 2013-10-07 PL PL13776702T patent/PL2903977T3/pl unknown
- 2013-10-07 MX MX2015004448A patent/MX355040B/es active IP Right Grant
- 2013-10-07 JP JP2015535852A patent/JP5877281B2/ja active Active
- 2013-10-07 CA CA2887312A patent/CA2887312C/en active Active
- 2013-10-07 SI SI201331662T patent/SI3295942T1/sl unknown
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- 2013-10-07 NZ NZ706729A patent/NZ706729A/en unknown
- 2013-10-07 PL PL19210167T patent/PL3656384T3/pl unknown
- 2013-10-07 LT LTEP13776702.6T patent/LT2903977T/lt unknown
- 2013-10-07 EP EP13776702.6A patent/EP2903977B1/en active Active
- 2013-10-07 DK DK13776702.6T patent/DK2903977T3/en active
- 2013-10-07 EP EP19210167.3A patent/EP3656384B1/en active Active
- 2013-10-07 EP EP17191307.2A patent/EP3295942B1/en active Active
- 2013-10-07 HU HUE17191307A patent/HUE048670T2/hu unknown
- 2013-10-07 RS RS20171164A patent/RS56543B1/sr unknown
- 2013-10-07 SI SI201330835T patent/SI2903977T1/sl unknown
- 2013-10-07 AU AU2013329552A patent/AU2013329552B8/en active Active
- 2013-10-07 GE GEAP201313818A patent/GEP20186838B/en unknown
- 2013-10-07 EA EA201590674A patent/EA033436B1/ru not_active IP Right Cessation
- 2013-10-07 HR HRP20220502TT patent/HRP20220502T1/hr unknown
- 2013-10-07 ES ES19210167T patent/ES2909190T3/es active Active
- 2013-10-07 TW TW105108710A patent/TWI598343B/zh active
- 2013-10-07 HU HUE13776702A patent/HUE037231T2/hu unknown
- 2013-10-07 CN CN201380061513.7A patent/CN104822670B/zh active Active
- 2013-10-07 ES ES13776702.6T patent/ES2645638T3/es active Active
- 2013-10-07 DK DK17191307.2T patent/DK3295942T3/da active
- 2013-10-07 US US14/047,515 patent/US9469634B2/en active Active
- 2013-10-07 DK DK19210167.3T patent/DK3656384T3/da active
- 2013-10-07 PL PL17191307T patent/PL3295942T3/pl unknown
- 2013-10-07 PE PE2015001782A patent/PE20151787A1/es active IP Right Grant
- 2013-10-07 MA MA37959A patent/MA37959A2/fr unknown
- 2013-10-07 LT LTEP17191307.2T patent/LT3295942T/lt unknown
- 2013-10-07 ME MEP-2017-264A patent/ME02918B/me unknown
- 2013-10-07 RS RS20220359A patent/RS63112B1/sr unknown
- 2013-10-07 PT PT137767026T patent/PT2903977T/pt unknown
- 2013-10-07 KR KR1020157011661A patent/KR101696128B1/ko active IP Right Grant
- 2013-10-07 RS RS20200052A patent/RS59863B1/sr unknown
- 2013-10-07 PT PT192101673T patent/PT3656384T/pt unknown
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2015
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