EA024804B1 - Ненуклеозидные ингибиторы обратной транскриптазы, композиции, их содержащие, и их применение - Google Patents
Ненуклеозидные ингибиторы обратной транскриптазы, композиции, их содержащие, и их применение Download PDFInfo
- Publication number
- EA024804B1 EA024804B1 EA201290976A EA201290976A EA024804B1 EA 024804 B1 EA024804 B1 EA 024804B1 EA 201290976 A EA201290976 A EA 201290976A EA 201290976 A EA201290976 A EA 201290976A EA 024804 B1 EA024804 B1 EA 024804B1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- compound
- pharmaceutically acceptable
- hiv
- compounds
- mmol
- Prior art date
Links
- 239000000203 mixture Substances 0.000 title 1
- 229940042402 non-nucleoside reverse transcriptase inhibitor Drugs 0.000 title 1
- 239000002726 nonnucleoside reverse transcriptase inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract 23
- 150000003839 salts Chemical class 0.000 claims abstract 16
- 238000011321 prophylaxis Methods 0.000 claims abstract 14
- 238000011282 treatment Methods 0.000 claims abstract 14
- 208000030507 AIDS Diseases 0.000 claims abstract 7
- 208000015181 infectious disease Diseases 0.000 claims abstract 7
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract 4
- 229910052736 halogen Inorganic materials 0.000 claims 9
- 150000002367 halogens Chemical class 0.000 claims 9
- 230000002265 prevention Effects 0.000 claims 6
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 5
- 125000000217 alkyl group Chemical group 0.000 claims 3
- 239000003937 drug carrier Substances 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 2
- 125000003709 fluoroalkyl group Chemical group 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 1
- 125000001188 haloalkyl group Chemical group 0.000 claims 1
- 108010078851 HIV Reverse Transcriptase Proteins 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
- 150000002390 heteroarenes Chemical class 0.000 abstract 1
- 239000002955 immunomodulating agent Substances 0.000 abstract 1
- 229940121354 immunomodulator Drugs 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
- 239000003419 rna directed dna polymerase inhibitor Substances 0.000 abstract 1
- 229960005486 vaccine Drugs 0.000 abstract 1
Classifications
-
- 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
- C07D401/02—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 two hetero rings
- C07D401/06—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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
-
- 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)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Communicable Diseases (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Virology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Molecular Biology (AREA)
- AIDS & HIV (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Steroid Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Saccharide Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US31882410P | 2010-03-30 | 2010-03-30 | |
| US32157310P | 2010-04-07 | 2010-04-07 | |
| PCT/CA2011/000320 WO2011120133A1 (en) | 2010-03-30 | 2011-03-28 | Non-nucleoside reverse transcriptase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA201290976A1 EA201290976A1 (ru) | 2013-03-29 |
| EA024804B1 true EA024804B1 (ru) | 2016-10-31 |
Family
ID=44710363
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201290976A EA024804B1 (ru) | 2010-03-30 | 2011-03-28 | Ненуклеозидные ингибиторы обратной транскриптазы, композиции, их содержащие, и их применение |
Country Status (44)
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HUE025336T2 (en) * | 2010-03-30 | 2016-03-29 | Merck Canada Inc | Non-nucleoside reverse transcriptase inhibitors |
| EP2625292B1 (en) | 2010-10-07 | 2018-12-05 | The General Hospital Corporation | Biomarkers of cancer |
| BR112015005997A8 (pt) * | 2012-09-26 | 2023-04-11 | Merck Sharp & Dohme | Composto |
| JO3470B1 (ar) * | 2012-10-08 | 2020-07-05 | Merck Sharp & Dohme | مشتقات 5- فينوكسي-3h-بيريميدين-4-أون واستخدامها كمثبطات ناسخ عكسي ل hiv |
| EP2928472B1 (en) * | 2012-12-05 | 2018-05-02 | Merck Sharp & Dohme Corp. | Process for making reverse transcriptase inhibitors |
| RU2661399C1 (ru) * | 2013-11-22 | 2018-07-16 | Мерк Шарп И Доум Корп. | Композиция ненуклеозидного ингибитора обратной транскриптазы |
| BR112016012658B1 (pt) | 2013-12-04 | 2022-06-21 | Merck Sharp & Dohme Corp | Métodos para sintetizar inibidores da transcriptase reversa e composto |
| PL3125894T3 (pl) * | 2014-04-01 | 2021-02-08 | Merck Sharp & Dohme Corp. | Proleki inhibitorów odwrotnej transkryptazy hiv |
| EP3161159B1 (en) | 2014-06-25 | 2020-08-05 | The General Hospital Corporation | Targeting human satellite ii (hsatii) |
| EP4424373B1 (en) | 2015-12-02 | 2025-11-12 | Merck Sharp & Dohme LLC | Pharmaceutical compositions containing doravirine, tenofovir disoproxil fumarate and lamivudine |
| WO2018175271A1 (en) * | 2017-03-24 | 2018-09-27 | Merck Sharp & Dohme Corp. | Formulation for parenteral administration |
| CN110769856A (zh) | 2017-04-18 | 2020-02-07 | 希普拉有限公司 | 用于治疗逆转录病毒感染的组合疗法 |
| EP4317972A3 (en) | 2018-02-06 | 2024-03-13 | The General Hospital Corporation | Repeat rna as biomarkers of tumor immune response |
| EP3823632B1 (en) * | 2018-07-17 | 2025-10-29 | Merck Sharp & Dohme LLC | Efda in combination with doravirine for use in treating f227c mutated hiv infections |
| PE20211704A1 (es) | 2018-12-18 | 2021-09-01 | Merck Sharp & Dohme | Derivados de pirimidona como agentes citotoxicos selectivos contra celulas infectadas por vih |
| CN110801455B (zh) * | 2019-11-12 | 2020-06-02 | 河北医科大学第二医院 | 用于治疗mrsa的药物组合物及其应用 |
| CN114163309B (zh) * | 2021-12-27 | 2023-04-25 | 甘肃皓天医药科技有限责任公司 | 一种多拉韦林中间体的制备方法 |
| CN114349690B (zh) * | 2022-02-15 | 2023-04-25 | 甘肃皓天医药科技有限责任公司 | 一种多拉韦林中间体合成方法 |
| CN116903590A (zh) * | 2023-06-06 | 2023-10-20 | 延边大学 | 一种含杂环结构的吡啶酮类化合物及其制备方法和用途 |
| CN120157613A (zh) * | 2023-12-15 | 2025-06-17 | 山东诚创蓝海医药科技有限公司 | 多拉韦林中间体及其应用和合成方法 |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2515151A1 (en) * | 2003-02-18 | 2004-09-02 | F. Hoffmann-La Roche Ag | Non-nucleoside reverse transcriptase inhibitors |
| CA2518437A1 (en) * | 2003-03-24 | 2004-10-07 | James Patrick Dunn | Non-nucleoside reverse transcriptase inhibitors i for treating hiv mediated diseases |
| CA2705834A1 (en) * | 2007-11-20 | 2009-05-28 | Merck Sharp & Dohme Corp. | Pyridinone non-nucleoside reverse transcriptase inhibitors |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SE9904045D0 (sv) | 1999-11-09 | 1999-11-09 | Astra Ab | Compounds |
| CN100469769C (zh) | 2003-03-24 | 2009-03-18 | 弗·哈夫曼-拉罗切有限公司 | 作为逆转录酶抑制剂的苄基-哒嗪酮 |
| BRPI0510059B8 (pt) | 2004-04-23 | 2021-05-25 | Hoffmann La Roche | inibidores da transcriptase reversa não-nucleosídica e seus usos |
| US7166738B2 (en) | 2004-04-23 | 2007-01-23 | Roche Palo Alto Llc | Non-nucleoside reverse transcriptase inhibitors |
| CA2592092A1 (en) | 2004-12-22 | 2006-06-29 | Pfizer Limited | Nonnucleoside inhibitors of hiv-1 reverse transcriptase |
| AR057455A1 (es) | 2005-07-22 | 2007-12-05 | Merck & Co Inc | Inhibidores de la transcriptasa reversa de vih y composicion farmaceutica |
| CN101291905A (zh) | 2005-10-19 | 2008-10-22 | 弗·哈夫曼-拉罗切有限公司 | 苯乙酰胺nnrt抑制剂 |
| CA2625039A1 (en) | 2005-10-19 | 2007-04-26 | F. Hoffmann-La Roche Ag | N-phenyl phenylacetamide non-nucleoside reverse transcriptase inihibitors |
| TW200831085A (en) | 2006-12-13 | 2008-08-01 | Merck & Co Inc | Non-nucleoside reverse transcriptase inhibitors |
| HUE025336T2 (en) * | 2010-03-30 | 2016-03-29 | Merck Canada Inc | Non-nucleoside reverse transcriptase inhibitors |
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2011
- 2011-03-28 HU HUE11761856A patent/HUE025336T2/en unknown
- 2011-03-28 ME MEP-2015-76A patent/ME02181B/me unknown
- 2011-03-28 SG SG2012072401A patent/SG184347A1/en unknown
- 2011-03-28 AU AU2011235568A patent/AU2011235568B2/en active Active
- 2011-03-28 MX MX2012011379A patent/MX2012011379A/es active IP Right Grant
- 2011-03-28 MA MA35324A patent/MA34170B1/fr unknown
- 2011-03-28 DK DK11761856.1T patent/DK2552902T3/en active
- 2011-03-28 EP EP11761856.1A patent/EP2552902B1/en active Active
- 2011-03-28 RS RS20150340A patent/RS54017B1/sr unknown
- 2011-03-28 JP JP2012538161A patent/JP5281718B2/ja active Active
- 2011-03-28 HU HUE15157348A patent/HUE031785T2/en unknown
- 2011-03-28 ME MEP-2016-282A patent/ME02570B/me unknown
- 2011-03-28 LT LTEP15157348.2T patent/LT2924034T/lt unknown
- 2011-03-28 ES ES11761856.1T patent/ES2536295T3/es active Active
- 2011-03-28 PH PH1/2012/501923A patent/PH12012501923A1/en unknown
- 2011-03-28 US US13/073,631 patent/US8486975B2/en active Active
- 2011-03-28 CA CA2794377A patent/CA2794377C/en active Active
- 2011-03-28 KR KR1020127025733A patent/KR101421861B1/ko active Active
- 2011-03-28 DK DK15157348.2T patent/DK2924034T3/en active
- 2011-03-28 NZ NZ602670A patent/NZ602670A/en unknown
- 2011-03-28 HR HRP20150427TT patent/HRP20150427T1/hr unknown
- 2011-03-28 CN CN201180018074.2A patent/CN102971308B/zh active Active
- 2011-03-28 PE PE2012001823A patent/PE20130158A1/es active IP Right Grant
- 2011-03-28 PL PL15157348T patent/PL2924034T3/pl unknown
- 2011-03-28 ES ES15157348.2T patent/ES2609636T3/es active Active
- 2011-03-28 RS RS20161093A patent/RS55505B1/sr unknown
- 2011-03-28 MY MYPI2012004342A patent/MY163979A/en unknown
- 2011-03-28 GE GEAP201112882A patent/GEP20156368B/en unknown
- 2011-03-28 PT PT151573482T patent/PT2924034T/pt unknown
- 2011-03-28 PL PL11761856T patent/PL2552902T3/pl unknown
- 2011-03-28 EA EA201290976A patent/EA024804B1/ru active Protection Beyond IP Right Term
- 2011-03-28 SI SI201131054A patent/SI2924034T1/sl unknown
- 2011-03-28 PT PT117618561T patent/PT2552902E/pt unknown
- 2011-03-28 WO PCT/CA2011/000320 patent/WO2011120133A1/en not_active Ceased
- 2011-03-28 BR BR112012024691-7A patent/BR112012024691B1/pt active IP Right Grant
- 2011-03-28 SI SI201130491T patent/SI2552902T1/sl unknown
- 2011-03-28 EP EP15157348.2A patent/EP2924034B1/en active Active
- 2011-03-29 AR ARP110101028A patent/AR080859A1/es active IP Right Grant
- 2011-03-29 TW TW100110833A patent/TWI458719B/zh active
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2012
- 2012-09-20 TN TNP2012000455A patent/TN2012000455A1/en unknown
- 2012-09-20 IL IL222030A patent/IL222030A/en active Protection Beyond IP Right Term
- 2012-09-27 HN HN2012002039A patent/HN2012002039A/es unknown
- 2012-09-28 DO DO2012000256A patent/DOP2012000256A/es unknown
- 2012-09-28 NI NI201200146A patent/NI201200146A/es unknown
- 2012-09-28 CL CL2012002744A patent/CL2012002744A1/es unknown
- 2012-10-01 EC ECSP12012201 patent/ECSP12012201A/es unknown
- 2012-10-01 CR CR20120503A patent/CR20120503A/es unknown
- 2012-10-01 CO CO12171897A patent/CO6630126A2/es active IP Right Grant
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2013
- 2013-05-23 JP JP2013108533A patent/JP5886790B2/ja not_active Expired - Fee Related
- 2013-07-03 US US13/934,633 patent/US20130296382A1/en not_active Abandoned
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2014
- 2014-06-23 IL IL233334A patent/IL233334A/en active IP Right Grant
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2016
- 2016-12-09 HR HRP20161680TT patent/HRP20161680T1/hr unknown
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2017
- 2017-01-25 CY CY20171100114T patent/CY1118774T1/el unknown
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2019
- 2019-04-09 HU HUS1900021C patent/HUS1900021I1/hu unknown
- 2019-04-09 HU HUS1900022C patent/HUS1900022I1/hu unknown
- 2019-04-11 LT LTPA2019506 patent/LTC2552902I2/lt unknown
- 2019-04-11 LT LTPA2019507C patent/LTC2924034I2/lt unknown
- 2019-04-16 NL NL300980C patent/NL300980I2/nl unknown
- 2019-04-17 FI FIC20190021C patent/FIC20190021I1/fi unknown
- 2019-04-17 LU LU00114C patent/LUC00114I2/fr unknown
- 2019-04-17 LU LU00113C patent/LUC00113I9/fr unknown
- 2019-04-24 NO NO2019019C patent/NO2019019I1/no unknown
- 2019-04-24 NO NO2019018C patent/NO2019018I1/no unknown
- 2019-05-16 CY CY2019026C patent/CY2019026I2/el unknown
- 2019-05-16 CY CY2019025C patent/CY2019025I1/el unknown
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2515151A1 (en) * | 2003-02-18 | 2004-09-02 | F. Hoffmann-La Roche Ag | Non-nucleoside reverse transcriptase inhibitors |
| CA2518437A1 (en) * | 2003-03-24 | 2004-10-07 | James Patrick Dunn | Non-nucleoside reverse transcriptase inhibitors i for treating hiv mediated diseases |
| CA2705834A1 (en) * | 2007-11-20 | 2009-05-28 | Merck Sharp & Dohme Corp. | Pyridinone non-nucleoside reverse transcriptase inhibitors |
Non-Patent Citations (1)
| Title |
|---|
| Sweeney Z. K. et al. "Discovery of triazolinone non-nucleoside inhibitors of HIV reverse transcriptase", Bioorganic & Medicinal Chemistry Letters, 18 (2008) 4348-4351, entire document * |
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| Date | Code | Title | Description |
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| MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): KG MD TJ TM |
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| ND4A | Extension of term of a eurasian patent |