KR102795662B1 - Hiv-1 억제제로서의 c-3 및 c-17 변형된 트리테르페노이드 - Google Patents
Hiv-1 억제제로서의 c-3 및 c-17 변형된 트리테르페노이드 Download PDFInfo
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- KR102795662B1 KR102795662B1 KR1020187025343A KR20187025343A KR102795662B1 KR 102795662 B1 KR102795662 B1 KR 102795662B1 KR 1020187025343 A KR1020187025343 A KR 1020187025343A KR 20187025343 A KR20187025343 A KR 20187025343A KR 102795662 B1 KR102795662 B1 KR 102795662B1
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- South Korea
- Prior art keywords
- ethyl
- methyl
- cyclohex
- oxy
- carboxylate
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- 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
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J53/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by condensation with a carbocyclic rings or by formation of an additional ring by means of a direct link between two ring carbon atoms, including carboxyclic rings fused to the cyclopenta(a)hydrophenanthrene skeleton are included in this class
- C07J53/002—Carbocyclic rings fused
-
- 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
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
-
- 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
- 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
-
- 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
- C07D401/12—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 chain containing hetero atoms as chain links
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J63/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by expansion of only one ring by one or two atoms
- C07J63/008—Expansion of ring D by one atom, e.g. D homo steroids
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
- C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
- C12N9/14—Hydrolases (3)
- C12N9/48—Hydrolases (3) acting on peptide bonds (3.4)
- C12N9/50—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25)
- C12N9/503—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from viruses
- C12N9/506—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from viruses derived from RNA viruses
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2603/00—Systems containing at least three condensed rings
- C07C2603/02—Ortho- or ortho- and peri-condensed systems
- C07C2603/52—Ortho- or ortho- and peri-condensed systems containing five condensed rings
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
- C12N2740/00—Reverse transcribing RNA viruses
- C12N2740/00011—Details
- C12N2740/10011—Retroviridae
- C12N2740/16011—Human Immunodeficiency Virus, HIV
- C12N2740/16211—Human Immunodeficiency Virus, HIV concerning HIV gagpol
- C12N2740/16222—New viral proteins or individual genes, new structural or functional aspects of known viral proteins or genes
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Virology (AREA)
- Molecular Biology (AREA)
- Medicinal Chemistry (AREA)
- Zoology (AREA)
- Wood Science & Technology (AREA)
- Genetics & Genomics (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Biotechnology (AREA)
- General Engineering & Computer Science (AREA)
- Biochemistry (AREA)
- Microbiology (AREA)
- Biomedical Technology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Tropical Medicine & Parasitology (AREA)
- AIDS & HIV (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Steroid Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Peptides Or Proteins (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662291298P | 2016-02-04 | 2016-02-04 | |
| US62/291,298 | 2016-02-04 | ||
| PCT/IB2017/050568 WO2017134596A1 (en) | 2016-02-04 | 2017-02-02 | C-3 and c-17 modified triterpenoids as hiv-1 inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| KR20180105229A KR20180105229A (ko) | 2018-09-27 |
| KR102795662B1 true KR102795662B1 (ko) | 2025-04-14 |
Family
ID=57995251
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020187025343A Active KR102795662B1 (ko) | 2016-02-04 | 2017-02-02 | Hiv-1 억제제로서의 c-3 및 c-17 변형된 트리테르페노이드 |
Country Status (39)
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR107512A1 (es) * | 2016-02-04 | 2018-05-09 | VIIV HEALTHCARE UK Nº 5 LTD | Triterpenoides modificados en c-3 y c-17 como inhibidores del vih-1 |
| EP4321164A3 (en) | 2018-04-24 | 2024-04-17 | ViiV Healthcare UK (No.5) Limited | Compounds with hiv maturation inhibitory activity |
| MX2022006940A (es) | 2019-12-09 | 2022-07-11 | Viiv Healthcare Co | Composiciones farmaceuticas. |
| WO2025068743A1 (en) | 2023-09-27 | 2025-04-03 | ViiV Healthcare UK (No.3) Limited | Pharmaceutical composition of cabotegravir |
| WO2024089216A1 (en) | 2022-10-27 | 2024-05-02 | Syngenta Crop Protection Ag | Novel sulfur-containing heteroaryl carboxamide compounds |
| WO2025037232A1 (en) | 2023-08-11 | 2025-02-20 | ViiV Healthcare UK (No.4) Limited | Tosylate salt form of a maturation inhibitor for treatment of hiv |
| US20250099464A1 (en) | 2023-09-27 | 2025-03-27 | ViiV Healthcare UK (No.3) Limited | Pharmaceutical compositions |
Family Cites Families (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5413999A (en) | 1991-11-08 | 1995-05-09 | Merck & Co., Inc. | HIV protease inhibitors useful for the treatment of AIDS |
| US5679828A (en) | 1995-06-05 | 1997-10-21 | Biotech Research Labs, Inc. | Betulinic acid and dihydrobetulinic acid derivatives and uses therefor |
| US20040110785A1 (en) | 2001-02-02 | 2004-06-10 | Tao Wang | Composition and antiviral activity of substituted azaindoleoxoacetic piperazine derivatives |
| US7365221B2 (en) | 2002-09-26 | 2008-04-29 | Panacos Pharmaceuticals, Inc. | Monoacylated betulin and dihydrobetulin derivatives, preparation thereof and use thereof |
| GB0301227D0 (en) | 2003-01-20 | 2003-02-19 | Keen Group Ltd | Seating apparatus |
| US7745625B2 (en) | 2004-03-15 | 2010-06-29 | Bristol-Myers Squibb Company | Prodrugs of piperazine and substituted piperidine antiviral agents |
| MXPA06010592A (es) | 2004-03-17 | 2007-06-12 | Panacos Pharmaceuticals Inc | Sales farmaceuticas de acido 3-o-(3',3'-dimetilsuccinil) betulinico. |
| TW200628161A (en) | 2004-11-12 | 2006-08-16 | Panacos Pharmaceuticals Inc | Novel betulin derivatives, preparation thereof and use thereof |
| US20110144069A1 (en) | 2006-10-16 | 2011-06-16 | Myriad Genetics, Incorporated | Compounds for treating viral infections |
| EP2257567A1 (en) | 2008-02-14 | 2010-12-08 | Virochem Pharma Inc. | Novel 17 beta lupane derivatives |
| US9067966B2 (en) | 2009-07-14 | 2015-06-30 | Hetero Research Foundation, Hetero Drugs Ltd. | Lupeol-type triterpene derivatives as antivirals |
| FR2956034B1 (fr) | 2010-02-09 | 2012-02-10 | Thales Sa | Dispositif d'entrainement pour des joueurs de rugby |
| MX2012013628A (es) | 2010-06-04 | 2012-12-17 | Bristol Myers Squibb Co | Amidas c-28 de derivados del acido betulinico c-3 modificados como inhibidores de la maduracion del virus de inmunodeficiencia humana (vih). |
| CN103038245B (zh) | 2010-06-04 | 2015-03-25 | 百时美施贵宝公司 | 作为hiv成熟抑制剂的c-3经修饰的桦木酸衍生物 |
| DE102010017786A1 (de) | 2010-07-07 | 2012-01-12 | Continental Reifen Deutschland Gmbh | Elastomerprodukt, enthaltend ein linienförmiges, textiles Gebilde zur Verstärkung |
| US8846647B2 (en) | 2011-01-31 | 2014-09-30 | Bristol-Myers Squibb Company | C-17 and C-3 modified triterpenoids with HIV maturation inhibitory activity |
| RS54352B1 (sr) | 2011-01-31 | 2016-02-29 | Bristol-Myers Squibb Company | C-28 amini c-3 modifikovanih derivata betulinske kiseline kao inhibitori sazrevanja hiv-a |
| ES2584684T3 (es) * | 2011-12-14 | 2016-09-28 | Glaxosmithkline Llc | Derivados de propenoato de betulina |
| US8906889B2 (en) * | 2012-02-15 | 2014-12-09 | Bristol-Myers Squibb Company | C-3 cycloalkenyl triterpenoids with HIV maturation inhibitory activity |
| US8889854B2 (en) * | 2012-05-07 | 2014-11-18 | Bristol-Myers Squibb Company | C-17 bicyclic amines of triterpenoids with HIV maturation inhibitory activity |
| JP2016505000A (ja) | 2012-12-21 | 2016-02-18 | エピザイム，インコーポレイティド | Ｐｒｍｔ５阻害剤およびその使用 |
| US9378035B2 (en) | 2012-12-28 | 2016-06-28 | Commvault Systems, Inc. | Systems and methods for repurposing virtual machines |
| SG11201505639SA (en) * | 2013-02-06 | 2015-08-28 | Bristol Myers Squibb Co | C-19 modified triterpenoids with hiv maturation inhibitory activity |
| MX2015010354A (es) * | 2013-02-25 | 2015-10-09 | Squibb Bristol Myers Co | Derivados de acido betulinico modificados con aquilo c-3 y alquenilo utiles en el tratamiento de virus de inmunodeficiencia humana (vih). |
| CN104877015B (zh) * | 2014-02-28 | 2019-02-01 | 中国人民解放军军事医学科学院毒物药物研究所 | 一种三萜-多肽缀合物、其药物组合物及用途 |
| PL3129392T3 (pl) * | 2014-04-11 | 2021-04-06 | VIIV Healthcare UK(No.4) Limited | Triterpenoidy o aktywności hamującej dojrzewanie hiv, podstawione w pozycji 3 niearomatycznym pierścieniem zawierającym podstawnik fluorowcoalkilowy |
| MA40886B1 (fr) | 2015-02-09 | 2020-03-31 | Hetero Research Foundation | Nouveau triterpénone en c-3 avec des dérivés d'amide inverse en c-28 en tant qu'inhibiteurs du vih |
| AR107512A1 (es) * | 2016-02-04 | 2018-05-09 | VIIV HEALTHCARE UK Nº 5 LTD | Triterpenoides modificados en c-3 y c-17 como inhibidores del vih-1 |
| DK3984994T3 (da) | 2016-02-04 | 2024-10-14 | Takeda Pharmaceuticals Co | Substitueret piperidinforbindelse som orexin-type 2-agonist til behandling af narkolepsi |
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2017
- 2017-02-01 AR ARP170100255A patent/AR107512A1/es active IP Right Grant
- 2017-02-02 EP EP21152161.2A patent/EP3831839B1/en active Active
- 2017-02-02 RU RU2018130181A patent/RU2716502C2/ru active
- 2017-02-02 KR KR1020187025343A patent/KR102795662B1/ko active Active
- 2017-02-02 JO JOP/2017/0029A patent/JOP20170029B1/ar active
- 2017-02-02 PE PE2018001378A patent/PE20181355A1/es unknown
- 2017-02-02 SM SM20210210T patent/SMT202100210T1/it unknown
- 2017-02-02 BR BR112018015629-9A patent/BR112018015629B1/pt active IP Right Grant
- 2017-02-02 UA UAA201808249A patent/UA123867C2/uk unknown
- 2017-02-02 MX MX2018009514A patent/MX375118B/es active IP Right Grant
- 2017-02-02 HR HRP20210502TT patent/HRP20210502T1/hr unknown
- 2017-02-02 MD MDE20181181T patent/MD3411381T2/ro unknown
- 2017-02-02 MA MA053358A patent/MA53358A/fr unknown
- 2017-02-02 RS RS20210450A patent/RS61746B1/sr unknown
- 2017-02-02 JP JP2018540806A patent/JP6735837B2/ja active Active
- 2017-02-02 PL PL17704093T patent/PL3411381T3/pl unknown
- 2017-02-02 HU HUE17704093A patent/HUE054337T2/hu unknown
- 2017-02-02 WO PCT/IB2017/050568 patent/WO2017134596A1/en not_active Ceased
- 2017-02-02 CA CA3013417A patent/CA3013417C/en active Active
- 2017-02-02 EP EP17704093.8A patent/EP3411381B1/en active Active
- 2017-02-02 MY MYPI2018702694A patent/MY199668A/en unknown
- 2017-02-02 CN CN201780018790.8A patent/CN109153700B/zh active Active
- 2017-02-02 EA EA201891649A patent/EA036211B1/ru unknown
- 2017-02-02 UY UY0001037109A patent/UY37109A/es not_active Application Discontinuation
- 2017-02-02 PT PT177040938T patent/PT3411381T/pt unknown
- 2017-02-02 MA MA43960A patent/MA43960B1/fr unknown
- 2017-02-02 US US16/071,925 patent/US10421774B2/en active Active
- 2017-02-02 DK DK17704093.8T patent/DK3411381T3/da active
- 2017-02-02 ES ES21152161T patent/ES2957767T3/es active Active
- 2017-02-02 TW TW106103410A patent/TWI719126B/zh active
- 2017-02-02 CR CR20180387A patent/CR20180387A/es unknown
- 2017-02-02 ES ES17704093T patent/ES2862325T3/es active Active
- 2017-02-02 AU AU2017215529A patent/AU2017215529B2/en active Active
- 2017-02-02 LT LTEP17704093.8T patent/LT3411381T/lt unknown
- 2017-02-02 SG SG11201806388XA patent/SG11201806388XA/en unknown
- 2017-02-02 SI SI201730647T patent/SI3411381T1/sl unknown
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2018
- 2018-07-23 IL IL260741A patent/IL260741B/en active IP Right Grant
- 2018-07-26 ZA ZA2018/05044A patent/ZA201805044B/en unknown
- 2018-07-30 DO DO2018000174A patent/DOP2018000174A/es unknown
- 2018-07-31 CO CONC2018/0008157A patent/CO2018008157A2/es unknown
- 2018-08-02 CL CL2018002084A patent/CL2018002084A1/es unknown
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2019
- 2019-08-07 US US16/534,208 patent/US11084845B2/en active Active
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2021
- 2021-04-08 CY CY20211100303T patent/CY1124353T1/el unknown
- 2021-06-09 US US17/342,941 patent/US20210323997A1/en not_active Abandoned
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2022
- 2022-12-16 US US18/083,037 patent/US20230295220A1/en not_active Abandoned
Also Published As
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Patent event date: 20180831 Patent event code: PA01051R01D Comment text: International Patent Application |
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Comment text: Notification of reason for refusal Patent event date: 20240424 Patent event code: PE09021S01D |
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Patent event code: PE07011S01D Comment text: Decision to Grant Registration Patent event date: 20250213 |
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Comment text: Registration of Establishment Patent event date: 20250409 Patent event code: PR07011E01D |
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