MX375118B - Triterpenoides modificados en c-3 y c-17 como inhibidores del vih-1. - Google Patents
Triterpenoides modificados en c-3 y c-17 como inhibidores del vih-1.Info
- Publication number
- MX375118B MX375118B MX2018009514A MX2018009514A MX375118B MX 375118 B MX375118 B MX 375118B MX 2018009514 A MX2018009514 A MX 2018009514A MX 2018009514 A MX2018009514 A MX 2018009514A MX 375118 B MX375118 B MX 375118B
- Authority
- MX
- Mexico
- Prior art keywords
- hiv
- inhibitors
- compounds
- modified triterpenoids
- formula
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 241000713772 Human immunodeficiency virus 1 Species 0.000 title 1
- 150000003648 triterpenes Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- 208000030507 AIDS Diseases 0.000 abstract 1
- 230000000840 anti-viral effect Effects 0.000 abstract 1
- QGJZLNKBHJESQX-FZFNOLFKSA-N betulinic acid Chemical class C1C[C@H](O)C(C)(C)[C@@H]2CC[C@@]3(C)[C@]4(C)CC[C@@]5(C(O)=O)CC[C@@H](C(=C)C)[C@@H]5[C@H]4CC[C@@H]3[C@]21C QGJZLNKBHJESQX-FZFNOLFKSA-N 0.000 abstract 1
- 230000035800 maturation Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 230000000144 pharmacologic effect Effects 0.000 abstract 1
Classifications
-
- 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
-
- 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
-
- 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)
- Genetics & Genomics (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Wood Science & Technology (AREA)
- Zoology (AREA)
- Engineering & Computer Science (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Biomedical Technology (AREA)
- General Engineering & Computer Science (AREA)
- Biotechnology (AREA)
- Microbiology (AREA)
- Biochemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- AIDS & HIV (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Tropical Medicine & Parasitology (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)
Abstract
Se exponen compuestos que tienen propiedades farmacológicas y que afectan a la bioactividad, sus composiciones farmacéuticas y procedimientos de uso. En particular, se proporcionan derivados de ácido betulínico que poseen actividad antivírica única como inhibidores de la maduración del VIH, tal como se representa mediante los compuestos de fórmula I: (ver Fórmula). Estos compuestos son útiles para el tratamiento del VIH y del SIDA.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662291298P | 2016-02-04 | 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 |
|---|---|
| MX2018009514A MX2018009514A (es) | 2018-09-05 |
| MX375118B true MX375118B (es) | 2025-03-06 |
Family
ID=57995251
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2018009514A MX375118B (es) | 2016-02-04 | 2017-02-02 | Triterpenoides modificados en c-3 y c-17 como inhibidores del vih-1. |
Country Status (39)
| Country | Link |
|---|---|
| US (4) | US10421774B2 (es) |
| EP (2) | EP3831839B1 (es) |
| JP (1) | JP6735837B2 (es) |
| KR (1) | KR102795662B1 (es) |
| CN (1) | CN109153700B (es) |
| AR (1) | AR107512A1 (es) |
| AU (1) | AU2017215529B2 (es) |
| BR (1) | BR112018015629B1 (es) |
| CA (1) | CA3013417C (es) |
| CL (1) | CL2018002084A1 (es) |
| CO (1) | CO2018008157A2 (es) |
| CR (1) | CR20180387A (es) |
| CY (1) | CY1124353T1 (es) |
| DK (1) | DK3411381T3 (es) |
| DO (1) | DOP2018000174A (es) |
| EA (1) | EA036211B1 (es) |
| ES (2) | ES2957767T3 (es) |
| HR (1) | HRP20210502T1 (es) |
| HU (1) | HUE054337T2 (es) |
| IL (1) | IL260741B (es) |
| JO (1) | JOP20170029B1 (es) |
| LT (1) | LT3411381T (es) |
| MA (2) | MA53358A (es) |
| MD (1) | MD3411381T2 (es) |
| MX (1) | MX375118B (es) |
| MY (1) | MY199668A (es) |
| PE (1) | PE20181355A1 (es) |
| PL (1) | PL3411381T3 (es) |
| PT (1) | PT3411381T (es) |
| RS (1) | RS61746B1 (es) |
| RU (1) | RU2716502C2 (es) |
| SG (1) | SG11201806388XA (es) |
| SI (1) | SI3411381T1 (es) |
| SM (1) | SMT202100210T1 (es) |
| TW (1) | TWI719126B (es) |
| UA (1) | UA123867C2 (es) |
| UY (1) | UY37109A (es) |
| WO (1) | WO2017134596A1 (es) |
| ZA (1) | ZA201805044B (es) |
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 |
| JP7436385B2 (ja) * | 2018-04-24 | 2024-02-21 | ヴィーブ ヘルスケア ユーケー（ナンバー５）リミテッド | Ｈｉｖ成熟阻害活性を有する化合物 |
| IL293566A (en) | 2019-12-09 | 2022-08-01 | Viiv Healthcare Co | Pharmaceutical preparations containing Cabotgravir |
| 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 |
| WO2025068912A1 (en) | 2023-09-27 | 2025-04-03 | 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 |
| CA2560266A1 (en) | 2004-03-17 | 2005-09-29 | Panacos Pharmaceuticals, Inc. | Pharmaceutical salts of 3-o-(3',3'-dimethylsuccinyl) betulinic acid |
| 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 |
| CA2714049A1 (en) | 2008-02-14 | 2009-08-20 | 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 |
| HRP20150977T1 (hr) | 2010-06-04 | 2015-10-09 | Bristol-Myers Squibb Company | C-28 amidi modificiranih derivata c-3 betulinske kiseline kao inhibitori sazrijevanja hiv-a |
| 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 |
| JP6000283B2 (ja) | 2011-01-31 | 2016-09-28 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | Ｈｉｖ成熟阻害剤としてのｃ−３修飾ベツリン酸誘導体のｃ−２８アミン |
| US8846647B2 (en) * | 2011-01-31 | 2014-09-30 | Bristol-Myers Squibb Company | C-17 and C-3 modified triterpenoids with HIV maturation inhibitory activity |
| JP6091520B2 (ja) * | 2011-12-14 | 2017-03-08 | グラクソスミスクライン エルエルシー | ベツリンのプロペン酸誘導体 |
| 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 |
| JP6186010B2 (ja) * | 2013-02-06 | 2017-08-23 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | Ｈｉｖ成熟阻害活性を有するｃ−１９修飾トリテルペノイド類 |
| SG11201506445PA (en) | 2013-02-25 | 2015-09-29 | Bristol Myers Squibb Co | C-3 alkyl and alkenyl modified betulinic acid derivatives useful in the treatment of hiv |
| 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 |
| UY36070A (es) | 2014-04-11 | 2015-10-30 | Bristol Myers Squibb Company Una Corporación Del Estado De Delaware | Triterpenoides con actividad inhibidora de la maduración de hiv |
| 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 |
| US10508083B2 (en) | 2016-02-04 | 2019-12-17 | Takeda Pharmaceutical Company Limited | Substituted piperidine compound and use thereof |
| 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 |
-
2017
- 2017-02-01 AR ARP170100255A patent/AR107512A1/es active IP Right Grant
- 2017-02-02 PL PL17704093T patent/PL3411381T3/pl unknown
- 2017-02-02 AU AU2017215529A patent/AU2017215529B2/en active Active
- 2017-02-02 RS RS20210450A patent/RS61746B1/sr unknown
- 2017-02-02 RU RU2018130181A patent/RU2716502C2/ru active
- 2017-02-02 SM SM20210210T patent/SMT202100210T1/it unknown
- 2017-02-02 LT LTEP17704093.8T patent/LT3411381T/lt unknown
- 2017-02-02 CR CR20180387A patent/CR20180387A/es unknown
- 2017-02-02 KR KR1020187025343A patent/KR102795662B1/ko active Active
- 2017-02-02 HU HUE17704093A patent/HUE054337T2/hu unknown
- 2017-02-02 HR HRP20210502TT patent/HRP20210502T1/hr unknown
- 2017-02-02 ES ES21152161T patent/ES2957767T3/es active Active
- 2017-02-02 CA CA3013417A patent/CA3013417C/en active Active
- 2017-02-02 TW TW106103410A patent/TWI719126B/zh active
- 2017-02-02 ES ES17704093T patent/ES2862325T3/es active Active
- 2017-02-02 EP EP21152161.2A patent/EP3831839B1/en active Active
- 2017-02-02 MX MX2018009514A patent/MX375118B/es active IP Right Grant
- 2017-02-02 PE PE2018001378A patent/PE20181355A1/es unknown
- 2017-02-02 JP JP2018540806A patent/JP6735837B2/ja active Active
- 2017-02-02 BR BR112018015629-9A patent/BR112018015629B1/pt active IP Right Grant
- 2017-02-02 WO PCT/IB2017/050568 patent/WO2017134596A1/en not_active Ceased
- 2017-02-02 MY MYPI2018702694A patent/MY199668A/en unknown
- 2017-02-02 SI SI201730647T patent/SI3411381T1/sl unknown
- 2017-02-02 SG SG11201806388XA patent/SG11201806388XA/en unknown
- 2017-02-02 PT PT177040938T patent/PT3411381T/pt unknown
- 2017-02-02 EP EP17704093.8A patent/EP3411381B1/en active Active
- 2017-02-02 DK DK17704093.8T patent/DK3411381T3/da active
- 2017-02-02 MA MA053358A patent/MA53358A/fr unknown
- 2017-02-02 MA MA43960A patent/MA43960B1/fr unknown
- 2017-02-02 MD MDE20181181T patent/MD3411381T2/ro unknown
- 2017-02-02 JO JOP/2017/0029A patent/JOP20170029B1/ar active
- 2017-02-02 CN CN201780018790.8A patent/CN109153700B/zh active Active
- 2017-02-02 US US16/071,925 patent/US10421774B2/en 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 UA UAA201808249A patent/UA123867C2/uk unknown
-
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
-
2019
- 2019-08-07 US US16/534,208 patent/US11084845B2/en active Active
-
2021
- 2021-04-08 CY CY20211100303T patent/CY1124353T1/el unknown
- 2021-06-09 US US17/342,941 patent/US20210323997A1/en not_active Abandoned
-
2022
- 2022-12-16 US US18/083,037 patent/US20230295220A1/en not_active Abandoned
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