MX2012013703A - Derivados de acido c-3-betulinico modificados como inhibidores de la maduracion del virus de inmunodeficiencia humana (vih). - Google Patents
Derivados de acido c-3-betulinico modificados como inhibidores de la maduracion del virus de inmunodeficiencia humana (vih).Info
- Publication number
- MX2012013703A MX2012013703A MX2012013703A MX2012013703A MX2012013703A MX 2012013703 A MX2012013703 A MX 2012013703A MX 2012013703 A MX2012013703 A MX 2012013703A MX 2012013703 A MX2012013703 A MX 2012013703A MX 2012013703 A MX2012013703 A MX 2012013703A
- Authority
- MX
- Mexico
- Prior art keywords
- modified
- betulinic acid
- maturation inhibitors
- acid derivatives
- hiv maturation
- Prior art date
Links
- 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 title abstract 2
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 230000035800 maturation Effects 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- QGJZLNKBHJESQX-UHFFFAOYSA-N 3-Epi-Betulin-Saeure Natural products C1CC(O)C(C)(C)C2CCC3(C)C4(C)CCC5(C(O)=O)CCC(C(=C)C)C5C4CCC3C21C QGJZLNKBHJESQX-UHFFFAOYSA-N 0.000 abstract 1
- CLOUCVRNYSHRCF-UHFFFAOYSA-N 3beta-Hydroxy-20(29)-Lupen-3,27-oic acid Natural products C1CC(O)C(C)(C)C2CCC3(C)C4(C(O)=O)CCC5(C)CCC(C(=C)C)C5C4CCC3C21C CLOUCVRNYSHRCF-UHFFFAOYSA-N 0.000 abstract 1
- 208000030507 AIDS Diseases 0.000 abstract 1
- DIZWSDNSTNAYHK-XGWVBXMLSA-N Betulinic acid Natural products CC(=C)[C@@H]1C[C@H]([C@H]2CC[C@]3(C)[C@H](CC[C@@H]4[C@@]5(C)CC[C@H](O)C(C)(C)[C@@H]5CC[C@@]34C)[C@@H]12)C(=O)O DIZWSDNSTNAYHK-XGWVBXMLSA-N 0.000 abstract 1
- 230000000840 anti-viral effect Effects 0.000 abstract 1
- PZXJOHSZQAEJFE-UHFFFAOYSA-N dihydrobetulinic acid Natural products C1CC(O)C(C)(C)C2CCC3(C)C4(C)CCC5(C(O)=O)CCC(C(C)C)C5C4CCC3C21C PZXJOHSZQAEJFE-UHFFFAOYSA-N 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- 229930014626 natural product Natural products 0.000 abstract 1
- MQYXUWHLBZFQQO-UHFFFAOYSA-N nepehinol Natural products C1CC(O)C(C)(C)C2CCC3(C)C4(C)CCC5(C)CCC(C(=C)C)C5C4CCC3C21C MQYXUWHLBZFQQO-UHFFFAOYSA-N 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
Classifications
-
- 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
-
- 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
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Virology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Immunology (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
- Molecular Biology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Se definen compuestos que tienen propiedades farmacológicas y bioafección, sus composiciones farmacéuticas y métodos de uso. En particular, ácido C3-betulínico modificado y otros derivados de productos naturales relacionados estructuralmente que poseen una actividad antiviral única se proporcionan como inhibidores de la maduración del VIH. Estos compuestos son útiles para el tratamiento del VIH y el SIDA.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US35133810P | 2010-06-04 | 2010-06-04 | |
| PCT/US2011/038879 WO2011153315A1 (en) | 2010-06-04 | 2011-06-02 | Modified c-3 betulinic acid derivatives as hiv maturation inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MX2012013703A true MX2012013703A (es) | 2012-12-17 |
Family
ID=44627236
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2012013703A MX2012013703A (es) | 2010-06-04 | 2011-06-02 | Derivados de acido c-3-betulinico modificados como inhibidores de la maduracion del virus de inmunodeficiencia humana (vih). |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US8754068B2 (es) |
| EP (1) | EP2576585B8 (es) |
| JP (1) | JP5752789B2 (es) |
| CN (1) | CN103038245B (es) |
| AR (1) | AR081637A1 (es) |
| BR (1) | BR112012030818A2 (es) |
| CA (1) | CA2801487C (es) |
| EA (1) | EA022393B1 (es) |
| ES (1) | ES2612452T3 (es) |
| MX (1) | MX2012013703A (es) |
| TW (1) | TW201201793A (es) |
| WO (1) | WO2011153315A1 (es) |
Families Citing this family (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2012106190A1 (en) * | 2011-01-31 | 2012-08-09 | Bristol-Myers Squibb Company | C-17 and c-3 modified triterpenoids with hiv maturation inhibitory activity |
| US11090313B2 (en) | 2010-05-20 | 2021-08-17 | University Of Iowa Research Foundation | Methods for inhibiting muscle atrophy |
| EP2571354B1 (en) | 2010-05-20 | 2020-07-08 | University of Iowa Research Foundation | Ursolic acid for inhibiting muscle atrophy |
| HRP20151212T1 (hr) * | 2011-01-31 | 2015-12-04 | Bristol-Myers Squibb Company | C-28 AMINI C-3 MODIFICIRANIH DERIVATA BETULINSKE KISELINE KAO INHIBITORI SAZRIJEVANJA HIV-a P |
| CN106822153B (zh) | 2011-06-06 | 2019-12-17 | 爱荷华大学研究基金会 | 用于抑制肌萎缩的方法 |
| EP2758419B8 (en) | 2011-09-21 | 2017-04-19 | VIIV Healthcare UK (No.5) Limited | Novel betulinic acid derivatives with antiviral activity |
| 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 |
| US9637516B2 (en) | 2012-12-31 | 2017-05-02 | Hetero Research Foundation | Betulinic acid proline derivatives as HIV inhibitors |
| EA027371B1 (ru) * | 2013-02-06 | 2017-07-31 | Бристол-Майерс Сквибб Компани | C-19 модифицированные тритерпеноиды с ингибиторной активностью созревания вич |
| BR112015019590A2 (pt) * | 2013-02-25 | 2017-07-18 | Bristol Myers Squibb Co | derivados de ácido betulínico modificado com c-3 alquila e alquenila úteis no tratamento de hiv |
| MX374543B (es) | 2014-04-11 | 2025-03-06 | Viiv Healthcare Uk No 4 Ltd | Triterpenoides con actividad inhibidora de la maduración del virus de inmunodeficiencia humana, sustituidos en la posición 3 con un anillo no aromático que lleva un sustituyente haloalquilo. |
| US9920090B2 (en) | 2014-06-19 | 2018-03-20 | VIIV Healthcare UK (No.5) Limited | Betulinic acid derivatives with HIV maturation inhibitory activity |
| US20170129916A1 (en) | 2014-06-26 | 2017-05-11 | Hetero Research Foundation | Novel betulinic proline imidazole derivatives as hiv inhibitors |
| AU2015346303B2 (en) * | 2014-11-14 | 2018-03-15 | VIIV Healthcare UK (No.5) Limited | Oxolupene derivatives |
| RU2017118576A (ru) | 2014-11-14 | 2018-12-14 | ВАЙВ ХЕЛТКЕР ЮКей (N5) ЛИМИТЕД | C-17-арил-замещённые аналоги бетулиновой кислоты |
| US9914747B2 (en) | 2014-11-14 | 2018-03-13 | VIIV Healthcare UK (No.5) Limited | Extended betulinic acid analogs |
| 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 |
| WO2016147099A2 (en) | 2015-03-16 | 2016-09-22 | Hetero Research Foundation | C-3 novel triterpenone with c-28 amide derivatives as hiv inhibitors |
| KR20180028534A (ko) | 2015-07-28 | 2018-03-16 | 글락소스미스클라인 인털렉츄얼 프로퍼티 (넘버 2) 리미티드 | Hiv 감염을 예방하거나 치료하기 위한 베투인 유도체 |
| RU2018105352A (ru) | 2015-07-28 | 2019-08-29 | ГлаксоСмитКлайн Интеллекчуал Проперти (N2) Лимитед | Производные бетулина для предупреждения или лечения ВИЧ-инфекций |
| RU2018112958A (ru) | 2015-09-24 | 2019-10-28 | ГлаксоСмитКлайн Интеллекчуал Проперти (N2) Лимитед | Соединения с ингибирующей созревание ВИЧ активностью |
| CN108699103A (zh) | 2016-01-20 | 2018-10-23 | 葛兰素史克知识产权第二有限公司 | 具有hiv成熟抑制活性的羽扇烷类的胺衍生物 |
| 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 |
| EP3478703A1 (en) * | 2016-06-30 | 2019-05-08 | ViiV Healthcare UK (No.5) Limited | Triterpenoid inhibitors of human immunodeficiency virus replication |
| WO2018002847A1 (en) | 2016-06-30 | 2018-01-04 | VIIV Healthcare UK (No.5) Limited | Aza-substituted inhibitors of human immunodeficiency virus replication |
| EP3478662B1 (en) | 2016-06-30 | 2020-09-16 | ViiV Healthcare UK (No.5) Limited | Azadecalin derivatives as inhibitors of human immunodeficiency virus replication |
| 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 |
| PL237998B1 (pl) | 2018-05-28 | 2021-06-28 | Narodowy Inst Lekow | Fosfonowe pochodne kwasu 3-karboksyacylobetulinowego, sposób ich otrzymywania oraz ich zastosowanie |
Family Cites Families (23)
| 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 |
| US5869535A (en) | 1995-03-21 | 1999-02-09 | The Board Of Trustees Of The University Of Illinois | Method and composition for selectively inhibiting melanoma |
| US5962527A (en) | 1995-03-21 | 1999-10-05 | The Board Of Trustees Of The University Of Illinois | Method and composition for treating cancers |
| US5679828A (en) | 1995-06-05 | 1997-10-21 | Biotech Research Labs, Inc. | Betulinic acid and dihydrobetulinic acid derivatives and uses therefor |
| NZ506623A (en) * | 1998-03-02 | 2002-10-25 | Univ North Carolina | Acylated betulin and dihydrobetulin derivatives, preparation thereof and use in treatment of retroviral infections |
| US20040110785A1 (en) | 2001-02-02 | 2004-06-10 | Tao Wang | Composition and antiviral activity of substituted azaindoleoxoacetic piperazine derivatives |
| WO2004028455A2 (en) * | 2002-09-26 | 2004-04-08 | Panacos Pharmaceuticals, Inc. | Monoacylated betulin and dihydrobetulin derivatives, preparation thereof and use thereof |
| US7365221B2 (en) | 2002-09-26 | 2008-04-29 | Panacos Pharmaceuticals, Inc. | Monoacylated betulin and dihydrobetulin derivatives, preparation thereof and use thereof |
| EP1594885B8 (de) * | 2003-02-11 | 2009-03-25 | Novelix Pharmaceuticals, Inc. | Medikament zur wachstumsinhibierung von tumoren |
| US20050014730A1 (en) | 2003-04-02 | 2005-01-20 | Carlson Robert M. | Anti-fungal formulation of triterpene and essential oil |
| US7745625B2 (en) | 2004-03-15 | 2010-06-29 | Bristol-Myers Squibb Company | Prodrugs of piperazine and substituted piperidine antiviral agents |
| EP1730163A4 (en) * | 2004-03-17 | 2009-12-30 | Panacos Pharmaceuticals Inc | Pharmaceutical salts of 3-O- (3,3-dimethylsuccinyl) betulinic acid |
| WO2005112929A2 (en) * | 2004-05-20 | 2005-12-01 | Cornell Research Foundation, Inc. | Anti-hiv-1 activity of betulinol derivatives |
| TW200628161A (en) * | 2004-11-12 | 2006-08-16 | Panacos Pharmaceuticals Inc | Novel betulin derivatives, preparation thereof and use thereof |
| JP2009527563A (ja) * | 2006-02-21 | 2009-07-30 | アキリオン ファーマシューティカルズ,インコーポレーテッド | ウイルス感染症を治療するのに有用な置換タラキサスタン |
| WO2008127364A2 (en) | 2006-10-13 | 2008-10-23 | Myriad Genetics, Inc. | Antiviral compounds and use thereof |
| WO2008115281A2 (en) * | 2006-10-16 | 2008-09-25 | Myriad Genetics, Inc. | Compounds for treating viral infections |
| WO2009020732A1 (en) * | 2007-08-03 | 2009-02-12 | Advanced Life Sciences, Inc. | Lupane-type triterpenoids modified at 30-position and analogues thereof |
| WO2009042166A1 (en) | 2007-09-25 | 2009-04-02 | Panacos Pharmaceuticals, Inc. | Liquid bevirimat dosage forms for oral administration |
| JP2011511812A (ja) | 2008-02-14 | 2011-04-14 | バイロケム ファーマ インコーポレイテッド | 新規17βルパン誘導体 |
| WO2009114083A2 (en) | 2008-03-03 | 2009-09-17 | Panacos Pharmaceuticals, Inc. | Determinants of antiviral response |
| HUE033288T2 (en) * | 2008-04-18 | 2017-11-28 | Reata Pharmaceuticals Inc | Antioxidant inflammation modulators: C-17 homologated oleic acid derivatives |
| SG182769A1 (en) * | 2010-02-11 | 2012-09-27 | Glaxosmithkline Llc | Derivatives of betulin |
-
2011
- 2011-06-02 CA CA2801487A patent/CA2801487C/en not_active Expired - Fee Related
- 2011-06-02 CN CN201180038211.9A patent/CN103038245B/zh not_active Expired - Fee Related
- 2011-06-02 US US13/151,706 patent/US8754068B2/en not_active Expired - Fee Related
- 2011-06-02 EA EA201270780A patent/EA022393B1/ru not_active IP Right Cessation
- 2011-06-02 WO PCT/US2011/038879 patent/WO2011153315A1/en not_active Ceased
- 2011-06-02 BR BR112012030818A patent/BR112012030818A2/pt not_active IP Right Cessation
- 2011-06-02 EP EP11726563.7A patent/EP2576585B8/en not_active Not-in-force
- 2011-06-02 MX MX2012013703A patent/MX2012013703A/es active IP Right Grant
- 2011-06-02 ES ES11726563.7T patent/ES2612452T3/es active Active
- 2011-06-02 JP JP2013513339A patent/JP5752789B2/ja not_active Expired - Fee Related
- 2011-06-03 TW TW100119644A patent/TW201201793A/zh unknown
- 2011-06-03 AR ARP110101944A patent/AR081637A1/es not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| EP2576585B1 (en) | 2016-10-12 |
| WO2011153315A1 (en) | 2011-12-08 |
| JP5752789B2 (ja) | 2015-07-22 |
| EA022393B1 (ru) | 2015-12-30 |
| CA2801487C (en) | 2017-12-05 |
| EA201270780A1 (ru) | 2013-04-30 |
| JP2013527242A (ja) | 2013-06-27 |
| CA2801487A1 (en) | 2011-12-08 |
| TW201201793A (en) | 2012-01-16 |
| CN103038245B (zh) | 2015-03-25 |
| BR112012030818A2 (pt) | 2019-09-24 |
| US8754068B2 (en) | 2014-06-17 |
| ES2612452T3 (es) | 2017-05-17 |
| EP2576585B8 (en) | 2016-12-21 |
| CN103038245A (zh) | 2013-04-10 |
| EP2576585A1 (en) | 2013-04-10 |
| AR081637A1 (es) | 2012-10-10 |
| US20120142707A1 (en) | 2012-06-07 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant or registration |