MX2018006429A - Derivados triterpenoides. - Google Patents
Derivados triterpenoides.Info
- Publication number
- MX2018006429A MX2018006429A MX2018006429A MX2018006429A MX2018006429A MX 2018006429 A MX2018006429 A MX 2018006429A MX 2018006429 A MX2018006429 A MX 2018006429A MX 2018006429 A MX2018006429 A MX 2018006429A MX 2018006429 A MX2018006429 A MX 2018006429A
- Authority
- MX
- Mexico
- Prior art keywords
- hif
- triterpenoid
- derivatives
- vivo
- activation
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C259/00—Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups
- C07C259/04—Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups without replacement of the other oxygen atom of the carboxyl group, e.g. hydroxamic acids
- C07C259/08—Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups without replacement of the other oxygen atom of the carboxyl group, e.g. hydroxamic acids having carbon atoms of hydroxamic groups bound to carbon atoms of rings other than six-membered aromatic rings
-
- 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
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- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- 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
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/12—Antidiuretics, e.g. drugs for diabetes insipidus
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
- C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
- C07D261/20—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings condensed with carbocyclic rings or ring systems
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Diabetes (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Urology & Nephrology (AREA)
- Immunology (AREA)
- Vascular Medicine (AREA)
- Endocrinology (AREA)
- Transplantation (AREA)
- Emergency Medicine (AREA)
- Dermatology (AREA)
- Pulmonology (AREA)
- Steroid Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Se describen derivados triterpenoides y composiciones que comprenden dichos derivados triterpenoides de Fórmula (I), donde R=-C(O)NHOH. Dichos triterpenoides y composiciones muestran capacidad de unión a PHD2, estabilizan las proteínas HIF-1a y HIF-2a, activan la ruta HIF en diferentes tipos celulares, inducen angiogénesis en células vasculares endoteliales humanas, muestran actividad neuroprotectora in vitro e in vivo, actividad antidiabética y reducen los niveles de lípidos in vivo, y aumentan los niveles en plasma de eritropoyetina in vivo. Los derivados triterpenoides descritos actúan también de forma selectiva y no inducen activación de Nrf2, inhibición de NF-?B, inhibición de STAT3, y activación de TGR5, que son actividades conocidas de precursores triterpenoides naturales. Dichos derivados triterpenoides son útiles en el tratamiento de afecciones y enfermedades que responden a la activación de HIF tales como apoplejía, parálisis cerebral, lesiones traumáticas y enfermedades neurodegenerativas; y también IBD, lesión miocárdica por isquemia-reperfusión, lesión pulmonar aguda, heridas diabéticas y crónicas, trasplante de órganos, lesión renal aguda o enfermedades arteriales. (ver Fórmula I).
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP16193684 | 2016-10-13 | ||
| PCT/EP2017/075042 WO2018069086A1 (en) | 2016-10-13 | 2017-10-03 | Hydroxamate triterpenoid derivatives |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| MX2018006429A true MX2018006429A (es) | 2018-09-27 |
| MX364919B MX364919B (es) | 2019-05-13 |
Family
ID=57136723
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2018006429A MX364919B (es) | 2016-10-13 | 2017-10-03 | Derivados triterpenoides. |
| MX2019005448A MX2019005448A (es) | 2016-10-13 | 2018-05-24 | Derivados triterpenoides. |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2019005448A MX2019005448A (es) | 2016-10-13 | 2018-05-24 | Derivados triterpenoides. |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US10766855B2 (es) |
| EP (1) | EP3365351B1 (es) |
| JP (1) | JP6598224B2 (es) |
| KR (1) | KR102038930B1 (es) |
| CN (1) | CN108368150B (es) |
| AU (1) | AU2017341257B2 (es) |
| BR (1) | BR112018068996A2 (es) |
| CA (1) | CA3020387C (es) |
| ES (1) | ES2774198T3 (es) |
| HK (1) | HK1254200A1 (es) |
| IL (1) | IL259391B (es) |
| MX (2) | MX364919B (es) |
| RU (1) | RU2018136782A (es) |
| WO (1) | WO2018069086A1 (es) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB2581035B (en) * | 2019-01-30 | 2021-08-04 | Rothamsted Res Ltd | Novel compounds and their use in therapy |
| CN114805469A (zh) * | 2021-01-27 | 2022-07-29 | 中国科学院上海药物研究所 | 含吡唑的白桦脂酸类衍生物，其制备方法及用途 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101367861A (zh) * | 2007-08-15 | 2009-02-18 | 中国药科大学 | 2-羟基-3-脱氧五环三萜类化合物及其衍生物、其制备方法及用途 |
| ES2718047T3 (es) * | 2008-01-11 | 2019-06-27 | Reata Pharmaceuticals Inc | Triterpenoides sintéticos y métodos de uso en el tratamiento de la enfermedad |
| WO2009146216A2 (en) * | 2008-04-18 | 2009-12-03 | Reata Pharmaceuticals. Inc. | Antioxidant inflammation modulators: novel derivatives of oleanolic acid |
| CN102180939B (zh) | 2011-03-30 | 2013-02-20 | 沈阳化工大学 | 一种抗肿瘤活性的熊果酸化学修饰物及其制备方法 |
| US8324264B1 (en) * | 2011-07-22 | 2012-12-04 | Sequoia Sciences, Inc. | Inhibitors of bacterial biofilms and related methods |
| CN102499925B (zh) * | 2011-10-21 | 2015-11-11 | 上海中医药大学 | 一种中性粒细胞弹性蛋白酶抑制剂 |
-
2017
- 2017-10-03 BR BR112018068996A patent/BR112018068996A2/pt not_active Application Discontinuation
- 2017-10-03 CA CA3020387A patent/CA3020387C/en active Active
- 2017-10-03 CN CN201780004882.0A patent/CN108368150B/zh active Active
- 2017-10-03 JP JP2018524188A patent/JP6598224B2/ja active Active
- 2017-10-03 US US16/099,800 patent/US10766855B2/en active Active
- 2017-10-03 WO PCT/EP2017/075042 patent/WO2018069086A1/en active Application Filing
- 2017-10-03 ES ES17790966T patent/ES2774198T3/es active Active
- 2017-10-03 MX MX2018006429A patent/MX364919B/es active IP Right Grant
- 2017-10-03 KR KR1020187028923A patent/KR102038930B1/ko active IP Right Grant
- 2017-10-03 AU AU2017341257A patent/AU2017341257B2/en active Active
- 2017-10-03 RU RU2018136782A patent/RU2018136782A/ru not_active Application Discontinuation
- 2017-10-03 EP EP17790966.0A patent/EP3365351B1/en active Active
-
2018
- 2018-05-15 IL IL25939118A patent/IL259391B/en active IP Right Grant
- 2018-05-24 MX MX2019005448A patent/MX2019005448A/es unknown
- 2018-10-18 HK HK18113340.0A patent/HK1254200A1/zh unknown
Also Published As
| Publication number | Publication date |
|---|---|
| JP2019519464A (ja) | 2019-07-11 |
| US10766855B2 (en) | 2020-09-08 |
| BR112018068996A2 (pt) | 2019-01-22 |
| MX364919B (es) | 2019-05-13 |
| EP3365351A1 (en) | 2018-08-29 |
| WO2018069086A1 (en) | 2018-04-19 |
| US20190367447A1 (en) | 2019-12-05 |
| KR20180117700A (ko) | 2018-10-29 |
| RU2018136782A (ru) | 2020-04-20 |
| IL259391B (en) | 2019-10-31 |
| AU2017341257A1 (en) | 2018-11-01 |
| KR102038930B1 (ko) | 2019-11-05 |
| EP3365351B1 (en) | 2019-12-04 |
| HK1254200A1 (zh) | 2019-07-12 |
| RU2018136782A3 (es) | 2020-04-20 |
| MX2019005448A (es) | 2019-07-04 |
| JP6598224B2 (ja) | 2019-10-30 |
| CA3020387A1 (en) | 2018-04-19 |
| AU2017341257B2 (en) | 2019-08-08 |
| CA3020387C (en) | 2020-07-28 |
| CN108368150B (zh) | 2022-02-25 |
| ES2774198T3 (es) | 2020-07-17 |
| CN108368150A (zh) | 2018-08-03 |
| IL259391A (en) | 2018-07-31 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant or registration |