MX364919B - Derivados triterpenoides. - Google Patents

Derivados triterpenoides.

Info

Publication number
MX364919B
MX364919B MX2018006429A MX2018006429A MX364919B MX 364919 B MX364919 B MX 364919B MX 2018006429 A MX2018006429 A MX 2018006429A MX 2018006429 A MX2018006429 A MX 2018006429A MX 364919 B MX364919 B MX 364919B
Authority
MX
Mexico
Prior art keywords
hif
triterpenoid
derivatives
vivo
activation
Prior art date
Application number
MX2018006429A
Other languages
English (en)
Other versions
MX2018006429A (es
Inventor
Muñoz Blanco Eduardo
Minassi Alberto
Luz Bellido Cabello De Alba María
Appendino Giovanni
Original Assignee
Vivacell Biotechnology Espana S L
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Vivacell Biotechnology Espana S L filed Critical Vivacell Biotechnology Espana S L
Publication of MX2018006429A publication Critical patent/MX2018006429A/es
Publication of MX364919B publication Critical patent/MX364919B/es

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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
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Diabetes (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (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).
MX2018006429A 2016-10-13 2017-10-03 Derivados triterpenoides. MX364919B (es)

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 MX2018006429A (es) 2018-09-27
MX364919B true 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 (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113710681A (zh) * 2019-01-30 2021-11-26 罗特哈姆斯泰德研究有限公司 从柳属植物中分离的用于癌症疗法的脱氢柳皮苷环二聚体及其衍生物
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
WO2024145502A1 (en) * 2022-12-29 2024-07-04 The Board Of Regents Of The University Of Texas System Synthetic triterpenoids and compositions thereof in weight management, skeletal muscle function, and appetite suppression

Family Cites Families (6)

* Cited by examiner, † Cited by third party
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
CA2711834C (en) * 2008-01-11 2017-03-14 Reata Pharmaceuticals, Inc. Synthetic triterpenoids and methods of use in the treatment of disease
TW201004627A (en) * 2008-04-18 2010-02-01 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

Also Published As

Publication number Publication date
CN108368150A (zh) 2018-08-03
RU2018136782A (ru) 2020-04-20
MX2018006429A (es) 2018-09-27
AU2017341257A1 (en) 2018-11-01
US20190367447A1 (en) 2019-12-05
HK1254200A1 (zh) 2019-07-12
CN108368150B (zh) 2022-02-25
MX2019005448A (es) 2019-07-04
EP3365351B1 (en) 2019-12-04
CA3020387A1 (en) 2018-04-19
KR20180117700A (ko) 2018-10-29
US10766855B2 (en) 2020-09-08
JP6598224B2 (ja) 2019-10-30
IL259391A (en) 2018-07-31
KR102038930B1 (ko) 2019-11-05
BR112018068996A2 (pt) 2019-01-22
JP2019519464A (ja) 2019-07-11
WO2018069086A1 (en) 2018-04-19
CA3020387C (en) 2020-07-28
EP3365351A1 (en) 2018-08-29
ES2774198T3 (es) 2020-07-17
AU2017341257B2 (en) 2019-08-08
RU2018136782A3 (es) 2020-04-20
IL259391B (en) 2019-10-31

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