BR112021022431A2 - Moduladores de molécula pequena de metabolismo bacteriano intestinal do ácido biliar - Google Patents

Moduladores de molécula pequena de metabolismo bacteriano intestinal do ácido biliar

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Publication number
BR112021022431A2
BR112021022431A2 BR112021022431A BR112021022431A BR112021022431A2 BR 112021022431 A2 BR112021022431 A2 BR 112021022431A2 BR 112021022431 A BR112021022431 A BR 112021022431A BR 112021022431 A BR112021022431 A BR 112021022431A BR 112021022431 A2 BR112021022431 A2 BR 112021022431A2
Authority
BR
Brazil
Prior art keywords
disease
hepatitis
cancer
liver
small molecule
Prior art date
Application number
BR112021022431A
Other languages
English (en)
Inventor
Sloan Devlin Abigail
Arijit Adhikari
Original Assignee
Harvard College
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 Harvard College filed Critical Harvard College
Publication of BR112021022431A2 publication Critical patent/BR112021022431A2/pt

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J31/00—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
    • C07J31/006—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring not covered by C07J31/003
    • 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
    • A61K31/575—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
    • 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
    • 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
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0005—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring the nitrogen atom being directly linked to the cyclopenta(a)hydro phenanthrene skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0005—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring the nitrogen atom being directly linked to the cyclopenta(a)hydro phenanthrene skeleton
    • C07J41/0027—Azides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/005—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the 17-beta position being substituted by an uninterrupted chain of only two carbon atoms, e.g. pregnane derivatives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0055—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the 17-beta position being substituted by an uninterrupted chain of at least three carbon atoms which may or may not be branched, e.g. cholane or cholestane derivatives, optionally cyclised, e.g. 17-beta-phenyl or 17-beta-furyl derivatives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0094—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 containing nitrile radicals, including thiocyanide radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J9/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J9/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
    • C07J9/005—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane containing a carboxylic function directly attached or attached by a chain containing only carbon atoms to the cyclopenta[a]hydrophenanthrene skeleton

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Toxicology (AREA)
  • Pain & Pain Management (AREA)
  • Child & Adolescent Psychology (AREA)
  • Rheumatology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Epidemiology (AREA)
  • Communicable Diseases (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)

Abstract

moduladores de molécula pequena de metabolismo bacteriano intestinal do ácido biliar. são descritos aqui métodos e composições relacionados à inibição de hidrolase do sal biliar (bsh) e usos da mesma. é fornecido neste documento um método para tratamento de uma desordem metabólica (por exemplo, diabete, obesidade), doença gastrointestinal (por exemplo, uma infecção gastrointestinal, doença inflamatória intestinal (ibd), apendicite, doença de crohn (cd), colite ulcerativa (uc), gastrite, enterite, esofagite, pancreatite, diabetes, hepatite, doenças do fígado (por exemplo, doença esteatótica não alcoólica do fígado (nafld), esteato-hepatite não alcoólica (nash), hepatite a, hepatite b, hepatite c, hepatite autoimune, e cirrose do fígado) doença de refluxo gastroesofágico (gerd), doença celíaca, diverticulite, intolerância alimentar, úlcera, colite infecciosa, síndrome do intestino irritável, intestino permeável, e câncer), câncer (por exemplo, câncer do sistema digestivo, câncer de fígado), ou uma doença inflamatória (por exemplo, doença de crohn, doença inflamatória intestinal, colite ulcerativa, pancreatite, hepatite, apendicite, gastrite, diverticulite, doença celíaca, intolerância alimentar, enterite, úlcera, doença de refluxo gastroesofágico (gerd), artrite psoriática, psoríase e artrite reumatoide) em um indivíduo em necessidade do mesmo, compreendendo a administração a um indivíduo de um composto de fórmulas (i)-(xviii).
BR112021022431A 2019-05-10 2020-05-08 Moduladores de molécula pequena de metabolismo bacteriano intestinal do ácido biliar BR112021022431A2 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962846457P 2019-05-10 2019-05-10
US202062962048P 2020-01-16 2020-01-16
PCT/US2020/032016 WO2020231776A1 (en) 2019-05-10 2020-05-08 Small molecule modulators of gut bacterial bile acid metabolism

Publications (1)

Publication Number Publication Date
BR112021022431A2 true BR112021022431A2 (pt) 2022-05-24

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BR112021022431A BR112021022431A2 (pt) 2019-05-10 2020-05-08 Moduladores de molécula pequena de metabolismo bacteriano intestinal do ácido biliar

Country Status (9)

Country Link
US (1) US20220204548A1 (pt)
EP (1) EP3965748A4 (pt)
JP (1) JP2022533069A (pt)
KR (1) KR20220007112A (pt)
CN (1) CN114641280A (pt)
AU (1) AU2020274319A1 (pt)
BR (1) BR112021022431A2 (pt)
CA (1) CA3137308A1 (pt)
WO (1) WO2020231776A1 (pt)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20230107927A1 (en) 2020-02-28 2023-04-06 First Wave Bio, Inc. Methods of treating iatrogenic autoimmune colitis
IT202200008861A1 (it) * 2022-05-03 2023-11-03 Chemelectiva S R L Processo per la preparazione di derivati dell’acido colico.
CN115337312A (zh) * 2022-08-19 2022-11-15 金熊药业(珠海横琴)有限公司 胆酸复合物及其制备方法和应用
CN117801047A (zh) * 2023-01-19 2024-04-02 北京华睿鼎信科技有限公司 神经甾体衍生物及其用途

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20140206657A1 (en) * 2013-01-18 2014-07-24 City Of Hope Bile acid analog tgr5 agonists
CN107531743B (zh) * 2015-04-29 2020-05-05 正大天晴药业集团股份有限公司 鹅去氧胆酸衍生物
TWI618714B (zh) * 2015-08-27 2018-03-21 中央研究院 涎酸轉移酶抑制劑及其用途
US20200262865A1 (en) * 2016-02-15 2020-08-20 Alexander Khoruts Compositions and methods for treating clostridium associated diseases
US20170233431A1 (en) * 2016-02-17 2017-08-17 City Of Hope Bile acid derivatives and methods for synthesis and use
CA3077429A1 (en) * 2017-10-13 2019-04-18 Battelle Memorial Institute Bile salt hydrolase probe and method of making and using the same

Also Published As

Publication number Publication date
EP3965748A4 (en) 2023-02-01
WO2020231776A8 (en) 2021-05-14
AU2020274319A1 (en) 2021-12-02
EP3965748A1 (en) 2022-03-16
JP2022533069A (ja) 2022-07-21
CN114641280A (zh) 2022-06-17
CA3137308A1 (en) 2020-11-19
US20220204548A1 (en) 2022-06-30
KR20220007112A (ko) 2022-01-18
WO2020231776A1 (en) 2020-11-19

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