BR112021022431A2 - Moduladores de molécula pequena de metabolismo bacteriano intestinal do ácido biliar - Google Patents
Moduladores de molécula pequena de metabolismo bacteriano intestinal do ácido biliarInfo
- 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
Links
- HSINOMROUCMIEA-FGVHQWLLSA-N (2s,4r)-4-[(3r,5s,6r,7r,8s,9s,10s,13r,14s,17r)-6-ethyl-3,7-dihydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1h-cyclopenta[a]phenanthren-17-yl]-2-methylpentanoic acid Chemical compound C([C@@]12C)C[C@@H](O)C[C@H]1[C@@H](CC)[C@@H](O)[C@@H]1[C@@H]2CC[C@]2(C)[C@@H]([C@H](C)C[C@H](C)C(O)=O)CC[C@H]21 HSINOMROUCMIEA-FGVHQWLLSA-N 0.000 title abstract 2
- 230000001580 bacterial effect Effects 0.000 title abstract 2
- 239000003613 bile acid Substances 0.000 title abstract 2
- 230000000968 intestinal effect Effects 0.000 title abstract 2
- 230000004060 metabolic process Effects 0.000 title abstract 2
- 150000003384 small molecules Chemical class 0.000 title abstract 2
- 208000006454 hepatitis Diseases 0.000 abstract 5
- 231100000283 hepatitis Toxicity 0.000 abstract 5
- 206010003011 Appendicitis Diseases 0.000 abstract 2
- 208000015943 Coeliac disease Diseases 0.000 abstract 2
- 206010009900 Colitis ulcerative Diseases 0.000 abstract 2
- 208000011231 Crohn disease Diseases 0.000 abstract 2
- 208000004232 Enteritis Diseases 0.000 abstract 2
- 208000007882 Gastritis Diseases 0.000 abstract 2
- 208000022559 Inflammatory bowel disease Diseases 0.000 abstract 2
- 206010028980 Neoplasm Diseases 0.000 abstract 2
- 206010033645 Pancreatitis Diseases 0.000 abstract 2
- 208000025865 Ulcer Diseases 0.000 abstract 2
- 201000006704 Ulcerative Colitis Diseases 0.000 abstract 2
- 201000011510 cancer Diseases 0.000 abstract 2
- 206010012601 diabetes mellitus Diseases 0.000 abstract 2
- 208000007784 diverticulitis Diseases 0.000 abstract 2
- 208000021302 gastroesophageal reflux disease Diseases 0.000 abstract 2
- 208000019423 liver disease Diseases 0.000 abstract 2
- 238000000034 method Methods 0.000 abstract 2
- 231100000397 ulcer Toxicity 0.000 abstract 2
- 206010003827 Autoimmune hepatitis Diseases 0.000 abstract 1
- 108010000231 Choloylglycine hydrolase Proteins 0.000 abstract 1
- 208000002699 Digestive System Neoplasms Diseases 0.000 abstract 1
- 206010058838 Enterocolitis infectious Diseases 0.000 abstract 1
- 206010016654 Fibrosis Diseases 0.000 abstract 1
- 206010061958 Food Intolerance Diseases 0.000 abstract 1
- 208000018522 Gastrointestinal disease Diseases 0.000 abstract 1
- 206010017964 Gastrointestinal infection Diseases 0.000 abstract 1
- 208000008589 Obesity Diseases 0.000 abstract 1
- 206010030216 Oesophagitis Diseases 0.000 abstract 1
- 201000004681 Psoriasis Diseases 0.000 abstract 1
- 201000001263 Psoriatic Arthritis Diseases 0.000 abstract 1
- 208000036824 Psoriatic arthropathy Diseases 0.000 abstract 1
- 230000001476 alcoholic effect Effects 0.000 abstract 1
- 230000007882 cirrhosis Effects 0.000 abstract 1
- 208000019425 cirrhosis of liver Diseases 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 208000010643 digestive system disease Diseases 0.000 abstract 1
- 208000019836 digestive system infectious disease Diseases 0.000 abstract 1
- 208000006881 esophagitis Diseases 0.000 abstract 1
- 208000018685 gastrointestinal system disease Diseases 0.000 abstract 1
- 208000027139 infectious colitis Diseases 0.000 abstract 1
- 208000027866 inflammatory disease Diseases 0.000 abstract 1
- 230000005764 inhibitory process Effects 0.000 abstract 1
- 208000002551 irritable bowel syndrome Diseases 0.000 abstract 1
- 210000004185 liver Anatomy 0.000 abstract 1
- 201000007270 liver cancer Diseases 0.000 abstract 1
- 208000014018 liver neoplasm Diseases 0.000 abstract 1
- 208000030159 metabolic disease Diseases 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 208000008338 non-alcoholic fatty liver disease Diseases 0.000 abstract 1
- 206010053219 non-alcoholic steatohepatitis Diseases 0.000 abstract 1
- 235000020824 obesity Nutrition 0.000 abstract 1
- 206010039073 rheumatoid arthritis Diseases 0.000 abstract 1
Classifications
-
- 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).
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 |
Family
ID=73289482
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
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)
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)
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 |
-
2020
- 2020-05-08 EP EP20805532.7A patent/EP3965748A4/en active Pending
- 2020-05-08 CN CN202080050183.1A patent/CN114641280A/zh active Pending
- 2020-05-08 AU AU2020274319A patent/AU2020274319A1/en active Pending
- 2020-05-08 KR KR1020217040058A patent/KR20220007112A/ko unknown
- 2020-05-08 JP JP2021567062A patent/JP2022533069A/ja active Pending
- 2020-05-08 US US17/610,037 patent/US20220204548A1/en active Pending
- 2020-05-08 CA CA3137308A patent/CA3137308A1/en active Pending
- 2020-05-08 BR BR112021022431A patent/BR112021022431A2/pt unknown
- 2020-05-08 WO PCT/US2020/032016 patent/WO2020231776A1/en unknown
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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Legal Events
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B06W | Patent application suspended after preliminary examination (for patents with searches from other patent authorities) chapter 6.23 patent gazette] |