WO2018169153A1 - Composition contenant en tant que principe actif un agent bloquant l'acide par compétition avec le potassium, pour le traitement et la prévention du syndrome de l'intestin perméable - Google Patents
Composition contenant en tant que principe actif un agent bloquant l'acide par compétition avec le potassium, pour le traitement et la prévention du syndrome de l'intestin perméable Download PDFInfo
- Publication number
- WO2018169153A1 WO2018169153A1 PCT/KR2017/010349 KR2017010349W WO2018169153A1 WO 2018169153 A1 WO2018169153 A1 WO 2018169153A1 KR 2017010349 W KR2017010349 W KR 2017010349W WO 2018169153 A1 WO2018169153 A1 WO 2018169153A1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- treatment
- composition
- leaky gut
- gut syndrome
- cab
- Prior art date
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- 229940126535 potassium competitive acid blocker Drugs 0.000 title claims abstract description 22
- 208000011580 syndromic disease Diseases 0.000 title claims abstract description 21
- 239000000203 mixture Substances 0.000 title claims abstract description 11
- 239000004480 active ingredient Substances 0.000 title claims abstract description 4
- 230000002265 prevention Effects 0.000 title claims description 4
- 229940021182 non-steroidal anti-inflammatory drug Drugs 0.000 claims abstract description 23
- 239000000041 non-steroidal anti-inflammatory agent Substances 0.000 claims abstract description 5
- 239000003112 inhibitor Substances 0.000 claims description 4
- 238000000034 method Methods 0.000 claims description 4
- PWILYDZRJORZDR-MISYRCLQSA-N (7r,8r,9r)-7-(2-methoxyethoxy)-2,3-dimethyl-9-phenyl-7,8,9,10-tetrahydroimidazo[1,2-h][1,7]naphthyridin-8-ol Chemical compound C1([C@@H]2[C@@H](O)[C@@H](C3=C(C4=NC(C)=C(C)N4C=C3)N2)OCCOC)=CC=CC=C1 PWILYDZRJORZDR-MISYRCLQSA-N 0.000 claims description 3
- GHVIMBCFLRTFHI-UHFFFAOYSA-N 8-[(2,6-dimethylphenyl)methylamino]-n-(2-hydroxyethyl)-2,3-dimethylimidazo[1,2-a]pyridine-6-carboxamide Chemical compound C=1C(C(=O)NCCO)=CN2C(C)=C(C)N=C2C=1NCC1=C(C)C=CC=C1C GHVIMBCFLRTFHI-UHFFFAOYSA-N 0.000 claims description 3
- ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 claims description 3
- 230000002860 competitive effect Effects 0.000 claims description 3
- 230000027119 gastric acid secretion Effects 0.000 claims description 3
- 229950010119 linaprazan Drugs 0.000 claims description 3
- 229910052700 potassium Inorganic materials 0.000 claims description 3
- 239000011591 potassium Substances 0.000 claims description 3
- 229950004825 soraprazan Drugs 0.000 claims description 3
- 229950003825 vonoprazan Drugs 0.000 claims description 3
- BFDBKMOZYNOTPK-UHFFFAOYSA-N vonoprazan Chemical compound C=1C=CN=CC=1S(=O)(=O)N1C=C(CNC)C=C1C1=CC=CC=C1F BFDBKMOZYNOTPK-UHFFFAOYSA-N 0.000 claims description 3
- 210000004211 gastric acid Anatomy 0.000 claims 1
- CGIGDMFJXJATDK-UHFFFAOYSA-N indomethacin Chemical compound CC1=C(CC(O)=O)C2=CC(OC)=CC=C2N1C(=O)C1=CC=C(Cl)C=C1 CGIGDMFJXJATDK-UHFFFAOYSA-N 0.000 description 24
- 229940126409 proton pump inhibitor Drugs 0.000 description 18
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- 230000035699 permeability Effects 0.000 description 13
- 229960000905 indomethacin Drugs 0.000 description 12
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- 230000000694 effects Effects 0.000 description 10
- 102000000591 Tight Junction Proteins Human genes 0.000 description 8
- 108010002321 Tight Junction Proteins Proteins 0.000 description 8
- 206010061218 Inflammation Diseases 0.000 description 7
- 230000004054 inflammatory process Effects 0.000 description 7
- 230000000968 intestinal effect Effects 0.000 description 7
- 210000001519 tissue Anatomy 0.000 description 7
- 230000002496 gastric effect Effects 0.000 description 6
- 239000000612 proton pump inhibitor Substances 0.000 description 6
- 230000006378 damage Effects 0.000 description 5
- 230000003870 intestinal permeability Effects 0.000 description 5
- 210000004379 membrane Anatomy 0.000 description 5
- 239000012528 membrane Substances 0.000 description 5
- 229950000859 revaprazan Drugs 0.000 description 5
- LECZXZOBEZITCL-UHFFFAOYSA-N revaprazan Chemical compound C1CC2=CC=CC=C2C(C)N1C(C(=C(C)N=1)C)=NC=1NC1=CC=C(F)C=C1 LECZXZOBEZITCL-UHFFFAOYSA-N 0.000 description 5
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- 206010030113 Oedema Diseases 0.000 description 2
- IQPSEEYGBUAQFF-UHFFFAOYSA-N Pantoprazole Chemical compound COC1=CC=NC(CS(=O)C=2NC3=CC=C(OC(F)F)C=C3N=2)=C1OC IQPSEEYGBUAQFF-UHFFFAOYSA-N 0.000 description 2
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- SUBDBMMJDZJVOS-DEOSSOPVSA-N esomeprazole Chemical compound C([S@](=O)C1=NC2=CC=C(C=C2N1)OC)C1=NC=C(C)C(OC)=C1C SUBDBMMJDZJVOS-DEOSSOPVSA-N 0.000 description 2
- 229960004770 esomeprazole Drugs 0.000 description 2
- 230000006872 improvement Effects 0.000 description 2
- 210000000936 intestine Anatomy 0.000 description 2
- 239000000463 material Substances 0.000 description 2
- 229960005019 pantoprazole Drugs 0.000 description 2
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- 108010033674 rho GTP-Binding Proteins Proteins 0.000 description 2
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- 206010009944 Colon cancer Diseases 0.000 description 1
- 102000004127 Cytokines Human genes 0.000 description 1
- 108090000695 Cytokines Proteins 0.000 description 1
- 208000037487 Endotoxemia Diseases 0.000 description 1
- 206010061459 Gastrointestinal ulcer Diseases 0.000 description 1
- 206010020751 Hypersensitivity Diseases 0.000 description 1
- 108060003951 Immunoglobulin Proteins 0.000 description 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 description 1
- 208000004221 Multiple Trauma Diseases 0.000 description 1
- 102000003940 Occludin Human genes 0.000 description 1
- 108090000304 Occludin Proteins 0.000 description 1
- 102000006270 Proton Pumps Human genes 0.000 description 1
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- 230000002757 inflammatory effect Effects 0.000 description 1
- 230000028709 inflammatory response Effects 0.000 description 1
- 230000004941 influx Effects 0.000 description 1
- 210000005027 intestinal barrier Anatomy 0.000 description 1
- 230000007358 intestinal barrier function Effects 0.000 description 1
- 210000004347 intestinal mucosa Anatomy 0.000 description 1
- 238000010253 intravenous injection Methods 0.000 description 1
- 230000007794 irritation Effects 0.000 description 1
- 208000004341 lymphocytic colitis Diseases 0.000 description 1
- 210000005004 lymphoid follicle Anatomy 0.000 description 1
- 210000002540 macrophage Anatomy 0.000 description 1
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Images
Classifications
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4375—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
Definitions
- each tissue was scored on the basis of villi loss, ulceration, inflammation, and the like, when viewed pathologically as an animal tissue, and the results are shown in FIG. 6.
- severe vili loss and inflammation were observed, with similar findings in the group receiving PPI.
- the group receiving P-CAB showed more improvement in vili loss and inflammation.
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
La présente invention concerne une composition capable de prévenir et de traiter efficacement le syndrome de l'intestin perméable ou le syndrome de l'intestin perméable induit par un médicament anti-inflammatoire non stéroïdien (AINS), la composition contenant en tant que principe actif un agent bloquant l'acide par compétition avec le potassium (p-cab, pour "potassium-competitive acid blocker").
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| KR10-2017-0033118 | 2017-03-16 | ||
| KR1020170033118A KR20180107341A (ko) | 2017-03-16 | 2017-03-16 | 칼륨 경쟁적 위산분비억제제를 유효성분을 함유하는 장 누수 증후군 치료 및 예방용 조성물 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| WO2018169153A1 true WO2018169153A1 (fr) | 2018-09-20 |
Family
ID=63522412
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PCT/KR2017/010349 WO2018169153A1 (fr) | 2017-03-16 | 2017-09-20 | Composition contenant en tant que principe actif un agent bloquant l'acide par compétition avec le potassium, pour le traitement et la prévention du syndrome de l'intestin perméable |
Country Status (2)
| Country | Link |
|---|---|
| KR (1) | KR20180107341A (fr) |
| WO (1) | WO2018169153A1 (fr) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IT202100010412A1 (it) | 2021-04-26 | 2022-10-26 | Anseris Farma S R L | Composizione per il trattamento dell’intestino irritabile e della sindrome metabolica correlata alle alterazioni della permeabilità intestinale. |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2020089488A1 (fr) * | 2018-11-02 | 2020-05-07 | 4D Pharma Research Limited | Compositions comprenant des souches bactériennes |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20010056078A1 (en) * | 2000-02-11 | 2001-12-27 | Norton Healthcare Limited | Novel method for treating gut disorders using polyanionic polyglycosides |
| KR20070057663A (ko) * | 2005-12-01 | 2007-06-07 | 주식회사유한양행 | 위장관 점막 손상의 예방 또는 치료용 조성물 |
| US8183211B2 (en) * | 2000-05-19 | 2012-05-22 | University Of Maryland, Baltimore | Pharmaceutical compositions for inhibiting intestinal permeability |
| US20150057349A1 (en) * | 2012-03-30 | 2015-02-26 | Nestec S.A. | 4-oxo-2-pentenoic acid and the health of the digestive tract |
| US20150258151A1 (en) * | 2012-12-07 | 2015-09-17 | Albert Einstein College Of Medicine Of Yeshiva University | Gut barrier dysfunction treatment and prevention |
-
2017
- 2017-03-16 KR KR1020170033118A patent/KR20180107341A/ko not_active Ceased
- 2017-09-20 WO PCT/KR2017/010349 patent/WO2018169153A1/fr active Application Filing
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20010056078A1 (en) * | 2000-02-11 | 2001-12-27 | Norton Healthcare Limited | Novel method for treating gut disorders using polyanionic polyglycosides |
| US8183211B2 (en) * | 2000-05-19 | 2012-05-22 | University Of Maryland, Baltimore | Pharmaceutical compositions for inhibiting intestinal permeability |
| KR20070057663A (ko) * | 2005-12-01 | 2007-06-07 | 주식회사유한양행 | 위장관 점막 손상의 예방 또는 치료용 조성물 |
| US20150057349A1 (en) * | 2012-03-30 | 2015-02-26 | Nestec S.A. | 4-oxo-2-pentenoic acid and the health of the digestive tract |
| US20150258151A1 (en) * | 2012-12-07 | 2015-09-17 | Albert Einstein College Of Medicine Of Yeshiva University | Gut barrier dysfunction treatment and prevention |
Non-Patent Citations (1)
| Title |
|---|
| CHA CANCER PREVENTION RESEARCH CENTER, CHA CANCER INSTITUTE, CHA UNIVERSITY ET AL.: "Indomethacin-induced Leaky Gut Syndrome Aggravated by Pantoprazole, but Not by Revaprazan: PPI Aggravated, but p-CAB Relieved NSAID-induced Intestinal Permeability", THE 10TH INTERNATIONAL GASTROINTESTINAL CONSENSUS SYMPOSIUM, vol. 4, 18 February 2017 (2017-02-18), pages 104 - 4 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IT202100010412A1 (it) | 2021-04-26 | 2022-10-26 | Anseris Farma S R L | Composizione per il trattamento dell’intestino irritabile e della sindrome metabolica correlata alle alterazioni della permeabilità intestinale. |
Also Published As
| Publication number | Publication date |
|---|---|
| KR20180107341A (ko) | 2018-10-02 |
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