KR890002128A - 실비빈의 가용성 유도체, 그것의 제조방법 및 그것을 함유하는 제약학적 조성물 - Google Patents
실비빈의 가용성 유도체, 그것의 제조방법 및 그것을 함유하는 제약학적 조성물 Download PDFInfo
- Publication number
- KR890002128A KR890002128A KR1019880008885A KR880008885A KR890002128A KR 890002128 A KR890002128 A KR 890002128A KR 1019880008885 A KR1019880008885 A KR 1019880008885A KR 880008885 A KR880008885 A KR 880008885A KR 890002128 A KR890002128 A KR 890002128A
- Authority
- KR
- South Korea
- Prior art keywords
- compound
- diester
- formula
- liver
- pharmaceutically acceptable
- Prior art date
Links
- 238000000034 method Methods 0.000 title claims 7
- 239000008194 pharmaceutical composition Substances 0.000 title claims 3
- 150000001875 compounds Chemical class 0.000 claims 8
- 230000006378 damage Effects 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 210000004185 liver Anatomy 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 208000027418 Wounds and injury Diseases 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000014674 injury Diseases 0.000 claims 2
- 230000001575 pathological effect Effects 0.000 claims 2
- 230000026731 phosphorylation Effects 0.000 claims 2
- 238000006366 phosphorylation reaction Methods 0.000 claims 2
- 208000030090 Acute Disease Diseases 0.000 claims 1
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims 1
- FDQAOULAVFHKBX-UHFFFAOYSA-N Isosilybin A Natural products C1=C(O)C(OC)=CC(C2C(OC3=CC(=CC=C3O2)C2C(C(=O)C3=C(O)C=C(O)C=C3O2)O)CO)=C1 FDQAOULAVFHKBX-UHFFFAOYSA-N 0.000 claims 1
- FYYHWMGAXLPEAU-UHFFFAOYSA-N Magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 claims 1
- SEBFKMXJBCUCAI-UHFFFAOYSA-N NSC 227190 Natural products C1=C(O)C(OC)=CC(C2C(OC3=CC=C(C=C3O2)C2C(C(=O)C3=C(O)C=C(O)C=C3O2)O)CO)=C1 SEBFKMXJBCUCAI-UHFFFAOYSA-N 0.000 claims 1
- 229910019142 PO4 Inorganic materials 0.000 claims 1
- ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 claims 1
- VLGROHBNWZUINI-UHFFFAOYSA-N Silybin Natural products COc1cc(ccc1O)C2OC3C=C(C=CC3OC2CO)C4Oc5cc(O)cc(O)c5C(=O)C4O VLGROHBNWZUINI-UHFFFAOYSA-N 0.000 claims 1
- 230000001154 acute effect Effects 0.000 claims 1
- 230000032683 aging Effects 0.000 claims 1
- 150000001413 amino acids Chemical class 0.000 claims 1
- 150000003863 ammonium salts Chemical class 0.000 claims 1
- 210000004556 brain Anatomy 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 230000003412 degenerative effect Effects 0.000 claims 1
- 230000002939 deleterious effect Effects 0.000 claims 1
- 150000005690 diesters Chemical class 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 210000002216 heart Anatomy 0.000 claims 1
- 230000007062 hydrolysis Effects 0.000 claims 1
- 238000006460 hydrolysis reaction Methods 0.000 claims 1
- 208000015181 infectious disease Diseases 0.000 claims 1
- 230000002458 infectious effect Effects 0.000 claims 1
- 208000019423 liver disease Diseases 0.000 claims 1
- 239000011777 magnesium Substances 0.000 claims 1
- 229910052749 magnesium Inorganic materials 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 230000002503 metabolic effect Effects 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 238000007911 parenteral administration Methods 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000010452 phosphate Substances 0.000 claims 1
- 230000000865 phosphorylative effect Effects 0.000 claims 1
- 239000011591 potassium Substances 0.000 claims 1
- 229910052700 potassium Inorganic materials 0.000 claims 1
- 239000011541 reaction mixture Substances 0.000 claims 1
- 230000000306 recurrent effect Effects 0.000 claims 1
- 238000010992 reflux Methods 0.000 claims 1
- SEBFKMXJBCUCAI-HKTJVKLFSA-N silibinin Chemical compound C1=C(O)C(OC)=CC([C@@H]2[C@H](OC3=CC=C(C=C3O2)[C@@H]2[C@H](C(=O)C3=C(O)C=C(O)C=C3O2)O)CO)=C1 SEBFKMXJBCUCAI-HKTJVKLFSA-N 0.000 claims 1
- 229940043175 silybin Drugs 0.000 claims 1
- 235000014899 silybin Nutrition 0.000 claims 1
- 239000011734 sodium Substances 0.000 claims 1
- 229910052708 sodium Inorganic materials 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 231100000331 toxic Toxicity 0.000 claims 1
- 230000002588 toxic effect Effects 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
- C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
- C07D407/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
- C07F9/65586—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system at least one of the hetero rings does not contain nitrogen as ring hetero atom
-
- 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
- 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
- A61P39/00—General protective or antinoxious agents
- A61P39/02—Antidotes
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Molecular Biology (AREA)
- Neurology (AREA)
- Biochemistry (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Urology & Nephrology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Gastroenterology & Hepatology (AREA)
- Vascular Medicine (AREA)
- Toxicology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
내용 없음
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (10)
- 다음 구조식 I의 화합물 또는 그것의 제약학적으로 허용가능한 염.식중, aR=H,R'=PO(OH)2또는 b R=PO(OH)2R'=PO(OH)2
- 실리빈 11-포스페이트 에스테르 또는 그것의 제약학적으로 허용가능한 염.
- 제1항에 또는 제2항에 있어서, 나트륨, 칼륨, 마그네슘 또는 암모늄 염이나 또는 염기성 아미노산을 갖는 염의 형태인 화합물.
- 제1항 내지 제3항의 어느 한 항의 화합물 및 제약학적으로 허용가능한 부형제로 구성되는 제약학적 조성물.
- 제4항에 있어서, 경구 투여, 직장 투여 또는 비경구 투여에 적합한 형태인 제약학적 조성물.
- 제1항 내지 제3항의 어느 한 항 화합물의 효과량을 투여하는 것으로 구성되는, 유리기로 인한 병적인 질환, 질병 또는 손상의 예방 및 치료방법.
- 제6항에 있어서, 상기 손상, 질병 또는 병적인 질환이 심장, 뇌 또는 간의 저형 상태 : 노화와 관계된 증후군 및 속의 상태후에 재환류로 결과하는 손상으로 구성되는 방법.
- 제1항 내지 제3항의 어느 한 항 화합물의 효과량을 투여하는 것으로 구성되는, 독성적, 대사적 및/또는 감염적 원인에 의한 또는 퇴행성에 의한 급성 및 만성 간질환으 치료방법 및 간에 유해한 기호물질 및/또는 약제의 사용으로 결과하는 간의 손상을 예방하는 방법.
- 실리빈이나 또는 그것의 에스테르-형성 유도체를 포스포릴화제와 반응시키고, (i)반응 혼합물로 부터 구조식(Ia) 화합물을 분리하며, (ii) 구조식(Ib) 의 3.11-디에스테르가 형성될 때까지 포스포릴화를 계속하여 상기 디에스테르를 분리하건, 또는(ⅲ) 구조식 (1b)의 3.11-디에스테르가 형성될 때까지 포스포릴화를 계속한 다음 3.11-디에스테르를 부분 가수분해하여 구조식(Ia)의 11-에스테르를 형성시키는 것으로 구성되는, 제1항 화합물의 제조방법.
- 제5항, 제6항, 제7항 또는 제8항의 방법에 사용되는 조성물을 제조하는데 제1항의 화합물을 사용하는 방법.※참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB878716918A GB8716918D0 (en) | 1987-07-17 | 1987-07-17 | Soluble derivatives of silybin |
| GB8716918 | 1987-07-17 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| KR890002128A true KR890002128A (ko) | 1989-04-08 |
Family
ID=10620836
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1019880008885A KR890002128A (ko) | 1987-07-17 | 1988-07-16 | 실비빈의 가용성 유도체, 그것의 제조방법 및 그것을 함유하는 제약학적 조성물 |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US4886791A (ko) |
| EP (1) | EP0299770A3 (ko) |
| JP (1) | JPS6447791A (ko) |
| KR (1) | KR890002128A (ko) |
| DK (1) | DK395788A (ko) |
| FI (1) | FI883392A (ko) |
| GB (1) | GB8716918D0 (ko) |
| PT (1) | PT88009A (ko) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5043273A (en) * | 1989-08-17 | 1991-08-27 | Monsanto Company | Phosphorylated glycosidase inhibitor prodrugs |
| US20020193424A1 (en) * | 2000-03-23 | 2002-12-19 | Slaga Thomas J. | Human cancerous cell anti-proliferation and survival inhibition agent |
| US20020151874A1 (en) | 2001-04-12 | 2002-10-17 | Kolster Alwin H. | Liposuction cannula device and method |
| CZ292832B6 (cs) * | 2001-08-30 | 2003-12-17 | Ivax Pharmaceuticals S.R.O. | Způsob přípravy silymarinu se zvýšenou rozpustností |
| CZ300846B6 (cs) * | 2008-06-26 | 2009-08-26 | Agra Group, A. S. | Vodorozpustný prípravek na bázi flavanonol lignanu a zpusob jeho prípravy |
| US8614341B2 (en) * | 2009-05-14 | 2013-12-24 | Euromed S.A. | Amorphous silibinin for the treatment of viral hepatitis |
| CN104098554B (zh) * | 2013-04-12 | 2016-06-29 | 佳木斯大学 | 水飞蓟宾氨基酸席夫碱的合成制备方法及其用途 |
| CN111925394A (zh) * | 2020-09-25 | 2020-11-13 | 嘉兴金派特生物科技有限公司 | 水飞蓟宾衍生物或其药学上可接受的盐及其制备方法和应用 |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE1963318A1 (de) * | 1969-12-17 | 1971-06-24 | Schwabe Willmar Gmbh & Co | Silybinhalbester der Bernsteinsaeure und der Phthalsaeure,ihre Salze mit pharmakologisch vertraglichen Basen,Verfahren zu ihrer Herstellung und ihre Verwendung zur Herstellung von Arzneipraeparaten |
| DE3442639A1 (de) * | 1984-11-22 | 1986-05-22 | Dr. Madaus & Co, 5000 Köln | Flavolignanderivate, verfahren zu deren herstellung und arzneimittel, die diese verbindungen enthalten |
| IT1215291B (it) * | 1985-07-17 | 1990-01-31 | Inverni Della Beffa Spa | Complessi di flavanolignani con fosfolipidi, loro preparazione e relative composizioni farmaceutiche. |
-
1987
- 1987-07-17 GB GB878716918A patent/GB8716918D0/en active Pending
-
1988
- 1988-07-13 US US07/219,058 patent/US4886791A/en not_active Expired - Fee Related
- 1988-07-14 EP EP88306459A patent/EP0299770A3/en not_active Ceased
- 1988-07-15 FI FI883392A patent/FI883392A/fi not_active Application Discontinuation
- 1988-07-15 PT PT88009A patent/PT88009A/pt unknown
- 1988-07-15 DK DK395788A patent/DK395788A/da not_active Application Discontinuation
- 1988-07-16 KR KR1019880008885A patent/KR890002128A/ko not_active Application Discontinuation
- 1988-07-18 JP JP63178905A patent/JPS6447791A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| GB8716918D0 (en) | 1987-08-26 |
| JPS6447791A (en) | 1989-02-22 |
| EP0299770A2 (en) | 1989-01-18 |
| US4886791A (en) | 1989-12-12 |
| PT88009A (pt) | 1989-06-30 |
| DK395788D0 (da) | 1988-07-15 |
| FI883392A0 (fi) | 1988-07-15 |
| FI883392A (fi) | 1989-01-18 |
| DK395788A (da) | 1989-01-18 |
| EP0299770A3 (en) | 1990-06-20 |
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| Date | Code | Title | Description |
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| WITN | Application deemed withdrawn, e.g. because no request for examination was filed or no examination fee was paid |