KR950701907A - 데스페리옥사민-B 염 및 경구투여에 유효한 철 킬레이트화제로서의 이의 용도(Desferrioxamine-B salts and their use as orally effective iron chelators) - Google Patents
데스페리옥사민-B 염 및 경구투여에 유효한 철 킬레이트화제로서의 이의 용도(Desferrioxamine-B salts and their use as orally effective iron chelators)Info
- Publication number
- KR950701907A KR950701907A KR1019940704389A KR19940704389A KR950701907A KR 950701907 A KR950701907 A KR 950701907A KR 1019940704389 A KR1019940704389 A KR 1019940704389A KR 19940704389 A KR19940704389 A KR 19940704389A KR 950701907 A KR950701907 A KR 950701907A
- Authority
- KR
- South Korea
- Prior art keywords
- salt
- acid
- general formula
- sulfonic acid
- group
- Prior art date
Links
- XEEYBQQBJWHFJM-UHFFFAOYSA-N Iron Chemical compound [Fe] XEEYBQQBJWHFJM-UHFFFAOYSA-N 0.000 title 2
- UBQYURCVBFRUQT-UHFFFAOYSA-N N-benzoyl-Ferrioxamine B Chemical class CC(=O)N(O)CCCCCNC(=O)CCC(=O)N(O)CCCCCNC(=O)CCC(=O)N(O)CCCCCN UBQYURCVBFRUQT-UHFFFAOYSA-N 0.000 title 1
- 239000002738 chelating agent Substances 0.000 title 1
- 229910052742 iron Inorganic materials 0.000 title 1
- 150000003839 salts Chemical class 0.000 claims abstract 30
- 125000004432 carbon atom Chemical group C* 0.000 claims abstract 7
- 125000001931 aliphatic group Chemical group 0.000 claims abstract 4
- 239000000203 mixture Substances 0.000 claims 8
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 claims 5
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 5
- LSNNMFCWUKXFEE-UHFFFAOYSA-M Bisulfite Chemical compound OS([O-])=O LSNNMFCWUKXFEE-UHFFFAOYSA-M 0.000 claims 4
- 239000002253 acid Substances 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- QPILZZVXGUNELN-UHFFFAOYSA-M sodium;4-amino-5-hydroxynaphthalene-2,7-disulfonate;hydron Chemical compound [Na+].OS(=O)(=O)C1=CC(O)=C2C(N)=CC(S([O-])(=O)=O)=CC2=C1 QPILZZVXGUNELN-UHFFFAOYSA-M 0.000 claims 4
- 208000024827 Alzheimer disease Diseases 0.000 claims 3
- 229910052782 aluminium Inorganic materials 0.000 claims 3
- XAGFODPZIPBFFR-UHFFFAOYSA-N aluminium Chemical compound [Al] XAGFODPZIPBFFR-UHFFFAOYSA-N 0.000 claims 3
- -1 hydrocarbyl sulfonic acid Chemical compound 0.000 claims 3
- 201000004792 malaria Diseases 0.000 claims 3
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 206010063837 Reperfusion injury Diseases 0.000 claims 2
- 229910052783 alkali metal Inorganic materials 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 206010020718 hyperplasia Diseases 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- KVGOXGQSTGQXDD-UHFFFAOYSA-N 1-decane-sulfonic-acid Chemical compound CCCCCCCCCCS(O)(=O)=O KVGOXGQSTGQXDD-UHFFFAOYSA-N 0.000 claims 1
- LDMOEFOXLIZJOW-UHFFFAOYSA-N 1-dodecanesulfonic acid Chemical compound CCCCCCCCCCCCS(O)(=O)=O LDMOEFOXLIZJOW-UHFFFAOYSA-N 0.000 claims 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- 206010020565 Hyperaemia Diseases 0.000 claims 1
- 206010022979 Iron excess Diseases 0.000 claims 1
- 241001465754 Metazoa Species 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- FYAQQULBLMNGAH-UHFFFAOYSA-N hexane-1-sulfonic acid Chemical compound CCCCCCS(O)(=O)=O FYAQQULBLMNGAH-UHFFFAOYSA-N 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- WLGDAKIJYPIYLR-UHFFFAOYSA-N octane-1-sulfonic acid Chemical compound CCCCCCCCS(O)(=O)=O WLGDAKIJYPIYLR-UHFFFAOYSA-N 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 238000002360 preparation method Methods 0.000 claims 1
- 150000003460 sulfonic acids Chemical class 0.000 claims 1
- 150000003457 sulfones Chemical class 0.000 abstract 1
Classifications
-
- 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
- C07C259/06—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 hydrogen atoms or to acyclic carbon atoms
-
- 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
- A61P33/00—Antiparasitic agents
- A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Tropical Medicine & Parasitology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Medicinal Preparation (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Macromolecular Compounds Obtained By Forming Nitrogen-Containing Linkages In General (AREA)
- Saccharide Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
Abstract
본 발명은 일반식(Ⅰ)의 염에 관한 것이다:
상기식에서, X는 구조식(Ⅱ)의 그룹
이고, Y는 구조식(Ⅲ)의 그룹
이며, R은 -SO3H 그룹의 제거후 탄소수가 3 이상인 지방족 또는 지환족 설폰사의 잔기이다.
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (24)
- 일반식 (I)의 염 :상기식에서, X는 구조식(Ⅱ)의 그룹이고, Y는 구조식(Ⅲ)의 그룹이며, R은 -SO3H 그룹의 제거후 탄소수가 3 이상인 지방족 또는 지환족 설폰산의 관기이다.
- 제1항에 있어서, R의 탄소수가 6 이상인 염.
- 제1항에 있어서, R의 탄소수가 6 내지 20 인 염.
- 제1항에 있어서, R의 탄소수가 6 내지 12 인 염.
- 제1항에 있어서, R의 탄소수가 8 내지 12 인 염.
- 제1항에 있어서, R의 탄소수가 8 내지 10 인 염.
- 제1항 내지 제6항중 어느 한 항에 있어서, R이 -S03H 그룹 제거후의 하이드로카빌 설폰산의 잔기인 염.
- 제7항에 있어서, 설폰산이 알칸설폰산인 염.
- 제8항에 있어서, 설폰산이 헥산-1-설폰산, 옥탄-1-설폰산, 데칸-1-설폰산 또는 도데칸-1-설폰산인 염.
- 제1항 내지 제9항중 어느 한 항에 있어서, R이 -S03H 그룹 제거후의 탄소수 3 이상의 지방족 또는 지환족 설폰산의 잔기인 일반식 RS03H 설폰산의 추가의 수용성 염과 혼합된 일반식(I)의 염.
- 제10항에 있어서, R이 제2항 내지 제9항중 어느 한 항에서 정의한 바와 같은 염.
- 제10항 또는 제11항에 있어서, 추가의 염이 알칼리 금속염인 염.
- 제10항, 제11항 또는 제12항에 있어서, 추가의 염이 일반식(I)의 염의 50 중랑% 이하의 양으로 존재하는 염.
- 활성성분으로서 제1항 내지 제13항중 어느 한 항에 따른 염 또는 데스페리옥사민-B 메탄설포네이트와 R이 제1항 내지 제9항중 어느 한 항에서 정의한 바와 같은 일반식 RS03H 산의 수용성 염과의 혼합물을 포함하는 약제학적 조성물.
- 제14항에 있어서, 수용성 염이 알칼리 금속염인 조성물.
- 제14항 또는 제15항에 있어서, 수용성 염이 데스페리옥사민-B 메탄설포네이트의 50중량% 이하의 양으로 존재하는 조성물.
- 제14항, 제15항 또는 제16항에 있어서, 경구 투여를 위한 조성물.
- 제14항 내지 제17항중 어느 한 항에 있어서, 약제학적으로 허용되는 부형제를 추가로 포함하는 조성물.
- 온혈동물의 치료방법에 사용하기 위한 제1항 내지 제13항중 어느 한 항에 따른 염, 또는 제14항 내지 제16항중 어느 한 항에서 정의한 바와 같은 데스페리옥사민-B 메탄설포네이트와 일반식 RS03H 산의 수용성 염과의 혼합물.
- 알루미늄 과다증, 알쯔하이머 질환, 말라리아, 재관류 손상 또는 암 치료용 약제학적 조성물을 제조하기 위한 제1항 내지 제13항중 어느 한 항에 따른 염, 또는 제14항 내지 제16항중 어느 한 항에서 정의한 바와 같은 데스페리옥사민-B 메탄설포네이트와 일반식 RS03H 산의 수용성염과의 혼합물의 용도.
- 철-과다 질환 치료용 약제학적 조성물을 제조하기 위한 제1항 내지 제13항중 어느 한 항에 따른 염, 또는 제14항 내지 제16항중 어느 한 항에서 정의한 바와 같은 데스페리옥사민-B 메탄설포네이트와 일반식 RS03H 산의 수용성염과의 혼합물의 용도.
- 알루미늄 과다증. 알쯔하이머 질환, 말라리아. 재관류 손상, 암 또는 철-과다 질환의 치료가 필요한 온혈동물에게 제1항에 따른 염 또는 제14항에 따른 약제학적 조성물을 투여하는 단계를 포함하여, 알루미늄 과다증, 알쯔하이머 질환, 말라리아, 재관류 손상, 암 또는 철-과다 질환을 치료하는 방법.
- 데스페리옥사민-B를 R이 -SO3H그룹 제거후 탄소수가 3 이상인 지방족 또는 지환족 설폰산의 잔기를 나타내는 일반식 RS03H의 산, 또는 이의 염-형성 유도체와 반응시키는 단계를 포함하여, 제1항에 따른 염을 제조하는 방법.
- 데스페리옥사민-B 메탄설포네이트와 R이 제1항 내지 제9항에서 정의한 바와 같은 일반식 RS03H 설폰산의 수용성 염과 혼합하는 단계를 포함하여 약제학적 조성물을 제조하는 방법.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB929211779A GB9211779D0 (en) | 1992-06-03 | 1992-06-03 | Amine salts |
| GB9211779.5 | 1992-06-03 | ||
| PCT/GB1993/000940 WO1993024451A1 (en) | 1992-06-03 | 1993-05-06 | Desferrioxamine-b salts and their use as orally effective iron chelators |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| KR950701907A true KR950701907A (ko) | 1995-05-17 |
Family
ID=10716488
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1019940704389A KR950701907A (ko) | 1992-06-03 | 1993-05-06 | 데스페리옥사민-B 염 및 경구투여에 유효한 철 킬레이트화제로서의 이의 용도(Desferrioxamine-B salts and their use as orally effective iron chelators) |
Country Status (17)
| Country | Link |
|---|---|
| US (2) | US5739167A (ko) |
| EP (1) | EP0643690B1 (ko) |
| JP (1) | JPH07507288A (ko) |
| KR (1) | KR950701907A (ko) |
| AT (1) | ATE166342T1 (ko) |
| AU (1) | AU672607B2 (ko) |
| CA (1) | CA2135394A1 (ko) |
| DE (1) | DE69318711T2 (ko) |
| DK (1) | DK0643690T3 (ko) |
| ES (1) | ES2117132T3 (ko) |
| FI (1) | FI945654A (ko) |
| GB (1) | GB9211779D0 (ko) |
| HK (1) | HK1009330A1 (ko) |
| NO (1) | NO302749B1 (ko) |
| NZ (1) | NZ252738A (ko) |
| TW (1) | TW230203B (ko) |
| WO (1) | WO1993024451A1 (ko) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PE27799A1 (es) * | 1996-12-10 | 1999-03-18 | Novartis Ag | Formulaciones y formas polimorficas de desferrioxamina y su preparacion |
| US7045531B1 (en) | 1997-03-11 | 2006-05-16 | The General Hospital Corporation | Composition comprising a metal chelator and a method of treating amyloidosis by administering the metal chelator |
| GB9727224D0 (en) * | 1997-12-23 | 1998-02-25 | Nycomed Imaging As | Method |
| US6323218B1 (en) | 1998-03-11 | 2001-11-27 | The General Hospital Corporation | Agents for use in the treatment of Alzheimer's disease |
| US6638711B1 (en) | 1999-04-29 | 2003-10-28 | The General Hospital Corporation | Methods for identifying an agent that inhibits oxygen-dependent hydrogen peroxide formation activity but does not inhibit superoxide-dependent hydrogen peroxide formation |
| GB0117645D0 (en) | 2001-07-19 | 2001-09-12 | Isis Innovation | Therapeutic stratergies for prevention and treatment of alzheimers disease |
| US6958161B2 (en) * | 2002-04-12 | 2005-10-25 | F H Faulding & Co Limited | Modified release coated drug preparation |
| US8614204B2 (en) | 2003-06-06 | 2013-12-24 | Fibrogen, Inc. | Enhanced erythropoiesis and iron metabolism |
| US8236783B2 (en) * | 2006-08-15 | 2012-08-07 | Duke University | ROS-sensitive iron chelators and methods of using the same |
| US9139456B2 (en) | 2008-04-16 | 2015-09-22 | The Curators Of The University Of Missouri | Chelating compounds and immobilized tethered chelators |
| US9259670B2 (en) | 2008-04-16 | 2016-02-16 | The University Of Kentucky Research Foundation | Flow-through filter to remove aluminum from medical solutions |
| US7932326B2 (en) * | 2008-04-16 | 2011-04-26 | The University Of Kentucky Research Foundation | Chelating compounds and immobilized tethered chelators |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CH438351A (de) * | 1959-09-25 | 1967-06-30 | Ciba Geigy | Verfahren zur Herstellung neuer Wuchsstoffe |
| FR1898M (fr) * | 1961-04-07 | 1963-07-08 | Ciba Geigy | Nouvelle substance utilisable en thérapeutique. |
| US3679660A (en) * | 1969-06-09 | 1972-07-25 | Agatha C Magnus | Glucosamine-alkylsulfonate and process |
| US3652411A (en) * | 1969-12-04 | 1972-03-28 | Mobil Oil Corp | Polyglycol base lubricant |
| US4419365A (en) * | 1981-12-21 | 1983-12-06 | Ciba-Geigy Corporation | Method of treating Alzheimer's disease |
| US4684482A (en) * | 1984-01-26 | 1987-08-04 | Oral-D (L.P.) | Orally effective ion chelators |
| IT1173992B (it) * | 1984-05-16 | 1987-06-24 | Bioresearch Spa | Sali stabili della solfo-adenosil-l-metionina (same) particolarmente idonei per uso farmaceutico orale |
| MX12394A (es) * | 1987-07-23 | 1993-12-01 | Ciba Geigy Ag | Procedimiento par la obtencion de carbamatos de polietilenglicol. |
| WO1992020227A1 (en) * | 1991-05-13 | 1992-11-26 | Oral-D | Substituted orally effective ion chelators related to deferoxamine |
-
1992
- 1992-06-03 GB GB929211779A patent/GB9211779D0/en active Pending
-
1993
- 1993-04-22 TW TW082103080A patent/TW230203B/zh active
- 1993-05-06 KR KR1019940704389A patent/KR950701907A/ko not_active Application Discontinuation
- 1993-05-06 NZ NZ252738A patent/NZ252738A/en unknown
- 1993-05-06 AT AT93911928T patent/ATE166342T1/de not_active IP Right Cessation
- 1993-05-06 JP JP6500277A patent/JPH07507288A/ja active Pending
- 1993-05-06 CA CA002135394A patent/CA2135394A1/en not_active Abandoned
- 1993-05-06 AU AU42700/93A patent/AU672607B2/en not_active Ceased
- 1993-05-06 US US08/343,599 patent/US5739167A/en not_active Expired - Lifetime
- 1993-05-06 EP EP93911928A patent/EP0643690B1/en not_active Expired - Lifetime
- 1993-05-06 DK DK93911928T patent/DK0643690T3/da active
- 1993-05-06 WO PCT/GB1993/000940 patent/WO1993024451A1/en active IP Right Grant
- 1993-05-06 DE DE69318711T patent/DE69318711T2/de not_active Expired - Lifetime
- 1993-05-06 ES ES93911928T patent/ES2117132T3/es not_active Expired - Lifetime
-
1994
- 1994-11-30 FI FI945654A patent/FI945654A/fi unknown
- 1994-12-01 NO NO944617A patent/NO302749B1/no not_active IP Right Cessation
-
1996
- 1996-03-11 US US08/613,562 patent/US5663201A/en not_active Expired - Lifetime
-
1998
- 1998-08-18 HK HK98109975A patent/HK1009330A1/xx not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| NO944617D0 (no) | 1994-12-01 |
| AU4270093A (en) | 1993-12-30 |
| DE69318711D1 (de) | 1998-06-25 |
| JPH07507288A (ja) | 1995-08-10 |
| ATE166342T1 (de) | 1998-06-15 |
| TW230203B (ko) | 1994-09-11 |
| US5663201A (en) | 1997-09-02 |
| ES2117132T3 (es) | 1998-08-01 |
| CA2135394A1 (en) | 1993-12-09 |
| EP0643690A1 (en) | 1995-03-22 |
| US5739167A (en) | 1998-04-14 |
| AU672607B2 (en) | 1996-10-10 |
| DE69318711T2 (de) | 1998-11-19 |
| HK1009330A1 (en) | 1999-05-28 |
| FI945654A0 (fi) | 1994-11-30 |
| NZ252738A (en) | 1996-08-27 |
| FI945654A (fi) | 1994-11-30 |
| EP0643690B1 (en) | 1998-05-20 |
| NO302749B1 (no) | 1998-04-20 |
| GB9211779D0 (en) | 1992-07-15 |
| WO1993024451A1 (en) | 1993-12-09 |
| DK0643690T3 (da) | 1999-01-25 |
| NO944617L (no) | 1995-01-05 |
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