KR960017680A - 포스포노술포네이트 스쿠알렌 합성 효소 억제제 염 및 그의 제조 방법 - Google Patents
포스포노술포네이트 스쿠알렌 합성 효소 억제제 염 및 그의 제조 방법 Download PDFInfo
- Publication number
- KR960017680A KR960017680A KR1019950039576A KR19950039576A KR960017680A KR 960017680 A KR960017680 A KR 960017680A KR 1019950039576 A KR1019950039576 A KR 1019950039576A KR 19950039576 A KR19950039576 A KR 19950039576A KR 960017680 A KR960017680 A KR 960017680A
- Authority
- KR
- South Korea
- Prior art keywords
- salt
- free acid
- general formula
- phosphonosulfonate
- butylamine
- Prior art date
Links
- 150000003839 salts Chemical class 0.000 title claims abstract 14
- LQHYUUBBIJGBNR-UHFFFAOYSA-N OP(O)(=O)S(O)(=O)=O Chemical compound OP(O)(=O)S(O)(=O)=O LQHYUUBBIJGBNR-UHFFFAOYSA-N 0.000 title claims abstract 8
- 239000004059 squalene synthase inhibitor Substances 0.000 title abstract 2
- 229940123495 Squalene synthetase inhibitor Drugs 0.000 title 1
- 238000002360 preparation method Methods 0.000 title 1
- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 claims abstract 7
- YBRBMKDOPFTVDT-UHFFFAOYSA-N tert-butylamine Chemical class CC(C)(C)N YBRBMKDOPFTVDT-UHFFFAOYSA-N 0.000 claims abstract 6
- QIJIUJYANDSEKG-UHFFFAOYSA-N 2,4,4-trimethylpentan-2-amine Chemical class CC(C)(C)CC(C)(C)N QIJIUJYANDSEKG-UHFFFAOYSA-N 0.000 claims abstract 5
- 230000002401 inhibitory effect Effects 0.000 claims abstract 5
- 201000001320 Atherosclerosis Diseases 0.000 claims abstract 4
- JVVXZOOGOGPDRZ-SLFFLAALSA-N [(1R,4aS,10aR)-1,4a-dimethyl-7-propan-2-yl-2,3,4,9,10,10a-hexahydrophenanthren-1-yl]methanamine Chemical class NC[C@]1(C)CCC[C@]2(C)C3=CC=C(C(C)C)C=C3CC[C@H]21 JVVXZOOGOGPDRZ-SLFFLAALSA-N 0.000 claims abstract 4
- 230000015572 biosynthetic process Effects 0.000 claims abstract 3
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 claims abstract 2
- 229910052791 calcium Inorganic materials 0.000 claims abstract 2
- 239000011575 calcium Substances 0.000 claims abstract 2
- 238000000034 method Methods 0.000 claims 14
- 239000002253 acid Substances 0.000 claims 10
- 208000031226 Hyperlipidaemia Diseases 0.000 claims 6
- -1 halomethyl pivalate Chemical compound 0.000 claims 5
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims 2
- 206010018852 Haematoma Diseases 0.000 claims 2
- 208000035150 Hypercholesterolemia Diseases 0.000 claims 2
- 150000001412 amines Chemical class 0.000 claims 2
- 159000000007 calcium salts Chemical class 0.000 claims 2
- 235000012000 cholesterol Nutrition 0.000 claims 2
- 208000020346 hyperlipoproteinemia Diseases 0.000 claims 2
- 229950010765 pivalate Drugs 0.000 claims 2
- YQTCQNIPQMJNTI-UHFFFAOYSA-N 2,2-dimethylpropan-1-one Chemical group CC(C)(C)[C]=O YQTCQNIPQMJNTI-UHFFFAOYSA-N 0.000 claims 1
- KAIFXEAFPYBTFL-UHFFFAOYSA-N CC(C)(C)C(=O)OC[Ca] Chemical class CC(C)(C)C(=O)OC[Ca] KAIFXEAFPYBTFL-UHFFFAOYSA-N 0.000 claims 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 1
- XGJQGEQHHDEVEW-UHFFFAOYSA-N P(=O)(=O)S(=O)(=O)O Chemical compound P(=O)(=O)S(=O)(=O)O XGJQGEQHHDEVEW-UHFFFAOYSA-N 0.000 claims 1
- 150000007513 acids Chemical class 0.000 claims 1
- DKNWSYNQZKUICI-UHFFFAOYSA-N amantadine Chemical compound C1C(C2)CC3CC2CC1(N)C3 DKNWSYNQZKUICI-UHFFFAOYSA-N 0.000 claims 1
- 150000001875 compounds Chemical class 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 235000013399 edible fruits Nutrition 0.000 claims 1
- 239000011521 glass Substances 0.000 claims 1
- 235000011187 glycerol Nutrition 0.000 claims 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-M hydroxide Chemical compound [OH-] XLYOFNOQVPJJNP-UHFFFAOYSA-M 0.000 claims 1
- TVZISJTYELEYPI-UHFFFAOYSA-N hypodiphosphoric acid Chemical compound OP(O)(=O)P(O)(O)=O TVZISJTYELEYPI-UHFFFAOYSA-N 0.000 claims 1
- 238000002955 isolation Methods 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 238000000746 purification Methods 0.000 claims 1
- 239000000376 reactant Substances 0.000 claims 1
- 239000002904 solvent Substances 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
Classifications
-
- 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
- C07F9/28—Phosphorus compounds with one or more P—C bonds
- C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
- C07F9/40—Esters thereof
- C07F9/4003—Esters thereof the acid moiety containing a substituent or a structure which is considered as characteristic
- C07F9/4056—Esters of arylalkanephosphonic acids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
-
- 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
- C07F9/28—Phosphorus compounds with one or more P—C bonds
- C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
- C07F9/40—Esters thereof
- C07F9/4071—Esters thereof the ester moiety containing a substituent or a structure which is considered as characteristic
- C07F9/4075—Esters with hydroxyalkyl compounds
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Enzymes And Modification Thereof (AREA)
Abstract
본 발명은 칼슘, t-부틸아민염, t-옥틸아민염 및 데히드로아비에틸아민염을 포함하는, 포스포노술포네이트 스쿠알렌 합성 효소 억제제의 새로운 염 형태에 관한 것이다. 이들 염은 콜레스케롤 생합성을 억제함에 따라 혈청 콜레스테롤의 저하 및 아테롬성 동맥 경화증 치료에 사용된다.
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (19)
- 하기 일반식의 구조를 갖는 포스포노술포네이트염.상기 식 중, X는 t-부틸아민염, t-옥틸아민염 또는 데히드로아비에틸아민염을 나타낸다.
- 제1항에 있어서, t-부틸아민형인 염.
- 제1항에 있어서, t-옥틸아미염인 염.
- 제1항에 있어서, 데히드로아미에틸아민염인 염.
- 제1항에 따른 포스포노술포네이트염 및 이를 위한 제약학상 허용되는 담체를 함유하는 제약 조성물.
- 콜레스테롤 생합성의 억제, 혈청 콜레스테롤의 저하, 또는 과지방혈증, 고지혈증, 과지단백혈증, 과콜레스테린혈증 및(또는) 과트리글리세린혈증의 억제 및(또는) 치료, 또는 아테롬성 동맥경화증 억제 및(또는) 치료를 요하는 환자에게, 하기 일반식의 화합물의 치료학적 유효량을 투여하는 것으로 이루어지는 콜레스테롤 생합성의 억제, 혈청 콜레스테롤의 저하, 또는 과지방혈종, 고지혈증, 과지단백혈증, 과콜레스테린혈종 및(또는) 과트리글리세린혈종의 억제 및(또는) 치료, 또는 아테롬성 동맥경화증 억제 및(또는) 치료 방법.상기 식 중, X는 t-부틸아민염, t-옥틸아민염 또는 데히드로아미에틸아민염을 나타낸다.
- 제6항에 있어서, 염이 t-부틸아민염인 방법.
- 제6항에 있어서, 염이 t-옥틸아민염인 방법.
- 제6항에 있어서, 염이 데히드로아비에틸아민염인 방법.
- 제6항에 있어서, 아테롬성 동맥 경화증의 치료 방법.
- 제6항에 있어서, 과콜레스테린혈증의 치료 방법.
- 유리산을 1-아다암탄아민 또는 시코니딘과 반응시켜 대응하는 염을 형성하고, 이 형성되는 염을 이은 교환시켜 상당히 정제된 유리산을 제공하는 것으로 이루어지는, 상당히 정제된 형태의 하기 일반식의 유리산의 단리 및 정제 방법.
- 제12항에 있어서, 1-아다만틴아민을 유리산과 반응시켜 상기 유리산의 대응하는 비스-아다만탄아민염을 형성하는 방법.
- 제12항에 있어서, 신코니딘을 유리산과 반응시켜 대응하는 비스-신코니딘염을 형성하는 방법.
- 제12항에 있어서, 유리산을 알코올 용매 중에 먼저 용해시키는 방법.
- 하기 일반식의 포스포노술포네이트 유리산을 제공하고, 이 유리산을 아민 염기 존재시에 불활성 분위기에서 할로메틸 피발레이트, 및 칼슘염 또는 수산화물로 처리하여 포스포노술포네이트의 피발로일 옥시에틸 칼슘을 형성하는 것을 이루어지는, 하기 일반식의 포스포노술포네이트의 피발로일옥시메틸 칼슘염의 형성 방법.
- 제16항에 있어서, 할로메틸 피발레이트가 클로로-, 브로모- 또는 요오드메틸 피발레이드인 방법.
- 하기 일반식의 포스노포술포네이트의 칼슘염을 제공하고, 이 칼슘염을 이온 교환 수지로 처리하여 하기 일반식의 유리산을 억고, 이 유리산을 아미 반응 물질과 반응시켜 하기 일반식의 포스포술포네이트의 아민염을 형성하는 것을 이루어지는, 하기 일반식의 포스포노술포네이트의 아민염의 제조 방법.
- 제18항에 있어서, 아민 반응 물질이 t-부틸아민, t-옥틸아민 또는 데히드로아비에틸아민인 방법.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US33366194A | 1994-11-03 | 1994-11-03 | |
| US08/333,661 | 1994-11-03 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| KR960017680A true KR960017680A (ko) | 1996-06-17 |
Family
ID=23303735
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1019950039576A KR960017680A (ko) | 1994-11-03 | 1995-11-03 | 포스포노술포네이트 스쿠알렌 합성 효소 억제제 염 및 그의 제조 방법 |
Country Status (14)
| Country | Link |
|---|---|
| EP (1) | EP0710665A1 (ko) |
| JP (1) | JPH08208672A (ko) |
| KR (1) | KR960017680A (ko) |
| CN (1) | CN1130188A (ko) |
| AU (1) | AU3458795A (ko) |
| CA (1) | CA2159850A1 (ko) |
| CZ (1) | CZ279595A3 (ko) |
| FI (1) | FI955256A (ko) |
| HU (1) | HUT73140A (ko) |
| IL (1) | IL115537A0 (ko) |
| NO (1) | NO954389L (ko) |
| PL (1) | PL311218A1 (ko) |
| TW (1) | TW318852B (ko) |
| ZA (1) | ZA959326B (ko) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2780974B1 (fr) * | 1998-07-08 | 2001-09-28 | Sod Conseils Rech Applic | Utilisation de derives d'imidazopyrazines pour preparer un medicament destine a traiter les pathologies qui resultent de la formation de la proteine g heterotrimetrique |
| AU2002212741A1 (en) * | 2000-11-09 | 2002-05-21 | Takeda Chemical Industries Ltd. | High-density lipoprotein-cholesterol level elevating agent |
| BRPI0610722A2 (pt) | 2005-04-18 | 2016-11-16 | Univ California | métodos para tratar uma infecção bacteriana, para prevenir, tratar ou melhorar o tratamento eficaz de mrsa, para inibir o crescimento de um micróbio, e para selecionar um agente terapêutico de mrsa útil pata tratar uma infcção bacteriana, e, composição |
| AU2007249792B2 (en) * | 2006-05-12 | 2012-08-02 | The Board Of Trustees Of The University Of Illinois | Antimicrobial therapy for bacterial infections |
| CN101580472B (zh) * | 2009-06-24 | 2013-07-10 | 广西壮族自治区化工研究院 | 1,1'-联-2-萘酚的拆分剂以及拆分方法 |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2107644A1 (en) * | 1992-10-28 | 1994-04-29 | David R. Magnin | .alpha.-phosphonosulfonae squalene synthetase inhibitors and methd |
| US5312814A (en) * | 1992-12-09 | 1994-05-17 | Bristol-Myers Squibb Co. | α-phosphonocarboxylate squalene synthetase inhibitors |
-
1995
- 1995-10-04 CA CA002159850A patent/CA2159850A1/en not_active Abandoned
- 1995-10-06 IL IL11553795A patent/IL115537A0/xx unknown
- 1995-10-25 CZ CZ952795A patent/CZ279595A3/cs unknown
- 1995-10-26 EP EP95307618A patent/EP0710665A1/en not_active Withdrawn
- 1995-10-27 JP JP7280397A patent/JPH08208672A/ja active Pending
- 1995-11-02 PL PL95311218A patent/PL311218A1/xx unknown
- 1995-11-02 AU AU34587/95A patent/AU3458795A/en not_active Abandoned
- 1995-11-02 NO NO954389A patent/NO954389L/no unknown
- 1995-11-02 HU HU9503136A patent/HUT73140A/hu unknown
- 1995-11-02 TW TW084111593A patent/TW318852B/zh active
- 1995-11-02 FI FI955256A patent/FI955256A/fi not_active Application Discontinuation
- 1995-11-03 CN CN95119023A patent/CN1130188A/zh active Pending
- 1995-11-03 KR KR1019950039576A patent/KR960017680A/ko not_active Application Discontinuation
- 1995-11-03 ZA ZA959326A patent/ZA959326B/xx unknown
Also Published As
| Publication number | Publication date |
|---|---|
| HUT73140A (en) | 1996-06-28 |
| FI955256A0 (fi) | 1995-11-02 |
| PL311218A1 (en) | 1996-05-13 |
| NO954389D0 (no) | 1995-11-02 |
| IL115537A0 (en) | 1996-01-19 |
| CN1130188A (zh) | 1996-09-04 |
| CZ279595A3 (en) | 1996-08-14 |
| EP0710665A1 (en) | 1996-05-08 |
| CA2159850A1 (en) | 1996-05-04 |
| JPH08208672A (ja) | 1996-08-13 |
| AU3458795A (en) | 1996-05-09 |
| ZA959326B (en) | 1997-05-05 |
| TW318852B (ko) | 1997-11-01 |
| FI955256A (fi) | 1996-05-04 |
| NO954389L (no) | 1996-05-06 |
| HU9503136D0 (en) | 1995-12-28 |
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