KR930019212A - 피소스티그민 유도체와 이의 용도 및 이를 함유한 제약적 조제물 - Google Patents
피소스티그민 유도체와 이의 용도 및 이를 함유한 제약적 조제물 Download PDFInfo
- Publication number
- KR930019212A KR930019212A KR1019930004010A KR930004010A KR930019212A KR 930019212 A KR930019212 A KR 930019212A KR 1019930004010 A KR1019930004010 A KR 1019930004010A KR 930004010 A KR930004010 A KR 930004010A KR 930019212 A KR930019212 A KR 930019212A
- Authority
- KR
- South Korea
- Prior art keywords
- salt
- physostigmine
- phosphatidic acid
- pharmaceutically acceptable
- active substance
- Prior art date
Links
- 239000000825 pharmaceutical preparation Substances 0.000 title 1
- 150000003839 salts Chemical class 0.000 claims abstract 17
- PIJVFDBKTWXHHD-UHFFFAOYSA-N Physostigmine Natural products C12=CC(OC(=O)NC)=CC=C2N(C)C2C1(C)CCN2C PIJVFDBKTWXHHD-UHFFFAOYSA-N 0.000 claims abstract 7
- PIJVFDBKTWXHHD-HIFRSBDPSA-N physostigmine Chemical class C12=CC(OC(=O)NC)=CC=C2N(C)[C@@H]2[C@@]1(C)CCN2C PIJVFDBKTWXHHD-HIFRSBDPSA-N 0.000 claims abstract 7
- 229960001697 physostigmine Drugs 0.000 claims abstract 7
- PORPENFLTBBHSG-MGBGTMOVSA-N 1,2-dihexadecanoyl-sn-glycerol-3-phosphate Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP(O)(O)=O)OC(=O)CCCCCCCCCCCCCCC PORPENFLTBBHSG-MGBGTMOVSA-N 0.000 claims abstract 6
- 208000024827 Alzheimer disease Diseases 0.000 claims abstract 4
- 206010039966 Senile dementia Diseases 0.000 claims abstract 2
- 239000013543 active substance Substances 0.000 claims 4
- 239000002552 dosage form Substances 0.000 claims 3
- 230000000694 effects Effects 0.000 claims 3
- 238000013268 sustained release Methods 0.000 claims 3
- 239000012730 sustained-release form Substances 0.000 claims 3
- 239000000203 mixture Substances 0.000 claims 2
- 239000002904 solvent Substances 0.000 claims 2
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 150000001768 cations Chemical class 0.000 claims 1
- 150000002170 ethers Chemical class 0.000 claims 1
- 239000004744 fabric Substances 0.000 claims 1
- 150000008282 halocarbons Chemical group 0.000 claims 1
- 239000004615 ingredient Substances 0.000 claims 1
- 150000002576 ketones Chemical class 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000000376 reactant Substances 0.000 claims 1
- 230000002490 cerebral effect Effects 0.000 abstract 1
- 239000000499 gel Substances 0.000 abstract 1
- 230000004060 metabolic process Effects 0.000 abstract 1
- 208000011580 syndromic disease Diseases 0.000 abstract 1
- 230000001225 therapeutic effect Effects 0.000 abstract 1
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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/70—Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
- A61K9/7023—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms
- A61K9/703—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms characterised by shape or structure; Details concerning release liner or backing; Refillable patches; User-activated patches
- A61K9/7038—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer
- A61K9/7046—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer the adhesive comprising macromolecular compounds
- A61K9/7053—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer the adhesive comprising macromolecular compounds obtained by reactions only involving carbon to carbon unsaturated bonds, e.g. polyvinyl, polyisobutylene, polystyrene
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- C07F9/06—Phosphorus compounds without P—C bonds
- C07F9/08—Esters of oxyacids of phosphorus
- C07F9/09—Esters of phosphoric acids
- C07F9/10—Phosphatides, e.g. lecithin
- C07F9/106—Adducts, complexes, salts of phosphatides
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Dermatology (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Molecular Biology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- General Chemical & Material Sciences (AREA)
- Biochemistry (AREA)
- Biomedical Technology (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Cephalosporin Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
노인성 대뇌대사변화에 관련된 질환들의 치료에 있어 피소스티그민의 신규염들이 치료용으로 이용된다. 포스파티드산에 근거한 피소스티그민의 신규염들은 고도의 친유성이고, 경구적, 경피적 투여시 탁월한 생물학적 효능을 나타낸다. 상기 신규염들은 깁스내 또는 적당한 겔 또는 적당한 제약적 형태들로 합체될때 노인성 치매 및 AlZheimer병의 치료용으로 특히 유용하다.
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (14)
- 안티콜린스테라제 활성을 지닌 피소스티그민 또는 그의 제약적으로 용인할 만한 유도체 및 포스파티드산의 염.
- 제1항에 있어서, 하기식(Ⅲ)를 갖는 염. [PS]X[PA]Y(Ⅲ) 식중 : PS는 안티콜린스테라제 활성을 지닌 피소스티그민 또는 그의 제약적으로 용인할만한 유도체로 부터 유도된 양이온, PA는 포스파티드산 또는 다른 포서파티드산들의 혼합물, 및 X:Y는 2:1 내지 1:2임.
- 제2항에 있어서, X:Y가 1.2:1 내지 1:1.2 바람직하게는 1.1:1 내지 1:1.1염.
- 제2항에 또는 제3항에 있어서, PS가 피소스티그민인 염.
- 제2항 내지 4항 중 어느 한항에 있어서, PA가 하기식(Ⅳ)를 갖는 포스파티드산인 염.식중: (서로 같거나 다를 수 있는) R1및 R2는 각자 C10-24알킬그룹, C|10-24알케닐그룹, 또는 C10-24알카디에닐그룹으로 표시됨.
- 제5항에 있어서, n이 15 내지 24인 염.
- 제6항에 있어서, n이 15 또는 17인 염.
- 피소스티그민 또는 그의 제약적으로 용인할만한 염을 포스파티드산과 반응시키는 것(상기 반응은 양 반응물에 적합한 용매내에서 수행하는)을 포함하는(전기한 항들 중 어느 한항에서 청구된 바와같은)염의 제조방법.
- 제8항에 있어서, 용매가 할로겐화된 탄화수소, 케톤, 에테르 및 그들의 혼합물에서 선택된 것인 염.
- 제약적으로 용인할만한 부형제와 제1항 내지 제7항 중 어느 한항에 청구된 바와같은 염을 포함하는 제약적 조성물.
- 제약적 활성물질이 제1항 내지 제7항중 어느 한항에 따른 염인것을 특징으로 하며, 일정기간동안 상기 제약적 활성물질을 방출할 수 있는 서방형 제약적 투약형태.
- 제11항에 있어서, 제약적 활성물질을 경피적으로 방출시키는데 적합한 서방형의 제약적 투약형태.
- 12항에 있어서, 피부의 상처에 대는 헝겊, 깁스 또는 붕대형태인 서방형의 제약적 투약형태.
- 노인성 치매 및 AlZheimer병 치료용의 제약적 성분으로 제조하는데 안티콜린 스테라제 활성을 지닌 피소스티그민 또는 그의 제약적으로 용인할 만한 유도체 및 포스파티드산의 염을 사용하는 방법.※ 참고사항 : 최초출원 내용에 의하여 공개되는 것임.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB9205670.4 | 1992-03-16 | ||
| GB929205670A GB9205670D0 (en) | 1992-03-16 | 1992-03-16 | New derivatives of physostigmine,their use and pharmaceutical formulations containing them |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| KR930019212A true KR930019212A (ko) | 1993-10-18 |
| KR100251395B1 KR100251395B1 (ko) | 2000-05-01 |
Family
ID=10712207
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1019930004010A KR100251395B1 (ko) | 1992-03-16 | 1993-03-16 | 피소스티그민 유도체와 이의 용도 및 이를 함유한 제약적 조제물 |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US5314906A (ko) |
| EP (1) | EP0561597B1 (ko) |
| JP (1) | JPH0640914A (ko) |
| KR (1) | KR100251395B1 (ko) |
| AT (1) | ATE147076T1 (ko) |
| CA (1) | CA2091550A1 (ko) |
| DE (1) | DE69306990T2 (ko) |
| DK (1) | DK0561597T3 (ko) |
| ES (1) | ES2096203T3 (ko) |
| GB (1) | GB9205670D0 (ko) |
| GR (1) | GR3022205T3 (ko) |
| HK (1) | HK61897A (ko) |
| SG (1) | SG67287A1 (ko) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5861431A (en) * | 1995-06-07 | 1999-01-19 | Iotek, Inc. | Incontinence treatment |
| US5709878A (en) * | 1996-08-02 | 1998-01-20 | Rosenbaum; Jerry | Transdermal delivery of dehydroepiandrosterone |
| IL121322A (en) * | 1997-07-16 | 2002-07-25 | Modus Biolog Membranes Ltd | Modular pharmacological preparation of the immune system based on fats and its preparation |
| AU8562998A (en) * | 1997-08-12 | 1999-03-01 | Takeda Chemical Industries Ltd. | Idebenone-containing preparation for percutaneous administration |
| US5869090A (en) * | 1998-01-20 | 1999-02-09 | Rosenbaum; Jerry | Transdermal delivery of dehydroepiandrosterone |
| DE10025644A1 (de) * | 2000-05-24 | 2001-12-06 | Lohmann Therapie Syst Lts | Schmales bandförmiges transdermales therapeutisches System zur Applikation von Wirkstoffen direkt über dem arteriellen oder venösen Gefäßsystem |
| CA2458068A1 (en) * | 2001-08-20 | 2003-02-27 | Tatton Technologies, Llc. | Methods and compositions for treating apoptosis associated disorders |
| KR100758089B1 (ko) * | 2005-08-04 | 2007-09-11 | 아이알 마이크로시스템 에스.에이. | 기체 검출 방법 및 기체 검출 장치 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IT1109003B (it) * | 1977-09-20 | 1985-12-16 | Univ Firenze | Derivati dell 1 2 3 8 3 a 8 a esai dropirrolo 23 b indolo |
| IT1199076B (it) * | 1984-03-01 | 1988-12-30 | Consiglio Nazionale Ricerche | Derivati della fisostigmina con proprieta'di inibizione della aceticolinesterasi e relativo procedimento di produzione |
| IT1225462B (it) * | 1987-04-03 | 1990-11-14 | Mediolanum Farmaceutici Srl | Sali organici di derivati della fisostigmina |
| EP0350672A1 (en) * | 1988-06-28 | 1990-01-17 | MAGIS FARMACEUTICI S.p.A. | Salts of diacyl-glycero-(di)-phosphates of L-(acyl) carnitine and of L-acyl-carnitine esters |
| IT1238684B (it) * | 1990-02-09 | 1993-09-01 | Indena Spa | Derivati del bilobalide,loro usi e formulazioni che li contegono |
| EP0513703A3 (en) * | 1991-05-13 | 1993-01-13 | Magis Farmaceutici S.P.A. | Carbamate esters of eseroline having anticholinesterase activity, a process for their preparation and relative pharmaceutical compositions containing them as the active principle |
-
1992
- 1992-03-16 GB GB929205670A patent/GB9205670D0/en active Pending
-
1993
- 1993-01-11 US US08/002,794 patent/US5314906A/en not_active Expired - Fee Related
- 1993-03-04 JP JP5082361A patent/JPH0640914A/ja active Pending
- 1993-03-11 CA CA002091550A patent/CA2091550A1/en not_active Abandoned
- 1993-03-15 DE DE69306990T patent/DE69306990T2/de not_active Expired - Fee Related
- 1993-03-15 SG SG1996000619A patent/SG67287A1/en unknown
- 1993-03-15 AT AT93301955T patent/ATE147076T1/de not_active IP Right Cessation
- 1993-03-15 EP EP93301955A patent/EP0561597B1/en not_active Expired - Lifetime
- 1993-03-15 ES ES93301955T patent/ES2096203T3/es not_active Expired - Lifetime
- 1993-03-15 DK DK93301955.6T patent/DK0561597T3/da active
- 1993-03-16 KR KR1019930004010A patent/KR100251395B1/ko not_active IP Right Cessation
-
1997
- 1997-01-03 GR GR960402200T patent/GR3022205T3/el unknown
- 1997-05-08 HK HK61897A patent/HK61897A/xx not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| SG67287A1 (en) | 1999-09-21 |
| DE69306990D1 (de) | 1997-02-13 |
| ATE147076T1 (de) | 1997-01-15 |
| HK61897A (en) | 1997-05-16 |
| GR3022205T3 (en) | 1997-04-30 |
| DK0561597T3 (da) | 1997-01-20 |
| KR100251395B1 (ko) | 2000-05-01 |
| CA2091550A1 (en) | 1993-09-17 |
| DE69306990T2 (de) | 1997-06-12 |
| EP0561597B1 (en) | 1997-01-02 |
| JPH0640914A (ja) | 1994-02-15 |
| EP0561597A1 (en) | 1993-09-22 |
| GB9205670D0 (en) | 1992-04-29 |
| US5314906A (en) | 1994-05-24 |
| ES2096203T3 (es) | 1997-03-01 |
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