KR940018387A - 위장 장애와 궤양 유발이 현저히 감소된 케토롤락 유도체 - Google Patents
위장 장애와 궤양 유발이 현저히 감소된 케토롤락 유도체 Download PDFInfo
- Publication number
- KR940018387A KR940018387A KR1019940000417A KR19940000417A KR940018387A KR 940018387 A KR940018387 A KR 940018387A KR 1019940000417 A KR1019940000417 A KR 1019940000417A KR 19940000417 A KR19940000417 A KR 19940000417A KR 940018387 A KR940018387 A KR 940018387A
- Authority
- KR
- South Korea
- Prior art keywords
- compound according
- ketorolac
- pyrrolidin
- pyrrolidinyl
- dihydro
- Prior art date
Links
- 206010061459 Gastrointestinal ulcer Diseases 0.000 title abstract 2
- 230000006698 induction Effects 0.000 title abstract 2
- OZWKMVRBQXNZKK-UHFFFAOYSA-N ketorolac Chemical class OC(=O)C1CCN2C1=CC=C2C(=O)C1=CC=CC=C1 OZWKMVRBQXNZKK-UHFFFAOYSA-N 0.000 title abstract 2
- 231100000397 ulcer Toxicity 0.000 title abstract 2
- 206010000059 abdominal discomfort Diseases 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract 10
- 150000003839 salts Chemical class 0.000 claims abstract 6
- -1 2- (1-pyrrolidinyl) ethyl Chemical group 0.000 claims abstract 2
- 239000002253 acid Substances 0.000 claims abstract 2
- 238000004519 manufacturing process Methods 0.000 claims 3
- 206010061218 Inflammation Diseases 0.000 claims 2
- 241001465754 Metazoa Species 0.000 claims 2
- 230000004054 inflammatory process Effects 0.000 claims 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims 2
- 239000008196 pharmacological composition Substances 0.000 claims 2
- MUBZPKHOEPUJKR-UHFFFAOYSA-N Oxalic acid Chemical group OC(=O)C(O)=O MUBZPKHOEPUJKR-UHFFFAOYSA-N 0.000 claims 1
- 229940100198 alkylating agent Drugs 0.000 claims 1
- 239000002168 alkylating agent Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 229960003750 ethyl chloride Drugs 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 238000007911 parenteral administration Methods 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
- 230000000694 effects Effects 0.000 abstract 2
- 208000018522 Gastrointestinal disease Diseases 0.000 abstract 1
- 230000000202 analgesic effect Effects 0.000 abstract 1
- 239000000730 antalgic agent Substances 0.000 abstract 1
- 229940121363 anti-inflammatory agent Drugs 0.000 abstract 1
- 239000002260 anti-inflammatory agent Substances 0.000 abstract 1
- 229960004752 ketorolac Drugs 0.000 abstract 1
- 150000003891 oxalate salts Chemical class 0.000 abstract 1
Classifications
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pain & Pain Management (AREA)
- Public Health (AREA)
- Rheumatology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Polysaccharides And Polysaccharide Derivatives (AREA)
- Steroid Compounds (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
본 발명은(±)-5-벤조일-2,3-디히드로-1H-피롤리진-1-카르복실- 또는 케토롤락-산의 신규한2-(1-피롤리디닐)에틸 에스테르인 구조식(Ⅰ)의 화합물. 약리적으로 허용되는그의 부가염, 바람직하게는 옥살산염에 관한 것이다. 시판되는 케토롤락(트로메타몰염)은 바람직하지 못한 부작용(위장 장애 및 궤양유발)을 일으키는 것으로 알려져 있다. 놀랍게도, 본 발명의 화합물의 적용시에는 상기한 바람직스럽지 못한 부작용들이 현저히 감소되며 따라서 본 발명의 화합물들은 진통/소염제로서 잠재적으로 유리하게 사용될 수 있다.
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (9)
- 다음 구조식(Ⅰ)로 표시되는(±)-5-벤조일-2,3-디히드로-1H-피롤리진-1-카르복실산의- 2-(1-피롤리디닐)에틸 에스테르 및 약리적으로 허용되는 그의 부가염.
- 제 1 항에 있어서, 상기 부가염이 옥살산염인 것이 특징인 화합물.
- 제 1 항 또는 2항에 있어서, 치료적 목적에 이용되는 것이 특징인 화합물.
- 제 1 항 또는 2항에 있어서, 인간과 동물의 통증 및 염증을 치료하기 위한 것이 특징인 화합물.
- 제 1 항 또는 2항에 따른 화합물의 치료적 유효량과 약리적으로 허용되는 부형제의 적절한 양으로 이루어진 약리적 조성물.
- 제 5 항에 있어서, 약리적으로 허용되는 보형제가 경구 또는 비경구 투여를 위한 적절한 추출제제인 것이 특징인 약리적 조성물.
- 인간 및 동물의 통증이나 염증 치료를 위한 약제 제조용으로서의 제 1 항 또는 2항에 따른 화합물의 용도.
- (±)-5-벤조일-2,3-디히드로-1H-피롤리진-1-카르복실산을- 2-1-피롤리디닐)-에틸 클로라이드나 그의 염 또는그에 상당하는 알킬화제로 알킬화시킨 다음 소망되는 부가염 생산을 위해 필요에 따라 상응하는 산을 첨가하는 것으로 됨을 특징으로 하는 제 1 항 또는 2항에 따른 화합물의 제조방법.
- 제 1 항 또는 2항에 따른 화합물의 치료적 유효량을 약리적으로 허용되는 적절한 부형제의 소망되는 양에 첨가하는 것을 포함하는 제 5 항 또는 6항에 따른 조성물의 제조방법.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE4300697A DE4300697C1 (de) | 1993-01-13 | 1993-01-13 | Keterolac-Derivat mit wesentlich geringerer gastrointestinaler Reizung und Ulzeration |
| DEP4300697.3 | 1993-01-13 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| KR940018387A true KR940018387A (ko) | 1994-08-16 |
Family
ID=6478109
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1019940000417A KR940018387A (ko) | 1993-01-13 | 1994-01-12 | 위장 장애와 궤양 유발이 현저히 감소된 케토롤락 유도체 |
Country Status (14)
| Country | Link |
|---|---|
| US (2) | US5508301A (ko) |
| EP (1) | EP0606657B1 (ko) |
| JP (1) | JPH06316577A (ko) |
| KR (1) | KR940018387A (ko) |
| AT (1) | ATE144775T1 (ko) |
| CA (1) | CA2113226A1 (ko) |
| DE (2) | DE4300697C1 (ko) |
| DK (1) | DK0606657T3 (ko) |
| ES (1) | ES2094454T3 (ko) |
| FI (1) | FI105919B (ko) |
| GR (1) | GR3021717T3 (ko) |
| HU (1) | HU216841B (ko) |
| NO (1) | NO301013B1 (ko) |
| ZA (1) | ZA94183B (ko) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20020050188A (ko) * | 2002-03-19 | 2002-06-26 | 에코바이오젠주식회사 | 경피흡수제로서의 용도를 위해 지용성이 부가된케토로락의 에스테르 유도체 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4089969A (en) * | 1976-07-14 | 1978-05-16 | Syntex (U.S.A.) Inc. | 5-Aroyl-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acid derivatives and process for the production thereof |
| JPS539788A (en) * | 1976-07-14 | 1978-01-28 | Syntex Inc | 55aloyll1*22dihydroo3hh pyroro *1*22a* pyroll11 carboxylic acid derivative |
| ZA882957B (en) * | 1987-04-27 | 1989-12-27 | Syntex Pharma Int | Omega-quaternary ammonium alkyl esters and thioesters of acidic nonsteroidal anti-inflammatory drugs |
| DK0519983T3 (da) * | 1990-03-16 | 1996-10-14 | Procter & Gamble | Anvendelse af ketorolac til behandling af periodontal sygdom |
-
1993
- 1993-01-13 DE DE4300697A patent/DE4300697C1/de not_active Expired - Fee Related
- 1993-12-30 DK DK93121130.4T patent/DK0606657T3/da active
- 1993-12-30 AT AT93121130T patent/ATE144775T1/de active
- 1993-12-30 EP EP93121130A patent/EP0606657B1/de not_active Expired - Lifetime
- 1993-12-30 DE DE59304359T patent/DE59304359D1/de not_active Expired - Fee Related
- 1993-12-30 ES ES93121130T patent/ES2094454T3/es not_active Expired - Lifetime
-
1994
- 1994-01-03 HU HU9400006A patent/HU216841B/hu not_active IP Right Cessation
- 1994-01-07 US US08/178,541 patent/US5508301A/en not_active Expired - Fee Related
- 1994-01-11 CA CA002113226A patent/CA2113226A1/en not_active Abandoned
- 1994-01-12 ZA ZA94183A patent/ZA94183B/xx unknown
- 1994-01-12 JP JP6013935A patent/JPH06316577A/ja active Pending
- 1994-01-12 KR KR1019940000417A patent/KR940018387A/ko not_active Application Discontinuation
- 1994-01-12 NO NO940109A patent/NO301013B1/no unknown
- 1994-01-13 FI FI940171A patent/FI105919B/fi active
-
1995
- 1995-06-06 US US08/468,648 patent/US5574170A/en not_active Expired - Fee Related
-
1996
- 1996-11-20 GR GR960403112T patent/GR3021717T3/el unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CA2113226A1 (en) | 1994-07-14 |
| FI105919B (fi) | 2000-10-31 |
| GR3021717T3 (en) | 1997-02-28 |
| DK0606657T3 (da) | 1997-04-14 |
| DE4300697C1 (de) | 1994-05-19 |
| FI940171A (fi) | 1994-07-14 |
| NO301013B1 (no) | 1997-09-01 |
| ES2094454T3 (es) | 1997-01-16 |
| HUT70410A (en) | 1995-10-30 |
| EP0606657A1 (de) | 1994-07-20 |
| DE59304359D1 (de) | 1996-12-05 |
| HU9400006D0 (en) | 1994-05-30 |
| US5508301A (en) | 1996-04-16 |
| ATE144775T1 (de) | 1996-11-15 |
| US5574170A (en) | 1996-11-12 |
| HU216841B (hu) | 1999-09-28 |
| NO940109D0 (no) | 1994-01-12 |
| JPH06316577A (ja) | 1994-11-15 |
| NO940109L (no) | 1994-07-14 |
| ZA94183B (en) | 1994-08-18 |
| EP0606657B1 (de) | 1996-10-30 |
| FI940171A0 (fi) | 1994-01-13 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A201 | Request for examination | ||
| E902 | Notification of reason for refusal | ||
| E601 | Decision to refuse application |