KR930006009A - 4-[4-[4-(4-히드록시페닐)-1-피페라지닐]페닐]-5-메틸-3h-1,2,4-트리아졸-3-온 유도체 - Google Patents
4-[4-[4-(4-히드록시페닐)-1-피페라지닐]페닐]-5-메틸-3h-1,2,4-트리아졸-3-온 유도체 Download PDFInfo
- Publication number
- KR930006009A KR930006009A KR1019920016515A KR920016515A KR930006009A KR 930006009 A KR930006009 A KR 930006009A KR 1019920016515 A KR1019920016515 A KR 1019920016515A KR 920016515 A KR920016515 A KR 920016515A KR 930006009 A KR930006009 A KR 930006009A
- Authority
- KR
- South Korea
- Prior art keywords
- compound
- formula
- addition salt
- acid addition
- choh
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Withdrawn
Links
- LBXGGCVIAMMNFV-UHFFFAOYSA-N 4-[4-[4-(4-hydroxyphenyl)piperazin-1-yl]phenyl]-3-methyl-1h-1,2,4-triazol-5-one Chemical class CC1=NNC(=O)N1C1=CC=C(N2CCN(CC2)C=2C=CC(O)=CC=2)C=C1 LBXGGCVIAMMNFV-UHFFFAOYSA-N 0.000 title abstract 2
- 238000000034 method Methods 0.000 claims abstract 6
- 150000001875 compounds Chemical class 0.000 claims 11
- 239000002253 acid Substances 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 5
- 239000000203 mixture Substances 0.000 claims 4
- RJJUJUCRHKNIMP-UHFFFAOYSA-N 2-[2-(4-chlorophenyl)-2-oxoethyl]-4-[4-[4-(4-hydroxyphenyl)piperazin-1-yl]phenyl]-5-methyl-1,2,4-triazol-3-one Chemical compound O=C1N(C=2C=CC(=CC=2)N2CCN(CC2)C=2C=CC(O)=CC=2)C(C)=NN1CC(=O)C1=CC=C(Cl)C=C1 RJJUJUCRHKNIMP-UHFFFAOYSA-N 0.000 claims 1
- 102000001381 Arachidonate 5-Lipoxygenase Human genes 0.000 claims 1
- 108010093579 Arachidonate 5-lipoxygenase Proteins 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 230000002378 acidificating effect Effects 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 239000003513 alkali Substances 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 239000005557 antagonist Substances 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 239000006071 cream Substances 0.000 claims 1
- 208000037765 diseases and disorders Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 239000012458 free base Substances 0.000 claims 1
- 230000001329 hyperkeratotic effect Effects 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 150000002617 leukotrienes Chemical class 0.000 claims 1
- 239000012038 nucleophile Substances 0.000 claims 1
- 239000006186 oral dosage form Substances 0.000 claims 1
- 208000017520 skin disease Diseases 0.000 claims 1
- 238000011200 topical administration Methods 0.000 claims 1
- 231100000331 toxic Toxicity 0.000 claims 1
- 230000002588 toxic effect Effects 0.000 claims 1
- 229940124125 5 Lipoxygenase inhibitor Drugs 0.000 abstract 1
- 239000000867 Lipoxygenase Inhibitor Substances 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
- C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
- C07D249/10—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D249/12—Oxygen or sulfur atoms
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Pulmonology (AREA)
- Dermatology (AREA)
- Immunology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
본 발명은 5-리폭시게나제 억제제로서 사용하기 위한 하기 일반식(Ⅰ)의 2-[2-(4-클로로페닐)-2-(히드록시 또는 옥소)에틸]-2, 4-디하이드로-4-[4-[4-(4-히드록시페닐)-1-피페라지닐]페닐]-5-메틸-3H-1, 2, 4-트리아졸-3-온, 그의 약제학적 조성물, 이들의 제조방법 및 류코트리엔-개제된 질병을 치료하는 방법에 관한 것이다.
상시 식에서, X는 C=0 또는 CHOH를 나타낸다.
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (10)
- 일반식(Ⅰ)의 화합물, 그의 약제학적으로 허용되는 산 부가염, 또는 그의 거울상 이성체.상기 식에서, X는 C=0 또는 CHOH를 나타낸다.
- 제1항에 있어서, 2-[2-(4-클로로페닐)-2-(옥소)에틸]-2, 4-디하이드로-4-[4-[4-(4-히드록시페닐)-1-피페라지닐]페닐]-5-메틸-3H-1, 2, 4-트리아졸-3-온 또는 그이 약제학적으로 허용되는 산 부가염인 화합물.
- 약제학적으로 허용되는 담체, 및 활성성분으로서 치료학적 유효량의 제1항에 따르는 화합물을 함유하는 5-리폭시게나게 억제 조성물.
- 제3항에 있어서, 경구 투여 형태의 조성물.
- 제3항에 있어서, 국소 투여하기에 적합한 형태의 조성물.
- 제5항에 있어서, 크림제인 조성물.
- 5-리폭시게나제 악제 유효량이 제1항에 따른 일반식(Ⅰ)의 화합물을 투여함을 특징으로 하여, 류코트리엔-개재된 질병 및 질환을 앓고 있는 온혈운동을 치료하는 방법.
- 치료학적 유효량의 제1항에 따르는 일반식(Ⅰ)의 화합물을 투여함을 특징으로 하여, 염증성 장 질환을 앓고 있는 온혈동물을 치료하는 방법.
- 치료학적 유효량의 제1항에 따르는 일반식(Ⅰ)의 화합물을 투여함을 특징으로 하여, 과각학성 피부병을 앓고 있는 온혈동물을 치료하는 방법.
- 일반식(Ⅱ)의 알콕시유도체를 산성매체중에서, 또는 강한 친핵체를 사용하여 탈알킬화시키고, 임의로 X가 C=0를 나타내는 일반식(Ⅰ)의 화합물을 X가 CHOH를 나타내는 일반식(Ⅰ)의 화합물로 환원시키고, 추가로 필요에 따라 X가 CHOH를 나타내는 화합물을 그의 거울상 이성체로 분리하고, 필요에 따라 일반식(Ⅰ)의 화합물을 산으로 치리하여 치료학적으로 활성인 우독성 산 부가염 형태로 전환시키거나, 또는 역으로, 산 부가염을 알칼리로 처리하여 유리 염기 형태로 전환시킴을 특징으로 하여, 제1항에 따르는 일반식(Ⅰ)의 화합물, 그의 약제학적으로 허용되는 산부가염 또는 그의 거울상 이성체를 제조하는 방법.상기 식에서, R1은 C1-6알킬이고, X는 C=0 또는 CHOH이다.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP91202351 | 1991-09-13 | ||
| EP91202351.2 | 1991-09-13 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| KR930006009A true KR930006009A (ko) | 1993-04-20 |
Family
ID=8207873
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1019920016515A Withdrawn KR930006009A (ko) | 1991-09-13 | 1992-09-09 | 4-[4-[4-(4-히드록시페닐)-1-피페라지닐]페닐]-5-메틸-3h-1,2,4-트리아졸-3-온 유도체 |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US5254553A (ko) |
| EP (1) | EP0532091A1 (ko) |
| JP (1) | JPH05194436A (ko) |
| KR (1) | KR930006009A (ko) |
| CN (1) | CN1071420A (ko) |
| AU (1) | AU652069B2 (ko) |
| BG (1) | BG96815A (ko) |
| CA (1) | CA2076257A1 (ko) |
| FI (1) | FI923723L (ko) |
| HU (1) | HUT62884A (ko) |
| IL (1) | IL102863A (ko) |
| MX (1) | MX9205186A (ko) |
| NO (1) | NO923532L (ko) |
| NZ (1) | NZ244297A (ko) |
| ZA (1) | ZA926967B (ko) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20160009750A (ko) * | 2014-07-16 | 2016-01-27 | 주식회사 큐리언트 | 염증성 질환 치료용 화합물 |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW279864B (ko) * | 1993-02-19 | 1996-07-01 | Janssen Pharmaceutica Nv | |
| AU685935B2 (en) * | 1994-04-06 | 1998-01-29 | Janssen Pharmaceutica N.V. | Anti-helicobacter ester and carbamate derivatives of azolones |
| US5607932A (en) * | 1994-07-12 | 1997-03-04 | Janssen Pharmaceutica N.V. | Heterocyclic derivatives of azolones |
| US5571811A (en) * | 1994-07-12 | 1996-11-05 | Janssen Pharmaceutica N.V. | Sulfonamide derivatives of azolones |
| US6001866A (en) * | 1995-10-05 | 1999-12-14 | Warner-Lambert Company | Method for treating and preventing inflammation and atherosclerosis |
| CA2759176C (en) | 2009-04-29 | 2016-03-15 | Amarin Corporation Plc | Pharmaceutical compositions comprising epa and a cardiovascular agent and methods of using the same |
| WO2012043791A1 (ja) * | 2010-10-01 | 2012-04-05 | 大正製薬株式会社 | １，２，４-トリアゾロン誘導体 |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA1292472C (en) * | 1985-12-03 | 1991-11-26 | Alfonsus Guilielmus Knaeps | Derivatives of ¬¬4-¬4-(4-phenyl-1-piperazinyl)- phenoxymethyl|-1,3-dioxolan-2-yl|methyl|-1h-imidazoles and 1h-1,2,4-triazoles |
| US4791111A (en) * | 1985-12-23 | 1988-12-13 | Janssen Pharmaceutica, N.V. | [[4-[4-(4-phenyl-1-piperazinyl)phenoxymethyl]-1,3-dioxolan-2-yl]methyl]-1H-imidazoles and 1H-1,2,4-triazoles having anti-microbial properties |
| CA1331757C (en) * | 1988-02-29 | 1994-08-30 | Janssen Pharmaceutica Naamloze Vennootschap | 5-lipoxygenase inhibiting 4-(4-phenyl-1-piperazinyl)phenols |
-
1992
- 1992-08-17 CA CA002076257A patent/CA2076257A1/en not_active Abandoned
- 1992-08-19 IL IL10286392A patent/IL102863A/en not_active IP Right Cessation
- 1992-08-19 FI FI923723A patent/FI923723L/fi not_active Application Discontinuation
- 1992-08-21 CN CN92110869A patent/CN1071420A/zh active Pending
- 1992-08-24 US US07/933,848 patent/US5254553A/en not_active Expired - Fee Related
- 1992-08-25 BG BG096815A patent/BG96815A/bg unknown
- 1992-08-27 JP JP4250403A patent/JPH05194436A/ja not_active Withdrawn
- 1992-09-03 EP EP92202663A patent/EP0532091A1/en not_active Withdrawn
- 1992-09-07 AU AU22819/92A patent/AU652069B2/en not_active Ceased
- 1992-09-09 KR KR1019920016515A patent/KR930006009A/ko not_active Withdrawn
- 1992-09-10 NZ NZ244297A patent/NZ244297A/en unknown
- 1992-09-11 NO NO92923532A patent/NO923532L/no unknown
- 1992-09-11 ZA ZA926967A patent/ZA926967B/xx unknown
- 1992-09-11 MX MX9205186A patent/MX9205186A/es unknown
- 1992-09-11 HU HU9202914A patent/HUT62884A/hu unknown
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20160009750A (ko) * | 2014-07-16 | 2016-01-27 | 주식회사 큐리언트 | 염증성 질환 치료용 화합물 |
Also Published As
| Publication number | Publication date |
|---|---|
| BG96815A (bg) | 1993-12-24 |
| IL102863A (en) | 1996-05-14 |
| FI923723A7 (fi) | 1993-03-14 |
| AU652069B2 (en) | 1994-08-11 |
| FI923723A0 (fi) | 1992-08-19 |
| CN1071420A (zh) | 1993-04-28 |
| NZ244297A (en) | 1994-03-25 |
| AU2281992A (en) | 1993-03-18 |
| CA2076257A1 (en) | 1993-03-14 |
| MX9205186A (es) | 1993-03-01 |
| NO923532L (no) | 1993-03-15 |
| IL102863A0 (en) | 1993-01-31 |
| US5254553A (en) | 1993-10-19 |
| FI923723L (fi) | 1993-03-14 |
| NO923532D0 (no) | 1992-09-11 |
| JPH05194436A (ja) | 1993-08-03 |
| ZA926967B (en) | 1994-03-11 |
| EP0532091A1 (en) | 1993-03-17 |
| HUT62884A (en) | 1993-06-28 |
| HU9202914D0 (en) | 1992-11-30 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PA0109 | Patent application |
Patent event code: PA01091R01D Comment text: Patent Application Patent event date: 19920909 |
|
| PG1501 | Laying open of application | ||
| PC1203 | Withdrawal of no request for examination | ||
| WITN | Application deemed withdrawn, e.g. because no request for examination was filed or no examination fee was paid |