KR910000714A - 항진균성 4[4-[4-[4-[[2-(2,4-디플루오로페닐)-2-(1h-아졸릴메틸)-1,3-디옥솔란-4-일]메톡시]페닐]-1-피페라지닐]페닐]트리아졸론 및 이미다졸론 - Google Patents
항진균성 4[4-[4-[4-[[2-(2,4-디플루오로페닐)-2-(1h-아졸릴메틸)-1,3-디옥솔란-4-일]메톡시]페닐]-1-피페라지닐]페닐]트리아졸론 및 이미다졸론 Download PDFInfo
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- KR910000714A KR910000714A KR1019900007765A KR900007765A KR910000714A KR 910000714 A KR910000714 A KR 910000714A KR 1019900007765 A KR1019900007765 A KR 1019900007765A KR 900007765 A KR900007765 A KR 900007765A KR 910000714 A KR910000714 A KR 910000714A
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero 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
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/10—Antimycotics
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Oncology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Communicable Diseases (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
Abstract
Description
Claims (8)
- 하기 구조식(Ⅰ)의 화합물과 약제학적으로 허용되는 이들의 산부가염 또는 입체화학적 이성체위의 식에서 Q는 CH또는 N이고, Y는 하기구조식의 라디칼이다.(위의 식에서 R1은 C5-7시클로알킬 또는 모노-, 디-, 트리-, 테트라- 또는 펜타할로 C1-4알킬이고, R2는 C1-4알킬, C5-7시클로알킬 또는 모노-, 디-, 드리-, 테트라- 또는 펜타할로 C1-4알킬이다)
- 제1항에 있어서,Q는 N이고, 디옥솔란 핵에 있는 치환기들이 시스배열을 가진 화합물.
- 제2항에 있어서,R1과 R2는 모노-, 디-, 트리-, 테트라- 또는 펜타할로 C1-4알킬, 시클로헥실 또는 시클로펜틸이거나 R2는 C1-4알킬인 화합물.
- 제3항에 있어서, R1과 R2는 2.2.2-트리플루오로에틸, 2.2.3.3-테트라플루오로프로필, 시클로펜틸이거나 R2가 프로필, 1-메틸프로필, 2-메틸프로릴 또는 부틸인 화합물.
- 제1항에 있어서 화합물이 시스-2-시클로펜틸-4-[4-[4-[4-[[2-(2,4-디플루오로페닐)-2-(1H-1,2,4-트리아졸-1-일메틸)-1,3-디옥솔린-4-일]메톡시]페닐]-1-피페라지닐]페닐]-2,4-디히드로-3H-1,2,4-트리아졸-3-온, 시스-4-[4-[4-[4-[[2-(2,4-디플루오로페닐)-2-(1H-1,2,4-트리아졸-1-일메틸)-1,3-디옥솔린-4-일]메톡시]페닐]-1-피페라지닐]페닐]-2,4-디히드로-2-(2,2,2-트리플루오로에틸)-3H-1,2,4-트리아졸-3-온, 또는 시스-1-[4-[4-[4-[[2-(2,4-디플루오로페닐)-2-(1H-1,2,4-트리아졸-1-일메틸)-1,3-디옥솔란-4-일]메톡시]페닐]-1-피페라지닐]페닐]-1,3-디히드로-3-(1-메틸프로필)-2H-이미다졸-2-온인 화합물.
- 비활성 담체와 활성성분으로서 제1항 내지 제5항중 어느 한 항에 의한 화합물을 항진균 유효량으로 하여 함유한 항진균성 조성물.
- 제1항 내지 제5항 중 어느 한 항에 의한 화합물을 항진균유효량으로 하여 온혈동물에 전신투여 또는 국소투여함으로서 균류에 의한 각종 질환을 앓고 있는 온형동물에 있어서 균류의 생장이나 발육을 억제 또는 예방하거나 균류를 박멸하는 방법.
- (a) 반응비활성 용매중에서 염기존재하에 하기 구조식(Ⅲ)의 페놀을 구조식 D-CH2-W(Ⅱ)(여기서 W는 반응성 이탈기)의 알킬화 제로 0-알킬화하거나,(b) 반응비활성용매중에서 산 존재하에 하기 구조식(Ⅳ)의 케톤을 구조식(Ⅴ)의 2,3-디히드록시프로필에테르 유도체로 아세탈화 반응시키거나,(c) 반응비활성용매중에서 염기존재하에 하기 구조식(Ⅵ)의 아졸 또는 그 금속염을 하기 구조식(Ⅶ)의 중간체로 N-알킬화하거나,(위의 식에서 w는 반응성 이탈기이다)(d)극성의 반응비활성 용매중에서 하기 구조식(Ⅷ)또는 (Ⅸ)의 중간체를 하기구조식(Ⅸ)또는 (Ⅹ)의 벤젠아민으로 폐환시키거나,(위의 식에서 w는 각각 반응성 이탈기이다)(e) 반응비활성 용매중에서 염기존재하에 하기 구조식(ⅩⅡ) 또는 (ⅩⅤ)의 피페라진을 하기 구조식(ⅩⅢ)또는 (ⅩⅣ)의 벤젠유도체로 N-알킬화하거나(위의 식에서 w′는 반응성 이탈기이다)(f) 반응비활성용매중에서 하기 구조식(ⅩⅥ)의 벤젠아민을 하기 구조식(ⅩⅦ)의 시약으로 폐환시켜 하기 구조식(I-a)의 화합물을 얻거나,(위의 식에서 L1과 L2는 모두 반응성 이탈기이다)(g) 반응비활성 용매중에서 하기 구조식(ⅩⅥ)의 벤젠아민을 하기 구조식(ⅩⅧ)의 시약으로 폐환시켜 하기 구조식(I-b)의 화합물을 얻거나,(위의 식에서 L1과 L2는 모두 반응성 이탈기이다)(h) 하기 구조식(ⅩⅨ)의 중간체를 구조식 HC(=NH)NH2(ⅩⅩ)의 아미딘으로 폐환시키고 여기서 수득한 중간체를 구조식 R1-W(ⅩⅩⅠ)(여기서 w는 반응성이탈기)의 시약으로 반응비활성용매중에서 N-알킬화하여 하기 구조식(Ⅰ-a)의 화합물을 얻거나(i) 반응비활성 용매중에서 산 존재하에 하기 구조식(ⅩⅩⅡ)의 중간체를 구조식 (L2)2-CH-CH2-NHR2(ⅩⅩⅢ)의 시약으로 폐환시키고.(위의 식들에 있어서 L1과 L2는 반응성 이탈기이고, D는필요에 따라서는 구조식(Ⅰ)의 화합물을 약제학적으로 허용되는 산으로 처리하여 염형태로 전환시키거나, 역으로는 염을 알칼리로 처리하여 유리염기로 전환시키며/또는 그 입체화학적 이성체를 제조함을 특징으로 하는 제1항 내지 제5항중 어느 한 항에 의한 구조식(Ⅰ)의 화합물의 제조방법.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US36379589A | 1989-06-09 | 1989-06-09 | |
| US07363795 | 1989-06-09 | ||
| BE363,795 | 1989-06-09 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| KR910000714A true KR910000714A (ko) | 1991-01-30 |
| KR0163034B1 KR0163034B1 (ko) | 1998-12-01 |
Family
ID=23431765
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1019900007765A Expired - Fee Related KR0163034B1 (ko) | 1989-06-09 | 1990-05-29 | 항진균성 4-[4-[4-[4-[[2-(2,4-디플루오로페닐)-2-(1h-아졸릴메틸)-1,3-디옥솔란-4-일]메톡시]페닐]-1-피페라지닐]페닐]트리아졸론 및 이미다졸론 |
Country Status (20)
| Country | Link |
|---|---|
| EP (1) | EP0402989B1 (ko) |
| JP (1) | JP2988689B2 (ko) |
| KR (1) | KR0163034B1 (ko) |
| CN (1) | CN1025193C (ko) |
| AT (1) | ATE136305T1 (ko) |
| AU (1) | AU624515B2 (ko) |
| CA (1) | CA2018442C (ko) |
| DE (1) | DE69026311T2 (ko) |
| DK (1) | DK0402989T3 (ko) |
| ES (1) | ES2087886T3 (ko) |
| FI (1) | FI96031C (ko) |
| GR (1) | GR3019686T3 (ko) |
| HU (1) | HU215602B (ko) |
| IE (1) | IE71196B1 (ko) |
| IL (1) | IL94660A (ko) |
| NO (1) | NO175477C (ko) |
| NZ (1) | NZ233502A (ko) |
| PT (1) | PT94320B (ko) |
| RU (1) | RU2056421C1 (ko) |
| ZA (1) | ZA904458B (ko) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL103558A0 (en) * | 1991-10-30 | 1993-03-15 | Schering Corp | Tri-substituted tetrahydrofuran antifungals |
| SK94393A3 (en) * | 1992-09-11 | 1994-08-10 | Thomae Gmbh Dr K | Cyclic derivatives of urea, process for their production and their pharmaceutical agents with the content of those |
| US5464610A (en) * | 1992-10-15 | 1995-11-07 | Schering-Plough Healthcare Products, Inc. | Method for treating onychomycosis |
| US5486625A (en) * | 1994-07-08 | 1996-01-23 | Schering Corporation | Process for the preparation of chiral intermediates useful for the synthesis of antifungal agents |
| US5521186A (en) * | 1994-10-27 | 1996-05-28 | Janssen Pharmaceutica N.V. | Apolipoprotein-β synthesis inhibitors |
| WO1998034934A1 (en) * | 1997-02-11 | 1998-08-13 | Janssen Pharmaceutica N.V. | Amino acid ester containing azole antifungals |
| TW593312B (en) | 1997-07-11 | 2004-06-21 | Janssen Pharmaceutica Nv | 2,4,4-trisubstituted-1,3-dioxolane antifungals |
| KR100342383B1 (ko) * | 1999-06-17 | 2002-12-06 | 한국화학연구원 | 이소옥사졸리딘 유도체, 그의 제조 방법 및 그를 포함하는 살균제 조성물 |
| WO2001007643A1 (en) * | 1999-07-28 | 2001-02-01 | Kaken Pharmaceutical Co., Ltd. | Method for detecting pathogenic microorganism and antimicrobial agent, method for evaluating the drug effect of antimicrobial agent, and antimicrobial agents |
| RU2173994C1 (ru) * | 2000-12-18 | 2001-09-27 | Д-Р Редди'С Лабораторис Лтд. | Лекарственное средство, содержащее флуконазол и способ получения флуконазола |
| RU2265844C1 (ru) * | 2004-05-26 | 2005-12-10 | Волгоградский научно-исследовательский противочумный институт | Способ обнаружения возбудителя кокцидиоидомикоза |
| CN1706834B (zh) * | 2004-06-11 | 2010-04-28 | 横店集团成都分子实验室有限公司 | 具抗真菌活性的三唑醇类新衍生物及制备方法和医药用途 |
| CN102234267A (zh) * | 2010-04-21 | 2011-11-09 | 中国科学院上海药物研究所 | 新型三氮唑类抗真菌化合物、其药物组合物及其制备方法和用途 |
| CN106146480B (zh) * | 2016-07-18 | 2019-08-06 | 山东罗欣药业集团恒欣药业有限公司 | 一种伊曲康唑的制备方法 |
| CN107455342B (zh) * | 2017-08-22 | 2020-03-10 | 沧州市农林科学院 | 三唑酮在提高资源昆虫成活率和/或体重中的应用 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4267179A (en) * | 1978-06-23 | 1981-05-12 | Janssen Pharmaceutica, N.V. | Heterocyclic derivatives of (4-phenylpiperazin-1-yl-aryloxymethyl-1,3-dioxolan-2-yl)methyl-1H-imidazoles and 1H-1,2,4-triazoles |
| US4619931A (en) * | 1983-02-28 | 1986-10-28 | 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 |
| 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 |
| NZ223799A (en) * | 1987-03-25 | 1989-12-21 | Janssen Pharmaceutica Nv | Azolylmethyl-dioxolanylmethoxyphenyl-piperazinyl-phenyl-triazolones and antimicrobial compositions |
-
1990
- 1990-04-30 NZ NZ233502A patent/NZ233502A/xx unknown
- 1990-05-29 KR KR1019900007765A patent/KR0163034B1/ko not_active Expired - Fee Related
- 1990-06-01 DK DK90201447.1T patent/DK0402989T3/da active
- 1990-06-01 DE DE69026311T patent/DE69026311T2/de not_active Expired - Fee Related
- 1990-06-01 AT AT90201447T patent/ATE136305T1/de not_active IP Right Cessation
- 1990-06-01 EP EP90201447A patent/EP0402989B1/en not_active Expired - Lifetime
- 1990-06-01 ES ES90201447T patent/ES2087886T3/es not_active Expired - Lifetime
- 1990-06-07 AU AU56894/90A patent/AU624515B2/en not_active Ceased
- 1990-06-07 IL IL9466090A patent/IL94660A/en not_active IP Right Cessation
- 1990-06-07 JP JP2149741A patent/JP2988689B2/ja not_active Expired - Fee Related
- 1990-06-07 CA CA002018442A patent/CA2018442C/en not_active Expired - Fee Related
- 1990-06-08 ZA ZA904458A patent/ZA904458B/xx unknown
- 1990-06-08 PT PT94320A patent/PT94320B/pt not_active IP Right Cessation
- 1990-06-08 HU HU903767A patent/HU215602B/hu not_active IP Right Cessation
- 1990-06-08 NO NO902553A patent/NO175477C/no not_active IP Right Cessation
- 1990-06-08 IE IE207290A patent/IE71196B1/en not_active IP Right Cessation
- 1990-06-08 FI FI902882A patent/FI96031C/fi active IP Right Grant
- 1990-06-08 RU SU4743999/04A patent/RU2056421C1/ru not_active IP Right Cessation
- 1990-06-09 CN CN90104230A patent/CN1025193C/zh not_active Expired - Fee Related
-
1996
- 1996-04-19 GR GR960401065T patent/GR3019686T3/el unknown
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