KR950701319A - 이소세린 유도체 및 류코트리엔 길항물질로서의 이의 용도(Isoserine derivatives and their use as leukotriene antagonists) - Google Patents
이소세린 유도체 및 류코트리엔 길항물질로서의 이의 용도(Isoserine derivatives and their use as leukotriene antagonists)Info
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- KR950701319A KR950701319A KR1019940703906A KR19940703906A KR950701319A KR 950701319 A KR950701319 A KR 950701319A KR 1019940703906 A KR1019940703906 A KR 1019940703906A KR 19940703906 A KR19940703906 A KR 19940703906A KR 950701319 A KR950701319 A KR 950701319A
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/12—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D215/14—Radicals substituted by oxygen atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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
- C07D215/18—Halogen atoms or nitro radicals
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
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- 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
- A61P11/06—Antiasthmatics
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
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- 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]
-
- 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
-
- 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
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/12—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
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- Veterinary Medicine (AREA)
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- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pulmonology (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Cardiology (AREA)
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- Heart & Thoracic Surgery (AREA)
- Urology & Nephrology (AREA)
- Immunology (AREA)
- Dermatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
본 발명은 종래 비공지의 일반식(Ⅰ)의 화합물에 관한 것이다.
상기식에서, Y는 -CH=CH-이고; R1은 수소 또는 할로겐, 바람직하게는 불소, 염소 또는 브롬이고; R2는 할로겐, 바람직하게는 불소, 염소 또는 브롬, CH3, OCH3, NO2또는 CF3이고, n은 0 내지 3, 바람직하게는 0,1 또는 2이고; A는 산성 그룹, 예를 들어 카복시, 1-H-테트라졸릴 또는 하이드록삼산 그룹이다.
본 발명의 화합물은 라폭시게나제 억제제 및/또는 류코트리엔 길항물질로 의학 및 수의학적 치료에 유용하다.
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (10)
- 일반식(Ⅰ)의 화합물, 이의 약제학적으로 허용되는 무독성염 및 생체내 가수분해가능한 에스테르.상기식에서, Y는 -CH=CH-이고; R1은 수소 또는 할로겐, 바람직하게는 불소, 염소 또는 브롬이고; R2는 할로겐, 바람직하게는 불소, 염소 또는 브롬, CH3, OCH3, NO2또는 CF3이고, n은 0 내지 3, 바람직하게는 0,1 또는 2이고; A는 산성 그룹이다.
- 제1항에 있어서, A가 카복시, 1-H-테트라졸릴 또는 하이드록삼산 그룹인 화합물.
- 제1항에 있어서, 염산, 브롬화수소산, 요오드화수소산, 인산, 황산, 질산, p-톨루엔설폰산, 메탄설폰산, 포름산, 아세트산, 프로피온산, 시트르산, 타타르산 및 말레산과 형성된 염 및 리튬, 나트륨, 칼륨, 마그네슘, 칼슘염과 같은 알칼리 금속염 및 알칼리토금속염 뿐만 아니라 암모니아 및 C1-C6-알킬아민(예 : 트리에틸아민), C1-C6알칸올아민(예 : 디에탄올아민 또는 트리에탄올아민), 프로카인, 사이클로알킬아민(예 : 디사이클로헥실아민), 벤질아민(예 : N-메틸벤질아민, N-에틸벤질아민, N-벤질-β-페네틸아민, N,N′-디벤질에틸렌디아민 또는 디벤질아민) 및 헤테로사이클릭 아민(예 : 모폴린, N-에틸피페리딘)과 같은 적합한 무독성 아민과의 염으로 이루어진 그룹으로부터 선택되는 염.
- 제1항에 있어서, E-(2R, 3R;2S, 3S)-N-3-[2-(7-클로로퀴놀릴)-2-에테닐]-페닐-3-페닐 이소세린; E-(2R, 3R;2S, 3S)-N-3-[2-(7-클로로퀴놀릴)-2-에테닐]-페닐-3-페닐 이소세린; E-(2R, 3R;2S, 3S)-N-3-[2-(7-클로로퀴놀릴)-2-에테닐]-페닐-3-(2, 6-디플루오로페닐) 이소세린; E-(2R, 3R;2S, 3S)-N-3-[2-(7-클로로퀴놀릴)-2-에테닐]-페닐-3-(2, 5-디플루오로페닐) 이소세린; E-(2R, 3R;2S, 3S)-N-3-[2-(7-클로로퀴놀릴)-2-에테닐]-페닐-3-(4-메톡시페닐) 이소세린; E-(2R, 3R;2S, 3S)-N-3-[2-(7-클로로퀴놀릴)-2-에테닐]-페닐-3-(4-클로로페닐) 이소세린; E-(2R, 3R;2S, 3S)-3-(4-메톡시페닐)-N-3-[(2-퀴놀릴)-2-에테닐] 이소세린으로 이루어진 그룹으로부터 선택되는 화합물 및 이의 염 및 순수한 거울상이성질체 형태.
- 제1항에 있어서, E-(-)-(2S,3S)-N-3-[2-(7-클로로퀴놀릴)-2-에테닐]-페닐-3-페닐 이소세린, 나트륨염인 화합물.
- 제1항 내지 제5항중의 어느 한 항에 따른 화합물을 단독으로 또는 필요한 보조제와 함께 함유하는 약제학적 제제.
- 유효량의 제1항 내지 제5항 중의 어느 한항에 따른 화합물을 하나 이상, 필요한 경우 하나 이상의 다른 요법적 활성 성분과 함께 투여함을 특징으로 하는, 치료가 필요한 환자의 치료 방법.
- 제7항에 있어서, 천식, 알레르기, 류마티스성 관절염, 척추관절염, 통풍, 죽상동맥경화증, 증식성 및 염증성 피부장애(예; 건선 및 아토피성 피부염), 만성 염증성 장 질환 및 기타 염증상태, 혈관경련성 협심증, 폐고혈압, 낭포성 섬유증, 성인 호흡장애 증후군, 허혈성 및 재관류 손상을 포함하는 다수의 질병 상태를 치료하고 예방하는 방법.
- a) 일반식(Ⅱ)의 아민을 일반식(Ⅲ)의 화합물과 반응시켜 일반식(Ⅰ)의 화합물을 생성하거나; b) 일반식(Ⅱ)의 아민을 일반식(Ⅳ)의 화합물과 반응시킴을 특징으로 하는, 제1항에 따른 일반식(Ⅰ)의 화합물의 제조방법.상기시에서, Y는 -CH=CH-이고; R1은 수소 또는 할로겐, 바람직하게는 불소, 염소 또는 브롬이고; R2는 할로겐, 바람직하게는 불소, 염소 또는 브롬, CH3, OCH3, NO2또는 CF3이고, n은 0 내지 3, 바람직하게는 0,1 또는 2이고; A는 산성 그룹이고; X는 “우수한 이탈 그룹”을 형성할 수 있는 할로겐 원자(예 : 염소, 브롬 또는 요오드) 또는 알킬- 또는 아릴설포닐옥시 그룹이지만, 알킬설페이트 그룹, 클로로설포닐옥시 그룹, 알킬설파이트 그룹, 모노- 또는 디알킬포스페이트 그룹 또는 니트레이트 그룹과 같은 다른 이탈그룹을 사용할 수도 있고; 또한 산성 작용성 그룹인 A는 임의로 A가 CN 또는 COOH인 일반식(Ⅰ)의 화합물로부터 하기 일반 반응 도식에 따라 제조한다.
- 천식, 알레르기, 류마티스성 관절염, 척추관절염, 통풍, 죽상동맥경화증, 증식성 및 염증성 피부장애(예; 건선 및 아토피성 피부염), 만성 염증성 장 질환 및 기타 염증상태, 혈관경련성 협심증, 폐고혈압, 낭포성 섬유증, 성인 호흡장애 증후군, 허혈성 및 재관류 손상을 포함하는 다수의 질병 상태를 치료하고 예방하는 약제의 제조에 있어서 제1항의 화합물의 용도.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GB929216768A GB9216768D0 (en) | 1992-08-07 | 1992-08-07 | Chemical compounds |
GB9216768.3 | 1992-08-07 | ||
PCT/DK1993/000254 WO1994003431A1 (en) | 1992-08-07 | 1993-08-05 | Isoserine derivatives and their use as leukotriene antagonists |
Publications (1)
Publication Number | Publication Date |
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KR950701319A true KR950701319A (ko) | 1995-03-23 |
Family
ID=10719973
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
KR1019940703906A KR950701319A (ko) | 1992-08-07 | 1993-08-05 | 이소세린 유도체 및 류코트리엔 길항물질로서의 이의 용도(Isoserine derivatives and their use as leukotriene antagonists) |
Country Status (16)
Country | Link |
---|---|
US (1) | US5576438A (ko) |
EP (1) | EP0654026B1 (ko) |
JP (1) | JPH08504749A (ko) |
KR (1) | KR950701319A (ko) |
AT (1) | ATE149030T1 (ko) |
AU (1) | AU666967B2 (ko) |
CA (1) | CA2134565A1 (ko) |
DE (1) | DE69308212T2 (ko) |
DK (1) | DK0654026T3 (ko) |
ES (1) | ES2100550T3 (ko) |
FI (1) | FI950515A (ko) |
GB (1) | GB9216768D0 (ko) |
GR (1) | GR3023069T3 (ko) |
NZ (1) | NZ254741A (ko) |
RU (1) | RU2126389C1 (ko) |
WO (1) | WO1994003431A1 (ko) |
Families Citing this family (5)
Publication number | Priority date | Publication date | Assignee | Title |
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GB9414590D0 (en) * | 1994-07-20 | 1994-09-07 | Leo Pharm Prod Ltd | Chemical compounds |
GB9524185D0 (en) * | 1995-11-27 | 1996-01-31 | Leo Pharm Prod Ltd | Substituted diols |
FR2751969B1 (fr) * | 1996-08-01 | 1998-12-04 | Centre Nat Rech Scient | Composes activateurs du canal cftr, et compositions pharmaceutiques les contenant |
KR20000044978A (ko) * | 1998-12-30 | 2000-07-15 | 성재갑 | 각질 박리 촉진용 조성물 |
CN103044277B (zh) * | 2013-01-07 | 2015-04-08 | 华东师范大学 | 光学纯α-羟基-β-氨基丙酸酯衍生物的制备方法 |
Family Cites Families (7)
Publication number | Priority date | Publication date | Assignee | Title |
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ES8801209A1 (es) * | 1985-06-18 | 1988-01-01 | Merck Frosst Canada Inc | Un procedimiento para la preparacion de quinolinas 2-sustituidas. |
US4962203A (en) * | 1985-06-18 | 1990-10-09 | Merck Frost Canada, Inc. | 2-substituted quinolines useful as leukotriene antagonists |
US4918081A (en) * | 1988-06-20 | 1990-04-17 | Rorer Pharmaceutical Corp. | Quinoline derivatives and use thereof as antagonists of leukotriene d4 |
US5102881A (en) * | 1988-06-27 | 1992-04-07 | Merck Frosst Canada, Inc. | Quinoline ether alkanoic acids |
GB8919504D0 (en) * | 1989-08-29 | 1989-10-11 | Leo Pharm Prod Ltd | Chemical compounds |
IE920499A1 (en) * | 1991-02-21 | 1992-08-26 | Merck Frosst Canada Inc | Quinoline-containing ketoacids as leukotriene antagonists |
US5270324A (en) * | 1992-04-10 | 1993-12-14 | Merck Frosst Canada, Inc. | Fluorinated hydroxyalkylquinoline acids as leukotriene antagonists |
-
1992
- 1992-08-07 GB GB929216768A patent/GB9216768D0/en active Pending
-
1993
- 1993-08-05 NZ NZ254741A patent/NZ254741A/en unknown
- 1993-08-05 KR KR1019940703906A patent/KR950701319A/ko active IP Right Grant
- 1993-08-05 DK DK93917564.2T patent/DK0654026T3/da active
- 1993-08-05 EP EP93917564A patent/EP0654026B1/en not_active Expired - Lifetime
- 1993-08-05 US US08/335,860 patent/US5576438A/en not_active Expired - Fee Related
- 1993-08-05 AT AT93917564T patent/ATE149030T1/de not_active IP Right Cessation
- 1993-08-05 RU RU94046453A patent/RU2126389C1/ru active
- 1993-08-05 ES ES93917564T patent/ES2100550T3/es not_active Expired - Lifetime
- 1993-08-05 CA CA002134565A patent/CA2134565A1/en not_active Abandoned
- 1993-08-05 DE DE69308212T patent/DE69308212T2/de not_active Expired - Fee Related
- 1993-08-05 JP JP6504910A patent/JPH08504749A/ja active Pending
- 1993-08-05 WO PCT/DK1993/000254 patent/WO1994003431A1/en active IP Right Grant
- 1993-08-05 AU AU46982/93A patent/AU666967B2/en not_active Ceased
-
1995
- 1995-02-06 FI FI950515A patent/FI950515A/fi unknown
-
1997
- 1997-04-08 GR GR970400737T patent/GR3023069T3/el unknown
Also Published As
Publication number | Publication date |
---|---|
JPH08504749A (ja) | 1996-05-21 |
RU94046453A (ru) | 1996-09-27 |
CA2134565A1 (en) | 1994-02-17 |
US5576438A (en) | 1996-11-19 |
EP0654026B1 (en) | 1997-02-19 |
GR3023069T3 (en) | 1997-07-30 |
WO1994003431A1 (en) | 1994-02-17 |
FI950515A0 (fi) | 1995-02-06 |
ATE149030T1 (de) | 1997-03-15 |
DE69308212D1 (de) | 1997-03-27 |
DE69308212T2 (de) | 1997-09-18 |
FI950515A (fi) | 1995-02-06 |
RU2126389C1 (ru) | 1999-02-20 |
AU666967B2 (en) | 1996-02-29 |
NZ254741A (en) | 1997-07-27 |
ES2100550T3 (es) | 1997-06-16 |
DK0654026T3 (da) | 1997-07-14 |
AU4698293A (en) | 1994-03-03 |
GB9216768D0 (en) | 1992-09-23 |
EP0654026A1 (en) | 1995-05-24 |
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