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KR970020107A - Pharmaceutical preparations for the treatment of acute and chronic inflammatory diseases - Google Patents

Pharmaceutical preparations for the treatment of acute and chronic inflammatory diseases Download PDF

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Publication number
KR970020107A
KR970020107A KR1019960048601A KR19960048601A KR970020107A KR 970020107 A KR970020107 A KR 970020107A KR 1019960048601 A KR1019960048601 A KR 1019960048601A KR 19960048601 A KR19960048601 A KR 19960048601A KR 970020107 A KR970020107 A KR 970020107A
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KR
South Korea
Prior art keywords
fluoro
chloro
formula
hydrogen
substituent
Prior art date
Application number
KR1019960048601A
Other languages
Korean (ko)
Inventor
노보루 아까사까
고지 아까이
히데히로 기따야마
미사오 쓰바끼하라
나나 와끼따
가쯔히로 가또
다다노리 나카쓰세
존 비 쳉
안토니 마팻
존 더블유 왓슨
Original Assignee
노보루 아까사까
고지 아까이
히데히로 기따야마
가부시키가이샤 나와리 쇼오지
원본미기재
와꼬 쥰야꾸 고오교 가부시끼가이샤
만담 가부시끼가이샤
스피겔 알렌 제이
화이자 인코포레이티드
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Priority claimed from JP24012595A external-priority patent/JPH0975310A/en
Priority claimed from JP7303258A external-priority patent/JPH09108259A/en
Priority claimed from JP7281862A external-priority patent/JPH09122083A/en
Application filed by 노보루 아까사까, 고지 아까이, 히데히로 기따야마, 가부시키가이샤 나와리 쇼오지, 원본미기재, 와꼬 쥰야꾸 고오교 가부시끼가이샤, 만담 가부시끼가이샤, 스피겔 알렌 제이, 화이자 인코포레이티드 filed Critical 노보루 아까사까
Publication of KR970020107A publication Critical patent/KR970020107A/en

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    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

본 발명은 포유 동물, 특히 사람에 있어서 염증 질환을 치료하는 방법에 관한 것으로, 하기 화학식(1)의 화합물 또는 약제학적으로 허용가능한 이의 산 부가염의 항 염증성 양을 상기 포유 동물에게 투여함을 포함한다:The present invention relates to a method of treating an inflammatory disease in a mammal, in particular a human, comprising administering to said mammal an anti-inflammatory amount of a compound of formula (1) or a pharmaceutically acceptable acid addition salt thereof: :

상기 식에서, R3는 1-피페리딜, 1-(3-인돌릴)에틸, (C1-C4)-알킬, 페닐, 벤질, 1-(1-페닐에틸) 또는 단치환된 벤질이고, 여기서 치환체는 클로로, 플루오로, 메틸 또는 메톡시이고 상기 치환체는 방향족 환상에 있고; R4는 비사이클로[2.2.1]헵트-2-일 또는 하기 화학식(2)이고Wherein R 3 is 1-piperidyl, 1- (3-indolyl) ethyl, (C 1 -C 4 ) -alkyl, phenyl, benzyl, 1- (1-phenylethyl) or monosubstituted benzyl Wherein the substituent is chloro, fluoro, methyl or methoxy and the substituent is in the aromatic ring; R 4 is bicyclo [2.2.1] hept-2-yl or formula (2)

여기서 Y는 수소, 플루오로 또는 클로로이고; X는 수소, 플루오로, 클로로, 메톡시, 트리플루오로메틸, 시아노, 카복시 메틸카바모일, 디메틸-카바모일 또는 카보(C1-C4)알콕시이다.Wherein Y is hydrogen, fluoro or chloro; X is hydrogen, fluoro, chloro, methoxy, trifluoromethyl, cyano, carboxy methylcarbamoyl, dimethyl-carbamoyl or carbo (C 1 -C 4 ) alkoxy.

Description

급성 및 만성 염증 질환을 치료하기 위한 약학적 제제Pharmaceutical preparations for the treatment of acute and chronic inflammatory diseases

본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음Since this is an open matter, no full text was included.

Claims (6)

화학식(1) 또는 약학적으로 허용가능한 이의 산 부가염의 항-염증성 양을 포유 동물, 특히 사람에 투여함을 포함하는, 상기 포유동물에서 포스포디에스터라아제 제IV형 또는 종양 괴사 인자의 생성을 억제하는 방법.Production of phosphodiesterase type IV or tumor necrosis factor in the mammal, comprising administering to the mammal, in particular, an anti-inflammatory amount of formula (1) or a pharmaceutically acceptable acid addition salt thereof How to suppress. 상기 식에서, R3는 1-피페리딜, 1-(3-인돌릴)에틸, (C1-C4)-알킬, 페닐, 벤질, 1-(1-페닐에틸) 또는 단치환된 벤질이고, 여기서 치환체는 클로로, 플루오로, 메틸 또는 메톡시이고 상기 치환체는 방향족 환상에 있고; R4는 비사이클로[2.2.1]헵트-2-일 또는 하기 화학식(2)의 그룹이고Wherein R 3 is 1-piperidyl, 1- (3-indolyl) ethyl, (C 1 -C 4 ) -alkyl, phenyl, benzyl, 1- (1-phenylethyl) or monosubstituted benzyl Wherein the substituent is chloro, fluoro, methyl or methoxy and the substituent is in the aromatic ring; R 4 is bicyclo [2.2.1] hept-2-yl or a group of formula (2) 여기서 Y는 수소, 플루오로 또는 클로로이고; X는 수소, 플루오로, 클로로, 메톡시, 트리플루오로메틸, 시아노, 카복시 메틸카바모일, 디에틸-카바모일 또는 카보(C1-C4)알콕시이다.Wherein Y is hydrogen, fluoro or chloro; X is hydrogen, fluoro, chloro, methoxy, trifluoromethyl, cyano, carboxy methylcarbamoyl, diethyl-carbamoyl or carbo (C 1 -C 4 ) alkoxy. 제1항에 있어서, R3가 1-피페리딜 또는 1-(3-인돌릴)에틸인 화합물이 투여되는 방법.The method of claim 1, wherein the compound is administered wherein R 3 is 1-piperidyl or 1- (3-indolyl) ethyl. 제1항에 있어서, R3가 1-(3-인돌릴)에틸이고, R4가 비사이클로[2.2.1]헵트-2-일인 화합물이 투여되는 방법.The method of claim 1, wherein R 3 is 1- (3-indolyl) ethyl and R 4 is bicyclo [2.2.1] hept-2-yl. 제1항에 있어서, R4가 하기 화학식(2)인 화합물이 투여되는 방법:The method of claim 1, wherein a compound of which R 4 is of formula (2) is administered: 여기서, Y는 수소이고, X는 카보(C1-C4)알콕시이다.Wherein Y is hydrogen and X is carbo (C 1 -C 4 ) alkoxy. 제1항에 있어서, R3가 1-피페리딜이고, R4가 하기 화학식(3)인 화합물이 투여되는 방법:The method of claim 1, wherein a compound is administered wherein R 3 is 1-piperidyl and R 4 is formula (3): 제1항에 있어서, 하기 화힉식(1)의 화합물 또는 약학적으로 허용가능한 이의 산 부가염의 유효량을 환자에게 투여함을 포함하여, 천식, 만성 기관지염, 아토피성피부염, 담마진, 알러지성 비염, 알러지성 결막염, 춘계 결막염, 코시노필 육아종, 건선, 류마티스 관절염, 패혈성 쇼크, 궤양성 대장염, 크론 질환, 심근 및 뇌의 재관류성 손상, 만성 사구체신염, 내독소성 쇼크, 성인 호흡곤란 증후, 요붕증, 다발성 경화증 및 중추신경계 장애, 뿐만 아니라 TNF 생성에 관련된 다른 질환으로 구성된 그룹에서 선택되는 증상을 치료 또는 예방 하는 방법:2. The method of claim 1, comprising administering to the patient an effective amount of a compound of formula (1) or a pharmaceutically acceptable acid addition salt thereof: Conjunctivitis, spring conjunctivitis, cosinophil granulomas, psoriasis, rheumatoid arthritis, septic shock, ulcerative colitis, Crohn's disease, myocardial and brain reperfusion injury, chronic glomerulonephritis, endotoxin shock, adult respiratory distress syndrome, diabetes insipidus, How to treat or prevent symptoms selected from the group consisting of multiple sclerosis and central nervous system disorders, as well as other diseases related to TNF production: 상기 식에서, R3는 1-피페리딜, 1-(3-인돌릴)에틸, (C1-C4)-알킬, 페닐, 벤질, 1-(1-페닐에틸) 또는 단치환된 벤질이고, 여기서 치환체는 클로로, 플루오로, 메틸 또는 메톡시이고 상기 치환체는 방향족 환상에 있고; R4는 비사이클로[2.2.1]헵트-2-일 또는 하기 화학식(2)의 그룹이고,Wherein R 3 is 1-piperidyl, 1- (3-indolyl) ethyl, (C 1 -C 4 ) -alkyl, phenyl, benzyl, 1- (1-phenylethyl) or monosubstituted benzyl Wherein the substituent is chloro, fluoro, methyl or methoxy and the substituent is in the aromatic ring; R 4 is bicyclo [2.2.1] hept-2-yl or a group of formula (2) 여기서 Y는 수소, 플루오로 또는 클로로이고; X는 수소, 플루오로, 클로로, 메톡시, 트리플루오로메틸, 시아노, 카복시, 메틸카바모일, 디메틸-카바모일 또는 카보(C1-C4)알콕시이다.Wherein Y is hydrogen, fluoro or chloro; X is hydrogen, fluoro, chloro, methoxy, trifluoromethyl, cyano, carboxy, methylcarbamoyl, dimethyl-carbamoyl or carbo (C 1 -C 4 ) alkoxy. ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.※ Note: The disclosure is based on the initial application.
KR1019960048601A 1995-09-19 1996-10-25 Pharmaceutical preparations for the treatment of acute and chronic inflammatory diseases KR970020107A (en)

Applications Claiming Priority (10)

Application Number Priority Date Filing Date Title
JP24012595A JPH0975310A (en) 1995-09-19 1995-09-19 Patient monitoring device
JP7-240125 1995-09-19
JP95-286685 1995-10-05
JP28668595 1995-10-05
JP7303258A JPH09108259A (en) 1995-10-18 1995-10-18 Eye mask
JP7-303258 1995-10-18
US8802495P 1995-10-27 1995-10-27
US60/088,024 1995-10-27
JP7281862A JPH09122083A (en) 1995-10-30 1995-10-30 Patient monitoring apparatus mountable regularly
JP7-281862 1995-10-30

Publications (1)

Publication Number Publication Date
KR970020107A true KR970020107A (en) 1997-05-28

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ID=66315612

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Application Number Title Priority Date Filing Date
KR1019960048601A KR970020107A (en) 1995-09-19 1996-10-25 Pharmaceutical preparations for the treatment of acute and chronic inflammatory diseases

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KR (1) KR970020107A (en)

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