KR940014396A - 이미다조피리딘 - Google Patents
이미다조피리딘 Download PDFInfo
- Publication number
- KR940014396A KR940014396A KR1019930027926A KR930027926A KR940014396A KR 940014396 A KR940014396 A KR 940014396A KR 1019930027926 A KR1019930027926 A KR 1019930027926A KR 930027926 A KR930027926 A KR 930027926A KR 940014396 A KR940014396 A KR 940014396A
- Authority
- KR
- South Korea
- Prior art keywords
- formula
- compound
- tetrazolyl
- cooh
- pyridine
- Prior art date
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
-
- 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
- A61P9/12—Antihypertensives
Abstract
하기 일반식(Ⅰ)의 신규한 이미다조피리딘 유도체 및 그의 염은 안지오텐신(Ⅱ)에 대해 길항 성질을 나타내며, 고혈압, 알로스테론증, 심부전증 및 증가된 안내압, 및 중추 신경계 질환을 치료하는데 사용할 수 있다:
상기식에서, R은
이고, R1내지 R4, X 및 Y는 제1항에 정의된 바와같다.
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (8)
- 하기 일반식(Ⅰ)의 이미다조피리딘 유도체 및 그의 염;상기식에서, R은R1은 C3-C7-사이클로알킬-CnH2n-또는 C1-C6-알킬이고, 여기에서 CH2그룹은 O 또는 S에 의해서 치환되고, R2는 H, COOR6, CN, NO2, NH2, NHCOR5, NHSO2R5또는 1H-5-테트라졸릴이고, R3는 -CmH2m-CN, C2-C6-알키닐, -CmH2m-Ar, -CmH2m-CO-R5, -CmH2m-CO-Ar, -CmH2m-Het 또는 -CmH2m-CO-Het이고, R4는 H 또는 Hal이고, R5는 C1-C6알킬이고, 여기에서 하나이상의 H원자는 또한 F로 치환될 수 있고, R6는 H 또는 A이고, X는 존재하지 않거나 또는 -NH-CO-, -CO-NH-, -O-CH(COOH)-, -NH-CH(COOH)-, -NA-CH(COOH)-, -CH=C(COOH)-, -CH=C(N)- 또는 -CH=C(1H-5-테트라졸릴)-이고, Y는 O 또는 S이고, A는 탄소수 1 내지 6의 알킬이고, Ar은 비치환된 페닐 그룹, 또는 Hal, R5, OH, OR5, COOR6, CN, NO2, NH2, NHA, N(A)2, HNCOR5, NHCOOA, NHSO2R5및/또는 1H-5-테트라졸릴로 일치환 또는 이치환된 페닐 그룹이고, Het는 1 내지 4개의 N, O 및/또는 S원자를 갖는 5- 또는 6-원 헤테로방향족 라디칼이고, 이때 사기 라디칼은 또한 벤젠 또는 피리딘 고리와 융합될 수 있고, Hal은 F, Cl, Br 또는 I이고, m은 1, 2, 3, 4, 5 또는 6이고, n은 0, 1, 2, 3, 4, 5 또는 6이다.
- a) 2-사이클로프로필-4, 5-디하이드로-5-(o-메톡시카보닐벤질)-4-옥소-3-[2′-(1H-5-테트라졸릴)비페닐릴-4-메틸]-3H-이미다조[4, 5-c]피리딘; b) 2-사이클로프로필-5-(o-메톡시카보닐벤질)-4, 5-디하이드로-4-옥소-3-[2′-(1H-5-테트라졸릴)비페닐릴-4-메틸]-3H-이미다조[4, 5-c]피리딘; 또는 c) 2-사이클로펜틸-4, 5-디하이드로-5-(o-메톡시카보닐벤질)-4-옥소-3-[2′-(1H-5-테트라졸릴)비페닐릴-4-메틸]-3H-이미다조[4, 5-c]피리딘; 또는 d) 2-사이클로프로필-5-(o-클로로벤질)-4, 5-디하이드로-4-옥소-3-[2′-(1H-5-테트라졸릴)비페닐릴-4-메틸]-3H-이미다조[4, 5-c]피리딘.
- (a) 하기 일반식(Ⅱ)의 화합물을 하기 일반식(Ⅲ)의 화합물과 반응시키거나, (b) 하기 일반식(Ⅳ)의 화합물을 환화제로 처리하거나, (c) X가 -NH-CO- 또는-CO-NH-인 일반식(Ⅰ)의 화합물을 제조하기 위해, 하기 일반식(Ⅴ)의 화합물 또는 그의 반응성 유도체를 하기 일반식(Ⅵ)의 화합물 또는 그의 반응성 유도체와 반응시키거나, (d) 일반식(Ⅰ) 화합물의 반응성 유도체들중 하나를 가용매분해제 또는 가수소분해제로 처리하여 그로부터 일반식(Ⅰ) 화합물의 유리시키거나, (e) 일반식(Ⅰ)에서 라디칼 R3대신 H원자를 함유하는 상응 화합물을 일반식 E-R3(여기서, E 및 R3는 하기 정의된 바와같다)의 화합물로 처리하고/하거나, 일반식(Ⅰ)의 화합물에서 하나이상의 라디칼 R 및/또는 R2를 하나이상의 다른 라디칼 R 및/또는 R2로 전환시키고/시키거나 일반식(Ⅰ)의 염기 또는 산을 그의 염들중 하나로 전환시킴을 특징으로 하는, 제1항에 따른 일반식(Ⅰ)의 이미다조피리딘 및 그의 염의 제조방법;상기식들에서, R, R1, R2, R3, R4, X 및 Y는 제1항에서 정의한 바와 같고, E는 Cl, Br, I, 유리 OH 그룹 또는 반응성을 갖도록 작용적으로 변형된 OH 그룹이고, R7은 R1-CO 또는 H이고, R8은 H(R7이 R1-CO인 경우) 또는 R1-CO(R7이 H인 경우)이고, X1은 NH2또는 COOH이고, X2는 COOH(X1이 NH2인 경우) 또는 NH2(X1이 COOH인 경우)이다.
- 제1항에 따른 일반식(Ⅰ)의 화합물 및/또는 그의 생리학적으로 허용가능한 산 부가염들중 하나를 적어도 하나의 고체, 액체 또는 반액체 부형제 또는 보조제와 함께 적합한 투여 형태로 배합시킴을 특징으로 하는, 약학 제형의 제조방법.
- 제1항에 따른 일반식(Ⅰ)의 적어도 한 화합물 및/또는 그의 생리학적으로 허용가능한 산 부가염들중 하나를 함유함을 특징으로 하는 약학 제형.
- 질병 억제를 위한 제1항에 따른 일반식(Ⅰ)의 화합물 및 그의 생리학적으로 허용가능한 산 부가염.
- 약물의 제조를 위한, 제1항에 따른 일반식(Ⅰ)의 화합물 및/또는 그의 생리학적으로 허용가능한 산부가염의 용도.
- 질병 억제를 위한, 제1항에 따른 일반식(Ⅰ)의 화합물 및/또는 그의 생리학적으로 허용가능한 산 부가염의 용도.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
DEP4242459.3 | 1992-12-16 | ||
DE4242459A DE4242459A1 (de) | 1992-12-16 | 1992-12-16 | Imidazopyridine |
Publications (1)
Publication Number | Publication Date |
---|---|
KR940014396A true KR940014396A (ko) | 1994-07-18 |
Family
ID=6475425
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
KR1019930027926A KR940014396A (ko) | 1992-12-16 | 1993-12-15 | 이미다조피리딘 |
Country Status (16)
Country | Link |
---|---|
US (1) | US5389642A (ko) |
EP (1) | EP0602521A1 (ko) |
JP (1) | JPH06228137A (ko) |
KR (1) | KR940014396A (ko) |
CN (1) | CN1094044A (ko) |
AU (1) | AU665877B2 (ko) |
CA (1) | CA2111362A1 (ko) |
CZ (1) | CZ275893A3 (ko) |
DE (1) | DE4242459A1 (ko) |
HU (1) | HUT66037A (ko) |
MX (1) | MX9307940A (ko) |
NO (1) | NO934622L (ko) |
PL (1) | PL301483A1 (ko) |
SK (1) | SK143593A3 (ko) |
TW (1) | TW256837B (ko) |
ZA (1) | ZA939433B (ko) |
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US4880804A (en) * | 1988-01-07 | 1989-11-14 | E. I. Du Pont De Nemours And Company | Angiotensin II receptor blocking benzimidazoles |
US5157026A (en) * | 1989-05-30 | 1992-10-20 | Merck & Co., Inc. | Oxo-purines as angiotensin II antagonists |
US5102880A (en) * | 1989-05-30 | 1992-04-07 | Merck & Co., Inc. | Substituted imidazo-fused 6-membered heterocycles as angiotensin II antagonists |
IL94390A (en) * | 1989-05-30 | 1996-03-31 | Merck & Co Inc | The 6-membered trans-nitrogen-containing heterocycles are compressed with imidazo and pharmaceutical preparations containing them |
US5223499A (en) * | 1989-05-30 | 1993-06-29 | Merck & Co., Inc. | 6-amino substituted imidazo[4,5-bipyridines as angiotensin II antagonists |
DE4110019C2 (de) * | 1991-03-27 | 2000-04-13 | Merck Patent Gmbh | Imidazopyridine, Verfahren zu ihrer Herstellung und diese enthaltende pharmazeutische Zubereitungen |
DE4141788A1 (de) * | 1991-12-18 | 1993-06-24 | Merck Patent Gmbh | Imidazopyridine |
DE4211474A1 (de) * | 1992-04-06 | 1993-10-07 | Merck Patent Gmbh | Imidazopyridine |
DE4305602A1 (de) * | 1992-06-17 | 1993-12-23 | Merck Patent Gmbh | Imidazopyridine |
-
1992
- 1992-12-16 DE DE4242459A patent/DE4242459A1/de not_active Withdrawn
-
1993
- 1993-12-08 EP EP93119780A patent/EP0602521A1/de not_active Withdrawn
- 1993-12-09 AU AU52286/93A patent/AU665877B2/en not_active Expired - Fee Related
- 1993-12-14 CA CA002111362A patent/CA2111362A1/en not_active Abandoned
- 1993-12-14 TW TW082110590A patent/TW256837B/zh not_active IP Right Cessation
- 1993-12-14 PL PL93301483A patent/PL301483A1/xx unknown
- 1993-12-14 MX MX9307940A patent/MX9307940A/es unknown
- 1993-12-15 KR KR1019930027926A patent/KR940014396A/ko not_active Application Discontinuation
- 1993-12-15 CN CN93120837A patent/CN1094044A/zh active Pending
- 1993-12-15 NO NO934622A patent/NO934622L/no unknown
- 1993-12-15 HU HU9303601A patent/HUT66037A/hu unknown
- 1993-12-15 CZ CZ932758A patent/CZ275893A3/cs unknown
- 1993-12-15 JP JP5315298A patent/JPH06228137A/ja active Pending
- 1993-12-15 ZA ZA939433A patent/ZA939433B/xx unknown
- 1993-12-16 US US08/167,369 patent/US5389642A/en not_active Expired - Fee Related
- 1993-12-16 SK SK1435-93A patent/SK143593A3/sk unknown
Also Published As
Publication number | Publication date |
---|---|
NO934622D0 (no) | 1993-12-15 |
AU665877B2 (en) | 1996-01-18 |
TW256837B (ko) | 1995-09-11 |
MX9307940A (es) | 1994-08-31 |
EP0602521A1 (de) | 1994-06-22 |
HUT66037A (en) | 1994-09-28 |
NO934622L (no) | 1994-06-17 |
SK143593A3 (en) | 1994-12-07 |
HU9303601D0 (en) | 1994-04-28 |
PL301483A1 (en) | 1994-06-27 |
CZ275893A3 (en) | 1994-07-13 |
CA2111362A1 (en) | 1994-06-17 |
ZA939433B (en) | 1994-08-09 |
DE4242459A1 (de) | 1994-06-23 |
CN1094044A (zh) | 1994-10-26 |
JPH06228137A (ja) | 1994-08-16 |
AU5228693A (en) | 1994-06-30 |
US5389642A (en) | 1995-02-14 |
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