KR920021534A - 류코트리엔 b_4길항 물질 - Google Patents
류코트리엔 b_4길항 물질 Download PDFInfo
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Abstract
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Claims (24)
- 하기 일반식[Ⅰ]으로 표시되는 화합물 또는 이것의 약제학적 허용성염:상기식 중에서 A는 C1-C5알킬렌쇄이고; B는 페닐렌 또는 탄소원자 및 1 또는 2개의 질소원자로 구성된 6원 헤테로 방향족기이고, 그리고 B는 C1-C5알킬기, C1-C5알콕시기, 히드록실기, 카르복실기, 니트로기 및 할로겐 원자로 구성된 군중에서 선택된 1 또는 2개의 치환체로 임의로 치환되며; R1은 C1-C5알킬기이고; R2는 히드록실기 또는 C1-C5알콕시기; R3및 R4는 각각 별도의 수소원자, C1-C5알킬기, C2-C5알케닐기 또는 C2-C5알키닐기이고; R5는 수소원자, C1-C5알킬기 또는 히드록실 C1-C5알킬기이고; R6은 -X-Y-Z-R6'일반식의 기이고; 이 식중에서 X는 페닐렌기 또는 단고리 5-6원 헤테로 방향족기이고, 그리고 X는 C1-C5알킬기, 히드록실기, 카르복실기, 니트로기 및 할로겐 원자로 구성된 군중에서 선택된 1 또는 2개의 치환체로 임의로 치환되고; Y는 단일 결합 또는 산소원자이고; Z는 단일 결합 또는 C1-C5알킬렌 쇄이고; 단 Y가 산소원자일때, X는 페닐렌기이고 Z는 C1-C5알킬렌쇄이고; R6'는 COOR7기, CONR8R9기, CONHCHR20(CH2)7COOR7기, CONHCHR20(CH2)nCONR8R9기, CONHCHR20CONHCHR22CO2R7기 또는 설파모일기로 표시되는 기이고, 여기에서 R7은 수소원자, 벤질기, C2-C5알킬기 또는 단고리 5-6원 헤테로방향족 기를 포함하는 아미노헤테로 방향족기로 치환된 C1-C5알킬기이고; R8및 R9은 각각 독립적으로 수소원자, C1-C5알킬기, 히드록시 C1-C5알킬기, 히드록시에틸피리딜기 또는 히드록시 에틸티아졸기, 또는 피롤리디노, 피페리디노, 또는 모르포리노기를 나타내는 일반식 -NR8R9의 기이고; R20은 수소원자, 히드록실기, C1-C5알킬기, 페닐기, 히드록시페닐기, 벤질기, 히드록시 벤질기 또는, 치환된 C1-C5알킬기(여기에서 치환체는 히드록실기, C1-C5알콕시기, 머캅토기, 메틸티오기, 아미노기, 인돌릴기, 이미다졸릴기, 카르복실기, C1-C5알콕시카르보닐기, 카르바모일기 및 구아니디노기로 구성된군 중에서 선택된다)이고; n은 0, 1, 2, 3, 4 또는 5이고; 그리고 R22은 수소원자, C1-C5알킬기 또는 C1-C5히드록시알킬기이며; 또는 R6는 CHR20(CH2)nCOOR7기, CH2CHR20COOR7기, CHR20(CH2)nCONR8R9기, CH2CHR20CONR8R9기, CHR20(CH2)nOH기, CR20R22(CH2)nOH기, CH2CHR20OH기, 또는 CHR20CONHCHR22CO2R7기로 표시되는 기이고,기는 아제티디노기, 피롤리디노기, 피페리디노기 또는 호모피페리디노기를 나타내고, 이것은 히드록실기, C1-C5히드록시알킬기, 카르복실기, C1-C5알콕시 카르보닐기 및 벤질옥시 카르보닐기로 구성된 군중에서 선택된 1 내지 2개의 치환체로 임의로 치환된다.
- 제1항에 있어서, R1이 메틸기이고 R2가 히드록실기인 것을 특징으로 하는 화합물.
- 제1항에 있어서, R3가 수소원자이고 A가 메틸렌기인 것을 특징으로 하는 화합물.
- 제1항에 있어서, R1이 메틸기, R2이 히드록실기, R3가 수소원자이고 A가 메틸렌기인 것을 특징으로 하는 화합물.
- 제4항에 있어서, B가 2,6-피리딘디일, 2,4-피리미딘디일 또는 2,6-피리딘디일 N-옥사이드기인 것을 특징으로 하는 화합물.
- 제4항에 있어서, R6가 일반식 X-Y-Z-R6'(이 식중에서 X, Y, Z, 및 R6'는 제1항에 정의된 바와 같다)인 것을 특징으로 하는 화합물.
- 제4항에 있어서, R6가 일반식 CHR20(CH2)nCOOR7(이 식중에서 R20, R7및 n은 제1항에 정의된 바와 같다)인 것을 특징으로 하는 화합물.
- 제4항에 있어서, R6가 일반식 CHR20(CH2)nCONR8R9(이 식중에서 R20, R8, R9및 n은 제1항에 정의된 바와 같다) 인 것을 특징으로 하는 화합물.
- 제4항에 있어서, R6가 일반식 CHR20CONHCHR22CO2R7기(이 식중에서, R20, R22, R7및 n은 제1항에 정의된 바와 같다)인 것을 특징으로 하는 화합물.
- 제4항에 있어서, R4가 에틸기인 것을 특징으로 하는 화합물.
- 제5항에 있어서, X가 2,6-피리딘디일기인 것을 특징으로 하는 화합물.
- 제10항에 있어서, R6'가 일반식 COOR7기 (이 식중에서 R7은 제1항에 정의된 바와 같다) 인 것을 특징으로 하는 화합물.
- 제10항에 있어서, R6'가 카르복실기인 것을 특징으로 하는 화합물.
- 제10항에 있어서, R6'가 일반식 CONHCHR20(CH2)nCOOR7기(이 식중에서 R20, R7및 n은 제1항에 정의된 바와 같다)인 것을 특징으로 하는 화합물.
- 하기 구조식의 화합물:
- 하기 구조식의 화합물:
- 하기 구조식의 화합물:
- 하기 구조식의 화합물:
- 하기 구조식의 화합물:
- 하기 구조식의 화합물:
- (a) 하기 일반식[Ⅱ]화합물과 [Ⅲ]화합물을 반응시켜[Ⅳ]화합물을 생성하거나: (b) 하기 일반식[Ⅴ]화합물을 가수분해하여 [Ⅵ]화합물을 생성하거나: (c) 하기 일반식[Ⅶ]화합물을 [Ⅷ]화합물과 반응시켜 [Ⅸ]화합물을 생성하거나: (d) 하기 일반식[Ⅸ]화합물을 가수분해하여 [Ⅹ]화합물을 생성하거나: (e) 하기 일반식[XI]화합물을 산화하여 [XII]화합물을 생성하거나: 또는 (f) 하기 일반식[XIII]화합물을 가수분해하여 [XIV]화합물을 생성하는 것을 포함하는 제1항에 청구된 화합물[Ⅰ]을 제조하는 방법.(상기 식중, R1, R2, R3, R4, R5, R6'', R20, R22, n, A, B, X, Y, 및 Z는 제1항에 정의된 바와 같고, R11은 R6'에서 정의된 것과 동일하나, 자유 카르복실기는 포함되지 않으며, R12는 X-Y-Z-COOR7', X-Y-Z-CONHCHR20(CH2)nCOOR7', X-Y-Z-CONHCHR20CONHCHR22CO2R7', CHR20(CH2)nCOOR7', CH2CHR20COOR7', 또는 CHR20CONHCHR22COOR7'로 표시되는 기이고, R7'는 R7에서 정의된 것과 동일하나, 수소원자를 포함하지 않으며, R13은 X-Y-Z-COOH, X-Y-Y-CONHCHR20(CH2)nCOOH, X-Y-X-CONHCHR20CONHCHR22CO2H, CHR20(CH2)nCOOH, CH2CHR20COOH, 또는 CHR20CONHCHR22COOH로 표시되는 기이며: R14는 (CH2)nCOOR7', 또는 CONHCHR22COOR7'로 표시되는 기이며: R15는 COOR7'CONHCHR20(CH2)nCOOR7', 또는 CONHCHR20CONHCHR22CO2R7'로 표시되는 기이며: R16는 COOH, CONHCHR20(CH2)nCOOH, 또는 CONHCHR20CONHCHR22CO2H로 표시되는 기이며: R26는 (CH2)nCOOH, 또는 CONHCHR22COOH로 표시되는 기이다.
- 활성성분으로서 제1항의 화합물 또는 이것의 약제학적 허용성염의 유효량 및 약제학적 허용성 담체 또는 희석제를 포함하는 항염증제 또는 항알레르기제로서 유용한 약제학적 조성물.
- 환자에게 제1항의 화합물 또는 이것의 약제학적 허용성 염의 약제학적 유효량을 투여하는 것을 포함하는 염증상태 또는 알레르기 상태를 치료하는 방법.
- 치료학적 활성 물질과 같은 약제로서 제1항의 화합물을 사용하는 방법.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
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JP15772591 | 1991-05-31 | ||
JP157725/91 | 1991-05-31 |
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Publication Number | Publication Date |
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KR920021534A true KR920021534A (ko) | 1992-12-18 |
Family
ID=15656005
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
KR1019920009440A KR920021534A (ko) | 1991-05-31 | 1992-05-30 | 류코트리엔 b_4길항 물질 |
Country Status (13)
Country | Link |
---|---|
US (1) | US5225422A (ko) |
EP (1) | EP0516069B1 (ko) |
JP (1) | JPH05239004A (ko) |
KR (1) | KR920021534A (ko) |
AT (1) | ATE137223T1 (ko) |
AU (1) | AU643140B2 (ko) |
CA (1) | CA2069667A1 (ko) |
DE (1) | DE69210091T2 (ko) |
DK (1) | DK0516069T3 (ko) |
ES (1) | ES2086579T3 (ko) |
GR (1) | GR3020050T3 (ko) |
MX (1) | MX9202612A (ko) |
TW (1) | TW204343B (ko) |
Families Citing this family (12)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US6407124B1 (en) | 1998-06-18 | 2002-06-18 | Bristol-Myers Squibb Company | Carbon substituted aminothiazole inhibitors of cyclin dependent kinases |
US6455554B1 (en) | 1999-06-07 | 2002-09-24 | Targacept, Inc. | Oxopyridinyl pharmaceutical compositions and methods for use |
TWI262185B (en) | 1999-10-01 | 2006-09-21 | Eisai Co Ltd | Carboxylic acid derivatives having anti-hyperglycemia and anti-hyperlipemia action, and pharmaceutical composition containing the derivatives |
DE10029077A1 (de) * | 2000-06-13 | 2001-12-20 | Bayer Ag | Thiazolylsubstituierte Heterocyclen |
DE10257785A1 (de) * | 2002-12-11 | 2004-07-01 | Bayer Healthcare Ag | Isophthalsäurederivate |
AU2011226942B2 (en) * | 2004-11-22 | 2012-06-28 | Eli Lilly And Company | Potentiators of glutamate receptors |
EP1817301B1 (en) | 2004-11-22 | 2012-02-01 | Eli Lilly And Company | Potentiators of glutamate receptors |
EP1879881A2 (en) * | 2005-04-14 | 2008-01-23 | Bristol-Myers Squibb Company | Inhibitors of 11-beta hydroxysteroid dehydrogenase type i |
BRPI0610506A2 (pt) | 2005-04-20 | 2010-06-29 | Johnson & Johnson | moduladores de trombina de n-óxidos de piridina fluorados e processo para n-oxidação de heteroarilas contendo nitrogênio |
TW201006801A (en) | 2008-07-18 | 2010-02-16 | Lilly Co Eli | Imidazole carboxamides |
US9321727B2 (en) * | 2011-06-10 | 2016-04-26 | Hoffmann-La Roche Inc. | Pyridine derivatives as agonists of the CB2 receptor |
EP3746124A4 (en) | 2018-01-30 | 2021-10-27 | Foghorn Therapeutics Inc. | COMPOUNDS AND USES THEREOF |
Family Cites Families (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4666928A (en) * | 1984-08-30 | 1987-05-19 | Merck Frosst Canada, Ind. | Propylphenoxy pyridine carboxylates as leukotriene antagonists |
US4672066A (en) * | 1985-04-22 | 1987-06-09 | Hoffmann-La Roche Inc. | Derivatives of 4-acetyl-3-hydroxy-2-alkyl-phenoxycarboxylic acids |
US4663332A (en) * | 1985-10-10 | 1987-05-05 | Hoffman-La Roche Inc. | 5-substituted N-alkylated tetrazoles |
CA1315279C (en) * | 1987-01-12 | 1993-03-30 | Nancy Grace Bollinger | Anti-inflammatory agents |
JPS6429363A (en) * | 1987-07-23 | 1989-01-31 | Yoshitomi Pharmaceutical | Heterocyclic derivative |
-
1992
- 1992-05-27 ES ES92108916T patent/ES2086579T3/es not_active Expired - Lifetime
- 1992-05-27 EP EP92108916A patent/EP0516069B1/en not_active Expired - Lifetime
- 1992-05-27 AT AT92108916T patent/ATE137223T1/de not_active IP Right Cessation
- 1992-05-27 DE DE69210091T patent/DE69210091T2/de not_active Expired - Fee Related
- 1992-05-27 CA CA002069667A patent/CA2069667A1/en not_active Abandoned
- 1992-05-27 DK DK92108916.5T patent/DK0516069T3/da active
- 1992-05-27 AU AU17193/92A patent/AU643140B2/en not_active Ceased
- 1992-05-27 TW TW081104131A patent/TW204343B/zh active
- 1992-05-28 JP JP4164065A patent/JPH05239004A/ja active Pending
- 1992-05-30 KR KR1019920009440A patent/KR920021534A/ko not_active Application Discontinuation
- 1992-06-01 MX MX9202612A patent/MX9202612A/es not_active IP Right Cessation
- 1992-06-01 US US07/891,256 patent/US5225422A/en not_active Expired - Fee Related
-
1996
- 1996-05-27 GR GR960401413T patent/GR3020050T3/el unknown
Also Published As
Publication number | Publication date |
---|---|
DE69210091D1 (de) | 1996-05-30 |
MX9202612A (es) | 1992-11-01 |
US5225422A (en) | 1993-07-06 |
JPH05239004A (ja) | 1993-09-17 |
DK0516069T3 (da) | 1996-05-13 |
EP0516069A1 (en) | 1992-12-02 |
ES2086579T3 (es) | 1996-07-01 |
AU643140B2 (en) | 1993-11-04 |
ATE137223T1 (de) | 1996-05-15 |
CA2069667A1 (en) | 1992-12-01 |
EP0516069B1 (en) | 1996-04-24 |
AU1719392A (en) | 1993-03-11 |
DE69210091T2 (de) | 1996-10-02 |
GR3020050T3 (en) | 1996-08-31 |
TW204343B (ko) | 1993-04-21 |
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