KR950008493A - 유착 수용체 길항물질(iii) - Google Patents
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- KR950008493A KR950008493A KR1019940023840A KR19940023840A KR950008493A KR 950008493 A KR950008493 A KR 950008493A KR 1019940023840 A KR1019940023840 A KR 1019940023840A KR 19940023840 A KR19940023840 A KR 19940023840A KR 950008493 A KR950008493 A KR 950008493A
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- C07D263/16—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member 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
- C07D263/18—Oxygen atoms
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- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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Abstract
하기 일반식(I)의 신규한 옥사졸리디논 유도체 및 그의 생리학적으로 무해한 염은 피브리노겐이 상응하는 수용체에 결합하는 것을 억제하고 혈전증, 발작, 심근, 경색증, 염증, 동맥경화증, 골다공증 및 또는 종양을 치료하는데 유용할 수 있다.
상기식에서, R1은 비치환되거나 또는 CN, H2N-CH2-, A2N-CH2-, H2N-C(=NH)-, H2N-C(=NH)-NH-, H2N-C(=NH)-NH-CH2-, HO-NH-C(=NH)- 또는 HO-NH-C(=NH)-NH-에 의해 일치환 되는 페닐라디칼이고, X는 O, S, SO2, -NH- 또는 -NA-이고,
A는 탄소 원자수가 1내지 6개의 알킬이고, R2는 H, A, Li, Na, K, NH4또는 벤질이고, R3은 H 또는 (CH2)nCOOR2이고, E는 각각의 경우에 서로 독립적으로, CH 또는 N이고, Q는 O, S 또는 NH이고, m은 1,2또는 3이고, n은 0, 1, 2또는 3이다.
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (8)
- 하기 일반식(i)의 옥사졸리디노 유도체 및 그의 생리학적으로 무해한 염;상기식에서, R1은 비치환되거나 또는 CN, H2N-CH2-, A2N-CH2-, H2N-C(=NH)-, H2N-C(=NH)-NH-, H2N-C(=NH)-NH-CH2-, HO-NH-C(=NH)- 또는 HO-NH-C(=NH)-NH-에 의해 일치환 되는 페닐라디칼이고, X는 O, S, SO, SO2, -NH- 또는 -NA-이고,A는 탄소 원자수가 1내지 6개의 알킬이고, R2는 H, A, Li, Na, K, NH4또는 벤질이고, R3은 H 또는 (CH2)nCOOR2이고, E는 각각의 경우에 서로 독립적으로, CH 또는 N이고, Q는 O, S 또는 NH이고, m은 1,2또는 3이고, n은 0, 1, 2또는 3이다.
- 제1항에 있어서, 하기 화합물(a)내지 (d)중에서 선택되는 유도체; (a)3-p-아미디노페닐-5-(p-카복시메틸페녹시메틸)-옥사졸리딘-2-온; (b)3-p-아미노페닐-5-(p-메톡시카보닐메틸페녹시메틸)-옥사졸리딘-2-온 (c)3-p-아미노메틸페닐-5-(p-카복시메틸페녹시메틸)-옥사졸리딘-2-온 나트륨 염; (d)3-p-구아니디노메틸페닐-5-(p-카복시메틸페녹시메틸)-옥사졸리딘-2-온.
- 제1항에 따르는 일반식(I)의 거울상이성질체 화합물 또는 하나의 그의 염.
- 하기 일반식(II)의 화합물을 하기 일반식(Ⅲ)의 화합물과 반응시키거나, 또는 사기 일반식(IV)의 화합물 또는 그의 반응성 유도체중 하나를 카본산의 반응성 유도체와 반응시키거나, 또는 일반식(I), (R1=H2N-C(=NH)-NH-에 의해 일치환되는 페닐 라디칼)의 구아니다노 화합물을 제조하기 위하여, 일반식(I)에 상응하지만 라디칼 R1대신에 아니노페닐 그룹을 함유하는 아미노 화합물을 아미딘화제로 처리하거나, 또는 가용매 분해 또는 수소화 분해제로 처리하므로써, 일반식(I)의 화합물을 하나의 그의 작용성 유도체로부터 유리시키고/시키거나, 일반식(I)의 화합물에서, 라디칼 R1및/또는 B중 하나 또는 모두를 다른 라디칼 R1및/또는 B로 전환하고/하거나 일반식(I)의 화합물을 산 또는 염기로 처리하므로써 그의 염중 하나로 전환함을 특징으로 하는, 제1항에 따르는 일반식(I)의 화합물 및 또한 그의 염의 제조 방법;상기식에서, R1은 비치환되거나 또는 CN, H2N-CH2-, A2N-CH2-, H2N-C(=NH)-, H2N-C(=NH)-NH-, H2N-C(=NH)-NH-CH2-, HO-NH-C(=NH)- 또는 HO-NH-C(=NH)-NH-에 의해 일치환 되는 페닐라디칼이고, X는 O, S, SO, SO2, -NH- 또는 -NA-이고,A는 탄소 원자수가 1내지 6개의 알킬이고, R2는 H, A, Li, Na, K, NH4또는 벤질이고, R3은 H 또는 (CH2)n-COOR2이고, E는 각각의 경우에 서로 독립적으로, CH 또는 N이고, Q는 O, S 또는 NH이고, m은 1,2또는 3이고, n은 0, 1, 2또는 3이고, Z는 Cl, Br, I, OH또는 에스테르화된 반응성 OH그룹이고, Y는 OH, SH, NH2또는 OH 또는 SH로부터 유도될 수 있는 염과 유사한 라디칼이다.
- 제1항에 따르는 일반식(I)의 화합물 및/또는 그의 생리학적으로 무해한 염 중 하나를 적어도 하나의 고형, 액체 또는 반액체 부형제 또는 보조 물질과 함께 적합한 투여 형태로 제조함을 특징으로 하는, 약학적 제제의 제조방법.
- 제1항에 따르는 적어도 하나의 일반식(I)의 화합물 및/또는 그의 약학적으로 무해한 염 중 하나를 함유함을 특징으로 하는, 약학적 제제.
- 약물을 제조하기 위한, 제1항에 따르는 일반식(I)의 화합물, 또는 그의 약학적으로 무해한 염의 용도.
- 혈전증, 심근 경색증, 발작, 골다공증, 동맥경화증, 염증 및/또는 종양의 치료에서, 제1항에 따르는 일반식(I)의 화합물 또는 그의 약학적으로 무해한 염의 용도.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
DEP4332384.7 | 1993-09-23 | ||
DE4332384A DE4332384A1 (de) | 1993-09-23 | 1993-09-23 | Adhäsionsrezeptor-Antagonisten III |
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Publication Number | Publication Date |
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KR950008493A true KR950008493A (ko) | 1995-04-17 |
KR100347849B1 KR100347849B1 (ko) | 2002-11-16 |
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KR1019940023840A KR100347849B1 (ko) | 1993-09-23 | 1994-09-22 | 유착수용체길항물질(iii) |
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US (3) | US5561148A (ko) |
EP (1) | EP0645376B1 (ko) |
JP (1) | JPH07179441A (ko) |
KR (1) | KR100347849B1 (ko) |
CN (1) | CN1052227C (ko) |
AT (1) | ATE178599T1 (ko) |
AU (1) | AU682050B2 (ko) |
CA (1) | CA2132579A1 (ko) |
CZ (1) | CZ288819B6 (ko) |
DE (2) | DE4332384A1 (ko) |
DK (1) | DK0645376T3 (ko) |
ES (1) | ES2132295T3 (ko) |
GR (1) | GR3030512T3 (ko) |
HU (1) | HU217980B (ko) |
NO (1) | NO305203B1 (ko) |
PL (1) | PL180462B1 (ko) |
RU (1) | RU2125560C1 (ko) |
SK (1) | SK282134B6 (ko) |
TW (1) | TW381086B (ko) |
UA (1) | UA40590C2 (ko) |
ZA (1) | ZA947405B (ko) |
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DE4332384A1 (de) * | 1993-09-23 | 1995-03-30 | Merck Patent Gmbh | Adhäsionsrezeptor-Antagonisten III |
DE4429461A1 (de) * | 1994-08-19 | 1996-02-22 | Merck Patent Gmbh | Adhäsionsrezeptor-Antagonisten |
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DE19516483A1 (de) | 1995-05-05 | 1996-11-07 | Merck Patent Gmbh | Adhäsionsrezeptor-Antagonisten |
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DE19601264A1 (de) * | 1996-01-16 | 1997-07-17 | Bayer Ag | Pyrido-annellierte Thienyl- und Furanyl-Oxazolidinone |
DE19601265A1 (de) | 1996-01-16 | 1997-07-17 | Bayer Ag | 2-Oxo- und 2-Thio-1,2-dihydrochinolinyl-oxazolidinone |
DE19601627A1 (de) | 1996-01-18 | 1997-07-24 | Bayer Ag | Heteroatomhaltige Cyclopentanopyridyl-Oxazolidinone |
DE19604223A1 (de) | 1996-02-06 | 1997-08-07 | Bayer Ag | Neue substituierte Oxazolidinone |
HRP970049A2 (en) | 1996-02-06 | 1998-04-30 | Bayer Ag | New heteroaryl oxazolidinones |
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PL372090A1 (en) * | 2002-02-28 | 2005-07-11 | Astrazeneca Ab | Chemical compounds |
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DE102005047558A1 (de) * | 2005-10-04 | 2008-02-07 | Bayer Healthcare Ag | Kombinationstherapie substituierter Oxazolidinone zur Prophylaxe und Behandlung von cerebralen Durchblutungsstörungen |
DE102005047561A1 (de) | 2005-10-04 | 2007-04-05 | Bayer Healthcare Ag | Feste, oral applizierbare pharmazeutische Darreichungsformen mit schneller Wirkstofffreisetzung |
DE502006009169D1 (en) | 2005-10-04 | 2011-05-05 | Bayer Schering Pharma Ag | NEUE POLYMORPHE FORM VON 5-CHLOR-N-(ä ( 5S )-2-0X0-3-Ä4-( 3-OXO-4-MORPHOLINYL)-PHENYLÜ-1,3-OXAZOLIDIN-5-YLü -METHYL)-2-THIOPHENCARBOXAMID |
DE102006051625A1 (de) * | 2006-11-02 | 2008-05-08 | Bayer Materialscience Ag | Kombinationstherapie substituierter Oxazolidinone |
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DK2222636T3 (da) | 2007-12-21 | 2013-06-03 | Ligand Pharm Inc | Selektive androgenreceptormodulatorer (SARMS) og anvendelser deraf |
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WO2023275715A1 (en) | 2021-06-30 | 2023-01-05 | Pfizer Inc. | Metabolites of selective androgen receptor modulators |
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BE791501A (fr) * | 1971-11-19 | 1973-05-17 | Albert Ag Chem Werke | Diamines cycliques n,n'-disubstituees et leur procede de preparation |
US4602093A (en) * | 1984-02-08 | 1986-07-22 | Merck & Co., Inc. | Novel substituted imidazoles, their preparation and use |
DE3723797A1 (de) * | 1987-07-18 | 1989-01-26 | Merck Patent Gmbh | Oxazolidinone |
US5053393A (en) * | 1988-07-20 | 1991-10-01 | Monsanto Company | Novel platelet-aggregation inhibitor |
US5084466A (en) * | 1989-01-31 | 1992-01-28 | Hoffmann-La Roche Inc. | Novel carboxamide pyridine compounds which have useful pharmaceutical utility |
DE4005371A1 (de) * | 1990-02-21 | 1991-08-22 | Merck Patent Gmbh | Oxazolidinone |
DE4017211A1 (de) * | 1990-05-29 | 1991-12-05 | Merck Patent Gmbh | Oxazolidinone |
DE69329106T2 (de) * | 1992-04-30 | 2001-03-22 | Taiho Pharmaceutical Co Ltd | Oxazolidinderivat und sein pharmazeutisch verträgliches salz |
US5532225A (en) * | 1992-07-31 | 1996-07-02 | Sri International | Acyclic purine phosphonate nucleotide analogs as antiviral agents, and related synthetic methods |
DK0623615T3 (da) * | 1993-05-01 | 1999-12-13 | Merck Patent Gmbh | Adhæsionsreceptor-antagonister |
IL109570A0 (en) * | 1993-05-17 | 1994-08-26 | Fujisawa Pharmaceutical Co | Guanidine derivatives, pharmaceutical compositions containing the same and processes for the preparation thereof |
DE4324393A1 (de) * | 1993-07-21 | 1995-01-26 | Merck Patent Gmbh | 4-Aryloxy- und 4-Arylthiopiperidinderivate |
DE4332384A1 (de) * | 1993-09-23 | 1995-03-30 | Merck Patent Gmbh | Adhäsionsrezeptor-Antagonisten III |
TW286317B (ko) * | 1993-12-13 | 1996-09-21 | Hoffmann La Roche | |
TW363051B (en) * | 1995-08-31 | 1999-07-01 | Mitsui Toatsu Chemicals | Substituted amidine derivatives and platelet aggregation inhibitor containing the same |
-
1993
- 1993-09-23 DE DE4332384A patent/DE4332384A1/de not_active Withdrawn
-
1994
- 1994-08-01 UA UA94085682A patent/UA40590C2/uk unknown
- 1994-09-14 CZ CZ19942247A patent/CZ288819B6/cs not_active IP Right Cessation
- 1994-09-15 AT AT94114519T patent/ATE178599T1/de not_active IP Right Cessation
- 1994-09-15 ES ES94114519T patent/ES2132295T3/es not_active Expired - Lifetime
- 1994-09-15 DE DE59408068T patent/DE59408068D1/de not_active Expired - Fee Related
- 1994-09-15 EP EP94114519A patent/EP0645376B1/de not_active Expired - Lifetime
- 1994-09-15 DK DK94114519T patent/DK0645376T3/da active
- 1994-09-16 AU AU73050/94A patent/AU682050B2/en not_active Ceased
- 1994-09-19 SK SK1121-94A patent/SK282134B6/sk unknown
- 1994-09-20 CN CN94115356A patent/CN1052227C/zh not_active Expired - Fee Related
- 1994-09-20 JP JP6224941A patent/JPH07179441A/ja not_active Withdrawn
- 1994-09-21 CA CA002132579A patent/CA2132579A1/en not_active Abandoned
- 1994-09-21 TW TW083108683A patent/TW381086B/zh not_active IP Right Cessation
- 1994-09-22 NO NO943523A patent/NO305203B1/no not_active IP Right Cessation
- 1994-09-22 HU HU9402724A patent/HU217980B/hu not_active IP Right Cessation
- 1994-09-22 PL PL94305144A patent/PL180462B1/pl unknown
- 1994-09-22 US US08/310,085 patent/US5561148A/en not_active Expired - Fee Related
- 1994-09-22 KR KR1019940023840A patent/KR100347849B1/ko not_active IP Right Cessation
- 1994-09-22 ZA ZA947405A patent/ZA947405B/xx unknown
- 1994-09-23 RU RU94034124A patent/RU2125560C1/ru not_active IP Right Cessation
-
1996
- 1996-05-29 US US08/654,690 patent/US5723480A/en not_active Expired - Fee Related
-
1997
- 1997-11-06 US US08/964,131 patent/US6028090A/en not_active Expired - Fee Related
-
1999
- 1999-06-15 GR GR990401587T patent/GR3030512T3/el unknown
Also Published As
Publication number | Publication date |
---|---|
TW381086B (en) | 2000-02-01 |
HU9402724D0 (en) | 1994-12-28 |
EP0645376A1 (de) | 1995-03-29 |
DK0645376T3 (da) | 1999-10-18 |
AU682050B2 (en) | 1997-09-18 |
HUT71233A (en) | 1995-11-28 |
NO943523D0 (no) | 1994-09-22 |
DE59408068D1 (de) | 1999-05-12 |
NO305203B1 (no) | 1999-04-19 |
CZ288819B6 (cs) | 2001-09-12 |
DE4332384A1 (de) | 1995-03-30 |
CA2132579A1 (en) | 1995-03-24 |
CZ224794A3 (en) | 1995-07-12 |
US6028090A (en) | 2000-02-22 |
UA40590C2 (uk) | 2001-08-15 |
NO943523L (no) | 1995-03-24 |
US5723480A (en) | 1998-03-03 |
JPH07179441A (ja) | 1995-07-18 |
RU94034124A (ru) | 1996-07-10 |
ES2132295T3 (es) | 1999-08-16 |
CN1052227C (zh) | 2000-05-10 |
EP0645376B1 (de) | 1999-04-07 |
ATE178599T1 (de) | 1999-04-15 |
ZA947405B (en) | 1995-05-15 |
SK112194A3 (en) | 1995-05-10 |
CN1106806A (zh) | 1995-08-16 |
AU7305094A (en) | 1995-04-06 |
SK282134B6 (sk) | 2001-11-06 |
HU217980B (hu) | 2000-05-28 |
US5561148A (en) | 1996-10-01 |
RU2125560C1 (ru) | 1999-01-27 |
PL180462B1 (pl) | 2001-02-28 |
PL305144A1 (en) | 1995-04-03 |
GR3030512T3 (en) | 1999-10-29 |
KR100347849B1 (ko) | 2002-11-16 |
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