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公开(公告)号:US5401849A
公开(公告)日:1995-03-28
申请号:US78658
申请日:1993-06-21
IPC分类号: C07D405/04 , C07D405/14
CPC分类号: C07D405/04 , C07D405/14
摘要: The invention concerns pharmaceutically useful 1,3-dioxane alkenoic acid derivatives of formula VII and formula XI containing a pyridyl moiety at position 4 of the dioxane ring and in which the groups at positions 2, 4 and 5 have cis-relative stereochemistry, wherein X is hydrogen, alkoxy or hydroxy, Y is vinylene, n is 1 or 2, A.sup.1 is alkylene, R.sup.1 is a variety of substituents defined hereinafter, Ra and Rb are independently methyl or ethyl, R.sup.2 is hydroxy, a physiologically acceptable alcohol residue or alkanesulphonamido, and the pharmaceutically acceptable salts thereof.
摘要翻译: 本发明涉及式VII和式XI的药学上有用的1,3-二恶烷烯酸衍生物,其在二恶烷环的4位含有吡啶基部分,其中2,4和5位的基团具有顺式相对立体化学,其中X 是氢,烷氧基或羟基,Y是亚乙烯基,n是1或2,A1是亚烷基,R1是下文定义的各种取代基,R a和R b独立地是甲基或乙基,R 2是羟基,生理上可接受的醇残基或烷基磺酰胺 ,及其药学上可接受的盐。
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公开(公告)号:US5166213A
公开(公告)日:1992-11-24
申请号:US310235
申请日:1989-02-14
IPC分类号: A61K31/44 , A61K31/443 , A61P7/02 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/08 , A61P29/00 , A61P43/00 , C07D405/04 , C07D405/14
CPC分类号: C07D405/04 , C07D405/14
摘要: The invention concerns novel, pharmaceutically useful 1,3-dioxane alkenoic acid derivatives of the formula I containing a pyridyl moiety at position 4 of the dioxane ring and in which the groups at positions 2, 4 and 5 have cis-relative stereochemistry, X is hydrogen, alkoxy or hydroxy, Y is vinylene, n is 1 or 2, A.sup.1 is alkylene, R.sup.1 is a variety of substituents defined hereinafter, and R.sup.2 is hydroxy, a physiologically acceptable alcohol residue or alkanesulphonamido, and the pharmaceutically acceptable salts thereof. The invention also includes processes for the manufacture and use of the acid derivatives as well as pharmaceutical compositions for therapeutic use in one or more of a variety of diseases such as ischaemic heart disease, cerebrovascular disease, asthmatic disease and/or inflammatory disease.
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公开(公告)号:US4921866A
公开(公告)日:1990-05-01
申请号:US185873
申请日:1988-04-25
IPC分类号: A61K31/44 , A61K31/443 , A61P7/04 , A61P9/00 , A61P11/00 , C07D405/04 , C07D405/06 , C07D405/12
CPC分类号: C07D405/04 , C07D405/06 , C07D405/12
摘要: The invention concerns novel, pharmaceutically useful 1,3-dioxane alkanoic and alkenoic acid derivatives of the formula I in which the groups at positions 2, 4 and 5 of the 1,3-dioxane ring have cis-relative stereochemistry, Y is ethylene or vinylene, n is 1-4, Z is hydrogen or hydroxy, and X is a pyridine containing group (as defined hereinafter); and the pharmaceutically acceptable salts thereof. The invention also includes processes for the manufacture and use of the acid derivatives as well as pharmaceutical compositions for therapeutic use in one or more of a variety of diseases such as ischaemic heart disease, cerebrovascular disease, asthmatic disease and/or inflammatory disease.
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公开(公告)号:US5248780A
公开(公告)日:1993-09-28
申请号:US951760
申请日:1992-09-25
IPC分类号: C07D405/04 , C07D405/14
CPC分类号: C07D405/04 , C07D405/14
摘要: The invention concerns novel, pharmaceutically useful 1,3-dioxane alkenoic acid derivatives of the formula I containing a pyridyl moiety at position 4 of the dioxane ring and in which the groups at positions 2, 4 and 5 have cis-relative stereochemistry, X is hydrogen, alkoxy or hydroxy, Y is vinylene, n is 1 or 2, A.sup.1 is alkylene, R.sup.1 is a variety of substituents defined hereinafter, and R.sup.2 is hydroxy, a physiologically acceptable alcohol residue or alkanesulphonamido, and the pharmaceutically acceptable salts thereof. The invention also includes processes for the manufacture and use of the acid derivatives as well as pharmaceutical compositions for therapeutic use in one or more of a variety of diseases such as ischaemic heart disease, cerebrovascular disease, asthmatic disease and/or inflammatory disease.
摘要翻译: 本发明涉及式I的新型药学上有用的1,3-二烷基链烯酸衍生物,其在二恶烷环的第4位含有吡啶基部分,其中第2,4和5位的基团具有顺式相对立体化学,X是 氢,烷氧基或羟基,Y是亚乙烯基,n是1或2,A1是亚烷基,R1是下文定义的各种取代基,R2是羟基,生理上可接受的醇残基或烷基磺酰氨基,及其药学上可接受的盐。 本发明还包括用于制备和使用酸衍生物的方法以及用于治疗用于一种或多种疾病如缺血性心脏病,脑血管疾病,哮喘病和/或炎性疾病的药物组合物。
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公开(公告)号:US5053415A
公开(公告)日:1991-10-01
申请号:US424611
申请日:1989-10-20
IPC分类号: A61K31/357 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61P9/00 , A61P9/08 , A61P9/10 , A61P11/08 , A61P29/00 , C07D405/00 , C07D405/04 , C07D405/14 , C07D407/14 , C07D409/00 , C07D409/14
CPC分类号: C07D405/04 , C07D407/14 , C07D409/14
摘要: The invention concerns novel, pharmaceutically useful 1,3-dioxane alkenoic acid derivatives of the formula I containing a pyridyl moiety at position 4 of the dioxane ring and in which the groups at positions 2, 4 and 5 have cis-relative stereochemistry, X is hydrogen, alkoxy or hydroxy, Y is vinylene, n is 1 or 2, A.sup.1 is alkylene, the substituents R.sup.1 and R.sup.2 at position 2 of the dioxane ring have a variety of values defined hereinafter, and R.sup.4 is hydroxy, a physiologically acceptable alcohol residue or alkanesulphonamido, and the pharmaceutically acceptable salts thereof. The invention also includes processes for the manufacture and use of the acid derivatives as well as pharmaceutical compositions for therapeutic use in one or more of a variety of diseases such as ischaemic heart disease, cerebrovascular disease, asthmatic disease and/or inflammatory disease.
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公开(公告)号:US4908380A
公开(公告)日:1990-03-13
申请号:US118226
申请日:1987-11-03
IPC分类号: A61K31/335 , A61K31/357 , A61K31/415 , A61K31/44 , A61K45/06 , A61P7/02 , A61P11/00 , A61P29/00 , A61P43/00 , C07D319/06
CPC分类号: A61K31/335 , A61K31/415 , A61K31/44
摘要: The invention concerns novel pharmaceutical compositions containing a 4(Z)-6-(2,4-diphenyl-1,3-dioxan-5-yl)-alkenoic acid which antagonizes one or more of the actions of thromboxane A.sub.2, together with a compound which inhibits the synthesis of thromboxane A.sub.2. The compositios are useful as medicines in treating a variety of diseases or medical conditions in which thromboxane A.sub.2 and/or other prostanoid contractile substances are involved.
摘要翻译: 本发明涉及含有4(Z)-6-(2,4-二苯基-1,3-二恶烷-5-基) - 烯酸的新型药物组合物,其拮抗血栓素A2的一种或多种作用,以及 抑制血栓素A2合成的化合物。 组合物可用作治疗涉及血栓素A2和/或其他前列腺素类收缩物质的各种疾病或医学病症的药物。
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公开(公告)号:US4895962A
公开(公告)日:1990-01-23
申请号:US218251
申请日:1988-07-13
IPC分类号: A61K31/335 , A61K31/357 , A61P7/02 , A61P9/08 , A61P9/10 , C07D319/06
CPC分类号: C07D319/06
摘要: The invention provides a novel group of 4(Z)-([2,4,5-cis]-2,4-diphenyl-1,3-dioxan-5-yl)hexenoic acids of formula I, wherein X is F, Cl, Br, CF.sub.3, CN, CH.sub.3 O or NO.sub.2 and one of Y and Z is hydrogen or fluoro and the other is hydrogen, and their pharmaceutically acceptable salts; together with their pharmaceutical compositions for use in treating a variety of disease conditions. Also provided are methods for the manufacture of novel compounds. Representative compounds are those in which X is 2-cyano or 2-chloro and Y and Z are both hydrogen.
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公开(公告)号:US4803220A
公开(公告)日:1989-02-07
申请号:US750101
申请日:1985-06-28
IPC分类号: A61K31/335 , A61K31/357 , A61P7/02 , A61P9/08 , A61P43/00 , C07C51/367 , C07C59/64 , C07D319/06
CPC分类号: C07D319/06 , C07C51/367 , C07C59/64
摘要: The invention concerns the novel racemic and laevorotatory optically active forms of the thromboxane A.sub.2 antagonist 5(Z)-7-([ 2,4,5-cis]-4-o-hydroxyphenyl-2-trifluoromethyl-1,3-dioxan-5-yl)heptenoic acid of formula I, their salts, pharmaceutical compositions, and processes for their manufacture and intermediates therefor. The pharmaceutical agents and their compositions are of value in certain pulmonary and/or vascular disorders.
摘要翻译: 本发明涉及血栓素A2拮抗剂5(Z)-7 - ([2,4,5-顺式] -4-邻羟基苯基-2-三氟甲基-1,3-二恶烷-2-酮的新型外消旋和左旋旋光活性形式, 噻唑-5-基)庚烯酸,其盐,药物组合物及其制备方法及其中间体。 药物及其组合物在某些肺和/或血管疾病中是有价值的。
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公开(公告)号:US4775685A
公开(公告)日:1988-10-04
申请号:US861329
申请日:1986-05-09
IPC分类号: A61K31/335 , A61K31/357 , A61P7/02 , A61P9/08 , A61P9/10 , C07D319/06
CPC分类号: C07D319/06
摘要: The invention provides a novel group of 4(Z)-([2,4,5-cis]-2,4-diphenyl-1,3-dioxan-5-yl)hexenoic acids of formula I, wherein X is F, Cl, Br, CF.sub.3, CN, CH.sub.3 O or NO.sub.2 and one of Y and Z is hydrogen or fluoro and the other is hydrogen, and their pharmaceutically acceptable salts; together with their pharmaceutical compositions for use in treating a variety of disease conditions. Also provided are methods for the manufacture of novel compounds. Representative compounds are those in which X is 2-cyano or 2-chloro and Y and Z are both hydrogen.
摘要翻译: 本发明提供了式I的4(Z) - ([2,4,5-顺式] -2,4-二苯基-1,3-二恶烷-5-基)己烯酸的新型基团,其中X为F, Cl,Br,CF 3,CN,CH 3 O或NO 2,Y和Z中的一个为氢或氟,另一个为氢,及其药学上可接受的盐; 以及用于治疗各种疾病状况的药物组合物。 还提供了制备新化合物的方法。 代表性的化合物是其中X是2-氰基或2-氯并且Y和Z都是氢的化合物。
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公开(公告)号:US5563141A
公开(公告)日:1996-10-08
申请号:US218174
申请日:1994-03-28
申请人: Michael G. Wayne , Michael J. Smithers , John W. Rayner , Alan W. Faull , Robert J. Pearce , Andrew G. Brewster , Richard E. Shute , Stuart D. Mills , Peter W. R. Caulkett
发明人: Michael G. Wayne , Michael J. Smithers , John W. Rayner , Alan W. Faull , Robert J. Pearce , Andrew G. Brewster , Richard E. Shute , Stuart D. Mills , Peter W. R. Caulkett
IPC分类号: A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/4427 , A61K31/445 , A61K31/4545 , A61K31/47 , A61K31/505 , A61K31/5377 , A61P7/02 , A61P43/00 , C07D213/74 , C07D213/81 , C07D215/14 , C07D215/42 , C07D239/42 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/12 , C07D521/00 , A61K31/495 , C07D401/00 , C07D403/00 , C07D405/00
CPC分类号: C07D213/74 , C07D213/81 , C07D215/42 , C07D239/42 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/12
摘要: A compound of the general formula(M.sup.1).sub.n --Q--(M.sup.2).sub.1-n --L--A Iwherein:n is 0 or 1;M.sup.1 is an amino group;Q is an aromatic heterocyclic group containing a basic nitrogen atom;M.sup.2 is an imino group;L is a template group; andA is an acidic group, or an ester or amide derivative thereof, or a sulphonamide group;and pharmaceutically acceptable salts and pro-drugs thereof, for use in the treatment of a disease in which platelet aggregation mediated by the binding of adhesion molecules to GPIIb-IIIa is involved. Novel compounds are also disclosed.
摘要翻译: 通式(M1)n-Q-(M2)1-n-L-1的化合物,其中n为0或1; M1是氨基; Q是含有碱性氮原子的芳香族杂环基; M2是亚氨基; L是模板组; A是酸性基团,或其酯或酰胺衍生物或磺酰胺基团; 和其药学上可接受的盐和前药,用于治疗由粘附分子与GPIIb-IIIa的结合介导的血小板聚集的疾病。 还公开了新的化合物。
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