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公开(公告)号：EP0452873B1
公开(公告)日：1996-07-03
申请号：EP91106040.8
申请日：1991-04-16
IPC分类号： C07D471/04 , A61K31/435
CPC分类号： C07D471/04
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公开(公告)号：EP0452873A1
公开(公告)日：1991-10-23
申请号：EP91106040.8
申请日：1991-04-16
IPC分类号： C07D471/04 , A61K31/435
CPC分类号： C07D471/04
摘要： Disclosed are naphthyridine derivatives represented by formula (I)
wherein:
X represents hydrogen; lower alkyl; aralkyl; substituted or unsubstituted aryl; substituted or unsubstituted aromatic heterocyclic group; -NR¹R² wherein R¹ and R² independently represent hydrogen or lower alkyl;
wherein W represents N or CH, Z represents a single bond, oxygen or NR³ (wherein R³ represents hydrogen, lower alkyl or benzyl) and n1 and n2 represent an integer of 1 to 3; or substituted or unsubstituted thiazolinyl; and
Y is a single bond or alkylene
and pharmaceutically acceptable salts thereof. The compounds show potent anti-inflammatory activity and are expected to be useful in treating rheumarthritis.摘要翻译： 公开了由式（I）表示的萘啶衍生物
其中：X表示氢; 低级烷基 芳; 取代或未取代的芳基; 取代或未取代的芳族杂环基; -NR 1 R 2其中R 1和R 2独立地表示氢或低级烷基; 其中W表示N或CH，Z表示单键，氧或NR 3（其中R 3表示氢，低级烷基或苄基），n1和n2表示1〜3的整数， 或取代或未取代的噻唑啉基; 并且Y是单键或其亚烷基及其药学上可接受的盐。 化合物显示有效的抗炎活性，并且预期可用于治疗风湿性关节炎。 -
公开(公告)号：EP0393574B1
公开(公告)日：1996-01-31
申请号：EP90107245.4
申请日：1990-04-17
IPC分类号： C07D493/04 , C07D519/00 , A61K31/34
CPC分类号： C07D493/04
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公开(公告)号：EP0386722A1
公开(公告)日：1990-09-12
申请号：EP90104336.4
申请日：1990-03-07
IPC分类号： C07D471/04 , A61K31/47
CPC分类号： C07D471/04
摘要： Novel imidazoquinolone derivative represented by the formula (I);
wherein R 1 represents hydrogen, alkyl, cycloalkyl, alkenyl aralkyl, aralkenyl or substituted or unsubstituted aryl; X represents nitrogen or C-R 2 where R 2 is hydrogen, hydroxyl, alkyl, cycloalkyl, alkenyl, aralkyl, aralkenyl, substituted or unsubstituted aryl, thiol, halogen, substituted or unsubstituted aromatic heterocyclic group, or -(CH 2 ) m C0 2 R 6 where R 6 is hydrogen or lower alkyl and m is an integer of 0 to 3; Y represents oxygen or sulfur; R 3 represents alkyl, cycloalkyl, alkoxyalkly, alkenyl, aralkyl; aralkenyl, -(CH 2 ) n -Het where Net is substituted or unsubstituted aromatic heterocyclic group and n is an integer of 1 to 3 or (CH 2 )- n CO 2 R 6a where n has the same meaning as defined above and R 6a has the same meaning as defined as to R 6 ; each of R 4 and R 5 independently represents hydrogen, lower alkyl, trifluoromethyl, cycloalkyl, halogen, hydroxyl, lower alkoxyl, lower alkylthio, nitro, amino, lower alkylamino, lower alkanoylamino, aroylamino, lower alkanoyl or aroyl; and a pharmaceutically acceptable salt thereof. The Compound (I) and a pharmaceutically acceptable salt thereof show bronchodilatory and antiallergic activities, and are useful for treating respiratory disorders such as bronchial asthma.摘要翻译： 式（I）代表的新型咪唑并喹诺酮衍生物; 其中R1代表氢，烷基，环烷基，烯基芳烷基，芳烯基或取代或未取代的芳基; X代表氮或C-R2，其中R2是氢，羟基，烷基，环烷基，烯基，芳烷基，芳烯基，取代或未取代的芳基，硫醇，卤素，取代或未取代的芳族杂环基团或 - （CH2）mCO2R6， 或低级烷基，并且m是0至3的整数; Y代表氧或硫; R3代表烷基，环烷基，烷氧基，链烯基，芳烷基; - （CH 2）n -Het其中Net是取代或未取代的芳族杂环基，n是1-3的整数或（CH2）-nCO2R6a，其中n具有与上述定义相同的含义，R6a具有与所定义的相同含义 至于R6; 低级烷基，三氟甲基，环烷基，卤素，羟基，低级烷氧基，低级烷硫基，硝基，氨基，低级烷基氨基，低级烷酰基氨基，芳酰基氨基，低级烷酰基或芳酰基; 及其药学上可接受的盐。 化合物（Ⅰ）及其药学上可接受的盐显示支气管扩张和抗过敏活性，可用于治疗呼吸障碍如支气管哮喘。
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公开(公告)号：EP0459505B1
公开(公告)日：1996-10-02
申请号：EP91108908.4
申请日：1991-05-31
IPC分类号： C07D471/14 , A61K31/435
CPC分类号： C07D471/14
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公开(公告)号：EP0393574A2
公开(公告)日：1990-10-24
申请号：EP90107245.4
申请日：1990-04-17
IPC分类号： C07D493/04 , C07D519/00 , A61K31/34
CPC分类号： C07D493/04
摘要： Disclosed are hexitol derivatives represented by the general formula (I):
wherein
Q represents a formula
wherein a represents NH, O or S,
each of b , c and d independently represents CH or N,
each of R¹, R², R³ and R⁴ independently represents hydrogen, lower alkyl, trifluoromethyl, aryl, lower alkanoyloxy, amino, lower alkylamino, lower alkanoylamino, lower alkanoyl, aroyl, halogen, nitro, (CH₂) m OR⁷, (CH₂) m SR⁷, (CH₂) m CO₂R⁷ where R⁷ represents hydrogen or lower alkyl and m represents an integer of 0 to 3,
each of R⁵ and R⁶ independently represents hydrogen or lower alkyl,
wherein each of Y¹ and Y² independently represents hydrogen, lower alkyl, hydroxyl, lower alkanoyloxy, nitrile or phenyl; or Y¹ and Y² are combined together to form oxygen,
each of Y³ and Y⁴ independently represents hydrogen or lower alkyl, and ℓ is an integer of 0 to 6, and where ℓ is an integer of 2 to 6, each
may be the same or different,
Z represents hydrogen or nitro, and, n is 2 or 3 or a pharmaceutically acceptable salt thereof. The compounds show prominent coronary vasodilative activities, and are useful in treating angina pectoris and myocardial infarction.摘要翻译： 公开了由通式（I）表示的己糖醇衍生物：其中Q表示式CHEM，其中a表示NH，O或S，b，c和d各自独立地表示CH或N， 1，R 2，R 3和R 4独立地表示氢，低级烷基，三氟甲基，芳基，低级烷酰氧基，氨基，低级烷基氨基，低级烷酰基氨基，低级烷酰基，芳酰基，卤素，硝基， ）mOR 7，（CH 2）m SR 7，（CH 2）m CO 2 R 7，其中R 7表示氢或低级烷基，m表示0〜3的整数，R 5和R 5， 6>独立地表示氢或低级烷基，CHEM，其中Y 1和Y 2各自独立地表示氢，低级烷基，羟基，低级烷酰氧基，腈或苯基; 或Y 1和Y 2组合在一起形成氧，Y 3和Y 4各自独立地表示氢或低级烷基，l是0-6的整数，其中l是 2〜6的整数，每个
可以相同或不同，Z表示氢或硝基，n为2或3或其药学上可接受的盐。 该化合物显示出显着的冠状动脉血管扩张活性，可用于治疗心绞痛和心肌梗死。 -
7.发明授权
公开(公告)号：EP0505058B1
公开(公告)日：1997-05-21
申请号：EP92301900.4
申请日：1992-03-05
发明人： Suzuki, Fumio , Miwa, Yoshikazu , Hayashi, Hiroaki , Kuroda, Takeshi , Ohmori, Kenji , Nakajima, Hiroshi
IPC分类号： C07D495/04 , A61K31/435
CPC分类号： C07D495/04
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8.发明公开Thienopyridine derivatives and pharmaceutical compositions containing them 失效Thienopyridinderivate und diese enthaltende pharmazeutische Zubereitungen。
公开(公告)号：EP0505058A1
公开(公告)日：1992-09-23
申请号：EP92301900.4
申请日：1992-03-05
发明人： Suzuki, Fumio , Miwa, Yoshikazu , Hayashi, Hiroaki , Kuroda, Takeshi , Ohmori, Kenji , Nakajima, Hiroshi
IPC分类号： C07D495/04 , A61K31/435
CPC分类号： C07D495/04
摘要： Disclosed ire thienopyridine derivatives of the formula (I):
wherein
one of A and B represents -S- and the other represents -CH=;
R represents hydrogen or C₁ - C₆ alkyl; and
Z represents pyridyl and their pharmaceutically acceptable acid addition or metal salts useful as immunoregulators and for the prevention and treatment of osteoporosis.摘要翻译： 公开的式（I）的噻吩并吡啶衍生物：其中A和B之一表示-S-，另一个表示-CH =; R表示氢或C 1 -C 6烷基; Z表示吡啶基及其药学上可接受的酸加成盐或金属盐，可用作免疫调节剂和预防和治疗骨质疏松症。
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公开(公告)号：EP0459505A1
公开(公告)日：1991-12-04
申请号：EP91108908.4
申请日：1991-05-31
IPC分类号： C07D471/14 , A61K31/435
CPC分类号： C07D471/14
摘要： Disclosed are imidazonaphthyridine derivatives represented by formula (I)
wherein:
R¹ represents lower alkyl or substituted or unsubstituted aryl; and
X-Y-Z represents
wherein R² represents hydrogen, lower alkyl, alkenyl, aralkenyl, or -C(R⁵)H-(CH₂) n -R⁴ (wherein R⁴ represents substituted or unsubstituted aryl, substituted or unsubstituted pyridyl, substituted or unsubstituted furyl, hydroxy-substituted lower alkyl, lower alkanoyloxy, morpholino, lower alkanoyl, carboxy, lower alkoxycarbonyl, cycloalkyl, hydroxy, lower alkoxy, halogen or NR⁶R⁷ wherein R⁶ and R⁷ independently represents hydrogen or lower alkyl; R⁵ represents hydrogen, lower alkyl, or phenyl; and n represents an integer of 0 to 3); and R³ represents hydrogen, mercapto, hydroxy, lower alkyl, or aryl
and pharmaceutically acceptable salts thereof.
The compounds show a potent anti-inflammatory, anti-allergic and broncho-dilative activity.摘要翻译： 公开了由式（I）表示的咪唑并萘啶衍生物，其中：R 1代表低级烷基或取代或未取代的芳基; XYZ表示其中R 2代表氢，低级烷基，烯基，芳烯基或-C（R 5）H-（CH 2）n -R 4（其中R 4代表取代或未取代的芳基，取代或未取代的吡啶基，取代或未取代的呋喃基， 低级链烷酰基，羧基，低级烷氧基羰基，环烷基，羟基，低级烷氧基，卤素或NR 6 R 8，其中R 6和R 7独立地代表氢或低级烷基; R 5代表氢，低级烷基或苯基;以及n 表示0至3的整数）; 和R 3代表氢，巯基，羟基，低级烷基或芳基及其药学上可接受的盐。 该化合物显示出强效的抗炎，抗过敏和支气管扩张活性。
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公开(公告)号：EP0411394A1
公开(公告)日：1991-02-06
申请号：EP90113760.4
申请日：1990-07-18
IPC分类号： C07D471/04 , A61K31/47
CPC分类号： C07D471/04
摘要： Novel imidazoquinolone derivative represented by formula (I);
wherein R¹ represents lower alkyl or -(CH₂) m CO-R³ where R³ represents hydrogen, lower alkyl, hydroxy or lower alkoxy; and m is an integer of 1 to 3;
R² represents lower alkyl;
or a pharmaceutically acceptable salt thereof.摘要翻译： 式（I）代表的新型咪唑并喹诺酮衍生物; 其中R 1代表低级烷基或 - （CH 2）mCO-R 3，其中R 3代表氢，低级烷基，羟基或低级烷氧基; m是1至3的整数; R 2代表低级烷基; 或其药学上可接受的盐。
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