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1. 发明授权

US5319085A Quinoline derivative having serotonin-3 receptor antagonizing activity 失效
标题翻译：具有5-羟色胺-3受体拮抗活性的喹啉衍生物
公开(公告)号：US5319085A
公开(公告)日：1994-06-07
申请号：US039131
申请日：1993-04-16
申请人： Fumio Suzuki , Hiroaki Hayashi , Yoshikazu Miwa , Takeshi Kuroda , Akio Ishii , Shunji Ichikawa , Ichiro Miki , Katsuichi Shuto
发明人： Fumio Suzuki , Hiroaki Hayashi , Yoshikazu Miwa , Takeshi Kuroda , Akio Ishii , Shunji Ichikawa , Ichiro Miki , Katsuichi Shuto
IPC分类号： C07D451/04 , C07D451/12 , C07D451/14 , C07D403/12 , C07D401/12
CPC分类号： C07D451/14 , C07D451/04 , C07D451/12
摘要： Quinoline derivatives represented by formula (I): ##STR1## wherein A-B-D represents --C(COO--Y).dbd.CH--C(OR).dbd. (wherein Y represents 8-methyl-8-azabicyclo[3.2.1]oct-3-yl group and R represents alkyl) or --C(OH).dbd.C(COX--Y)--CH.dbd. (wherein X represents --O-- or --NH--; and Y has the same meaning as described above), or a pharmaceutically acceptable salt thereof, possess potent 5HT.sub.3 antagonizing activity and are useful as antiemetic agents.
摘要翻译： PCT No.PCT / JP91 / 01758 Sec。 371日期：1993年04月16日 102（e）日期1993年4月16日PCT 1991年12月25日PCT公布。出版物WO92 / 12150 PCT （I）表示的喹啉衍生物：其中ABD表示-C（COO-Y）= CH-C（OR）=（其中Y表示8-甲基-8- 氮杂双环[3.2.1]辛-3-基，R代表烷基）或-C（OH）= C（COX-Y）-CH =（其中X表示-O-或-NH-; Y具有相同意义如上所述）或其药学上可接受的盐具有有效的5HT3拮抗活性，并且可用作止吐剂。

2. 发明授权

US5219864A Thienopyridine derivatives 失效
标题翻译：噻吩衍生物
公开(公告)号：US5219864A
公开(公告)日：1993-06-15
申请号：US847665
申请日：1992-03-04
申请人： Fumio Suzuki , Yoshikazu Miwa , Hiroaki Hayashi , Takeshi Kuroda , Kenji Ohmori , Hiroshi Nakajima
发明人： Fumio Suzuki , Yoshikazu Miwa , Hiroaki Hayashi , Takeshi Kuroda , Kenji Ohmori , Hiroshi Nakajima
IPC分类号： A61K31/44 , A61K31/4365 , A61P3/00 , A61P19/10 , A61P37/02 , A61P37/06 , A61P43/00 , C07D495/04
CPC分类号： C07D495/04
摘要： Disclosed is a thienopyridine derivative represented by formula (I): ##STR1## wherein one of A and B represents --S-- and the other represents --CH.dbd.; R represents hydrogen or lower alkyl, and Z represents pyridyl; or a pharmaceutically acceptable salt thereof.The thienopyridine derivative is useful as an immunoregulator and for the prevention and treatment of osteoporosis.

3. 发明授权

US5342843A Thienoimidazoppyridone derivatives 失效
标题翻译：噻吩并咪唑吡啶衍生物
公开(公告)号：US5342843A
公开(公告)日：1994-08-30
申请号：US98329
申请日：1993-08-06
申请人： Fumio Suzuki , Yoshikazu Miwa , Takeshi Kuroda , Shigeto Kitamura , Haruhiko Manabe
发明人： Fumio Suzuki , Yoshikazu Miwa , Takeshi Kuroda , Shigeto Kitamura , Haruhiko Manabe
IPC分类号： C07D495/14 , C07D491/12 , A61K31/44
CPC分类号： C07D495/14
摘要： The present invention relates to a thienoimidazopyridone derivative represented by Formula (I): ##STR1## wherein A and B independently represent --S-- or --CH.dbd., X-Y-Z represents --N(R.sup.2)--CH.dbd.N-- or --N.dbd.CH--N (R.sup.2)-- wherein R.sup.2 is hydrogen, lower alkyl or --CH(R.sup.3)--(CH.sub.2).sub.n --R.sup.4 wherein R.sup.4 is phenyl, n is 0 or 1, and R.sup.3 is hydrogen or lower alkyl, and R.sup.1 represents lower alkyl, or a pharmaceutically acceptable salt thereof.
摘要翻译： PCT No.PCT / JP92 / 01602 Sec。 371日期：1993年8月6日 102（e）日期1993年8月6日PCT提交1992年12月8日PCT公布。公开号WO93 / 12116 PCT 本发明涉及由式（I）表示的噻吩并咪唑并吡啶酮衍生物：本发明-S-或-CH =，XYZ表示-N（R2）-CH = N-或-N = CH-N （R2） - 其中R2是氢，低级烷基或-CH（R3） - （CH2）n-R4，其中R4是苯基，n是0或1，R3是氢或低级烷基，R1代表低级烷基，或其药学上可接受的盐。

4. 发明授权

US5053408A Hexitol derivatives having vasodilative activity 失效
标题翻译：具有血液活性的HEXITOL衍生物
公开(公告)号：US5053408A
公开(公告)日：1991-10-01
申请号：US508701
申请日：1990-04-13
申请人： Fumio Suzuki , Hiroaki Hayashi , Takeshi Kuroda , Kazuhiro Kubo , Junichi Ikeda
发明人： Fumio Suzuki , Hiroaki Hayashi , Takeshi Kuroda , Kazuhiro Kubo , Junichi Ikeda
IPC分类号： A61K31/00 , A61K31/495 , A61K31/496 , A61K31/505 , A61P9/00 , A61P9/08 , A61P9/10 , C07D493/04 , C07D519/00
CPC分类号： C07D493/04
摘要： Disclosed is a hexitol derivative represented by the formula (I): ##STR1## wherein Q represents a formula selected from the group consisting of ##STR2## wherein a represents NH, O or S;each of b, c and d independently represents CH or N;each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represents hydrogen, lower alkyl, trifluoromethyl, aryl, lower alkanoyloxy, amino, lower alkylamino, lower alkanoylamino, lower alkanoyl, aroyl, halogen, nitro, (CH.sub.2).sub.m OR.sup. 7, (CH.sub.2).sub.m SR.sup.7, (CH.sub.2).sub.m CO.sub.2 R.sup.7 where R.sup.7 represents hydrogen or lower alkyl and m represents an integer of 0 to 3;each of R.sup.5 and R.sup.6 independently represents hydrogen or lower alkyl;U represents >N-- or ##STR3## W represents a single bond, --O-- or --S--; X represents ##STR4## wherein each of Y.sup.1 and Y.sup.2 independently represents hydrogen, lower alkyl, hydroxyl, lower alkanoyloxy, nitrile or phenyl; or Y.sup.1 and Y.sup.2 are combined together to form oxygen;each of Y.sup.3 and Y.sup.4 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 ##STR5## 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.

5. 发明授权

US4994468A Imidazoquinolone derivatives 失效
标题翻译：咪唑喹啉酮衍生物
公开(公告)号：US4994468A
公开(公告)日：1991-02-19
申请号：US489025
申请日：1990-03-05
申请人： Fumio Suzuki , Takeshi Kuroda , Yoshisuke Nakazato , Kenji Ohmori , Haruhiko Manabe
发明人： Fumio Suzuki , Takeshi Kuroda , Yoshisuke Nakazato , Kenji Ohmori , Haruhiko Manabe
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： Novel imidazoquinolone derivative represented by the formula (I); ##STR1## wherein R.sup.1 represents hydrogen, alkyl, cycloalkyl, alkenyl aralkyl, aralkenyl or substituted or unsubstituted aryl; X represents nitrogen or ##STR2## where R.sup.2 is hydrogen, hydroxyl, alkyl, cycloalkyl, alkenyl, aralkyl, aralkenyl, substituted or unsubstituted aryl, thiol, halogen, substituted or unsubstituted aromatic heterocyclic group, or --(CH.sub.2).sub.m CO.sub.2 R.sup.6 where R.sup.6 is hydrogen or lower alkyl and m is an integer of 0 to 3; Y represents oxygen or sulfur; R.sup.3 represents alkyl, cycloalkyl, alkoxyalkly, alkenyl, aralkyl, aralkenyl, --(CH.sub.2).sub.n -- Het where Het is substituted or unsubstituted aromatic heterocyclic group and n is an integer of 1 to 3 or --(CH.sub.2).sub.n CO.sub.2 R.sup.6a where n has the same meaning as defined above and R.sup.6a has the same meaning as defined as to R.sup.6 ; each of R.sup.4 and R.sup.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.

6. 发明授权

US5536730A Imidazonaphthyridine derivatives 失效
标题翻译：咪唑并萘啶衍生物
公开(公告)号：US5536730A
公开(公告)日：1996-07-16
申请号：US526323
申请日：1995-09-11
申请人： Fumio Suzuki , Takeshi Kuroda , Shigeto Kitamura , Kenji Ohmori
发明人： Fumio Suzuki , Takeshi Kuroda , Shigeto Kitamura , Kenji Ohmori
IPC分类号： A61K31/435 , A61K31/4375 , A61P11/08 , A61P29/00 , A61P37/08 , C07D471/14 , A61K31/41
CPC分类号： C07D471/14
摘要： Disclosed are imidazonaphthyridine derivatives represented by formula (I) ##STR1## wherein: R.sup.1 represents lower alkyl or substituted or unsubstituted aryl; andX-Y-Z represents ##STR2## wherein R.sup.2 represents hydrogen, lower alkyl, alkenyl, aralkenyl, or --C(R.sup.5)H--(CH.sub.2).sub.n --R.sup.4 (wherein R.sup.4 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 NR.sup.6 R.sup.7 wherein R.sup.6 and R.sup.7 independently represents hydrogen, or lower alkyl; R.sup.5 represents hydrogen, lower alkyl, or phenyl; and n represents an integer of 0 to 3); and R.sup.3 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）表示的咪唑并吡啶衍生物其中：R1表示低级烷基或取代或未取代的芳基; 并且XYZ表示其中R2表示氢，低级烷基，烯基，芳烯基或-C（R5）H-（CH2）n-R4（其中R4表示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，羟基取代的低级烷基，低级烷酰氧基，吗啉代，低级烷酰基，羧基，低级烷氧基羰基，环烷基，羟基，低级烷氧基，卤素或NR6R7，其中R6和R7独立代表氢或低级烷基; R5代表氢，低级烷基或苯基; n表示0〜3的整数）; 并且R 3表示氢，巯基，羟基，低级烷基或芳基及其药学上可接受的盐。这些化合物显示有效的抗炎，抗过敏和支气管扩张活性。

7. 发明授权

US5270316A Condensed purine derivatives 失效
标题翻译：凝血嘌呤衍生物
公开(公告)号：US5270316A
公开(公告)日：1993-12-14
申请号：US599758
申请日：1990-10-19
申请人： Fumio Suzuki , Junichi Shimada , Takeshi Kuroda , Kazuhiro Kubo , Akira Karasawa , Tetsuji Ohno , Kenji Ohmori
发明人： Fumio Suzuki , Junichi Shimada , Takeshi Kuroda , Kazuhiro Kubo , Akira Karasawa , Tetsuji Ohno , Kenji Ohmori
IPC分类号： A61K31/00 , A61K31/495 , A61K31/505 , A61K31/519 , A61K31/529 , A61P7/00 , A61P7/10 , A61P9/00 , A61P9/12 , A61P11/00 , A61P11/06 , A61P11/08 , A61P13/00 , A61P13/02 , A61P13/12 , A61P15/00 , C07D471/14 , C07D487/14 , A61K31/52
CPC分类号： C07D471/14 , C07D487/14
摘要： There are disclosed condensed purine derivatives represented by formula; ##STR1## in which R.sup.3 represents hydrogen, lower alkyl or benzyl; each of X.sup.1 and X.sup.2 independently represents hydrogen, lower alkyl, aralkyl or phenyl; and n is an integer of 0 or 1; R.sup.1 represents hydrogen, lower alkyl, alicyclic alkyl, noradamantan-3-yl, dicyclopropylmethyl or styryl; and R.sup.2 represents hydrogen, lower alkyl or alicyclic alkyl; or a pharmaceutically acceptable salt thereof. The derivatives and pharmaceutically acceptable salts are useful as diuretics, renal protecting agents, antiallergic agents and hypotensives.

8. 发明授权

US5468756A Imidazonaphthyridine derivatives 失效
标题翻译：咪唑并萘啶衍生物
公开(公告)号：US5468756A
公开(公告)日：1995-11-21
申请号：US241631
申请日：1994-05-12
申请人： Fumio Suzuki , Takeshi Kuroda , Shigeto Kitamura , Kenji Ohmori
发明人： Fumio Suzuki , Takeshi Kuroda , Shigeto Kitamura , Kenji Ohmori
IPC分类号： A61K31/435 , A61K31/4375 , A61P11/08 , A61P29/00 , A61P37/08 , C07D471/14 , C07D471/00 , A61K31/44
CPC分类号： C07D471/14
摘要： Disclosed are imidazonaphthyridine derivatives represented by formula (I) ##STR1## wherein: R.sup.1 represents lower alkyl or substituted or unsubstituted aryl; andX--Y--Z represents ##STR2## wherein R.sup.2 represents hydrogen, lower alkyl, alkenyl, aralkenyl, or --C (R.sup.5)H--(CH.sub.2).sub.n --R.sup.4 (wherein R.sup.4 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 NR.sup.6 R.sup.7 wherein R.sup.6 and R.sup.7 independently represents hydrogen or lower alkyl; R.sup.5 represents hydrogen, lower alkyl, or phenyl; and n represents an integer of 0 to 3); and R.sup.3 represents hydrogen, mercapto, hydroxy, lower alkyl, or aryland 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）表示的咪唑并吡啶衍生物其中：R1表示低级烷基或取代或未取代的芳基; 并且XYZ表示其中R2表示氢，低级烷基，烯基，芳烯基或-C（R5）H-（CH2）n-R4（其中R4表示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羟基取代的低级烷基，低级烷酰氧基，吗啉代，低级烷酰基，羧基，低级烷氧基羰基，环烷基，羟基，低级烷氧基，卤素或NR6R7，其中R6和R7独立地表示氢或低级烷基; R5表示氢，低级烷基或苯基; n表示0〜3的整数）。并且R 3表示氢，巯基，羟基，低级烷基或芳基及其药学上可接受的盐。这些化合物显示有效的抗炎，抗过敏和支气管扩张活性。

9. 发明授权

US5281610A Condensed naphthyridine derivatives 失效
标题翻译：缩合萘啶衍生物
公开(公告)号：US5281610A
公开(公告)日：1994-01-25
申请号：US993920
申请日：1992-12-18
申请人： Fumio Suzuki , Takashi Kawakita , Takeshi Kuroda , Kenji Ohmori , Hiroshi Nakajima , Toshikazu Kamiya , Tatsuya Tamaoki
发明人： Fumio Suzuki , Takashi Kawakita , Takeshi Kuroda , Kenji Ohmori , Hiroshi Nakajima , Toshikazu Kamiya , Tatsuya Tamaoki
IPC分类号： C07D471/14 , A61K31/435 , C07D471/22
CPC分类号： C07D471/14 , Y10S514/88
摘要： Disclosed is a pyrazolonaphthyridine compound represented by the formula: ##STR1## wherein R.sup.1 is represents hydrogen, lower alkyl, aralkyl, or substituted or unsubstituted aryl, R.sup.2 represents hydrogen, lower alkyl, thienyl, substituted or unsubsutituted aryl, hydroxy or amino, or a pharmaceutically acceptable salt thereof.The compound possesses antiinflammatory effect, immunosuppressive effect, broncho-dilatory effect and hair growth-stimulative effect.
摘要翻译：公开了由下式表示的吡唑并萘啶化合物：其中R 1表示氢，低级烷基，芳烷基或取代或未取代的芳基，R 2表示氢，低级烷基，噻吩基，取代或未取代的芳基，羟基或氨基，或其药学上可接受的盐。该化合物具有抗炎作用，免疫抑制作用，支气管扩张作用和毛发生长刺激作用。

10. 发明授权

US5192769A Condensed naphthyridine derivatives 失效
公开(公告)号：US5192769A
公开(公告)日：1993-03-09
申请号：US921720
申请日：1992-07-30
申请人： Fumio Suzuki , Takashi Kawakita , Takeshi Kuroda , Kenji Ohmori , Hiroshi Nakajima , Toshikazu Kamiya , Tatsuya Tamaoki
发明人： Fumio Suzuki , Takashi Kawakita , Takeshi Kuroda , Kenji Ohmori , Hiroshi Nakajima , Toshikazu Kamiya , Tatsuya Tamaoki
摘要： Disclosed is a pyrazolonaphthyridine compound represented by the formula: ##STR1## wherein R.sup.1 is represents hydrogen, lower alkyl, aralkyl, or substituted or unsubstituted aryl, R.sup.2 represents hydrogen, lower alkyl, thienyl, substituted or unsubstituted aryl, hydroxy or amino, or a pharmaceutically acceptable salt thereof.The compound possesses antiinflammatory effect, immunosuppressive effect, broncho-dilatory effect and hair growth-stimulative effect.

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