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1. 发明授权

US4604390A Antibacterial benzo(chalcogeno)[4,3,2-cd]indazoles 失效
标题翻译：抗菌苯并（硫霉素）[4,3,2-cd]吲唑
公开(公告)号：US4604390A
公开(公告)日：1986-08-05
申请号：US738195
申请日：1985-05-24
申请人： Edward F. Elslager , Leslie M. Werbel , Daniel F. Ortwine , Donald F. Worth , Howard D. H. Showalter , David B. Capps , Ellen M. Berman , Vlad E. Gregor , Anthony D. Sercel
发明人： Edward F. Elslager , Leslie M. Werbel , Daniel F. Ortwine , Donald F. Worth , Howard D. H. Showalter , David B. Capps , Ellen M. Berman , Vlad E. Gregor , Anthony D. Sercel
IPC分类号： C07C205/38 , C07C391/02 , C07D311/86 , C07D335/16 , C07D345/00 , C07D491/06 , C07D495/06 , C07D517/06 , A61K31/415 , A61K31/54
CPC分类号： C07D491/06 , C07C205/38 , C07C243/00 , C07C323/00 , C07C391/02 , C07D311/86 , C07D335/16 , C07D345/00 , C07D495/06 , C07D517/06 , C07D517/08
摘要： Substituted 2H-[1]benzopyrano[4,3,2-cd]indazoles, 2H-[1]benzothiopyrano[4,3,2-cd]indazoles, and 2H-[1]benzoselenino[4,3,2-cd]indazoles have demonstrated pharmacological activity against a broad spectrum of Gram-positive and Gram-negative bacteria, yeasts, and fungi, as well as activity against the L1210 and P388 murine leukemia cells lines.Pharmaceutical compositions containing the compounds and methods of employing the compounds in methods of treating bacterial or fungal infections and of inhibiting the growth of neoplasms in mammals are also disclosed.
摘要翻译：取代的2H- [1]苯并吡喃并[4,3,2-cd]吲唑，2H- [1]苯并噻喃并[4,3,2-cd]吲唑和2H- [1]苯并硒[4,3,2-cd ]吲唑已经证明了对广谱革兰氏阳性和革兰氏阴性细菌，酵母和真菌的药理活性，以及针对L1210和P388鼠白血病细胞系的活性。还公开了含有化合物的药物组合物和在治疗细菌或真菌感染和抑制哺乳动物肿瘤生长的方法中使用该化合物的方法。

2. 发明授权

US4626540A Substituted 1-amino-4-nitro-acridinones and methods of treating bacterial infections and leukemia with them 失效
标题翻译：取代的1-氨基-4-硝基吖啶酮及其治疗细菌感染和白血病的方法
公开(公告)号：US4626540A
公开(公告)日：1986-12-02
申请号：US658100
申请日：1984-10-10
申请人： David B. Capps
发明人： David B. Capps
IPC分类号： C07D219/06 , C07D219/08 , A61K31/47
CPC分类号： C07D219/08 , C07D219/06
摘要： Substituted 1-amino-4-nitroacridinones, their method of manufacture, pharmaceutical compositions and their use as antibacterial and antitumor agents are herein described.
摘要翻译：本文描述了取代的1-氨基-4-硝基吖啶酮，其制备方法，药物组合物及其作为抗细菌剂和抗肿瘤剂的用途。

3. 发明授权

US4555572A Pyrazolo[3,4,5-kl]acridine compositions and methods for their production and use 失效
标题翻译：吡唑并[3,4,5-kl]吖啶组合物及其生产和使用方法
公开(公告)号：US4555572A
公开(公告)日：1985-11-26
申请号：US619258
申请日：1984-06-15
申请人： David B. Capps
发明人： David B. Capps
IPC分类号： A61K31/47 , A61K31/435 , A61K31/695 , A61P31/04 , A61P35/00 , A61P35/02 , C07D471/04 , C07D471/06 , C07F7/18 , C07D471/02 , A61K31/41
CPC分类号： C07D471/06
摘要： Pyrazolo[3,4,5-kl]acridines are described as antibacterial agents and antitumor agents as well as pharmaceutical compositions and methods for their preparation.
摘要翻译：吡唑并[3,4,5-kl]吖啶被描述为抗菌剂和抗肿瘤剂，以及其制备方法。

4. 发明授权

US4207320A Amino-substituted imidazo[1,2-a:3,4-a']diquinolin-15-ium salts compositions and method of use 失效
标题翻译：氨基取代的咪唑并[1,2-a：3,4-a']二喹啉-15-盐组合物和使用方法
公开(公告)号：US4207320A
公开(公告)日：1980-06-10
申请号：US937234
申请日：1978-08-28
申请人： David B. Capps , Mario M. Angelo , Townley P. Culbertson
发明人： David B. Capps , Mario M. Angelo , Townley P. Culbertson
IPC分类号： C07D215/04 , C07D215/18 , C07D215/26 , C07D471/14 , A61K31/535
CPC分类号： C07D215/04 , C07D215/18 , C07D215/26 , C07D471/14
摘要： Amino-substituted imidazo[1,2-a:3,4-a']diquinolin-15-ium salts having the formula I: ##STR1## wherein R.sub.1 is hydrogen, lower alkyl, C.sub.4 -C.sub.6 cycloalkyl, di(lower alkyl)amino, 1-azetidinyl, 1-pyrrolidinyl, 1-piperidinyl, methyl-1-pyrrolidinyl, methyl-1-piperidinyl, 4-morpholinyl or 2,2-dimethylhydrazino;R.sub.2 is hydrogen, lower alkyl, lower alkylamino, di(lower alkyl)amino, C.sub.4 -C.sub.6 cycloalkylamino, lower alkoxy(lower alkyl)amino, 1-azetidinyl, 1-pyrrolidinyl, 1-piperidinyl, methyl-1-pyrrolidinyl, methyl-1-piperidinyl, hexahydro-1H-azepin-1-yl, 4-morpholinyl, benzylamino, N-methylbenzylamino or 2-phenylethylamino;R.sub.3 is hydrogen or methyl;X is an anion;with the proviso that at least one of R.sub.1 and R.sub.2 is other than hydrogen, lower alkyl or C.sub.4 -C.sub.6 cycloalkyl; and with the further proviso that when R.sub.2 is dimethylamino, at least one of R.sub.1 and R.sub.3 is other than hydrogen, and intermediates used in the preparation thereof are disclosed. The compounds of the invention are prepared by amination of the corresponding chloro or fluoro-substituted imidazo [1,2-a:3,4-a']diquinolin-15-ium salts; either the halo substituted intermediates or the amino substituted salts may be further treated, typically using ion exchange techniques to obtain a variety of physiologically acceptable amino-substituted [1,2-a:3,4-a']diquinolin-15-ium salts which exhibit antifungal activity.
摘要翻译：具有式I的氨基取代的咪唑并[1,2-a：3,4-a']二喹啉-15-盐其中R 1是氢，低级烷基，C 4 -C 6环烷基，二（低级烷基）氨基，1-氮杂环丁烷基，1-吡咯烷基，1-哌啶基，甲基-1-吡咯烷基，甲基-1-哌啶基，4-吗啉基或2,2-二甲基肼; R2是氢，低级烷基，低级烷基氨基，二（低级烷基）氨基，C4-C6环烷基氨基，低级烷氧基（低级烷基）氨基，1-氮杂环丁烷基，1-吡咯烷基，1-哌啶基，甲基-1-吡咯烷基， 1-哌啶基，六氢-1H-吖庚因-1-基，4-吗啉基，苄基氨基，N-甲基苄基氨基或2-苯乙基氨基; R3是氢或甲基; X是阴离子; 条件是R 1和R 2中的至少一个不是氢，低级烷基或C 4 -C 6环烷基; 并且进一步的条件是当R 2是二甲基氨基时，R 1和R 3中的至少一个不是氢，并且公开了其制备中使用的中间体。本发明的化合物是通过胺化相应的氯或氟取代的咪唑并[1,2-a：3,4-a']二喹啉-15-盐制备的; 可以进一步处理卤代替中间体或氨基取代的盐，通常使用离子交换技术获得各种生理上可接受的氨基取代的[1,2-a：3,4-a']二喹啉-15-盐其具有抗真菌活性。

5. 发明授权

US4621086A Method of treating leukemia with pyrazolo[3,4,5-kl]acridines 失效
标题翻译：用吡唑并[3,4,5-kl]吖啶处理白血病的方法
公开(公告)号：US4621086A
公开(公告)日：1986-11-04
申请号：US821318
申请日：1986-01-22
申请人： David B. Capps
发明人： David B. Capps
IPC分类号： C07D471/06 , A61K31/41 , C07D471/02
CPC分类号： C07D471/06 , Y10S514/908
摘要： Pyrazolo[3,4,5-kl]acridines are described as antibacterial agents and antitumor agents as well as pharmaceutical compositions and methods for their preparation.
摘要翻译：吡唑并[3,4,5-kl]吖啶被描述为抗菌剂和抗肿瘤剂，以及其制备方法。

6. 发明授权

US4588730A Pyrazolo[3,4,5-k1]acridine compositions and methods for their use as antimicrobials 失效
标题翻译：吡唑并[3,4,5-k1]吖啶组合物及其用作抗微生物剂的方法
公开(公告)号：US4588730A
公开(公告)日：1986-05-13
申请号：US768310
申请日：1985-08-22
申请人： David B. Capps
发明人： David B. Capps
IPC分类号： C07D471/06 , A61K31/44 , C07D219/06 , C07D219/08 , C07D401/04
CPC分类号： C07D471/06
摘要： Pyrazolo[3,4,5-k1]acridines are described as antibacterial agents and antitumor agents as well as pharmaceutical compositions and methods for their preparation.
摘要翻译：吡唑并[3,4,5-k1]吖啶被描述为抗菌剂和抗肿瘤剂，以及其制备方法和药物组合物。

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