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51. 发明授权

US5432172A Biological applications of alkaloids derived from the tunicate Eudistoma sp. 失效
标题翻译：生物应用生物碱衍生自细枝柄菌（Eudistoma sp。）
公开(公告)号：US5432172A
公开(公告)日：1995-07-11
申请号：US28322
申请日：1993-03-09
申请人： Ilan Spector , Nava R. Shochet , Yoel Kashman , Amira Rudi , Gary Gellerman
发明人： Ilan Spector , Nava R. Shochet , Yoel Kashman , Amira Rudi , Gary Gellerman
IPC分类号： A61K31/44 , C07D215/38 , C07D215/48 , C07D219/08 , C07D471/04 , C07D471/06 , C07D471/16 , C07D471/22 , A61K31/54
CPC分类号： C07D471/04 , A61K31/44 , C07D215/38 , C07D215/48 , C07D219/08 , C07D471/06
摘要： Biological applications of synthetic and natural alkaloids derived from the tunicate Eudistoma sp. are disclosed. A method regulating cell growth includes contacting one or more cells with an effective concentration of a compound for regulating cell growth. These compounds include: Segoline A, Segoline B, Isosegoline A, Norosegoline, Debromoshermilamine, Eilatin, 4-methylpyrido[2,3,4-kl]acridine, pyrido[2,3,4-kl]acridine, 1-acetyl-2,6-dimethylpyrido[2,3,4-kl]acridine, and derivatives and combinations of these compounds. An effective concentration range for using these compounds can range from approximately 0.1 .mu.M to 100 .mu.M. The effective concentration range for Eilatin, the most potent of these compounds is from 0.01 .mu.M to 0.99 .mu.M, and the effective concentration range for the other compounds of the present invention is from about 1.0 .mu.M to 100 .mu.M. The method has been shown to suppress growth of tumor cells, to induce differentiation of the tumor cells, and induce reverse transformation of the tumor cells. In transformed cells, the method induces reverse transformation. The method also inhibits the proliferation of cells. The examples show that the method of the present invention affects cyclic AMP mediated biological processes. At the effective concentrations this method affects the cyclic AMP mediated biological processes of cells to achieve the results described above.
摘要翻译：合成和天然生物碱的生物应用来源于调味汁。被披露。调节细胞生长的方法包括使一种或多种细胞与有效浓度的化合物接触以调节细胞生长。这些化合物包括：Segoline A，Segoline B，Isosegoline A，Norosegoline，脱氯西米明，Eilatin，4-甲基吡啶并[2,3,4-kl]吖啶，吡啶并[2,3,4-kl]吖啶，1-乙酰基-2 ，6-二甲基吡啶并[2,3,4-k]]吖啶，以及这些化合物的衍生物和组合。使用这些化合物的有效浓度范围可以为约0.1μM至100μM。这些化合物中最有效的Eilatin的有效浓度范围为0.01μM至0.99μM，并且对于本发明的其它化合物为约1.0μM至100μM。已经显示该方法抑制肿瘤细胞的生长，诱导肿瘤细胞的分化，并诱导肿瘤细胞的逆转化。在转化细胞中，该方法诱导逆转化。该方法还抑制细胞增殖。实施例表明本发明的方法影响环AMP介导的生物过程。在有效浓度下，该方法影响环AMP介导的细胞生物过程，以达到上述结果。

52. 发明授权

US5256532A Methods, reagents and test kits for determination of subpopulations of biological entities 失效
标题翻译：用于确定生物实体亚群的方法，试剂和试剂盒
公开(公告)号：US5256532A
公开(公告)日：1993-10-26
申请号：US345436
申请日：1989-05-01
申请人： Meryle J. Melnicoff , Katharine A. Muirhead , Paul K. Horan
发明人： Meryle J. Melnicoff , Katharine A. Muirhead , Paul K. Horan
IPC分类号： G01N33/53 , A61K41/00 , A61K47/48 , A61K49/00 , A61K49/06 , A61K49/18 , C07C229/16 , C07D209/08 , C07D219/08 , C07D263/62 , G01N33/532 , G01N33/534 , G01N33/543 , G01N33/553 , G01N33/569 , G01N33/577 , C12Q1/70
CPC分类号： A61K41/0085 , A61K47/48215 , A61K49/0002 , A61K49/0032 , A61K49/06 , A61K49/18 , A61K49/1896 , C07C229/16 , C07D209/08 , C07D219/08 , C07D263/62 , G01N33/569 , G01N33/56972 , Y10T436/24
摘要： Analytes, having a characteristic determinant that selectively interacts with a specific binding substance, are determined by coupling a reporter substance to the analyte, or to the specific binding substance, causing complex formation between the analyte and the specific binding substance in a test medium, separating the complexes thus formed from the test medium, and determining the presence or quantity of the analyte of interest by detecting the occurrence of the reporter substance in the complexes or the separated test medium. The determination is preferably performed on biomembrane-containing entities, such as cell subpopulations and/or subsets thereof, the reporter substance being stably associated with the lipid component of the biomembrane. Reagents and test kits are disclosed for performing the analyte determination.
摘要翻译：具有与特异性结合物质选择性相互作用的特征决定簇的分析物通过将报道物质与分析物或特异性结合物质偶联，导致测试介质中分析物与特异性结合物质之间的复合物形成，分离由测试培养基形成的复合物，并通过检测复合物或分离的测试培养基中报道物质的出现来确定感兴趣分析物的存在或数量。该测定优选在含有生物膜的实体（例如细胞亚群和/或其子集）上进行，报告物质与生物膜的脂质组分稳定相关。公开了用于进行分析物测定的试剂和测试试剂盒。

53. 发明授权

US5053513A Method of reducing a carbonyl containing acridine 失效
标题翻译：减少含有亚油酸的方法
公开(公告)号：US5053513A
公开(公告)日：1991-10-01
申请号：US500967
申请日：1990-03-29
申请人： Thomas B. K. Lee , George E. Lee , George S. K. Wong , Donna M. Borek , Keith E. Goehring
发明人： Thomas B. K. Lee , George E. Lee , George S. K. Wong , Donna M. Borek , Keith E. Goehring
IPC分类号： B01J23/40 , C07B61/00 , C07D219/08 , C07D219/10 , C07D221/16
CPC分类号： C07D219/10
摘要： A method of reducing a carbonyl containing acridine of the formula ##STR1## where n is 1, 2 or 3; X is hydrogen, loweralkyl, loweralkoxy, halogen, hydroxy, trifluoromethyl, or NR.sub.3 R.sub.4 where R.sub.3 and R.sub.4 are independently hydrogen or loweralkyl; R is hydrogen or loweralkyl and R.sub.1 is hydrogen, loweralkyl, diloweralkylaminoloweralkyl, arylloweralkyl, diarylloweralkyl, furylloweralkyl, thienylloweralkyl, oxygen-bridged arylloweralkyl, oxygen-bridged diarylloweralkyl, oxygen-bridged furylloweralkyl or oxygen-bridged thienylloweralkyl, is disclosed.

54. 发明授权

US4937345A Process for the preparation of 2-(arylamino)-3-carboxy-9(10H)-acridones 失效
标题翻译：制备2-（芳基氨基）-3-羧基-9（10H） - 吖啶酮的方法
公开(公告)号：US4937345A
公开(公告)日：1990-06-26
申请号：US254365
申请日：1988-10-06
申请人： Erwin Dietz , Heinrich Hamal , Frank Prokschy
发明人： Erwin Dietz , Heinrich Hamal , Frank Prokschy
IPC分类号： C07D219/08 , C07D471/04
CPC分类号： C07D219/08
摘要： A process for the preparation of 2-(arylamino)-3-carboxy-9(10H)-acridones of the formula A ##STR1## in which R and R' represent hydrogen, fluorine, chlorine or bromine atoms, alkyl(C.sub.1 -C.sub.4)-, oxalkyl(C.sub.1 -C.sub.4)- or carbonamide groups and x and y denote integers from 1 to 4, by cyclizing 2,5-diarylaminoterephthalic acids of the formula D ##STR2## in which R, R', x and y have the meanings mentioned previously, in a 5- to 15-fold amount by weight of polyphosphoric acid (P.sub.4 O.sub.10 content 80 to about 85%) or of an acidic polyphosphate (P.sub.4 O.sub.10 contents 75 to about 85%) as a water-abstracting agent at about 60.degree. C. to about 100.degree. C.
摘要翻译：制备式A的2-（芳基氨基）-3-羧基-9（10H） - 吖啶酮的方法，其中R和R'代表氢，氟，氯或溴原子，烷基（C1- C4） - ，氧代烷基（C1-C4） - 或酰胺基团，x和y表示1至4的整数，通过使式D的2,5-二芳基氨基对苯二甲酸环化，其中R，R'，x和 y具有上述含义，以聚磷酸（P4O10含量80-约85％）或酸性多磷酸酯（P4O10含量为75-约85％）的5-至15重量份作为取水剂在约60℃至约100℃

55. 发明授权

US4839364A 9-Amino-3,4-dihydroacridines and related compounds useful for enhancing memory 失效
标题翻译： 9-氨基-3,4-二氢吖啶和有助于增强记忆的相关化合物
公开(公告)号：US4839364A
公开(公告)日：1989-06-13
申请号：US7885
申请日：1987-01-28
申请人： Gregory M. Shutske , Frank A. Pierrat
发明人： Gregory M. Shutske , Frank A. Pierrat
IPC分类号： C07C255/42 , A61K31/435 , A61K31/47 , C07C20060101 , C07C67/00 , C07C253/00 , C07C255/58 , C07C255/59 , C07C255/60 , C07D219/08 , C07D219/10 , C07D219/12 , C07D221/16 , C07D409/12
CPC分类号： C07D409/12 , C07C255/00 , C07D219/10 , C07D219/12 , C07D221/16
摘要： There are disclosed compounds having the formula ##STR1## wherein n is 1, 2 or 3; X is hydrogen, loweralkyl, loweralkoxy, halogen, hydroxy, nitro, trifluoromethyl, NHCOR.sub.2 where R.sub.2 is loweralkyl, or NR.sub.3 R.sub.4 where R.sub.3 and R.sub.4 are independently hydrogen or loweralkyl; R is hydrogen or loweralkyl; R.sub.1 is hydrogen, loweralkyl, diloweralkylaminoloweralkyl, arylloweralkyl, diarylloweralkyl, furylloweralkyl, thienylloweralkyl, oxygen-bridged arylloweralkyl, oxygen-bridged diarylloweralkyl, oxygen-bridged furylloweralkyl or oxygen-bridged thienylloweralkyl; Y is C.dbd.O or CR.sub.5 OH where R.sub.5 is hydrogen or loweralkyl; Z is CH.sub.2 or C.dbd.CR.sub.6 R.sub.7 where R.sub.6 and R.sub.7 are independently hydrogen or loweralkyl; or Y and Z taken together is CR.sub.5 .dbd.Ch where CR.sub.5 and CH correspond to Y and Z respectively; an optical antipode thereof, or a pharmaceutically acceptable acid addition salt thereof, which are useful for enhancing memory, methods for synthesizing them, and pharmaceutical compositions comprising an effective memory enhancing amount of such a compound.
摘要翻译：公开了具有式“IMAGE”的化合物，其中n为1,2或3; X是氢，低级烷基，低级烷氧基，卤素，羟基，硝基，三氟甲基，NHCOR 2，其中R2是低级烷基，或NR3R4，其中R3和R4独立地是氢或低级烷基; R是氢或低级烷基; R 1是氢，低级烷基，二低级烷基氨基低级烷基，芳基低级烷基，二芳基低级烷基，呋喃基烷基，噻吩基低级烷基，氧桥连的芳基低级烷基，氧桥连的二芳基低级烷基，氧桥连的呋喃基低级烷基或氧桥连的噻吩基低级烷基。 Y是C = O或CR5OH，其中R5是氢或低级烷基; Z是CH 2或C = CR 6 R 7，其中R 6和R 7独立地是氢或低级烷基; 或Y和Z一起为CR5 = Ch，其中CR5和CH分别对应于Y和Z; 可用于增强记忆力的光学对映体或其药学上可接受的酸加成盐，以及合成它们的方法和包含有效记忆增加量的这种化合物的药物组合物。

56. 发明授权

US4745181A Polysubstituted aryl acridinium esters 失效
公开(公告)号：US4745181A
公开(公告)日：1988-05-17
申请号：US915527
申请日：1986-10-06
申请人： Say-Jong Law , Steve C. S. Chang , Stephen A. Palmacci , Roger S. Cubicciotti
发明人： Say-Jong Law , Steve C. S. Chang , Stephen A. Palmacci , Roger S. Cubicciotti
IPC分类号： C07D219/04 , C07D401/12 , C09K11/07 , G01N21/76 , G01N21/78 , G01N33/532 , C07K15/14 , C07D219/00 , C07D219/08 , C07H5/04 , C07H15/12 , C07H19/06
CPC分类号： C07D219/04 , Y10S530/802
摘要： The present invention relates to novel acridinium esters which are useful as luminescent labels in specific binding assays such as immunoassays or nucleic acid hybridization assays. More particularly, polysubstituted aryl acridinium esters are highly stable labels for use in a chemiluminescent immunoassay.

57. 发明授权

US3947449A Tetrahydroacridones having chemotherapeutic action and process for preparing them 失效
标题翻译：具有化疗作用的四氢吖啶酮及其制备方法
公开(公告)号：US3947449A
公开(公告)日：1976-03-30
申请号：US490652
申请日：1974-07-22
申请人： Walter Durckheimer , Wolfgang Raether , Hubert Georg Seliger
发明人： Walter Durckheimer , Wolfgang Raether , Hubert Georg Seliger
IPC分类号： C07D219/02 , A61K31/47 , A61K31/473 , A61P33/02 , C07D219/06 , C07D219/08
CPC分类号： C07D219/06 , C07D219/08
摘要： Tetrahydroacridones and their salts with physiologically tolerated acids and bases and process for preparing them. The compounds have a valuable chemotherapeutic action and may be used as drugs against protozoan diseases.
摘要翻译：四氢吖啶酮及其与生理上耐受的酸和碱的盐及其制备方法。这些化合物具有有价值的化学治疗作用，可用作抗原生动物疾病的药物。

58. 发明授权

US3838130A N10-oxides of 1-nitro-9-(dialkylamino-alkylamino)acridine 失效
标题翻译： 1-硝基-9-（二氨基甲酰基氨基）丙酸的N10-氧化物
公开(公告)号：US3838130A
公开(公告)日：1974-09-24
申请号：US20194671
申请日：1971-11-24
申请人： STAROGARDZKIE ZAKL FARMA
发明人： LEDOCHOWSKI A , STEFANSKA B
IPC分类号： C07D219/08 , C07D219/10 , C07D37/24
CPC分类号： C07D219/10 , C07D219/08
摘要： THE N-OXIDES OF 1-NITRO-9-(DIALKYLAMINOALKYLAMINO)ACRIDINE WHICH ARE ANTITUMOR AGENTS ARE PRODUCED BY OXIDIZING THE CORRESPONDING N10 OR NW OXIDES.

59. 发明授权

US3794723A Complexes of phosphanilic acid and 9-amino-3-nitroacridine useful as antifungal or antibacterial agents 失效
标题翻译：用作抗真菌剂或抗菌剂的磷酸和9-氨基-3-硝基吡啶的复合物
公开(公告)号：US3794723A
公开(公告)日：1974-02-26
申请号：US3794723D
申请日：1972-08-09
申请人： SMITHKLINE CORP
发明人： PAGANO J
IPC分类号： A01N43/42 , C07D219/08 , C07D219/10 , C07F9/38 , A01N9/36
CPC分类号： C07D219/10 , A01N43/42 , C07D219/08 , C07F9/3834 , A01N57/22 , A01N2300/00
摘要： Complexes of phosphanilic acid and an aminoacridine possess broad-spectrum antibacterial and antifungal activity when used topically. The preferred complex is a 1:1 complex of phosphanilic acid and 9-amino-3-nitroacridine.
摘要翻译：磷酸铵和氨基吖啶的配合物在局部使用时具有广谱抗菌和抗真菌活性。优选的络合物是磷酸铵和9-氨基-3-硝基吖啶的1:1复合物。

60. 发明授权

US3694448A 1-nitro-9-(dialkylaminoalkylamino)acridine n{11 oxides 失效
标题翻译： 1-硝基-9-（二氨基甲酰氨基）丙酸N {11氧化物
公开(公告)号：US3694448A
公开(公告)日：1972-09-26
申请号：US3694448D
申请日：1969-09-02
申请人： ANDRZEJ LEDOCHOWSKI , BARBARA STEFANSKA
发明人： LEDOCHOWSKI ANDRZEJ , STEFANSKA BARBARA
IPC分类号： C07F9/02 , C07D219/08 , C07D219/10 , C07D219/12 , C07D37/18
CPC分类号： C07D219/10 , C07D219/08 , C07D219/12
摘要： The N-oxides of 1-nitro-9-(dialkylaminoalkylamino)-acridine which are antitumor agents having low toxicity are produced by oxidizing the corresponding N10 of N oxides.
摘要翻译：作为具有低毒性的抗肿瘤剂的1-硝基-9-（二烷基氨基烷基氨基） - 吖啶的N-氧化物通过氧化相应的N氧化物的N10而产生。

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