公开(公告)号：US5908933A

公开(公告)日：1999-06-01

申请号：US897057

申请日：1997-07-18

申请人： Mladen Trkovnik ,  Zrinka Ivezic ,  Zeljko Kelneric ,  Ljerka Polak

发明人： Mladen Trkovnik ,  Zrinka Ivezic ,  Zeljko Kelneric ,  Ljerka Polak

IPC分类号： C07D491/02 ,  A61K31/435 ,  A61K31/436 ,  A61K31/47 ,  A61P31/04 ,  A61P31/12 ,  A61P35/00 ,  C07D411/04 ,  C07D491/052 ,  C07D491/12 ,  C07D491/14 ,  C07D491/147 ,  A61K31/44 ,  C07D471/02 ,  C07D471/04

CPC分类号： C07D411/04 ,  C07D491/14

摘要： The present invention relates to novel coumarin quinolone carboxylic acids wherein the pyridone system is fused in 3,4-, 6,7- and 7,8-positions of the coumarin system, of the general formula I ##STR1## wherein R.sup.1 R.sup.2 =--NHCH=C(CO.sub.2 R.sup.6)CO, R.sup.3 =NO.sub.2 or NH.sub.2, R.sup.4 =R.sup.5 =H, R.sup.6 =H or C.sub.2 H.sub.5 ;R.sup.1 R.sup.2 =--NHCH=C(CO.sub.2 R.sup.6)CO, R.sup.3 =R.sup.4 =H, R.sup.5 =F, R.sup.6 =H or C.sub.2 H.sub.5 ;R.sup.1 R.sup.2 =--CO(CO.sub.2 R.sup.6)C=CHNH, R.sup.3 =R.sup.4 =R.sup.5 =H, R.sup.6 =H or C.sub.2 H.sub.5 ;R.sup.1 R.sup.2 =R.sup.3 R.sup.4 =--NHCH=C(CO.sub.2 R.sup.6)CO, R.sup.5 =H, R.sup.6 =H or C.sub.2 H.sub.5 ;R.sup.1 =H or OH, R.sup.2 =R.sup.5 =H, R.sup.3 R.sup.4 =--NHCH (CO.sub.2 R.sup.6)CO, R.sup.6 =H or C.sub.2 H.sub.5 ;R.sup.1 =OH, R.sup.2 =R.sup.3 =H, R.sup.4 R.sup.5 =--CO(CO.sub.2 R.sup.6) C=CHNH, R.sup.6 =H or C.sub.2 H.sub.5 ;R.sup.1 =R.sup.5 =H, R.sup.2 =CH.sub.3 or CF.sub.3, R.sup.3 R.sup.4 =--CO(CO.sub.2 R.sup.6)C=CHNH, R.sup.6 =H or C.sub.2 H.sub.5,as well as pharmaceutically acceptable salts thereof.The object of the invention are also processes for the preparation of novel coumarin quinolone carboxylic acids and the biological action thereof.

摘要翻译： 本发明涉及新颖的香豆素喹诺酮羧酸，其中吡啶酮体系在香豆素体系的3,4,6,7和7,8位融合，通式Ⅰ其中R1R2 = -NHCH = C（ CO 2 R 6）CO，R 3 = NO 2或NH 2，R 4 = R 5 = H，R 6 = H或C 2 H 5; R1R2 = -NHCH = C（CO2R6）CO，R3 = R4 = H，R5 = F，R6 = H或C2H5; R1R2 = -CO（CO2R6）C = CHNH，R3 = R4 = R5 = H，R6 = H或C2H5; R1R2 = R3R4 = -NHCH = C（CO2R6）CO，R5 = H，R6 = H或C2H5; R1 = H或OH，R2 = R5 = H，R3R4 = -NHCH（CO2R6）CO，R6 = H或C2H5; R1 = OH，R2 = R3 = H，R4R5 = -CO（CO2R6）C = CHNH，R6 = H或C2H5; R1 = R5 = H，R2 = CH3或CF3，R3R4 = -CO（CO2R6）C = CHNH，R6 = H或C2H5，以及其药学上可接受的盐。 本发明的目的还在于制备新型香豆素喹诺酮羧酸及其生物学作用。

公开(公告)号：US5840922A

公开(公告)日：1998-11-24

申请号：US887217

申请日：1997-07-02

申请人： Mladen Trkovnik ,  Zrinka Ivezic ,  Ljerka Polak

发明人： Mladen Trkovnik ,  Zrinka Ivezic ,  Ljerka Polak

IPC分类号： C07D311/08 ,  A61K31/37 ,  C07D311/06 ,  C07D311/14 ,  C07D311/16 ,  C07D311/18 ,  C07D311/74 ,  C07D311/12

CPC分类号： C07D311/14 ,  C07D311/16 ,  C07D311/18

摘要： The present invention relates to new coumarin derivatives represented by the general formula I ##STR1## wherein R.sup.1 =NH.sub.2 or --NHCH.dbd.C(CO.sub.2 C.sub.2 H.sub.5).sub.2, R.sup.2 =R.sup.3 =R.sup.4 =H, R.sup.5 =F, R.sup.1 =R.sup.3 =NHCH.dbd.C(CO.sub.2 C.sub.2 H.sub.5).sub.2, R.sup.2 =R.sup.4 =R.sup.5 =H, R.sup.1 =H or OH, R.sup.3 =NHCH.dbd.C(CO.sub.2 C.sub.2 H.sub.5).sub.2, R.sup.2 =R.sup.4 =R.sup.5 =H, R.sup.1 =OH, R.sup.2 =R.sup.3 =R.sup.4 =H, R.sup.5 =--NHCH.dbd.C(CO.sub.2 C.sub.2 H.sub.5).sub.2, R.sup.1 =R.sup.3 =R.sup.5 =H, R.sup.2 =CH.sub.3 or CF.sub.3, R.sup.4 =--NHCH.dbd.C(CO.sub.2 C.sub.2 H.sub.5).sub.2, processes for the preparation thereof and their use as intermediates for the synthesis of new coumarin derivatives with potential biological action.

摘要翻译： 本发明涉及通式Ⅰ的化合物，其中R1 = NH2或-NHCH = C（CO2C2H5）2，R2 = R3 = R4 = H，R5 = F，R1 = R3 = NHCH = C（CO2C2H5）2，R2 = R4 = R5 = H，R1 = H或OH，R3 = NHCH = C（CO2C2H5）2，R2 = R4 = R5 = H，R1 = OH，R2 = R3 = R4 = R5 = -NHCH = C（CO2C2H5）2，R1 = R3 = R5 = H，R2 = CH3或CF3，R4 = -NHCH = C（CO2C2H5）2，其制备方法及其作为合成 新的香豆素衍生物具有潜在的生物学作用。

公开(公告)号：US20050075388A1

公开(公告)日：2005-04-07

申请号：US10491369

申请日：2001-10-01

申请人： Zrinka Ivezic ,  Mladen Trkovnik

发明人： Zrinka Ivezic ,  Mladen Trkovnik

IPC分类号： A61P31/18 ,  C07D311/48 ,  C07D493/04 ,  A61K31/366 ,  C07D45/14

CPC分类号： C07D493/04 ,  C07D311/48

摘要： Disclosed are a novel class of components obtained in reactions of condensation of hydroxycoumarin derivatives with aromatic and aliphatic dialdehydes, their preparation and antiviral action thereof, such as against HIV.

摘要翻译： 公开了在羟基香豆素衍生物与芳族和脂族二醛的缩合反应中获得的新一类成分，它们的制备和抗病毒作用，例如抗HIV。

公开(公告)号：US06100409A

公开(公告)日：2000-08-08

申请号：US165424

申请日：1998-10-02

申请人： Mladen Trkovnik ,  Zrinka Ivezic

发明人： Mladen Trkovnik ,  Zrinka Ivezic

IPC分类号： C07D311/42 ,  A61K31/35 ,  A61K31/352 ,  A61K31/353 ,  A61K31/37 ,  A61P31/12 ,  A61P31/18 ,  A61P37/04 ,  C07D311/04 ,  C07D311/44 ,  C07D311/46 ,  C07D311/48 ,  C07D311/54 ,  C07D311/56 ,  C07D311/84 ,  C07D407/06 ,  C07D407/10 ,  C07D407/14 ,  C07D311/16

CPC分类号： C07D311/46 ,  A61K31/37 ,  C07D311/44 ,  C07D311/48 ,  C07D311/56

摘要： The present invention relates to novel hydroxy and polyhydroxy derivatives of coumarin fused with dialdehydes and aldehyde acids of the general formulae I, II, III and IV: ##STR1## wherein R.sup.1 =R.sup.2 =4-hydroxycoumarin;R.sup.1 =R.sup.2 =4,7-dihydroxycoumarin;R.sup.1 =R.sup.2 =4,5,7-trihydroxycoumarin;R.sup.1 =4-hydroxycoumarin, R.sup.2 =--CH(OH)CH.sub.3.An object of the invention are also processes for the preparation of hydroxy and polyhydroxy derivatives of coumarin fused with dialdehydes and aldehyde acids, and the antiviral action thereof.Novel hydroxy and polyhydroxy derivatives of coumarin according to the present invention exhibit antiviral action against HIV-1 virus.

摘要翻译： 本发明涉及与通式I，II，III和IV的二醛和醛酸稠合的香豆素的新型羟基和多羟基衍生物：其中R1 = R2 = 4-羟基香豆素; R1 = R2 = 4,7-二羟基香豆素; R1 = R2 = 4,5,7-三羟基香豆素; R1 = 4-羟基香豆素，R2 = -CH（OH）CH3。 本发明的目的还在于制备与二醛和醛酸稠合的香豆素的羟基和多羟基衍生物及其抗病毒作用的方法。 根据本发明的香豆素的新型羟基和多羟基衍生物显示针对HIV-1病毒的抗病毒作用。

公开(公告)号：US06407073B1

公开(公告)日：2002-06-18

申请号：US09530973

申请日：2000-07-14

申请人： Mladen Trkovnik ,  Miroslav Trkovnik

发明人： Mladen Trkovnik ,  Miroslav Trkovnik

IPC分类号： A61K3135

CPC分类号： A61K31/37

摘要： A compound of the formula wherein W is H or a &bgr;-D-glucopyranoslyloxy group, and Y and Z are independently H, C1-6 alkyl, or C1-6 alkoxy or a pharmacologically acceptable derivative thereof, is effective in the treatment or prophylaxis of a disorder benefitting from a decrease in the activity or concentration of transaminase enzymes, particularly liver disorders. The compound is preferably administered orally as a dietary supplement in combination with one or more of bee pollen, matricaria camomile, asperula oderata, royal jelly or honey.

摘要翻译： 式Ⅳ的化合物是H或β-D-吡喃葡糖酰氧基，Y和Z独立地为H，C1-6烷基或C1-6烷氧基或其药理学上可接受的衍生物，在治疗或预防 这是由于转氨酶的活性或浓度的降低，特别是肝脏疾病的益处。 该化合物优选作为膳食补充剂与一种或多种蜂花粉，玫瑰花甘菊，杏仁，蜂王浆或蜂蜜一起口服给药。

公开(公告)号：US06291518B1

公开(公告)日：2001-09-18

申请号：US09476133

申请日：2000-01-03

申请人： Mladen Trkovnik ,  Zrinka Ivezić

发明人： Mladen Trkovnik ,  Zrinka Ivezić

IPC分类号： A61K31352

CPC分类号： C07D311/46 ,  A61K31/37 ,  C07D311/44 ,  C07D311/48 ,  C07D311/56

摘要： The present invention relates to novel hydroxy and polyhydroxy derivatives of coumarin fused with dialdehydes and aldehyde acids of the general formulae I, II, III and IV: wherein R1=R2=4-hydroxycoumarin; R1=R2=4,7-dihydroxycoumarin; R1=R2=4,5,7-trihydroxycoumarin; R1=4-hydroxycoumarin, R2=—CH(OH)CH3. An object of the invention are also processes for the preparation of hydroxy and polyhydroxy derivatives of coumarin fused with dialdehydes and aldehyde acids, and the antiviral action thereof. Novel hydroxy and polyhydroxy derivatives of coumarin according to the present invention exhibit antiviral action against HIV-1 virus.

摘要翻译： 本发明涉及与通式I，II，III和IV的二醛和醛酸稠合的香豆素的新型羟基和多羟基衍生物：其中R1 = R2 = 4-羟基香豆素; R1 = R2 = 4,7-二羟基香豆素; R1 = R2 = 4,5,7-三羟基香豆素; R1 = 4-羟基香豆素，R2 = -CH（OH）CH3。本发明的目的还是制备与二醛和醛酸稠合的香豆素的羟基和多羟基衍生物的方法， 和其抗病毒作用。根据本发明的香豆素的新型羟基和多羟基衍生物显示针对HIV-1病毒的抗病毒作用。