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1. 发明授权

US5614628A Process for the preparation of 9-amino camptothecin 失效
标题翻译：制备9-氨基喜树碱的方法
公开(公告)号：US5614628A
公开(公告)日：1997-03-25
申请号：US313906
申请日：1994-09-28
申请人： Walter Cabri , Ilaria Candiani , Franco Zarini , Angelo Bedeschi , Sergio Penco
发明人： Walter Cabri , Ilaria Candiani , Franco Zarini , Angelo Bedeschi , Sergio Penco
IPC分类号： A61K31/4375 , A61K31/47 , A61K31/4745 , A61P35/00 , A61P35/02 , A61P43/00 , C07B53/00 , C07D20060101 , C07D209/00 , C07D221/00 , C07D311/00 , C07D491/147 , C07D491/22 , F23C5/02
CPC分类号： C07D491/22 , F23C5/02
摘要： A process for preparing 9-amino camptothecin comprising the steps of: (1) reacting a compound of formula (III) ##STR1## wherein the hydroxy group on ring A is in the 10- or 12-position, with a nitrating agent, to form the corresponding 9-nitro compound; (2) converting the 9-nitro compound into a corresponding compound of formula (V) ##STR2## wherein XO is a group that can be removed reductively; and (3) reductively removing the XO group and reducing the nitro group of the compound of formula (V), to form the 9-amino camptothecin, a known antitumor compound. The present invention also includes compound having the above formula (V) and their 9-amino analogs, which have antitumor activity.
摘要翻译：一种制备9-氨基喜树碱的方法，包括以下步骤：（1）使环A上的羟基在10或12位的式（III）化合物（III）与硝化试剂，形成相应的9-硝基化合物; （2）将9-硝基化合物转化为相应的式（V）化合物其中XO是可以还原的基团; 和（3）还原性除去XO基团并还原式（Ⅴ）化合物的硝基，形成已知的抗肿瘤化合物9-氨基喜树碱。本发明还包括具有上述式（V）的化合物及其9-氨基类似物，其具有抗肿瘤活性。

2. 发明授权

US5916897A Process for the preparation of 9-amino camptothecin 失效
公开(公告)号：US5916897A
公开(公告)日：1999-06-29
申请号：US775605
申请日：1996-12-31
申请人： Walter Cabri , Ilaria Candiani , Franco Zarini , Angelo Bedeschi , Sergio Penco
发明人： Walter Cabri , Ilaria Candiani , Franco Zarini , Angelo Bedeschi , Sergio Penco
IPC分类号： A61K31/4375 , A61K31/47 , A61K31/4745 , A61P35/00 , A61P35/02 , A61P43/00 , C07B53/00 , C07D20060101 , C07D209/00 , C07D221/00 , C07D311/00 , C07D491/147 , C07D491/22 , F23C5/02
CPC分类号： C07D491/22 , F23C5/02
摘要： The present invention relates to compounds of the following formulas: ##STR1## which are endowed with antitumor activity. The invention also relates to methods of treating tumors using these compounds.

3. 发明授权

US5998426A 9,10 disubstituted camptothecin derivatives with antitumor activity 失效
标题翻译： 9,10具有抗肿瘤活性的二取代喜树碱衍生物
公开(公告)号：US5998426A
公开(公告)日：1999-12-07
申请号：US913855
申请日：1997-09-29
申请人： Angelo Bedeschi , Walter Cabri , Ilaria Candiani , Franco Zarini , Sergio Penco
发明人： Angelo Bedeschi , Walter Cabri , Ilaria Candiani , Franco Zarini , Sergio Penco
IPC分类号： A61K31/47 , A61P35/00 , C07D491/22
CPC分类号： C07D491/22
摘要： The present invention relates to 9-amino-10-(1-naphthylsulfonyloxy)-20(S)-camptothecin, 9-amino-10-phenylsulfonyloxy-20(S)-camptothecin, 7-ethyl-9-amino-10-(p-toluensulfonyloxy)-20(S)-camptothecin, their pharmaceutically acceptable salts, a process for their preparation, pharmaceutically compositions comprising them and their use as antitumor agents.
摘要翻译： PCT No.PCT / EP97 / 00194 Sec。 371日期：1997年9月29日 102（e）1997年9月29日PCT PCT 1997年1月11日PCT公布。出版物WO97 / 28164 日期：1997年8月7日本发明涉及9-氨基-10-（1-萘磺酰氧基）-20（S） - 喜树碱，9-氨基-10-苯基磺酰氧基-20（S） - 喜树碱，7-乙基-9- 氨基-10-（对甲苯磺酰氧基）-20（S） - 喜树碱，它们的药学上可接受的盐，其制备方法，包含它们的药物组合物及其作为抗肿瘤剂的用途。

4. 发明授权

US5856333A Substituted camptothecin derivatives and process for their preparation 失效
公开(公告)号：US5856333A
公开(公告)日：1999-01-05
申请号：US776192
申请日：1997-01-27
申请人： Walter Cabri , Ilaria Candiani , Angelo Bedeschi , Franco Zarini , Sergio Penco
发明人： Walter Cabri , Ilaria Candiani , Angelo Bedeschi , Franco Zarini , Sergio Penco
IPC分类号： A61K31/435 , A61P35/00 , C07D491/22
CPC分类号： C07D491/22
摘要： The present invention relates to substituted camptothecin derivatives of formula (I) wherein the symbol - - - - represents a single or double bond; R.sub.1, R.sub.2 and R.sub.3 are as defined under (a) or (b) below: (a) R.sub.1 and R.sub.2 are, each independently, hydrogen; C.sub.1 -C.sub.4 alkyl; C.sub.3 -C.sub.7 cycloalkyl; phenyl C.sub.1 -C.sub.6 alkyl; an optionally substituted phenyl ring; --NR.sub.5 R.sub.6 wherein one of R.sub.5 and R.sub.6 is hydrogen, C.sub.1 -C.sub.6 alkyl or benzyl and the other is hydrogen, C.sub.1 -C.sub.6 alkanoyl, an optionally substituted C.sub.1 -C.sub.6 alkoxycarbonyl, an optionally substituted benzoyl, phenyl C.sub.1 -C.sub.6 alkanoyl, an optionally substituted C.sub.1 -C.sub.6 alkoxycarbonyl, an optionally substituted phenoxycarbonyl or phenyl C.sub.1 -C.sub.6 alkoxycarbonyl, or R.sub.5 and R.sub.6, combined together with the nitrogen atom to which they are linked, form a 4-7 membered saturated, optionally substituted, heteromonocyclic ring residue; COOR.sub.8 wherein R.sub.8 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl or phenyl C.sub.1 -C.sub.6 alkyl; or COR.sub.9 wherein Rg is C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, phenyl C.sub.1 -C.sub.6 alkyl, an optionally substituted phenyl ring or NR.sub.10 R.sub.11 wherein R.sub.10 and R.sub.11 are, each independently, hydrogen or C.sub.1 -C.sub.6 alkyl; and R.sub.3 is hydrogen, C.sub.1 -C.sub.6 alkyl or an optionally substituted phenyl ring; or (b) R.sub.1 and R.sub.3, combined together, form a 5-8 membered, optionally substituted, carbomonocyclic ring, and R.sub.2 is hydrogen, C.sub.1 -C.sub.4 alkyl or C.sub.3 -C.sub.7 cycloalkyl; R.sub.4 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl or phenyl C.sub.1 -C.sub.6 alkyl; X is hydrogen,C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.3 -C.sub.7 cycloalkoxy, C.sub.1 -C.sub.6 alkanoyloxy, benzoyloxy, amino, hydroxy, nitro, halogen or it is a methylenedioxy group linked to the positions 10 and 11 of the molecule, and the pharmaceutically acceptable salts thereof. The compounds according to the invention are useful in therapy as antitumor agents. ##STR1##

5. 发明授权

US5801167A Camptothecin derivatives and process for their preparation 失效
标题翻译：喜树碱衍生物及其制备方法
公开(公告)号：US5801167A
公开(公告)日：1998-09-01
申请号：US697125
申请日：1996-08-20
申请人： Angelo Bedeschi , Franco Zarini , Walter Cabri , Ilaria Candiani , Sergio Penco , Laura Capolongo
发明人： Angelo Bedeschi , Franco Zarini , Walter Cabri , Ilaria Candiani , Sergio Penco , Laura Capolongo
IPC分类号： A61K31/47 , A61P35/00 , C07D491/22
CPC分类号： C07D491/22
摘要： The present invention relates to new camptothecin derivatives which display antitumor activity. The present invention also provides processes for their preparation as well as pharmaceutical compositions containing the same.
摘要翻译：本发明涉及显示抗肿瘤活性的新的喜树碱衍生物。本发明还提供了它们的制备方法以及含有它们的药物组合物。

6. 发明授权

US5602141A Camptothecin derivatives and process for their preparation 失效
标题翻译：喜树碱衍生物及其制备方法
公开(公告)号：US5602141A
公开(公告)日：1997-02-11
申请号：US389190
申请日：1995-02-15
申请人： Angelo Bedeschi , Franco Zarini , Walter Cabri , Ilaria Candiani , Sergio Penco , Laura Capolongo
发明人： Angelo Bedeschi , Franco Zarini , Walter Cabri , Ilaria Candiani , Sergio Penco , Laura Capolongo
IPC分类号： A61K31/47 , A61P35/00 , C07D491/22
CPC分类号： C07D491/22
摘要： The present invention relates to new camptothecin derivatives of the formula (I) ##STR1## wherein B is a group B' or B" ##STR2## wherein each of (x) and (y) is a single or double bond. The present invention also provides processes for their preparation as well as pharmaceutical compositions containing the same.
摘要翻译：本发明涉及式（I）的新喜树碱衍生物，其中B是B'或B“”B'“B”，其中（x）和（y）各自为单键或双键。本发明还提供了它们的制备方法以及含有它们的药物组合物。

7. 发明授权

US06403603B1 Process for the preparation of 9-amino camptothecin 失效
标题翻译：制备9-氨基喜树碱的方法
公开(公告)号：US06403603B1
公开(公告)日：2002-06-11
申请号：US08284129
申请日：1994-08-02
申请人： Angelo Bedeschi , Walter Cabri , Ilaria Candiani , Franco Zarini
发明人： Angelo Bedeschi , Walter Cabri , Ilaria Candiani , Franco Zarini
IPC分类号： C07D49122
CPC分类号： C07D491/22
摘要： 9-Amino-20(S)-camptothecin (I) is prepared by reducing 12-nitro-20(S)-camptothecin (II); converting the resulting 12-amino-20(S)-camptothecin (III) into a compound of formula (IV) wherein X is a group which can be reductively removed; reacting the compound of formula (IV) with a nitrating agent, to obtain thereby the corresponding 9-nitro-20(S)-camptothecin compound of formula (V) substituted at the 12-position by the group X; reducing in a single step the compound of formula (V), so obtaining the 9-amino-20(S)-camptothecin of formula (I); or reducing the compound of formula (V), so obtaining the corresponding 9-amino-20(S)-camptothecin compound of formula (VI) substituted at the 12-position by the group X and reductively removing the X group from the compound of formula (VI), so obtaining 9-amino-20(S)-camptothecin.
摘要翻译：通过还原12-硝基-20（S） - 喜树碱（II）制备9-氨基-20（S） - 喜树碱（I）将所得的12-氨基-20（S） - 喜树碱（III）转化成式（IV）的化合物，其中X是可被还原去除的基团; 使式（Ⅳ）化合物与硝化剂反应，由此获得在X-12位被12位取代的相应的9-硝基-20（S）喜树碱化合物。在一步中还原式（Ⅴ）化合物，从而得到式（I）的9-氨基-20（S） - 喜树碱; 或降低式（Ⅴ）化合物，从而得到在X基上被12位取代的相应的式（Ⅵ）的9-氨基-20（S） - 喜树碱化合物，并将X基团从式（VI），因此得到9-氨基-20（S） - 喜树碱。

8. 发明授权

US5382669A Process for the preparation of ergoline derivatives 失效
标题翻译：麦角灵衍生物的制备方法
公开(公告)号：US5382669A
公开(公告)日：1995-01-17
申请号：US28286
申请日：1993-03-09
申请人： Ilaria Candiani , Walter Cabri , Angelo Bedeschi , Franco Zarini
发明人： Ilaria Candiani , Walter Cabri , Angelo Bedeschi , Franco Zarini
IPC分类号： A61K31/48 , A61P5/08 , A61P25/16 , C07D457/06 , C07D457/04
CPC分类号： C07D457/06
摘要： The invention provides a process for the preparation of ergoline derivatives of the formula I ##STR1## the process comprising reacting an ergoline amide of the formula II with an isocyanate of formula III ##STR2## in presence of a metal catalyst and of a phosphorus compound. The compounds of the formula I are useful antiprolactinic and antiparkinson agents.
摘要翻译：本发明提供了制备式I的麦角灵衍生物的方法，该方法包括使式II的麦角灵酰胺与式III的异氰酸酯在金属催化剂和磷化合物的存在下反应。式I的化合物是有益的促乳素和抗帕金森药剂。

9. 发明授权

US5840899A Method for the preparation of 9-amino camptothecin 失效
标题翻译： 9-氨基喜树碱的制备方法
公开(公告)号：US5840899A
公开(公告)日：1998-11-24
申请号：US602792
申请日：1996-09-30
申请人： Angelo Bedeschi , Walter Cabri , Ilaria Candiani , Franco Zarini
发明人： Angelo Bedeschi , Walter Cabri , Ilaria Candiani , Franco Zarini
IPC分类号： C07D491/22
CPC分类号： C07D491/22
摘要： 9-Amino camptothecin of formula (I) ##STR1## is prepared by: 1) reducing a compound of formula (II): ##STR2## wherein Hal is 10- or 12-halogen, in a single step to the 9-amino-camptothecin of formula (I) or, alternatively, 2a) reductively removing the Hal group from a compound of formula (II) so obtaining the compound of formula (III): ##STR3## and 2b) reducing the compound of formula (III) so obtaining the 9-amino camptothecin of formula (I); the said steps 1 and 2a) and, optionally, step 2b) each being carried out in the presence of a catalytic amount of a compound of formula PdL.sub.2 wherein L is acetate or halogen and, additionally, in the presence of an ammonium formate as a hydrogen source. The 9-amino camptothecin of formula (I) is useful as inhibitor of the enzyme topoisomerase I. It is useful in the treatment of cancers, in particular leukaemia, colon and rectal tumours.
摘要翻译： PCT No.PCT / EP95 / 01692 Sec。 371日期1996年9月30日 102（e）1996年9月30日PCT PCT 1995年5月4日PCT公布。公开号WO95 / 32207 PCT （I）的氨基喜树碱的制备通过以下方法制备：1）还原式（II）的化合物：其中Hal是10-或12-卤素（I）的9-氨基喜树碱的单步骤，或者替代地，2a）从式（II）化合物还原性除去Hal基团，从而得到式（III）的化合物： III）和2b）还原式（III）的化合物，从而获得式（I）的9-氨基喜树碱; 所述步骤1和2a）和任选的步骤2b）各自在催化量的式PdL 2化合物的存在下进行，其中L是乙酸酯或卤素，另外在甲酸铵存在下，作为氢源。式（I）的9-氨基喜树碱可用作拓扑异构酶I的抑制剂。它可用于治疗癌症，特别是白血病，结肠和直肠肿瘤。

10. 发明授权

US5399679A (1'R,3S,4R)4-acylthio azetidinones 失效
标题翻译：（1'R，3S，4R）4-酰硫基氮杂环丁酮
公开(公告)号：US5399679A
公开(公告)日：1995-03-21
申请号：US54233
申请日：1993-04-30
申请人： Walter Cabri , Ilaria Candiani , Franco Zarini , Angelo Bedeschi
发明人： Walter Cabri , Ilaria Candiani , Franco Zarini , Angelo Bedeschi
IPC分类号： C07D205/09 , C07D401/12 , C07D405/12 , C07D499/88 , C07D499/897 , C07F7/18 , C07D499/00 , A61K31/425
CPC分类号： C07D401/12 , C07D205/09 , C07D405/12 , C07D499/88 , C07F7/186 , Y02P20/55
摘要： There is provided a process for preparing a compound of formula (I) ##STR1## wherein R is H or a hydroxy protecting group, R.sub.2 is an organic residue and R.sub.3 is H or a nitrogen protecting group, which process comprises reacting together a compound of formula (II) ##STR2## wherein R.sub.1 is a C.sub.1 -C.sub.4 alkyl or a phenyl group, R and R.sub.3 are as defined above, a compound of formula (III) ##STR3## wherein R.sub.2 is as defined above and X is a cation or a silicon-containing residue, and a salt of a group IIa, IIb or transition element. The compounds of formula (I) are intermediates in the synthesis of penem antibiotics.
摘要翻译：提供了制备式（I）化合物的方法，其中R是H或羟基保护基，R 2是有机残基，R 3是H或氮保护基，该方法包括使式（II）化合物其中R1是C1-C4烷基或苯基，R和R3如上所定义，式（III）化合物其中R 2是如上所定义，X是阳离子或含硅残基，以及Ⅱa，Ⅱb族或过渡元素的盐。式（I）化合物是合成penin抗生素的中间体。

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