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公开(公告)号:US06420379B1
公开(公告)日:2002-07-16
申请号:US09715083
申请日:2000-11-20
申请人: Ilaria Candiani , Angelo Bedeschi , Giuseppina Visentin , Maria Chiara Fagnola , Laura Capolongo
发明人: Ilaria Candiani , Angelo Bedeschi , Giuseppina Visentin , Maria Chiara Fagnola , Laura Capolongo
IPC分类号: A61K314745
CPC分类号: C07D491/22
摘要: The present invention relates to alkynyl-substituted camptothecins of formula (I) wherein X, R1, R2 are as defined herein, and the pharmaceutically salts thereof. These compounds are useful in therapy as antitumor agents.
摘要翻译: 本发明涉及其中X,R 1,R 2如本文所定义的式(I)的炔基取代的喜树碱及其药学上可接受的盐。 这些化合物可用于治疗作为抗肿瘤剂。
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公开(公告)号:US06211192B1
公开(公告)日:2001-04-03
申请号:US09355952
申请日:1999-08-12
申请人: Ilaria Candiani , Angelo Bedeschi , Giuseppina Visentin , Maria Chiara Fagnola , Laura Capolongo
发明人: Ilaria Candiani , Angelo Bedeschi , Giuseppina Visentin , Maria Chiara Fagnola , Laura Capolongo
IPC分类号: A61K314745
CPC分类号: C07D491/22
摘要: The present invention relates to alkynyl-substituted camptothecins of formula (I) wherein X, R1, R2 are as defined herein, and the pharmaceutically salts thereof. These compounds are useful in therapy as antitumor agents.
摘要翻译: 本发明涉及其中X,R 1,R 2如本文所定义的式(I)的炔基取代的喜树碱及其药学上可接受的盐。 这些化合物可用于治疗作为抗肿瘤剂。
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公开(公告)号:US5856496A
公开(公告)日:1999-01-05
申请号:US981472
申请日:1998-01-12
申请人: Maria Chiara Fagnola , Angelo Bedeschi , Ilaria Candiani , Giuseppina Visentin , Nicola Mongelli
发明人: Maria Chiara Fagnola , Angelo Bedeschi , Ilaria Candiani , Giuseppina Visentin , Nicola Mongelli
IPC分类号: C07D209/10 , B01J31/22 , C07D209/08 , C07D209/12 , C07D209/14 , C07D209/42 , C07D401/04 , C07D471/04
CPC分类号: C07D401/04 , C07D209/08 , C07D209/42 , B01J2219/0072
摘要: A process for preparing libraries of indole compounds by solid phase synthesis in the presence of organometallic catalysts. The resulting compounds have a very high purity degree, which allows biological testing on the crude products with a high confidence degree, without any cross contaminations.
摘要翻译: PCT No.PCT / EP97 / 02600 Sec。 371日期:1998年1月12日 102(e)日期1998年1月12日PCT提交1997年5月13日PCT公布。 第WO97 / 44319号公报 日期1997年11月27日在有机金属催化剂存在下通过固相合成制备吲哚化合物文库的方法。 所得化合物具有非常高的纯度,其允许对具有高置信度的粗产品进行生物测试,而没有任何交叉污染。
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公开(公告)号:US6093721A
公开(公告)日:2000-07-25
申请号:US269177
申请日:1999-05-13
IPC分类号: C07D491/22 , A61K31/47 , A61K31/4745 , A61P35/00 , C07D20060101
CPC分类号: C07D491/22
摘要: A water soluble camptothecin derivative which is 20(S)-7-ethyl-9(N-methyl-N-phenyl)amidino-camptothecin and pharmaceutically acceptable salts thereof, pharmaceutical compositions containing them and a process for their preparation are described. The compound of the invention and its pharmaceutically acceptable salts are useful antitumor agents and are further charactcrised by having a remarkable therapeutic index.
摘要翻译: PCT No.PCT / EP98 / 04919 371日期1999年5月13日 102(e)日期1999年5月13日PCT提交1998年7月20日PCT公布。 公开号WO99 / 05103 日期1999年2月4日为20(S)-7-乙基-9(N-甲基-N-苯基)脒基喜树碱及其药学上可接受的盐的水溶性喜树碱衍生物,含有它们的药物组合物及其制备方法 被描述。 本发明的化合物及其药学上可接受的盐是有用的抗肿瘤剂,并且通过具有显着的治疗指数进一步表征。
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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。
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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。
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公开(公告)号:US5459161A
公开(公告)日:1995-10-17
申请号:US78293
申请日:1993-06-25
IPC分类号: C07D307/84 , A61K31/34 , A61K31/343 , C07D307/79 , C07D307/83 , C07D405/12 , C07D451/04 , C07D451/14 , C07D453/02 , C07D453/06 , C07D455/02 , C07D471/08 , A61K31/40 , C07D207/08 , C07D307/78
CPC分类号: C07D307/79 , C07D307/83 , C07D307/84 , C07D405/12 , C07D451/04 , C07D453/02 , C07D453/06 , C07D455/02 , C07D471/08 , Y02P20/55
摘要: Substituted benzofuran derivatives of the formula (I): ##STR1## wherein one of R.sub.1 and R.sub.2 is hydrogen or halogen and the other is, independently, an amino group or a C.sub.2 -C.sub.4 alkanoyl amino group; R.sub.3 is hydrogen; a linear or branched C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy or C.sub.2 -C.sub.4 alkoxycarbonyl group; halogen; or phenyl unsubstituted or substituted by a C.sub.1 -C.sub.4 alkyl group; A is a group --(CH.sub.2).sub.n -Het wherein Het is an optionally substituted heteromonocyclic or heterobicyclic ring containing one or two nitrogen atoms, and n is zero or an integer of 1 to 3; and the symbol ..... represents a single or double bond; may be prepared by a process comprising reacting a compound of formula II: ##STR2## in which L is a leaving group and R.sub.4 is hydrogen or a carboxy protecting group, with a compound of formula III;R'.sub.3 --C.dbd.C--R'.sub.3 IIIto obtain a compound of formula IV; ##STR3## which is then cyclized to obtain a compound of formula V; ##STR4## which is reacted with a compound of formula VI;H.sub.2 N--A VI.
摘要翻译: PCT No.PCT / EP91 / 02512 Sec。 371日期:1993年6月25日 102(e)日期1993年6月25日PCT 1991年12月27日PCT PCT。 出版物WO92 / 12147 日本时间1992年7月23日。式(I)的取代苯并呋喃衍生物:其中R 1和R 2之一是氢或卤素,另一个独立地是氨基或C 2 -C 4烷酰基氨基; R3是氢; 直链或支链C 1 -C 4烷基,C 1 -C 4烷氧基或C 2 -C 4烷氧基羰基; 卤素; 或未被取代或被C 1 -C 4烷基取代的苯基; A是基团 - (CH 2)n -Het,其中Het是含有一个或两个氮原子的任选取代的杂单环或杂双环,且n为0或1至3的整数; 符号.....表示单键或双键; 可以通过包括使式II化合物:其中L是离去基团且R4是氢或羧基保护基的式II化合物与式III化合物反应来制备; R'3-C = C-R'3 III,得到式Ⅳ化合物; IV,然后将其环化以获得式V化合物; 其与式VI化合物反应; H2N-A VI。
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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。
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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。
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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.
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