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公开(公告)号：US06284887B1
公开(公告)日：2001-09-04
申请号：US09588339
申请日：2000-06-06
申请人： Achille Panzeri , Matteo D'Anello , Antonio Longo , Marcella Nesi
发明人： Achille Panzeri , Matteo D'Anello , Antonio Longo , Marcella Nesi
IPC分类号： C07J4300
CPC分类号： C07J73/005
摘要： A process for producing a compound of formula (I): wherein the dotted lines - - - independently represent a single or double bond and R, R1, R2 and R3 are each hydrogen or an organic radical, comprises treating the corresponding 17&bgr;-carbonylimidazole intermediates with anhydrous acids in the presence of an amine and, optionally, hydrogenating the resulting compound.
摘要翻译： 一种制备式（I）化合物的方法：其中虚线 - - - 独立地表示单键或双键，R，R 1，R 2和R 3各自为氢或有机基团，包括处理相应的17β-羰基咪唑中间体 与无水酸在胺的存在下，并任选地氢化所得化合物。
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公开(公告)号：US6121449A
公开(公告)日：2000-09-19
申请号：US367847
申请日：1999-08-27
申请人： Achille Panzeri , Matteo D'Anello , Antonio Longo , Marcella Nesi
发明人： Achille Panzeri , Matteo D'Anello , Antonio Longo , Marcella Nesi
CPC分类号： C07J73/005
摘要： A process for producing a compound of formula (I): ##STR1## wherein the dotted lines - - - independently represent a single or double bond and R, R.sub.1, R.sub.2 and R.sub.3 are each hydrogen or an organic radical, comprises treating the corresponding 17.beta.-carbonylimidazole intermediates with anhydrous acids in the presence of an amine and, optionally, hydrogenating the resulting compound.
摘要翻译： PCT No.PCT / EP98 / 08527 Sec。 371日期1999年8月27日第 102（e）1999年8月27日PCT 1998年12月17日PCT PCT。 公开号WO99 / 35161 日期1999年7月15日制备式（I）化合物的方法：其中虚线 - - - 独立地表示单键或双键，并且R，R 1，R 2和R 3各自为氢或有机基团， 在胺的存在下与无水酸反应，并任选地将所得化合物氢化，得到相应的17β-羰基咪唑中间体。
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3.发明授权Process for the preparation of 4-amino-unsaturated androstanedione derivatives 失效制备4-氨基 - 不饱和的雄烷二酮衍生物的方法
公开(公告)号：US5241090A
公开(公告)日：1993-08-31
申请号：US885856
申请日：1992-05-20
CPC分类号： C07J41/0094 , C07J41/0011 , C07J41/0022 , C07J71/001
摘要： 4-amino-unsaturated androstanedione derivatives provided with aromatase inhibitory activity are obtained by hydrolyzation of a corresponding compound of formula II ##STR1##
摘要翻译： 通过水解相应的式II化合物（II）得到具有芳香酶抑制活性的4-氨基 - 不饱和雄甾二醇衍生物
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公开(公告)号：USD663596S1
公开(公告)日：2012-07-17
申请号：US29319542
申请日：2008-06-11
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5.发明授权Azaindole derivatives, process for their preparation, and their use as antitumor agents 失效Azaindole衍生物，其制备方法及其作为抗肿瘤剂的用途公开(公告)号：US06486322B1
公开(公告)日：2002-11-26
申请号：US09968042
申请日：2001-10-02
申请人： Antonio Longo , Maria Gabriella Brasca , Paolo Orsini , Gabriella Traquandi , Valeria Pittalà , Anna Vulpetti , Mario Varasi , Paolo Pevarello
发明人： Antonio Longo , Maria Gabriella Brasca , Paolo Orsini , Gabriella Traquandi , Valeria Pittalà , Anna Vulpetti , Mario Varasi , Paolo Pevarello
IPC分类号： C07D47104
CPC分类号： C07D471/04
摘要： Novel 1H-pyrrolo[2,3-b]pyridines which are represented by formula (I): wherein R is a hydrogen or halogen atom or a group selected from —CN, —OH, —OCOR4, —(CH2)nNH2, —(CH2)nNHR4, —(CH2)nNHCOR4, —(CH2)nNHCONR4R5, —(CH2)nNHCOOR4, or —(CH2)nNHSO2R4, wherein n is either 0 or 1, R4 and R5 are as described in the specification; R1 is hydrogen or an optionally substituted alkyl group; R2 is an optionally substituted group selected from alkyl or aryl; R3 is hydrogen or a group selected from —CONR4R5, —COOR4, —CONHOR4, —SO2NHR4, alkylsulphonylaminocarbonyl or perfluorinated alkylsulphonylaminocarbonyl; or a pharmaceutically acceptable salt thereof, are disclosed. These compounds are useful for treating cell proliferative disorders associated with an altered cell dependent kinase activity.
摘要翻译： 由式（I）表示的新颖的1H-吡咯并[2,3-b]吡啶：其中R是氢或卤素原子或选自-CN，-OH，-OCOR 4， - （CH 2）n NH 2， （CH2）nNHR4， - （CH2）nNHCOR4， - （CH2）nNHCONR4R5， - （CH2）nNHCOOR4或 - （CH2）nNHSO2R4，其中n为0或1，R4和R5如说明书所述; R1是氢或任选取代的烷基; R2是任选取代的选自烷基或芳基的基团; R3是氢或选自-CONR4R5，-COOR4，-CONHOR4，-SO2NHR4，烷基磺酰基氨基羰基或全氟化烷基磺酰基氨基羰基的基团; 或其药学上可接受的盐。这些化合物可用于治疗与改变的细胞依赖性激酶活性相关的细胞增殖性病症。
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6.发明授权Hydrosoluble 3-arylidene-2-oxindole derivatives as tyrosine kinase inhibitors 失效可溶性3-亚芳基-2-羟吲哚衍生物作为酪氨酸激酶抑制剂
公开(公告)号：US5840745A
公开(公告)日：1998-11-24
申请号：US704760
申请日：1996-09-25
IPC分类号： A61K31/40 , A61K31/403 , A61K31/404 , A61K31/445 , A61P3/08 , A61P9/10 , A61P11/00 , A61P35/00 , A61P43/00 , C07D209/34 , C07D401/06 , C07D209/14 , C07D211/06
CPC分类号： C07D401/06 , C07D209/34
摘要： Novel hydrosoluble 3-arylidene-2-oxindole derivatives, having tyrosine kinase inhibitor activity, encompassed by general formula (I), wherein m is zero, 1 or 2; A is a bicyclic ring chosen from tetralin, naphthalene, quinoline and indole; R.sup.1 is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.2 -C.sub.6 alkanoyl; one of R.sup.2 and R.sup.3 independently is hydrogen and the other is a substituent selected from: a C.sub.1 -C.sub.6 alkyl group substituted by 1, 2 or 3 hydroxy groups; --SO.sub.3 R.sup.4 in which R.sup.4 is hydrogen or C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by 1, 2 or 3 hydroxy groups; --SO.sub.2 NHR.sup.5 in which R.sup.5 is as R.sup.4 defined above or a --(CH.sub.2).sub.n --N(C.sub.1 -C.sub.6 alkyl).sub.2 group in which n is 2 or 3; --COOR.sup.6 in which R.sup.6 is C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by phenyl or by 1, 2 or 3 hydroxy groups or phenyl; --CONHR.sup.7 in which R.sup.7 is hydrogen, phenyl or C.sub.1 -C.sub.6 alkyl substituted by 1, 2 or 3 hydroxy groups or by phenyl; --NHSO.sub.2 R.sup.8 in which R.sup.8 is C.sub.1 -C.sub.6 alkyl or phenyl unsubstituted or substituted by halogen or by C.sub.1 -C.sub.4 alkyl; --N(R.sup.9).sub.2, --NHR.sup.9 or --OR.sup.9 wherein R.sup.9 is C.sub.2 -C.sub.6 alkyl substituted by 1, 2 or 3 hydroxy groups; --NHCOR.sup.10, --OOCR.sup.10 or --CH.sub.2 OOCR.sup.10 in which R.sup.10 is C.sub.1 -C.sub.6 alkyl substituted by 1, 2 or 3 hydroxy groups; --NHCONH.sub.2 ; --NH--C(NH.sub.2).dbd.NH; --C(NH.sub.2).dbd.NH; --CH.sub.2 NHC(NH.sub.2).dbd.NH; --CH.sub.2 NH.sub.2 ; --OPO(OH).sub.2 ; --CH.sub.2 OPO(OH).sub.2 ; --PO(OH).sub.2 ; or (a), (b), (c), or (d) group, wherein p is 1, 2 or 3 and Z is --CH.sub.2 --, --O-- or (e), in which R.sup.11 is hydrogen or is as R.sup.9 defined above; and the pharmaceutically acceptable salts thereof, are disclosed.
摘要翻译： PCT No.PCT / EP95 / 05176 Sec。 371日期1996年9月25日 102（e）1996年9月25日PCT 1995年12月22日PCT PCT。 公开号WO96 / 22976 日期：1996年8月1日由通式（I）包含的具有酪氨酸激酶抑制剂活性的新型水溶性3-亚芳基-2-羟基吲哚衍生物，其中m为0,1或2; A是选自四氢化萘，萘，喹啉和吲哚的双环; R1是氢，C1-C6烷基或C2-C6烷酰基; R2和R3中的一个独立地是氢，另一个是选自：被1,2或3个羟基取代的C1-C6烷基; -SO 3 R 4，其中R 4是氢或未被取代或被1,2或3个羟基取代的C 1 -C 6烷基; -SO 2 NHR 5，其中R 5为上述定义的R 4或其中n为2或3的 - （CH 2）n -N（C 1 -C 6烷基）2基团; -COOR 6，其中R6是未被取代或被苯基取代或被1,2或3个羟基或苯基取代的C1-C6烷基; -CONHR 7，其中R 7是氢，苯基或被1,2或3个羟基取代的C 1 -C 6烷基或被苯基取代; -NHSO 2 R 8，其中R 8是C 1 -C 6烷基或未被取代或被卤素或被C 1 -C 4烷基取代的苯基; -N（R 9）2，-NHR 9或-OR 9，其中R 9为被1,2或3个羟基取代的C 2 -C 6烷基; -NHCOR 10，-OOCR 10或-CH 2 OO 10，其中R 10是被1,2或3个羟基取代的C 1 -C 6烷基; -NHCONH 2; -NH-C（NH 2）= NH; -C（NH 2）= NH; -CH 2 NHC（NH 2）= NH; -CH 2 NH 2; -OPO（OH）2; -CH 2 OPO（OH）2; -PO（OH）2; 或（a），（b），（c）或（d）基团，其中p为1,2或3，Z为-CH 2 - ， - O-或（e），其中R 11为氢或为 R9定义如下; 及其药学上可接受的盐。
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7.发明授权
公开(公告)号：US5663346A
公开(公告)日：1997-09-02
申请号：US592297
申请日：1996-02-09
IPC分类号： A61K31/435 , A61K31/445 , A61K31/495 , A61K31/535 , A61K45/06 , A61P35/00 , C07D471/04 , C07F9/6561 , C07D471/02 , A01N43/34 , C07D403/02 , C07D405/02
CPC分类号： C07D471/04 , C07F9/6561
摘要： The present invention relates to compounds useful as tyrosine kinase inhibitors, having the following general formula (I) ##STR1## wherein one of the groups X.sup.1, X.sup.2, X.sup.3, X.sup.4 is N and the others are CH; R is a group of formula (a), (b), (c) or (d) ##STR2## each of R.sup.1 and R.sup.3 independently is hydrogen, amino, carboxy, cyano, --SO.sub.3 R.sup.4, --SO.sub.2 NHR.sup.5, ##STR3## --COOR.sup.6, --CONH(CH.sub.2).sub.o Ph, --CONHCH.sub.2 (CHOH).sub.n CH.sub.2 OH, ##STR4## --N (CH.sub.2 CH.sub.2 OH).sub.2, --NHCH.sub.2 (CHOH).sub.n CH.sub.2 OH, --NHCONH.sub.2, --NHC(NH.sub.2).dbd.NH, --NHCO(CHOH).sub.n CH.sub.2 OH, ##STR5## --NHSO.sub.2 R.sup.7, --OCH.sub.2 (CHOH).sub.n CH.sub.2 OH, --OOC(CHOH).sub.n CH.sub.2 OH, --OPO(OH).sub.2, --OCH.sub.2 SO.sub.2 NH.sub.2, --CH.sub.2 NH.sub.2, --C(NH.sub.2).dbd.NH, --CH.sub.2 NHC(NH.sub.2).dbd.NH, ##STR6## --CH.sub.2 OH, --CH.sub.2 OOC(CHOH).sub.n C.sub.2 OH, --CH.sub.2 OPO(OH).sub.2, --PO(OH).sub.2 ;R.sup.2 is H, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkanoyl, --CH.sub.2 OH, --CH.sub.2 CH.sub.2 CONH.sub.2, --SO.sub.2 Me, --COCH.sub.2 SO.sub.2 NH.sub.2 ;R.sup.4 is H, --CH.sub.2 (CHOH).sub.n CH.sub.2 OH, C.sub.1 -C.sub.6 alkyl;R.sup.5 is H, C.sub.1 -C.sub.6 alkyl, --CH.sub.2 (CHOH).sub.n CH.sub.2 OH, --(CH.sub.2).sub.m NMe.sub.2 ;R.sup.6 is C.sub.1 -C.sub.6 alkyl, unsubstituted or substituted by phenyl, --CH.sub.2 (CHOH).sub.n CH.sub.2 OH;R.sup.7 is Me, --C.sub.6 H.sub.4 Me;Z is CH.sub.2, O, NH, NCH.sub.2 CH.sub.2 OH;n is 1 or 1;m is 2 or 3;o is 0, 1, 2 or 3;p is 1, 2 or 3;provided that when R is (a), (b), or (c) then R.sup.1 is not H and when R is (d) then one of R.sup.1 and R.sup.3 is not H; and the pharmaceutically acceptable salts thereof.
摘要翻译： PCT No.PCT / EP95 / 02043 Sec。 371日期1996年2月9日 102（e）日期1996年2月9日PCT提交1995年5月30日PCT公布。 出版物WO96 / 00226 日本1996年1月4日本发明涉及可用作酪氨酸激酶抑制剂的化合物，具有以下通式（I）其中X 1，X 2，X 3，X 4基团之一为N且其它基团为CH ; （a），（b），（c）或（d）中的每一个，R 1和R 3分别为 独立地是氢，氨基，羧基，氰基，-SO 3 R 4，-SO 2 NHR 5，-COOR 6，-CONH（CH 2）oPh，-CONHCH 2（CHOH）n CH 2 OH，-N（CH 2 CH 2 OH）2，-NHCH 2（CHOH ）nCH 2 OH，-NHCONH 2，-NHC（NH 2）= NH，-NHCO（CHOH）n CH 2 OH，图像 - -NHSO 2 R 7，-OCH 2（CHOH）n CH 2 OH，-OOC（CHOH）n CH 2 OH，-OPO（OH）2，-OCH 2 SO 2 NH ，-CH 2 NH 2，-C（NH 2）= NH，-CH 2 NHC（NH 2）= NH，-CH 2 OH，-CH 2 OOC（CHOH）n C 2 OH，-CH 2 OPO（OH）2，-PO（OH） R2是H，C1-C6烷基，C2-C6烷酰基，-CH2OH，-CH2CH2CONH2，-SO2Me，-COCH2SO2NH2; R4是H，-CH2（CHOH）nCH2OH，C1-C6烷基; R5是H，C1-C6烷基，-CH2（CHOH）nCH2OH， - （CH2）mNMe2; R6是未取代或被苯基取代的C1-C6烷基，-CH2（CHOH）nCH2OH; R7是Me，-C6H4Me; Z是CH 2，O，NH，NCH 2 CH 2 OH; n为1或1; m为2或3; o为0,1,2或3; p为1,2或3; 条件是当R是（a），（b）或（c）时，R 1不是H，当R是（d）时，R 1和R 3之一不是H; 及其药学上可接受的盐。
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8.发明授权Synthesis of 6-methylene derivatives of androsta-1,4-diene-3,17-dione 失效雄甾-1,4-二烯-3,17-二酮的6-亚甲基衍生物的合成
公开(公告)号：US4990635A
公开(公告)日：1991-02-05
申请号：US294016
申请日：1989-01-06
申请人： Antonio Longo , Paolo Lombardi
发明人： Antonio Longo , Paolo Lombardi
IPC分类号： A61K31/565 , A61P35/00 , C07J1/00 , C07J75/00
CPC分类号： C07J1/0011 , C07J75/00
摘要： The invention relates to a new process for the preparation of known aromatase inhibitors of the following formula (I) ##STR1## wherein each of R.sub.1 and R.sub.3, independently, is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.2 is hydrogen, halogen or C.sub.1 -C.sub.6 alkyl; andR.sub.4 is hydrogen or fluorine;the process comprising submitting to Mannich reaction a compound of formula (II) ##STR2## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as defined above and R is a lower alkyl group, and then dehydrogenating the respective 6-methylene-3-oxo-.DELTA..sup.4 -steroid derivative thus obtained, by methods known per se.
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公开(公告)号：US4865766A
公开(公告)日：1989-09-12
申请号：US192138
申请日：1988-05-10
IPC分类号： A61K31/565 , C07J41/00
CPC分类号： C07J41/0011
摘要： A process for the preparation of 4-aminoandrostenediones of formula (I) ##STR1## and pharmaceutically acceptable salts thereof, wherein one of R.sub.1 and R.sub.2 is hydrogen and the other is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl or C.sub.2 -C.sub.6 alkynyl, and the symbol indicates that each of (x) and (y), independently, is a single bond or a double bond, comprising reacting a compound of formula (II) ##STR2## wherein E is a halogen atom and R.sub.1, R.sub.2, (x) and (y) each are as defined as above with ammonia.
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公开(公告)号：US09173546B2
公开(公告)日：2015-11-03
申请号：US10579014
申请日：2004-11-16
CPC分类号： A61B1/00085 , A61B1/00087 , A61B1/31 , A61B1/32
摘要： A diagnostic device (10) for pathologies of tubular anatomical structures comprises a tubular elongated structure (12, 28) developing between a proximal end and a distal end and is adapted to be inserted in the tubular anatomical structure, means (22) for locally dilating the walls of the tubular anatomical structure being associated with the distal end of said elongated structure, said means for locally dilating being movable between a closed position for introducing the device and at least one open position for viewing and evaluating the pathology, and control means being associated with the proximal end of the elongated structure, said control means being operatively connected to said means for locally dilating, in order to move them between the closed position and the open position, and vice versa.
摘要翻译： 用于管状解剖结构病理的诊断装置（10）包括在近端和远端之间形成的管状细长结构（12,28），并适于插入管状解剖结构中，用于局部扩张的装置（22） 所述管状解剖结构的壁与所述细长结构的远端相关联，所述用于局部扩张的装置可在用于引入装置的关闭位置和用于观察和评估病理的至少一个打开位置之间移动，以及控制装置 与所述细长结构的近端相关联，所述控制装置可操作地连接到所述用于局部扩张的装置，以便在关闭位置和打开位置之间移动它们，反之亦然。
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