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公开(公告)号：US5922750A
公开(公告)日：1999-07-13
申请号：US131290
申请日：1998-08-07
IPC分类号： C07D493/08 , A61K31/335 , A61K31/415 , A61K31/4178 , A61P35/00 , C07D233/64
CPC分类号： A61K31/4178
摘要： The present invention relates to terpenoidic derivatives, known in the art as Sarcodictyins, for use as therapeutic agents, and to pharmaceutical compositions containing them.In particular, Sarcodictyins can be useful as therapeutic antineoplastic agents in the treatment of cancers in human or animal beings.
摘要翻译： 本发明涉及本领域已知的作为Sarcodictyin用作治疗剂的萜类衍生物和含有它们的药物组合物。 特别地，Sarcodictyins可用作治疗人类或动物中的癌症的治疗性抗肿瘤剂。
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公开(公告)号：US5869514A
公开(公告)日：1999-02-09
申请号：US765436
申请日：1997-01-15
IPC分类号： C07D493/08 , A61K31/335 , A61K31/415 , A61K31/4178 , A61P35/00 , C07D233/64
CPC分类号： A61K31/4178
摘要： A method of treating tumors in a human or animal by administering thereto a pharmaceutically effective amount of a Sarcodictyin compound selected from Sarcodictyin A, B, C, D, E, and F. Sarcodictyin A has the formula (-)-(4R,4aR,7R,10S,11S,12aR,1Z,5E,8Z)-7,10-Epoxy3,4,4a,7,10,11,12,12a-octahydro-7-hydroxy-6-(methoxy-carbonyl)-1,10- dimethyl-4-(1-methylethyl)benzo cyclodecen-11-yl(E)-3-(1-Methyl-1H-imidazol-4-yl) acrylate (Sarcodictyin A).
摘要翻译： PCT No.PCT / EP96 / 01688 Sec。 371日期1997年1月15日 102（e）日期1997年1月15日PCT 1996年4月23日PCT PCT。 出版物WO96 / 36335 日本1996年11月21日一种通过向其施用药学有效量的选自Sarcodictyin A，B，C，D，E和F的Sarcodictyin化合物来治疗人或动物肿瘤的方法。Sarcodictyin A具有式（ - ） - （4R，4aR，7R，10S，11S，12aR，1Z，5E，8Z）-7,10-环氧基3,4,4a，7,10,11,12,12a-八氢-7-羟基-6-（ 甲氧基羰基）-1,10-二甲基-4-（1-甲基乙基）苯并环十一碳烯-11-基（E）-3-（1-甲基-1H-咪唑-4-基）丙烯酸酯（Sarcodictyin A）。
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公开(公告)号：US09408850B2
公开(公告)日：2016-08-09
申请号：US14116512
申请日：2012-05-07
IPC分类号： C07D231/56 , C07D401/12 , C07D295/185 , C07D405/12 , C07D403/12 , A61K31/496 , A61K31/416 , A61K31/5377 , C07D401/14 , C07D403/14 , A61K31/454 , A61K45/06 , C07D295/155
CPC分类号： A61K31/416 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K45/06 , C07D231/56 , C07D295/155 , C07D295/185 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C12N9/12 , C12Y207/10001
摘要： The present invention relates to substituted indazole compounds which modulate the activity of protein kinases and are therefore useful in treating diseases caused by degulated protein kinase activity, like cancer. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such these compounds or the pharmaceutical compositions containing them.
摘要翻译： 本发明涉及调节蛋白激酶活性的取代的吲唑化合物，因此可用于治疗由脱蛋白激酶活性引起的疾病，如癌症。 本发明还提供了制备这些化合物的方法，包含这些化合物的药物组合物，以及使用这些化合物治疗疾病的方法或含有它们的药物组合物的方法。
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公开(公告)号：US20050288238A1
公开(公告)日：2005-12-29
申请号：US10878212
申请日：2004-06-28
申请人： Mauro Angiolini , Sylvie Ducki , Maria Menichincheri , Nicola Mongelli , Ermes Vanotti , Marina Ciomei
发明人： Mauro Angiolini , Sylvie Ducki , Maria Menichincheri , Nicola Mongelli , Ermes Vanotti , Marina Ciomei
IPC分类号： A61K31/225 , A61K31/704 , C07C67/02 , C07C67/293 , C07C69/007 , C07C69/013 , C07C69/618 , C07D213/55 , C07D233/54 , C07D263/32 , C07D277/30 , C07H15/24
CPC分类号： C07D233/64 , C07C67/08 , C07C67/29 , C07C67/293 , C07C69/007 , C07C69/013 , C07C69/618 , C07C2602/12 , C07D213/55 , C07D263/32 , C07D277/30 , C07C69/16
摘要： A compound which is a benzocyclodecane of the formula I: wherein: at positions 8-9 and 11-12 independently represents a single or double bond, —R1 is ═O, or —OR7, R7 is H, C1-C7 alkanoyl, benzoyl, C1-C10 alkyl, C2-C10 alkenyl or COCH═CHR8, R8 is aryl or heterocyclyl; —R2 and —R3 are H, ═O or —OR9, R9 is H, C1-C7 alkanoyl or benzoyl; when at position 11-12 there is a single bond, then —R4 represents ═O, ═CH2, ═CHCOOR10, R10 is C1-C10 alkyl or aryl; ═CH(OCH3), —OR9; —CH2OR11, R11 is H or a sugar residue, —COR12, R12 is H, —OH or —OR10; or when at position 11-12 there is a double bond, then —R4 is —CH2OR11 or —COR12; —R5 and —R6 are H or, when at position 8-9 there is a single bond, taken together form a cyclopropane ring; R13 is H or 1-3 substituents selected from C1-C6 alkyl, C2-C6 alkenyl, phenyl, phenyl C1-C6 alkyl, halogen, hydroxy, C1-C6 alkoxy, aryloxy, cyano, nitro, amino, C1-C10 alkylamino, arylamino, C1-C7 alkanoylamino, aroylamino, hydroxycarbonyl, aminocarbonyl, C1-C6 alkylcarbonyl, C1-C6 alkylaminosulfonyl and arylaminosulfonyl group; with the provisos that if R1 and R4 ═O, then one of R2, R3, R5, R6 and R13 is not H atom; or a pharmaceutically acceptable salt thereof. These benzocyclodecane derivatives are endowed with antitumor activity; a process and new intermediates for their preparation, the pharmaceutical compositions containing them, and their use in the prevention, control and treatment of cancer are also provided.
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5.发明授权
公开(公告)号：US5420296A
公开(公告)日：1995-05-30
申请号：US66583
申请日：1993-05-25
申请人： Nicola Mongelli , Giovanni Biasoli , Alfredo Paio , Maria Grandi , Marina Ciomei
发明人： Nicola Mongelli , Giovanni Biasoli , Alfredo Paio , Maria Grandi , Marina Ciomei
IPC分类号： A61K31/40 , A61K31/7056 , A61P3/10 , A61P27/02 , A61P29/00 , A61P35/00 , A61P43/00 , C07D207/325 , C07D207/335 , C07D207/34 , C07D403/02 , C07D403/14
CPC分类号： C07D207/34
摘要： The invention relates to ureido derivatives of substituted pyrroles of formula ##STR1## wherein each of m and n, being the same, is an integer of 1 to 3; W is oxygen of sulphur;each of the B groups, which are the same, isa) a saturated or unsaturated, carbocyclic or condensed carbocyclic ring substituted by one or more acid groups;b) a saturated or unsaturated, heteromonocyclic or heterobicyclic ring, containing one or more heteroatoms chosen from nitrogen, oxygen and sulphur, substituted by one or more acid groups;c) a pyranyl or furanyl sugar residue substituted by one or more acid groups; ord) a --CH.sub.2 (CHA).sub.r CH.sub.2 A group, wherein each A group, being the same or different, is an acid group and r is 0, 1 or 2; and the pharmaceutically acceptable salts thereof, which are useful as angiogenesis inhibitors.
摘要翻译： 本发明涉及式（I）的取代吡咯的脲基衍生物，其中m和n各自相同，为1〜3的整数; W是硫的氧; 每个B基团相同，是a）被一个或多个酸基团取代的饱和或不饱和的碳环或稠合的碳环; b）饱和或不饱和的异单环或杂双环，其含有一个或多个选自氮，氧和硫的杂原子，被一个或多个酸基取代; c）被一个或多个酸基取代的吡喃基或呋喃基糖残基; 或d）-CH 2（CHA）r CH 2 A基团，其中每个A基团相同或不同，为酸基团，r为0,1或2; 及其药学上可接受的盐，其可用作血管生成抑制剂。
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6.发明申请Antitumor Combination Comprising Substituted Acryloyl Distamycin Derivatives and Antibodies Inhibiting Growth Factors or Their Receptors 审中-公开包含取代的丙烯酰基间质霉素衍生物和抑制生长因子或其受体的抗体的抗肿瘤组合公开(公告)号：US20090074757A1
公开(公告)日：2009-03-19
申请号：US11887998
申请日：2006-03-29
IPC分类号： A61K39/395 , A61P35/00
CPC分类号： A61K31/40 , A61K39/395 , A61K39/39533 , A61K39/39558 , C07K2317/24 , A61K2300/00
摘要： The present invention provides the combined use of acryloyl distamycin derivatives, in particular α-homo- and α-chloro-acryloyl distamycin derivatives of formula (I), as set forth in the specification, and an antibody inhibiting a growth factor or its receptor, in the treatment of tumors. Also provided is the use of the said combinations in the treatment or prevention of metastasis or in the treatment of tumors by inhibition of angiogenesis.
摘要翻译： 本发明提供丙烯酰基地霉素衍生物，特别是说明书所述的式（I）的α-均 - 和α-氯 - 丙烯酰基霉霉素衍生物和抑制生长因子或其受体的抗体的组合使用， 在治疗肿瘤。 还提供了所述组合在治疗或预防转移中或在通过抑制血管生成治疗肿瘤中的用途。
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公开(公告)号：US5912263A
公开(公告)日：1999-06-15
申请号：US964889
申请日：1997-11-05
申请人： Maria Menichincheri , Walter Ceccarelli , Marina Ciomei , Domenico Fusar Bassini , Nicola Mongelli , Ermes Vanotti
发明人： Maria Menichincheri , Walter Ceccarelli , Marina Ciomei , Domenico Fusar Bassini , Nicola Mongelli , Ermes Vanotti
IPC分类号： A61K31/335 , A61K31/337 , A61P35/00 , C07D305/14
CPC分类号： C07D305/14
摘要： Taxane derivatives modified at 13-position of the taxane derivative skeleton (taxol numbering) of formula (I), wherein R, R.sub.a, R.sub.b, R.sub.c, R.sub.1, R.sub.2, R.sub.3 are appropriate organic residues can be antitumor agents.
摘要翻译： 在式（I）的紫杉烷衍生物骨架（紫杉醇编号）的13位修饰的紫杉烷衍生物，其中R，Ra，Rb，Rc，R 1，R 2，R 3是合适的有机残基可以是抗肿瘤剂。
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公开(公告)号：US08946226B2
公开(公告)日：2015-02-03
申请号：US13055533
申请日：2009-07-28
IPC分类号： A61K45/06 , A61K31/4188 , A61K31/519
CPC分类号： A61K31/519 , A61K31/4188 , A61K45/06 , A61K2300/00
摘要： The invention provides a low molecular weight ATP-competitive CDK inhibitor able to cross the blood brain barrier for use in the treatment of malignant glioma and, in particular, of glioblastoma. The compound can be administered together with one or more agents selected from the group consisting of cytotoxic or cytostatic agents and ionizing radiation.
摘要翻译： 本发明提供了能够跨越血脑屏障用于治疗恶性胶质瘤，特别是胶质母细胞瘤的低分子量ATP竞争性CDK抑制剂。 化合物可以与一种或多种选自细胞毒性或细胞抑制剂和电离辐射剂的药物一起施用。
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公开(公告)号：US20110190311A1
公开(公告)日：2011-08-04
申请号：US13055533
申请日：2009-07-28
IPC分类号： C07D471/04 , A61K31/496 , A61P35/00
CPC分类号： A61K31/519 , A61K31/4188 , A61K45/06 , A61K2300/00
摘要： The invention provides a low molecular weight ATP-competitive CDK inhibitor able to cross the blood brain barrier for use in the treatment of malignant glioma and, in particular, of glioblastoma. The compound can be administered together with one or more agents selected from the group consisting of cytotoxic or cytostatic agents and ionizing radiation.
摘要翻译： 本发明提供了能够跨越血脑屏障用于治疗恶性胶质瘤，特别是胶质母细胞瘤的低分子量ATP竞争性CDK抑制剂。 化合物可以与一种或多种选自细胞毒性或细胞抑制剂和电离辐射剂的药物一起施用。
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10.发明授权Irreversible peptide ligands for bombesin receptors, their use, and process for making the same 失效BOMBESIN受体的不可逆肽配体，其使用及其制备方法
公开(公告)号：US5100873A
公开(公告)日：1992-03-31
申请号：US380539
申请日：1989-07-17
申请人： Roberto de Castiglione , Mauro Galantino , Fabio Corradi , Luigia Gozzini , Marina Ciomei , Isabella Molinari
发明人： Roberto de Castiglione , Mauro Galantino , Fabio Corradi , Luigia Gozzini , Marina Ciomei , Isabella Molinari
摘要： A peptide of formula (I):A-B-C-D-Gln-Trp-Ala-Val-X-Y-T-W (I)wherein either:(i) A represents a hydrogen atom, a Boc group or an acetyl group, one of B and C represents a pMel or mMel residue, and the other of B and C represents a sigma bond or a Gly, Leu-Gly, E-Leu-Gly or Gln-E-Leu-Gly, E, or E-Gly residue with E=Arg(A), arg(A), Lys(A), lys(A), Orn(A) and orn(A); or(ii) A represents a hydrogen atom;B represents a Glp-Arg-Leu-Gly residue;C represents a pMel or mMel residue;D represents a sigma bond or an Asn or Thr residue;X represents a Gly or ala residue;Y represents a sigma bond or a His(R.sub.1);his(R.sub.1), Phe, phe, Ser, ser, Ala or ala residue,T represents a sigma bond or a Leu, leu, Phe or phe residue;W represents an OH, amino, pentylamino or phenethyl-amino group or a Met-R.sub.2, Leu-R.sub.2, Ile-R.sub.2 or Nle-R.sub.2 residue;R.sub.1 represents a hydrogen atom or a Tos, Dnp or Bzl group; andR.sub.2 represents an amino, hydroxy, methoxy or hydrazino group;and its pharmaceutically acceptable salts are disclosed.
摘要翻译： 式（I）的肽：ABCD-Gln-Trp-Ala-Val-XYTW（I）其中：（i）A表示氢原子，Boc基或乙酰基，B和C之一表示pMel 或mMel残基，B和C中的另一个表示σ键或具有E = Arg（Gly）的Gly，Leu-Gly，E-Leu-Gly或Gln-E-Leu-Gly，E或E-Gly残基 ），arg（A），Lys（A），lys（A），Orn（A）和orn（A）; 或（ii）A表示氢原子; B表示Glp-Arg-Leu-Gly残基; C表示pMel或mMel残基; D表示σ键或Asn或Thr残基; X表示Gly或ala残基; Y表示σ键或His（R1）; 他的（R1），Phe，phe，Ser，ser，Ala或ala残基，T表示σ键或Leu，leu，Phe或phe残基; W表示OH，氨基，戊基氨基或苯乙基 - 氨基或Met-R2，Leu-R2，Ile-R2或Nle-R2残基; R1表示氢原子或Tos，Dnp或Bzl基团; 并且R 2表示氨基，羟基，甲氧基或肼基; 及其药学上可接受的盐。
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