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1.发明公开COMPOUNDS AND METHODS FOR DIAGNOSING AND TREATING AMYLOID-RELATED CONDITIONS 审中-公开化合物和方法进行诊断和治疗淀粉样蛋白相关疾病
公开(公告)号：EP1318982A1
公开(公告)日：2003-06-18
申请号：EP01968919.9
申请日：2001-09-17
发明人： RAUB, Thomas, J. , TANIS, Steven, P. , BUHL, Allen, Edwin , CARTER, Donald, Bainbridge , BANDIERA, Tiziano , LANSEN, Jacqueline , PELLERANO, Cesare , SAVINI, Luisa
IPC分类号： C07D215/38 , A61K31/47
CPC分类号： C07D215/38 , A61K31/47 , A61K45/06 , A61K51/0455 , A61K2300/00 , A61K31/00
摘要： The invention provides methods for diagnosing and treating amyloid-related conditions and compounds useful for the same. The invention provides for detecting, imaging, monitoring, diagnosing, and treating conditions characterized by the binding or aggregation of amyloid fibrils. More particularly, the invention relates to using quinolinehydrazone compounds for diagnosing and treating amyloidotic conditions and also as an antioxidant.
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2.发明公开COMBINED PREPARATIONS COMPRISING MORPHOLINE ANTHRACYCLINES AND ANTICANCER AGENT 有权联合制剂THAT吗啉蒽环类抗癌和培养基中
公开(公告)号：EP1173187A2
公开(公告)日：2002-01-23
申请号：EP00925158.8
申请日：2000-04-04
CPC分类号： A61K45/06 , A61K31/675 , A61K31/70 , A61K2300/00
摘要： The present invention relates to combined preparations comprising a morpholinyl anthracycline administered in combination anticancer agents chosen from an alkylating agent, an antimetabolite, a topoisomerase II inihbitor, a topoisomerase I inhibitor, an antimitotic drug and a platinum derivative, which are useful anticancer therapy, particularly in the treatment of a primary or metastatic liver cancer.
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公开(公告)号：EP1169035A2
公开(公告)日：2002-01-09
申请号：EP00904990.9
申请日：2000-01-31
IPC分类号： A61K31/396 , A61K31/351 , A61K31/555 , A61K31/352 , A61P35/00
CPC分类号： A61K31/704 , A61K31/335 , A61K31/555 , A61K31/70 , A61K45/06 , A61K2300/00
摘要： There are provided the combined use of 4-demethoxy-3'-deamino-3'-aziridinyl-4'-methansulfonyl daunorubicin or 4-demethoxy-N,N-bis(2-chloroethyl)-4'-methansulfonyl daunorubicin and an anti-neoplastic anti-mitotic compound and/or a platinum derivative in the treatment of tumors, as well as in the prevention or treatment of metastasis or in the treatment of tumors by inhibition of angiogenesis.
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4.发明授权SUBSTITUTED TETRALYLMETHYLEN-OXINDOLE ANALOGUES AS TYROSINE KINASE INHIBITORS 失效取代TETRALYLMETHYLENOXINDOL物作为酪氨酸激酶抑制剂
公开(公告)号：EP0853614B1
公开(公告)日：2001-10-04
申请号：EP97927034.5
申请日：1997-05-15
IPC分类号： C07D209/34 , A61K31/40 , A61P35/00 , A61P37/02
CPC分类号： C07D209/34
摘要： Tetralylmethylen-2-oxindole derivatives having formula (I) wherein one or two of R, R1, R2 and R3 the said two being the same or different, are selected from: a) -X-(CH2)m-NH2, -X-(CH2)m-NR4R5 or -X-(CH2)m-NHR6 group, b) -NH-C(=NH)-NR4R5, -NH-C(=NH)-NHR6, -N=CH-NH2, -N=CH-NR4R5 or -N=CH-NHR6, c) -X-(CH2)n-COR7, d) -CORa or -COR8, e) -Y-CO-Y'-R9 group, f) -NHR6 or -NHR10 group and the pharmaceutically acceptable salts of the salt forming derivatives of formula (I) as defined above, are tyrosine kinase inhibitors.
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5.发明授权BICYCLIC 4-ARALKYLAMINOPYRIMIDINE DERIVATIVES AS TYROSINE KINASE INHIBITORS 失效双环4- aralkylaminopyrimidine衍生物作为酪氨酸激酶抑制剂
公开(公告)号：EP0853616B1
公开(公告)日：2001-09-19
申请号：EP97925987.6
申请日：1997-06-03
IPC分类号： C07D239/94 , C07D473/34 , A61K31/70 , A61K31/505
CPC分类号： C07D473/34 , C07D239/94
摘要： Novel and known bicyclic 4-aralkylaminopyrimidine derivatives of formula (I) wherein A is a benzene or imidazole ring; B is a benzene, tetralin, indane or 2-oxindole ring R is (C1-C4)perfluoroalkyl, phenyl, phenyl-(C1-C4)alkyl, hydroxy-(C1-C4)alkyl, (C1-C4)alkoxy-(C1-C4)alkyl, (C2-C4)acyloxy-(C1-C4)alkyl, halobenzoyloxy-(C1-C4)alkyl, carboxy, carbamoyl, (C1-C4)alkoxycarbonyl, cyano, (C1-C4)alkylcarbonyl, carboxy-(C1-C4)alkyl, carbamoyl-(C1-C4)alkyl, (C1-C4)alkoxycarbonyl-(C1-C4)alkyl, halo-(C1-C4)alkyl, amino-(C1-C4)alkyl, mono- or di-(C1-C4)alkylamino-(C1-C4)alkyl, sulfo-(C1-C4)alkyl or sulfamido-(C1-C4)alkyl; each of R1 and R2, which may be the same or different, is hydrogen, C1-C4 alkyl, C1-C4 alkoxy, halogen or -NR5R6 in which each of R5 and R6, which may be the same or different, is H or C1-C4 alkyl; each of R3 and R4, which may the same or different, is hydrogen, C1-C4 alkyl, halogen, hydroxy, C1-C4 alkoxy, C1-C4 alkoxycarbonyl, nitro, cyano or CF3; and the pharmaceutically acceptable salts thereof, are tyrosine kinase inhibitors.
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公开(公告)号：EP1126851A1
公开(公告)日：2001-08-29
申请号：EP00947971.8
申请日：2000-07-11
IPC分类号： A61K31/4745 , A61K9/52 , A61K47/38
CPC分类号： A61K9/4866 , A61K9/4816 , A61K31/4745 , Y10S514/962
摘要： An oral pharmaceutical formulation which comprises, in a hydroxypropylmethylcellulose capsule, a camptothecin analogue dispersed or solubilised in a semi-solid matrix. These formulations are useful for the treatment of neoplastic diseases.
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7.发明公开2-AMINO-THIAZOLE DERIVATIVES, PROCESS FOR THEIR PREPARATION, AND THEIR USE AS ANTITUMOR AGENTS 有权2 AMINOTHIAZOLEDERIVATE，生产方式及其作为抗肿瘤药
公开(公告)号：EP1124810A1
公开(公告)日：2001-08-22
申请号：EP99955931.3
申请日：1999-10-27
发明人： PEVARELLO, Paolo , AMICI, Raffaella , TRAQUANDI, Gabriella , VILLA, Manuela , VULPETTI, Anna , ISACCHI, Antonella
IPC分类号： C07D277/46 , C07D417/12 , A61K31/426 , A61K31/427 , A61P35/00
CPC分类号： C07D417/12 , A61K31/426 , A61K31/427 , C07D277/46
摘要： Compounds which are 2-amino-1,3-thiazole derivatives of formula (I) wherein R is a halogen atom, a nitro group, an optionally substituted amino group or it is a group, optionally further substituted, selected from i) straight or branched C1-C8 alkyl, C2-C6 alkenyl or C2-C6 alkynyl; ii) C3-C6 cycloalkyl; iii) aryl or arylalkyl with from 1 to 8 carbon atoms within the straight or branched alkyl chain; R1 is an optionally substituted group selected from: i) straight or branched C1-C8 alkyl or C2-C6 alkenyl; ii) 3 to 6 membered carbocycle or 5 to 7 membered heterocycle ring; iii) aryl or arylcarbonyl; iv) arylalkyl with from 1 to 8 carbon atoms within the straight or branched alkyl chain; v) arylalkenyl with from 2 to 6 carbon atoms within the straight or branched alkenyl chain; vi) an optionally protected amino acid residue; or a pharmaceutically acceptable salt thereof; are useful for treating cell proliferative disorders associated with an altered cell dependent kinase activity.
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8.发明授权
公开(公告)号：EP0858454B1
公开(公告)日：2001-06-20
申请号：EP97923966.2
申请日：1997-05-13
IPC分类号： C07D307/80 , C07D307/81 , C07D307/79
CPC分类号： C07D307/79 , C07D307/80 , C07D307/81 , C40B40/04 , C40B50/14
摘要： A process for preparing libraries of benzofuran derivatives of formula (I) by solid phase synthesis in the presence of organometallic catalysts. The resulting compound libraries have a very high purity degree, which allows biological testing on the crude products with a high confidence degree, without any cross contaminations.
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9.发明公开SULFURATED DISTAMYCIN DERIVATIVES, PROCESS FOR PREPARING THEM, AND THEIR USE AS ANTITUMOR AGENTS 有权含硫醚偏端霉素衍生物，用于生产及其作为抗肿瘤药
公开(公告)号：EP1100777A1
公开(公告)日：2001-05-23
申请号：EP99936609.9
申请日：1999-07-21
IPC分类号： C07D207/34 , A61K31/40
CPC分类号： C07D207/34
摘要： Compounds which are sulfurated distamycin derivatives of formula (I) wherein n is 2, 3 or 4; A is a bond, a C1-C4 alkylene or C2-C4 alkenylene group; R1 and R2, which are the same or different, are selected from hydrogen, C1-C4 alkyl optionally substituted by one or more fluorine atoms, and C1-C4 alkoxy; X is a halogen atom; B is selected from formulas (a), (b), (c), (d), (e), (f), (g), (h), (i), (j) and (k); wherein R3, R4, R5, R6, R7, R8, R9 and R10, which are the same or different, are selected from hydrogen or C1-C4 alkyl; R11 is hydrogen, C1-C4 alkyl or hydroxy, and m is 0, 1 or 2; or pharmaceutically acceptable salts thereof; are useful as antitumor agents.
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10.发明授权TERPENOIDIC DERIVATIVES (SARCODICTYINS) USEFUL AS ANTITUMOR AGENTS 失效TERPENDERIVATE（SARCODICTYINE）ALS ANTIKREBSMITTEL
公开(公告)号：EP0773782B1
公开(公告)日：2001-03-14
申请号：EP96914976.4
申请日：1996-04-23
发明人： BATTISTINI, Carlo , CIOMEI, Marina , PIETRA, Francesco , D'AMBROSIO, Michele , GUERRIERO, Antonio
IPC分类号： A61K31/415
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.
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