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1. 发明申请

WO1991006540A1 1,4-BIS(ALKYLAMINO)-2,3-DIAZA-ANTHRACENE-9,10-DIONES 审中-公开
标题翻译： 1,4-二（烷基氨基）-2,3-二氮杂 - 蒽-9,10-二酮
公开(公告)号：WO1991006540A1
公开(公告)日：1991-05-16
申请号：PCT/EP1990001794
申请日：1990-10-23
申请人： BOEHRINGER BIOCHEMIA ROBIN S.P.A. , GANDOLFI, Carmelo, A. , JOHNSON, Francis , MENTA, Ernesto , SPINELLI, Silvano , TOGNELLA, Sergio
发明人： BOEHRINGER BIOCHEMIA ROBIN S.P.A.
IPC分类号： C07D237/34
CPC分类号： C07D403/06 , C07D237/26
摘要： Compounds of formula (I) are described, wherein R1 and R2, that can be the same or different, are hydrogen or acyl groups; R3 and R4, that can be the same or different, are hydrogen or optionally substituted alkyl groups. The compounds of formula (I) are prepared by oxidation of the compounds of formula (II), wherein the groups R'1, R'2, R'3 and R'4 have the same meanings as R1, R2, R3 and R4 or groups convertible to the latter. The compounds of formula (I) have remarkable antitumor activity.

2. 发明申请

WO1989005815A1 AMINO ANTHRACENEDIONES-BIS PLATINUM COMPLEXES, USEFUL AS ANTITUMORAL AGENTS 审中-公开
标题翻译：用作抗肿瘤药物的氨基二苯胺二钠复合物
公开(公告)号：WO1989005815A1
公开(公告)日：1989-06-29
申请号：PCT/EP1988001110
申请日：1988-12-07
申请人： BOEHRINGER BIOCHEMIA ROBIN S.P.A. , PASINI, Alessandro , ZUNINO, Franco , TOFANETTI, Odoardo , GANDOLFI, Carmelo, A. , TOGNELLA, Sergio , SPINELLI, Silvano
发明人： BOEHRINGER BIOCHEMIA ROBIN S.P.A.
IPC分类号： C07F15/00
CPC分类号： C07H23/00 , C07F15/0093
摘要： Bis-platinum complexes of formula (I), wherein A is a disubstituted 1,4-anthracenedione; X, X' are ligands selected from the group consisting of Cl, Br, OH, CH3SOCH3.OH or CH3SOCH3.Hal or, taken together, form the anion of a dicarboxylic acid; n is zero, 0.5 or an integer from 1 to 5; Solv is a solvent of crystallization; Ra is hydrogen, alkyl optionally substituted by hydroxy groups and/or interrupted by oxygen atoms; Rb is alkyl optionally substituted by hydroxy, alkoxy, polyalkoxy or sulphonic groups or a residue of an amino-sugar. Compounds (I) are useful as anti-tumor agents.

3. 发明申请

WO1988000187A1 2-(AMINOALKYLTHIO)METHYL-1,4-DIHYDROPYRIDINE, A METHOD FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 审中-公开
标题翻译： 2-（氨基甲酰基）甲基-1,4-二氢吡啶，其制备方法和含有它们的药物组合物
公开(公告)号：WO1988000187A1
公开(公告)日：1988-01-14
申请号：PCT/EP1987000335
申请日：1987-06-25
申请人： BOEHRINGER BIOCHEMIA ROBIN S.P.A. , GANDOLFI, Carmelo, A. , FRIGERIO, Marco , SPINELLI, Silvano , TOFANETTI, Odoardo , TOGNELLA, Sergio
发明人： BOEHRINGER BIOCHEMIA ROBIN S.P.A.
IPC分类号： C07D211/90
CPC分类号： C07D231/12 , C07D211/90 , C07D233/56 , C07D249/08 , C07D401/04 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D413/12 , C07D417/12
摘要： Compounds of formula (I), wherein P and P1 groups represent hydrogen, alkyl, heteroalkyl, aryl or aralkyl groups, optionally substituted or forming a ring, n is an integer between 0 and 2, m is an integer from 1 to 3, R1 and R3, that may be the same or different, represent alcoxycarbonyl groups, CN, NO2 or acyl groups, whereas R2 is an aryl group or a heteroaryl group that may be optionally substituted, are useful as active principles of pharmaceutical compositions.
摘要翻译：式（I）化合物，其中P和P1基团表示氢，烷基，杂烷基，芳基或芳烷基，任选取代或形成环，n是0和2之间的整数，m是1至3的整数，R 1 和R3可以相同或不同，表示烷氧基羰基，CN，NO2或酰基，而R2是可以任选取代的芳基或杂芳基，可用作药物组合物的活性成分。

4. 发明申请

WO1989008648A1 'beta'-CARBONYL-CARBOXYAMIDES OF 1,3-THIAZOLIDINES 审中-公开
标题翻译：（BETA） - 1,3-噻唑啉的羧基 - 羧酰胺
公开(公告)号：WO1989008648A1
公开(公告)日：1989-09-21
申请号：PCT/EP1989000205
申请日：1989-03-02
申请人： BOEHRINGER BIOCHEMIA ROBIN S.P.A. , GANDOLFI, Carmelo, A. , DI DOMENICO, Roberto , SPINELLI, Silvano , GALLICO, Licia , LUMACHI, Bruno , TOGNELLA, Sergio
发明人： BOEHRINGER BIOCHEMIA ROBIN S.P.A.
IPC分类号： C07D277/04
CPC分类号： C07D417/12 , C07D277/04
摘要： Compounds of formula (I) wherein R is hydrogen, C1-C4-alkyl, allyl or propargyl; X is O, CH2 or S; R1 is a linear or cyclic alkyl, hydroxy, alkoxy, amino group, are useful as antitussive agents.

5. 发明申请

WO1991005791A1 GEM-DIPHOSPHONIC ACIDS, A PROCESS FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 审中-公开
标题翻译： GEM-二磷酸，其制备方法和含有它们的药物组合物
公开(公告)号：WO1991005791A1
公开(公告)日：1991-05-02
申请号：PCT/EP1990001710
申请日：1990-10-11
申请人： BOEHRINGER BIOCHEMIA ROBIN S.P.A. , TOGNELLA, Sergio , LIVI, Valeria , MENTA, Ernesto , SPINELLI, Silvano
发明人： BOEHRINGER BIOCHEMIA ROBIN S.P.A.
IPC分类号： C07F09/38
CPC分类号： C07F9/405 , C07F9/3873 , C07F9/564
摘要： Diphosphonic acids of formula (I), wherein R1 and R2 are hydrogen or C1-C4 alkyl; (A) is hydrogen, halogen, hydroxy or C1-C12 alkyl; (B) is a bond, a C1-C8 alkylene chain, a cycloalkylalkylene chain, an alkylene chain substituted by cyclohexyl or cyclopentyl groups, or an aralkyl chain, an alkyl chain containing an heteroatom (O, S or N-CH3) or an ureido residue -(CH2)n1-NHCONH -(CH2)n- with n ranging from 1 to 5, R3 is hydrogen, C1-C9 alkyl, C3-C6 cycloalkyl, benzyl, phenyl or p-methoxybenzyl; (C) is C1-C5 alkyl, phenyl or an aralkyl chain; R4 is hydrogen, C1-C4 alkyl or an amino group optionally substituted by alkyl, phenyl, benzyl, p-methoxybenzyl, acyl, amminoacidic or peptide groups; R5 and R6 are 2-haloethyl or together form a 1-aziridinyl residue, are useful as antitumor agent.
摘要翻译：式（I）的二膦酸，其中R 1和R 2是氢或C 1 -C 4烷基; （A）是氢，卤素，羟基或C 1 -C 12烷基; （B）是键，C1-C8亚烷基链，环烷基亚烷基链，被环己基或环戊基取代的亚烷基链或芳烷基链，含有杂原子（O，S或N-CH 3）的烷基链或脲基残基 - （CH 2）n1-NHCONH - （CH 2）n - ，n为1至5，R 3为氢，C 1 -C 9烷基，C 3 -C 6环烷基，苄基，苯基或对甲氧基苄基; （C）是C 1 -C 5烷基，苯基或芳烷基链; R4是氢，C1-C4烷基或任选被烷基，苯基，苄基，对甲氧基苄基，酰基，氨基酸或肽基团取代的氨基; R5和R6是2-卤代乙基或一起形成1-氮丙啶基残基，可用作抗肿瘤剂。

6. 发明申请

WO1989009218A1 PLATINUM(II) COMPLEXES, THEIR PREPARATION AND USE AS ANTI-TUMOUR AGENTS 审中-公开
标题翻译：铂（II）复合物，其制备和用作抗肿瘤剂
公开(公告)号：WO1989009218A1
公开(公告)日：1989-10-05
申请号：PCT/EP1989000330
申请日：1989-03-25
申请人： BOEHRINGER BIOCHEMIA ROBIN S.P.A. , SPINELLI, Silvano , PASINI, Alessandro , MENTA, Ernesto , ZUNINO, Franco , TOGNELLA, Sergio
发明人： BOEHRINGER BIOCHEMIA ROBIN S.P.A.
IPC分类号： C07F15/00
CPC分类号： C07F15/0093
摘要： Compounds of formula (I), wherein R1 and R2, that can be the same or different, are hydrogen, alkyl, aryl, aralkyl groups or, if taken together, cycloalkyl groups; A is a carbon atom, a residue of 2,3-dioxybutandioic-2,4-dioxyphthalic acid or disubstituted malonic acid derivatives; n1 and n2 are selected in such a manner that the result of their addition is from 2 to 40; T1 and T2 that can be the same or different, are hydrogen, alkyl, benzyl, phenyl, acyl or cycloalkyl or a residue of formulae alpha and beta. Compounds of formula (I) are useful as anti-tumour agents in human therapy.

7. 发明申请

WO1989001932A1 2-ALKYL AND 2-ALKENYL SUBSTITUTED 1,4-DIHYDROPYRIDINES, A METHOD FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 审中-公开
标题翻译： 2-烷基和2-烷基取代的1,4-二氢吡啶类，其制备方法和含有它们的药物组合物
公开(公告)号：WO1989001932A1
公开(公告)日：1989-03-09
申请号：PCT/EP1988000746
申请日：1988-08-21
申请人： BOEHRINGER BIOCHEMIA ROBIN S.P.A. , FRIGERIO, Marco , ZALIANI, Andrea , GANDOLFI, Carmelo, A. , GERMINI, Mauro , TOFANETTI, Odoardo , TOGNELLA, Sergio
发明人： BOEHRINGER BIOCHEMIA ROBIN S.P.A.
IPC分类号： C07D211/90
CPC分类号： C07D401/06 , C07D211/90 , C07D409/06
摘要： 2-(substituted)-propyl-1,4-dihydropyridines, a method for their preparation and pharmaceutical compositions containing them are described.

8. 发明申请

WO1988005043A1 NEW ARALKYL-1,4-DIHYDROPYRIDINES, A METHOD FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 审中-公开
标题翻译：新的ARALKYL-1,4-二氢吡啶类，其制备方法和含有它们的药物组合物
公开(公告)号：WO1988005043A1
公开(公告)日：1988-07-14
申请号：PCT/EP1987000815
申请日：1987-12-21
申请人： BOEHRINGER BIOCHEMIA ROBIN S.P.A. , FRIGERIO, Marco , ZALIANI, Andrea , GANDOLFI, Carmelo, A. , GERMINI, Mauro , TOFANETTI, Odoardo , TOGNELLA, Sergio
发明人： BOEHRINGER BIOCHEMIA ROBIN S.P.A.
IPC分类号： C07D211/90
CPC分类号： C07D401/06 , C07D211/90 , C07D409/06
摘要： 1,4-Dihydropyridines of formula (I), wherein: X is a -CO2R1, cyano, nitro, -COCH3 group; R and R1, that can be the same or different, are a primary, secondary or tertiary, saturated or unsaturated, linear or branched C1-C6 alkyl group that can be substituted or not by one or more hydroxy, C1-C7-monoalkylamino, di-C1-C7-alkylamino, benzylamino, C1-C6-alkoxy, phenoxy groups optionally substituted by one or more C1-C6 alkyl, C1-C6 alkoxy, halo-C1-C6 alkyl, halo-C1-C6-alkoxy, halogen, nitro, cyano, C1-C6 alkoxycarbonyl, C1-C6 alkylthio, NHCOR5, SO2R6, C1-C4-alkylamino, di(C1-C4)alkylamino, hydroxy; R2 is hydrogen; R3 is hydrogen or a hydroxy, -OCOR5, OSO2R6, azide, amino, -NHPO(OR7)2, -NHCOR5 group, a C1-C4-alkoxy group or a fluorine, chlorine, bromine or iodine atom, a SH group, a SCOR6 or a C1-C6-alkylthio, phenylthio or benzylthio group; R4 is an optionally substituted aromatic or an optionally substituted 5- or 6-membered heteroaromatic group, containing one or more heteroatoms selected in the group of N,S,O, wherein the substituent is selected from one or more hydroxy, C1-C7-monoalkylamino, di-C1-C7-alkylamino, benzylamino, C1-C6-alkoxy, phenoxy groups optionally substituted by one or more C1-C6 alkyl, C1-C6 alkoxy, halo-C1-C6 alkyl, halo-C1-C6-alkoxy, halogen, nitro, cyano, C1-C6 alkoxycarbonyl, C1-C6 alkylthio, NHCOR5, SO2R6, C1-C4-alkylamino, di(C1-C4)alkylamino, hydroxy; Y is one or more substituents, that can be the same or different, selected in the group of C1-C4-alkoxy, halogen, nitro, cyano, C1-C6-alkoxycarbonyl, C1-C6-alkylthio, halo-C1-C6-alkyl, halo-C1-C6-alkoxy, NHCOR5 or NHSO2R6; R5 is hydrogen or a C1-C4-alkyl, thrihalomethyl, C1-C4-alkoxy or phenyl group, optionally substituted by one or more nitro, halogen, C1-C4-alkyl, C1-C4-alkoxy, amino groups; R6 is hydrogen or a C1-C4-alkyl, trihalomethyl, phenyl, or p-methylphenyl group; R7 is a C1-C4-alkyl group or a phenyl group, are useful as antihypertensive, cytoprotecting or anti-ulcer agents.

9. 发明申请

WO1990009376A1 A PROCESS FOR PREPARATION OF ENANTIOMERICALLY PURE POLYSUBSTITUTED 1,4-DIHYDROPYRIDINES 审中-公开
标题翻译：一种制备全自由基多取代1,4-二羟基吡啶的方法
公开(公告)号：WO1990009376A1
公开(公告)日：1990-08-23
申请号：PCT/EP1990000243
申请日：1990-02-15
申请人： BOEHRINGER BIOCHEMIA ROBIN S.P.A. , GANDOLFI, Carmelo, A. , FRIGERIO, Marco , RIVA, Carlo , ZALIANI, Andrea , LONG, Giorgio , DI DOMENICO, Roberto
发明人： BOEHRINGER BIOCHEMIA ROBIN S.P.A.
IPC分类号： C07D211/90
CPC分类号： C07D401/12 , C07D211/90 , C07D405/12
摘要： A process for the optical resolution of racemic 1,4-dihydropyridines, containing isothioureido groups. Salification of racemic isothioureas with optically active acids produces diasteroisomeric mixtures of isothiouronium salts, that, using conventional techniques, are separated in the individual components to give optically pure isothioureides of 1,4-dihydropyridines and salts thereof with conventional acids. Said optically pure 1,4-dihydropyridines can then be subjected to desulphuration and to different transformations to give other enantiomerically pure and therapeutically useful 1,4-dihydropyridines.

10. 发明申请

WO1990013553A1 RUTHENIUM(III) COMPLEXES AS ANTINEOPLASTIC AGENTS 审中-公开
标题翻译：钌（III）复合物作为抗肿瘤药物
公开(公告)号：WO1990013553A1
公开(公告)日：1990-11-15
申请号：PCT/EP1990000699
申请日：1990-05-02
申请人： BOEHRINGER BIOCHEMIA ROBIN S.P.A. , ALESSIO, Enzo , MESTRONI, Giovanni , PACOR, Sabrina , SAVA, Gianni , SPINELLI, Silvano
发明人： BOEHRINGER BIOCHEMIA ROBIN S.P.A.
IPC分类号： C07F15/00
CPC分类号： C07F15/0053
摘要： Complexes of formula (I), wherein: R1 and R2 are alkyl, alkylaryl, aryl or hetaryl groups, A is chloride, or a group of formula (a), (R1 and R2 as above defined); B is a nitrogen ligand selected from ammonia, primary, secondary or tertiary amines or nitrogen containing heterocycles, are useful as antineoplastic agents.
摘要翻译：式（I）的络合物，其中：R 1和R 2是烷基，烷基芳基，芳基或杂芳基，A是氯化物或式（a），（R 1和R 2如上所定义） B是选自氨，伯，仲或叔胺或含氮杂环的氮配体，可用作抗肿瘤剂。

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