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1. 发明申请

WO1992012147A1 PROCESS FOR THE PREPARATION OF SUBSTITUTED BENZOFURAN DERIVATIVES 审中-公开
标题翻译：制备替代苯唑嘌呤衍生物的方法
公开(公告)号：WO1992012147A1
公开(公告)日：1992-07-23
申请号：PCT/EP1991002512
申请日：1991-12-27
申请人： FARMITALIA CARLO ERBA S.R.L. , BEDESCHI, Angelo , CABRI, Walter , CANDIANI, Ilaria , DE BERNARDINIS, Silvia , MARCHI, Marcello
发明人： FARMITALIA CARLO ERBA S.R.L.
IPC分类号： C07D405/12
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 formula (I), wherein one of R1 and R2 is hydrogen or halogen and the other is, independently, an amino group or a C2-C4 alkanoyl amino group; R3 is hydrogen; a linear or branched C1-C4 alkyl, C1-C4 alkoxy or C2-C4 alkoxycarbonyl group; halogen; or phenyl unsubstituted or substituted by a C1-C4 alkyl group; A is a group -(CH2)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), in which L is a leaving group and R4 is hydrogen or a carboxy protecting group, with a compound of the formula (III): R'3-C=C-R'3 to obtain a compound of formula (IV) which is then cyclized to obtain a compound of formula (V) which is reacted with a compound of the formula (VI): H2N-A.

2. 发明申请

WO1990009974A1 PROCESS FOR PREPARING ANTHRACYCLINONES 审中-公开
标题翻译：制备蒽醌的方法
公开(公告)号：WO1990009974A1
公开(公告)日：1990-09-07
申请号：PCT/EP1990000334
申请日：1990-02-28
申请人： FARMITALIA CARLO ERBA S.R.L. , CABRI, Walter , CANDIANI, Ilaria , DE BERNARDINIS, Silvia , FRANCALANCI, Franco
发明人： FARMITALIA CARLO ERBA S.R.L.
IPC分类号： C07C50/38
CPC分类号： C07C46/00 , Y02P20/55 , C07C50/38
摘要： 4-Substituted anthracyclinones of general formula (I), wherein R represents a hydrogen atom or a COOR1 group in which R1 may be a hydrogen atom or an optionally substituted C1-C10 alkyl group, which are intermediates in the preparation of antitumor anthracycline glycosides, are prepared by: (i) (a) reacting a 4-demethyl-4-sulfonyl-7-deoxy-13-dioxolanyl daunomycinone of formula (V), wherein R' represents an alkyl group having from 1 to 10 carbon atoms optionally substituted by one or more halogen atoms or an aryl group optionally substituted by halogen, alkyl, alkoxy or nitro, in a reducing environment with a catalytic amount of a compound of formula (VIII): MLnL'm, wherein M represents a transition metal atom, L and L', which may be the same or different, each represents an anion or a neutral molecule and n and m may vary from 0 to 4, such as to obtain a compound of formula (VII), wherein R represents hydrogen; or (b) carbonylating a 4-demethyl-4-sulfonyl-7-deoxy-13-dioxolanyl daunomycinone of formula (V) as defined above, with carbon monoxide in the presence of a nucleophile R1OH, wherein R1 is as defined above, an organic or inorganic base and as catalyst a compound of formula (VIII) as defined above, such as to obtain a compound of formula (VII) as shown above wherein R represents a COOR1 group; and (ii) introducing an α-hydroxy group at the 7-position and removing the 13-oxo protecting group by acid hydrolysis from the resultant compound of formula (VII).

3. 发明申请

WO1991013064A1 PROCESS FOR PREPARING URACIL DERIVATIVES 审中-公开
标题翻译：制备尿嘧啶衍生物的方法
公开(公告)号：WO1991013064A1
公开(公告)日：1991-09-05
申请号：PCT/EP1991000324
申请日：1991-02-21
申请人： FARMITALIA CARLO ERBA S.R.L. , BEDESCHI, Angelo , CABRI, Walter , CANDIANI, Ilaria , MARTINENGO, Tiziano
发明人： FARMITALIA CARLO ERBA S.R.L.
IPC分类号： C07D239/54
CPC分类号： C07D239/54 , C07D239/60
摘要： The present invention relates to a novel process for preparing uracil derivatives useful as intermediates in the synthesis of uridines having antiviral or antitumor activity or useful as coadjuvants in antiviral therapy, characterized by converting a compound of formula (II) into its mesylate derivative of formula (III) which is the reduced to give the desired compound of formula (I), in which R1 is H, halogen, alkyl, aryl or aralkyl.
摘要翻译：本发明涉及一种制备尿嘧啶衍生物的新方法，其用作合成具有抗病毒或抗肿瘤活性的尿苷的中间体，或用作抗病毒治疗中的辅佐剂，其特征在于将式（II）的化合物转化为式（II）的甲磺酸酯衍生物 III），其是还原得到所需的式（I）化合物，其中R 1是H，卤素，烷基，芳基或芳烷基。

4. 发明申请

WO1991014691A1 PROCESS FOR PREPARING PENEM ESTERS 审中-公开
标题翻译：制备梨子的方法
公开(公告)号：WO1991014691A1
公开(公告)日：1991-10-03
申请号：PCT/EP1991000522
申请日：1991-03-18
申请人： FARMITALIA CARLO ERBA S.R.L. , BEDESCHI, Angelo , CABRI, Walter , MARCHI, Marcello , PERRONE, Ettore
发明人： FARMITALIA CARLO ERBA S.R.L.
IPC分类号： C07D499/88
CPC分类号： C07D205/09 , C07C67/307 , C07C67/313 , C07D499/88 , Y02P20/55
摘要： There is provided a process for preparing penem esters having antibacterial activity, starting from a compound of formula (II) wherein R1 is H or a hydroxy protecting group and Z is a C1-C10 alkyl or an aryl group which is reacted with a compound of formula (III) to give an azeotidinon which is condensed with a compound of the formula (V): XOC - COO - CH2OCOCH3, and cyclized to obtain the desired penem esters. The present invention also comprises a process for preparing a compound of formula (V) oxydizing a compound of the formula: HO-CH2-COO-CH2OCOCH3.
摘要翻译：提供了制备具有抗菌活性的苦参酯的方法，由式（II）化合物开始，其中R1是H或羟基保护基，Z是C1-C10烷基或芳基，其与式（III）化合物，得到与式（Ⅴ）化合物缩合的α-甜菜碱：XOC-COO-CH 2 OCOCH 3，并环化得到所需的pen em酯。本发明还包括制备式（Ⅴ）化合物氧化式HO-CH2-COO-CH2OCOCH3化合物的方法。

5. 发明申请

WO1990001490A1 4-SUBSTITUTED ANTHRACYCLINONES AND ANTHRACYCLINE GLYCOSIDES AND THEIR PREPARATION 审中-公开
标题翻译： 4-取代的安非他酮和安非他酮糖苷及其制备
公开(公告)号：WO1990001490A1
公开(公告)日：1990-02-22
申请号：PCT/EP1989000869
申请日：1989-07-24
申请人： FARMITALIA CARLO ERBA S.R.L. , CABRI, Walter , DE BERNARDINIS, Silvia , FRANCALANCI, Frano , PENCO, Sergio
发明人： FARMITALIA CARLO ERBA S.R.L.
IPC分类号： C07H15/252
CPC分类号： C07H15/252
摘要： 4-Substituted anthracyclinones of formula (I), wherein R represents a hydrogen atom or a straight or branched alkyl, alkenyl or alkynyl group having from 1 to 10 carbon atoms, are intermediates in the preparation of antitumor anthracycline glycosides of formula (IX), wherein R is as defined above and R1 is a hydrogen atom or a hydroxy group, and pharmaceutically acceptable salts thereof.

6. 发明申请

WO1990004601A1 NEW 4-SUBSTITUTED ANTHRACYCLINONES AND ANTHRACYCLINE GLYCOSIDES AND THE PROCESS FOR PREPARING THEM 审中-公开
标题翻译：新的4-取代的蒽醌和蒽醌糖苷及其制备方法
公开(公告)号：WO1990004601A1
公开(公告)日：1990-05-03
申请号：PCT/EP1989001266
申请日：1989-10-24
申请人： FARMITALIA CARLO ERBA S.R.L. , CABRI, Walter , DE BERNARDINIS, Silvia , FRANCALANCI, Franco , PENCO, Sergio
发明人： FARMITALIA CARLO ERBA S.R.L.
IPC分类号： C07H15/252
CPC分类号： C07H15/252
摘要： 4-substituted anthracyclinones of formula (I), wherein R represents a straight or branched alkyl, alkenyl or alkynyl group of up to 16 carbon atoms optionally substituted by (a) an aryl group which is unsubstituted or substituted by an inert group such as an alkyl, alkoxy or nitro group; (b) an alkoxy group; (c) a trialkylsilyl group, (d) an ester group or (e) an amido group, are intermediates in the preparation of antitumor anthracycline glycosides of formula (IX), wherein R is as defined above and R1 is a hydrogen atom or a hydroxy group, and pharmaceutically acceptable salts thereof.

7. 发明申请

WO1994026311A1 ANTHRACYCLINE CONJUGATES, THEIR PREPARATION AND THEIR USE AS ANTITUMOR AGENTS 审中-公开
标题翻译：蒽醌类化合物，其制备及其作为抗菌剂的用途
公开(公告)号：WO1994026311A1
公开(公告)日：1994-11-24
申请号：PCT/EP1994001100
申请日：1994-04-08
申请人： FARMITALIA CARLO ERBA S.R.L. , ANGELUCCI, Francesco , GRANDI, Maria , SUARATO, Antonino
发明人： FARMITALIA CARLO ERBA S.R.L.
IPC分类号： A61K47/48
CPC分类号： A61K47/58 , Y02P20/582
摘要： The present invention provides polymer-bound anthracyclines of formula (A) which consists essentially of three units represented by formulae (1), (2) and (3), wherein: Gly represents glycine; n is 0 or 1; x is from 70 to 98 mol %, y is from 1 to 29 mol %, z is from 1 to 29 mol %, R1 is a C1-C6 alkyl group substituted by one or more hydroxy groups; Y is an amino acid residue or a peptide spacer; [NH-D] is the residue of an anthracycline aminoglycoside [NH2-D]; and Z is a hydroxy group or a residue of formula -NHR1 wherein R1 is as defined above. Methods for their preparation and pharmaceutical compositions containing them are also provided.
摘要翻译：本发明提供了式（A）的聚合物结合的蒽环类，其基本上由式（1），（2）和（3）表示的三个单元组成，其中：Gly表示甘氨酸; n为0或1; x为70〜98摩尔％，y为1〜29摩尔％，z为1〜29摩尔％，R1为被一个或多个羟基取代的C1-C6烷基。 Y是氨基酸残基或肽间隔基; [NH-D]是蒽环类氨基糖苷[NH2-D]的残基; 并且Z是羟基或式-NHR1的残基，其中R 1如上所定义。还提供了它们的制备方法和含有它们的药物组合物。

8. 发明申请

WO1994011347A1 PHENYL-IMIDAZOLIDINONE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS 5HT3 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：苯并咪唑啉酮衍生物，其制备方法及其作为5HT3受体拮抗剂的用途
公开(公告)号：WO1994011347A1
公开(公告)日：1994-05-26
申请号：PCT/EP1993002924
申请日：1993-10-22
申请人： FARMITALIA CARLO ERBA S.R.L.
发明人： FARMITALIA CARLO ERBA S.R.L. , VARASI, Mario , HEIDEMPERGHER, Franco , CACCIA, Carla , ARRIGONI, Claudio
IPC分类号： C07D233/61
CPC分类号： C07D233/64 , Y02P20/55
摘要： The invention relates to new derivatives of 1-imidazolylalkyl-3-phenyl-imidazolidin-2-ones of general formula (I), wherein n is 1, 2 or 3; each of R, R1 and R2, which may be the same or different, is hydrogen, halogen, hydroxy, cyano, C1-C6 alkyl, CF3, C1-C6 alkoxy, C1-C6 alkylthio, formyl, C2-C6 alkanoyl, carboxy, C1-C6 alkoxy-carbonyl, nitro, -N(R4 R5) in which each of R4 and R5 independently is hydrogen, C1-C6 alkyl, formyl or C2-C6 alkanoyl; or a (R6 R7)N-SO2 group, in which each of R6 and R7 independently is hydrogen or C1-C6 alkyl; R3 is an imidazolyl group of formula (a) or (b), wherein each of R8 and R10, which may be the same or different, is hydrogen or C1-C6 alkyl, R9 is hydrogen, C1-C6 alkyl or a nitrogen protecting group, or pharmaceutically acceptable salts thereof, which are useful in the treatment of CNS disorders, such as, e.g., anxiety and psychosis, and in the treatment of gut motility disorders, and/or emesis.
摘要翻译：本发明涉及通式（I）的1-咪唑基烷基-3-苯基 - 咪唑烷-2-酮的新衍生物，其中n为1,2或3; R，R 1和R 2可以相同或不同，为氢，卤素，羟基，氰基，C 1 -C 6烷基，CF 3，C 1 -C 6烷氧基，C 1 -C 6烷硫基，甲酰基，C 2 -C 6烷酰基，羧基，其中R 4和R 5各自独立地为氢，C 1 -C 6烷基，甲酰基或C 2 -C 6烷酰基的C 1 -C 6烷氧羰基，硝基，-N（R 4 R 5）或（R6R7）N-SO2基团，其中R6和R7各自独立地为氢或C1-C6烷基; R 3是式（a）或（b）的咪唑基，其中R 8和R 10各自可以相同或不同，是氢或C 1 -C 6烷基，R 9是氢，C 1 -C 6烷基或氮保护组或其药学上可接受的盐，其可用于治疗CNS疾病，例如焦虑和精神病，以及用于治疗肠蠕动障碍和/或呕吐。

9. 发明申请

WO1994010190A1 6,7'alpha'-DIFLUOROMETHYLENANDROSTA-1,4-DIEN-3-ONE DERIVATIVES AND PROCESS FOR THEIR PREPARATION 审中-公开
标题翻译： 6,7α-二氟甲基磺酰胺-1,4-二苯基-3-酮衍生物及其制备方法
公开(公告)号：WO1994010190A1
公开(公告)日：1994-05-11
申请号：PCT/EP1993002864
申请日：1993-10-18
申请人： FARMITALIA CARLO ERBA S.R.L.
发明人： FARMITALIA CARLO ERBA S.R.L. , BUZZETI, Franco , LONGO, Antonio , DI SALLE, Enrico
IPC分类号： C07J53/00
CPC分类号： C07J53/007
摘要： This invention refers to the use of compounds of formula (I), wherein R is hydrogen or C1-C4 alkyl; and A is a (a), (b) or (c) group, in which R' is an acyl group; in the manufacture of a medicament for use as an aromatase inhibitor; and compounds of formula (I) excluding 17 alpha -acetoxy-6,7 alpha -difluoromethylenandrosta-1,4-dien-3-one.
摘要翻译：本发明涉及式（I）化合物的用途，其中R是氢或C 1 -C 4烷基; 和A是（a），（b）或（c）基团，其中R'是酰基; 在制备用作芳香酶抑制剂的药物中; 和不包括17α-乙酰氧基-6,7α-二氟甲基雄甾-1,4-二烯-3-酮的式（I）化合物。

10. 发明申请

WO1994003476A1 17'beta'-SUBSTITUTED 4-AZA-5'alpha'-ANDROSTAN-3-ONE DERIVATIVES 审中-公开
标题翻译： 17β-取代的4-AZA-5α-二脱氧-3-α衍生物
公开(公告)号：WO1994003476A1
公开(公告)日：1994-02-17
申请号：PCT/EP1993002038
申请日：1993-07-29
申请人： FARMITALIA CARLO ERBA S.R.L.
发明人： FARMITALIA CARLO ERBA S.R.L. , PANZERI, Achille , NESI, Marcella , DI SALLE, Enrico
IPC分类号： C07J73/00
CPC分类号： C07J73/005
摘要： A compound of formula (I), wherein R is a hydrogen atom or a C1-C4 alkyl group; A is a single bond or a straight or branched C1-C6 alkylene chain; R1 is a hydrogen atom or a C1-C6 alkyl group; R2 is a C1-C6 alkyl group, a C5-C7 cycloalkyl or a C6-C10 cycloalkylalkyl group, aryl or a C7-C10 arylalkyl group, or a C6-C10 heterocycloalkyl group; R3 is hydrogen, a C1-C4 alkyl group or an aryl or a C7-C10 arylalkyl group; Z is a C1-C6 alkyl group, an -OR5 group wherein R5 is a C1-C6 alkyl group, a (a) group wherein each of R6 and R7 is hydrogen, C1-C6 alkyl, C5-C7 cycloalkyl, phenyl or R6 and R7 taken together with the nitrogen to which they are linked form a pentatomic or hexatomic saturated heteromonocyclic ring; and the symbol .Ÿ .Ÿ .Ÿ .Ÿ represents a single or a double bond, is a testosterone 5(alpha)-reductase inhibitor and is therapeutically useful in benign prostatic hyperplasia, prostatic and breast cancers, seborrhoea, female hirsutism and male pattern baldness.
摘要翻译：式（I）的化合物，其中R是氢原子或C1-C4烷基; A是单键或直链或支链C1-C6亚烷基链; R1是氢原子或C1-C6烷基; R2是C1-C6烷基，C5-C7环烷基或C6-C10环烷基烷基，芳基或C7-C10芳基烷基或C6-C10杂环烷基; R3是氢，C1-C4烷基或芳基或C7-C10芳烷基; Z是C1-C6烷基，其中R5是C1-C6烷基的-OR5基团，其中R6和R7各自为氢，C1-C6烷基，C5-C7环烷基，苯基或R6 和R7与它们所连接的氮原子一起形成五原子或六原子饱和杂单环; 和符号.Ÿ.Ÿ。表示单键或双键，是睾酮5（α） - 还原酶抑制剂，可用于良性前列腺增生，前列腺和乳腺癌，皮脂溢，女性多毛症和雄性模式秃顶。

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