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1. 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。

2. 发明申请

WO1994020504A1 2-ACYLOXYCEPHEM DERIVATIVES AS ELASTASE INHIBITORS 审中-公开
标题翻译： 2-ACYLOXYCEPHEM衍生物作为弹性酶抑制剂
公开(公告)号：WO1994020504A1
公开(公告)日：1994-09-15
申请号：PCT/EP1994000529
申请日：1994-02-24
申请人： PHARMACIA/FARMITALIA CARLO ERBA S.R.L. , ALPEGIANI, Marco , BISSOLINO, Pierluigi , PERRONE, Ettore
发明人： PHARMACIA/FARMITALIA CARLO ERBA S.R.L.
IPC分类号： C07D501/00
CPC分类号： C07D501/00
摘要： The present invention provides cephalosporin sulphones of formula (I) and the pharmaceutically and veterinarily acceptable salts thereof, wherein n is one or two; A and B are both or each independently hydrogen or an organic radical; R represents halogen, A, OA, -S(O)mA wherein m is 0-2, -OC(O)A, -OS(O)2A, -NHC(O)A or -NH-Z wherein Z is a mono, di- or tripeptide and A is as defined above; R represents a halogen, A, -S(O)mA, -O-A, -C(O)A, -C(O)OA, -CH2-OA, -CH2S(O)mA, -CH2OC(O)A, -CH2O-Z, -CH2SC(O)A, -CH2-N(A)A', -CH2N (A)(A')A", -CH2NH-C(O)A or -CH2NH-Z wherein A and Z are as defined above. The compounds of formula (I) and their salts are elastase inhibitors.
摘要翻译：本发明提供式（I）的头孢菌素砜及其药学上和兽医学上可接受的盐，其中n为1或2; A和B各自独立地为氢或有机基团; R 1表示卤素，A，OA，-S（O）mA，其中m为0-2，-OC（O）A，-OS（O）2A，-NHC（O）A或-NH-Z，其中 Z是单，二或三肽，A如上所定义; R 2表示卤素，A，-S（O）mA，-OA，-C（O）A，-C（O）OA，-CH 2 OA，-CH 2 S（O））A，-CH 2 O-Z，-CH 2 SC（O）A，-CH 2 -N（A）A'， - CH 2 N +（A）（A'）A“，-CH 2 NH- C（O） CH2NH-Z其中A和Z如上所定义。式（I）化合物及其盐是弹性蛋白酶抑制剂。

3. 发明申请

WO1994019365A1 FLUORINATED 4-AMINOANDROSTADIENONE DERIVATIVES AND PROCESS FOR THEIR PREPARATION 审中-公开
标题翻译：氟化4-氨基二氢萘酮衍生物及其制备方法
公开(公告)号：WO1994019365A1
公开(公告)日：1994-09-01
申请号：PCT/EP1994000282
申请日：1994-02-01
申请人： PHARMACIA/FARMITALIA CARLO ERBA S.R.L.
发明人： PHARMACIA/FARMITALIA CARLO ERBA S.R.L. , BUZZETTI, Franco , LONGO, Antonio , DI SALLE, Enrico
IPC分类号： C07J41/00
CPC分类号： C07J41/0005 , C07J1/0011 , C07J41/0011 , C07J41/0027 , C07J71/001
摘要： The present invention relates to compounds of formula (I) wherein (x) and (y) are single or double bonds; A is (1) or (2); R and R are hydrogen or acyl; R is hydrogen or fluorine; and wherein: when (y) is a single bond, R is hydrogen, fluorine methyl, trifluoromethyl; when (y) is a double bond, R is methylene provided that when one of (x) or (y) is a double bond the other is a single bond and at least one of R1 and R2 is fluorine or trifluoromethyl and the pharmaceutically acceptable salts thereof. The compounds of formula (I) are useful as aromatase inhibitors.
摘要翻译：本发明涉及式（I）的化合物，其中（x）和（y）是单键或双键; A是（1）或（2）; R 3和R 3是氢或酰基; R 1是氢或氟; 并且其中：当（y）为单键时，R 2为氢，氟甲基，三氟甲基; 当（y）是双键时，R 2是亚甲基，条件是当（x）或（y）中的一个是双键时，另一个是单键，并且R 1和R 2中的至少一个是氟或三氟甲基，其药学上可接受的盐。式（I）化合物可用作芳香酶抑制剂。

4. 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。

5. 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。

6. 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。

7. 发明申请

WO1993014105A1 DIFLUOROMETHYLENANDROSTENONE DERIVATIVES AND PROCESS FOR THEIR PREPARATION 审中-公开
标题翻译：二氟代吗啉衍生物及其制备方法
公开(公告)号：WO1993014105A1
公开(公告)日：1993-07-22
申请号：PCT/EP1993000105
申请日：1993-01-18
申请人： FARMITALIA CARLO ERBA S.R.L.
发明人： FARMITALIA CARLO ERBA S.R.L. , BUZZETTI, Franco , LONGO, Antonio , CRUGNOLA, Angelo , DI SALLE, Enrico
IPC分类号： C07J01/00
CPC分类号： C07J1/0014 , C07J1/0011 , C07J1/0022 , C07J1/0025 , C07J71/001
摘要： The invention relates to new 6-difluoromethylenandrostenones having formula (I) wherein the symbol - &cir& _- &cir& _- &cir& _ represents a double or single bond; R is hydrogen or C1-C4 alkyl; and A is a =C=O, =CH OH or =CH OR1 group, in which R1 is an acyl group, which are useful as steroidal aromatase inhibitors.
摘要翻译：本发明涉及具有式（I）的新的6-二氟亚甲基雄酮，其中符号 - ＆C 1 -C 2 - 表示双键或单键; R是氢或C 1 -C 4烷基; 并且A是A = C = O，= CH OH或= CH OR1基团，其中R1是酰基，其可用作甾体芳香酶抑制剂。

8. 发明申请

WO1992002255A1 NEW LINKER FOR BIOACTIVE AGENTS 审中-公开
标题翻译：生物活性剂的新连接器
公开(公告)号：WO1992002255A1
公开(公告)日：1992-02-20
申请号：PCT/EP1991001449
申请日：1991-08-01
申请人： FARMITALIA CARLO ERBA S.R.L. , ANGELUCCI, Francesco , BERSANI, Laura , CARUSO, Michele , RIPAMONTI, Marina , RUGGIERI, Daniela , SUARATO, Antonino
发明人： FARMITALIA CARLO ERBA S.R.L.
IPC分类号： A61K47/48
CPC分类号： C07H15/252 , A61K47/58 , A61K47/64 , A61K47/6809 , A61K47/6883 , A61K47/6889 , C07H19/24
摘要： Conjugates of general formula (1): [A-O-W-Z]a-T wherein the moiety A-O- is the residue of drug of formula A-O-H in which -O-H is a primary or secondary hydroxyl group; a is an integer of from 1 to 30; W is a group of general formula (2) wherein b is an integer of from 1 to 4, B represents a C1-C3 alkylene group and R1 and R2 each independently represent hydrogen, halogen, alkyl, phenyl or substituted phenyl; Z is a spacer group and T is a carrier moiety.
摘要翻译：通式（1）的结合物：[A-O-W-Z] a-T其中部分A-O-是式A-O-H的药物的残基，其中-O-H是伯或仲羟基; a为1〜30的整数; W是通式（2）的基团，其中b是1至4的整数，B表示C1-C3亚烷基，R1和R2各自独立地表示氢，卤素，烷基，苯基或取代的苯基; Z是间隔基，T是载体部分。

9. 发明申请

WO1991012261A1 17'beta'-SUBSTITUTED-4-AZA-5'alpha'-ANDROSTAN-3-ONE DERIVATIVES AND PROCESS FOR THEIR PREPARATION 审中-公开
标题翻译： 17β-巯基-4-AZA-5α-二巯基-3-酮衍生物及其制备方法
公开(公告)号：WO1991012261A1
公开(公告)日：1991-08-22
申请号：PCT/EP1991000228
申请日：1991-02-06
申请人： FARMITALIA CARLO ERBA S.R.L.
发明人： FARMITALIA CARLO ERBA S.R.L. , PANZERI, Achille , DI SALLE, Enrico , NESI, Marcella
IPC分类号： C07J73/00
CPC分类号： C07J73/005
摘要： The present invention concerns steroidic 5α-reductase inhibitors having formula (I) wherein R1 is hydrogen, a C1-C6 alkyl group, an aryl-C1-C6alkyl group, or an aroyl group; Y is oxygen or sulphur; W is a group (2) wherein each of R2 and R3 is independently selected from the group consisting of hydrogen, C1-C6 alkyl, C5-C6 cycloalkyl, C6-C9 cycloalkylalkyl and aryl, wherein each of the groups alkyl, cycloalkyl, cycloalkylalkyl and aryl may be unsubstituted or substituted by a substituent -OR4 wherein R4 is hydrogen or C1-C4 alkyl; A is hydrogen, C1-C6 alkyl, C5-C6 cycloalkyl or C6-C9 cycloalkylalkyl wherein each of the groups alkyl, cycloalkyl and cycloalkylalkyl, may be unsubstituted or substituted by a substituent chosen from: a) -OR4 wherein R4 is as defined above, and b) (3) wherein either each of R5 and R6 is independently selected from the group consisting of hydrogen, C1-C6 alkyl, C5-C6 cycloalkyl and aryl, or R5 and R6, taken together with the nitrogen atom to which they are linked, form a pentatomic or hexatomic saturated heteromonocyclic ring, optionally containing at least one additional heteroatom selected from oxygen and nitrogen; and the symbol (----) represents a single or a double bond, and pharmaceutical acceptable salts thereof. In view of their 5α-reductase inhibiting activity the compounds of the invention can be useful for the treatment of androgen dependent conditions.

10. 发明申请

WO1991006563A1 REDUCED IRREVERSIBLE BOMBESIN ANTAGONISTS 审中-公开
标题翻译：减少不可逆的BOMBESIN ANTAGONISTS
公开(公告)号：WO1991006563A1
公开(公告)日：1991-05-16
申请号：PCT/EP1990001836
申请日：1990-11-02
申请人： FARMITALIA CARLO ERBA S.R.L. , DE CASTIGLIONE, Roberto , GOZZINI, Luigia , CORRADI, Fabio , CIOMEI, Marina , MOLINARI, Isabella , FRANZETTI, Cristina
发明人： FARMITALIA CARLO ERBA S.R.L.
IPC分类号： C07K07/02
CPC分类号： C07K7/086 , A61K38/00
摘要： A peptide of the formula (I): R-A-B-C-Trp-Ala-Val-X-Y-T-W, wherein R represents a group of the formula 4-(ClCH2CH2)2N-C6H4-CH2CH(NHR1)CO-; 3-(ClCH2CH2)2N-C6H4-CH2CH(NHR1)CO-; 4-(ClCH2CH2)2N-C6H4-CO-; 3-(ClCH2CH2)2N-C6H4-CO-; ClCH2CH2NHCO-; ClCH=CH-CO-, BrCH=CH-CO-, CH2=CClCO-, CH2=CBrCO- (either cis or trans isomers); (a); CH=C-CO-; ClCH2CH2CH2N(NO)CO-; ClCH2CO-CH(R2)NHCO(CH2)2CO-; A represents a valence bond, or a Gly, Leu-Gly, Arg-Leu-Gly, or Gln-Arg-Leu-Gly residue, B represents a valence bond or a Asn, Phe or Thr residue; C represents a Gln or His residue, X represents a Gly or ala residue; Y represents a valence bond, or a His(R3), his(R3), Phe, phe, Ser, ser, Ala or ala residue; T represents a valence bond, or a Leu, leu, Phe or phe residue; W represents a group of the formula OR2, NH2, NH(CH2)4)CH3, NH(CH2)2C6H5, Met-R4, Leu-R4, Ile-R4 or Nle-R4; R1 represents a hydrogen atom, a Boc group or an acyl group, R2 represents a hydrogen atom, a linear or branched alyphatic chain having from 1 to 11 carbon atoms, a benzyl or a C1-C21 phenyl group, R3 represents a hydrogen atom or a Tos, Dnp or Bzl group, R4 represents NH2, NH-NH2 or OR2, one or more peptide bonds (CONH) are replaced by reduced peptide bonds (CH2, NH), and the pharmaceutically acceptable salts thereof and pharmaceutically acceptable salts are bombesin antagonists. Their preparation and pharmaceutical compositions containing them are also described.
摘要翻译：式（I）的肽：R-A-B-C-Trp-Ala-Val-X-Y-T-W，其中R表示式4-（ClCH 2 CH 2）2 N-C 6 H 4 -CH 2 CH（NHR 1）CO-; 3-（ClCH2CH2）2 N-C 6 H 4 CH 2 CH（NHR 1）CO-; 4-（ClCH2CH2）2 N-C6H4-CO-; 3-（ClCH2CH2）2 N-C6H4-CO-; ClCH2CH2NHCO-; ClCH = CH-CO-，BrCH = CH-CO-，CH2 = CClCO-，CH2 = CBrCO-（顺式或反式异构体）; （一个）; CH = C-CO-; ClCH2CH2CH2N（NO）CO-; ClCH2CO-CH（R2）NHCO（CH 2）2 CO-; A表示价键，或Gly，Leu-Gly，Arg-Leu-Gly或Gln-Arg-Leu-Gly残基，B表示价键或Asn，Phe或Thr残基; C表示Gln或His残基，X表示Gly或ala残基; Y代价键，或His（R3），他的（R3），Phe，phe，Ser，ser，Ala或ala残基; T表示价键，或Leu，leu，Phe或phe残基; W表示式OR2，NH2，NH（CH2）4）CH3，NH（CH2）2C6H5，Met-R4，Leu-R4，Ile-R4或Nle-R4的基团; R 1表示氢原子，Boc基或酰基，R 2表示氢原子，具有1至11个碳原子的直链或支链亚构链，苄基或C 1 -C 21苯基，R 3表示氢原子或 Tos，Dnp或Bzl基团，R4代表NH2，NH-NH2或OR2，一个或多个肽键（CONH）被还原的肽键（CH2，NH）取代，其药学上可接受的盐和药学上可接受的盐是铃蟾肽拮抗剂。还描述了它们的制备方法和含有它们的药物组合物。

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