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公开(公告)号:US5547667A
公开(公告)日:1996-08-20
申请号:US328697
申请日:1994-10-25
Applicant: Francesco Angelucci , Laura Bersani , Michele Caruso , Marina Ripamonti , Daniela Ruggieri , Antonino Suarato
Inventor: Francesco Angelucci , Laura Bersani , Michele Caruso , Marina Ripamonti , Daniela Ruggieri , Antonino Suarato
IPC: A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61K31/7042 , A61K39/395 , A61K47/00 , A61K47/48 , A61P35/00 , C07H20060101 , C07H15/252 , C07H17/00 , C07H19/24 , A61K39/44 , C07K17/06 , C07K15/252 , C07K19/06
CPC classification number: C07H15/252 , A61K47/48176 , A61K47/48246 , A61K47/48407 , A61K47/48692 , A61K47/48715 , C07H19/24
Abstract: Conjugates of general formula 1:[A--O--W--Z].sub.a --T 1wherein 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: ##STR1## wherein b is an integer of from 1 to 4, B represents a C.sub.1 -C.sub.3 alkylene group and R.sub.1 and R.sub.2 each independently represent hydrogen, halogen, alkyl, phenyl or substituted phenyl; Z is a spacer group and T is a carrier moiety.
Abstract translation: 通式1的缀合物:[A-O-W-Z] a-T1,其中A-O-部分是式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。
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公开(公告)号:US5776458A
公开(公告)日:1998-07-07
申请号:US412220
申请日:1995-03-27
Applicant: Francesco Angelucci , Daniela Ruggieri , Stefania Stefanelli , Antonino Suarato , Laura Bersani
Inventor: Francesco Angelucci , Daniela Ruggieri , Stefania Stefanelli , Antonino Suarato , Laura Bersani
IPC: A61K47/48 , C07H15/252 , A61K39/395 , A61K39/00 , C07K16/00 , C07K17/00
CPC classification number: C07H15/252 , A61K47/48407
Abstract: The present invention provides anthracycline conjugates with carriers such as monoclonal polyclonal antibodies, proteins or peptides, or other synthetic carriers. These anthracycline conjugates provide pharmaceutical compositions which are useful for treating certain mammalian tumors. The compounds of the present invention have higher potency than anthracyclines, and improved therapeutic efficacy and reduced toxic effects.
Abstract translation: 本发明提供了与载体例如单克隆多克隆抗体,蛋白质或肽或其它合成载体的蒽环霉素缀合物。 这些蒽环霉素缀合物提供可用于治疗某些哺乳动物肿瘤的药物组合物。 本发明的化合物具有比蒽环类药更高的效力,并且具有改善的治疗功效和降低的毒性作用。
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公开(公告)号:US5387578A
公开(公告)日:1995-02-07
申请号:US842171
申请日:1992-04-03
Applicant: Francesco Angelucci , Laura Bersani , Michele Caruso , Marina Ripamonti , Daniela Ruggieri , Antonino Suarato
Inventor: Francesco Angelucci , Laura Bersani , Michele Caruso , Marina Ripamonti , Daniela Ruggieri , Antonino Suarato
IPC: A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61K31/7042 , A61K39/395 , A61K47/00 , A61K47/48 , A61P35/00 , C07H20060101 , C07H15/252 , C07H17/00 , C07H19/24 , A61K37/00 , C07H19/06 , C07K17/06
CPC classification number: C07H15/252 , A61K47/48176 , A61K47/48246 , A61K47/48407 , A61K47/48692 , A61K47/48715 , C07H19/24
Abstract: Conjugate of general formula 1:[A--O--W-Z].sub.a -T 1wherein the moity 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: ##STR1## wherein b is an integer of from 1 to 4, B represents a C.sub.1 -C.sub.3 alkylene group and R.sub.1 and R.sub.2 each independently represent hydrogen, halogen, alkyl, phenyl or substituted phenyl; Z is a spacer group and T is a carrier moiety.
Abstract translation: PCT No.PCT / EP91 / 01449 371日期:1992年4月3日 102(e)日期1992年4月3日PCT 1991年8月1日PCT PCT。 公开号WO92 / 02255 通式1:[A-O-W-Z] a-T1的结合物,其中,A-O-是式A-O-H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。
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