公开(公告)号：US08900589B2

公开(公告)日：2014-12-02

申请号：US12502433

申请日：2009-07-14

Applicant: Italo Beria ,  Michele Caruso ,  John A. Flygare ,  Vittoria Lupi ,  Rita Perego ,  Paul Polakis ,  Andrew Polson ,  Matteo Salsa ,  Susan D. Spencer ,  Barbara Valsasina ,  Robert L. Cohen

Inventor： Italo Beria ,  Michele Caruso ,  John A. Flygare ,  Vittoria Lupi ,  Rita Perego ,  Paul Polakis ,  Andrew Polson ,  Matteo Salsa ,  Susan D. Spencer ,  Barbara Valsasina ,  Robert L. Cohen

IPC: A61K47/48 ,  A61K39/00 ,  C07K16/28 ,  C07K14/00

CPC classification number: C07K16/2863 ,  A61K47/64 ,  A61K47/6809 ,  C07K2317/76

Abstract: The present invention relates to conjugates of therapeutically useful anthracyclines with carriers such as polyclonal and monoclonal antibodies, proteins or peptides of natural or synthetic origin; methods for their preparation, pharmaceutical composition containing them and use thereof in treating certain mammalian tumors.

Abstract translation: 本发明涉及治疗有用的蒽环类与载体的缀合物，例如天然或合成来源的多克隆和单克隆抗体，蛋白质或肽; 其制备方法，含有它们的药物组合物及其在治疗某些哺乳动物肿瘤中的用途。

公开(公告)号：US20100010008A1

公开(公告)日：2010-01-14

申请号：US12444792

申请日：2007-10-09

Applicant: Michele Caruso ,  Italo Beria ,  Maria Gabriella Brasca ,  Ron Ferguson ,  Helena Posteri

Inventor： Michele Caruso ,  Italo Beria ,  Maria Gabriella Brasca ,  Ron Ferguson ,  Helena Posteri

IPC: A61K31/4162 ,  C07D487/04 ,  A61P35/00 ,  A61P25/28 ,  A61P31/12 ,  A61P37/00 ,  C07D401/14 ,  A61K31/454 ,  A61K31/496 ,  C07D403/14

CPC classification number: C07D487/04

Abstract: Substituted pyrrolo-pyrazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with dysregulated protein kinase activity, like cancer.

Abstract translation: 公开了如说明书中定义的式（I）的取代吡咯并吡唑衍生物及其药学上可接受的盐，其制备方法和包含它们的药物组合物; 本发明的化合物可用于治疗与失调的蛋白激酶活性相关的疾病如癌症。

公开(公告)号：US06593303B1

公开(公告)日：2003-07-15

申请号：US09926055

申请日：2001-08-22

Applicant: Cristina Geroni ,  Marina Ripamonti ,  Michele Caruso ,  Antonino Suarato

Inventor： Cristina Geroni ,  Marina Ripamonti ,  Michele Caruso ,  Antonino Suarato

IPC: A01N4304

CPC classification number: A61K31/704 ,  A61K31/335 ,  A61K31/555 ,  A61K31/70 ,  A61K45/06 ,  A61K2300/00

Abstract: 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.

Abstract translation: 提供了4-脱甲氧基-3'-脱氨基-3'-吖啶基-4'-甲磺酰基柔红霉素或4-脱甲氧基-N，N-双（2-氯乙基）-4'-甲磺酰基柔红霉素和抗 - - 肿瘤抗有丝分裂化合物和/或铂衍生物用于治疗肿瘤，以及通过抑制血管发生来预防或治疗转移瘤或治疗肿瘤。

公开(公告)号：US5744454A

公开(公告)日：1998-04-28

申请号：US635957

申请日：1996-05-06

Applicant: Antonino Suarato ,  Michele Caruso ,  Alberto Bargiotti ,  Dario Ballinari ,  Jacqueline Lansen

Inventor： Antonino Suarato ,  Michele Caruso ,  Alberto Bargiotti ,  Dario Ballinari ,  Jacqueline Lansen

IPC: A61K31/70 ,  A61K31/7028 ,  A61K31/7034 ,  A61K31/704 ,  A61K31/7042 ,  A61K31/7052 ,  A61P25/00 ,  A61P25/28 ,  C07H15/252 ,  C07H17/02 ,  C07H15/24

CPC classification number: A61K31/704 ,  C07H15/252

Abstract: The present invention provides the new use in the manufacture of a medicament for use in the treatment of amyloidosis of an anthracycline of formula A: wherein R1, R2, R3 and X are appropriate substituents. Novel compounds of the formula A, processes for their production and pharmaceutical compositions containing them are also described.

Abstract translation: PCT No.PCT / EP95 / 03480第 371日期：1996年5月6日 102（e）日期1996年5月6日PCT提交1995年9月5日PCT公布。 公开号WO96 / 07665 日期：1996年3月14日本发明提供了用于制备用于治疗式A的蒽环霉素的淀粉样变性的药物的新用途：其中R1，R2，R3和X是适当的取代基。 还描述了式A的新型化合物，其制备方法和含有它们的药物组合物。

公开(公告)号：US4906743A

公开(公告)日：1990-03-06

申请号：US181506

申请日：1988-04-14

Applicant: Michele Caruso ,  Antonino Suarato ,  Francesco Angelucci ,  Federico Arcamone

Inventor： Michele Caruso ,  Antonino Suarato ,  Francesco Angelucci ,  Federico Arcamone

Abstract: Anthracycline glycosides of the general formula (I): ##STR1## wherein R.sub.1 represents a hydrogen atom or a hydroxyl group, one of R.sub.2 and R.sub.3 represents a hydrogen atom and the other of R.sub.2 and R.sub.3 represents a hydrogen atom or a hydroxyl group; and pharmaceutically acceptable acid addition salts thereof are antitumor agents. These glycosides may be prepared from a daunomycinone derivative of formula (II): ##STR2## in which the 4-amino group is protected. 4-Demethoxy-4-amino-daunomycinone (II) and an earlier intermediate in its preparation, 4-demethoxy-4-amino-7-deoxy-daunomycinone (IX), can be diazotized followed by mild reduction to form 4-demethoxy-daunomycinone or 4-demethoxy-7-deoxy-daunomycinone respectively. 4-Demethoxy-daunomycinone can be converted into another antitumor anthracycline glycoside, 4-demethoxy-daunorubicin.

公开(公告)号：US09073893B2

公开(公告)日：2015-07-07

申请号：US14233963

申请日：2012-07-18

Applicant: Gianluca Mariano Enrico Papeo ,  Daniela Borghi ,  Michele Caruso ,  Helena Posteri ,  Mikhail Yurievitch Krasavin

Inventor： Gianluca Mariano Enrico Papeo ,  Daniela Borghi ,  Michele Caruso ,  Helena Posteri ,  Mikhail Yurievitch Krasavin

IPC: C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D401/10 ,  C07D403/04 ,  C07D409/14 ,  A61K31/4188 ,  A61K31/454

CPC classification number: C07D401/04 ,  A61K31/4188 ,  A61K31/454 ,  C07D401/10 ,  C07D401/14 ,  C07D403/04 ,  C07D405/14 ,  C07D409/14

Abstract: There are provided 3-oxo-2,3-dihydro-1H-indazole-4-carboxamide derivatives which selectively inhibit the activity of poly (ADP-ribose) polymerase PARP-1 with respect to poly (ADP-ribose) polymerase PARP-2. The compounds of this invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.

Abstract translation: 提供了选择性抑制聚（ADP-核糖）聚合酶PARP-1相对于聚（ADP-核糖）聚合酶PARP-2的活性的3-氧代-2,3-二氢-1H-吲唑-4-甲酰胺衍生物 。 因此，本发明的化合物可用于治疗诸如癌症，心血管疾病，中枢神经系统损伤和不同形式的炎症的疾病。 本发明还提供了制备这些化合物的方法，包含这些化合物的药物组合物，以及利用包含这些化合物的药物组合物治疗疾病的方法。

公开(公告)号：US08623876B2

公开(公告)日：2014-01-07

申请号：US13495688

申请日：2012-06-13

Applicant: Michele Caruso ,  Italo Beria ,  Maria Gabriella Brasca ,  Ron Ferguson ,  Helena Posteri

Inventor： Michele Caruso ,  Italo Beria ,  Maria Gabriella Brasca ,  Ron Ferguson ,  Helena Posteri

IPC: A61K31/497 ,  A01N43/40 ,  A61K31/445 ,  A01N43/56 ,  A61K31/415 ,  C07D211/32 ,  C07D231/54 ,  C07D487/02

CPC classification number: C07D487/04

Abstract: Substituted pyrrolo-pyrazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with dysregulated protein kinase activity, like cancer.

Abstract translation: 公开了如说明书中定义的式（I）的取代吡咯并吡唑衍生物及其药学上可接受的盐，其制备方法和包含它们的药物组合物; 本发明的化合物可用于治疗与失调的蛋白激酶活性相关的疾病如癌症。

公开(公告)号：US08614220B2

公开(公告)日：2013-12-24

申请号：US12520842

申请日：2007-12-17

Applicant: Michele Caruso ,  Italo Beria ,  Maria Gabriella Brasca ,  Ron Ferguson ,  Helena Posteri ,  Barbara Valsasina

Inventor： Michele Caruso ,  Italo Beria ,  Maria Gabriella Brasca ,  Ron Ferguson ,  Helena Posteri ,  Barbara Valsasina

IPC: A61K31/519 ,  C07D239/70

CPC classification number: C07D487/04 ,  C07D295/135 ,  C07D295/155 ,  C40B40/04 ,  C40B50/14

Abstract: Pyrazolo-quinazoline derivatives of formula (I) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.

Abstract translation: 公开了说明书中定义的式（I）的吡唑并喹唑啉衍生物及其药学上可接受的盐，其制备方法和包含它们的药物组合物; 本发明的化合物在治疗中可用于治疗与失调的蛋白激酶活性相关的疾病，如癌症。

公开(公告)号：US08598172B2

公开(公告)日：2013-12-03

申请号：US12744770

申请日：2008-11-26

Applicant: Michele Caruso ,  Italo Beria ,  Maria Gabriella Brasca ,  Helena Posteri ,  Gabriele Fachin

Inventor： Michele Caruso ,  Italo Beria ,  Maria Gabriella Brasca ,  Helena Posteri ,  Gabriele Fachin

IPC: A61K31/495 ,  C07D475/00

CPC classification number: C07D475/00

Abstract: Dihydropteridin-6-one derivatives of formula (I) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.

Abstract translation: 公开了说明书中定义的式（I）的二氢蝶啶-6-酮衍生物及其药学上可接受的盐，其制备方法和包含它们的药物组合物; 本发明的化合物在治疗中可用于治疗与失调的蛋白激酶活性相关的疾病，如癌症。

公开(公告)号：US08426417B2

公开(公告)日：2013-04-23

申请号：US12679716

申请日：2008-09-25

Applicant: Michele Caruso ,  Italo Beria ,  Maria Gabriella Brasca ,  Helena Posteri ,  Marina Caldarelli ,  Walter Ceccarelli ,  Barbara Valsasina

Inventor： Michele Caruso ,  Italo Beria ,  Maria Gabriella Brasca ,  Helena Posteri ,  Marina Caldarelli ,  Walter Ceccarelli ,  Barbara Valsasina

IPC: C07D403/04 ,  C07D471/04 ,  A61K31/506

CPC classification number: C07D403/04 ,  C07D401/14 ,  C07D405/14 ,  C07D471/04

Abstract: Substituted pyrrolo-pyrimidine derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a dysregulated protein kinase activity, like cancer.

Abstract translation: 公开了如本说明书中定义的式（I）的取代的吡咯并 - 嘧啶衍生物及其药学上可接受的盐，其制备方法和包含它们的药物组合物; 本发明的化合物可用于治疗与失调的蛋白激酶活性相关的疾病如癌症。