公开(公告)号：US08110676B2

公开(公告)日：2012-02-07

申请号：US11659269

申请日：2005-08-02

Applicant: Ivano Bertini ,  Claudio Luchinat ,  Alessandro Quattrone ,  Massimo Calamante ,  Alessandro Mordini

Inventor： Ivano Bertini ,  Claudio Luchinat ,  Alessandro Quattrone ,  Massimo Calamante ,  Alessandro Mordini

IPC: C07H19/20

CPC classification number: A61K31/7115 ,  A61K31/663 ,  A61K31/7125

Abstract: The invention provides prodrugs activated by RNA-dependent DNA-polymerases, and methods for treating hematological tumors, blood, and blood derivatives from patients affected by retroviral infections by administering the prodrugs. The invention also provides methods for the preparation of pharmaceutical compositions containing the prodrugs.

Abstract translation: 本发明提供了通过RNA依赖性DNA聚合酶活化的前体药物，以及通过施用前药来治疗受到逆转录病毒感染的患者的血液肿瘤，血液和血液衍生物的方法。 本发明还提供了制备含有前体药物的药物组合物的方法。

公开(公告)号：US20080300215A1

公开(公告)日：2008-12-04

申请号：US11659269

申请日：2005-08-02

Applicant: Ivano Bertini ,  Claudio Luchinat ,  Alessandro Quattrone ,  Massimo Calamante ,  Alessandro Mordini

Inventor： Ivano Bertini ,  Claudio Luchinat ,  Alessandro Quattrone ,  Massimo Calamante ,  Alessandro Mordini

IPC: A61K31/7076 ,  C07H19/06 ,  A61K31/708 ,  C07H19/16 ,  A61K31/7068 ,  A61K31/7072 ,  C12P19/38 ,  C12P19/40 ,  A61K35/00

CPC classification number: A61K31/7115 ,  A61K31/663 ,  A61K31/7125

Abstract: Herein described are prodrugs activated by RNA-dependent DNA-polymerases, such as telomerase and retroviral reverse transcriptases, their use for the treatment of haematological tumours and of blood and blood derivatives from patients affected by retroviral infections, and their use for the preparation of pharmaceutical compositions, to be used for the treatment of solid tumours, of precancerous states and of diseases caused by infection with retroviruses.

Abstract translation: 本文描述的是通过RNA依赖性DNA聚合酶如端粒酶和逆转录病毒逆转录酶活化的前药，其用于治疗血液肿瘤的用途，以及受到逆转录病毒感染影响的患者的血液和血液衍生物的用途及其用于制备药物 组合物，用于治疗实体瘤，癌前期状态和由逆转录病毒感染引起的疾病。

公开(公告)号：US07772430B2

公开(公告)日：2010-08-10

申请号：US11659431

申请日：2005-07-29

Applicant: Ivano Bertini ,  Marco Fragai ,  Mauro Lo Conte ,  Claudio Luchinat ,  Cristina Nativi ,  Chiara Venturi

Inventor： Ivano Bertini ,  Marco Fragai ,  Mauro Lo Conte ,  Claudio Luchinat ,  Cristina Nativi ,  Chiara Venturi

IPC: C07C303/00 ,  C07C307/00 ,  C07C309/00 ,  C07C311/00 ,  A01N41/06 ,  A61K31/18 ,  A61K31/70 ,  A01N43/04 ,  C07H15/00 ,  C07H17/00 ,  C07H17/02

CPC classification number: C07C311/29 ,  C07C311/19 ,  C07H3/02

Abstract: Described herein are derivatives of arylsulfonamido-substituted hydroxamic acid of formula (I) having good solubility in water and inhibitory activity of matrix metalloproteinases, useful for the preparation of pharmaceutical compositions for the treatment of diseases associated to a pathologic activity and/or an over-expression of metalloproteinases, and of cosmetic preparations having anti-ageing properties in particular for hair and skin.

Abstract translation: 本文描述了在水中具有良好的溶解性和基质金属蛋白酶的抑制活性的式（I）的芳基亚磺酰氨基取代的异羟肟酸的衍生物，其可用于制备用于治疗与病理活性相关的疾病的药物组合物和/ 金属蛋白酶的表达，以及具有抗衰老特性的化妆品制品，尤其用于头发和皮肤。

公开(公告)号：US20100047894A1

公开(公告)日：2010-02-25

申请号：US12063644

申请日：2006-08-10

Applicant: Ivano Bertini ,  Claudio Luchinat ,  Lucia Banci ,  Rebecca Del Conte ,  Marco Fragai

Inventor： Ivano Bertini ,  Claudio Luchinat ,  Lucia Banci ,  Rebecca Del Conte ,  Marco Fragai

IPC: C12N9/50 ,  C07H21/04 ,  C12N15/63 ,  C12N5/10

CPC classification number: C12N9/6491

Abstract: The use of matrix metalloproteinases, mutated and not mutated, for the preparation of pharmaceutical compositions useful in the treatment of pathologies associated with an accumulation of matrix bio-polymers and/or an excess of TIMPs (Tissue Inhihitors MetalloProteinases) is described; mutated matrix metalloproteinases, in which at least an aminoacid residue in a definite position in the protein, has been mutated into a hydrophilic and/or charged aminoacidic residue, obtaining an increased stability toward autoproteolysis are also described.

Abstract translation: 描述了用于制备用于治疗与基质生物聚合物的积累和/或过量的TIMP相关的病理学的药物组合物（Tissue Inhihitor MetalloProteinases）的突变和未突变的基质金属蛋白酶的用途; 还描述了突变的基质金属蛋白酶，其中蛋白质中一定位置的至少一个氨基酸残基已被突变成亲水和/或带电荷的氨基酸残基，获得了对自身蛋白水解的增加的稳定性。