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1. 发明申请

US20120165254A1 SULPHATED HYALURONIC ACID FOR TREATING DEGENERATIVE OSTEOARTHRITIS 有权
标题翻译：用于治疗变应性OSTEOARTHRITIS的硫酸羟丙酸
公开(公告)号：US20120165254A1
公开(公告)日：2012-06-28
申请号：US13410227
申请日：2012-03-01
申请人： Lanfranco Callegaro , Davide Renier
发明人： Lanfranco Callegaro , Davide Renier
IPC分类号： A61K31/728 , A61P19/02 , A61K38/22 , A61P19/00 , A61K38/39 , A61K38/18
CPC分类号： A61K31/737 , A61K9/0019 , A61K9/1652 , A61K9/4866 , A61K31/726 , A61K38/014 , A61K38/39 , A61K45/06 , A61K2300/00
摘要： This invention relates to oral and intra-articular formulations based on sulphated hyaluronic acid which are effective in the treatment of degenerative osteoarthritis.
摘要翻译：本发明涉及基于硫酸化透明质酸的口服和关节内制剂，其有效治疗退行性骨关节炎。

2. 发明授权

US6020484A Process for preparing a hyaluronic acid fraction having a low polydispersion index 失效
$Process for preparing a hyaluronic acid fraction having a low polydispersion index$
标题翻译：具有低多分散指数的透明质酸级分的制备方法
公开(公告)号：US6020484A
公开(公告)日：2000-02-01
申请号：US96646
申请日：1998-06-12
申请人： Lanfranco Callegaro , Davide Renier
发明人： Lanfranco Callegaro , Davide Renier
IPC分类号： C08B37/08 , C07H1/00
CPC分类号： C08B37/0072
摘要： A process for preparing a hyaluronic acid fraction having an average molecular weight comprised between 5000 and 300,000 and a polydispersion index lower than 1.7, comprising treating the starting high molecular weight hyaluronic acid, contemporaneously with sodium hypochlorite and ultrasounds.
摘要翻译： PCT No.PCT / EP96 / 05701 Sec。 371日期：1998年7月12日 102（e）1998年7月12日PCT 1996年12月19日PCT PCT。公开号WO97 / 22629 日期1997年6月26日制备平均分子量为5000〜300000，多分散指数低于1.7的透明质酸级分的方法，其包括用次氯酸钠和超声波同时处理起始高分子量透明质酸。

3. 发明授权

US09789200B2 Therapeutic use of new pharmaceutical preparations containing antitumoral drugs bound to hyaluronic acid in the treatment of neoplasias 有权
公开(公告)号：US09789200B2
公开(公告)日：2017-10-17
申请号：US12988630
申请日：2009-04-21
申请人： Monica Campisi , Davide Renier , Pasquale Pierimarchi , Annalucia Serafino
发明人： Monica Campisi , Davide Renier , Pasquale Pierimarchi , Annalucia Serafino
IPC分类号： A61K47/48
CPC分类号： A61K47/61
摘要： The present invention describes the new use in the oncologic field of bioconjugates as differentiating agents obtained by the conjugation between hyaluronic acid (HA) and a chemotherapeutic product (identified hereafter with the trade-name ONCOFID®) among which, in particular, Irinotecan, Doxorubicin, Paclitaxel, Cis-platinum and 5-Fluorouracyl (5-FU) for treating primary tumors and metastasis. In particular, the biological behavior is described in terms of action mechanism, efficacy and tolerability of pharmaceutical preparations of derivative of ONCOFID® soluble in water. More specifically, the invention relates to the surprising biological and pharmacological effect demonstrated by formulations based on ONCOFID-S (HA-SN38 conjugates) and ONCOFID-D (HA-Doxorubicin conjugates) in promoting the differentiation of tumoral cells towards a untransformed phenotype, compared with the reference drug Irinotecan (or CPT11 whose active form is represented by SN38) and Doxorubicin.

4. 发明申请

US20100197631A1 HYALURONIC ACID DERIVATIVES CONTAINING GROUPS ABLE TO RELEASE NO 审中-公开
标题翻译：含有可释放NO的组合物的羟丙酸衍生物
公开(公告)号：US20100197631A1
公开(公告)日：2010-08-05
申请号：US12665151
申请日：2008-06-25
申请人： Davide Renier , Matteo D'este
发明人： Davide Renier , Matteo D'este
IPC分类号： A61K31/728 , C07H1/00
CPC分类号： A61K31/728 , A61K9/0014 , A61K9/0021 , A61K45/06 , A61K47/36 , A61K47/61 , C08B37/0072
摘要： Disclosed are hyaluronic acid derivatives functionalised with S-nitrosothiol groups of the general formula: wherein HA indicates hyaluronic acid and G indicates a suitable spacer.
摘要翻译：本发明公开了具有以下通式的S-亚硝基硫醇官能化的透明质酸衍生物：其中HA表示透明质酸，G表示合适的间隔基。

5. 发明申请

US20090197807A1 SULPHATED HYALURONIC ACID FOR TREATING DEGENERATIVE OSTEOARTHRITIS 审中-公开
标题翻译：用于治疗变应性OSTEOARTHRITIS的硫酸羟丙酸
公开(公告)号：US20090197807A1
公开(公告)日：2009-08-06
申请号：US12302511
申请日：2007-05-03
申请人： Lanfranco Callegaro , Davide Renier
发明人： Lanfranco Callegaro , Davide Renier
IPC分类号： A61K31/728 , A61P19/00 , A61K8/65
CPC分类号： A61K31/737 , A61K9/0019 , A61K9/1652 , A61K9/4866 , A61K31/726 , A61K38/014 , A61K38/39 , A61K45/06 , A61K2300/00
摘要： This invention relates to oral and intra-articular formulations based on sulphated hyaluronic acid which are effective in the treatment of degenerative osteoarthritis.
摘要翻译：本发明涉及基于硫酸化透明质酸的口服和关节内制剂，其有效治疗退行性骨关节炎。

6. 发明授权

US09687558B2 Antitumoral bioconjugates of hyaluronic acid or its derivatives obtained by indirect chemical conjugation, and their use in the pharmaceutical field 有权
公开(公告)号：US09687558B2
公开(公告)日：2017-06-27
申请号：US11989716
申请日：2006-08-02
申请人： Davide Renier , Fabio Bettella
发明人： Davide Renier , Fabio Bettella
IPC分类号： A61K47/48
CPC分类号： A61K47/4823 , A61K47/61
摘要： The present invention describes a new group of bioconjugates which can be obtained by means of indirect synthesis, via a molecular spacer, between hyaluronic acid and/or its derivatives and drugs with an antitumoral activity belonging to different groups, their preparation process and use in the oncological field. The new derivatives, in relation to the type of bond and Substitution degree, have different physico-chemical properties which improve their tolerability and efficiency and allow a more accurate modulation of the dosage, exploiting an active targeting mechanism.

7. 发明申请

US20120114602A1 PROCESS FOR THE SYNTHESIS OF CONJUGATES OF GLYCOSAMINOGLYCANES (GAG) WITH BIOLOGICALLY ACTIVE MOLECULES, POLYMERIC CONJUGATES AND RELATIVE USES THEREOF 有权
标题翻译：合成具有生物活性分子的糖蛋白氨基酸（GAG）结合的方法，聚合物共聚物及其相关用途
公开(公告)号：US20120114602A1
公开(公告)日：2012-05-10
申请号：US13378660
申请日：2010-06-04
申请人： Matteo D'Este , Davide Renier , Gianfranco Pasut , Antonio Rosato
发明人： Matteo D'Este , Davide Renier , Gianfranco Pasut , Antonio Rosato
IPC分类号： A61K38/21 , C07K17/10 , C07H21/00 , C07H1/00 , A61P31/12 , C12N9/96 , C07H21/02 , A61K38/17 , A61K31/726 , A61P35/00 , C08B37/00 , C07K1/04
CPC分类号： C08B37/0072 , A61K31/726 , C08B37/0063 , C08B37/0069 , C08B37/0075
摘要： The present invention relates to a process for the synthesis of conjugates of glycosaminoglycanes (GAG) with biologically active molecules of varying nature, comprising small molecules and macro-molecules. In particular, the present invention relates to the conjugation of hyaluronic acid (HA) and its derivatives with polypeptides and proteins with a biological action, such as, for example, interferons, erythropoietins, growth factors, insulin, cytokines, antibodies and hormones.An object of the present invention also relates to isolatable intermediates obtained by the partial or total reaction of GAG with protected amino aldehydes in the conjugation process mentioned above.
摘要翻译：本发明涉及一种用于合成糖胺聚糖（GAG）与不同性质的生物活性分子的缀合物的方法，其包含小分子和大分子。特别地，本发明涉及透明质酸（HA）及其衍生物与具有生物作用的多肽和蛋白质（例如干扰素，促红细胞生成素，生长因子，胰岛素，细胞因子，抗体和激素）的缀合。本发明的目的还涉及通过上述共轭方法中GAG与被保护的氨基醛的部分或全部反应获得的可分离的中间体。

8. 发明申请

US20110189265A1 THERAPEUTIC USE OF NEW PHARMACEUTICAL PREPARATIONS CONTAINING ANTITUMORAL DRUGS BOUND TO HYALURONIC ACID IN THE TREATMENT OF NEOPLASIAS 有权
标题翻译：在治疗NEOPLASIAS中治疗含有抗高血压药物的抗药物的新药物制剂的治疗应用
公开(公告)号：US20110189265A1
公开(公告)日：2011-08-04
申请号：US12988630
申请日：2009-04-21
申请人： Monica Campisi , Davide Renier , Pasquale Pierimarchi , Annalucia Serafino
发明人： Monica Campisi , Davide Renier , Pasquale Pierimarchi , Annalucia Serafino
IPC分类号： A61K9/127 , A61K47/48 , A61P35/00 , A61P35/04
CPC分类号： A61K47/61
摘要： The present invention describes the new use in the oncologic field of bioconjugates as differentiating agents obtained by the conjugation between hyaluronic acid (HA) and a chemotherapeutic product (identified hereafter with the trade-name ONCOFID®) among which, in particular, Irinotecan, Doxorubicin, Paclitaxel, Cis-platinum and 5-Fluorouracyl (5-FU) for treating primary tumors and metastasis. In particular, the biological behaviour is described in terms of action mechanism, efficacy and tolerability of pharmaceutical preparations of derivative of ONCOFID® soluble in water. More specifically, the invention relates to the surprising biological and pharmacological effect demonstrated by formulations based on ONCOFID-S (HA-SN38 conjugates) and ONCOFID-D (HA-Doxorubicin conjugates) in promoting the differentiation of tumoral cells towards a untransformed phenotype, compared with the reference drug Irinotecan (or CPT11 whose active form is represented by SN38) and Doxorubicin.
摘要翻译：本发明描述了在生物缀合物的肿瘤领域中的新用途，其作为通过透明质酸（HA）和化学治疗产品（以下称为商品名ONCOFID）之间缀合获得的分化剂），其中尤其是伊立替康，多柔比星，紫杉醇，顺铂和5-氟尿酰基（5-FU）用于治疗原发性肿瘤和转移。特别地，根据可溶于水的ONCOFID的衍生物的药物制剂的作用机制，功效和耐受性来描述生物学行为。更具体地，本发明涉及通过基于ONCOFID-S（HA-SN38缀合物）和ONCOFID-D（HA-多柔比星缀合物）的制剂在促进肿瘤细胞向未转化表型的分化中所证明的令人惊奇的生物学和药理作用，参考药物伊立替康（或活性形式由SN38代表的CPT11）和多柔比星。

9. 发明授权

US07125860B1 Cross-linked derivatives of hyaluronic acid 有权
标题翻译：透明质酸的交联衍生物
公开(公告)号：US07125860B1
公开(公告)日：2006-10-24
申请号：US10363273
申请日：2001-08-31
申请人： Davide Renier , Vittorio Crescenzi , Andrea Francescangeli
发明人： Davide Renier , Vittorio Crescenzi , Andrea Francescangeli
IPC分类号： A61K31/728 , A61K31/715 , C08B37/08
CPC分类号： A61K9/0019 , A61K47/36 , A61L24/08 , A61L31/042 , C08B37/0072 , C08L5/08
摘要： The present invention describes a new class of cross-linked derivatives of partially N-deacetylated hyaluronic acid or derivatives thereof, comprising at least one repeating unit of formula (I) hereinafter depicted and a process for the preparation of said cross-linked derivatives, comprising a multicomponent condensation reaction involving the carboxy groups and the amino groups originating from a partial N-deacetylation of hyaluronic acid or derivatives, together with an aldeyde and an isocyanide. The derivatives thus obtained can be used, alone or in association with biologically and/or pharmacologically active substances, for the preparation of pharmaceutical compositions, biomaterials, surgical and healthcare articles, slow release systems and for the coating of biomedical objects.
摘要翻译：本发明描述了一类新的部分N-脱乙酰化透明质酸或其衍生物的交联衍生物，其包含至少一种下文所述的式（I）重复单元和制备所述交联衍生物的方法，包括包括羧基和源自透明质酸或衍生物的部分N-脱乙酰基的氨基的多组分缩合反应与醛和二异氰酸酯反应。由此获得的衍生物可以单独使用或与生物和/或药理学活性物质结合使用，用于制备药物组合物，生物材料，外科和保健用品，缓释系统和用于生物医学物体的涂覆。

10. 发明授权

US09034624B2 Process for the synthesis of conjugates of glycosaminoglycanes (GAG) with biologically active molecules, polymeric conjugates and relative uses thereof 有权
标题翻译：用于合成糖胺聚糖（GAG）与生物活性分子，聚合物共轭物的缀合物的方法及其相关用途
公开(公告)号：US09034624B2
公开(公告)日：2015-05-19
申请号：US13378660
申请日：2010-06-04
申请人： Matteo D'Este , Davide Renier , Gianfranco Pasut , Antonio Rosato
发明人： Matteo D'Este , Davide Renier , Gianfranco Pasut , Antonio Rosato
IPC分类号： C08B37/08 , A61K31/726 , C08B37/00
CPC分类号： C08B37/0072 , A61K31/726 , C08B37/0063 , C08B37/0069 , C08B37/0075
摘要： The present invention relates to a process for the synthesis of conjugates of glycosaminoglycanes (GAG) with biologically active molecules of varying nature, comprising small molecules and macro-molecules. In particular, the present invention relates to the conjugation of hyaluronic acid (HA) and its derivatives with polypeptides and proteins with a biological action, such as, for example, interferons, erythropoietins, growth factors, insulin, cytokines, antibodies and hormones.An object of the present invention also relates to isolatable intermediates obtained by the partial or total reaction of GAG with protected amino aldehydes in the conjugation process mentioned above.
摘要翻译：本发明涉及一种用于合成糖胺聚糖（GAG）与不同性质的生物活性分子的缀合物的方法，其包含小分子和大分子。特别地，本发明涉及透明质酸（HA）及其衍生物与具有生物作用的多肽和蛋白质（例如干扰素，促红细胞生成素，生长因子，胰岛素，细胞因子，抗体和激素）的缀合。本发明的目的还涉及通过上述共轭方法中GAG与被保护的氨基醛的部分或全部反应获得的可分离的中间体。

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