公开(公告)号：US06960344B2

公开(公告)日：2005-11-01

申请号：US10114465

申请日：2002-04-03

Applicant: Dante J. Marciani

Inventor： Dante J. Marciani

IPC: A61K39/00 ,  A61K39/39 ,  A61K47/48 ,  A61P37/04 ,  C08B37/00 ,  C08B37/06 ,  C08B37/08 ,  A61K39/385 ,  A61K31/715

CPC classification number: C08B37/003 ,  A61K47/61

Abstract: The present invention relates to polysaccharide conjugates that comprise: a polysaccharide that binds to surface-receptors present on Antigen Presenting Cells, conjugated to one or more compounds having stable carbonyl groups covalently attached, either directly or via a bifunctional linker. The conjugates are useful as immuno-stimulants and adjuvants.

Abstract translation: 本发明涉及多糖缀合物，其包含：直接或通过双功能连接体结合存在于存在于抗原呈递细胞上的表面受体的多糖，缀合至一个或多个具有共价连接的稳定羰基的化合物。 缀合物可用作免疫兴奋剂和佐剂。

公开(公告)号：US20040242502A1

公开(公告)日：2004-12-02

申请号：US10820036

申请日：2004-04-08

Applicant: Galenica Pharmaceuticals, Inc.

Inventor： Dante J. Marciani

IPC: A61K031/704 ,  C07H015/24 ,  C07J017/00

CPC classification number: C07J17/00 ,  C07H15/24 ,  C07H15/256

Abstract: The present invention discloses novel saponin derivatives for use with nucleic acids that induce an immune response when administered to animals and humans. The novel saponin derivatives disclosed comprise (a) a saponin aglycone core, wherein the aglycone core is covalently linked to one or more oligosaccharide chains; (b) a positively charged cationic chain, and optionally (c) a naturally occurring or synthetic lipophilic chain. Pharmaceutical and veterinary compositions comprising one or more of the novel saponin derivatives and saponin derivative/polynucleotide complexes are also disclosed. Disclosed as well are methods of using the novel saponin derivatives to deliver a polynucleotide molecule to cells of an animal, to stimulate or generate an immune response in an animal, and to generate a detectable immune response in an animal.

Abstract translation: 本发明公开了用于当被给予动物和人时诱导免疫应答的核酸的新型皂苷衍生物。 所公开的新型皂苷衍生物包含（a）皂苷苷元糖苷配基核心，其中糖苷配基核共价连接至一个或多个寡糖链; （b）带正电的阳离子链，和任选地（c）天然存在的或合成的亲脂链。 还公开了包含一种或多种新型皂苷衍生物和皂苷衍生物/多核苷酸复合物的药物和兽药组合物。 还公开了使用新型皂苷衍生物将多核苷酸分子递送至动物细胞，刺激或产生动物免疫应答并在动物中产生可检测的免疫应答的方法。

公开(公告)号：US20040220142A1

公开(公告)日：2004-11-04

申请号：US10859577

申请日：2004-06-03

Applicant: Galenica Pharmaceuticals, Inc.

Inventor： Dante J. Marciani

IPC: A61K031/715 ,  C07H015/04

CPC classification number: C08B37/003 ,  A61K47/61

Abstract: The present invention relates to polysaccharide conjugates that comprise: a polysaccharide that binds to surface-receptors present on Antigen Presenting Cells, conjugated to one or more compounds having stable carbonyl groups covalently attached, either directly or via a bifunctional linker. The conjugates are useful as immuno-stimulants and adjuvants.

公开(公告)号：US20020150585A1

公开(公告)日：2002-10-17

申请号：US10114465

申请日：2002-04-03

Applicant: Galenica Pharmaceuticals, Inc.

Inventor： Dante J. Marciani

IPC: A61K039/00 ,  A61K031/739 ,  A61K031/715

CPC classification number: C08B37/003 ,  A61K47/61

Abstract: The present invention relates to polysaccharide conjugates that comprise: a polysaccharide that binds to surface-receptors present on Antigen Presenting Cells, conjugated to one or more compounds having stable carbonyl groups covalently attached, either directly or via a bifunctional linker. The conjugates are useful as immuno-stimulants and adjuvants.

Abstract translation: 本发明涉及多糖缀合物，其包含：直接或通过双功能连接体结合存在于存在于抗原呈递细胞上的表面受体的多糖，缀合至一个或多个具有共价连接的稳定羰基的化合物。 缀合物可用作免疫兴奋剂和佐剂。

公开(公告)号：US6080725A

公开(公告)日：2000-06-27

申请号：US290606

申请日：1999-04-13

Applicant: Dante J. Marciani

Inventor： Dante J. Marciani

IPC: A61K39/39 ,  A61K47/48 ,  C07H15/256 ,  A61K31/705 ,  A61K39/00

CPC classification number: C07H15/256 ,  A61K39/39 ,  A61K47/48023 ,  A61K47/48038 ,  A61K2039/55577

Abstract: The present invention is directed to vaccines comprising (1) one or more bacterial, viral or tumor-associated antigens; and (2) one or more saponin-lipophile conjugate in which a lipophilic moiety such as a lipid, fatty acid, polyethylene glycol or terpene is covalently attached to a non-acylated or desacylated triterpene saponin via a carboxyl group present on the 3-O-glucuronic acid of the triterpene saponin. The attachment of a lipophile moiety to the 3-O-glucuronic acid of a saponin such as Quillaja desacylsaponin, lucyoside P, or saponin from Gypsophila, Saponaria and Acanthophyllum enhances their adjuvant effects on humoral and cell mediated immunity. Additionally, the attachment of a lipophile moiety to the 3-O-glucuronic acid residue of non- or des-acylsaponin yields a saponin analog that is easier to purify, less toxic, chemically more stable, and possesses equal or better adjuvant properties than the original saponin.

Abstract translation: 本发明涉及包含（1）一种或多种细菌，病毒或肿瘤相关抗原的疫苗; 和（2）一种或多种皂苷 - 亲脂性缀合物，其中亲脂性部分如脂质，脂肪酸，聚乙二醇或萜烯通过存在于3-O上的羧基共价连接到非酰化或去酰化三萜皂苷上 - 三葡萄糖皂苷的葡萄糖醛酸。 亲油部分连接到诸如Quillaja desacylsaponin，Lucyoside P或皂甙皂甙皂甙皂甙皂甙皂甙皂甙的3-O-葡萄糖醛酸增强了其对体液和细胞介导的免疫的佐剂效应。 另外，将亲油部分连接到非或去酰基皂苷的3-O-葡糖醛酸残基产生皂化物类似物，其更易于纯化，毒性较小，化学性更稳定，并且具有等于或优于佐剂性质 原皂甙

公开(公告)号：US5977081A

公开(公告)日：1999-11-02

申请号：US81647

申请日：1998-05-20

Applicant: Dante J. Marciani

Inventor： Dante J. Marciani

IPC: A61K31/56 ,  A61K31/704 ,  A61K36/00 ,  A61K39/39 ,  A61K47/48 ,  A61P37/04 ,  A61P43/00 ,  C07H15/256 ,  C07J63/00 ,  A61K31/70 ,  A61K31/705 ,  C07H15/24

CPC classification number: A61K47/48023 ,  A61K39/39 ,  A61K47/48038 ,  C07H15/256 ,  A61K2039/55577

Abstract: The present invention is directed to novel chemical compounds in which a lipophilic moiety such as a lipid, fatty acid, polyethylene glycol or terpene is covalently attached to a non-acylated or desacylated triterpene saponin via a carboxyl group present on the 3-O-glucuronic acid of the triterpene saponin. The attachment of a lipophile moiety to the 3-O-glucuronic acid of a saponin such as Quillaja desacylsaponin, lucyoside P, or saponin from Gypsophila, Saponaria and Acanthophyllum enhances their adjuvant effects on humoral and cell mediated immunity. Additionally, the attachment of a lipophile moiety to the 3-O-glucuronic acid residue of non- or des-acylsaponin yields a saponin analog that is easier to purify, less toxic, chemically more stable, and possesses equal or better adjuvant properties than the original saponin.

Abstract translation: 本发明涉及新型化合物，其中亲脂性部分如脂质，脂肪酸，聚乙二醇或萜烯通过存在于3-O-葡萄糖醛酸上的羧基共价连接到非酰化或去酰化三萜皂苷上 三萜皂苷的酸。 亲油部分连接到皂角苷的3-O-葡糖醛酸如Quillaja desacylsaponin，Lucyoside P或来自Gypsophila，Saponaria和Acanthophyllum的皂角苷增强了它们对体液和细胞介导的免疫的佐剂效应。 另外，将亲油部分连接到非或去酰基皂苷的3-O-葡糖醛酸残基产生皂化物类似物，其更易于纯化，毒性较小，化学性更稳定，并且具有等于或优于佐剂性质 原皂甙