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1. 发明申请

WO2007067515A3 NOVEL FIVE-MEMBERED IMINOCYCLITOL DERIVATIVES AS SELECTIVE AND POTENT GLYCOSIDASE INHIBITORS: NEW STRUCTURES FOR ANTIVIRALS AND OSTEOARTHRITIS THERAPEUTICS 审中-公开
标题翻译：作为选择性和糖度糖苷酶抑制剂的新型五分子蛋白胆固醇衍生物：用于抗病毒和骨质疏松症治疗的新结构
公开(公告)号：WO2007067515A3
公开(公告)日：2008-01-10
申请号：PCT/US2006046348
申请日：2006-12-05
申请人： ACADEMIA SINICA , LIANG PI-HUI , LIN YI-LING , WONG CHI-HUEY
发明人： LIANG PI-HUI , LIN YI-LING , WONG CHI-HUEY
IPC分类号： A61K31/04
CPC分类号： A61K31/4015
摘要： Novel 5-membered iminocyclitol derivatives were found to be a potent and selective inhibitors of the glycoprotein processing a-and ß-glucosidase which were further found to be active antiviral agents against Japanese encephalitis virus, dengue virus serotype 2 (DEN-2), human SARS coronavirus and human ß-hexosaminidase, a new target for development of osteoarthritis therapeutics.
摘要翻译：发现新的5元亚氨基环醇衍生物是加工α-葡萄糖苷酶的糖蛋白的有效和选择性抑制剂，其进一步被发现是针对日本脑炎病毒，登革热病毒血清型2（DEN-2），人类 SARS冠状病毒和人β-淀粉氨酸酶是骨关节炎治疗的新靶点。

2. 发明申请

WO2012094540A3 METHODS FOR PREPARATION OF GLYCOSPHINGOLIPIDS AND USES THEREOF 审中-公开
标题翻译：制备糖苷类化合物的方法及其用途
公开(公告)号：WO2012094540A3
公开(公告)日：2012-08-30
申请号：PCT/US2012020388
申请日：2012-01-05
申请人： LIANG PI-HUI , UNIV NAT TAIWAN
发明人： LIANG PI-HUI
IPC分类号： C07H15/06 , A61K39/39 , A61P31/04 , A61P31/12 , A61P35/00 , C07H15/04 , C07H15/18
CPC分类号： C07H1/00 , A61K39/39 , C07B2200/07 , C07H15/04 , C07H15/06 , C07H15/18 , Y02P20/55 , A61K31/7028 , A61K31/715
摘要： Methods for synthesis and preparation of alpha-glycosphingolipids are provided. Methods for synthesis of a-galactosyl ceramides, and pharmaceutically active analogs and variants thereof are provided. Novel alpha-glycosphingolipids are provided, wherein the compounds are immunogenic compounds which serve as ligands for NKT (natural killer T) cells. A process for preparing a chiral compound comprising an R-form or S- form of a glycosphingolipid of formula (1 ) is provided, wherein R1=OH, NH2, NHCOR2, R2 = H or an alkyl, alkenyl, or alkyl terminating in aryl, substituted aryl, heteroaryl, or substituted heteroaryl, X=alkyl group, R3= OH or H, R4=OH or H, R5= aryl, substituted aryl, heteroaryl, or substituted heteroaryl, or a pharmaceutically acceptable salt thereof, wherein the compound of formula 1 is prepared by (a) deprotecting a compound of formula (2): wherein PG is a hydroxyl protecting group, with hydrogen under hydrogenation catalysis.
摘要翻译：提供了α-糖苷脂的合成和制备方法。提供了α-半乳糖苷类神经酰胺的合成方法及其药物活性类似物及其变体。提供了新的α-糖苷脂，其中所述化合物是用作NKT（天然杀伤T）细胞配体的免疫原性化合物。提供了制备包含式（1）的R型或S-形式的鞘糖脂的手性化合物的方法，其中R 1 = OH，NH 2，NHCOR 2，R 2 = H或烷基，烯基或烷基，其末端芳基，取代的芳基，杂芳基或取代的杂芳基，X =烷基，R 3 = OH或H，R 4 = OH或H，R 5 =芳基，取代的芳基，杂芳基或取代的杂芳基或其药学上可接受的盐，通过（a）在氢化催化下用氢去除保护式（2）的化合物：其中PG是羟基保护基。

3. 发明专利

AU2020288770A1 Saponin conjugate and vaccine or pharmaceutical composition comprising the same 未知
公开(公告)号：AU2020288770A1
公开(公告)日：2022-01-06
申请号：AU2020288770
申请日：2020-06-01
申请人： LIANG PI HUI
发明人： LIANG PI-HUI , LAI YEN-HSUN , CHANG CHUN-KAI , CHAW CHEE-WAI
IPC分类号： C07H15/20 , A61K31/704 , C07J9/00
摘要： Provided are 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.

4. 发明专利

CA3140411A1 SAPONIN CONJUGATE AND VACCINE OR PHARMACEUTICAL COMPOSITION COMPRISING THE SAME 未知
公开(公告)号：CA3140411A1
公开(公告)日：2020-12-10
申请号：CA3140411
申请日：2020-06-01
申请人： LIANG PI HUI
发明人： LAI YEN-HSUN , CHANG CHUN-KAI , CHAW CHEE-WAI , LIANG PI-HUI
IPC分类号： C07H15/20 , A61K31/704
摘要： Provided are 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.

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