公开(公告)号：WO2012100366A1

公开(公告)日：2012-08-02

申请号：PCT/CN2011/000111

申请日：2011-01-25

Applicant: THE PROCTER AND GAMBLE COMPANY ,  TECHNICAL INSTITUTE OF PHYSICS AND CHEMISTRY, CHINESE ACADEMY OF SCIENCES ,  LU, Chengwu ,  YOSHIMI, Naohisa ,  HU, Xincheng ,  LI, Shuang ,  GAO, Yunhua

Inventor： LU, Chengwu ,  YOSHIMI, Naohisa ,  HU, Xincheng ,  LI, Shuang ,  GAO, Yunhua

IPC: A61K9/127 ,  A61K8/14 ,  A61K31/00 ,  A61K47/16

CPC classification number: A61K31/19 ,  A61K8/14 ,  A61K8/44 ,  A61K8/4946 ,  A61K8/4993 ,  A61K8/602 ,  A61K8/86 ,  A61K9/0014 ,  A61K9/06 ,  A61K9/1271 ,  A61K31/198 ,  A61K31/203 ,  A61K31/375 ,  A61K31/704 ,  A61K2800/10 ,  A61K2800/56 ,  A61Q19/00

Abstract: A liposome comprising a phospholipid, a hydrophobic active comprising a carboxylate group, and a component selected from a group consisting of: a hydrophilic adjuvant comprising a positively charged group, a complex of said hydrophobic active with said hydrophilic adjuvant, and combinations thereof. An aqueous liposome dispersion comprising the liposome, and a personal care composition comprising the liposome. A process of preparing the liposome, comprising the steps of: forming a premix by dissolving a phospholipid, a hydrophobic active comprising a carboxylate group in an organic solvent; evaporating off said organic solvent from the premix to form a phospholipid film; and hydrating said lipid film with a hydration medium comprising a hydrophilic adjuvant comprising a positively charged group and homogenize the medium to form an aqueous liposome dispersion.

Abstract translation: 包含磷脂，包含羧酸酯基团的疏水性活性物质和选自以下的组分的脂质体：包含带正电基团的亲水性佐剂，所述疏水性活性物质与所述亲水性佐剂的配合物及其组合。 包含脂质体的脂质体水分散体和包含脂质体的个人护理组合物。 一种制备脂质体的方法，包括以下步骤：通过将磷脂，包含羧酸酯基团的疏水活性物质溶于有机溶剂中形成预混物; 从预混物中蒸发出所述有机溶剂以形成磷脂膜; 以及用包含带正电基团的亲水性佐剂的水合介质水合所述脂质膜，并均质培养基以形成脂质体水分散体。

公开(公告)号：WO2021102624A1

公开(公告)日：2021-06-03

申请号：PCT/CN2019/120572

申请日：2019-11-25

Applicant: HANGZHOU BRANCH OF TECHNICAL INSTITUTE OF PHYSICS AND CHEMISTRY, CHINESE ACADEMY OF SCIENCES

Inventor： WANG, Qian

IPC: A61K31/197 ,  C07K1/113 ,  C07C381/02 ,  A61K31/198 ,  A61P35/00

Abstract: Provided a proximity-enabled reactive therapeutics (PERx) approach to generate covalent protein drugs. A latent bioreactive amino acid FSY was incorporated into human programmed cell death protein 1 (PD-1), which selectively reacted with a proximal histidine of human PD-L1 upon binding, enabling irreversible binding of PD-1 with PD-L1 in vitro, on cancer cells, and in tumor in mice. When administrated in humanized mouse models, the covalent PD-1 (FSY) exhibited robust antitumor effect over wildtype PD-1, achieving therapeutic efficacy equivalent to the FDA approved therapeutic monoclonal antibody atezolizumab. The PERx approach should provide a general method for converting interacting proteins into covalent protein drugs for high therapeutic efficacy.