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1.WO/2025/140339USE OF ERGOTHIONEINE, COMPOSITION COMPRISING SAME, AND USE THEREOF
WO 03.07.2025
Int.Class A61K 31/4172
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
41having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
41641,3-Diazoles
4172Imidazole-alkanecarboxylic acids, e.g. histidine
Appl.No PCT/CN2024/142425 Applicant BLOOMAGE BIOTECHNOLOGY CORPORATION LIMITED Inventor LIU, Shaoying
Use of ergothioneine, a composition comprising same, and use thereof. As a fibronectin (FN) inhibitor and/or an α-smooth muscle actin (α-SMA) inhibitor, ergothioneine can effectively inhibit the up-regulated expression of fibronectin and α-smooth muscle actin, thereby effectively inhibiting the process of skin cell fibrosis, and providing a new inhibitor active ingredient for skin cell fibrosis.
2.WO/2025/140595ASYMMETRIC CATIONIC LIPID HAVING BRANCHED PIPERAZINE RING
WO 03.07.2025
Int.Class C07D 295/088
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
295Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
04with substituted hydrocarbon radicals attached to ring nitrogen atoms
08substituted by singly bound oxygen or sulfur atoms
084with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
088to an acyclic saturated chain
Appl.No PCT/CN2024/143287 Applicant XIAMEN SINOPEG BIOTECH CO., LTD Inventor WEI, Guohua
The present invention belongs to the field of drug delivery. Provided is an asymmetric cationic lipid containing a branched piperazine ring and having a structure as shown in general formula (1), wherein the definition of each symbol is consistent with that described in the text. In the cationic lipid of the present invention, a degradable group is introduced at an appropriate position, and the presence of the degradable group makes an LNP-pharmaceutical composition prepared therefrom be degraded at an appropriate time in vivo and have a low cytotoxicity, which solves the problems in the prior art that an LNP-pharmaceutical composition prepared from a non-degradable lipid can accumulate in endosomes and acidify the endosomal environment, so that the endosomal escape of a drug (e.g., mRNA) is hindered, and the drug delivered into cells cannot fully function. In the cationic lipid of the present invention, a heterofunctionalized small molecule containing a piperazine ring is used as a raw material. The preparation process is simple and convenient, has a lower cost, and is more environmentally friendly. The LNP-mRNA composition prepared therefrom has the advantages of low toxicity, high biocompatibility, high cell transfection, etc.
3.WO/2025/142929COMPOSITION FOR TREATING AND/OR PREVENTING GRANULOMA OR DISEASE ASSOCIATED WITH GRANULOMA, AND METHOD AND KIT FOR DETERMINING WHETHER SUBJECT HAS GRANULOMA OR NOT
WO 03.07.2025
Int.Class A61K 45/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
45Medicinal preparations containing active ingredients not provided for in groups A61K31/-A61K41/132
Appl.No PCT/JP2024/045701 Applicant KYOTO UNIVERSITY Inventor KABASHIMA, Kenji
Provided is a composition for treating and/or preventing granuloma, the composition containing an inhibitor of an enzyme involved in the pentose phosphate pathway. Also provided is a composition for treating and/or preventing a disease associated with granuloma, the composition containing an inhibitor of an enzyme involved in the pentose phosphate pathway. Further provided are a method and a kit for determining whether a subject has granuloma or not on the basis of the level of an enzyme involved in the pentose phosphate pathway in a sample collected from the subject.
4.WO/2025/143049PROPHYLACTIC AND/OR THERAPEUTIC AGENT FOR NEURODEGENERATIVE DISEASE
WO 03.07.2025
Int.Class A61K 45/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
45Medicinal preparations containing active ingredients not provided for in groups A61K31/-A61K41/132
Appl.No PCT/JP2024/045989 Applicant RIKEN Inventor FUKUI Masahiro
The purpose of the present invention is to provide a novel prophylactic and/or therapeutic agent for a neurodegenerative disease, which can increase the number of new neurons in an adult brain. The present invention is a prophylactic and/or therapeutic agent for a neurodegenerative disease, the agent containing, as an active ingredient, an inhibitor of any one of genes shown in table 1 or a protein derived from any one of the genes.
5.WO/2025/140155NUCLEIC ACID MOLECULE FOR INHIBITING D2HGDH, INHIBITOR AND USE THEREOF
WO 03.07.2025
Int.Class A61K 45/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
45Medicinal preparations containing active ingredients not provided for in groups A61K31/-A61K41/132
Appl.No PCT/CN2024/141683 Applicant XIAMEN UNIVERSITY Inventor LI, Qinxi
A nucleic acid molecule for specifically inhibiting the transcription or translation of a D2HGDH gene or an inhibitor for inhibiting the activity of a protein encoded by the D2HGDH gene, and the use thereof in preparing a drug for treating tumors. The nucleic acid molecule for specifically inhibiting the transcription or translation of the D2HGDH gene is a shRNA, a siRNA and/or a sgRNA. The inhibitor for inhibiting the activity of the protein encoded by the D2HGDH gene comprises at least one of ginkgolic acid C15:1 and NSC87877.
6.WO/2025/140590CATIONIC LIPID COMPRISING NITROGEN-CONTAINING HETEROCYCLE AND GLYCINE
WO 03.07.2025
Int.Class C07D 295/088
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
295Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
04with substituted hydrocarbon radicals attached to ring nitrogen atoms
08substituted by singly bound oxygen or sulfur atoms
084with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
088to an acyclic saturated chain
Appl.No PCT/CN2024/143275 Applicant XIAMEN SINOPEG BIOTECH CO., LTD Inventor LIN, Sheng
The present invention provides a glycine-containing cationic lipid. The structure of the glycine-containing cationic lipid is shown as general formula (1-A), wherein the definition of each symbol is consistent with that in the description. The glycine-branched cationic lipid has a nitrogen-containing heterocycle as a central branched core, has glycine as a secondary branched core, and has a saturated or unsaturated hydrocarbon group as a tail chain, and has the advantages of low toxicity, low immunogenicity, and high biocompatibility. Glycine contained in the novel cationic lipid of the present invention can provide a tertiary amine structure while serving as the secondary branched core, and form a multi-stage tertiary amine structure together with the nitrogen-containing heterocycle central core, increasing the number of tertiary amines capable of being ionized to produce positive charges. When preparing an LNP, the amount of cationic lipid used is less, which is safer and improves the translation efficiency of nucleic acids.
7.WO/2025/137891USE OF COMBINED COMPOUND MEDICINE IN TREATING PATHOGENIC BACTERIA PERSISTENT INFECTION
WO 03.07.2025
Int.Class A61K 45/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
45Medicinal preparations containing active ingredients not provided for in groups A61K31/-A61K41/132
06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
Appl.No PCT/CN2023/142138 Applicant SOOCHOW UNIVERSITY Inventor HONG, Yuzhi
Disclosed is use of a combined compound medicine in treating pathogenic bacteria persistent infection. Existing antibiotic monotherapy or combination therapy is usually difficult to kill pathogenic bacteria in the persister state, especially nutrient-insensitive persister bacteria, which often lead to a series of problems of long treatment period, frequent condition recurrence and deterioration, treatment failure, drug-resistant mutation, etc. At present, drugs capable of efficiently killing highly persistent pathogenic bacteria in a clinically applicable concentration range are still unavailable. The novel compound medicine of polymyxin and aminoglycoside antibiotics disclosed in the present disclosure without precedence is capable of destroying bacterial cell membranes in a short time within a relatively wide range of clinically achievable plasma concentrations, leading to rapid death of a large number of bacteria, but is safe for human-derived cells. Therefore, the compound medicine is expected to be applied to the clinical treatment of various acute or chronic infectious diseases caused by pathogenic bacteria in the persister state, shortening the treatment course, preventing the recurrence of infection recurrence, and slowing down the emergence of drug-resistant mutations.
8.WO/2025/138371PHB2 AS TUMOR IMMUNOTHERAPY TARGET AND USE THEREOF IN DRUG DEVELOPMENT
WO 03.07.2025
Int.Class C12Q 1/6886
CCHEMISTRY; METALLURGY
12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
QMEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
1Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
68involving nucleic acids
6876Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes
6883for diseases caused by alterations of genetic material
6886for cancer
Appl.No PCT/CN2024/073620 Applicant SHENZHEN INSTITUTES OF ADVANCED TECHNOLOGY Inventor PAN, Fan
Disclosed is the use of a PHB2 gene or a PHB2 protein as a new immune checkpoint. Targeting PHB2 can inhibit mitochondrial fusion, thereby increasing mitochondrial fragmentation, elevating mitochondrial metabolic levels, and enhancing the anti-tumor function of cells in vivo and in vitro. Moreover, targeting PHB2 can reduce the expression of PD-1, and when used in combination with a CTLA-4 monoclonal antibody, can enhance anti-tumor effects. On this basis, further disclosed is the use of a drug having an inhibitory effect on a PHB2 gene or a PHB2 protein in the preparation of a PD-1 inhibitor, or the use of same in combination with a PD-1 monoclonal antibody in the preparation of a therapeutic product or a preventive product for treating or preventing tumors. Further disclosed is the use of a drug having an inhibitory effect on a PHB2 gene or a PHB2 protein in combination with a CTLA-4 monoclonal antibody in the preparation of a therapeutic product or a preventive product for treating or preventing tumors. Further disclosed is the use of a drug having an inhibitory effect on a PHB2 gene or a PHB2 protein alone, in combination with a PD-1 monoclonal antibody or in combination with a CTLA-4 monoclonal antibody in immunotherapy, especially tumor immunotherapy. It has been found in experiments that tumors in PHB2+/- tumor-bearing mice are significantly reduced compared with those in the control. It has been further found that targeting mitochondrial PHB2 can increase mitochondrial fragmentation by means of inhibiting mitochondrial fusion, so that the mitochondrial metabolism is enhanced; moreover, after PHB2 knockout, PD-1 expression is reduced, and when used in combination with a CTLA-4 monoclonal antibody, can enhance anti-tumor effects.
9.WO/2025/141131A GABAA RECEPTOR LIGAND AND THE USE THEREOF IN MEDICINE, IN PARTICULAR IN THE TREATMENT OF EPILEPSY
WO 03.07.2025
Int.Class A61K 31/437
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435having six-membered rings with one nitrogen as the only ring hetero atom
4353ortho- or peri-condensed with heterocyclic ring systems
437the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
Appl.No PCT/EP2024/088522 Applicant SANIONA A/S Inventor POULSEN, Pernille Hartveit
The present invention relates to a novel compound useful in the treatment of central nervous system diseases and disorders which are responsive to modulation of the GABAA receptor complex.
10.WO/2025/137772DNA DOUBLE-STRAND BREAK-CAPTURING NUCLEAR ENVELOPE TUBULES DRIVE DNA REPAIR
WO 03.07.2025
Int.Class A61K 38/45
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
38Medicinal preparations containing peptides
16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
43Enzymes; Proenzymes; Derivatives thereof
45Transferases (2)
Appl.No PCT/CA2024/051735 Applicant THE GOVERNING COUNCIL OF THE UNIVERSITY OF TORONTO Inventor MEKHAIL, Karim
The present disclosure describes a method of treating a dsbNETs-associated pathology or con- dition in a subject in need thereof, comprising administering a therapeutically effective amount of a dsbNETs modulator in the subject, wherein dsbNETs repair or misrepair damaged DNA or wherein excessively induced or persistent dsbNETs trigger DNA damage.