Alerta

COMPOUNDS AND METHOD FOR UPREGULATION OF P53 THROUGH INDUCTION OF MDM2 DEGRADATION

Absstract of: US20260257987A1

0000 Anthraquinone analogs that have anticancer properties are disclosed. Pharmaceutical formulations in forms suitable for the delivery of the compounds to a subject in need thereof are disclosed. Methods of using the compounds for treating or ameliorating one or more symptoms associated with a cancer, such as leukemia, in a subject are also disclosed. The methods include (i) administering to the subject the pharmaceutical formulation containing one or more compounds, for one or more times. The compounds can induce apoptosis in cancer cells, such as leukemia cells harboring WT-p53 (e.g., EU-1 leukemia cells), MCF7 cells, RS4;11 cells, and/or HeLa cells, by downregulating MDM2 and upregulating p53 in these cancer cells.

CD74 CAR-T THERAPY AND METHODS OF USE THEREOF

Absstract of: US20260256912A1

0000 The present disclosure provides for a chimeric antigen receptor (CAR) polypeptide comprising a CD74 antigen binding domain, a transmembrane domain, an intracellular signaling domain, and a co-stimulatory signaling region. Further provided herein is an isolated nucleic acid encoding the recombinant polypeptide as disclosed herein, a vector comprising the isolated nucleic acid, and a cell comprising the vector. Also provided herein is a method of treating lymphoma in a subject in need thereof, the method comprising administering to the subject a therapeutically effective amount of the chimeric antigen receptor polypeptide as disclosed herein. Further described herein is a method of reducing tumor activity in a subject with lymphoma, the method comprising administering to the subject a therapeutically effective amount of the chimeric antigen receptor polypeptide as described herein.

USE OF HYPOXIA-INDUCIBLE FACTOR-PROLYL HYDROXYLASE INHIBITOR (HIF-PHI) IN RARE ANEMIA

Absstract of: EP4799642A1

0001 The present application relates to use of a hypoxia-inducible factor-prolyl hydroxylase inhibitors (HIF-PHI) in rare anemia. Specifically disclosed in the present application is use of certain hypoxia-inducible factor-prolyl hydroxylase inhibitors (HIF-PHIs) in the treatment of anemia of myelodysplastic syndromes (MDS anemia), beta-thalassemia (β-thalassemia), and/or sickle cell disease (sickle cell anemia, SCD anemia).

SUPPRESSING THE PI3KGAMMA/AKT SIGNALLING PATHWAY FOR THE TREATMENT OF ACUTE MYELOID LEUKEMIA

Absstract of: WO2025087879A2

Dose-limiting toxicity poses a major limitation to the clinical utility of targeted cancer therapies, often arising from target engagement in non-malignant tissues. This obstacle can be minimized by targeting cancer dependencies driven by proteins with tissue- and/or tumor-restricted expression. Here, the inventors show that in acute myeloid leukemia (AML), suppression of the myeloid-restricted PIK3CG/p110γ-PIK3R5/p101 axis blocks AKT signaling, compromises cell fitness, and sensitizes to established AML therapies. Importantly, the inventors find that existing small molecule inhibitors against PIK3CG are insufficient to achieve a sustained longterm anti-leukemic effect. To address this concern, the inventors developed a proteolysis- targeting chimera (PROTAC) heterobifunctional molecule that specifically degrades PIK3CG and potently suppresses AML progression alone and in combination with venetoclax in human AML cell lines, primary AML patient samples, and syngeneic mouse models.

METTL3 INHIBITOR

Absstract of: EP4800016A1

The present invention discloses a METTL3 inhibitor represented by general formula (I), its pharmaceutical composition, preparation method, and the use thereof in the preparation of drugs, prevention and/or treatment of drugs for indications associated with METTL3. The compound of the present invention is an ideal high-activity METTL3 inhibitor, which can be used for the treatment and/or prevention of diseases, including AML, myeloid leukemia, solid tumors such as hepatocellular carcinoma, colorectal cancer, and prostate cancer.

Cd22 targeting-moiety for the treatment of b-cell acute lymphoblastic leukemia (b-all)

Absstract of: NZ792974A

The present invention provides therapeutics for the treatment of CD22-positive cancers such as B-cell acute lymphoblastic leukemia (B-ALL). In particular, the present invention provides an anti-CD22 monoclonal antibody whose scFv as a part of chimeric antigen receptors (CAR) T-cells can target the first Ig extracellular domain of the CD22 antigen, the farthest domain from the membrane, for use in the treatment of CD22-positive cancers.

Treatment paradigm for an anti-cd19 antibody and venetoclax combination treatment

Absstract of: NZ758315A

The present disclosure provides a combination of anti-CD19 antibody (MOR00208) and BCL-2 inhibitor (venetoclax) for use in the treatment of non-Hodgkin’s lymphoma, chronic lymphocytic leukemia and/or small lymphocytic lymphoma. Said treatment includes administration of the anti-CD19 antibody, MOR00208, at least 7 days prior to the first administration of venetoclax to patients suffering non-Hodgkin’s lymphoma (NHL), chronic lymphocytic leukemia (CLL) and/or small lymphocytic lymphoma (SLL) to mitigate therapy associated tumor lysis syndrome.

INHIBITION OF APELIN SIGNALING TO TREAT ACUTE MYELOID LEUKEMIA

Absstract of: WO2026178316A1

Disclosed herein are methods of inhibiting apelin, including but not limited to blocking the apelin ligand and/or the apelin receptors and/or signaling thereof, to prevent or reduce endothelial cell clonal expansion and transcriptional remodeling which promotes hematopoietic disorder progression, including but not limited to acute myeloid leukemia (AML).

TREATMENT OF MYELOID DISORDERS AND ACUTE LEUKEMIAS TARGETING NOVEL TUMOR SPECIFIC ANTIGENS

Absstract of: US20260250409A1

0000 The present disclosure relates to a method of diagnosing or treating myeloid disorders and acute leukemias by using a tumor specific antigen selected from CD63, CD151, CD72, CD84, CD69, and CD109. Further provided are an antigen binding protein (ABP), an ABP-drug conjugate, and a CAR targeting the tumor specific antigen, and methods for their use.

Pharmaceutical formulations of Bruton's tyrosine kinase inhibitor

Absstract of: AU2026214088A1

#48183531_1 PHARMACEUTICAL FORMULATIONS OF BRUTON'S TYROSINE KINASE INHIBITOR Abstract Described herein are pharmaceutical formulations of Bruton's tyrosine kinase (Btk) inhibitor I-((R)-3-(4-amino-3-(4-phenoxyphenyl)-IH-pyrazolo 3,4-dpyrimidin- l-yl)piperidin-l-yl)prop-2-en-I-one. Also disclosed are methods of using the Btk inhibitor, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions. PHARMACEUTICAL FORMULATIONS OF BRUTON'S TYROSINE KINASE INHIBITOR Abstract Formulation A Formulation B Mean Ibrutinib Plasma Concentration (ng/mL) Formulation C Formulation D 0 6 12 18 24 Nominal Time Post-Dose (h) ug ' u g b s t r a c t o r m u l a t i o n o r m u l a t i o n Mean Ibrutinib Plasma Concentration (ng/mL)

A Vaccine Composition of Cells Expressing a Lentiviral Vector and Methods of Using

Absstract of: US20260250717A1

0000 A vector construct is described that is a lentiviral construct including DNA encoding for GM-CSF. A vaccine composition is also described that is includes K562 cells transfected with this vector construct, and also possibly including the U266 and H929. Methods are described for using the vaccine composition in methods of immunizing against plasma cell disorders, including multiple myeloma and related disorders.

Substituted straight chain spiro derivatives

Absstract of: AU2026205213A1

The present invention relates to pharmaceutical agents useful for therapy and/or prophylaxis in 5 a mammal, pharmaceutical composition comprising such compounds, and their use as menin/MLL protein/protein interaction inhibitors, useful for treating diseases such as cancer, including but not limited to leukemia, myelodysplastic syndrome (MDS), and myeloproliferative neoplasms (MPN); and diabetes. ul u l

TREATMENT OF HEMATOLOGICAL MALIGNANCIES WITH ANTIBODIES INHIBITING GALECTIN-9

Absstract of: US20260250394A1

0000 Disclosed herein are methods for treating a hematologic malignancy (e.g., acute myeloid leukemia (AML), myelodysplastic syndromes (MDS), or acute lymphoblastic leukemia (ALL)), using an anti-Galectin-9 antibody (e.g., G9.2-17(IgG4). In some embodiments, the anti-Galectin-9 antibody is used as a monotherapy.

METHOD AND DRUG FOR TREATING CANCER BY JOINT USE OF NKG2D CHIMERIC ANTIGEN RECEPTOR AND PD1 INHIBITOR

Absstract of: US20260248853A1

0000 The present disclosure provides a novel chimeric antigen receptor and a combination thereof with a PD1 inhibitor. Further provided are expression vectors and host cells expressing the chimeric antigen receptor and the composition of said receptor with the PD1 inhibitor. Further provided are uses of the chimeric antigen receptor and the composition of said receptor with the PD1 inhibitor in treating cancer or preparing a drug for treating cancer. The drug and the method provided by the present invention can effectively treat cancer, particularly myeloma and solid tumors.

Compounds

Absstract of: GB2704114A

A compound of formula (I), or a pharmaceutically acceptable salt or hydrate thereof, is provided, wherein X-Y is -NHSO₂-. A is selected from C₄-C₈ cycloalkyl, bicyclic C₅-C₁₂ cycloalkyl, or a C₄-C₈ cycloalkyl fused to an aryl or heteroaryl group, each optionally substituted by one or more R₄ groups. R₁ is haloalkyl or OR₃; R₂ is H or halo; R₃ is alkyl or benzyl; and each R₄ is independently alkyl or halo. B is an azetidine group substituted by (R₅)ₘ, wherein R₅ is independently selected from COOH, (CR₁ₐR1b)ₐNR₆R₇, alkyl, haloalkyl, halo, alkoxy, hydroxyalkyl, cycloalkyl, heteroaryl or heterocycloalkyl, optionally substituted. R1a and R1b are independently H, OH, alkyl or hydroxyalkyl; a is 0-3; R₆ and R₇ are independently H, alkyl, SO-alkyl, haloalkyl or heterocycloalkyl; and m is 0-6. The compounds modulate ERAP2 and are useful in treating proliferative, viral, immune or inflammatory disorders, particularly cancer or leukaemia. The compounds stimulate a neo-antigen directed immune response. Methods of producing antigen-presenting cells and immunogenic compositions comprising such cells are also disclosed. Exemplified compounds include N-(2-(cyclohexylamino)-4-fluoro-5-(trifluoromethyl)phenyl)-3-(pyridin-4-yl)azetidine-1-sulfonamide. Formula (I)

Compounds

Absstract of: GB2704145A

A compound of formula (I), or a pharmaceutically acceptable salt or hydrate thereof, is provided, wherein R groups are as defined herein, X-Y is -NHSO2-, A is selected from: a C4-C8-cycloalkyl group; a bicyclic C5-C12-cycloalkyl group; and a C4-C8-cycloalkyl group fused to an aryl or heteroaryl group; each of which is optionally substituted by one or more R4 groups; B is a fused bicyclic group selected from the hetero groups as defined herein, the group is further substituted by zero or more R5 groups; each R5 is independently selected from COOH, CONR8R9, CONHSO2R10, SO2R35, NR36R37, alkyl, OH, halo, haloalkyl, alkoxy, and hydroxyalkyl. The compounds modulate ERAP2 and are useful in treating proliferative, viral, immune or inflammatory disorders, particularly cancer or leukaemia. The compounds stimulate a neo-antigen directed immune response. Methods of producing antigen-presenting cells and immunogenic compositions are also disclosed. Exemplified compounds include N-(2-(cyclohexylamino)-4-fluoro-5-(trifluoromethyl)phenyl)-5,6-dihydro-1,2,4triazolo1,5-apyrazine-7(8H)-sulfonamide No figure

Compounds

Absstract of: GB2704162A

A compound of formula (I), or a pharmaceutically acceptable salt or hydrate thereof, is provided, wherein R groups are as defined herein, X-Y is -NHSO2-, A is selected from: a C4-C8-cycloalkyl group; a bicyclic C5-C12-cycloalkyl group; and a C4-C8-cycloalkyl group fused to an aryl or heteroaryl group; each of which is optionally substituted by one or more R4 groups; R1 is haloalkyl or OR3; R2 is H or halo; R3 is alkyl or benzyl; and each R4 is independently alkyl or halo. B is NR6R7, wherein R6 and R7, together with the nitrogen to which they are attached, form a heterocycloalkyl group, wherein said heterocycloalkyl group is fused to at least one saturated cyclic group to form a fused polycyclic group wherein one or more carbons in the fused polycyclic group is optionally replaced by a group indepependetly selected from NR10, CO, N, O, S, SO and SO2, and is optionally further substituted by one or more R5 groups; each R5 is independently selected from NR8R9, OH, alkyl, halo, haloalkyl, alkoxy, and hydroxyalkyl. The compounds modulate ERAP2 and are useful in treating proliferative, viral, immune or inflammatory disorders, particularly cancer or leukaemia. The compounds stimulate a neo-antigen directed immune response. Methods of producing antigen-presenting cells and immunogenic compositions are also disclosed. Exemplified compounds include N-(2-(cyclohexylamino)-4-fluoro-5-(trifluoromethyl)phenyl)-2-methyl-3-oxooctahydropyrrolo3,4-cpyridine-5-sulfonamide. No Figure

Compounds

Absstract of: GB2704209A

A compound of formula (I), or a pharmaceutically acceptable salt or hydrate thereof, is provided, wherein R groups are as defined herein, X-Y is -NHSO2- or -SO2NH; A is selected from: a C4-C8-cycloalkyl group; a bicyclic C5-C12-cycloalkyl group; and a C4-C8-cycloalkyl group fused to an aryl or heteroaryl group; each of which is optionally substituted by one or more R4 groups; R1 is haloalkyl or OR3; R2 is H or halo; R3 is alkyl or benzyl; and each R4 is independently alkyl or halo. R5 is selected from CO2H, CONHSO2R10, CONR11R12 and tetrazolyl. R6 and R7 are independently H, alkoxy or halo. R8 is selected from halo, alkoxy, haloalkoxy, alkyl, haloalkyl, (CH2)k-cycloalkyl, hydroxyalkyl, CN, OH, SOR9, SO2R9 and heteroaryl. R9 is alkyl, R10 is alkyl, cycloalkyl, aryl or heteroaryl optionally substituted, R11 is H or alkyl, R12 is H, CN, alkyl or CONH2, and k is 0, 1, 2 or 3. The compounds modulate ERAP2 and are useful in treating proliferative, viral, immune or inflammatory disorders, particularly cancer or leukaemia. The compounds stimulate a neo-antigen directed immune response. Methods of producing antigen-presenting cells and immunogenic compositions are also disclosed. Exemplified compounds include 3-(N-(2-(cyclobutylamino)-5-(trifluoromethyl)phenyl)sulfamoyl)-4-methylbenzoic acid. No Figure

Compounds

Absstract of: GB2704197A

A compound of formula (I), or a pharmaceutically acceptable salt or hydrate thereof, is provided, wherein X-Y is -NHSO2-, A is selected from: a C4-C8-cycloalkyl group; a bicyclic C5-C12-cycloalkyl group; and a C4-C8-cycloalkyl group fused to an aryl or heteroaryl group; each of which is optionally substituted by one or more R4 groups; B is NR6R7, wherein R6 and R7 together with the nitrogen to which they are attached form a 5 to 7-membered heterocycloalkyl group optionally containing one or more further groups selected from S, SO and SO2, optionally wherein two non-adjacent carbons in the heterocycloalkyl group are linked by a one or two carbon alkylene bridge, and wherein the said hetrocycloalkyl group is substituted by one or more R5 groups, and is optionally further substituted by one or more R35 groups; R5 is selected from (CR1aR1b)aCOOH, CONR8R9, CONHSO2R10, SO(N=H)-R10 and tetrazolyl. Rxx groups are as defined herein. The compounds modulate ERAP2 and are useful in treating proliferative, viral, immune or inflammatory disorders, particularly cancer or leukaemia. The compounds stimulate a neo-antigen directed immune response. Methods of producing antigen-presenting cells and immunogenic compositions are also disclosed. Exemplified compounds include (S)-1-(N-(2-(cyclohexylamino)-5-(trifluoromethyl)phenyl)sulfamoyl)piperidine-3-carboxylic acid. Formula (I)

Compounds

Absstract of: GB2704195A

A compound of formula (I), or a pharmaceutically acceptable salt or hydrate thereof, is provided, wherein X-Y is -NHSO2-, A is selected from: a C4-C8-cycloalkyl group; a bicyclic C5-C12-cycloalkyl group; and a C4-C8-cycloalkyl group fused to an aryl or heteroaryl group; each of which is optionally substituted by one or more R4 groups; B is NR6R7, wherein R6 and R7 together with the nitrogen to which they are attached form a 5-, 6- or 7-membered heterocycloalkyl group that is substituted by one or more R5 groups, and is optionally further substituted by one or more R13 groups, optionally wherein two non-adjacent carbons in the heterocycloalkyl group are linked by a one or two carbon alkylene bridge; each R5 is independently selected from (CR1aR1b)aNR8R9, OR10, NR8CO2R11 and NR8COR12. The compounds modulate ERAP2 and are useful in treating proliferative, viral, immune or inflammatory disorders, particularly cancer or leukaemia. The compounds stimulate a neo-antigen directed immune response. Methods of producing antigen-presenting cells and immunogenic compositions are also disclosed. Exemplified compounds include (R)(N-(2-(cyclohexylamino)-4-fluoro-5-(trifluoromethyl)phenyl)-3-hydroxypiperidine-1-sulfonamide Formula (I)

Compounds

Absstract of: GB2704140A

A compound of formula (I), or a pharmaceutically acceptable salt or hydrate thereof, is provided, wherein X-Y is -NHSO2-, v is 1 or 2; A is selected from C4-C8-cycloalkyl, fused or bridged bicyclic C6-C12- cycloalkyl, or C4-C8-cycloalkyl fused to an aryl or heteroaryl group, each optionally substituted by one or more R4 groups. R1 is haloalkyl or OR3; R2 is H or halo; R3 is alkyl or benzyl; and each R4 is independently alkyl or halo. R5a is selected from COOH, CONR8R9, CONHSO2R10 and heteroaryl; R5b is H, alkyl or halo. R6a and R6b are each independently H or alkyl, or together form a CO group with the carbon atom to which they are attached. R7a and R7b are each independently H or alkyl, may together form a cycloalkyl group, or R7a is H and R7b and R5b together form a 1- or 2-carbon alkylene bridge. The compounds modulate ERAP2 and are useful in treating proliferative, viral, immune or inflammatory disorders, particularly cancer or leukaemia. Methods of producing antigen-presenting cells and immunogenic compositions are also disclosed. Exemplified compounds include (R)-4-(N-(2-(cyclohexylamino)-5-(trifluoromethyl)phenyl)sulfamoyl)morpholine-2-carboxylic acid Formula (I)

Compounds

Absstract of: GB2704272A

A compound of formula (I), or a pharmaceutically acceptable salt or hydrate thereof, is provided, wherein X-Y is -NHSO2-, A is selected from: a C4-C8-cycloalkyl group; a bicyclic C5-C12-cycloalkyl group; and a C4-C8-cycloalkyl group fused to an aryl or heteroaryl group; each of which is optionally substituted by one or more R4 groups; B is NR6R7, wherein R6 and R7 together with the nitrogen to which they are attached form a 5 to 8-membered heterocycloalkyl group containing at least one further group selected from NR38, CO, SO2 and SONH, optionally wherein two non-adjacent carbons in the heterocycloalkyl group are linked by a one or two carbon alkylene bridge or an ether bridge, and wherein the said hetrocycloalkyl group is optionally substituted by one or more groups selected from R5 and R35, R5 is selected from COOH, CONR8R9, CONHSO2R10, tetrazolyl and hydroxyalkyl; R38 is selected from H, alkyl and CO-alkyl. The compounds modulate ERAP2 and are useful in treating proliferative, viral, immune or inflammatory disorders, particularly cancer or leukaemia. The compounds stimulate a neo-antigen directed immune response. Methods of producing antigen-presenting cells and immunogenic compositions are also disclosed. Exemplified compounds include 4-(N-(2-(cyclohexylamino)-5-(trifluoromethyl)phenyl)sulfamoyl)-1-methylpiperazine-2-carboxylic acid Formula (I)

Bispecific anti-CD28 x anti-CD22 antibodies and uses thereof

Absstract of: AU2026210818A1

The present invention provides bispecific antigen-binding molecules comprising a first antigen-binding domain that specifically binds human CD28, and a second antigen- binding molecule that specifically binds human CD-22. In certain embodiments, the bispecific antigen- binding molecules of the present invention are capable of inhibiting the growth of tumors expressing CD-22, such as B-cell lymphomas. The antibodies and bispecific antigen-binding molecules of the invention are useful for the treatment of diseases and disorders in which an up-regulated or induced targeted immune response is desired and/or therapeutically beneficial. ul u l

DENOSUMAB FORMULATION

Absstract of: US20260242496A1

0000 An aqueous pharmaceutical formulation having improved stability includes denosumab and a poloxamer, and preferably a histidine buffer and/or sugar or sugar alcohol. The formulation is for use in treating or preventing osteoporosis, loss of bone mass, skeletal-related events associated with multiple myeloma, solid tumor bone metastases, giant cell tumors of the bone or hypercalcemia.

USE OF ANTI-CD20 ANTIBODY DRUG CONJUGATE IN PREPARATION OF DRUG FOR TREATING NON-HODGKIN LYMPHOMA

Nº publicación: US20260241027A1 20/08/2026

Applicant:

ZHEJIANG TERUISI PHARMACEUTICAL INC [CN]
ZHEJIANG TERUISI PHARMACEUTICAL INC.

Absstract of: US20260241027A1

0000 The present disclosure discloses a use of anti-CD20 ADC in the preparation of a drug for treating NHL, and the drug has excellent clinical efficacy and safety in treating a R/R NHL patient after receiving at least two standard treatments.