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4-(hetero)aryl-7-(hetero)aryl-2-methyl-5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-carboxylic acid derivatives as coronin-1 modulators

Resumen de: AU2025251398A1

The present invention relates to immunosuppressive compounds that deplete coronin 1 levels, in particular to coronin 1 promoter inhibitors. Accordingly, the present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt, stereoisomer, diastereoisomer, enantiomer, polymorph, racemic mixture, or solvate thereof. The compound of formula (I) can be used as a medicament, in particular for inhibiting coronin 1 expression in the induction of immunosuppression or in the treatment and/or prevention of a disease or disorder selected from the group consisting of transplant rejection, autoimmune diseases, inflammatory diseases, infectious diseases, and lymphoproliferative disorders. The present invention further relates to a pharmaceutical composition comprising the compound of the present invention and a pharmaceutically acceptable carrier.

NEW 5H-PYRROLO3,2-B:5,4-C'DIPYRIDINE DERIVATIVES AND 6,7,8,9-TETRAHYDRO-5H-PYRROLO3,2-B:5,4-C'DIPYRIDINE USEFUL IN THE TREATMENT OF CANCER

Resumen de: US20260315461A1

0000 The present invention relates to a compound of formula (I), or any of its pharmaceutically acceptable salt: 0000 0000 wherein R<1 >represents a halogen atom, a (C<1>-C<6>)alkyl group, a (C<3>-C<6>)cycloalkyl group, a (C<2>-C<6>)alkenyl group, a (C<1>-C<6>)alkoxy group or a (C<3>-C<6>)cycloalkoxy group, X and Y independently represent a —CH═ group, a —CR<3>═ group or a —N═ group, Z1 and Z2 independently represent a —CH<2>— group, a ═CH— group or a ═N— group and R<3 >and R<4 >independently represent a hydrogen atom or a halogen atom. 0000 It further relates to such a compound for its use as a medicament, and in particular for its use in treating and/or prevention of cancer, in particular cancer exhibiting recruitment of MDM2 to chromatin, more particularly selected from the group consisting of bone cancer, brain cancer, ovary cancer, breast cancer, lung cancer, colorectal cancer, osteosarcoma, skin cancer, blood cancer, including acute myeloid leukemia, pancreatic cancer, prostate cancer and liposarcoma and even more particularly selected from the group consisting of skin cancer, blood cancer, for example but not limited to acute myeloid leukemia, melanoma and liposarcoma.

USE OF ANTI-CD38 ANTIBODY IN THE TREATMENT OF NEW DIAGNOSED MULTIPLE MYELOMA

Resumen de: WO2025122791A1

Provided herein are methods and uses for treating multiple myeloma (such as Newly Diagnosed Multiple Myeloma) in a patient in need thereof. The methods comprise administering to the patient an anti-CD38 antibody, bortezomib, lenalidomide, and dexamethasone.

MULTISPECIFIC-ANTIBODY COMPOSITION, PREPARATION METHOD THEREFOR, AND USE THEREOF

Resumen de: EP4821484A1

0001 The present disclosure relates to a composition, which can be a lyophilization preparation liquid or a lyophilized powder preparation. The composition comprises a multispecific antibody, a surfactant, a buffer system, and a stabilizer/a osmotic pressure regulator. Further disclosed are a preparation method and use of the composition, for example use in the treatment of a tumor, in particular multiple myeloma.

THERAPY FOR THE TREATMENT OF MULTIPLE MYELOMA

Resumen de: WO2025120113A1

Provided herein are methods of treating and/or managing multiple myeloma, which comprise administering to a patient 3-(4-((4-(morpholinomethyl)benzyl)oxy)-1-oxoisoindolin-2-yl)piperidine-2,6-dione ("Compound A"), or an enantiomer or a mixture of enantiomers, a tautomer, an isotopolog, a pharmaceutically acceptable salt, solvate, hydrate, co-crystal, clathrate, or polymorph thereof, in combination with a bispecific antibody comprising a first binding part binding to B cell maturation antigen (BCMA) and a second binding part binding to cluster of differentiation 3 (CD3).

METHODS OF TREATING ACUTE MYELOID LEUKEMIA USING COMBINATIONS OF GCN2 MODULATORS, VENETOCLAX, AND AZACITIDINE

Resumen de: WO2025122985A1

Provided herein are methods of treating acute myeloid leukemia (AML) in a subject in need thereof, comprising administering to the subject combinations of Compound 1, or a pharmaceutically acceptable salt thereof, venetoclax, and 5-azacitidine. Also provided herein are methods of inhibiting/overcoming resistance of AML to venetoclax in a subject in need thereof, and/or improving the efficacy of venetoclax in the treatment of AML in a subject in need thereof, comprising administering to the subject combinations of Compound 1, or a pharmaceutically acceptable salt thereof, venetoclax, and 5-azacitidine.

PROLIFERATING CELL NUCLEAR ANTIGEN INHIBITOR, AND PREPARATION METHOD THEREFOR, INTERMEDIATE THEREOF, PHARMACEUTICAL COMPOSITION THEREOF AND USE THEREOF

Resumen de: EP4821917A1

0001 A compound represented by formula (I) as a PCNA inhibitor, or a pharmaceutically acceptable salt thereof, or a deuterated compound thereof, a preparation method therefor, an intermediate compound thereof, a pharmaceutical composition thereof and the use thereof. The PCNA inhibitor and the pharmaceutical composition comprising same can be used for treating cancers, comprising lung cancer, melanoma, colon cancer, rectal cancer, prostate cancer, ovarian cancer, leukemia, etc with PCNA overexpression.

NK CELL COMPOSITIONS AND PREPARATIONS FOR IMMUNOTHERAPY AND METHODS FOR THEIR PRODUCTION

Resumen de: US20260308226A1

The present invention provides NK cell compositions and/or preparations and methods of using such NK cell compositions and/or preparations for immunotherapy. The NK cell compositions and/or preparations can be used in therapies of a broad range of viral infections, bacterial infections, cancer and leukemia malignancies, and other diseases.

BICYCLIC INHIBITORS OF CBX CHROMODOMAINS

Resumen de: US20260308130A1

0000 A genus of bicyclic inhibitors of CBX chromodomains is disclosed. The compounds are of the following genus: 0000 0000 The compounds inhibit CBX proteins and, as a consequence, they are useful for treating prostate cancer, ovarian cancer, and B-cell lymphoma.

SULFUR-CONTAINING ISOINDOLINE DERIVATIVE, AND PREPARATION METHOD THEREFOR AND MEDICAL USE THEREOF

Resumen de: US20260308148A1

The present application relates to a sulfur-containing isoindoline derivative, and a preparation method therefor and medical use thereof. In particular, the present disclosure relates to a sulfur-containing isoindoline derivative as represented by general formula (I), a preparation method therefor, a pharmaceutical composition containing the derivative, and use thereof as a therapeutic agent, particularly use thereof as a Cereblon modulator in the field of treatment of multiple myeloma.

CRENOLANIB FOR TREATING FLT3 MUTATED PROLIFERATIVE DISORDERS ASSOCIATED MUTATIONS

Resumen de: US20260308696A1

The present invention includes methods for treating a human patient with Crenolanib, wherein the human patient is suffering from a FLT3 mutated leukemia, the method comprising: determining that the human patient has a poor prognosis by: obtaining or having obtained a leukemia biological sample and performing or having performed a genotyping assay on the biological sample to determine that the human patient has both a mutated FLT3 or a constitutively active FLT3 mutant and one or more driver mutations in one or more epigenetic regulator proteins that results in a loss of normal function of the epigenetic regulator proteins which, indicates that the patient has a poor prognosis; and administering to the patient determined to have the poor prognosis a therapeutically effective amount of Crenolanib, or a pharmaceutically acceptable salt thereof having the formula:to treat the leukemia.

Epigenetic Signature of T Cell Aging and Malignancy

Resumen de: US20260308690A1

0000 A 139-gene epigenetic signature for use in. methods for assessing the age and longevity of a T cell, selecting a T cell for a T cell therapy, and/or determining a T-cell acute lymphoblastic leukemia subtype is provided.

REVERSE TRANSCRIPTASE WITH IMPROVED PROPERTIES

Resumen de: US20260308541A1

0000 The present invention relates to reverse transcriptase enzymes comprising a modified Moloney Murine Leukaemia Virus reverse transcriptase amino acid sequence, wherein said amino acid sequence comprises a mutation compared to the wild-type Moloney Murine Leukaemia Virus reverse transcriptase, and said enzyme possesses increased inhibitor resistance compared to the wild-type Moloney Murine Leukaemia Virus reverse transcriptase. The present invention also relates to compositions, reaction mixtures, and kits comprising the said reverse transcriptase enzymes are used to synthesize cDNA from RNA.

COMBINATION THERAPY WITH CLK/DYRK INHIBITORS AND BCL2 INHIBITORS TO TREAT LEUKEMIA

Resumen de: US20260306486A1

The present disclosure provides methods for treating leukemia (e.g., AML) using a CLK/DYRK inhibitor and a B-cell lymphoma 2 (BCL2) inhibitor (e.g., venetoclax). Kits for use in practicing the methods are also provided.

BCMA-TARGETED CAR-T CELL THERAPY FOR MULTIPLE MYELOMA

Resumen de: AU2025235980A1

Provided herein are methods of treating a subject who has multiple myeloma and has received one to three prior treatment(s). Infusions of chimeric antigen receptor (CAR)-T cells comprising a CAR capable of specifically binding to an epitope of BCMA are administered to the subject.

GENOMIC PROFILING OF CELLS TO MONITOR MINIMUM RESIDUAL DISEASE

Resumen de: US20260311880A1

0000 Disclosed are methods of monitoring minimum residual disease using genomic profiling. In some methods, a subject has or has had multiple myeloma or a precursor thereof. The methods include amplifying a sample using primary template-directed whole genome amplification (PTWGA) and enable monitoring of liquid samples, such as blood samples.

METHODS AND KITS FOR DIAGNOSING B-CELL LYMPHOMAS OF THE CENTRAL NERVOUS SYSTEM

Resumen de: WO2026210100A1

The invention relates to a method for the in vitro diagnosis of a B-cell lymphoma of the central nervous system, comprising analysing the methylation status of at least one, in particular of at least two, more particularly of at least three, preferably of at least four, more preferably of the five CpG motifs of the LRP5 (Low-density lipoprotein receptor-related protein 5) gene present in the circulating free DNA derived from at least one cerebrospinal fluid sample. The invention also relates to a method for monitoring the response to an anti-cancer treatment and to kits associated with the method for in vitro diagnosis.

PIPERIDINYL-METHYL-PURINEAMINE NSD2 INHIBITOR THERAPEUTIC METHODS AND COMPOSITIONS FOR TREATING CANCER

Resumen de: WO2026213527A1

The present invention provides methods and compositions for using a piperidinyl-methylpurineamine nuclear SET domain- containing protein 2 (NSD2) inhibitor to treat light chain myeloma in subjects with reduced activity of the TP53 gene or elevated expression of NSD2 due to a medical defect other than a t(4; 14) translocation.

TERTIARY AMINE COMPOUNDS CONTAINING AN ALKYNE OR AN AZIDE MOIETY AND THEIR USE

Resumen de: US20260308116A1

0000 Tertiary amine compounds that have an alkyne group or an azide group, in particular an alkyne group, and/or their pharmaceutically acceptable salts and solvates that are useful to monitor DNA lesions and to reveal interstrand crosslinks repair defects are disclosed herein. Methods of monitoring DNA lesions in patients selected from Fanconi Anemia (FA) patients, xeroderma pigmentosum (XP) patients, acute myeloid leukemia (AML) patients, head-and-neck cancer patients, ovarian cancer patients, and breast cancer patients using the tertiary amine compounds and/or their pharmaceutically acceptable salts and solvates are also disclosed.

INHIBITORS OF HRI KINASE FOR TREATMENT OF DISEASE

Resumen de: WO2026213197A1

The present invention relates to lH-pyrazolo3,4-bpyridine compounds and methods useful as inhibitors of HRI kinase for the treatment or prevention of hematological disorders The invention includes a method of treating myelodysplastic syndrome in patients who are non-responders to luspatercept or elythropoiesis-stimulating agents comprising the administration, to a patient in need thereof, of a HRI kinase inhibitor.

SMALL MOLECULE ALLOSTERIC INHIBITORS OF IMPDH1/2

Resumen de: WO2026213556A1

The present disclosure is concerned with pharmaceutical compositions comprising an inosine-5' -monophosphate dehydrogenase 2 (IMPDH2) inhibitor and methods of treating cancer (e.g., a sarcoma, a carcinoma, a hematological cancer, a solid tumor, breast cancer, cervical cancer, gastrointestinal cancer, colorectal cancer, brain cancer, skin cancer, prostate cancer, ovarian cancer, non-small cell lung carcinoma, thyroid cancer, testicular cancer, pancreatic cancer, liver cancer, endometrial cancer, melanoma, glioma, leukemia, lymphoma, chronic myeloproliferative disorder, myelodysplastic syndrome, myeloproliferative neoplasm, and plasma cell neoplasm (myeloma). This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

USE OF A MEDICAMENT SIMULTANEOUSLY TARGETING THE TYROSINE KINASE ACTIVITY AND GEF ACTIVITY OF EGFR

Resumen de: EP4817602A1

The present invention provides an EGFR inhibitor for use in the preparation of a medicament for treating diseases mediated by guanosine exchange factor (GEF) activity or co-mediated by guanosine nucleotide exchange factor (GEF) activity and EGFR tyrosine kinase activity, wherein the diseases are selected from the group consisting of: lung cancer, colon cancer, breast cancer, endometrial cancer, thyroid cancer, glioma, squamous cell carcinoma, prostate cancer, melanoma, leukemia, and glioblastoma. Specifically, the present invention has discovered that in addition to its conventional tyrosine kinase activity, EGFR also possesses a GEF function that promotes the activation of Ras homologous protein (Rheb), this function is independent of its tyrosine kinase activity and relies critically on the glutamate residue at position 804 on the EGFR molecule. The Rheb-GEF activity of EGFR induces allosteric activation of mammalian target of rapamycin complex 1 (mTORC1), ultimately promoting tumor growth.

Chimeric protein

Resumen de: GB2705211A

A chimeric protein comprising a first peptide linked to a second peptide. The second peptide includes an epitope. The second peptide is formed from C-terminal and N-terminal segments of a target peptide comprising the epitope. The relative positions of the C-terminal segment and the N-terminal segment are transposed in the second peptide relative to the target peptide. The epitope can be formed from both first and second segments of the second peptide. The second peptide can be IL-31, IL-6, IL-11, ciliary neurotrophic factor (CNTF), leukemia inhibitory factor (LIF), oncostatin M (OSM), cardiotrophin 1 (CT-1), cardiotrophin-like cytokine (CLC), or IL-27. The second peptide can be human or canine IL-31. The first peptide can be a bacterial colicin, bacterial ribonuclease, spycatcher protein, ColE7, or Barnase. A further aspect is a virus-like particle comprising the chimeric protein. A further aspect is a polynucleotide capable of hybridizing the polynucleotide. A further aspect is a method of producing the chimeric protein wherein the target peptide is split at a division site without disrupting formation of secondary structure elements. A further aspect is an immunogenic composition comprising the chimeric protein for use in treating atopic dermatitis, cancer, inflammatory, neurodegenerative, metabolic, cardiovascular, renal, gastrointestinal, respiratory, autoimmune diseases. Figure 6

Chimeric protein

Resumen de: GB2705174A

A chimeric protein comprising a first peptide and first and second segments of a second peptide. The second peptide includes an epitope. The N-terminus of the first peptide is linked to either the first or the second segment of the second peptide. The C-terminus of the first peptide is linked to the other of the first or second segment of the second peptide. The epitope can be formed from both segments of the second peptide. The second peptide can be IL-31, IL-6, IL-11, ciliary neurotrophic factor (CNTF), leukemia inhibitory factor (LIF), oncostatin M (OSM), cardiotrophin 1 (CT-1), cardiotrophin-like cytokine (CLC), or IL-27. The second peptide can be human or canine IL-31. The first peptide can be a bacterial colicin, bacterial ribonuclease, spycatcher protein, ColE7, or Barnase. The second peptide can be divided into the first and second segments at a division site from an unstructured region or a glycine residue. A further aspect is a virus-like particle comprising the chimeric protein. A further aspect is a polynucleotide capable of hybridizing the polynucleotide. A further aspect is an immunogenic composition comprising the chimeric protein for use in treating atopic dermatitis, cancer, inflammatory, neurodegenerative, metabolic, cardiovascular, renal, gastrointestinal, respiratory, autoimmune diseases. Figure 5

METHODS, BIOMARKERS, AND KITS FOR DETECTION OF MULTIPLE MYELOMA

Nº publicación: EP4818333A1 07/10/2026

Solicitante:

UNIV HEIDELBERG [DE]
Universit\u00E4t Heidelberg
Universit\u00E4tsklinikum Heidelberg

Resumen de: EP4818333A1

The present invention relates to an in vitro method for detecting multiple myeloma in a subject. The invention further provides the use of chemokine receptor CXCR3 (CXCR3) as a biomarker for diagnosing, prognosing, and/or treatment monitoring of multiple myeloma in a subject. The invention further provides a kit for the detection of multiple myeloma in a subject.