4 minute read
Jan. 29, 2024

Patent Highlights: NLRP3 and NaV1.8 Inhibitors, SMARCA2 Degraders, and More from December 2023

The Drug Hunter team is piloting a new series highlighting notable disclosures in the patent literature to provide our readers a timely and scientifically flavorful synopsis of therapeutic targets being actively pursued, emerging industry breakthroughs, and fascinating chemical matter. Here we highlight 12 patents published in December 2023 that piqued our interest, and compiled a searchable table comprising key information from more than 180 additional patents of potential interest to drug hunters. If you would like us to keep this new series going or have any suggestions on how to make this more useful, please let us know

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Macrocyclic MCL-1 Inhibitors from AbbVie

A patent application from AbbVie (US2023399340-A1) disclosed MCL-1 protein-protein interaction inhibitors for oncology with in vivo activity in xenografts. ABBV-467 was recently highlighted in Molecules of the Month, but no longer appears in AbbVie's pipeline.

Boron-Warhead JAK Inhibitors from Boehringer Ingelheim/Borah 

Boehringer Ingelheim filed a patent application for reversible-covalent JAK1/2 inhibitors (WO2023244775A1) that showcases a benzo-borane warhead, a core similar to FDA approved JAK2 inhibitor, fedratinib, and a cyanotetrahydro-2H-pyran moiety similar to other JAK inhibitors reported. Example 33a is a potent JAK1 and JAK2 inhibitor (IC50 of 0.4 nM and 8.1 nM, respectively) and induced antipruritic effects in Beagle dog pruritus animal model dosed orally at 1 mg/kg with a t1/2 of 14.6 h.

Ascentage Patents Alrizomadlin Derivatives

Ascentage published a patent (US11850239B2) on MDM2-p53 inhibitors related to their Ph. II clinical candidate alrizomadlin (APG-115). MDM2 is a highly pursued target with multiple candidates currently under investigation, including navtemadlin (Amgen), siremadlin (Novartis), idasanutlin (Roche), ALRN-6924 (Roche), and brigimadlin (Boehringer Ingelheim).

AstraZeneca Discloses FAP Inhibitors as Potential NASH Treatments

AstraZeneca published a patent application (US20230406840A1) for FAP inhibitors as a unique therapeutic strategy to treat NASH. Example 20 displayed a hFAP inhibition IC50 of 0.48 nM and an in vivo mouse IC50 of 3.0 nM. 

Orally Available SMARCA2 Degraders from C4 Therapeutics

A series of SMARCA2 degraders was disclosed by C4 Therapeutics (WO2023244764A1) with example 153 showing a remarkable bioavailability of 72%. SMARCA2 is a vital component of the SWI/SNF chromatin remodeling complex, which is mutated in 20% of human cancers, and recognized as a synthetic lethal target in SMARCA4-deficient tumors.

Potent Troponin Activators Published from Cytokinetics and Astellas 

A patent application detailing a series of troponin activators for the treatment of heart failure and ALS was published by Cytokinetics and Astellas (WO2023245137A1) with example 6 showing potent activation of myofibril cells. Recently, a Ph. III clinical trial for Cytokinetics’ troponin activator reldesemtiv was discontinued due to lack of functional benefit in the treatment of ALS.

Denali Patents New LRRK2 Inhibitors

A patent containing novel LRRK2 inhibitors (US11834439B2) intended for the treatment of Parkinson’s disease was published by Denali. Example 118 was a standout entry with LRRK2 TR-FRET ID50 of 1.55 nM, human liver microsome CLhep of 7.81 mL/min/kg, and MDR1 efflux ratio of 0.83. This comes on the heels of Danali’s clinical LRRK2 inhibitor, DNL 151, being terminated in Ph. III trials

Roche’s NLRP3 Inhibitors are Structurally Distinct from Selnoflast

Roche published a patent application for a series of NLRP3 inhibitors (WO2023232917A1) with example 2 showing THP-1 pyroptosis inhibition IC50 of 2.7 nM and human whole blood IL-1β IC50 of 9.5 nM. The series is structurally distinct from the aniline-containing sulfonylurea core common to other NLRP3 inhibitors, including Roche’s selnoflast in Ph. I clinical trials for Parkinson’s disease.

Macrocyclic STING Antagonists from Roche

Roche disclosed a series of macrocyclic STING antagonists (WO2023237457A1) with example 11 showing a FRET IC50 of 21.4 nM, no hERG activity at 20 μM, and good mouse PK (CL of 11.1 mL/min/kg, Vss of 0.8 L/kg, t1/2 of 1 h, and F of 48%). STING antagonists are still in early stages of development but they are hypothesized to have therapeutic benefit in cancer and autoimmune diseases.

GSK Reports Macrocyclic NaV1.8 Inhibitors

GlaxoSmithkline published a patent application detailing a series of macrocyclic inhibitors of the voltage-gated sodium ion channel NaV1.8 (WO2023238065A1), with example 1 showing a NaV1.8 pIC50 of 5.1. These NaV1.8 inhibitors are intended to treat pain and pain-associated disease, as well as cardiovascular diseases, such as atrial fibrillation.

BMS has a New KRAS(G12C) Warhead Design

Bristol-Myers Squibb published two patent applications detailing a series of KRAS(G12C) inhibitors (WO2023240189A1, WO2023240188A1) that utilize a unique α-fluoro-β-heterocyclic substituted acrylamide warhead. Example 66 from WO2023240188A1 and example 8 from WO2023240189A1 displayed potent activity in a KRAS(G12C) disruption assay with IC50’s of <2 nM and 55 nM, respectively.

Be sure to search the table below to find out what else was disclosed in the patent literature last month!

Patent NumberTarget/MoATherapeutic AreaOriginatorDescription
US-2023399340-A1MCL-1 inhibitorsoncologyAbbviemacrocycles with activity in xenograft models
WO-2023233130-A1CD73 inhibitorsoncologyAdoRx Therapeutics inhibitors with nanomolar potency in cellular assays
WO-2023235880-A1CD38 inhibitorsneurologyAeovian PharmaceuticalsCD38 modulation observed in NAD+ cydase activity assay
US-11845760-B2PRMT5 inhibitorsoncology, hematology, metabolic diseasesAmgenanti-proliferative activity observed in HCT116-MTAP null cell assays
US-2023406860-A1KRAS G12C inhibitorsoncologyAmgenpotent activity in MIA PaCa-2 and A549 cell assays
WO-2023242598-A1ER/AR degradersoncology, cardiology, neurologyAmphista Therapeutics ER and AR degradation observed in cell assays
WO-2023242597-A1bifunctional degraders-Amphista Therapeutics bifunctional non-E3 ligase-based ubiquitin degraders
US-2023399307-A1ALDH-2 inhibitorsneurologyAmygdala Neurosciencesselectivity and potency observed in enzymatic assays
US-2023399299-A1ALDH-2 inhibitorsneurologyAmygdala Neurosciencesselectivity and potency observed in enzymatic assays
WO-2023244574-A1ALDH-2 inhibitorsneurologyAmygdala Neurosciencesselectivity and potency observed in enzymatic assays
WO-2023244584-A1ALDH-2 inhibitorsneurologyAmygdala Neurosciencesselectivity and potency observed in enzymatic assays
WO-2023244563-A1ALDH-2 inhibitorsneurologyAmygdala Neurosciencesselectivity and potency observed in enzymatic assays
US-2023416277-A1AXL inhibitorsoncologyArcus BiosciencesAXL phosphorylation inhibition at nanomolar potency
US-2023406843-A1progranulin modulatorsneurologyArkuda Therapeuticsincrease in progranulin secretion detected in animal models
WO-2023239892-A1CD68 modulatorsoncology, immunologyArkuda TherapeuticsCD68 binding confirmed by photoaffinity labeling using compound 2
US-11851434-B2RET inhibitorsoncologyArray Biopharmapyrazine with nanomolar potency in cells expressing a Kif5b-RET fusion
US-11850239-B2MDM2 inhibitorsoncologyAscentage Pharmaalrizomadlin analogs for the treatment of cancer
US-2023407285-A1PCSK9 inhibitorscardiologyAstrazenecaPCSK9 inhibition through allosteric binding mode
US-2023406840-A1FAP inhibitorshepatology Astrazenecaazabicycles treat NASH with potent FAP engagement in mice
US-2023416249-A1EGFR inhibitorsoncologyBayer, The Broad Institute, Dana-Farber Cancer Instituteactivity observed in cell assays against exon 20 insertion EGFR mutants
US-2023391769-A1CSNK1 inhibitorsoncologyBayer, The Broad Institute, Dana-Farber Cancer Instituteactivity against CSNK1A1 and CSNKD
US-2023405015-A1PDE3 inhibitorsoncologyBayer, The Broad Institute, Dana-Farber Cancer Instituteoxadiazines with oral efficacy noted in murine PDX models
WO-2023235360-A1apelin receptor agonistsneurologyBioAge Labsazelaprag and analog compounds
WO-2023240140-A1FLT3 inhibitorsoncologyBlossomhill Therapeuticsindazole macrocycles with oral efficacy in mouse CDX models
WO-2023240138-A1EGFR inhibitorsoncologyBlossomhill Therapeuticsmacrocycles with inhibitory activity against EGFR mutants
US-2023391780-A1KIT/PDGFRα mutants inhibitorshematologyBlueprint Medicinesoral non-CNS penetrant for systemic mastocytosis
US-2023416232-A1EGFR/HER2 mutants inhibitorsoncologyBlueprint Medicinespyrimidines with inhibitory activity against EGFR/HER2 mutants
US-11840536-B2PTPN11 inhibitorsoncologyThe University Of Texasheterocycles with oral efficacy in xenograft models
WO-2023244775-A1JAK inhibitorsimmunology, oncologyBoehringer Ingelheim, Borahboron containing compounds with anti-pruritic effect in dog models
US-11851418-B2plasma kallikrein inhibitorsimmunologyBoehringer Ingelheimcarboxamide derivatives with PKK activity in biochemical assays
WO-2023237504-A1HSD17B13 inhibitorshepatology Boehringer Ingelheimpotent heteroaryl compounds to treat NASH and NAFLD
US-2023390249-A1LPA1 receptor antagonistsimmunologyBristol-Myers Squibbnanomolar triazoles LPA1 antagonists for fibrotic diseases
WO-2023240189-A1KRAS G12C(ON) inhibitorsoncologyBristol-Myers Squibbcompounds with activity against KRAS- G12C(ON)
WO-2023240188-A1KRAS G12C(ON) inhibitorsoncologyBristol-Myers Squibbcompounds with activity against KRAS- G12C(ON)
US-2023416251-A1cereblon bindersoncologyC4 Therapeuticsspirocyclic compounds with a high affinity for CRBN
WO-2023239750-A1cereblon bindersoncologyC4 Therapeuticsbicyclic-substituted glutarimide CRBN binders
WO-2023244764-A1SMARCA2 degradersoncologyC4 TherapeuticsSMARCA2 degraders with oral bioavailability observed in mice
US-11834452-B2CXCR7 antagonistsoncology, immunologyChemocentryxcompounds with in vivo efficacy in rabbit, rat, and xenografts models
US-2023416233-A1P2X3 inhibitorsrespiratory diseasesChiesi Farmaceuticicompounds with selectivity towards P2X3 over P2X2/4
WO-2023245123-A2IRAK/FLT3 inhibitorsoncologyChildren's Hospital Medical Center, Department of Health and Human Services, Kurome Therapeuticsin vivo efficacy observed in MOLM14-FLT3-ITD(D835Y) xenograft models
US-2023398096-A1ALK inhibitorsoncology, neurologyChugai Seiyaku Kabushiki Kaishatetracyclic compounds for ALK inhibition
US-11834515-B2proteasome inhibitorsinfectious diseases, immunology, neurologyCornell University, Tri-Institutional Therapeutics Discovery Institutemacrocycles with activity against proteasome
WO-2023245137-A1skeletal troponin activatorscardiology, neurologyCytokinetics, Astellas Pharma heterocycles with slow skeletal myofibrils activation properties
US-11834427-B2TNF-α inhibitorsinflammatory diseasesDaiichi Sankyooral griseofulvin derivatives with TNF-α inhibitory activity in mice
US-2023391768-A2JAK2 inhibitorsoncologyDana-Farber Cancer Institutecompounds with cellular efficacy against JAK2 mutants
US-2023406838-A1EGFR inhibitorsoncologyDana-Farber Cancer Institutecompounds with against mEGFR
WO-2023241322-A1POLQ inhibitorsoncologyDanatlas Pharmaceuticalsheterocycles with submicromolar activity in PolQ polymerase assay
US-2023416205-A1NLRP3 inhibitorsinflammatory diseasesDenali Therapeutics compounds exhibiting anti-inflammatory effects in cellular assays
US-11834439-B2LRRK2 inhibitorsneurologyDenali Therapeutics LRRK2 inhibitors featuring CNS pentetration
US-11840529-B2LRRK2 inhibitorsneurologyDenali Therapeutics potent LRRK2 ihnibitors with acitivity in TR-FRET assays
US-11851433-B2RIPK1 inhibitorsneurology, immunologyDenali Therapeutics RIPK1 inhibitors with submicromolar potency in FP binding assays
US-11851440-B2eIF2B modulatorsneurologyDenali Therapeutics compounds with activity in the ATF4 Nano Luciferase reporter assay
WO-2023240084-A2SARM1 inhibitorsneurologyDenali Therapeutics compounds that inhibit FL-SARM1
WO-2023233033-A1PAR-2 inhibitorsoncology, neurology, cardiology, immunologyDomain TherapeuticsPAR-2 inhibitors with activity confirmed using calcium assays
US-11834436-B2ASK-1 inhibitorshepatology Enanta Pharmaceuticalstetrazole ASK-1 inhibitors in HTRF assay for NASH
US-2023416268-A117β-HSD13 inhibitorsmetabolic disease, hepatologyEnanta Pharmaceuticals17β-HSD13 inhibitors with activity observed in RF/MS assays
WO-2023244713-A1KRAS G12D inhibitorsoncologyEnsem Therapeuticsquinazoline KRAS G12D inhibitors in 2D CTG assay
WO-2023244710-A1CDK2 inhibitorsoncologyEnsem Therapeuticsanilino-pyrazole CDK2 inhibitors in cell assay
US-11834455-B2CARM1 inhibitorsoncology, immunology, neurologyEpizymeheteroaryl CARM1 inhibitors in MM cell lines
US-2023416263-A1CARM1 inhibitorsoncology, immunology, neurologyEpizymeheteroaryl CARM1 inhibitors in MM cell lines
US-11845761-B2KRAS G12C inhibitorsoncologyErascaKRAS(G12C) compounds with CNS penetration observed in rats
US-11840521-B2MRGPRX4 antagonistsimmunologyEscient PharmaceuticalsMRGPRX4 modulators with PK observed in mice models
WO-2023192901-A9MRGPRX2 antagonistsimmunology, neurology, oncology Escient PharmaceuticalsMRGPRX2 modulators with PK observed in mice models
WO-2023232917-A1NLRP3 inhibitorsimmunology, oncology, cardiologyRocheNLRP3 inhibition observed in human whole blood
WO-2023232776-A1KRAS G12C/G12D/G12V inhibitorsoncologyRochemacrocycles with activity toward KRAS mutants
WO-2023237457-A1STING antagonistsimmunologyRocheoral macrocyclic STING inhibitors with PK
WO-2023242324-A1ASO progranulin splicing modulatorsneurologyRocheantisense oligonucleotides as progranulin modulators
US-2023406856-A1BTK inhibitorsoncology, immunologyFochonoral BTK inhibitors with antitumor activity and PK observed in dog
WO-2023231777-A1BCL-2 inhibitorsoncology, immunologyFochoninhibitors of BCL-2 mutants cell lines evaluated in proliferation assays
US-2023416248-A1SMARCA2/SMARCA4 inhibitorsoncologyFoghorn Therapeuticstumor regression observed upon oral dosage in xenograft models
WO-2023240253-A2TNF-α inhibitorsimmunologyForward TherapeuticsTNF-α inhibitors in HEK Blue reporter cellular assay
US-11834461-B2RIPK1 inhibitorsoncology, immunologyGenentechbicyclic ketone RIPK1 inhibitors in Transcreener ADP assay
US-2023391766-A1VHL inhibitorshematology, oncologyGenentechcellular VHL engagement in HEK-293 NanoBRET assays
US-2023391747-A1GLP-1R agonistsmetabolic diseasesGilead SciencesGLP-1R activation assessed with cAMP increase in CHO cells
US-11845723-B2DGKα inhibitorsoncology, infectious diseasesGilead SciencesDGKα inhibitors in Jurkat NFκB-Luciferase assays
US-11845755-B2antiviral agentsinfectious diseasesGilead Sciencesnucleoside derivatives with rat and monkey PK
US-11851419-B2GLP-1R agonistsmetabolic diseasesGilead SciencesGLP-1R activation in CHO cells
US-11851438-B2antiviral agentsinfectious diseasesGilead Sciences1′-cyano nucleoside analogs with rat and monkey PK
WO-2023238065-A1NaV1.8 inhibitorsneurology, cardiologyGlaxosmithklinedihydroquinazolinone Nav1.8 inhibitors in cell assays
US-11851425-B2PDE1 inhibitorsneurologyH. Lundbeck A/S1H-pyrazolo[4,3-B]pyridines against PDE1A, PDE1B, and PDE1
US-2023416272-A1LRRK2 inhibitorsneurologyH. Lundbeck A/SCNS-penetrant LRRK2 inhibitors in TR-FRET assays
US-2023391778-A1ENT1 inhibitorsneurology, immunologyRocheindolin-2-one or pyrrolo-pyridin-2-one in cell assays
US-2023391764-A1HBsAg/HBeAg inhibitorsinfectious diseasesRocheHBsAg/HBeAg inhibitors PHH infection assays for HBV
US-11840528-B2GABAA α5 receptor positive allosteric modulatorsneurologyRocheGABAA α5 receptor activity analyzed in Xenopus Oocytes models
US-2023416238-A1HBsAg/HBeAg inhibitorsinfectious diseasesRocheHBsAg/HBeAg inhibitors PHH infection assays for HBV
US-2023404985-A1WNT inhibitorsoncologyIcahn School Of Medicine At Mount Sinaioral efficacy in xenograft models
US-2023391765-A1ENL degradersoncologyIcahn School Of Medicine At Mount Sinai, Van Andel Research InstituteIP efficacy in mice leukemia models
WO-2023233295-A1Polθ inhibitorsoncologyIdeaya Biosciences, Glaxosmithklinethiadiazolyl derivatives CR in xenograft models with niraparib
US-11839613-B2EP2/EP4 receptor antagonistsoncologyIdorsia Pharmaceuticalspyrimidines with EP2/EP4 activity in cell assays
US-11833152-B2JAK1 inhibitorsimmunology, oncologyIncyte Corporationoral efficacy in mouse cytokine release syndrome models
US-11840546-B2ALK2 inhibitorsoncologyIncyte Corporationimidazopyridazine ALK2 inhibitors in HTRF assays
US-2023398225-A1PD-1/PD-L1 PPI inhibitors, STING agonistsoncologyIncyte CorporationPd-l1/sting conjugates in cellular assays
US-2023399342-A1DGKα/DGKξ inhibitorsoncologyIncyte CorporationDGKα and DGKξ selective tricyclic triazolos in kinase assays
US-11851426-B2CDK2 inhibitorsoncologyIncyte Corporationbicyclic amines in CDK2/Cyclin E1 HTRF assays
WO-2023239768-A1DGKα/DGKξ inhibitorsoncologyIncyte CorporationDGKα and DGKξ selective tricyclic triazolos in kinase assays
US-11840534-B2FGFR inhibitorsoncologyIncyte Corporationtricyclic FGFR1, FGFR2, and FGFR3 inhibitors
US-11851442-B2JAK inhibitorsimmunology, oncologyIncyte Corporationtricyclic fused thiophene JAK1/JAK2 inhibitors
US-11834440-B2QPCTL inhibitorsoncology, infectious diseases, neurologyInsilico Medicinebeta-lactam QPCTL inhibitors
WO-2023241627-A1CDK8/19 dual inhibitorsoncologyInsilico Medicinebicyclic dual CDK8/19 kinase inhibitors
WO-2023239954-A1chymase inhibitorshepatology Invea Therapeutics, Ez Bioxcel Solutions7-membered ring chymase inhibitors for hepatobiliary disease
US-11833221-B2DMPK inhibitorsgenetic diseaseIonis Pharmaceuticalsoligomer DMPK inhibitors for myotonic dystrophy
US-2023399297-A1glutamine analogsoncologyJacobio Pharmaceuticalssubcutaneous efficacy in MC38 syngeneic mice models
US-11845808-B2IL-23 receptor inhibitorsimmunologyJanssen, Protagonist Therapeuticspeptides IL-23 inhibitors in SIF/SGF models
US-2023416256-A1NIK inhibitorsoncology, immunology, metabolic disordersJanssenNF-kB inhibitors in L363 cell assay
US-2023391756-A1NLRP3 inhibitorsimmunologyJanssenNLRP3 activity observed in the PBMC assay
US-11845748-B2Factor XIa inhibitorshematology, immunology, oncologyJanssenbicyclic pyridine FXIa inhibitors in FLINT assays
WO-2023237732-A1RSV fusion inhibitors/RSV polymerase inhibitorsinfectious diseasesJanssentriazolo derivatives with antiviral activity for RSV
WO-2023237730-A1RSV fusion inhibitors/RSV polymerase inhibitorsinfectious diseasesJanssentriazolo and spiro derivatives with antiviral activity for RSV
WO-2023232966-A1OX2R agonistsneurologyJazz Pharmaceuticalsmacrocyclic agonists with OX2R activity in IP-1 accumulation assay
US-2023416286-A1MEK inhibitorsoncologyKinnate Biopharmadiphenylamines MEK inhibitors with cell activity
US-11845754-B2CDK9 inhibitorsoncology, infectious diseases, cardiologyKronos Bioinhibitors of CDK9/cyclin T1 as evidenced by LANCE assays
US-2023405008-A1menin inhibitorsoncologyKura Oncologymenin-MLL interaction blockade observed
US-2023398223-A1IRAK degradersoncology, immunologyKymera TherapeuticsIRAK degraders with PK data
US-2023416242-A1IRAK/BTK degradersoncology, immunologyKymera TherapeuticsIRAK4 degraders with activity in OCI-LY10 cells
WO-2023239645-A1SMARCA2/SMARCA4/PB1 degradersoncology, immunologyKymera TherapeuticsSMARCA2/SMARCA4 degraders with activity in MV411 cells
WO-2023242631-A1ENPP-1 inhibitorsoncologyLegochem BiosciencesENPP-1 inhibitors with activity in enzyme assays
US-11833162-B2BCL-2 inhibitorsoncology, immunologyServier, Vernalismacrocyclic activators of caspase 3 observed in xenograft models
WO-2023244657-A1IP6K inhibitorsneurology, metabolic disorderLieber Institute, The Johns Hopkins Universitytricyclic inhibitors with activity against IP6K
US-2023391807-A1antiviral agentsinfectious diseasesLigand Pharmaceuticalsnucleotide prodrugs for viral infection treatment
US-11851431-B2JAK1 inhibitorsoncology, immunologyLynk PharmaceuticalsJAK1 inhibitors with oral/IV PK profiles
US-2023416235-A1JAK inhibitorsoncology, immunologyLynk PharmaceuticalsJAK inhibitors for topical use or GI indications
US-2023391776-A1IRAK4/BTK inhibitorsimmunology, oncologyMedshine Discoveryamide oxazole IRAK4/BTK inhibitors in xenograft models
US-2023416204-A1antifungal agentsinfectious diseasesMedshine Discoveryoral aminopyridine in candidemia mouse models
US-2023416266-A1KRAS G12C inhibitorsoncologyMerckpyrimidines in SOS-catalyzed nucleotide exchange and phospho-ERK cell assays
US-2023391758-A1GCS inhibitorsgenetic diseaseMerckbenzofuran-carboxamides GCSi for lysosomal storage diseases
US-2023391795-A1orexin receptor agonistsneurologyMerckmacrocyclic OX2R agonists with activity in IPOne assay
US-2023399341-A1HPK1 inhibitorsoncologyMerckHPK1 inhibitotrs with activity in TR-FRET assays
US-2023406885-A1IL-1β inhibitorscardiologyMerckcyclic peptides that block IL-1β induced IL-6 secretion
US-2023406844-A1LRRK2 inhibitorsneurologyMerckcompounds with LRRK2 kinase activity
US-2023406864-A1HPK1 inhibitorsoncologyMerckHPK1 inhibotrs with activity in TR-FRET assays
US-2023416225-A1HPK1 inhibitorsoncologyMerckHPK1 inhibotrs with activity in TR-FRET assays
US-2023416227-A1PKK inhibitorsophthalmology, cardiologyMercknanomolar activity in plasma kallikrein assay
WO-2023224894-A4LRRK2 inhibitorsneurology, immunology, oncologyMerckmacrocycle compounds for LRRK2 inhibition
WO-2023244554-A1IL-1β inhibitorscardiologyMerckcyclic peptides that block IL-1β induced IL-6 secretion
WO-2023244604-A1pan KRAS inhibitorsoncologyMirati Therapeuticstetrahydropyridopyrimidine inhiibitors for KRAS mutants
WO-2023244615-A1pan KRAS inhibitorsoncologyMirati Therapeuticsazaquinazoline with activity towards KRAS mutants
WO-2023244599-A1pan KRAS inhibitorsoncologyMirati Therapeuticscompounds with activity towards KRAS mutants
WO-2023244817-A1CK1α degradersoncologyMonte Rosa TherapeuticsCK1α degraders with PK data in mice
WO-2023244815-A1CK1α molecular glue degradersoncologyMonte Rosa TherapeuticsCK1α molecular glue degraders
WO-2023244818-A1CK1α molecular glue degradersoncologyMonte Rosa TherapeuticsCK1α molecular glues with oral PK in mice
WO-2023241608-A1CSF-1R inhibitorsoncology, neurology, immunologyMyrobalan Therapeuticsoral efficacy in microglial depletion mice models
WO-2023240024-A1CDK2 inhibitorsoncologyNikang Therapeuticssulfamide CDK2 inhibitors
US-2023391797-A1TYK2 inhibitorsimmunologyNimbusTYK2 inhibiiors
US-11833142-B2IKZF2 degradersoncologyNovartisdegradation activity observed in cell assays
US-2023391782-A1IL-17 inhibitorsimmunologyNovartisIL-17 inhibitors with activity in cell and TR-FRET assays
US-2023398117-A1BTK degradersoncology, immunologyNovartisBTK degradation observed in vitro cellular assays
US-11845730-B2TRPV1 receptor antagonistsneurologyNovartisTRPV1 antagonism noticed in cell assay
US-2023416211-A1NLRP3 antagonistsimmunology, metabolic diseasesNovartisIL-1β suppression activity in THP-1 assay
US-2023414598-A1CBL inhibitorsoncologyNurix TherapeuticsCBL inhibitors with human PK data disclosed
WO-2023239710-A1PI3K inhibitorsoncologyOnkurecell-based mutant PI3Ka assay and mouse PK
WO-2023242537-A1GPR65 antagonistsimmunology, oncologyPathios Therapeutics GPR65 antagonists with tropane core
US-2023405002-A1DGAT2 and ACC inhibitor combinationshepatology Pfizer DGAT2 and ACC inhibitor combinations to treat NASH
WO-2023239839-A1KCNT1 inhibitorsneurologyPraxis Precision Medicines, Yale Universityisoxazole or oxadiazole core KCNT1 inhibitors
US-2023416240-A1KAT6 degradersoncologyPrelude Therapeutics KAT6 degraders with CRBN ligand
WO-2023244996-A2HTT inhibitorsgenetic diseasePtc Therapeuticscompounds for treating Huntington's disease.
US-2023391772-A1KRAS(G12C) degraderoncologyRanok Therapeutics (Hangzhou)series of KRAS(G12C) degraders
WO-2023240263-A1RAS inhibitors oncologyRevolution Medicinesmacrocyclic RAS inhibitors
WO-2023242810-A1MCHR1 antagonistgenetic disease Richter Gedeon Nyrt.MCHR1 antagonist to treat Prader-Willi Syndrome
US-11851457-B2NMDA modulatorimmunologySage Therapeuticssubstituted oxysterols to treat NMDA-mediated disorders
US-2023391816-A1GABA receptor complex (GRC)neurologySage Therapeuticsneuroactive steroids to treat neuological conditions
US-11844758-B2mutant IDH1/2 inhibitorsoncologyServier Pharmaceuticalsvorasidenib derivatives
WO-2023240267-A2CFTR stabilizersgenetic diseaseSionna Therapeuticsheterocyclic CFTR stabilizers to treat Cystic Fibrosis
US-2023391770-A1METTL3 inhibitorsoncologyStorm Therapeuticsnanomolar METTL3 inhibitors
US-2023399308-A1dual 5-HT1A and D4 agonistneurologySumitomo Pharmadual agonists for serotonin 5-HT1A and dopamine D4 receptors
WO-2023239846-A1PI3Ka modulatorsoncologySynnovation Therapeuticsindazole PI3Ka inhibitors
US-11834449-B2TYK2 inhibitorsimmunology, oncologyTakeda azaindole TYK2 inhibitors
US-11834409-B2NMDA receptor antagonisticneurologyTakeda compounds with antagonistic activity against NMDA
US-2023391773-A1pKal inhibitorsgenetic diseaseTakedapKaI inhibitors to treat hereditary angioedema (HAE)
US-11851449-B2RORγt inhibitorsimmunologyTakeda RORγt inhibitors to prevent differentiation of Th17 cells
WO-2023239925-A1cyclophilin inhibitorsneurology, oncology, cardiologyThe Broad Institute, President And Fellows of Harvard Collegemacrocyclic cyclophilin inhibitors
US-11840523-B2IRE1α inhibitorsoncologyThe Regents of The University Of California, University of Washingtonheterocycles for inhibiting IRE1α
WO-2023235719-A2SARM1 inhibitorsneurologyThe Scripps Research Instituteseelctive and covalent SARM2 inhibitors
US-2023390404-A1BCL-XL degradersoncologyTreeline BiosciencesCRBN ligand BCL-XL degraders
WO-2023240038-A1BCL6 degradersoncologyTreeline BiosciencesCRBN ligand BCL6 degraders
WO-2023244917-A1BCL6 degradersoncologyTreeline BiosciencesCRBN ligand BCL6 degraders
WO-2023244918-A1BCL6 degradersoncologyTreeline BiosciencesCRBN ligand BCL6 degraders
US-2023406849-A1KRAS inhibitorsoncologyTyligand Bioscience (Shanghai) covalent KRAS inhibitors
US-2023399328-A1IL-17 modulatorsimmunologyUCB Biopharma SRLdicyclopropylmethyl derivatives as IL-17 modulators
US-2023406830-A1HDAC8 inhibitorsonocologyValo Healthspirocyclic HDAC8 inhibitors
US-2023414585-A1HDAC8 inhibitorsonocologyValo Healthspirocyclic indanes as HDAC8 inhibitors
WO-2023239789-A1PARP inhibitorsonocologyValo HealthCNS-penetrant tricyclic phthalazinone PARP inhibitors
US-11851406-B2positive allosteric modulators of mAChR M1neurologyVanderbilt Universitypositive allosteric modulators of mAChR M2
US-11834441-B2NaVs inhibitorsneurologyVertex Pharmaceuticals substituted tetrahydrofurans as NaVs inhibitors
US-2023416275-A1CFTR modulatorgenetic diseaseVertex Pharmaceuticals macrocyclic CFTR modulator
WO-2023239729-A1potassium channel allosteric modulatorsneurologyXenon Pharmaceuticals voltage-gated potassium channel allosteric modulators
US-11845751-B2A2A receptor antagonistsoncologyZhejiang Vimgreen Pharmaceuticalstriazolotriazines as A2A receptor antagonists
WO-2023237116-A1GSPT1 degraderoncologyZhuhai Yufan Biotechnologieslenalidomide derived GSPT1 degraders

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