Researchers from Janssen Pharmaceutica NV have reported the discovery of novel hepatitis B virus (HBV) capsid assembly modulators (CAMs) as potential therapeutic candidates against HBV infection. Synthesis and optimization of a new series of di-fluoro azepane HBV CAMs resulted in the identification of compound [I] as the lead candidate with DNA EC50 value of 8.5 nM when assessed in the HepG2.2.15 cellular assay.
Janssen Pharmaceutica NV has divulged pyrazolopyrimidines acting as spermine oxidase (polyamine oxidase 1; SMOX) inhibitors reported to be useful for the treatment of colorectal cancer.
Protease form factor Xia (FXIa) is a therapeutic target for thrombosis prevention due to its well-known contribution to VTE and ischemic stroke in humans. Researchers from Janssen Pharmaceutica NV presented an antithrombotic target FXIa inhibitor obtained through a non-classical interactions strategy to improve the pharmacokinetic and pharmacological activity for the treatment of thrombosis. In the series, the potency was increased by using water-mediated hydrogen bonds to reduce polar hydrogen bond donors and using methyl to displace high-energy waters.
Nanobiotix SA has landed Johnson & Johnson Inc. subsidiary Janssen Pharmaceutica NV as commercialization partner for NBTXR-3, a radioenhancer for boosting the effectiveness of standard radiotherapy, in a deal worth up to $1.86 billion for the initial indications. That headline figure covers current programs in head and neck cancers and lung cancers. There is the potential for Nanobiotix to earn up to $650 million more if Janssen decides to pursue up to five new indications that it will select, while for new indications that Nanobiotix selects to develop in alignment with Janssen, Nanobiotix will receive up to $220 million per program.
Janssen Pharmaceutica NV has identified bicyclic pyridin-2-one and pyrimidin-4-one derivatives acting as coagulation factor XIa inhibitors and thus reported to be useful for the treatment of thromboembolism, diabetes, diabetic retinopathy, septic shock, hereditary angioedema, arthritis, nephropathy and inflammatory disorders, among others.
Janssen Pharmaceutica NV has divulged macrocyclic compounds acting as induced myeloid leukemia cell differentiation protein Mcl-1 inhibitors reported to be useful for the treatment of cancer.
Janssen Pharmaceutica NV has disclosed IL-17A/IL-17 receptor A (IL-17RA) interaction modulators reported to be useful for the treatment of psoriasis, rheumatoid arthritis, radiographic axial spondyloarthritis (ankylosing spondylitis), multiple sclerosis, asthma and more.
Pipeline Therapeutics Inc., which received U.S. FDA approval to move into a phase Ib/IIa study of PIPE-307 in relapsing-remitting multiple sclerosis (RRMS) last year, will be advancing the oral, small-molecule muscarinic M1 receptor antagonist in collaboration with Janssen Pharmaceutica NV in an agreement that could be worth more than $1 billion.
Janssen Pharmaceutica NV has disclosed 5-oxo-1,2,3,5,8,8a-hexahydroindolizine-3-carboxamide derivatives acting as coagulation factor XIa and plasma kallikrein (KLKB1) inhibitors reported to be useful for the treatment of thromboembolism, diabetes, diabetic retinopathy, septic shock, hereditary angioedema, arthritis, nephropathy and inflammatory disorders, among others.
