Abstract

Therapeutics targeting the bacterium Porphyromonas gingivalis, including its proteases arginine gingipain A and arginine gingipain B, are disclosed, as well as the use thereof for the treatment of disorders associated with P. gingivalis infection, including brain disorders such as Alzheimer's disease. In certain embodiments, the invention provides compounds according to Formula I, Formula Ia, and Formula Ib, as described herein, and pharmaceutically acceptable salts thereof.

IPC Classes  ?

• C07D 239/34 - One oxygen atom
• C07C 279/28 - Derivatives of guanidine, i.e. compounds containing the group the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to cyano groups, e.g. cyanoguanidines, dicyandiamides
• C07C 279/24 - Y being a hetero atom
• C07C 279/12 - Derivatives of guanidine, i.e. compounds containing the group the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to acyclic carbon atoms of a carbon skeleton being further substituted by nitrogen atoms not being part of nitro or nitroso groups
• C07D 213/68 - One oxygen atom attached in position 4
• C07D 213/82 - AmidesImides in position 3
• C07D 261/12 - Oxygen atoms

Abstract

Compounds and methods for the treatment of coronavirus infections are disclosed. Compounds according to Formula I as described herein, containing reactive functional groups for covalent binding to active site residues in target proteases, can be used for treating infection by SARS-CoV-2 and other coronaviruses.

IPC Classes  ?

• A61K 31/7056 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom
• A61K 31/706 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom

Abstract

Methods for detecting microbial nucleic acids in a body fluid of a subject are provided. The methods include highly sensitive and specific procedures for detecting DNA derived from the bacteria such as Porphyromonas gingivalis, e.g., using PCR amplification and qPCR detection, in clinical and/or laboratory samples containing CSF or other biofluids.

IPC Classes  ?

• C12Q 1/689 - Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for detection or identification of organisms for bacteria
• C12Q 1/686 - Polymerase chain reaction [PCR]

Abstract

Porphyromonas gingivalisP. gingivalisP. gingivalis infection, including brain disorders such as Alzheimer's disease. In certain embodiments, the invention provides compounds according to Formula I, Formula Ia, and Formula Ib, as described herein, and pharmaceutically acceptable salts thereof.

IPC Classes  ?

• A61P 31/04 - Antibacterial agents
• C07C 279/12 - Derivatives of guanidine, i.e. compounds containing the group the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to acyclic carbon atoms of a carbon skeleton being further substituted by nitrogen atoms not being part of nitro or nitroso groups
• C07D 277/64 - Benzothiazoles with only hydrocarbon or substituted hydrocarbon radicals attached in position 2

Abstract

Porphyromonas gingivalis, e.g.Porphyromonas gingivalis, e.g., using PCR amplification and qPCR detection, in clinical and/or laboratory samples containing CSF or other biofluids.

IPC Classes  ?

• C12Q 1/68 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving nucleic acids
• C12P 19/34 - Polynucleotides, e.g. nucleic acids, oligoribonucleotides

Goods & Services

Pharmaceutical preparations for the treatment and prevention of Alzheimer's, brain disorders, neurological disorders, arthritis, infectious diseases, autoimmune diseases, inflammatory diseases, genetic diseases, diabetes, cardiovascular diseases, cancers, and other types of diseases and disorders; biological preparations for the treatment and prevention of Alzheimer's, brain disorders, neurological disorders, arthritis, infectious diseases, autoimmune diseases, inflammatory diseases, genetic diseases, diabetes, cardiovascular diseases, cancers, and other types of diseases and disorders; medicinal preparations for the treatment and prevention of Alzheimer's, brain disorders, neurological disorders, arthritis, infectious diseases, autoimmune diseases, inflammatory diseases, genetic diseases, diabetes, cardiovascular diseases, cancers, and other types of diseases and disorders. Medical research; medical research services in the fields of Alzheimer's, brain disorders, neurological disorders, arthritis, infectious diseases, autoimmune diseases, inflammatory diseases, genetic diseases, diabetes, cardiovascular diseases, cancers, and other types of diseases and disorders; conducting clinical trials for others in the fields of Alzheimer's, brain disorders, neurological disorders, arthritis, infectious diseases, autoimmune diseases, inflammatory diseases, genetic diseases, diabetes, cardiovascular diseases, cancers, and other types of diseases and disorders; medical and scientific study and research; pharmaceutical research and development; pharmaceutical and biological research, testing, and product development consultation.

Abstract

The present invention relates generally to therapeutics targeting the bacterium Porphyromonas gingivalis, including its proteases arginine gingipain A/B (Rgp), and their use for the treatment of disorders associated with P. gingivalis infection, including brain disorders such as Alzheimer's disease. In certain embodiments, the invention provides compounds according to Formula I and Formula III, as described herein, and pharmaceutically acceptable salts thereof.

IPC Classes  ?

• A61K 31/44 - Non-condensed pyridinesHydrogenated derivatives thereof
• C07D 213/72 - Nitrogen atoms
• C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links

Abstract

The present invention provides compounds according to Formula (I) as described herein, and their use for inhibiting the lysine gingipain protease (Kgp) from the bacterium Porphyromonas gingivalis. Also described are gingipain activity probe compounds and methods for assaying gingipain activity are also described, as well as methods for the treatment of disorders associated with P. gingivalis infection, including brain disorders such as Alzheimer's disease.

IPC Classes  ?

• C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 277/64 - Benzothiazoles with only hydrocarbon or substituted hydrocarbon radicals attached in position 2

Abstract

The invention provides methods for treating or preventing osteoarthritis. The method includes administering a therapeutically effective amount of one or more gingipain-blocking agents to a patient in need thereof. In certain embodiments, the gingipain blocking agent is a Kgp inhibitor, an RgpA inhibitor, an RgpB inhibitor, a bacteriocidal agent, a bacteriostatic agent, a gingipain-specific antibody, a vaccine, or a combination thereof.

IPC Classes  ?

• C07K 14/195 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from bacteria

Abstract

The present invention relates generally to therapeutics targeting the bacterium Porphyromonas gingivalis, including its proteases arginine gingipain A/B (Rgp), and their use for the treatment of disorders associated with P. gingivalis infection, including brain disorders such as Alzheimer's disease. In certain embodiments, the invention provides compounds according to Formula I, as described herein, and pharmaceutically acceptable salts thereof.

IPC Classes  ?

• C07D 277/64 - Benzothiazoles with only hydrocarbon or substituted hydrocarbon radicals attached in position 2
• C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

Abstract

The present invention relates generally to therapeutics targeting the bacterium Porphyromonas gingivalis, including its protease Lysine gingipain (Kgp), and their use for the treatment of disorders associated with P. gingivalis infection, including brain disorders such as Alzheimers disease. In certain embodiments, the invention provides compounds according to Formula (I), as described herein, and pharmaceutically acceptable salts thereof.

IPC Classes  ?

• C07C 233/62 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups