C07C279/12

ARGININE GINGIPAIN INHIBITORS

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.

ARGININE GINGIPAIN INHIBITORS

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.

Compounds and compositions for intracellular delivery of therapeutic agents
11220476 · 2022-01-11 · ·

The disclosure features novel lipids and compositions involving the same. Nanoparticle compositions include a novel lipid as well as additional lipids such as phospholipids, structural lipids, and PEG lipids. Nanoparticle compositions further including therapeutic and/or prophylactics such as RNA are useful in the delivery of therapeutic and/or prophylactics to mammalian cells or organs to, for example, regulate polypeptide, protein, or gene expression.

Compounds and compositions for intracellular delivery of therapeutic agents
11220476 · 2022-01-11 · ·

The disclosure features novel lipids and compositions involving the same. Nanoparticle compositions include a novel lipid as well as additional lipids such as phospholipids, structural lipids, and PEG lipids. Nanoparticle compositions further including therapeutic and/or prophylactics such as RNA are useful in the delivery of therapeutic and/or prophylactics to mammalian cells or organs to, for example, regulate polypeptide, protein, or gene expression.

RENEWABLE POLYMERS AND RESINS AND METHODS OF MAKING THE SAME

The present disclosure relates to methods for producing polymers and resins, the method including a first reacting of at least a first diamine with a first carbonate-containing compound and a second carbonate-containing compound to produce at least one of the polymer or the resin, where the first reacting is according to

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each of R.sub.1, R.sub.2, R.sub.3, and R.sub.4 include at least one of a hydrogen atom, a methyl group, a saturated hydrocarbon chain, and/or an unsaturated hydrocarbon chain, and R comprises at least one of a carbon atom, a saturated hydrocarbon chain, and/or an unsaturated hydrocarbon chain.

RENEWABLE POLYMERS AND RESINS AND METHODS OF MAKING THE SAME

The present disclosure relates to methods for producing polymers and resins, the method including a first reacting of at least a first diamine with a first carbonate-containing compound and a second carbonate-containing compound to produce at least one of the polymer or the resin, where the first reacting is according to

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each of R.sub.1, R.sub.2, R.sub.3, and R.sub.4 include at least one of a hydrogen atom, a methyl group, a saturated hydrocarbon chain, and/or an unsaturated hydrocarbon chain, and R comprises at least one of a carbon atom, a saturated hydrocarbon chain, and/or an unsaturated hydrocarbon chain.

NOVEL P62 LIGAND COMPOUND, AND COMPOSITION FOR PREVENTING, AMELIORATING OR TREATING PROTEINOPATHIES COMPRING THE SAME

The present invention relates to a novel p62 ligand compound, a stereoisomer, hydrate, solvate or prodrug thereof, and a pharmaceutical or food composition for preventing or treating proteinopathies comprising the same as an active ingredient. The p62 ligand compound according to the present invention can be usefully used as a pharmaceutical composition for the prevention, amelioration or treatment of various proteinopathies by activating autophagy in cells and thus selectively eliminating in vivo proteins, organelles and aggregates.

CRYSTALLINE L-ARGININE SALT OF (R)-2-(7-(4-CYCLOPENTYL-3- (TRIFLUOROMETHYL)BENZYLOXY)-1,2,3, 4-TETRAHYDROCYCLO-PENTA [B]INDOL-3-YL)ACETIC ACID(COMPOUND1) FOR USE IN SIPI RECEPTOR-ASSOCIATED DISORDERS

The present invention relates to, inter alia, a novel crystalline free-plate habit or morphology, processes for preparing the crystalline free-plate habit, and uses of the crystalline free-plate habit of the L-arginine salt of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclo-penta[b]indol-3-yl)acetic acid (Compound 1) in the treatment of S1P.sub.1 receptor-associated disorders, for example, diseases and disorders mediated by lymphocytes, transplant rejection, autoimmune diseases and disorders, inflammatory diseases and disorders (e.g., acute and chronic inflammatory conditions), cancer, and conditions characterized by an underlying defect in the vascular integrity or that are associated with angiogenesis such as may be pathologic (e.g., as may occur in inflammation, tumor development, and atherosclerosis).

CRYSTALLINE L-ARGININE SALT OF (R)-2-(7-(4-CYCLOPENTYL-3- (TRIFLUOROMETHYL)BENZYLOXY)-1,2,3, 4-TETRAHYDROCYCLO-PENTA [B]INDOL-3-YL)ACETIC ACID(COMPOUND1) FOR USE IN SIPI RECEPTOR-ASSOCIATED DISORDERS

The present invention relates to, inter alia, a novel crystalline free-plate habit or morphology, processes for preparing the crystalline free-plate habit, and uses of the crystalline free-plate habit of the L-arginine salt of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclo-penta[b]indol-3-yl)acetic acid (Compound 1) in the treatment of S1P.sub.1 receptor-associated disorders, for example, diseases and disorders mediated by lymphocytes, transplant rejection, autoimmune diseases and disorders, inflammatory diseases and disorders (e.g., acute and chronic inflammatory conditions), cancer, and conditions characterized by an underlying defect in the vascular integrity or that are associated with angiogenesis such as may be pathologic (e.g., as may occur in inflammation, tumor development, and atherosclerosis).

ANALGESIC AND ANTI-ADDICTIVE COMPOSITIONS FOR TREATMENT OF CHRONIC PAIN AND OPIOID ADDICTION

The invention provides a compound of formula I and stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the formula I compounds, as well as methods of using such as therapeutic agents for the treatment of pain-related disorders and diseases and in combination with other therapeutic agents.

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