A61K31/4025

COMPOUNDS FOR USE IN THE TREATMENT OF ACUTE INTERMITTENT PORPHYRIA

The invention provides compounds of formula (I), their pharmaceutically acceptable salts and prodrugs thereof for use in preventing, inhibiting or treating a disease caused by a mutation in the gene coding for hydroxymethylbilane synthase, in particular for preventing, inhibiting or treating acute intermittent porphyria: (I) wherein: A is selected from N and CR.sup.10 (wherein R.sup.10 is H, —NO.sub.2, C.sub.1-6 haloalkyl or —C(O)R.sup.17 in which R.sup.17 is H or C.sub.1-6 alkyl); Z is selected from N and CR.sup.9 (wherein R.sup.9 is H, halogen (e.g. F, Cl, Br or I) or —OR.sup.16 in which R.sup.16 is H, C.sub.1-6 haloalkyl, or optionally substituted C.sub.1-6 alkyl); L is selected from —CH.sub.2—, —C(O)—, —CH(OH)—, —C(O)—NR′—, and —NR′—C(O)— (wherein R′ is H or C.sub.1-3 alkyl, e.g. —CH.sub.3); R.sup.1 is H; R.sup.2 is selected from H, halogen (e.g. F, Cl, Br or I), —NR.sup.11R.sup.12 (wherein R.sup.11 and R.sup.12 are independently selected from H and C.sub.1-6 alkyl or, together with the nitrogen atom to which they are attached, form a 5- or 6-membered saturated ring), and —OR13 (wherein R.sup.13 is H or C.sub.1-6 alkyl); R.sup.3 is selected from H, —CH.sup.2OH and —C(O)R.sup.14 (wherein R.sup.14 is H or C.sub.1-6 alkyl); R.sup.4 is selected from H, halogen (e.g. F, Cl, Br or I) and —OR.sup.15 (where R.sup.15 is H or C.sub.1-6 alkyl); R.sup.5 is selected from H and C.sub.1-6 alkyl; R.sup.6 is selected from H, —NO.sub.2 and halogen (e.g. F, Cl, Br or I); R.sup.7 is H; and R.sup.8 is selected from H, C.sub.1-6 alkyl, and halogen (e.g. F, Cl, Br or I); or wherein: R.sup.7 and R.sup.8 together with the intervening ring carbon atoms form an unsaturated ring, preferably an aryl ring.

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5-membered heteroaryl carboxamide compounds for treatment of HBV

The present disclosure provides, in part, 5-membered heteroaryl carboxamide compounds, and pharmaceutical compositions thereof, useful for disruption of HBV core protein assembly, and methods of treating Hepatitis B (HBV) infection.

METHODS AND FORMULATIONS FOR TREATING AND PREVENTING LONG HAUL CORONAVIRUS (LONG COVID) SYMPTOMS AND SEQUELAE

Methods and formulations for treating and preventing LONG COVID sequelae are provided. An example method treats loss of smell and taste from SARS-CoV-2 infection, including assessing the patient, administering a composition with dosage between 1750-3600 mg per day, wherein the composition comprises a mixture of at least a withanolide-A, a boswellic acid, a [6]-gingerol, and a curcuminoid. Another example method treats memory loss or brain fog from SARS-CoV-2 infection, including assessing the patient, and administering a regenerative and neuroprotective composition comprising a mixture of withanoside VI, withanolide A, a Boswellia serrata plant, a Zingiber officinale rhizome, and a Curcuma longa rhizome. The compositions were found effective, achieving statistical significance in a multi-center, randomized, double-blind, placebo-controlled phase III clinical trial.

METHODS AND FORMULATIONS FOR TREATING AND PREVENTING LONG HAUL CORONAVIRUS (LONG COVID) SYMPTOMS AND SEQUELAE

Methods and formulations for treating and preventing LONG COVID sequelae are provided. An example method treats loss of smell and taste from SARS-CoV-2 infection, including assessing the patient, administering a composition with dosage between 1750-3600 mg per day, wherein the composition comprises a mixture of at least a withanolide-A, a boswellic acid, a [6]-gingerol, and a curcuminoid. Another example method treats memory loss or brain fog from SARS-CoV-2 infection, including assessing the patient, and administering a regenerative and neuroprotective composition comprising a mixture of withanoside VI, withanolide A, a Boswellia serrata plant, a Zingiber officinale rhizome, and a Curcuma longa rhizome. The compositions were found effective, achieving statistical significance in a multi-center, randomized, double-blind, placebo-controlled phase III clinical trial.

1-AMINOSULFONYL-2-CARBOXYPYRROLE DERIVATIVES AS METALLO-BETA-LACTAMASE INHIBITORS

This invention relates to compounds of formula (I) and methods of treatment using the compounds. The compounds of the invention can be used in combination with antibacterial agents to treat bacterial infections. More specifically, the compounds of formula (I) can be used in combination with a class of antibacterial agents known as carbapenems. The novel compounds of the present invention are enzyme inhibitors and more particularly are metallo-β-lactamase inhibitors.

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1-AMINOSULFONYL-2-CARBOXYPYRROLE DERIVATIVES AS METALLO-BETA-LACTAMASE INHIBITORS

This invention relates to compounds of formula (I) and methods of treatment using the compounds. The compounds of the invention can be used in combination with antibacterial agents to treat bacterial infections. More specifically, the compounds of formula (I) can be used in combination with a class of antibacterial agents known as carbapenems. The novel compounds of the present invention are enzyme inhibitors and more particularly are metallo-β-lactamase inhibitors.

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ARYL-ANILINE AND HETEROARYL-ANILINE COMPOUNDS FOR TREATMENT OF BIRTHMARKS
20230013227 · 2023-01-19 ·

Provided herein are compounds and pharmaceutical compositions thereof for treating a birthmark in a subject in need thereof, wherein the compound is according to any one of formula (I), (II), (III), (IV), and (V). wherein, X.sup.1, X.sup.2, X.sup.3, R.sup.1, R.sup.2, R.sup.2a, R.sup.13, R.sup.13a, R.sup.23, R.sup.23a, R.sup.23b, R.sup.33, R.sup.33a, R.sup.33b, R.sup.43, R.sup.43a, R.sup.51, R.sup.53, R.sup.53a, R.sup.53b, bond “a”, and subscript n are described herein.

ARYL-ANILINE AND HETEROARYL-ANILINE COMPOUNDS FOR TREATMENT OF BIRTHMARKS
20230013227 · 2023-01-19 ·

Provided herein are compounds and pharmaceutical compositions thereof for treating a birthmark in a subject in need thereof, wherein the compound is according to any one of formula (I), (II), (III), (IV), and (V). wherein, X.sup.1, X.sup.2, X.sup.3, R.sup.1, R.sup.2, R.sup.2a, R.sup.13, R.sup.13a, R.sup.23, R.sup.23a, R.sup.23b, R.sup.33, R.sup.33a, R.sup.33b, R.sup.43, R.sup.43a, R.sup.51, R.sup.53, R.sup.53a, R.sup.53b, bond “a”, and subscript n are described herein.

INHALED STATINS AS BRONCHODILATORS TO IMPROVE LUNG FUNCTION IN RESPIRATORY DISEASES
20230014352 · 2023-01-19 ·

present disclosure relates to methods for relaxing airway smooth muscle tissue, alleviating or preventing bronchospasm, and treating lung diseases by administering an HMG-CoA reductase inhibitor (statin) directly to lung tissue by inhalation. The disclosure also relates to formulations and compositions useful for the practice of methods of the disclosure.

INHALED STATINS AS BRONCHODILATORS TO IMPROVE LUNG FUNCTION IN RESPIRATORY DISEASES
20230014352 · 2023-01-19 ·

present disclosure relates to methods for relaxing airway smooth muscle tissue, alleviating or preventing bronchospasm, and treating lung diseases by administering an HMG-CoA reductase inhibitor (statin) directly to lung tissue by inhalation. The disclosure also relates to formulations and compositions useful for the practice of methods of the disclosure.