The methods disclosed herein relate to methods of orally administering norketotifen to human subjects. Oral norketotifen can be administered with food to reduce nausea and vomiting in the human subject. Oral norketotifen can be coadministered with additional medications such as dupilumab or crisaborole, or it can be administered after discontinuation of dupilumab or crisaborole.
A61K 31/4535 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
A61K 9/00 - Medicinal preparations characterised by special physical form
Described herein are methods of treating human and canine patients suffering from dermal Cytokine Storm syndromes related to dermal diseases such as atopic dermatitis, psoriasis or urticaria. A method of reducing the incidence and/or the intensity of a symptom of dermal hypercytokinemia in a patient suffering from an underlying dermal condition who develops the dermal hypercytokinemia as a consequence of the underlying dermal condition includes administering to the patient a therapeutically effective amount of norketotifen an isomer, an isomeric mixture, a prodrug or a pharmaceutically acceptable salt thereof. The symptom of dermal hypercytokinemia is an eruption of new dermal lesions accompanied by intense lesional and / or non-lesional pruritus.
A61K 31/4535 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
Methods of treating a patient suffering from a TNFα associated arthritic disorder with the cytokine release inhibitor norketotifen include orally or topically administering to the subject in need thereof a therapeutically effective amount of norketotifen, an isomeric mixture, a prodrug, or a pharmaceutically acceptable salt thereof. Also included are methods of intra-articular injection of norketotifen, such as into a joint of a subject in need thereof.
A61K 31/4535 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
Described herein are methods of administering the non-steroidal anti-inflammatory drug norketotifen, an isomer, an isomeric mixture, a prodrug, or a pharmaceutically acceptable salt thereof for the treatment of a respirator}'- disorders such as CQPD and asthma to human patient in need of such treatment, without exposing said patient to adverse immune·· suppressive effects. Methods include treating acute and potentially life-threatening exacerbations of COPD and asthma with norketotifen.
A61K 31/445 - Non-condensed piperidines, e.g. piperocaine
A61K 31/4535 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
Described herein are methods of administering the non-steroidal anti-inflammatory drug norketotifen, an isomer, an isomeric mixture, a prodrug, or a pharmaceutically acceptable salt thereof for the treatment of a respirator}'- disorders such as CQPD and asthma to human patient in need of such treatment, without exposing said patient to adverse immune·· suppressive effects. Methods include treating acute and potentially life-threatening exacerbations of COPD and asthma with norketotifen.
A61K 31/445 - Non-condensed piperidines, e.g. piperocaine
A61K 31/4535 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
Described herein are methods of administering the non-steroidal anti-inflammatory drug norketotifen, an isomer, an isomeric mixture, a prodrug, or a pharmaceutically acceptable salt thereof for the treatment of a respiratory disorders such as COPD and asthma to human patient in need of such treatment, without exposing said patient to adverse immune-suppressive effects. Methods include treating acute and potentially life-threatening exacerbations of COPD and asthma with norketotifen.
Described herein are methods of administering the non-steroidal anti-inflammatory drug norketotifen, an isomer, an isomeric mixture, a prodrug, or a pharmaceutically acceptable salt thereof for the treatment of a respiratory disorders such as COPD and asthma to human patient in need of such treatment, without exposing said patient to adverse immune-suppressive effects. Methods include treating acute and potentially life-threatening exacerbations of COPD and asthma with norketotifen.
Described herein are methods of administering the anti-inflammatory drug norketotifen, an isomer, a prodrug, or a pharmaceutically acceptable salt thereof for the treatment of a respiratory disorder such as asthma and COPD in a human patient in need of such treatment, without exposing said patient to adverse immune-suppression. Dosage regimens for oral administration including a loading dosage followed by a maintenance dosage are described. Also described are methods and conditions wherein norketotifen is administered by oral inhalation. Yet, further included are methods of administering norketotifen directly to the nasal passages of the human patients in need thereof, in order to reduce or eliminate inflammatory symptoms of airways disorders, such as sinusitis, laryngitis, nasopharyngitis and various forms of rhinitis.
A61K 9/72 - Medicinal preparations characterised by special physical form for smoking or inhaling
A61K 31/4535 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
A61P 11/00 - Drugs for disorders of the respiratory system
Described herein are methods of administering the anti-inflammatory drug norketotifen, an isomer, a prodrug, or a pharmaceutically acceptable salt thereof for the treatment of a respiratory disorder such as asthma and COPD in a human patient in need of such treatment, without exposing said patient to adverse immune-suppression. Dosage regimens for oral administration including a loading dosage followed by a maintenance dosage are described. Also described are methods and conditions wherein norketotifen is administered by oral inhalation. Yet, further included are methods of administering norketotifen directly to the nasal passages of the human patients in need thereof, in order to reduce or eliminate inflammatory symptoms of airways disorders, such as sinusitis, laryngitis, nasopharyngitis and various forms of rhinitis.
Disclosed herein are methods of treating a mammal in need of a reduction in intraocular pressure by administering an intraocular formulation including a therapeutically effective amount of norketotifen for the reduction of intraocular pressure to the eye of the mammal in need thereof, wherein the intraocular formulation includes about 0.02 wt % to about 1.0 wt % norketotifen or a salt or an isomer thereof, calculated as the norketotifen free base. In certain aspects, the intraocular formulation is free from any added preservative and the intraocular formulation is self-preserving. Also included herein is a method of treating a human in need of a reduction in intraocular pressure by administering an intranasal formulation that includes a therapeutically effective amount of norketotifen for the reduction of intraocular pressure to the eye of the human in need thereof. Also, the beneficial effects of known drugs for high IOP are improved by co-administration with norketotifen.
A61K 31/445 - Non-condensed piperidines, e.g. piperocaine
A61K 31/4535 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
Disclosed herein are methods of treating a mammal in need of a reduction in intraocular pressure by administering an intraocular formulation including a therapeutically effective amount of norketotifen for the reduction of intraocular pressure to the eye of the mammal in need thereof, wherein the intraocular formulation includes about 0.02 wt% to about 1.0 wt% norketotifen or a salt or an isomer thereof, calculated as the norketotifen free base. In certain aspects, the intraocular formulation is free from any added preservative and the intraocular formulation is self-preserving. Also included herein is a method of treating a human in need of a reduction in intraocular pressure by administering an intranasal formulation that includes a therapeutically effective amount of norketotifen for the reduction of intraocular pressure to the eye of the human in need thereof. Also, the beneficial effects of known drugs for high IOP are improved by co-administration with norketotifen.
A61K 31/4535 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
A61K 9/00 - Medicinal preparations characterised by special physical form
Described herein are methods of treating a mammal in need of treatment for non-histaminic pruritus by administering to the mammal in need thereof a therapeutically effective amount of RS-norketotifen, an isomer, or a pharmaceutically acceptable salt thereof, thereby reducing the desire to scratch in the mammal. Non-histaminergic types of pruritus are resistant to treatment with selective histamine H-1-, H-2- and H-4-receptor inhibitors. In certain aspects, the non-histaminergic pruritus is associated with a dermal disorder, a nerve disorder, or a systemic disorder.
A61K 31/4535 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
Described herein are methods of treating a mammal in need of treatment for non-histaminic pruritus by administering to the mammal in need thereof a therapeutically effective amount of RS-norketotifen, an isomer, or a pharmaceutically acceptable salt thereof, thereby reducing the desire to scratch in the mammal. Non-histaminergic types of pruritus are resistant to treatment with selective histamine H-1-, H-2- and H-4-receptor inhibitors. In certain aspects, the non-histaminergic pruritus is associated with a dermal disorder, a nerve disorder, or a systemic disorder.
A61K 31/4535 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
Described herein are methods of treating a mammal in need of treatment for non-histaminic pruritus by administering to the mammal in need thereof a therapeutically effective amount of RS-norketotifen or a pharmaceutically acceptable salt thereof, thereby reducing the desire to scratch in the mammal. Non-histaminergic types of pruritus are resistant to treatment with selective histamine H-1-, H-2- and H-4-receptor inhibitors. In certain aspects, the non-histaminergic pruritus is associated with diabetes.
A01N 43/40 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings
A61K 31/445 - Non-condensed piperidines, e.g. piperocaine
A61K 31/4535 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
A61K 9/00 - Medicinal preparations characterised by special physical form
15.
Medicinal treatment of dermal infectious disorders with norketotifen
The methods disclosed herein relate to the treatment of dermal infectious disorders, in human patients, by administering a therapeutically effective amount of RS-norketotifen.
A61K 31/4535 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61K 31/56 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids
A61K 31/137 - Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine
A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
A61K 31/573 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
The methods disclosed herein relate to the treatment of histamine H-4-related pruritus associated with nerve disorders, by administering a combined histamine H-1 and H-4 receptor inhibitor, specifically RS-norketotifen or a pharmaceutically acceptable salt thereof. Potentiated antipruritic activity by simultaneous inhibition of histamine H-1 receptors and histamine H-4 receptors are described.
A01N 43/40 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings
A61K 31/445 - Non-condensed piperidines, e.g. piperocaine
A61K 31/4535 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
A61K 9/00 - Medicinal preparations characterised by special physical form
Described herein are methods of treating a mammal in need of treatment for non-histaminic pruritus by administering to the mammal in need thereof a therapeutically effective amount of RS-norketotifen or a pharmaceutically acceptable salt thereof, thereby reducing the desire to scratch in the mammal. Non-histaminergic types of pruritus are resistant to treatment with selective histamine H-1-, H-2- and H-4-receptor inhibitors. In certain aspects, the non-histaminergic pruritus is associated with a dermal disorder, a psychological disorder, a mental disorder, a nerve disorder, or a systemic disorder.
A01N 43/40 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings
A61K 31/445 - Non-condensed piperidines, e.g. piperocaine
A61K 31/4535 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
A61K 9/00 - Medicinal preparations characterised by special physical form
18.
TREATMENT OF PRURITIC CONDITIONS MEDIATED THROUGH HISTAMINE H-4 RECEPTORS
The methods disclosed herein relate to the treatment of histamine H-4 - related dermal disorders, by administering a histamine H-4 receptor inverse agonist that selectively accumulates at the biophases for the disorders, specifically RS-norketotifen or a pharmaceutically acceptable salt thereof. Potentiated antipruritic activity by simultaneous inhibition of histamine H-1 receptors and histamine H-4 receptors are described.
A61K 31/4535 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
The methods disclosed herein relate to the treatment of histamine H-4—related pruritus, by administering a histamine H-4 receptor inverse agonist that selectively accumulates at the biophases of the disorders, specifically RS-norketotifen or a pharmaceutically acceptable salt thereof. Potentiated antipruritic activity by simultaneous inhibition of histamine H-1 receptors and histamine H-4 receptors are described.
A01N 43/40 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings
A61K 31/445 - Non-condensed piperidines, e.g. piperocaine
A61K 31/4535 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
20.
METHODS OF TREATING PRURITIC CONDITIONS MEDIATED THROUGH HISTAMINE H-4 RECEPTORS
The methods disclosed herein relate to the treatment of histamine H-4 - related dermal disorders, by administering a histamine H-4 receptor inverse agonist that selectively accumulates at the biophases for the disorders, specifically RS-norketotifen or a pharmaceutically acceptable salt thereof. Potentiated antipruritic activity by simultaneous inhibition of histamine H-1 receptors and histamine H-4 receptors are described.
A61K 31/4535 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
The methods disclosed herein relate to the treatment of chronic dermal disorders, such as for example atopic dermatitis or psoriasis, in human patients, by orally or topically administering a therapeutically effective amount of RS-norketotifen. Therapeutic antimicrobial activity of RS-norketotifen against Malassezia sp. and Staphylococcus aureus are also described.
A61K 31/4535 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
The methods disclosed herein relate to the treatment of chronic dermal disorders, such as for example atopic dermatitis or psoriasis, in human patients, by orally or topically administering a therapeutically effective amount of RS-norketotifen. Therapeutic antimicrobial activity of RS-norketotifen against Malassezia sp. and Staphylococcus aureus are also described.
A01N 43/40 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings
A61K 31/445 - Non-condensed piperidines, e.g. piperocaine
C07D 409/00 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
23.
MEDICINAL TREATMENT OF DERMAL DISEASES IN COMPANION ANIMALS WITH NORKETOTIFEN
The methods disclosed herein relate to the treatment of dermal disorders, such as for example atopic dermatitis, in dogs, by administering a therapeutically effective amount of norketotifen. Therapeutic antimicrobial activity of norketotifen against Malassezia sp. is also described.
A01N 43/40 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings
A61K 31/445 - Non-condensed piperidines, e.g. piperocaine
24.
Medicinal treatment of dermal diseases in companion animals
A61K 31/4535 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
The methods disclosed herein relate to the treatment of dermal disorders, such as for example atopic dermatitis, in dogs, by administering a therapeutically effective amount of racemic norketotifen. Co-administrations with steroids or immunosuppressant drugs are described.
A61K 31/4535 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
26.
TREATING XEROPHTHALMIA WITH COMPOUNDS INCREASING MEIBOMIAN GLAND SECRETION
Methods for the treatment of patients suffering from dry eyes, by using adrenergic beta-receptor agonists, particularly salbutamol and in particular the optically pure or substantially pure R-enantiomer thereof. The embodiments disclosed herein include methods of increasing the Meibomian lipid secretion and thereby reducing or eliminating xerophthalmia symptoms by the administration of formulations containing therapeutically effective amounts of an adrenergic beta-receptor agonist to said patients. In particular, certain embodiments disclosed herein concern compositions that contain R-salbutamol as the active beta-receptor stimulating ingredient. In certain embodiments, the formulations are administered to the ocular surface of the eye and/or to the eyelid (the underside of the eyelid and/or the top of the eyelid) of a patient in need thereof.
Ophthalmic compositions containing norketotifen and methods of making the same and the use thereof are disclosed. The methods also comprise administering to the eyes of a mammal in need thereof topical ophthalmic compositions containing norketotifen.
Methods of using a cycloheptathiophene compound for the treatment of xerophthalmia are described, as are formulations and compositions for such treatment.
A01N 43/04 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atom with one hetero atom
A method of promoting or improving the feed efficiency and the muscle-to-fat ratio in animals by administering to the animals a therapeutically effective amount of a mixture of RR-ractopamine and SR- ractopamine is disclosed. Manufacturing methods for making RR/SR-ractopamine are presented.
Dermal compositions comprising topical formulations of bupivacaine or ropivacaine, characterized by effective dermal absorption and long duration of dermal anesthetic activity, and intended for use in patients suffering from pruritus and dermal pain, including neuropathic pain, are provided. Compositions containing both bupivacaine and capsaicin are provided. Methods of alleviating pain by the topically administration of these compounds are also provided.
A01N 43/40 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings
A61K 31/445 - Non-condensed piperidines, e.g. piperocaine
The present invention relates to new tetralin compounds, the methods of preparing said tetralin compounds, the method of using said tetralin compounds as local anesthetics and dermal anesthetics, said compounds having particularly valuable properties as dermal and topical anesthetics in mammals, including man, as well as compositions containing said compounds.
A01N 43/40 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings
33.
INDANYLAMINES AND THEIR USE FOR LOCAL ANESTHESIA AND CHRONIC PAIN
Dermal and mucosal formulations of 2-[2-(N-phenyl-N-2-indanyl) aminoethyl] piperidine, characterized by rapid dermal and mucosal absorption and long duration of therapeutic activity are provided. Also provided are solutions of 2-[2-(N-phenyl-N-2-indanyl) aminoethyl] piperidine for injection, characterized by short onset time and long duration of activity. Formulations containing both 2-[2-(N-phenyl-N-2-indanyl) aminoethyl] piperidine and capsaicin are also provided.
A61K 31/535 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
A61K 31/54 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame
patents
