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 - Pipéridines non condensées, p. ex. pipérocaïne contenant d'autres systèmes hétérocycliques contenant un hétérocycle avec le soufre comme hétéro-atome du cycle, p. ex. pizotifène
A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
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 - Pipéridines non condensées, p. ex. pipérocaïne contenant d'autres systèmes hétérocycliques contenant un hétérocycle avec le soufre comme hétéro-atome du cycle, p. ex. pizotifène
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 - Pipéridines non condensées, p. ex. pipérocaïne contenant d'autres systèmes hétérocycliques contenant un hétérocycle avec le soufre comme hétéro-atome du cycle, p. ex. pizotifène
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 - Pipéridines non condensées, p. ex. pipérocaïne
A61K 31/4535 - Pipéridines non condensées, p. ex. pipérocaïne contenant d'autres systèmes hétérocycliques contenant un hétérocycle avec le soufre comme hétéro-atome du cycle, p. ex. pizotifène
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.
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 - Pipéridines non condensées, p. ex. pipérocaïne
A61K 31/4535 - Pipéridines non condensées, p. ex. pipérocaïne contenant d'autres systèmes hétérocycliques contenant un hétérocycle avec le soufre comme hétéro-atome du cycle, p. ex. pizotifène
A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
A61K 45/06 - Mélanges d'ingrédients actifs sans caractérisation chimique, p. ex. composés antiphlogistiques et pour le cœur
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 - Pipéridines non condensées, p. ex. pipérocaïne contenant d'autres systèmes hétérocycliques contenant un hétérocycle avec le soufre comme hétéro-atome du cycle, p. ex. pizotifène
A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
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 - Pipéridines non condensées, p. ex. pipérocaïne contenant d'autres systèmes hétérocycliques contenant un hétérocycle avec le soufre comme hétéro-atome du cycle, p. ex. pizotifène
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, produits repoussant ou attirant les animaux nuisibles, ou régulateurs de croissance des végétaux, contenant des composés hétérocycliques comportant des cycles avec un atome d'azote comme unique hétéro-atome du cycle des cycles à six chaînons
A61K 31/445 - Pipéridines non condensées, p. ex. pipérocaïne
A61K 31/4535 - Pipéridines non condensées, p. ex. pipérocaïne contenant d'autres systèmes hétérocycliques contenant un hétérocycle avec le soufre comme hétéro-atome du cycle, p. ex. pizotifène
A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
12.
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 - Pipéridines non condensées, p. ex. pipérocaïne contenant d'autres systèmes hétérocycliques contenant un hétérocycle avec le soufre comme hétéro-atome du cycle, p. ex. pizotifène
A61K 45/06 - Mélanges d'ingrédients actifs sans caractérisation chimique, p. ex. composés antiphlogistiques et pour le cœur
A61K 31/56 - Composés contenant des systèmes cycliques du cyclopenta[a]hydrophénanthrèneLeurs dérivés, p. ex. stéroïdes
A61K 31/137 - Arylalkylamines, p. ex. amphétamine, épinéphrine, salbutamol, éphédrine
A61K 31/167 - Amides, p. ex. acides hydroxamiques ayant des cycles aromatiques, p. ex. colchicine, aténolol, progabide ayant l'atome d'azote d'un groupe carboxamide lié directement au cycle aromatique, p. ex. lidocaïne, paracétamol
A61K 31/573 - Composés contenant des systèmes cycliques du cyclopenta[a]hydrophénanthrèneLeurs dérivés, p. ex. stéroïdes substitués en position 17 bêta par une chaîne à deux atomes de carbone, p. ex. prégnane ou progestérone substitués en position 21, p. ex. cortisone, dexaméthasone, prednisone ou aldostérone
A61K 9/127 - Vecteurs à bicouches synthétiques, p. ex. liposomes ou liposomes comportant du cholestérol en tant qu’unique agent tensioactif non phosphatidylique
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, produits repoussant ou attirant les animaux nuisibles, ou régulateurs de croissance des végétaux, contenant des composés hétérocycliques comportant des cycles avec un atome d'azote comme unique hétéro-atome du cycle des cycles à six chaînons
A61K 31/445 - Pipéridines non condensées, p. ex. pipérocaïne
A61K 31/4535 - Pipéridines non condensées, p. ex. pipérocaïne contenant d'autres systèmes hétérocycliques contenant un hétérocycle avec le soufre comme hétéro-atome du cycle, p. ex. pizotifène
A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
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, produits repoussant ou attirant les animaux nuisibles, ou régulateurs de croissance des végétaux, contenant des composés hétérocycliques comportant des cycles avec un atome d'azote comme unique hétéro-atome du cycle des cycles à six chaînons
A61K 31/445 - Pipéridines non condensées, p. ex. pipérocaïne
A61K 31/4535 - Pipéridines non condensées, p. ex. pipérocaïne contenant d'autres systèmes hétérocycliques contenant un hétérocycle avec le soufre comme hétéro-atome du cycle, p. ex. pizotifène
A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
15.
Methods of treatment of histamine H-4 receptor-related pruritus
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, produits repoussant ou attirant les animaux nuisibles, ou régulateurs de croissance des végétaux, contenant des composés hétérocycliques comportant des cycles avec un atome d'azote comme unique hétéro-atome du cycle des cycles à six chaînons
A61K 31/445 - Pipéridines non condensées, p. ex. pipérocaïne
A61K 31/4535 - Pipéridines non condensées, p. ex. pipérocaïne contenant d'autres systèmes hétérocycliques contenant un hétérocycle avec le soufre comme hétéro-atome du cycle, p. ex. pizotifène
16.
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 - Pipéridines non condensées, p. ex. pipérocaïne contenant d'autres systèmes hétérocycliques contenant un hétérocycle avec le soufre comme hétéro-atome du cycle, p. ex. pizotifène
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, produits repoussant ou attirant les animaux nuisibles, ou régulateurs de croissance des végétaux, contenant des composés hétérocycliques comportant des cycles avec un atome d'azote comme unique hétéro-atome du cycle des cycles à six chaînons
A61K 31/445 - Pipéridines non condensées, p. ex. pipérocaïne
C07D 409/00 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes de soufre comme uniques hétéro-atomes du cycle
18.
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, produits repoussant ou attirant les animaux nuisibles, ou régulateurs de croissance des végétaux, contenant des composés hétérocycliques comportant des cycles avec un atome d'azote comme unique hétéro-atome du cycle des cycles à six chaînons
A61K 31/445 - Pipéridines non condensées, p. ex. pipérocaïne
19.
Medicinal treatment of dermal diseases in companion animals
A61K 31/4535 - Pipéridines non condensées, p. ex. pipérocaïne contenant d'autres systèmes hétérocycliques contenant un hétérocycle avec le soufre comme hétéro-atome du cycle, p. ex. pizotifène
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 - Pipéridines non condensées, p. ex. pipérocaïne contenant d'autres systèmes hétérocycliques contenant un hétérocycle avec le soufre comme hétéro-atome du cycle, p. ex. pizotifène
21.
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, produits repoussant ou attirant les animaux nuisibles, ou régulateurs de croissance des végétaux, contenant des composés hétérocycliques comportant des cycles avec un ou plusieurs atomes d'oxygène ou de soufre comme uniques hétéro-atomes du cycle avec un hétéro-atome
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, produits repoussant ou attirant les animaux nuisibles, ou régulateurs de croissance des végétaux, contenant des composés hétérocycliques comportant des cycles avec un atome d'azote comme unique hétéro-atome du cycle des cycles à six chaînons
A61K 31/445 - Pipéridines non condensées, p. ex. pipérocaïne
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, produits repoussant ou attirant les animaux nuisibles, ou régulateurs de croissance des végétaux, contenant des composés hétérocycliques comportant des cycles avec un atome d'azote comme unique hétéro-atome du cycle des cycles à six chaînons
brevets
