Embodiments described herein are directed to methods for treating moderate to severe plaque psoriasis, atopic dermatitis, or radiation dermatitis in a subject comprising administering about 1.0% tapinarof in a topical composition to the affected areas of the subject once a day for an initial period of time until the plaque psoriasis, atopic dermatitis, or radiation dermatitis is clear at which time the administration is stopped, and reassessing the subject from about 3 months to about 12 months after administration is stopped to determine if further treatment is required. Also described is the remittive effect observed after once daily administration of 1% tapinarof cream.
Disclosed is composition and a method for treating atopic dermatitis by applying a 1.0% tapinarof topical cream to the affected area of a subject once daily for a minimum of 8 weeks. The treatment results in a significant improvement in the vIGA-AD score, achieving at least a 2-grade improvement from baseline and a final score of 0. Additionally, a reduction of at least 4 points in the PP-NRS score is observed during the treatment period. In some instances, the method ensures that the plasma concentration of tapinarof remains below 50 pg/mL throughout the application of the topical cream, providing an effective and safe treatment for atopic dermatitis.
The present invention relates to topical pharmaceutical emulsion compositions comprising a therapeutically effective amount of 3,5-Dihydroxy-4-isopropyl-trans-stilbene or a pharmaceutically acceptable salt thereof, an oil phase, a water phase, a surfactant, and an antioxidant, and wherein the emulsion composition is homogeneous and/or the active is solubilized in the oil phase. The invention also relates to methods of treating a dermatological condition or disorder in a patient by administering the present compositions to the skin of the patient.
A61K 9/113 - Émulsions multiples, p. ex. huile-dans l'eau-dans l'huile
A61K 47/06 - Composés organiques, p. ex. hydrocarbures naturels ou synthétiques, polyoléfines, huile minérale, gelée de pétrole ou ozocérite
A61K 47/10 - AlcoolsPhénolsLeurs sels, p. ex. glycérolPolyéthylène glycols [PEG]PoloxamèresAlkyléthers de PEG/POE
A61K 47/14 - Esters d’acides carboxyliques, p. ex. acides gras monoglycérides, triglycérides à chaine moyenne, parabènes ou esters d’acide gras de PEG
A61K 47/26 - Hydrates de carbone, p. ex. polyols ou sucres alcoolisés, sucres aminés, acides nucléiques, mono-, di- ou oligosaccharidesLeurs dérivés, p. ex. polysorbates, esters d’acide gras de sorbitan ou glycyrrhizine
4.
ISOQUINOLINE COMPOUNDS AND THEIR USE IN TREATING AhR IMBALANCE
The present invention is directed to novel compounds of Formula (I), or a pharmaceutically acceptable salt, solvate or hydrate thereof. Pharmaceutical compositions comprising a compound of Formula (I), or a pharmaceutically acceptable salt, solvate or hydrate thereof, are also described. The invention is also directed to use of the compounds of Formula (I) for treating a condition in a mammal associated with AhR imbalance, such as an inflammatory disease or disorder.
A61P 29/00 - Agents analgésiques, antipyrétiques ou anti-inflammatoires non centraux, p. ex. agents antirhumatismauxMédicaments anti-inflammatoires non stéroïdiens [AINS]
5.
TAPINAROF AND ANALOGS THEREOF FOR USE IN TREATING AHR MEDIATED DISEASES
The present invention is directed to methods of treating certain diseases comprising administering compounds or pharmaceutical compositions of Formula (I), Formula (II), Formula (III), or Formula (IV), or a pharmaceutically acceptable salt, solvate or hydrate thereof. Pharmaceutical compositions comprising a compound of Formula (I), Formula (II), Formula (III), or Formula (IV), or a pharmaceutically acceptable salt, solvate or hydrate thereof, are also described.
The present invention is directed to methods of treating certain diseases comprising administering compounds or pharmaceutical compositions of Formula (I), Formula (Ia), or a pharmaceutically acceptable salt, solvate or hydrate thereof. Pharmaceutical compositions comprising a compound of Formula (I), Formula (Ia), or a pharmaceutically acceptable salt, solvate or hydrate thereof, are also described.
Topical compositions and methods for using topical compositions comprising tapinarof to treat mild to moderate atopic dermatitis or plaque psoriasis are described herein. Also described are clinical endpoints for treatment of subjects diagnosed with mild to moderate atopic dermatitis, wherein about 5% to about 35% of body surface area was affected, and Investigator Global Assessment (IGA) score was greater than or equal to 3. Also described are clinical endpoints for treatment of subjects diagnosed with chronic mild to moderate plaque psoriasis for greater than or equal to 6 months, wherein about 3% to about 20% of body surface area was affected, and Physician Global Assessment (PGA) score was greater than or equal to 2.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for human use for the treatment of dermatitis and acne; biologic preparations for medical and therapeutic purposes for the treatment of dermatitis and acne; pharmaceutical preparations and biologic preparations for the treatment of skin diseases and disorders; pharmaceutical preparations and biologic preparations for the treatment of psoriasis and atopic dermatitis
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
(1) Pharmaceutical preparations for human use for the treatment of dermatitis and acne; biologic preparations for medical and therapeutic purposes for the treatment of dermatitis and acne; pharmaceutical preparations and biologic preparations for the treatment of skin diseases and disorders; pharmaceutical preparations and biologic preparations for the treatment of psoriasis and atopic dermatitis
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for human use; biologic
preparations for medical and therapeutic purposes;
pharmaceutical preparations and biologic preparations for
the treatment of skin diseases and disorders; pharmaceutical
preparations and biologic preparations for the treatment of
psoriasis and atopic dermatitis.
The present invention relates to topical pharmaceutical emulsion compositions comprising a therapeutically effective amount of 3,5-Dihydroxy-4-isopropyl-trans-stilbene or a pharmaceutically acceptable salt thereof, an oil phase, a water phase, a surfactant, and an antioxidant, and wherein the emulsion composition is homogeneous and/or the active is solubilized in the oil phase. The invention also relates to methods of treating a dermatological condition or disorder in a patient by administering the present compositions to the skin of the patient.
Topical compositions and methods for using topical compositions comprising tapinarof to treat mild to moderate atopic dermatitis or plaque psoriasis are described herein. Also described are clinical endpoints for treatment of subjects diagnosed with mild to moderate atopic dermatitis, wherein about 5% to about 35% of body surface area was affected, and Investigator Global Assessment (IGA) score was greater than or equal to 3. Also described are clinical endpoints for treatment of subjects diagnosed with chronic mild to moderate plaque psoriasis for greater than or equal to 6 months, wherein about 3% to about 20% of body surface area was affected, and Physician Global Assessment (PGA) score was greater than or equal to 2.
The present invention provides processes for the preparation of 3, 5-Dihydroxy-4-isopropyl-trans-stilbene or a salt or solvate thereof and novel intermediates used therein. In some embodiments the 3, 5-Dihydroxy-4-isopropyl-trans-stilbene is prepared from (E)-2-chloro-2-isopropyl-5-styrylcyclohexane-1,3-dione. Also disclosed are crystal forms of 3, 5-Dihydroxy-4-isopropyl-trans-stilbene or a salt or solvate thereof and pharmaceutical compositions comprising same.
C07C 37/00 - Préparation de composés comportant des groupes hydroxyle ou O-métal liés à un atome de carbone d'un cycle aromatique à six chaînons
C07C 50/24 - Quinones contenant des atomes d'halogène
C07C 51/38 - Préparation d'acides carboxyliques, de leurs sels, halogénures ou anhydrides par des réactions ne créant pas de groupes carboxyle par élimination d'hydrogène ou de groupes fonctionnelsPréparation d'acides carboxyliques, de leurs sels, halogénures ou anhydrides par des réactions ne créant pas de groupes carboxyle par hydrogénolyse de groupes fonctionnels par décarboxylation
C07C 67/03 - Préparation d'esters d'acides carboxyliques par réaction d'un groupe ester avec un groupe hydroxyle
C07C 67/293 - Préparation d'esters d'acides carboxyliques par modification de la partie hydroxyle de l'ester sans introduction d'un groupe ester par isomérisationPréparation d'esters d'acides carboxyliques par modification de la partie hydroxyle de l'ester sans introduction d'un groupe ester par modification de la taille du squelette carboné
C07C 59/353 - Composés saturés comportant plusieurs groupes carboxyle contenant des groupes cétone contenant des cycles
C07C 45/63 - Préparation de composés comportant des groupes C=O liés uniquement à des atomes de carbone ou d'hydrogènePréparation des chélates de ces composés par des réactions ne créant pas de groupe C=O par introduction d'atomes d'halogènePréparation de composés comportant des groupes C=O liés uniquement à des atomes de carbone ou d'hydrogènePréparation des chélates de ces composés par des réactions ne créant pas de groupe C=O par substitution d'atomes d'halogène par des atomes d'autres halogènes
C07C 51/09 - Préparation d'acides carboxyliques, de leurs sels, halogénures ou anhydrides à partir de lactones ou d'esters d'acides carboxyliques
C07C 67/343 - Préparation d'esters d'acides carboxyliques par modification de la partie acide de l'ester sans introduction d'un groupe ester par isomérisationPréparation d'esters d'acides carboxyliques par modification de la partie acide de l'ester sans introduction d'un groupe ester par modification de la taille du squelette carboné par augmentation du nombre d'atomes de carbone
C07C 45/72 - Préparation de composés comportant des groupes C=O liés uniquement à des atomes de carbone ou d'hydrogènePréparation des chélates de ces composés par des réactions ne créant pas de groupe C=O par isomérisationPréparation de composés comportant des groupes C=O liés uniquement à des atomes de carbone ou d'hydrogènePréparation des chélates de ces composés par des réactions ne créant pas de groupe C=O par modification de la taille du squelette carboné par augmentation du nombre d'atomes de carbone par réaction de composés comportant des groupes C=O sur eux-mêmes ou avec d'autres composés comportant des groupes C=O
C07C 45/54 - Préparation de composés comportant des groupes C=O liés uniquement à des atomes de carbone ou d'hydrogènePréparation des chélates de ces composés par pyrolyse, réarrangement ou décomposition de composés contenant des atomes d'oxygène liés par des liaisons doubles, p. ex. d'esters
C07C 37/07 - Préparation de composés comportant des groupes hydroxyle ou O-métal liés à un atome de carbone d'un cycle aromatique à six chaînons par conversion de cycles non aromatiques à six chaînons ou de tels cycles formés in situ, en cycles aromatiques à six chaînons, p. ex. par déshydrogénation avec réduction simultanée du groupe C=O de ce cycle
The present invention relates to topical pharmaceutical emulsion compositions comprising a therapeutically effective amount of 3,5-Dihydroxy-4-isopropyl-trans-stilbene or a pharmaceutically acceptable salt thereof, an oil phase, a water phase, a surfactant, and an antioxidant, and wherein the emulsion composition is homogeneous and/or the active is solubilized in the oil phase. The invention also relates to methods of treating a dermatological condition or disorder in a patient by administering the present compositions to the skin of the patient.
A61K 47/26 - Hydrates de carbone, p. ex. polyols ou sucres alcoolisés, sucres aminés, acides nucléiques, mono-, di- ou oligosaccharidesLeurs dérivés, p. ex. polysorbates, esters d’acide gras de sorbitan ou glycyrrhizine
A61K 47/06 - Composés organiques, p. ex. hydrocarbures naturels ou synthétiques, polyoléfines, huile minérale, gelée de pétrole ou ozocérite
A61K 47/14 - Esters d’acides carboxyliques, p. ex. acides gras monoglycérides, triglycérides à chaine moyenne, parabènes ou esters d’acide gras de PEG
A61K 47/10 - AlcoolsPhénolsLeurs sels, p. ex. glycérolPolyéthylène glycols [PEG]PoloxamèresAlkyléthers de PEG/POE
The present invention is directed to novel compounds of Formula (I), or a pharmaceutically acceptable salt, solvate or hydrate thereof. Pharmaceutical compositions comprising a compound of Formula (I), or a pharmaceutically acceptable salt, solvate or hydrate thereof, are also described. The invention is also directed to use of the compounds of Formula (I) for treating a condition in a mammal associated with AhR imbalance, such as an inflammatory disease or disorder.
C07D 217/20 - Radicaux aralkyle avec des atomes d'oxygène liés directement au noyau aromatique dudit radical aralkyle, p. ex. papavérine
A61P 29/00 - Agents analgésiques, antipyrétiques ou anti-inflammatoires non centraux, p. ex. agents antirhumatismauxMédicaments anti-inflammatoires non stéroïdiens [AINS]
A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
Aspects of the disclosure include fixed dose pharmaceutical compositions including a plurality of immediate release beads of oxybutynin, or pharmaceutically acceptable salt thereof, beads and a plurality of delayed-immediate release beads of pilocarpine, or pharmaceutically acceptable salt thereof and methods for treating hyperhidrosis in a subject. In some embodiments the plurality of beads are encapsulated in a size 3 capsule. In practicing methods according to certain embodiments, a variety of formulations are described to achieve a delayed-immediate release profile wherein the pilocarpine, or pharmaceutically acceptable salt thereof, is released not more than 30% in 10 minutes and not less than 85% at 45 minutes of administration of the pharmaceutical composition to the subject and oxybutynin is released soon after administration.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
(1) Pharmaceutical preparations for human use; biologic preparations for medical and therapeutic purposes; pharmaceutical preparations and biologic preparations for the treatment of skin diseases and disorders; pharmaceutical preparations and biologic preparations for the treatment of psoriasis and atopic dermatitis.
18.
REMITTIVE EFFECTS OF TAPINAROF IN THE TREATMENT OF PLAQUE PSORIASIS, ATOPIC DERMATITIS, OR RADIATION DERMATITIS
Embodiments described herein are directed to methods for treating moderate to severe plaque psoriasis, atopic dermatitis, or radiation dermatitis in a subject comprising administering about 1.0% tapinarof in a topical composition to the affected areas of the subject once a day for an initial period of time until the plaque psoriasis, atopic dermatitis, or radiation dermatitis is clear at which time the administration is stopped, and reassessing the subject from about 3 months to about 12 months after administration is stopped to determine if further treatment is required. Also described is the remittive effect observed after once daily administration of 1% tapinarof cream.
Topical compositions and methods for using topical compositions comprising tapinarof to treat mild to moderate atopic dermatitis or plaque psoriasis are described herein. Also described are clinical endpoints for treatment of subjects diagnosed with mild to moderate atopic dermatitis, wherein about 5% to about 35% of body surface area was affected, and Investigator Global Assessment (IGA) score was greater than or equal to 3. Also described are clinical endpoints for treatment of subjects diagnosed with chronic mild to moderate plaque psoriasis for greater than or equal to 6 months, wherein about 3% to about 20% of body surface area was affected, and Physician Global Assessment (PGA) score was greater than or equal to 2.
Topical compositions and methods for using topical compositions comprising tapinarof to treat mild to moderate atopic dermatitis are described herein. Also described are clinical endpoints for treatment of subjects diagnosed with mild to moderate atopic dermatitis, wherein about 5% to about 35% of body surface area was affected, and Investigator Global Assessment (IGA) score was greater than or equal to 3.
36 - Services financiers, assurances et affaires immobilières
42 - Services scientifiques, technologiques et industriels, recherche et conception
44 - Services médicaux, services vétérinaires, soins d'hygiène et de beauté; services d'agriculture, d'horticulture et de sylviculture.
Produits et services
Printed products, namely, lists featuring a registry of patients with atopic dermatitis, acne, psoriasis, skin related diseases, disorders and conditions for medical treatment purposes Patient consumer support, namely, providing consumer product information in the field of pharmaceuticals via a website and
telecommunications networks; patient support services, namely, business administration of patient reimbursement programs via a
website and telecommunications networks Patient support services, namely, financial administration of patient reimbursement programs via a website and
telecommunications networks Medical and scientific research services; providing information in the field of medical and scientific research featuring a registry of
patients with atopic dermatitis, acne, psoriasis, skin related diseases, disorders and conditions; administering a scientific advisory
committee in the nature of providing scientific advice and scientific consultation relating to atopic dermatitis, acne, psoriasis, skin
related diseases, disorders and conditions; hosting an online community website featuring shared communications between
community members in the field of atopic dermatitis, acne, psoriasis, skin related diseases, disorders and conditions; providing an
online community for users to engage with and share information in the field of atopic dermatitis, acne, psoriasis, skin related
diseases, disorders and conditions Providing medical information; Providing a website and an Internet website portal featuring a registry of patients with atopic
dermatitis, acne, psoriasis, skin related diseases, disorders and conditions for medical treatment purposes; providing medical and
health information to consumers, patients, doctors, and caregivers in the field of atopic dermatitis, acne, psoriasis, skin related
diseases, disorders and conditions
36 - Services financiers, assurances et affaires immobilières
41 - Éducation, divertissements, activités sportives et culturelles
42 - Services scientifiques, technologiques et industriels, recherche et conception
44 - Services médicaux, services vétérinaires, soins d'hygiène et de beauté; services d'agriculture, d'horticulture et de sylviculture.
Produits et services
(1) Patient consumer support featuring consumer product information in the field of pharmaceuticals via a website or telecommunications networks; patient support services, namely, business administration of patient reimbursement programs via a website or telecommunications networks.
(2) Patient support services, namely, financial administration of patient reimbursement programs via a website or telecommunications networks.
(3) Medical and scientific research services; providing an online computer database that contains data on clinical outcomes, patient-reported outcomes, clinician-reported outcomes, caregiver outcomes and health care resource utilization for medical and scientific research purposes; providing information in the field of medical and scientific research featuring a registry of patients with atopic dermatitis, acne, psoriasis, skin related diseases, disorders and conditions; administering a scientific advisory committee in the nature of providing scientific advice and scientific consultation relating to atopic dermatitis, acne, psoriasis, skin related diseases, disorders and conditions; hosting an online community website featuring shared communications between community members in the field of atopic dermatitis, acne, psoriasis, skin related diseases, disorders and conditions; providing an online community for users to engage with and share information in the field of atopic dermatitis, acne, psoriasis, skin related diseases, disorders and conditions; computer services, namely, creating an online community for registered users to participate in discussions, get feedback from their peers, form virtual communities, and engage in social networking services in the field of atopic dermatitis, acne, psoriasis, skin related diseases, disorders and conditions; creating an on-line community for doctors, patients, clinicians and caregivers for the purpose of participating in discussions about atopic dermatitis, acne, psoriasis, skin related diseases, disorders and conditions.
(4) Providing medical information; Providing a website, portal and printed information featuring a registry of patients with atopic dermatitis, acne, psoriasis, skin related diseases, disorders and conditions for medical treatment purposes; providing medical and health information to consumers, patients, doctors, and caregivers in the field of atopic dermatitis, acne, psoriasis, skin related diseases, disorders and conditions.
23.
REMITTIVE EFFECTS OF TAPINAROF IN THE TREATMENT OF PLAQUE PSORIASIS, ATOPIC DERMATITIS, OR RADIATION DERMATITIS
Embodiments described herein are directed to methods for treating moderate to severe plaque psoriasis, atopic dermatitis, or radiation dermatitis in a subject comprising administering about 1.0% tapinarof in a topical composition to the affected areas of the subject once a day for an initial period of time until the plaque psoriasis, atopic dermatitis, or radiation dermatitis is clear at which time the administration is stopped, and reassessing the subject from about 3 months to about 12 months after administration is stopped to determine if further treatment is required. Also described is the remittive effect observed after once daily administration of 1% tapinarof cream.
Embodiments described herein are directed to methods for treating moderate to severe plaque psoriasis, atopic dermatitis, or radiation dermatitis in a subject comprising administering about 1.0% tapinarof in a topical composition to the affected areas of the subject once a day for an initial period of time until the plaque psoriasis, atopic dermatitis, or radiation dermatitis is clear at which time the administration is stopped, and reassessing the subject from about 3 months to about 12 months after administration is stopped to determine if further treatment is required. Also described is the remittive effect observed after once daily administration of 1% tapinarof cream.
C07K 16/24 - Immunoglobulines, p. ex. anticorps monoclonaux ou polyclonaux contre du matériel provenant d'animaux ou d'humains contre des cytokines, des lymphokines ou des interférons
25.
CERDULATINIB-CONTAINING TOPICAL SKIN PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
Embodiments described herein are directed to topical compositions for administering cerdulatinib or a pharmaceutically acceptable salt, hydrate or solvate thereof. Embodiments described herein are also directed to methods for preparing the topical compositions. The disclosed compositions are suitable for the treatment of dermatologic conditions such as atopic dermatitis, cutaneous lupus, lichen planus, cutaneous graft versus host disease, contact dermatitis, psoriasis, rosacea, scleroderma, morphea and dermatomyositis.
Embodiments described herein relate to topical pharmaceutical compositions comprising tapinarof, wherein the topical pharmaceutical composition is formulated as an aqueous gel, an anhydrous gel, an ointment, or a foam. Embodiments also relate to methods of treating a dermatological condition or disorder in a patient by administering the present compositions to the skin of the patient.
Embodiments described herein relate to topical pharmaceutical compositions comprising tapinarof, wherein the topical pharmaceutical composition is formulated as an aqueous gel, an anhydrous gel, an ointment, or a foam. Embodiments also relate to methods of treating a dermatological condition or disorder in a patient by administering the present compositions to the skin of the patient.
Embodiments described herein relate to topical pharmaceutical compositions comprising tapinarof, wherein the topical pharmaceutical composition is formulated as an aqueous gel, an anhydrous gel, an ointment, or a foam. Embodiments also relate to methods of treating a dermatological condition or disorder in a patient by administering the present compositions to the skin of the patient.
A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
A61K 47/12 - Acides carboxyliquesLeurs sels ou anhydrides
A61K 47/26 - Hydrates de carbone, p. ex. polyols ou sucres alcoolisés, sucres aminés, acides nucléiques, mono-, di- ou oligosaccharidesLeurs dérivés, p. ex. polysorbates, esters d’acide gras de sorbitan ou glycyrrhizine
A61K 47/18 - AminesAmidesUréesComposés d’ammonium quaternaireAcides aminésOligopeptides ayant jusqu’à cinq acides aminés
29.
Isoquinoline compounds and their use in treating AhR imbalance
The present invention is directed to novel compounds of Formula (I), or a pharmaceutically acceptable salt, solvate or hydrate thereof. Pharmaceutical compositions comprising a compound of Formula (I), or a pharmaceutically acceptable salt, solvate or hydrate thereof, are also described. The invention is also directed to use of the compounds of Formula (I) for treating a condition in a mammal associated with AhR imbalance, such as an inflammatory disease or disorder.
C07D 217/20 - Radicaux aralkyle avec des atomes d'oxygène liés directement au noyau aromatique dudit radical aralkyle, p. ex. papavérine
A61P 29/00 - Agents analgésiques, antipyrétiques ou anti-inflammatoires non centraux, p. ex. agents antirhumatismauxMédicaments anti-inflammatoires non stéroïdiens [AINS]
A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
30.
ISOQUINOLINE COMPOUNDS AND THEIR USE IN TREATING AhR IMBALANCE
The present invention is directed to novel compounds of Formula (I), or a pharmaceutically acceptable salt, solvate or hydrate thereof. Pharmaceutical compositions comprising a compound of Formula (I), or a pharmaceutically acceptable salt, solvate or hydrate thereof, are also described. The invention is also directed to use of the compounds of Formula (I) for treating a condition in a mammal associated with AhR imbalance, such as an inflammatory disease or disorder.
The present invention is directed to novel compounds of Formula (I), or a pharmaceutically acceptable salt, solvate or hydrate thereof. Pharmaceutical compositions comprising a compound of Formula (I), or a pharmaceutically acceptable salt, solvate or hydrate thereof, are also described. The invention is also directed to use of the compounds of Formula (I) for treating a condition in a mammal associated with AhR imbalance, such as an inflammatory disease or disorder.
The present invention is directed to novel compounds of Formula (I), or a pharmaceutically acceptable salt, solvate or hydrate thereof. Pharmaceutical compositions comprising a compound of Formula (I), or a pharmaceutically acceptable salt, solvate or hydrate thereof, are also described. The invention is also directed to use of the compounds of Formula (I) for treating a condition in a mammal associated with AhR imbalance, such as an inflammatory disease or disorder.
C07D 217/20 - Radicaux aralkyle avec des atomes d'oxygène liés directement au noyau aromatique dudit radical aralkyle, p. ex. papavérine
A61P 29/00 - Agents analgésiques, antipyrétiques ou anti-inflammatoires non centraux, p. ex. agents antirhumatismauxMédicaments anti-inflammatoires non stéroïdiens [AINS]
A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
The present invention relates to topical pharmaceutical emulsion compositions comprising a therapeutically effective amount of 3,5-Dihydroxy-4-isopropyl-trans-stilbene or a pharmaceutically acceptable salt thereof, an oil phase, a water phase, a surfactant, and an antioxidant, and wherein the emulsion composition is homogeneous and/or the active is solubilized in the oil phase. The invention also relates to methods of treating a dermatological condition or disorder in a patient by administering the present compositions to the skin of the patient.
The present invention relates to topical pharmaceutical emulsion compositions comprising a therapeutically effective amount of 3,5-Dihydroxy-4-isopropyl-trans-stilbene or a pharmaceutically acceptable salt thereof, an oil phase, a water phase, a surfactant, and an antioxidant, and wherein the emulsion composition is homogeneous and/or the active is solubilized in the oil phase. The invention also relates to methods of treating a dermatological condition or disorder in a patient by administering the present compositions to the skin of the patient.
The present invention provides processes for the preparation of 3, 5-Dihydroxy-4-isopropyl-trans-stilbene or a salt or solvate thereof and novel intermediates used therein. In some embodiments the 3, 5-Dihydroxy-4-isopropyl-trans-stilbene is prepared from (E)-2-chloro-2-isopropyl-5-styrylcyclohexane-1,3-dione. Also disclosed are crystal forms of 3, 5-Dihydroxy-4-isopropyl-trans-stilbene or a salt or solvate thereof and pharmaceutical compositions comprising same.
C07C 37/02 - Préparation de composés comportant des groupes hydroxyle ou O-métal liés à un atome de carbone d'un cycle aromatique à six chaînons par remplacement des groupes fonctionnels liés à un cycle aromatique à six chaînons par des groupes hydroxyle, p. ex. par hydrolyse par substitution d'atomes d'halogène
C07C 45/54 - Préparation de composés comportant des groupes C=O liés uniquement à des atomes de carbone ou d'hydrogènePréparation des chélates de ces composés par pyrolyse, réarrangement ou décomposition de composés contenant des atomes d'oxygène liés par des liaisons doubles, p. ex. d'esters
C07C 45/72 - Préparation de composés comportant des groupes C=O liés uniquement à des atomes de carbone ou d'hydrogènePréparation des chélates de ces composés par des réactions ne créant pas de groupe C=O par isomérisationPréparation de composés comportant des groupes C=O liés uniquement à des atomes de carbone ou d'hydrogènePréparation des chélates de ces composés par des réactions ne créant pas de groupe C=O par modification de la taille du squelette carboné par augmentation du nombre d'atomes de carbone par réaction de composés comportant des groupes C=O sur eux-mêmes ou avec d'autres composés comportant des groupes C=O
C07C 37/00 - Préparation de composés comportant des groupes hydroxyle ou O-métal liés à un atome de carbone d'un cycle aromatique à six chaînons
C07C 50/24 - Quinones contenant des atomes d'halogène
C07C 51/38 - Préparation d'acides carboxyliques, de leurs sels, halogénures ou anhydrides par des réactions ne créant pas de groupes carboxyle par élimination d'hydrogène ou de groupes fonctionnelsPréparation d'acides carboxyliques, de leurs sels, halogénures ou anhydrides par des réactions ne créant pas de groupes carboxyle par hydrogénolyse de groupes fonctionnels par décarboxylation
C07C 67/03 - Préparation d'esters d'acides carboxyliques par réaction d'un groupe ester avec un groupe hydroxyle
C07C 67/293 - Préparation d'esters d'acides carboxyliques par modification de la partie hydroxyle de l'ester sans introduction d'un groupe ester par isomérisationPréparation d'esters d'acides carboxyliques par modification de la partie hydroxyle de l'ester sans introduction d'un groupe ester par modification de la taille du squelette carboné
C07C 59/353 - Composés saturés comportant plusieurs groupes carboxyle contenant des groupes cétone contenant des cycles
C07C 45/63 - Préparation de composés comportant des groupes C=O liés uniquement à des atomes de carbone ou d'hydrogènePréparation des chélates de ces composés par des réactions ne créant pas de groupe C=O par introduction d'atomes d'halogènePréparation de composés comportant des groupes C=O liés uniquement à des atomes de carbone ou d'hydrogènePréparation des chélates de ces composés par des réactions ne créant pas de groupe C=O par substitution d'atomes d'halogène par des atomes d'autres halogènes
C07C 51/09 - Préparation d'acides carboxyliques, de leurs sels, halogénures ou anhydrides à partir de lactones ou d'esters d'acides carboxyliques
C07C 67/343 - Préparation d'esters d'acides carboxyliques par modification de la partie acide de l'ester sans introduction d'un groupe ester par isomérisationPréparation d'esters d'acides carboxyliques par modification de la partie acide de l'ester sans introduction d'un groupe ester par modification de la taille du squelette carboné par augmentation du nombre d'atomes de carbone
C07C 37/07 - Préparation de composés comportant des groupes hydroxyle ou O-métal liés à un atome de carbone d'un cycle aromatique à six chaînons par conversion de cycles non aromatiques à six chaînons ou de tels cycles formés in situ, en cycles aromatiques à six chaînons, p. ex. par déshydrogénation avec réduction simultanée du groupe C=O de ce cycle
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for human use for the treatment of dermatitis and acne; biologic preparations for medical and therapeutic purposes for the treatment of dermatitis and acne; pharmaceutical preparations and biologic preparations for the treatment of skin diseases and disorders; pharmaceutical preparations and biologic preparations for the treatment of psoriasis and atopic dermatitis
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for human use; biological
preparations for medical or therapeutic use; pharmaceutical
preparations and biological preparations for the treatment
of skin diseases and disorders; pharmaceutical preparations
and biological preparations for the treatment of psoriasis
and atopic dermatitis.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for human use; biological
preparations for medical or therapeutic use; pharmaceutical
preparations and biological preparations for the treatment
of skin diseases and disorders; pharmaceutical preparations
and biological preparations for the treatment of psoriasis
and atopic dermatitis.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for human use; biological
preparations for medical or therapeutic use; pharmaceutical
preparations and biological preparations for the treatment
of skin diseases and disorders; pharmaceutical preparations
and biological preparations for the treatment of psoriasis
and atopic dermatitis.
The present invention provides processes for the preparation of 3, 5-Dihydroxy-4-isopropyl-trans-stilbene or a salt or solvate thereof and novel intermediates used therein. In some embodiments the 3, 5-Dihydroxy-4-isopropyl-trans-stilbene is prepared from (E)-2-chloro-2-isopropyl-5-styrylcyclohexane-1,3-dione. Also disclosed are crystal forms of 3, 5-Dihydroxy-4-isopropyl-trans-stilbene or a salt or solvate thereof and pharmaceutical compositions comprising same.
C07C 51/38 - Préparation d'acides carboxyliques, de leurs sels, halogénures ou anhydrides par des réactions ne créant pas de groupes carboxyle par élimination d'hydrogène ou de groupes fonctionnelsPréparation d'acides carboxyliques, de leurs sels, halogénures ou anhydrides par des réactions ne créant pas de groupes carboxyle par hydrogénolyse de groupes fonctionnels par décarboxylation
C07C 59/353 - Composés saturés comportant plusieurs groupes carboxyle contenant des groupes cétone contenant des cycles
C07C 45/63 - Préparation de composés comportant des groupes C=O liés uniquement à des atomes de carbone ou d'hydrogènePréparation des chélates de ces composés par des réactions ne créant pas de groupe C=O par introduction d'atomes d'halogènePréparation de composés comportant des groupes C=O liés uniquement à des atomes de carbone ou d'hydrogènePréparation des chélates de ces composés par des réactions ne créant pas de groupe C=O par substitution d'atomes d'halogène par des atomes d'autres halogènes
C07C 51/09 - Préparation d'acides carboxyliques, de leurs sels, halogénures ou anhydrides à partir de lactones ou d'esters d'acides carboxyliques
C07C 67/343 - Préparation d'esters d'acides carboxyliques par modification de la partie acide de l'ester sans introduction d'un groupe ester par isomérisationPréparation d'esters d'acides carboxyliques par modification de la partie acide de l'ester sans introduction d'un groupe ester par modification de la taille du squelette carboné par augmentation du nombre d'atomes de carbone
C07C 45/72 - Préparation de composés comportant des groupes C=O liés uniquement à des atomes de carbone ou d'hydrogènePréparation des chélates de ces composés par des réactions ne créant pas de groupe C=O par isomérisationPréparation de composés comportant des groupes C=O liés uniquement à des atomes de carbone ou d'hydrogènePréparation des chélates de ces composés par des réactions ne créant pas de groupe C=O par modification de la taille du squelette carboné par augmentation du nombre d'atomes de carbone par réaction de composés comportant des groupes C=O sur eux-mêmes ou avec d'autres composés comportant des groupes C=O
C07C 45/54 - Préparation de composés comportant des groupes C=O liés uniquement à des atomes de carbone ou d'hydrogènePréparation des chélates de ces composés par pyrolyse, réarrangement ou décomposition de composés contenant des atomes d'oxygène liés par des liaisons doubles, p. ex. d'esters
C07C 37/07 - Préparation de composés comportant des groupes hydroxyle ou O-métal liés à un atome de carbone d'un cycle aromatique à six chaînons par conversion de cycles non aromatiques à six chaînons ou de tels cycles formés in situ, en cycles aromatiques à six chaînons, p. ex. par déshydrogénation avec réduction simultanée du groupe C=O de ce cycle
C07C 50/24 - Quinones contenant des atomes d'halogène
C07C 67/293 - Préparation d'esters d'acides carboxyliques par modification de la partie hydroxyle de l'ester sans introduction d'un groupe ester par isomérisationPréparation d'esters d'acides carboxyliques par modification de la partie hydroxyle de l'ester sans introduction d'un groupe ester par modification de la taille du squelette carboné
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for human use for the treatment of dermatitis and acne; biologic preparations for medical and therapeutic purposes for the treatment of dermatitis and acne; pharmaceutical preparations and biologic preparations for the treatment of skin diseases and disorders; pharmaceutical preparations and biologic preparations for the treatment of psoriasis and atopic dermatitis
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
(1) Pharmaceutical preparations for human use for inflammatory diseases and disorders, namely arthritis, rheumatoid arthritis, inflammatory bowel diseases, inflammatory connective tissue diseases, vasculitis, synovitis, inflammatory-related pain, inflammatory connective tissue diseases and injuries; anti-inflammatory pharmaceutical preparations; biologic preparations for medical and therapeutic purposes for inflammatory diseases and disorders, namely arthritis, rheumatoid arthritis, inflammatory bowel diseases, inflammatory connective tissue diseases, vasculitis, synovitis, inflammatory-related pain, inflammatory connective tissue diseases and injuries; anti-inflammatory biologic preparations; pharmaceutical preparations and biologic preparations for the treatment of skin diseases and disorders namely dermatitis, skin and skin structure infections namely bacterial skin infections, fungal skin infections, viral skin infections and parasitic skin infections, psoriasis, eczema and sexually transmitted diseases, and for the treatment of damaged skin and tissue namely bee stings, sunburn, rashes, sores, corns, calluses and acne; pharmaceutical preparations and biologic preparations for the treatment of psoriasis and atopic dermatitis.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
(1) Pharmaceutical preparations for human use for inflammatory diseases and disorders, namely arthritis, rheumatoid arthritis, inflammatory bowel diseases, inflammatory connective tissue diseases, vasculitis, synovitis, inflammatory-related pain, inflammatory connective tissue diseases and injuries; anti-inflammatory pharmaceutical preparations; biologic preparations for medical and therapeutic purposes for inflammatory diseases and disorders, namely arthritis, rheumatoid arthritis, inflammatory bowel diseases, inflammatory connective tissue diseases, vasculitis, synovitis, inflammatory-related pain, inflammatory connective tissue diseases and injuries; anti-inflammatory biologic preparations; pharmaceutical preparations and biologic preparations for the treatment of skin diseases and disorders namely dermatitis, skin and skin structure infections namely bacterial skin infections, fungal skin infections, viral skin infections and parasitic skin infections, psoriasis, eczema and sexually transmitted diseases, and for the treatment of damaged skin and tissue namely bee stings, sunburn, rashes, sores, corns, calluses and acne; pharmaceutical preparations and biologic preparations for the treatment of psoriasis and atopic dermatitis.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
(1) Pharmaceutical preparations for human use for inflammatory diseases and disorders, namely arthritis, rheumatoid arthritis, inflammatory bowel diseases, inflammatory connective tissue diseases, vasculitis, synovitis, inflammatory-related pain, inflammatory connective tissue diseases and injuries; anti-inflammatory pharmaceutical preparations; biologic preparations for medical and therapeutic purposes for inflammatory diseases and disorders, namely arthritis, rheumatoid arthritis, inflammatory bowel diseases, inflammatory connective tissue diseases, vasculitis, synovitis, inflammatory-related pain, inflammatory connective tissue diseases and injuries; anti-inflammatory biologic preparations; pharmaceutical preparations and biologic preparations for the treatment of skin diseases and disorders namely dermatitis, skin and skin structure infections namely bacterial skin infections, fungal skin infections, viral skin infections and parasitic skin infections, psoriasis, eczema and sexually transmitted diseases, and for the treatment of damaged skin and tissue namely bee stings, sunburn, rashes, sores, corns, calluses and acne; pharmaceutical preparations and biologic preparations for the treatment of psoriasis and atopic dermatitis.
45.
CERDULATINIB-CONTAINING TOPICAL SKIN PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
Embodiments described herein are directed to topical compositions for administering cerdulatinib or a pharmaceutically acceptable salt, hydrate or solvate thereof. Embodiments described herein are also directed to methods for preparing the topical compositions. The disclosed compositions are suitable for the treatment of dermatologic conditions such as atopic dermatitis, cutaneous lupus, lichen planus, cutaneous graft versus host disease, contact dermatitis, psoriasis, rosacea, scleroderma, morphea and dermatomyositis.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for human use for the treatment of dermatitis and acne; biologic preparations for medical and therapeutic purposes for the treatment of dermatitis and acne; pharmaceutical preparations and biologic preparations for the treatment of skin diseases and disorders; pharmaceutical preparations and biologic preparations for the treatment of psoriasis and atopic dermatitis
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical preparations for human use for the treatment of dermatitis and acne; biologic preparations for medical and therapeutic purposes for the treatment of dermatitis and acne; pharmaceutical preparations and biologic preparations for the treatment of skin diseases and disorders; pharmaceutical preparations and biologic preparations for the treatment of psoriasis and atopic dermatitis
The present invention relates to topical pharmaceutical emulsion compositions comprising a therapeutically effective amount of 3,5-Dihydroxy-4-isopropyl-trans-stilbene or a pharmaceutically acceptable salt thereof, an oil phase, a water phase, a surfactant, and an antioxidant, and wherein the emulsion composition is homogeneous and/or the active is solubilized in the oil phase. The invention also relates to methods of treating a dermatological condition or disorder in a patient by administering the present compositions to the skin of the patient.
A61K 47/06 - Composés organiques, p. ex. hydrocarbures naturels ou synthétiques, polyoléfines, huile minérale, gelée de pétrole ou ozocérite
A61K 47/44 - Huiles, graisses ou cires couvertes par plus d’un des groupes Huiles, graisses ou cires naturelles ou naturelles modifiées, p. ex. huile de ricin, huile de ricin polyéthoxylée, cire de lignite, lignite, gomme-laque, colophane, cire d’abeille ou lanoline
A61K 47/08 - Composés organiques, p. ex. hydrocarbures naturels ou synthétiques, polyoléfines, huile minérale, gelée de pétrole ou ozocérite contenant de l'oxygène
A61K 47/10 - AlcoolsPhénolsLeurs sels, p. ex. glycérolPolyéthylène glycols [PEG]PoloxamèresAlkyléthers de PEG/POE
A61K 47/22 - Composés hétérocycliques, p. ex. acide ascorbique, tocophérol ou pyrrolidones
49.
TOPICAL FORMULATIONS OF DGAT1 INHIBITORS AND THEIR METHODS OF USE
Embodiments herein are directed to topical compositions comprising 2-(4-(4-(6-carbamoyl-3,5-dimethylpyrazin-2-yl)phenyl)cyclohexyl)acetic acid and a combination of one or more of the following components: benzyl alcohol, PEG 400, diisopropyl adipate, diethyl sebacate, dimethyl isosorbide, propylene glycol, 2-(2-ethoxyethoxy)ethanol, hexylene glycol, oleic acid, polysorbate 80, isopropyl myristate, glycerin, DMSO, water, butylated hydroxytoluene, phenoxyethanol, cellulose polymer, Carbomer Homopolymer Type B, and optionally one or more pharmaceutically acceptable topical excipients. The topical compositions may be used to treat a variety of skin conditions.
Embodiments herein are directed to topical compositions comprising 2-(4-(4-(6-carbamoyl-3,5-dimethylpyrazin-2-yl)phenyl)cyclohexyl)acetic acid and a combination of one or more of the following components: benzyl alcohol, PEG 400, diisopropyl adipate, diethyl sebacate, dimethyl isosorbide, propylene glycol, 2-(2-ethoxyethoxy)ethanol, hexylene glycol, oleic acid, polysorbate 80, isopropyl myristate, glycerin, DMSO, water, butylated hydroxytoluene, phenoxyethanol, cellulose polymer, Carbomer Homopolymer Type B, and optionally one or more pharmaceutically acceptable topical excipients. The topical compositions may be used to treat a variety of skin conditions.
A61K 31/495 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec deux azote comme seuls hétéro-atomes d'un cycle, p. ex. pipérazine
05 - Produits pharmaceutiques, vétérinaires et hygièniques
42 - Services scientifiques, technologiques et industriels, recherche et conception
44 - Services médicaux, services vétérinaires, soins d'hygiène et de beauté; services d'agriculture, d'horticulture et de sylviculture.
Produits et services
Pharmaceutical preparations for human use; biological
preparations for medical or therapeutic use. Scientific and technological services and research and
design relating thereto; pharmaceutical, biomedical and
biological therapeutic research services; research in the
field of pharmaceutical and biological therapeutic products,
clinical trials and post-authorization research for the
marketing of medicines and/or commercial post-launching of
medicines; pharmaceutical research and development;
providing scientific research information in the field of
pharmaceutical products, biomedicine, clinical trials and
post-authorization research for the marketing of medicines
and/or commercial post-launching of medicines. Providing health and medical information; providing
information relating to the diagnostic, prophylactic and
therapeutic properties of pharmaceutical and biological
products for the prevention and treatment of diseases,
disorders and conditions.
52.
CERDULATINIB-CONTAINING TOPICAL SKIN PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
Embodiments of topical formulations for administering cerdulatinib or a pharmaceutically acceptable salt, hydrate or solvate thereof are disclosed. Embodiments of methods for preparing the topical formulations are also disclosed. The disclosed formulations are suitable for the treatment of dermatologic conditions such as atopic dermatitis.
A61K 31/506 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime non condensées et contenant d'autres hétérocycles
A61K 47/08 - Composés organiques, p. ex. hydrocarbures naturels ou synthétiques, polyoléfines, huile minérale, gelée de pétrole ou ozocérite contenant de l'oxygène
A61K 47/10 - AlcoolsPhénolsLeurs sels, p. ex. glycérolPolyéthylène glycols [PEG]PoloxamèresAlkyléthers de PEG/POE
Embodiments of topical formulations for administering cerdulatinib or a pharmaceutically acceptable salt, hydrate or solvate thereof are disclosed. Embodiments of methods for preparing the topical formulations are also disclosed. The disclosed formulations are suitable for the treatment of dermatologic conditions such as atopic dermatitis.
A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
A61K 47/08 - Composés organiques, p. ex. hydrocarbures naturels ou synthétiques, polyoléfines, huile minérale, gelée de pétrole ou ozocérite contenant de l'oxygène
A61K 47/10 - AlcoolsPhénolsLeurs sels, p. ex. glycérolPolyéthylène glycols [PEG]PoloxamèresAlkyléthers de PEG/POE
The present invention relates to topical pharmaceutical emulsion compositions comprising a therapeutically effective amount of 3,5-Dihydroxy-4-isopropyl-trans-stilbene or a pharmaceutically acceptable salt thereof, an oil phase, a water phase, a surfactant, and an antioxidant, and wherein the emulsion composition is homogeneous and/or the active is solubilized in the oil phase. The invention also relates to methods of treating a dermatological condition or disorder in a patient by administering the present compositions to the skin of the patient.
A61K 47/06 - Composés organiques, p. ex. hydrocarbures naturels ou synthétiques, polyoléfines, huile minérale, gelée de pétrole ou ozocérite
A61K 47/44 - Huiles, graisses ou cires couvertes par plus d’un des groupes Huiles, graisses ou cires naturelles ou naturelles modifiées, p. ex. huile de ricin, huile de ricin polyéthoxylée, cire de lignite, lignite, gomme-laque, colophane, cire d’abeille ou lanoline
A61K 47/08 - Composés organiques, p. ex. hydrocarbures naturels ou synthétiques, polyoléfines, huile minérale, gelée de pétrole ou ozocérite contenant de l'oxygène
A61K 47/10 - AlcoolsPhénolsLeurs sels, p. ex. glycérolPolyéthylène glycols [PEG]PoloxamèresAlkyléthers de PEG/POE
A61K 47/22 - Composés hétérocycliques, p. ex. acide ascorbique, tocophérol ou pyrrolidones
The present invention relates to topical pharmaceutical emulsion compositions comprising a therapeutically effective amount of 3,5-Dihydroxy-4-isopropyl-trans-stilbene or a pharmaceutically acceptable salt thereof, an oil phase, a water phase, a surfactant, and an antioxidant, and wherein the emulsion composition is homogeneous and/or the active is solubilized in the oil phase. The invention also relates to methods of treating a dermatological condition or disorder in a patient by administering the present compositions to the skin of the patient.
A61K 47/10 - AlcoolsPhénolsLeurs sels, p. ex. glycérolPolyéthylène glycols [PEG]PoloxamèresAlkyléthers de PEG/POE
A61K 47/44 - Huiles, graisses ou cires couvertes par plus d’un des groupes Huiles, graisses ou cires naturelles ou naturelles modifiées, p. ex. huile de ricin, huile de ricin polyéthoxylée, cire de lignite, lignite, gomme-laque, colophane, cire d’abeille ou lanoline
A61K 9/113 - Émulsions multiples, p. ex. huile-dans l'eau-dans l'huile
A61K 47/06 - Composés organiques, p. ex. hydrocarbures naturels ou synthétiques, polyoléfines, huile minérale, gelée de pétrole ou ozocérite
A61K 47/08 - Composés organiques, p. ex. hydrocarbures naturels ou synthétiques, polyoléfines, huile minérale, gelée de pétrole ou ozocérite contenant de l'oxygène
A61K 47/22 - Composés hétérocycliques, p. ex. acide ascorbique, tocophérol ou pyrrolidones
56.
TOPICAL OINTMENT FORMULATIONS AND THEIR USE IN TREATING SKIN CONDITIONS
Embodiments herein are directed to topical compositions comprising PEG 400, PEG 4000, white petrolatum, vitamin E, glycerol monostearate/glycerides, isopropyl myristate, and water. Embodiments herein are directed to topical compositions comprising PEG 400, PEG 4000, white petrolatum, vitamin E, glycerol monostearate/glycerides, isopropyl myristate, water and a topically active therapeutic agent. The topical compositions may be used to treat a variety of skin conditions, including atopic dermatitis.
Embodiments herein are directed to topical compositions comprising a therapeutically effective amount of methyl N-[3-(6,7-dimethoxy-2-methylaminoquinazolin-4-yl)phenyl]terephthalamic acid, PEG 400, PEG 4000, white petrolatum, vitamin E, glycerol monostearate/glycerides, isopropyl myristate, and water. The topical compositions may be used to treat a variety of skin conditions, including atopic dermatitis. Patients treated include pediatrics, adolescents and adults.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
42 - Services scientifiques, technologiques et industriels, recherche et conception
Produits et services
(1) Pharmaceutical preparations for human use for use in dermatology, namely, dermatitis, atopic dermatitis, acne vulgaris, vitiligo, hyperhidrosis, eczema, psoriasis, vitiligo, and skin pigmentation diseases; biologic preparations for medical and therapeutic purposes for use in dermatology, namely, dermatitis, atopic dermatitis, acne vulgaris, vitiligo, hyperhidrosis, eczema, psoriasis, vitiligo, and skin pigmentation diseases (1) Scientific and technological services and research and design relating thereto, namely, medical research, scientific research and analysis in the fields of pharmaceuticals, biomedicine, clinical trials and post-market trials; pharmaceutical, biomedical and biological therapeutic research services; research in the fields of pharmaceutical and biologic therapeutic preparations, clinical trials and post-market trials; pharmaceutical research and development; providing scientific research information in the fields of pharmaceuticals, biomedicine, clinical trials and post-market trials.
The present invention relates to topical pharmaceutical emulsion compositions comprising a therapeutically effective amount of 3,5-Dihydroxy-4-isopropyl-trans-stilbene or a pharmaceutically acceptable salt thereof, an oil phase, a water phase, a surfactant, and an antioxidant, and wherein the emulsion composition is homogeneous and/or the active is solubilized in the oil phase. The invention also relates to methods of treating a dermatological condition or disorder in a patient by administering the present compositions to the skin of the patient.
A61K 47/44 - Huiles, graisses ou cires couvertes par plus d’un des groupes Huiles, graisses ou cires naturelles ou naturelles modifiées, p. ex. huile de ricin, huile de ricin polyéthoxylée, cire de lignite, lignite, gomme-laque, colophane, cire d’abeille ou lanoline
A61K 47/06 - Composés organiques, p. ex. hydrocarbures naturels ou synthétiques, polyoléfines, huile minérale, gelée de pétrole ou ozocérite
A61K 47/08 - Composés organiques, p. ex. hydrocarbures naturels ou synthétiques, polyoléfines, huile minérale, gelée de pétrole ou ozocérite contenant de l'oxygène
A61K 47/10 - AlcoolsPhénolsLeurs sels, p. ex. glycérolPolyéthylène glycols [PEG]PoloxamèresAlkyléthers de PEG/POE
A61K 47/22 - Composés hétérocycliques, p. ex. acide ascorbique, tocophérol ou pyrrolidones
There is a need for large-scale production of antibacterials, antioxidants and therapeutic compounds including anti-cancer compounds with low toxicity. The present invention provides processes for the preparation of 3, 5-Dihydroxy-4-isopropyl-trans-stilbene or a salt or solvate thereof and intermediates used therein. The processes comprise decarboxylation, esterification, cyclization, halogenation and aromatization. In some embodiments the 3, 5-Dihydroxy-4-isopropyl-trans-stilbene is prepared from (E)-2-chloro- 2-isopropyl-5-styrylcyclohexane-l,3-dione. Also disclosed are crystal forms of 3, 5- Dihydroxy-4-isopropyl-trans-stilbene or a salt or solvate thereof and pharmaceutical compositions comprising same. The compounds and processes of the present invention can be manufactured on a larger scale, including with high-yielding synthesis, and have low toxicity.
C07C 37/07 - Préparation de composés comportant des groupes hydroxyle ou O-métal liés à un atome de carbone d'un cycle aromatique à six chaînons par conversion de cycles non aromatiques à six chaînons ou de tels cycles formés in situ, en cycles aromatiques à six chaînons, p. ex. par déshydrogénation avec réduction simultanée du groupe C=O de ce cycle
C07C 39/23 - Composés comportant au moins un groupe hydroxyle ou O-métal lié à un atome de carbone d'un cycle aromatique à six chaînons polycycliques contenant des cycles aromatiques à six chaînons et d'autres cycles avec une insaturation autre que celle des cycles aromatiques
C07C 45/68 - Préparation de composés comportant des groupes C=O liés uniquement à des atomes de carbone ou d'hydrogènePréparation des chélates de ces composés par des réactions ne créant pas de groupe C=O par isomérisationPréparation de composés comportant des groupes C=O liés uniquement à des atomes de carbone ou d'hydrogènePréparation des chélates de ces composés par des réactions ne créant pas de groupe C=O par modification de la taille du squelette carboné par augmentation du nombre d'atomes de carbone
C07C 49/693 - Composés non saturés comportant un groupe cétone faisant partie d'un cycle contenant des atomes d'halogène polycycliques
C07C 67/08 - Préparation d'esters d'acides carboxyliques par réaction d'acides carboxyliques ou d'anhydrides symétriques avec le groupe hydroxyle ou O-métal de composés organiques
C07C 69/732 - Esters d'acides carboxyliques dont le groupe carboxyle estérifié est lié à un atome de carbone acyclique et dont l'un des groupes OH, O-métal, —CHO, céto, éther, acyloxy, des groupes , des groupes ou des groupes se trouve dans la partie acide d'acides non saturés d'acides hydroxycarboxyliques non saturés
The present invention provides processes for the preparation of 3, 5-Dihydroxy-4-isopropyl-trans-stilbene or a salt or solvate thereof and novel intermediates used therein. In some embodiments the 3, 5-Dihydroxy-4-isopropyl-trans-stilbene is prepared from (E)-2-chloro-2-isopropyl-5-styrylcyclohexane-1,3-dione. Also disclosed are crystal forms of 3, 5-Dihydroxy-4-isopropyl-trans-stilbene or a salt or solvate thereof and pharmaceutical compositions comprising same.
A61K 31/00 - Préparations médicinales contenant des ingrédients actifs organiques
C07C 50/24 - Quinones contenant des atomes d'halogène
C07C 51/38 - Préparation d'acides carboxyliques, de leurs sels, halogénures ou anhydrides par des réactions ne créant pas de groupes carboxyle par élimination d'hydrogène ou de groupes fonctionnelsPréparation d'acides carboxyliques, de leurs sels, halogénures ou anhydrides par des réactions ne créant pas de groupes carboxyle par hydrogénolyse de groupes fonctionnels par décarboxylation
C07C 67/03 - Préparation d'esters d'acides carboxyliques par réaction d'un groupe ester avec un groupe hydroxyle
C07C 67/293 - Préparation d'esters d'acides carboxyliques par modification de la partie hydroxyle de l'ester sans introduction d'un groupe ester par isomérisationPréparation d'esters d'acides carboxyliques par modification de la partie hydroxyle de l'ester sans introduction d'un groupe ester par modification de la taille du squelette carboné
C07C 59/353 - Composés saturés comportant plusieurs groupes carboxyle contenant des groupes cétone contenant des cycles
C07C 45/63 - Préparation de composés comportant des groupes C=O liés uniquement à des atomes de carbone ou d'hydrogènePréparation des chélates de ces composés par des réactions ne créant pas de groupe C=O par introduction d'atomes d'halogènePréparation de composés comportant des groupes C=O liés uniquement à des atomes de carbone ou d'hydrogènePréparation des chélates de ces composés par des réactions ne créant pas de groupe C=O par substitution d'atomes d'halogène par des atomes d'autres halogènes
C07C 51/09 - Préparation d'acides carboxyliques, de leurs sels, halogénures ou anhydrides à partir de lactones ou d'esters d'acides carboxyliques
C07C 67/343 - Préparation d'esters d'acides carboxyliques par modification de la partie acide de l'ester sans introduction d'un groupe ester par isomérisationPréparation d'esters d'acides carboxyliques par modification de la partie acide de l'ester sans introduction d'un groupe ester par modification de la taille du squelette carboné par augmentation du nombre d'atomes de carbone
C07C 45/72 - Préparation de composés comportant des groupes C=O liés uniquement à des atomes de carbone ou d'hydrogènePréparation des chélates de ces composés par des réactions ne créant pas de groupe C=O par isomérisationPréparation de composés comportant des groupes C=O liés uniquement à des atomes de carbone ou d'hydrogènePréparation des chélates de ces composés par des réactions ne créant pas de groupe C=O par modification de la taille du squelette carboné par augmentation du nombre d'atomes de carbone par réaction de composés comportant des groupes C=O sur eux-mêmes ou avec d'autres composés comportant des groupes C=O
C07C 45/54 - Préparation de composés comportant des groupes C=O liés uniquement à des atomes de carbone ou d'hydrogènePréparation des chélates de ces composés par pyrolyse, réarrangement ou décomposition de composés contenant des atomes d'oxygène liés par des liaisons doubles, p. ex. d'esters
C07C 37/07 - Préparation de composés comportant des groupes hydroxyle ou O-métal liés à un atome de carbone d'un cycle aromatique à six chaînons par conversion de cycles non aromatiques à six chaînons ou de tels cycles formés in situ, en cycles aromatiques à six chaînons, p. ex. par déshydrogénation avec réduction simultanée du groupe C=O de ce cycle
C07C 39/00 - Composés comportant au moins un groupe hydroxyle ou O-métal lié à un atome de carbone d'un cycle aromatique à six chaînons
C07C 39/205 - Composés comportant au moins un groupe hydroxyle ou O-métal lié à un atome de carbone d'un cycle aromatique à six chaînons polycycliques ne contenant que des cycles aromatiques à six chaînons dans la partie cyclique, avec une insaturation autre que celle des cycles
C07C 39/21 - Composés comportant au moins un groupe hydroxyle ou O-métal lié à un atome de carbone d'un cycle aromatique à six chaînons polycycliques ne contenant que des cycles aromatiques à six chaînons dans la partie cyclique, avec une insaturation autre que celle des cycles au moins un groupe hydroxyle étant lié à un cycle non condensé
05 - Produits pharmaceutiques, vétérinaires et hygièniques
42 - Services scientifiques, technologiques et industriels, recherche et conception
44 - Services médicaux, services vétérinaires, soins d'hygiène et de beauté; services d'agriculture, d'horticulture et de sylviculture.
Produits et services
Pharmaceutical preparations for human use for the treatment of dermatological diseases, disorders and conditions; biologic preparations for medical and therapeutic purposes for the treatment of dermatological diseases, disorders and conditions Scientific and technological services, namely, medical research, scientific research and analysis in the field of pharmaceuticals and biomedicine; pharmaceutical, biomedical and biological therapeutic research services; scientific research in the fields of pharmaceutical and biologic therapeutic preparations, clinical trials and post-market trials; pharmaceutical research and development; providing scientific research information in the fields of pharmaceuticals, biomedicine, clinical trials and post-market trials Providing health and medical information; providing information relating to the diagnostic, prophylactic and therapeutic properties of pharmaceutical preparations and biologic preparations for the prevention and treatment of diseases, disorders and conditions
42 - Services scientifiques, technologiques et industriels, recherche et conception
Produits et services
(1) Scientific and technological services, namely, medical research, scientific research and analysis in the fields of pharmaceuticals, biomedicine, clinical trials and post-market trials; pharmaceutical, biomedical and biological therapeutic research services; research in the fields of pharmaceutical and biologic therapeutic preparations and post-market trials; pharmaceutical research and development; providing scientific research information in the fields of pharmaceuticals, biomedicine, clinical trials and post-market trials.
(2) Research in the fields of pharmaceutical and biologic therapeutic preparations, namely clinical trials.
42 - Services scientifiques, technologiques et industriels, recherche et conception
Produits et services
Scientific and technological services and research and design relating thereto; pharmaceutical, biomedical and biological therapeutic research services; research in the fields of pharmaceutical and biologic therapeutic preparations, clinical trials and post-market trials; pharmaceutical research and development; providing scientific research information in the fields of pharmaceuticals, biomedicine, clinical trials and post-market trials.
42 - Services scientifiques, technologiques et industriels, recherche et conception
Produits et services
Scientific and technological services, namely, medical research, scientific research and analysis in the field of pharmaceuticals and biomedicine; pharmaceutical, biomedical and biological therapeutic research services; scientific research in the fields of pharmaceutical and biologic therapeutic preparations, clinical trials and post-market trials; pharmaceutical research and development; providing scientific research information in the fields of pharmaceuticals, biomedicine, clinical trials and post-market trials
The present invention relates to topical pharmaceutical emulsion compositions comprising a therapeutically effective amount of 3,5-Dihydroxy-4-isopropyl-trans-stilbene or a pharmaceutically acceptable salt thereof, an oil phase, a water phase, a surfactant, and an antioxidant, and wherein the emulsion composition is homogeneous and/or the active is solubilized in the oil phase. The invention also relates to methods of treating a dermatological condition or disorder in a patient by administering the present compositions to the skin of the patient.
A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
A61K 47/26 - Hydrates de carbone, p. ex. polyols ou sucres alcoolisés, sucres aminés, acides nucléiques, mono-, di- ou oligosaccharidesLeurs dérivés, p. ex. polysorbates, esters d’acide gras de sorbitan ou glycyrrhizine
A61K 47/06 - Composés organiques, p. ex. hydrocarbures naturels ou synthétiques, polyoléfines, huile minérale, gelée de pétrole ou ozocérite
A61K 47/14 - Esters d’acides carboxyliques, p. ex. acides gras monoglycérides, triglycérides à chaine moyenne, parabènes ou esters d’acide gras de PEG
05 - Produits pharmaceutiques, vétérinaires et hygièniques
44 - Services médicaux, services vétérinaires, soins d'hygiène et de beauté; services d'agriculture, d'horticulture et de sylviculture.
Produits et services
Pharmaceutical and biological preparations for medical purposes, namely, to treat dermatological conditions Providing health and medical information via a website; providing information relating to the diagnostic, prophylactic and therapeutic properties of pharmaceutical preparations and biologic preparations for the prevention and treatment of diseases, disorders and conditions via a website
The present invention relates to a novel method of treatment of acne in a human patient in need thereof, comprising administering topically to said patient an effective amount of the compound 3,5-Dihydroxy-4-isopropyl-trans-stilbene (Compound 1) or a pharmaceutically acceptable salt thereof.
Embodiments herein are directed to topical formulations of a compound represented by the formula (I), salt, metabolite, prodrug, or hydrate thereof along with a solvent, and a base. The compound is a PDE4 inhibitor and the topical formulations may be used to treat dermatological conditions such as, but not limited to, atopic dermatitis, seborrheic dermatitis, alopecia, contact dermatitis, psoriasis, urticaria, eczema, burns, sunburn, pancreatitis, hepatitis, lichen planus, scleritis, scleroderma, dermatomyositis, itching associated with any of the preceding conditions or a combination thereof.
A61K 31/517 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des systèmes carbocycliques, p. ex. quinazoline, périmidine
Embodiments herein are directed to topical formulations of a compound represented by the formula (I), salt, metabolite, prodrug, or hydrate thereof along with a solvent, and a base. The compound is a PDE4 inhibitor and the topical formulations may be used to treat dermatological conditions such as, but not limited to, atopic dermatitis, seborrheic dermatitis, alopecia, contact dermatitis, psoriasis, urticaria, eczema, burns, sunburn, pancreatitis, hepatitis, lichen planus, scleritis, scleroderma, dermatomyositis, itching associated with any of the preceding conditions or a combination thereof.
A61K 31/517 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des systèmes carbocycliques, p. ex. quinazoline, périmidine
A61K 47/06 - Composés organiques, p. ex. hydrocarbures naturels ou synthétiques, polyoléfines, huile minérale, gelée de pétrole ou ozocérite
A61K 47/10 - AlcoolsPhénolsLeurs sels, p. ex. glycérolPolyéthylène glycols [PEG]PoloxamèresAlkyléthers de PEG/POE
A61K 47/14 - Esters d’acides carboxyliques, p. ex. acides gras monoglycérides, triglycérides à chaine moyenne, parabènes ou esters d’acide gras de PEG
A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
The present invention relates to topical pharmaceutical emulsion compositions comprising a therapeutically effective amount of 3,5-Dihydroxy-4-isopropyl-trans,-stilbene or a pharmaceutically acceptable salt thereof, an oil phase, a water phase, a surfactant, and an antioxidant, and wherein the emulsion composition is homogeneous and/or the active is solubilized in the oil phase. The invention also relates to methods of treating a dermatological condition or disorder in a patient by administering the present compositions to the skin of the patient.
A61K 47/00 - Préparations médicinales caractérisées par les ingrédients non actifs utilisés, p. ex. les supports ou les additifs inertesAgents de ciblage ou de modification chimiquement liés à l’ingrédient actif
A61P 17/00 - Médicaments pour le traitement des troubles dermatologiques
The present invention relates to topical pharmaceutical emulsion compositions comprising a therapeutically effective amount of 3,5-Dihydroxy-4-isopropyl-trans-stilbene or a pharmaceutically acceptable salt thereof, an oil phase, a water phase, a surfactant, and an antioxidant, and wherein the emulsion composition is homogeneous and/or the active is solubilized in the oil phase. The invention also relates to methods of treating a dermatological condition or disorder in a patient by administering the present compositions to the skin of the patient.
A61K 47/08 - Composés organiques, p. ex. hydrocarbures naturels ou synthétiques, polyoléfines, huile minérale, gelée de pétrole ou ozocérite contenant de l'oxygène
A61K 47/10 - AlcoolsPhénolsLeurs sels, p. ex. glycérolPolyéthylène glycols [PEG]PoloxamèresAlkyléthers de PEG/POE
A61K 47/22 - Composés hétérocycliques, p. ex. acide ascorbique, tocophérol ou pyrrolidones
A61K 47/44 - Huiles, graisses ou cires couvertes par plus d’un des groupes Huiles, graisses ou cires naturelles ou naturelles modifiées, p. ex. huile de ricin, huile de ricin polyéthoxylée, cire de lignite, lignite, gomme-laque, colophane, cire d’abeille ou lanoline
05 - Produits pharmaceutiques, vétérinaires et hygièniques
41 - Éducation, divertissements, activités sportives et culturelles
42 - Services scientifiques, technologiques et industriels, recherche et conception
44 - Services médicaux, services vétérinaires, soins d'hygiène et de beauté; services d'agriculture, d'horticulture et de sylviculture.
Produits et services
(1) Pharmaceutical preparations for use in dermatology, namely, dermatitis, atopic dermatitis, acne vulgaris, vitiligo, hyperhidrosis, eczema, psoriasis, vitiligo, and skin pigmentation diseases (1) Information services in the health and medical fields, namely, providing a website featuring information about pharmaceutical drug development
(2) Internet-based health care information services namely a website featuring information about health issues, diseases and related medical treatments in the field of dermatology; providing medical information regarding health issues, diseases and related medical treatments in the field of dermatology; providing health care information pertaining to the treatment of skin diseases and conditions; educational services, namely, providing information in the fields of health, namely, dermatology
The present invention relates to a novel method of treatment of acne in a human patient in need thereof, comprising administering topically to said patient an effective amount of the compound 3,5-Dihydroxy-4-isopropyl-trans-stilbene (Compound 1) or a pharmaceutically acceptable salt thereof.
The invention provides novel 1,2-diphenylethene derivatives and pharmaceutically acceptable salts thereof, the process for production of these compounds and their pharmaceutical composition and the use of these compounds as modulators of T-cells, neutrophils, macrophages and their associated cytokines as agents for treating immune, inflammatory and auto-immune diseases.
