The present disclosure provides a process for the preparation of 3,5-Dihydroxy-4-isopropyl-trans-stilbene [Tapinarof] and related compounds. Aryl hydrocarbon receptor (AHR) agonists are a novel class of drugs for topical treatment of plaque psoriasis in adults. AHR agonists are believed to inhibiting the release of proinflammatory proteins (cytokines) and downregulating inflammation. 3,5-Dihydroxy-4-isopropyl-trans-stilbene, also known as (E)-2-isopropyl-5-styrylbenzene-1,3-diol or Tapinarof, is a naturally occurring compound found in bacterial symbionts of nematodes.
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
C07C 37/055 - 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'un groupe lié au cycle par un oxygène, p. ex. d'un groupe éther
The present disclosure provides a process for the preparation of Trifarotene. The disclosure also provides for intermediates in the process described herein. Also provided are methods of making polymorph Form E of Trifarotene.
C07D 207/06 - Composés hétérocycliques contenant des cycles à cinq chaînons, non condensés avec d'autres cycles, ne comportant qu'un atome d'azote comme unique hétéro-atome du cycle avec uniquement des atomes d'hydrogène ou de carbone liés directement à l'atome d'azote du cycle ne comportant pas de liaison double entre chaînons cycliques ou entre chaînons cycliques et chaînons non cycliques avec des radicaux contenant uniquement des atomes d'hydrogène et de carbone, liés aux atomes de carbone du cycle
The present disclosure provides an oral care device including a hollow shaft (120, 920, 1320), a sleeve (110, 910, 1310), and a cleaning portion (115). The hollow shaft can include a first end having a first suction aperture (140, 940, 1340), and a second end having a second suction aperture (125, 925). The hollow shaft can be configured for insertion into a hand grip. The sleeve can surround the hollow shaft of the oral care device, and can be configured to slide along a longitudinal axis and conceal at least a portion of the first suction aperture or the second suction aperture. The sleeve can conceal the first suction aperture or the second suction aperture to easily adjust an amount of suction provided to an oral cavity of a patient. The cleaning portion can be coupled to a portion of the sleeve at the first end of the hollow shaft.
The present disclosure provides a topical sprayable composition comprising: (a) about 0.05% to about 5% by weight naftifine or pharmaceutical acceptable salt thereof, (b) a film forming agent comprising octylacrylamide acrylate copolymer and, (c) an alcoholic solvent, topical spray composition wherein the ratio of the alcoholic solvent to the propellant in the composition is about 1:1 to about 3:1 (w/w). The disclosure also provides a method of treating a dermatophyte skin infection or onychomycosis in a subject in need thereof, the method comprising topically administering to the subject the topical compositions as described herein.
A61K 47/32 - Composés macromoléculaires obtenus par des réactions faisant intervenir uniquement des liaisons non saturées carbone-carbone, p. ex. carbomères
A61K 47/06 - Composés organiques, p. ex. hydrocarbures naturels ou synthétiques, polyoléfines, huile minérale, gelée de pétrole ou ozocérite
A61P 17/00 - Médicaments pour le traitement des troubles dermatologiques
The present disclosure provides a topical sprayable composition comprising: (a) about 0.05% to about 5% by weight naftifine or pharmaceutical acceptable salt thereof, (b) a film forming agent comprising octylacrylamide acrylate copolymer and, (c) an alcoholic solvent, topical spray composition wherein the ratio of the alcoholic solvent to the propellant in the composition is about 1:1 to about 3:1 (w/w). The disclosure also provides a method of treating a dermatophyte skin infection or onychomycosis in a subject in need thereof, the method comprising topically administering to the subject the topical composition s as described herein.
The present disclosure provides methods of treating an inflammatory ocular condition, the methods comprising topically administering to an ocular surface of a subject in need thereof a composition comprising an allylamine, for example, terbinafine, naftifine, or a pharmaceutically acceptable salt, conjugate or derivative thereof. The present disclosure also provides methods of treating an ocular condition selected from keratitis, chronic conjunctivitis, allergic conjunctivitis, dry-eye disease, blepharitis, uveitis or combinations thereof, the methods comprising topically administering to an ocular surface of a subject in need thereof a composition comprising an allylamine, for example, terbinafine or pharmaceutically acceptable salt, conjugate or derivative thereof.
Yissum Research Development Company of the Hebrew University of Jerusalem Ltd. (Israël)
Inventeur(s)
Khan, Wahid
Shifrin, Helena
Schlinger, Ron
Avramoff, Avi
Domb, Abraham Jacob
Abrégé
Embodiments of stable topical compositions for administering fenoldopam (compound (I) or a pharmaceutically acceptable salt or solvate thereof are disclosed for immediate or continued slow release administration, over prolonged periods of time with safe minimal systemic exposure of fenoldopam (reducing the risk for lowering blood pressure). The compositions include those compositions that increase the stability and skin absorption of the drug, particularly anhydrous semi-solid compositions and creams. This is accomplished by incorporating fenoldopam in soluble or dispersed form into semi-solid compositions like ointments or anhydrous gels that are not irritative. Embodiments of methods for using the topical compositions in the treatment of dermatological disorders including psoriasis, alopecia atopic dermatitis and vitiligo are disclosed.
Embodiments of stable topical compositions for administering fenoldopam (compound (I) or a pharmaceutically acceptable salt or solvate thereof are disclosed for immediate or continued slow release administration, over prolonged periods of time with safe minimal systemic exposure of fenoldopam (reducing the risk for lowering blood pressure). The compositions include those compositions that increase the stability and skin absorption of the drug, particularly anhydrous semi-solid compositions and creams. This is accomplished by incorporating fenoldopam in soluble or dispersed form into semi-solid compositions like ointments or anhydrous gels that are not irritative. Embodiments of methods for using the topical compositions in the treatment of dermatological disorders including psoriasis, alopecia atopic dermatitis and vitiligo are disclosed.
A61K 31/55 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à sept chaînons, p. ex. azélastine, pentylènetétrazole
A61K 45/06 - Mélanges d'ingrédients actifs sans caractérisation chimique, p. ex. composés antiphlogistiques et pour le cœur
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 47/12 - Acides carboxyliquesLeurs sels ou anhydrides
A61K 47/32 - Composés macromoléculaires obtenus par des réactions faisant intervenir uniquement des liaisons non saturées carbone-carbone, p. ex. carbomères
An oral care device includes a housing having a first end and a second end. The first end of the housing includes an opening that receives an external suction tube. The second end of the housing includes a cleaning portion. The oral care device includes a hollow tube disposed within the housing and configured to couple with the external suction tube. The hollow tube includes a suction aperture at an end proximate to the cleaning portion of the housing. The hollow tube is configured to slide within the housing to expose or conceal the suction aperture. The oral care device includes a fluid dispenser coupled to the housing and fluidly coupled to at least one channel defined in part by the housing.
A61C 17/12 - Dispositifs de commande, p. ex. pour l'aspiration
A61C 17/22 - Dispositifs à entraînement mécanique pour nettoyer ou pour polir avec des brosses, des éponges, des cupules ou analogues
A46B 9/04 - Position ou disposition des soies par rapport à la surface de la monture, p. ex. inclinées, en rangées, en groupes pour les brosses à dents
A46B 11/00 - Brosses à réservoir ou autre système permettant l'application de produits, p. ex. peintures, pâtes, eau
A46B 11/04 - Brosses à réservoir ou autre système permettant l'application de produits, p. ex. peintures, pâtes, eau avec écoulement du produit du réservoir autrement que par pression
10.
PREPARATION OF TRIFAROTENE AND INTERMEDIATES AND POLYMORPHS THEREOF
The present disclosure provides a process for the preparation of Trifarotene. The disclosure also provides novel intermediates in the process described herein. Also provided are novel polymorphs of Trifarotene.
The present disclosure provides a process for the preparation of Trifarotene. The disclosure also provides novel intermediates in the process described herein. Also provided are novel polymorphs of Trifarotene.
C07D 207/08 - Composés hétérocycliques contenant des cycles à cinq chaînons, non condensés avec d'autres cycles, ne comportant qu'un atome d'azote comme unique hétéro-atome du cycle avec uniquement des atomes d'hydrogène ou de carbone liés directement à l'atome d'azote du cycle ne comportant pas de liaison double entre chaînons cycliques ou entre chaînons cycliques et chaînons non cycliques avec des radicaux hydrocarbonés, substitués par des hétéro-atomes, liés aux atomes de carbone du cycle
11.
TOPICAL MONTELUKAST FOR TREATMENT OF ATOPIC DERMATITIS
A topical formulation comprising Montelukast or a pharmaceutically acceptable salt thereof, a gelling agent and water for the treatment of atopic dermatitis.
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
A61K 45/06 - Mélanges d'ingrédients actifs sans caractérisation chimique, p. ex. composés antiphlogistiques et pour le cœur
12.
TOPICAL CAPECITABINE FOR THE TREATMENT OF HYPERPROLIFERATIVE SKIN CONDITIONS
The present invention relates to a novel and unexpected method of using topical Capecitabine composition to obtain therapeutically effective amounts of fluorouracil (FU) within the skin of a subject afflicted with hyperproliferative or inflammatory skin condition. The method comprising topically administering a pharmaceutical composition comprising Capecitabine or a hydrate or solvate thereof to the affected area of the skin of the subject, to form therapeutically effective amounts of FU within the skin.
A61K 31/7068 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'azote comme hétéro-atome d'un cycle, p. ex. nucléosides, nucléotides contenant des cycles à six chaînons avec l'azote comme hétéro-atome d'un cycle contenant des pyrimidines condensées ou non-condensées ayant des groupes oxo liés directement au cycle pyrimidine, p. ex. cytidine, acide cytidylique
A61P 17/12 - Kératolytiques, p. ex. préparations pour le traitement des verrues ou des cors
A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
A61K 31/122 - Cétones ayant l'atome d'oxygène lié directement à un cycle, p. ex. quinones, vitamine K1, anthraline
A61K 31/196 - Acides carboxyliques, p. ex. acide valproïque ayant un groupe amino le groupe amino étant lié directement à un cycle, p. ex. acide anthranilique, acide méfénamique, diclofénac, chlorambucil
A61K 31/437 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec un azote comme seul hétéro-atome d'un cycle condensés en ortho ou en péri avec des systèmes hétérocycliques le système hétérocyclique contenant un cycle à cinq chaînons ayant l'azote comme hétéro-atome du cycle, p. ex. indolizine, bêta-carboline
A61K 31/4412 - Pyridines non condenséesLeurs dérivés hydrogénés ayant des groupes oxo liés directement à l'hétérocycle
A61K 31/513 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime ayant des groupes oxo liés directement à l'hétérocycle, p. ex. cytosine
13.
COMPOSITIONS COMPRISING DESOXIMETASONE AND TAZAROTENE
The present disclosure provides formulations comprising desoximetasone, tazarotene, a polymer comprising polyurethane, and a solvent. Also provided herein are methods of co-administering desoximetasone and tazarotene.
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 31/4436 - Pyridines non condenséesLeurs dérivés hydrogénés contenant d'autres systèmes hétérocycliques contenant un hétérocycle avec le soufre comme hétéro-atome du cycle
A61K 47/59 - 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 l’ingrédient non actif étant chimiquement lié à l’ingrédient actif, p. ex. conjugués polymère-médicament l’ingrédient non actif étant un agent de modification l’agent de modification étant un composé organique macromoléculaire, p. ex. une molécule oligomérique, polymérique ou dendrimérique obtenu par des réactions autres que celles faisant intervenir uniquement des liaisons non saturées carbone-carbone, p. ex. polyurées ou polyuréthanes
A61K 47/34 - Composés macromoléculaires obtenus par des réactions autres que celles faisant intervenir uniquement des liaisons non saturées carbone-carbone, p. ex. polyesters, acides polyaminés, polysiloxanes, polyphosphazines, copolymères de polyalkylène glycol ou de poloxamères
A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
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
14.
Preparation of Trifarotene and intermediates and polymorphs thereof
The present disclosure provides a process for the preparation of Trifarotene. The disclosure also provides novel intermediates in the process described herein. Also provided are novel polymorphs of Trifarotene.
C07D 207/08 - Composés hétérocycliques contenant des cycles à cinq chaînons, non condensés avec d'autres cycles, ne comportant qu'un atome d'azote comme unique hétéro-atome du cycle avec uniquement des atomes d'hydrogène ou de carbone liés directement à l'atome d'azote du cycle ne comportant pas de liaison double entre chaînons cycliques ou entre chaînons cycliques et chaînons non cycliques avec des radicaux hydrocarbonés, substitués par des hétéro-atomes, liés aux atomes de carbone du cycle
The present disclosure provides an oral care device including a hollow shaft (120, 920, 1320), a sleeve (110, 910, 1310), and a cleaning portion (115). The hollow shaft can include a first end having a first suction aperture (140, 940, 1340), and a second end having a second suction aperture (125, 925). The hollow shaft can be configured for insertion into a hand grip. The sleeve can surround the hollow shaft of the oral care device, and can be configured to slide along a longitudinal axis and conceal at least a portion of the first suction aperture or the second suction aperture. The sleeve can conceal the first suction aperture or the second suction aperture to easily adjust an amount of suction provided to an oral cavity of a patient. The cleaning portion can be coupled to a portion of the sleeve at the first end of the hollow shaft.
The present disclosure provides an oral care device including a hollow shaft (120, 920, 1320), a sleeve (110, 910, 1310), and a cleaning portion (115). The hollow shaft can include a first end having a first suction aperture (140, 940, 1340), and a second end having a second suction aperture (125, 925). The hollow shaft can be configured for insertion into a hand grip. The sleeve can surround the hollow shaft of the oral care device, and can be configured to slide along a longitudinal axis and conceal at least a portion of the first suction aperture or the second suction aperture. The sleeve can conceal the first suction aperture or the second suction aperture to easily adjust an amount of suction provided to an oral cavity of a patient. The cleaning portion can be coupled to a portion of the sleeve at the first end of the hollow shaft.
The present disclosure is directed to a topical composition, e.g., a physically and chemically stable topical composition of Fenoldopam comprising about 0.1% to about 5% by weight of Fenoldopam or a pharmaceutically acceptable salt thereof, at least one polyacrylamide-type gelling agent, at least one cellulose-type gelling agent, and at least one solvent, wherein the Fenoldopam is substantially solubilized in the composition, and wherein the composition is stable for at least twelve months at 25° C. and 60% relative humidity.
A61K 9/14 - Préparations médicinales caractérisées par un aspect particulier à l'état particulaire, p. ex. poudres
A61K 31/55 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à sept chaînons, p. ex. azélastine, pentylènetétrazole
A61K 47/32 - Composés macromoléculaires obtenus par des réactions faisant intervenir uniquement des liaisons non saturées carbone-carbone, p. ex. carbomères
The present disclosure provides for topical emulsion comprising about 0.5% to about 10% Montelukast or pharmaceutically acceptable salt thereof; and about 0.4% to about 4% carbomer; wherein particles comprising the Montelukast in the emulsion have D90 of less than about 50 wherein the Montelukast or pharmaceutically acceptable salt thereof is homogeneously dispersed in the emulsion, and wherein the emulsion has a pH of about 3.0 to about 6.5. The present disclosure also provides a topical gel comprising (a) about 0.5% to about 10% Montelukast or pharmaceutically acceptable salt thereof; (b) about 0.2% to about 8% cellulose polymer; and (c) about 80% to about 95% amphiphilic compound; wherein the gel comprises less than 4% water.
A61K 47/10 - AlcoolsPhénolsLeurs sels, p. ex. glycérolPolyéthylène glycols [PEG]PoloxamèresAlkyléthers de PEG/POE
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 47/32 - Composés macromoléculaires obtenus par des réactions faisant intervenir uniquement des liaisons non saturées carbone-carbone, p. ex. carbomères
The present disclosure provides for topical emulsion comprising about 0.5% to about 10% Montelukast or pharmaceutically acceptable salt thereof; and about 0.4% to about 4% carbomer; wherein particles comprising the Montelukast in the emulsion have D90 of less than about 50 μm, wherein the Montelukast or pharmaceutically acceptable salt thereof is homogeneously dispersed in the emulsion, and wherein the emulsion has a pH of about 3.0 to about 6.5. The present disclosure also provides a topical gel comprising (a) about 0.5% to about 10% Montelukast or pharmaceutically acceptable salt thereof; (b) about 0.2% to about 8% cellulose polymer; and (c) about 80% to about 95% amphiphilic compound; wherein the gel comprises less than 4% water.
The present disclosure provides formulations comprising desoximetasone, tazarotene, a polymer comprising polyurethane, and a solvent. Also provided herein are methods of co-administering desoximetasone and tazarotene.
A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
A61K 31/4436 - Pyridines non condenséesLeurs dérivés hydrogénés contenant d'autres systèmes hétérocycliques contenant un hétérocycle avec le soufre comme hétéro-atome du cycle
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 47/10 - AlcoolsPhénolsLeurs sels, p. ex. glycérolPolyéthylène glycols [PEG]PoloxamèresAlkyléthers de PEG/POE
A61K 47/34 - Composés macromoléculaires obtenus par des réactions autres que celles faisant intervenir uniquement des liaisons non saturées carbone-carbone, p. ex. polyesters, acides polyaminés, polysiloxanes, polyphosphazines, copolymères de polyalkylène glycol ou de poloxamères
A61P 17/00 - Médicaments pour le traitement des troubles dermatologiques
The present disclosure provides for topical emulsion comprising about 0.5% to about 10% Montelukast or pharmaceutically acceptable salt thereof; and about 0.4% to about 4% carbomer; wherein particles comprising the Montelukast in the emulsion have D90 of less than about 50 ?m, wherein the Montelukast or pharmaceutically acceptable salt thereof is homogeneously dispersed in the emulsion, and wherein the emulsion has a pH of about 3.0 to about 6.5. The present disclosure also provides a topical gel comprising (a) about 0.5% to about 10% Montelukast or pharmaceutically acceptable salt thereof; (b) about 0.2% to about 8% cellulose polymer; and (c) about 80% to about 95% amphiphilic compound; wherein the gel comprises less than 4% water.
A61K 47/10 - AlcoolsPhénolsLeurs sels, p. ex. glycérolPolyéthylène glycols [PEG]PoloxamèresAlkyléthers de PEG/POE
A61K 47/32 - Composés macromoléculaires obtenus par des réactions faisant intervenir uniquement des liaisons non saturées carbone-carbone, p. ex. carbomères
A61P 17/00 - Médicaments pour le traitement des troubles dermatologiques
The present disclosure provides for topical emulsion comprising about 0.5% to about 10% Montelukast or pharmaceutically acceptable salt thereof; and about 0.4% to about 4% carbomer; wherein particles comprising the Montelukast in the emulsion have D90 of less than about 50 μm, wherein the Montelukast or pharmaceutically acceptable salt thereof is homogeneously dispersed in the emulsion, and wherein the emulsion has a pH of about 3.0 to about 6.5. The present disclosure also provides a topical gel comprising (a) about 0.5% to about 10% Montelukast or pharmaceutically acceptable salt thereof; (b) about 0.2% to about 8% cellulose polymer; and (c) about 80% to about 95% amphiphilic compound; wherein the gel comprises less than 4% water.
A61K 47/10 - AlcoolsPhénolsLeurs sels, p. ex. glycérolPolyéthylène glycols [PEG]PoloxamèresAlkyléthers de PEG/POE
A61K 47/32 - Composés macromoléculaires obtenus par des réactions faisant intervenir uniquement des liaisons non saturées carbone-carbone, p. ex. carbomères
A61P 17/00 - Médicaments pour le traitement des troubles dermatologiques
The present disclosure provides for topical emulsion comprising about 0.5% to about 10% Montelukast or pharmaceutically acceptable salt thereof; and about 0.4% to about 4% carbomer; wherein particles comprising the Montelukast in the emulsion have D90 of less than about 50 μm, wherein the Montelukast or pharmaceutically acceptable salt thereof is homogeneously dispersed in the emulsion, and wherein the emulsion has a pH of about 3.0 to about 6.5. The present disclosure also provides a topical gel comprising (a) about 0.5% to about 10% Montelukast or pharmaceutically acceptable salt thereof; (b) about 0.2% to about 8% cellulose polymer; and (c) about 80% to about 95% amphiphilic compound; wherein the gel comprises less than 4% water.
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 47/32 - Composés macromoléculaires obtenus par des réactions faisant intervenir uniquement des liaisons non saturées carbone-carbone, p. ex. carbomères
A61K 47/10 - AlcoolsPhénolsLeurs sels, p. ex. glycérolPolyéthylène glycols [PEG]PoloxamèresAlkyléthers de PEG/POE
A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
24.
PREPARATION OF TRIFAROTENE AND INTERMEDIATES AND POLYMORPHS THEREOF
The present disclosure provides a process for the preparation of Trifarotene. The disclosure also provides novel intermediates in the process described herein. Also provided are novel polymorphs of Trifarotene.
C07D 207/06 - Composés hétérocycliques contenant des cycles à cinq chaînons, non condensés avec d'autres cycles, ne comportant qu'un atome d'azote comme unique hétéro-atome du cycle avec uniquement des atomes d'hydrogène ou de carbone liés directement à l'atome d'azote du cycle ne comportant pas de liaison double entre chaînons cycliques ou entre chaînons cycliques et chaînons non cycliques avec des radicaux contenant uniquement des atomes d'hydrogène et de carbone, liés aux atomes de carbone du cycle
A61K 31/402 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à cinq chaînons avec un azote comme seul hétéro-atome d'un cycle, p. ex. sulpiride, succinimide, tolmétine, buflomédil substitués par un groupe aryle en position 1, p. ex. pirétanide
The present invention relates to a novel and unexpected method of using topical Capecitabine composition to obtain therapeutically effective amounts of fluorouracil (FU) within the skin of a subject afflicted with hyperproliferative or inflammatory skin condition. The method comprising topically administering a pharmaceutical composition comprising Capecitabine or a hydrate or solvate thereof to the affected area of the skin of the subject, to form therapeutically effective amounts of FU within the skin.
A61K 31/7068 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'azote comme hétéro-atome d'un cycle, p. ex. nucléosides, nucléotides contenant des cycles à six chaînons avec l'azote comme hétéro-atome d'un cycle contenant des pyrimidines condensées ou non-condensées ayant des groupes oxo liés directement au cycle pyrimidine, p. ex. cytidine, acide cytidylique
A61P 17/12 - Kératolytiques, p. ex. préparations pour le traitement des verrues ou des cors
A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
A61K 31/122 - Cétones ayant l'atome d'oxygène lié directement à un cycle, p. ex. quinones, vitamine K1, anthraline
A61K 31/196 - Acides carboxyliques, p. ex. acide valproïque ayant un groupe amino le groupe amino étant lié directement à un cycle, p. ex. acide anthranilique, acide méfénamique, diclofénac, chlorambucil
A61K 31/437 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec un azote comme seul hétéro-atome d'un cycle condensés en ortho ou en péri avec des systèmes hétérocycliques le système hétérocyclique contenant un cycle à cinq chaînons ayant l'azote comme hétéro-atome du cycle, p. ex. indolizine, bêta-carboline
A61K 31/4412 - Pyridines non condenséesLeurs dérivés hydrogénés ayant des groupes oxo liés directement à l'hétérocycle
A61K 31/513 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime ayant des groupes oxo liés directement à l'hétérocycle, p. ex. cytosine
The present disclosure is directed to a topical composition, e.g., a physically and chemically stable topical composition of Fenoldopam comprising about 0.1% to about 5% by weight of Fenoldopam or a pharmaceutically acceptable salt thereof, at least one polyacrylamide-type gelling agent, at least one cellulose-type gelling agent, and at least one solvent, wherein the Fenoldopam is substantially solubilized in the composition, and wherein the composition is stable for at least twelve months at 25ºC and 60% relative humidity.
A61K 31/55 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à sept chaînons, p. ex. azélastine, pentylènetétrazole
A61K 47/32 - Composés macromoléculaires obtenus par des réactions faisant intervenir uniquement des liaisons non saturées carbone-carbone, p. ex. carbomères
The present disclosure is directed to a topical composition, e.g., a physically and chemically stable topical composition of Fenoldopam comprising about 0.1% to about 5% by weight of Fenoldopam or a pharmaceutically acceptable salt thereof, at least one polyacrylamide-type gelling agent, at least one cellulose-type gelling agent, and at least one solvent, wherein the Fenoldopam is substantially solubilized in the composition, and wherein the composition is stable for at least twelve months at 25ºC and 60% relative humidity.
A61K 31/55 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à sept chaînons, p. ex. azélastine, pentylènetétrazole
A61K 47/32 - Composés macromoléculaires obtenus par des réactions faisant intervenir uniquement des liaisons non saturées carbone-carbone, p. ex. carbomères
A topical formulation comprising Montelukast or a pharmaceutically acceptable salt thereof, a gelling agent and water for the treatment of atopic dermatitis.
A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
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
A61K 45/06 - Mélanges d'ingrédients actifs sans caractérisation chimique, p. ex. composés antiphlogistiques et pour le cœur
A61K 31/00 - Préparations médicinales contenant des ingrédients actifs organiques
29.
Fenoldopam topical formulations for treating skin disorders
Embodiments of stable topical compositions for administering fenoldopam (compound (I) or a pharmaceutically acceptable salt or solvate thereof are disclosed for immediate or continued slow release administration, over prolonged periods of time with safe minimal systemic exposure of fenoldopam (reducing the risk for lowering blood pressure). The compositions include those compositions that increase the stability and skin absorption of the drug, particularly anhydrous semi-solid compositions and creams. This is accomplished by incorporating fenoldopam in soluble or dispersed form into semi-solid compositions like ointments or anhydrous gels that are not irritative. Embodiments of methods for using the topical compositions in the treatment of dermatological disorders including psoriasis, alopecia atopic dermatitis and vitiligo are disclosed.
A61K 31/55 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à sept chaînons, p. ex. azélastine, pentylènetétrazole
A61K 45/06 - Mélanges d'ingrédients actifs sans caractérisation chimique, p. ex. composés antiphlogistiques et pour le cœur
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 47/12 - Acides carboxyliquesLeurs sels ou anhydrides
A61K 47/32 - Composés macromoléculaires obtenus par des réactions faisant intervenir uniquement des liaisons non saturées carbone-carbone, p. ex. carbomères
30.
TOPICAL CAPECITABINE FOR THE TREATMENT OF HYPERPROLIFERATIVE SKIN CONDITIONS
The present invention relates to a novel and unexpected method of using topical Capecitabine composition to obtain therapeutically effective amounts of fluorouracil (FU) within the skin of a subject afflicted with hyperproliferative or inflammatory skin condition. The method comprising topically administering a pharmaceutical composition comprising Capecitabine or a hydrate or solvate thereof to the affected area of the skin of the subject, to form therapeutically effective amounts of FU within the skin.
A61K 31/513 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime ayant des groupes oxo liés directement à l'hétérocycle, p. ex. cytosine
A61K 31/7068 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'azote comme hétéro-atome d'un cycle, p. ex. nucléosides, nucléotides contenant des cycles à six chaînons avec l'azote comme hétéro-atome d'un cycle contenant des pyrimidines condensées ou non-condensées ayant des groupes oxo liés directement au cycle pyrimidine, p. ex. cytidine, acide cytidylique
A61K 31/7072 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'azote comme hétéro-atome d'un cycle, p. ex. nucléosides, nucléotides contenant des cycles à six chaînons avec l'azote comme hétéro-atome d'un cycle contenant des pyrimidines condensées ou non-condensées ayant des groupes oxo liés directement au cycle pyrimidine, p. ex. cytidine, acide cytidylique ayant deux groupes oxo liés directement au cycle pyrimidine, p. ex. uridine, acide uridylique, thymidine, zidovudine
A61P 17/00 - Médicaments pour le traitement des troubles dermatologiques
The present invention relates to a novel and unexpected method of using topical Capecitabine composition to obtain therapeutically effective amounts of fluorouracil (FU) within the skin of a subject afflicted with hyperproliferative or inflammatory skin condition. The method comprising topically administering a pharmaceutical composition comprising Capecitabine or a hydrate or solvate thereof to the affected area of the skin of the subject, to form therapeutically effective amounts of FU within the skin.
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 31/196 - Acides carboxyliques, p. ex. acide valproïque ayant un groupe amino le groupe amino étant lié directement à un cycle, p. ex. acide anthranilique, acide méfénamique, diclofénac, chlorambucil
YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM LTD. (Israël)
Inventeur(s)
Khan, Wahid
Shifrin, Helena
Schlinger, Ron
Avramoff, Avi
Domb, Avi
Abrégé
Embodiments of stable topical compositions for administering fenoldopam (compound (I) or a pharmaceutically acceptable salt or solvate thereof are disclosed for immediate or continued slow release administration, over prolonged periods of time with safe minimal systemic exposure of fenoldopam (reducing the risk for lowering blood pressure). The compositions include those compositions that increase the stability and skin absorption of the drug, particularly anhydrous semi-solid compositions and creams. This is accomplished by incorporating fenoldopam in soluble or dispersed form into semi-solid compositions like ointments or anhydrous gels that are not irritative. Embodiments of methods for using the topical compositions in the treatment of dermatological disorders including psoriasis, alopecia atopic dermatitis and vitiligo are disclosed.
A61K 31/55 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à sept chaînons, p. ex. azélastine, pentylènetétrazole
A61P 17/00 - Médicaments pour le traitement des troubles dermatologiques
The present invention provides a process for the preparation of a stable polymorph III of Atovaquone exhibiting characteristic peaks (expressed in degrees 2θ±0.2°θ) at about 6.9, 9.6, 14.1, 14.7, 17.0, 18.5, 19.1, 19.9, 20.3, 22.0, 22.6, 23.2, 24.2, 26.8, and 28.5, which comprises: (a) providing a sample of Atovaquone particles; (b) heating the sample of Atovaquone particles at a minimal temperature of between 140 °C to 160 °C depending on the particle size of the sample; and (c) cooling the sample to obtain the stable polymorphic form of Atovaquone.
The present invention is related to a novel synthetic procedure that provides a simple, safe and commercially valuable method for the preparation of 2-phenyl-1,3-propanediol. The process for the preparation of 2-phenyl-1,3-propanediol involves reducing diethyl phenylmalonate with sodium borohydride (NaBH4) in the presence of an alkali metal dihydrogen phosphate buffer or the hydrate thereof.
The present invention provides an improved process for the preparation of 17-desoxy corticosteroid derivatives in a single chemical step by reacting the 17-hydroxy starting material with an excess of Trimethylsilyl Iodide. The present invention is specifically advantageous in preparing 17-desoxy corticosteroid derivatives having one or more halogen groups at positions 2, 6, 7 or 9 of the corticosteroid such as Clocortolone or Desoximetasone.
C07J 3/00 - Stéroïdes normaux contenant du carbone, de l'hydrogène, un halogène ou de l'oxygène, substitués en position 17bèta par un atome de carbone
C07J 1/00 - Stéroïdes normaux contenant du carbone, de l'hydrogène, un halogène ou de l'oxygène, non substitués en position 17bêta par un atome de carbone, p. ex. œstrane, androstane
C07J 7/00 - Stéroïdes normaux contenant du carbone, de l'hydrogène, un halogène ou de l'oxygène, substitués en position 17bèta par une chaîne de deux atomes de carbone
C07J 43/00 - Stéroïdes normaux ayant un hétérocycle contenant de l'azote non condensé ou condensé en spiro avec le squelette du cyclopenta[a]hydrophénanthrène
39.
Process for preparing malathion for pharmaceutical use
The present invention provides a process for preparing a highly pure form of malathion having a reduced level of toxic impurities. In addition, the malathion prepared by the process of this invention is storage stable. The level of toxic impurities in the malathion, e.g., isomalathion, O,O,S-trimethyl phosphorodithioate (MeOOSPS), O,O,S-trimethyl phosphorothioate (MeOOSPO), O,S,S-trimethyl phosphorodithioate (MeOSSPO), malaoxon, isomalathion, diethyl fumarate, methyl malathion, dimethyl malathion, O,O-methyl,ethyl-S-(1,2-dicarboethoxy)ethyl-phosphorodithioate are lower than that of any other commercial preparation of malathion that may be used for pharmaceutical purposes.
This invention is directed to a process for the preparation of pure ropinirole hydrochloride with purity of equal to or greater than 99.8% and less than 0.1% isatine impurity. In the process of the present invention, the isatine is removed during the reaction steps and no further cleaning steps are required.
The present invention provides a pharmaceutical composition comprising a combination of an anti-androgen agent and an antibiotic/anti-inflammatory agent or pharmaceutically acceptable salts thereof, useful for treating a subject with a dermatological disorder. The combination of this invention preferably provides a synergistic effect in treating a subject with a dermatological disorder, specifically a subject with acne. In a preferred embodiment, the present invention provides a pharmaceutical composition comprising combination of spironolactone and doxycycline or pharmaceutically acceptable salts or hydrates thereof.
The present invention provides a process for preparing a highly pure form of malathion having a reduced level of toxic impurities. In addition, the malathion prepared by the process of this invention is storage stable. The level of toxic impurities in the malathion, e.g., isomalathion, O,O,S-trimethyl phosphorodithioate (MeOOSPS), O,O,S-trimethyl phosphorothioate (MeOOSPO), O,S,S-trimethyl phosphorodithioate (MeOSSPO), malaoxon, isomalathion, diethyl fumarate, methyl malathion, dimethyl malathion, O,O-methyl,ethyl-S-(1,2-dicarboethoxy)ethyl-phosphorodithioate are lower than that of any other commercial preparation of malathion that may be used for pharmaceutical purposes.
The present invention provides a process for preparing a highly pure form of malathion having a reduced level of toxic impurities. In addition, the malathion prepared by the process of this invention is storage stable. The level of toxic impurities in the malathion, e.g., isomalathion, O,O,S-trimethyl phosphorodithioate (MeOOSPS), O,O,S-trimethyl phosphorothioate (MeOOSPO), O,S,S-trimethyl phosphorodithioate (MeOSSPO), malaoxon, isomalathion, diethyl fumarate, methyl malathion, dimethyl malathion, O,O-methyl,ethyl-S-(1,2-dicarboethoxy)ethyl-phosphorodithioate are lower than that of any other commercial preparation of malathion that may be used for pharmaceutical purposes.
The present invention provides for a storage stable pharmaceutical liquid solution for oral administration having a pharmaceutically effective amount of an antihistamine and having a purity equal to or greater than about 99% by weight-based HPLC assay, residual solvents of less than about 0.5%, and a total impurity of less than about 0.2%. The storage stable solution preferably contains cetirizine. The present invention further provides a process of preparing the storage stable pharmaceutical liquid solution as well as a method of treating a mammal with a therapeutically effective amount of cetirizine in the stable pharmaceutical liquid solution.
A01N 43/00 - Biocides, produits repoussant ou attirant les animaux nuisibles, ou régulateurs de croissance des végétaux, contenant des composés hétérocycliques
The present invention provides a process for preparing a highly pure form of malathion having a reduced level of toxic impurities. In addition, the malathion prepared by the process of this invention is storage stable. The level of toxic impurities in the malathion, e.g., isomalathion, O,O,S-trimethyl phosphorodithioate (MeOOSPS), O,O,S-trimethyl phosphorothioate (MeOOSPO), O,S,S-trimethyl phosphorodithioate (MeOSSPO), malaoxon, isomalathion, diethyl fumarate, methyl malathion, dimethyl malathion, O,O-methyl,ethyl-S-(1,2-dicarboethoxy)ethyl-phosphorodithioate are lower than that of any other commercial preparation of malathion that may be used for pharmaceutical purposes.
The present invention provides a process of preparing a crystalline azithromycin monohydrate. The process involves dissolving azithromycin in a solution containing ethanol, adding the dissolved azithromycin into water to precipitate the crystals, isolating and drying the precipitate to a water content of about 5% (w/w) to about 7% (w/w). The resulting azithromycin monohydrate is stable, exhibiting less than 2% degradation, and non-hydroscopic.
