The invention relates to combinations, pharmaceutical compositions and kits comprising Tinostamustine, and an immune checkpoint inhibitor. The combinations, pharmaceutical compositions and kits are effective for use in the treatment of cancer.
C07K 16/28 - Immunoglobulines, p. ex. anticorps monoclonaux ou polyclonaux contre du matériel provenant d'animaux ou d'humains contre des récepteurs, des antigènes de surface cellulaire ou des déterminants de surface cellulaire
A61K 31/00 - Préparations médicinales contenant des ingrédients actifs organiques
A61K 39/395 - AnticorpsImmunoglobulinesImmunsérum, p. ex. sérum antilymphocitaire
A61P 35/04 - Agents anticancéreux spécifiques pour le traitement des métastases
A61K 39/00 - Préparations médicinales contenant des antigènes ou des anticorps
Dispensers, in particular dispensers for dispensing a dose of a gaseous, gas borne or droplet substance from a substance source and dispensers containing dosage counters are described herein.
A61M 11/04 - Pulvérisateurs ou vaporisateurs spécialement destinés à des usages médicaux agissant par pression de la vapeur des liquides à pulvériser ou vaporiser
A61M 16/12 - Préparation de gaz ou vapeurs à respirer par mélange de gaz différents
G06M 1/08 - Caractéristiques d'ordre général pour actionner l'entraînement
G06M 1/04 - Caractéristiques d'ordre général pour entraîner l'étage du rang le plus bas
3.
HUMANIZED ANTIBODIES TARGETING HUMAN TISSUE FACTOR
The present disclosure provides humanized antibodies and antibody-drug conjugates that specifically bind to human tissue factor, and which do not inhibit tissue factor mediated blood coagulation compared to a normal plasma control. Further described are methods of making and methods of using the disclosed humanized antibodies and antibody-drug conjugates in the treatment of cancer.
A61K 47/68 - 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 anticorps, une immunoglobuline ou son fragment, p. ex. un fragment Fc
C07K 16/36 - Immunoglobulines, p. ex. anticorps monoclonaux ou polyclonaux contre du matériel provenant d'animaux ou d'humains contre des facteurs de coagulation sanguine
There is provided tinostamustine or a pharmaceutically acceptable salt thereof for use in the treatment of triple negative breast cancer (TNBC)to a patient in need thereof.
T-PLLTherapy There is provided tinostamustine or a pharmaceutically acceptable salt thereof for use in the treatment of T-cell prolymphocytic leukemia (T-PLL) in a patient in need thereof.
There is provided tinostamustine or a pharmaceutically acceptable salt thereof for use in the treatment of ovarian cancer in a patient in need thereof.
A61K 31/337 - Composés hétérocycliques ayant l'oxygène comme seul hétéro-atome d'un cycle, p. ex. fungichromine ayant des cycles à quatre chaînons, p. ex. taxol
A61K 41/00 - Préparations médicinales obtenues par traitement de substances par énergie ondulatoire ou par rayonnement corpusculaire
A61K 45/06 - Mélanges d'ingrédients actifs sans caractérisation chimique, p. ex. composés antiphlogistiques et pour le cœur
There is provided a compound of formula I or a pharmacologically acceptable salt thereof for use in a method of treating Hodgkin lymphomain a patient in need thereof comprising administering to said patient an effective amount of said compound of formula I or a pharmacologically acceptable salt thereof: I, a combination of said compound of formula I or a pharmaceutically acceptable salt thereof with Brentuximab Vedotinand said combination for use in a method of treating Hodgkin lymphomain a patient in need thereof comprising administering to said patient an effective amount of said combination.
The present invention relates to methods of treatment comprising, inter alia, administering a high daily dose of oxycodone, such as a daily dose of at least 90 mg oxycodone, and naloxone in a 2:1 weight ratio to a patient in need thereof.
The present invention relates to prolonged release pharmaceutical dosage forms comprising hydromorphone or a pharmaceutically acceptable salt thereof and naloxone or a pharmaceutically acceptable salt thereof for use in the treatment of pain.
The present application is concerned with oxycodone or a pharmaceutically acceptable salt thereof for use in the treatment of pain, preferably post-operative pain, in a cancer patient undergoing cancer surgery or in a patient undergoing surgery, wherein said patient exhibits immunodeficiency.
The present invention provides a process for the preparation of a compound of formula (VI), or a salt or derivative thereof,
1-8 alkyl and * represents a stereocentre.
A61K 31/485 - Dérivés du morphinane, p. ex. morphine, codéine
C07D 489/12 - Composés hétérocycliques contenant des systèmes cycliques 4 aH-8, 9 c-imino-éthano-phénantro [4, 5-b, c, d] furanne, p. ex. dérivés d'époxy-4, 5 morphinane de formule contenant des systèmes cycliques 4 aH-8, 9 c-imino-éthano-phénantro [4, 5-b, c, d] furanne condensés avec des carbocycles ou avec des systèmes carbocycliques avec un pont entre les positions 6 et 14 le pont ne contenant que deux atomes de carbone
C07D 489/02 - Composés hétérocycliques contenant des systèmes cycliques 4 aH-8, 9 c-imino-éthano-phénantro [4, 5-b, c, d] furanne, p. ex. dérivés d'époxy-4, 5 morphinane de formule avec des atomes d'oxygène liés en position 3 et 6, p. ex. morphine, morphinone
ABUSE RESISTANT TRANSDERMAL DELIVERY DEVICES AND COMPOSITIONS COMPRISING AN OPIOID AGONIST AND A NON-TRANSDERMALLY DELIVERED N-OXIDE DERIVATIVE OF AN OPIOID ANTAGONIST FOR THE TREATMENT OF PAIN
The present invention provides a transdermal delivery device comprising a pharmaceutical composition, wherein said composition comprises a N-oxide derivative of an opioid antagonist, or a salt thereof, and an opioid agonist or salt thereof.
A61K 31/485 - Dérivés du morphinane, p. ex. morphine, codéine
A61P 25/04 - Analgésiques centraux, p. ex. opioïdes
15.
A PROLONGED RELEASE DOSAGE FORM COMPRISING OXYCODONE OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF AND NALOXONE OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF IN THE TREATMENT OF BLADDER PAIN SYNDROME (BPS)
The present invention provides a pharmaceutical dosage form comprising oxycodone and naloxone (or pharmaceutically acceptable salts thereof) for use in the treatment of Bladder Pain Syndrome (BPS) and/or at least one, preferably at least two symptoms thereof.
The present invention provides a transdermal patch comprising: a drug-containing layer comprising (R)-dihydroetorphine, or a salt or a hydrate thereof, and a poly(meth)acrylate; and a backing layer.
A61K 31/44 - Pyridines non condenséesLeurs dérivés hydrogénés
A61P 25/04 - Analgésiques centraux, p. ex. opioïdes
A61K 47/32 - Composés macromoléculaires obtenus par des réactions faisant intervenir uniquement des liaisons non saturées carbone-carbone, p. ex. carbomères
The present invention provides a transdermal delivery system comprising (R)-dihydroetorphine, or a salt, hydrate or derivative thereof, wherein said system has a rapid onset of (R)-dihydroetorphine plasma concentration characterised by the mean in vivo plasma concentration of (R)-dihydroetorphine achieving at least 50 % of its Cmax in less than 20 hours, preferably in less than 18 hours and more preferably in less than 12 hours, after application of the system to the skin of a human subject, e.g. when based on the mean plasma concentration versus time curve.
The present invention relates to prolonged release pharmaceutical dosage forms comprising hydromorphone or a pharmaceutically acceptable salt thereof and naloxone or a pharmaceutically acceptable salt thereof for use in the treatment of pain.
A61K 31/44 - Pyridines non condenséesLeurs dérivés hydrogénés
A61K 31/485 - Dérivés du morphinane, p. ex. morphine, codéine
A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
A61K 9/48 - Préparations en capsules, p. ex. de gélatine, de chocolat
19.
A COMBINATION OF HYDROMORPHONE AND NALOXONE FOR USE IN TREATING PAIN IN PATIENTS SUFFERING FROM PAIN AND A DISEASE RESULTING IN INTESTINAL DYSBIOSIS AND/OR INCREASING THE RISK FOR INTESTINAL BACTERIAL TRANSLOCATION
The present invention is concerned with an oral pharmaceutical dosage form comprising hydromorphone or a pharmaceutically acceptable salt thereof and naloxone or a pharmaceutically acceptable salt thereof for use in the treatment of pain in patients suffering from i) pain and at least one further disease ii), wherein said at least one further disease ii) results in intestinal dysbiosis, or for use in the treatment of pain in patients suffering from i) pain and at least one further disease iii), wherein said at least one further disease iii) increases the risk for intestinal bacterial translocation and thus for peritonitis, SIRS and/or sepsis.
Combination of oxycodone and naloxone for use in treating pain in patients suffering from pain and a disease resulting in intestinal dysbiosis and/or increasing the risk for intestinal bacterial translocation
The present invention is concerned with an oral pharmaceutical dosage form comprising oxycodone or a pharmaceutically acceptable salt thereof and naloxone or a pharmaceutically acceptable salt thereof for use in the treatment of pain in patients suffering from i) pain and at least one further disease ii), wherein said at least one further disease ii) results in intestinal dysbiosis, or for use in the treatment of pain in patients suffering from i) pain and at least one further disease iii), wherein said at least one further disease iii) increases the risk for intestinal bacterial translocation and thus for peritonitis, SIRS and/or sepsis.
The present invention provides a process for the preparation of a compound of formula (VI), or a salt or derivative thereof,
1-8 alkyl and * represents a stereocentre.
A61K 31/485 - Dérivés du morphinane, p. ex. morphine, codéine
C07D 489/12 - Composés hétérocycliques contenant des systèmes cycliques 4 aH-8, 9 c-imino-éthano-phénantro [4, 5-b, c, d] furanne, p. ex. dérivés d'époxy-4, 5 morphinane de formule contenant des systèmes cycliques 4 aH-8, 9 c-imino-éthano-phénantro [4, 5-b, c, d] furanne condensés avec des carbocycles ou avec des systèmes carbocycliques avec un pont entre les positions 6 et 14 le pont ne contenant que deux atomes de carbone
C07D 489/02 - Composés hétérocycliques contenant des systèmes cycliques 4 aH-8, 9 c-imino-éthano-phénantro [4, 5-b, c, d] furanne, p. ex. dérivés d'époxy-4, 5 morphinane de formule avec des atomes d'oxygène liés en position 3 et 6, p. ex. morphine, morphinone
The present invention provides a method of providing pain relief in a human subject in need thereof comprising administering (R)-dihydroetorphine to said subject, wherein said (R)-dihydroetorphine is administered in a dose of at least 0.01 μg/kg, preferably at least 0.05 μg/kg, and the level of respiratory depression in said subject is 65 or less % relative to the baseline level pre-administration of (R)-dihydroetorphine.
A61K 31/485 - Dérivés du morphinane, p. ex. morphine, codéine
A61K 45/06 - Mélanges d'ingrédients actifs sans caractérisation chimique, p. ex. composés antiphlogistiques et pour le cœur
C07D 489/12 - Composés hétérocycliques contenant des systèmes cycliques 4 aH-8, 9 c-imino-éthano-phénantro [4, 5-b, c, d] furanne, p. ex. dérivés d'époxy-4, 5 morphinane de formule contenant des systèmes cycliques 4 aH-8, 9 c-imino-éthano-phénantro [4, 5-b, c, d] furanne condensés avec des carbocycles ou avec des systèmes carbocycliques avec un pont entre les positions 6 et 14 le pont ne contenant que deux atomes de carbone
b) projecting from a base (17) and the protrusion being arranged between the dispenser driver and the junction member such that a force applied by the cam of the dispenser driver to the protrusion causes the cam follower to slideably move in the longitudinal axis of the body and apply a force to the junction member so as to release a dose of a substance from a substance source. The dispenser also comprises a dispenser cap (91) comprising a hollow body having a lower open end (92) engageable with the body, and an upper open end (94) for receiving a cap closure device (120) for closing the upper open end. The dispenser also comprises a dose counter (203) for indicating a number of actuations of the dispenser corresponding to a number of doses dispensed from a substance source, or a number of doses remaining in a substance source, the dose counter comprising: a first ring member (202) having a first indicia and being rotatable in increments about the longitudinal axis, the first indicia indicating a count; and a limiting member comprising a limiting mechanism (1506), wherein the limiting mechanism comprises an engaging portion arranged to act radially with respect to the first ring member to contact the first ring member to limit free rotation of the first member relative to the limiting member about the axis.
There is provided a compound of formula I or a pharmacologically acceptable salt thereof: for use in the treatment of a brain cancer selected from a MGMT positive astrocytic brain tumour, a metastatic brain cancer and primary CNS lymphoma and a method of treating said brain cancers in a patient in need thereof comprising administering to the patient said compound of formula I or a pharmacologically acceptable salt thereof.
A61K 31/395 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines
A61K 31/4184 - 1,3-Diazoles condensés avec des carbocycles, p. ex. benzimidazoles
A61K 31/502 - PyridazinesPyridazines hydrogénées condensées en ortho ou en péri avec des systèmes carbocycliques, p. ex. cinnoline, phtalazine
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
The present invention is directed to a combination comprising a proteasome inhibitor and a compound of formula (I), or a pharmaceutically acceptable salt thereof: to a pharmaceutical composition and to a kit both comprising said combination, to the combination, composition or kit for use in the treatment of cancer, and to a method of treatment of cancer in a patient in need thereof comprising administering to said patient an effective amount of said combination, composition or kit.
A61K 31/407 - 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 condensés avec des systèmes hétérocycliques, p. ex. kétorolac, physostigmine
A61K 31/427 - Thiazoles non condensés et contenant d'autres hétérocycles
A61K 31/5377 - 1,4-Oxazines, p. ex. morpholine non condensées et contenant d'autres hétérocycles, p. ex. timolol
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 31/58 - Composés contenant des systèmes cycliques du cyclopenta[a]hydrophénanthrèneLeurs dérivés, p. ex. stéroïdes contenant des hétérocycles, p. ex. danazol, stanozolol, pancuronium ou digitogénine
This invention generally relates to counters and in particular to counters for use with dispensers and to dispensers comprising said counters. More particularly the present invention relates to counters for use with metered-dose dispensers, such as metered-dose inhalers (MDIs). In particular, the present invention provides a counter comprising: a first ring member having a first indicia and being rotatable in increments about an axis, the first indicia indicating a count; a limiting member comprising a limiting mechanism, wherein the limiting mechanism comprises an engaging portion arranged to act radially with respect to the first ring member to contact the first ring member to limit free rotation of the first ring member relative to the limiting member about the axis.
G05G 5/24 - Moyens pour empêcher, limiter ou inverser le mouvement de certaines pièces d'un mécanisme de commande, p. ex. verrouillage des organes de commande pour maintenir les organes sur un nombre indéterminé de positions, p. ex. par un secteur denté par verrouillage d'un secteur, d'une tige ou d'un organe analogue porté par l'organe de commande par engrènement sans glissement, p. ex. par cliquet
G06M 1/22 - Caractéristiques d'ordre général pour indication visuelle du résultat du comptage, sur le mécanisme de comptage, p. ex. fenêtre avec loupe
G06M 1/16 - Caractéristiques d'ordre général pour effectuer un transfert d'un étage à l'étage supérieur directement, p. ex. par croix de Malte
PHARMACEUTICAL COMBINATION COMPRISING A CLASS III RECEPTOR TYROSINE KINASE INHIBITOR AND THE ALKYLATING HISTONE-DEACETYLASE INHIBITOR FUSION MOLECULE EDO-S101 TOGETHER WITH ITS USE IN THE TREATMENT OF CANCER
The present invention is directed to a combination comprising a class III receptor tyrosine kinase inhibitor and a compound of formula I or a pharmaceutically acceptable salt thereof: to a pharmaceutical composition and to a kit both comprising said combination, to the combination, composition or kit for use in the treatment of cancer, and to a method of treatment of cancer in a patient in need thereof comprising administering to said patient an effective amount of said combination, composition or kit.
A61K 31/407 - 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 condensés avec des systèmes hétérocycliques, p. ex. kétorolac, physostigmine
A61K 31/416 - 1,2-Diazoles condensés avec des systèmes carbocycliques, p. ex. indazole
A61K 31/4184 - 1,3-Diazoles condensés avec des carbocycles, p. ex. benzimidazoles
A61K 31/4709 - Quinoléines non condensées contenant d'autres hétérocycles
A61K 31/517 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des systèmes carbocycliques, p. ex. quinazoline, périmidine
The present invention is directed to a combination comprising a glucocorticoid and a compound of formula I or a pharmaceutically acceptable salt thereof: to a pharmaceutical composition and to a kit both comprising said combination, to the combination, composition or kit for use in the treatment of cancer, and to a method of treatment of cancer in a patient in need thereof comprising administering to said patient an effective amount of said combination, composition or kit.
A61K 45/06 - Mélanges d'ingrédients actifs sans caractérisation chimique, p. ex. composés antiphlogistiques et pour le cœur
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 31/4184 - 1,3-Diazoles condensés avec des carbocycles, p. ex. benzimidazoles
A counter containing a first ring member having first indicia and a second ring member having second indicia, each of the first and second ring members being rotatable in increments about a common axis, one or both of the first and second indicia indicating a count; and a drive mechanism for rotating the first ring member and for rotating the second ring member after one or more predetermined degrees of rotation of the first ring member, wherein the drive mechanism contains a pawl-and-teeth mechanism which contains a first and second pawl engageable with a plurality of teeth, and wherein each of the first and second pawls contains a driving engagement face for engaging in a driving engagement with one of the plurality of teeth, and a sliding engagement face for sliding over one of the plurality of teeth.
The present invention relates to prolonged release pharmaceutical dosage forms comprising hydromorphone or a pharmaceutically acceptable salt thereof and naloxone or a pharmaceutically acceptable salt thereof for use in the treatment of pain.
A61K 31/485 - Dérivés du morphinane, p. ex. morphine, codéine
A61K 45/06 - Mélanges d'ingrédients actifs sans caractérisation chimique, p. ex. composés antiphlogistiques et pour le cœur
A61P 29/00 - Agents analgésiques, antipyrétiques ou anti-inflammatoires non centraux, p. ex. agents antirhumatismauxMédicaments anti-inflammatoires non stéroïdiens [AINS]
A61P 1/00 - Médicaments pour le traitement des troubles du tractus alimentaire ou de l'appareil digestif
32.
A COMBINATION OF OXYCODONE AND NALOXONE FOR USE IN TREATING PAIN IN PATIENTS SUFFERING FROM PAIN AND A DISEASE RESULTING IN INTESTINAL DYSBIOSIS AND/OR INCREASING THE RISK FOR INTESTINAL BACTERIAL TRANSLOCATION
The present invention is concerned with an oral pharmaceutical dosage form comprising oxycodone or a pharmaceutically acceptable salt thereof and naloxone or a pharmaceutically acceptable salt thereof for use in the treatment of pain in patients suffering from i) pain and at least one further disease ii), wherein said at least one further disease ii) results in intestinal dysbiosis, or for use in the treatment of pain in patients suffering from i) pain and at least one further disease iii), wherein said at least one further disease iii) increases the risk for intestinal bacterial translocation and thus for peritonitis, SIRS and/or sepsis.
The present invention provides a method of providing pain relief in a human subject in need thereof comprising administering (R)-dihydroetorphine to said subject, wherein said (R)-dihydroetorphine is administered in a dose of at least 0.01 μg/kg, preferably at least 0.05 μg/kg, and the level of respiratory depression in said subject is 65 or less % relative to the baseline level pre-administration of (R)-dihydroetorphine.
Dispensers, in particular dispensers for dispensing a dose of a gaseous, gas borne or droplet substance from a substance source and dispensers containing dosage counters are described herein.
A61M 11/04 - Pulvérisateurs ou vaporisateurs spécialement destinés à des usages médicaux agissant par pression de la vapeur des liquides à pulvériser ou vaporiser
A61M 16/12 - Préparation de gaz ou vapeurs à respirer par mélange de gaz différents
G06M 1/04 - Caractéristiques d'ordre général pour entraîner l'étage du rang le plus bas
G06M 1/08 - Caractéristiques d'ordre général pour actionner l'entraînement
The present invention relates to dispensers, in particular to dispensers for dispensing a dose of a gaseous, gas borne or droplet substance from a substance source and dispensers comprising dosage counters. The present invention therefore provides a dispenser for dispensing a dose of a gaseous, gas borne or droplet substance from a substance source, the dispenser comprising: a body (1) for receiving a substance source, the body having a mouthpiece (2); a junction member (41) slideably arranged in the body for movement in a longitudinal axis of the body to release a dose of a substance from a substance source (C), the junction member receiving a spout (S) of a substance source in a socket (43); and a dispenser driver for moving the junction member in the longitudinal axis of the body to release a dose of a substance from a substance source. A cam follower (16) is slideably arranged within the body having rigid protrusions (18a, 18b) projecting from a base (17)and the protrusion being arranged between the dispenser driver and the junction member such that a force applied by the cam of the dispenser driver to the protrusion causes the cam follower to slideably move in the longitudinal axis of the body and apply a force to the junction member so as to release a dose of a substance from a substance source. The dispenser also comprises a dispenser cap (91) comprising a hollow body having a lower open end (92) engageable with the body, and an upper open end (94) for receiving a cap closure device (120) for closing the upper open end. The dispenser also comprises a dose counter (203) for indicating a number of actuations of the dispenser corresponding to a number of doses dispensed from a substance source, or a number of doses remaining in a substance source, the dose counter comprising: a first ring member (202) having a first indicia and being rotatable in increments about the longitudinal axis, the first indicia indicating a count; and a limiting member comprising a limiting mechanism (1506), wherein the limiting mechanism comprises an engaging portion arranged to act radially with respect to the first ring member to contact the first ring member to limit free rotation of the first member relative to the limiting member about the axis.
A61M 5/00 - Dispositifs pour faire pénétrer des agents dans le corps par introduction sous-cutanée, intravasculaire ou intramusculaireAccessoires à cet effet, p. ex. dispositifs de remplissage ou de nettoyage, appuis-bras
This invention generally relates to counters and in particular to counters for use with dispensers and to dispensers comprising said counters. More particularly the present invention relates to counters for use with metered-dose dispensers, such as metered-dose inhalers (MDIs). In particular, the present invention provides a counter comprising: a first ring member having a first indicia and being rotatable in increments about an axis, the first indicia indicating a count; a limiting member comprising a limiting mechanism, wherein the limiting mechanism comprises an engaging portion arranged to act radially with respect to the first ring member to contact the first ring member to limit free rotation of the first ring member relative to the limiting member about the axis.
Benzomorphan compounds are found to be useful for treating, ameliorating or preventing pruritus, and in particular pruritus associated with (including induced by) the administration of opioids. Antipruritic activity is believed to be mediated through the dual action of the compounds as mu opioid receptor antagonists and kappa opioid receptor agonists. Pharmaceutical compositions contain therapeutically effective amounts of these useful compounds, optionally in combination with second therapeutic agents, such as opioid or non-opioid analgesics or other compounds.
A61K 31/439 - 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 le cycle formant une partie d'un système cyclique ponté, p. ex. quinuclidine
The present invention relates to a class of hydroxamic acid compounds of Formula (I), which act as alkylating agents and/or inhibitors of the HDAC pathway, having potential utility in the treatment of a neoplastic disease and immune diseases.
C07D 235/12 - Radicaux substitués par des atomes d'oxygène
C07D 235/14 - Radicaux substitués par des atomes d'azote
C07D 235/16 - Radicaux substitués par des atomes de carbone comportant trois liaisons à des hétéro-atomes, avec au plus une liaison à un halogène, p. ex. radicaux ester ou nitrile
C07D 235/24 - BenzimidazolesBenzimidazoles hydrogénés avec des hétéro-atomes ou avec des atomes de carbone comportant trois liaisons à des hétéro-atomes, avec au plus une liaison à un halogène, p. ex. radicaux ester ou nitrile, liés directement en position 2
C07D 235/30 - Atomes d'azote ne faisant pas partie d'un radical nitro
C07D 401/14 - Composés hétérocycliques contenant plusieurs hétérocycles comportant des atomes d'azote comme uniques hétéro-atomes du cycle, au moins un cycle étant un cycle à six chaînons avec un unique atome d'azote contenant au moins trois hétérocycles
C07D 403/06 - Composés hétérocycliques contenant plusieurs hétérocycles, comportant des atomes d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant deux hétérocycles liés par une chaîne carbonée ne contenant que des atomes de carbone aliphatiques
C07D 403/12 - Composés hétérocycliques contenant plusieurs hétérocycles, comportant des atomes d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant deux hétérocycles liés par une chaîne contenant des hétéro-atomes comme chaînons
C07D 403/14 - Composés hétérocycliques contenant plusieurs hétérocycles, comportant des atomes d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant au moins trois hétérocycles
C07D 413/06 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes d'azote et d'oxygène comme uniques hétéro-atomes du cycle contenant deux hétérocycles liés par une chaîne carbonée contenant uniquement des atomes de carbone aliphatiques
A61K 31/4184 - 1,3-Diazoles condensés avec des carbocycles, p. ex. benzimidazoles
The present invention relates to a class of hydroxamic acid compounds of Formula (I), which act as alkylating agents and/or inhibitors of the HDAC pathway, having potential utility in the treatment of a neoplastic disease and immune diseases.
The present invention relates to prolonged release pharmaceutical dosage forms, the manufacture thereof as well as their use for administration to human being.
The present invention relates to prolonged release pharmaceutical dosage forms, the manufacture thereof as well as their use for administration to human beings.
The present invention relates to prolonged release pharmaceutical dosage forms, the manufacture thereof as well as their use for administration to human beings.
A61J 3/10 - Dispositifs ou procédés spécialement conçus pour donner à des produits pharmaceutiques une forme physique déterminée ou une forme propre à leur administration la forme de tablettes comprimées
The present invention provides a rack for holding sample vials comprising: (i) a solid base; (ii) an upwardly extending wall around the perimeter of said base; (iii) a plurality of means for supporting a plurality of vials, each means for supporting one vial; and (iv) a means for draining liquid from said rack.
The present invention relates to dispensers, in particular to dispensers for dispensing a dose of a gaseous, gas borne or droplet substance from a substance source and dispensers comprising dosage counters. The present invention therefore provides: a dispenser for dispensing a dose of a gaseous, gas borne or droplet substance from a substance source (C), the dispenser comprising: a body for receiving a substance source, the body having a mouthpiece; a junction member slideably arranged in the body for movement in a longitudinal axis of the body to release a dose of a substance from a substance source, the junction member comprising a socket for receiving a spout of a substance source; a dispenser driver (A) for moving the junction member in the longitudinal axis of the body to release a dose of a substance from a substance source, the dispenser driver comprising a pivot shaft and a cam arranged on the shaft, the dispenser driver being arranged within the body such that rotation of the pivot shaft causes the cam to rotate and apply a force to the junction member so as to move the junction member in the longitudinal axis; and a cam follower slideably arranged within the body, the cam follower comprising a base and a substantially rigid protrusion extending from the base, the protrusion being arranged between the dispenser driver and the junction member such that a force applied by the cam of the dispenser driver to the protrusion causes the cam follower to slideably move in the longitudinal axis of the body and apply a force to the junction member so as to release a dose of a substance from a substance source.
The present invention relates to a dispenser cap arrangement for enclosing a portion of a dispenser of a medicament. In particular, the present invention relates to a dispenser cap arrangement, a dispenser cap a dispenser cap closure device, a method of closing a dispenser, and a closure arrangement. The dispenser cap arrangement comprises a dispenser cap (71) comprising a hollow body having a lower open end for engaging with a body portion of a dispenser, and an upper open end for receiving a cap closure device for closing the upper open end, the upper open end comprising an engageable portion; and a cap closure device, comprising: an upper cap closure portion (101) for engaging with the upper open end of the dispenser cap to close the upper open end of the dispenser cap; a lower cap closure portion (102) for engaging with the engageable portion to secure the cap closure device to the dispenser cap; and a bistable portion (111, 112, 113) connecting the upper cap portion and the lower cap closure portion, the bistable portion being switchable between a first stable form in which the bistable portion is extended, and a second stable form in which the bistable portion is collapsed, wherein, when the bistable portion is in the second stable form, the upper cap closure portion engages with the upper open end of the dispenser cap to close the dispenser cap.
The disclosure includes compounds of Formula (1): wherein X1, X2, Q, Z, R1, and R2 are defined herein. Also disclosed is a method for treating a neoplastic disease or an immune disease with these compounds.
C07D 417/12 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes de soufre et d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant deux hétérocycles liés par une chaîne contenant des hétéro-atomes comme chaînons
C07D 417/14 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes de soufre et d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant au moins trois hétérocycles
A61K 31/427 - Thiazoles non condensés et contenant d'autres hétérocycles
The present invention is directed to pharmaceutical compositions comprising: (a) a cyclopolysaccharide and (b) a compound of Formula (I) or its pharmaceutical acceptable salt: wherein X1, X2, Q, Z, and m are defined herein. Also disclosed is a method for treating a neoplastic disease or an immune disease with these compositions.
The present invention relates to an intranasal pharmaceutical dosage form comprising a dosing unit comprising naloxone or a pharmaceutically acceptable salt thereof in an amount of equivalent to ≥ 0.5 mg naloxone HCl dissolved in an application fluid of a volume of ≤ 250 µl. Furthermore, the present invention relates to such an intranasal pharmaceutical dosage form for use in the treatment of opioid overdosing and/or at least one symptom thereof.
The present invention provides a pharmaceutical dosage form comprising an opioid agonist and an opioid antagonist for use in the treatment of Parkinson's disease. The present invention also refers to the use of an opioid agonist and an opioid antagonist in such a dosage form.
The present invention provides a dosage form, particularly a tamper resistant dosage form, comprising; non-stretched melt extruded particulates comprising a drug selected from an opioid agonist, a tranquilizer, a CNS depressant, a CNS stimulant or a sedative hypnotic; and a matrix; wherein said melt extruded particulates are present as a discontinuous phase in said matrix.
The present invention provides a dosage form, particularly a tamper resistant dosage form, comprising: melt-extruded particulates comprising a drug; and a matrix; wherein said melt-extruded particulates are present as a discontinuous phase in said matrix.
The present invention relates to storage stable prolonged release pharmaceutical dosage forms comprising oxycodone or a pharmaceutically acceptable salt thereof and naloxone or a pharmaceutically acceptable salt thereof, the manufacture thereof as well as their use for administration to human beings.
The present invention relates to prolonged release pharmaceutical dosage forms, the manufacture thereof as well as their use for administration to human being.
The present invention relates to prolonged release pharmaceutical dosage forms comprising hydromorphone and naloxone, or salts thereof, the manufacture thereof as well as their use for administration to human beings.
The present invention relates to prolonged release pharmaceutical dosage forms, the manufacture thereof as well as their use for administration to human beings.
The present invention provides a dosage form, particularly a tamper resistant dosage form, comprising: melt-extruded particulates comprising a drug; and a matrix; wherein said melt-extruded particulates are present as a discontinuous phase in said matrix.
The present invention pertains to oral immediate release pharmaceutical compositions suitable for treating patients suffering from pain comprising oxycodone and naloxone or their pharmaceutically acceptable salts.
A counter comprising: a first ring member having first indicia and a second ring member having second indicia, each of said first and second ring members being rotatable in increments about a common axis, one or both of said first and second indicia indicating a count; a drive mechanism for rotating said first ring member; and a coupling mechanism for releasably coupling said first ring member to said second ring member, to allow said first and second ring members to rotate cooperatively when coupled and to allow independent rotating of said first ring member when not coupled; wherein said coupling mechanism comprises first and second engagement means, said first engagement means being movable radially outwardly and radially inwardly relative to said axis.
The present invention provices a counter comprising: a first member disposed in at least a partial helical turn about a longitudinal axis of an entity whose movements and/or contents are to be counted, said first member having an indicium or indicia indicative of a count; a second member extending generally in the direction of said longitudinal axis, said second member being operatively disposed in overlapping relationship under and over one or more portions of said at least partial helical turn of said first member; and means to effect relative movement between said first and second members, said movement comprising a relative incremental rotation about said longitudinal axis.
The present invention relates to a pharmaceutical composition for topical application, comprising as active ingredients (a) at least one antiseptic agent and/or at least one agent promoting wound healing, and (b) L-arginine.
The present invention provides a process for the preparation of a compound of formula (Vl), or a salt or derivative thereof, wherein R1 and R2 are independently C1-8 alkyl and * represents a stereocentre.
C07D 489/12 - Composés hétérocycliques contenant des systèmes cycliques 4 aH-8, 9 c-imino-éthano-phénantro [4, 5-b, c, d] furanne, p. ex. dérivés d'époxy-4, 5 morphinane de formule contenant des systèmes cycliques 4 aH-8, 9 c-imino-éthano-phénantro [4, 5-b, c, d] furanne condensés avec des carbocycles ou avec des systèmes carbocycliques avec un pont entre les positions 6 et 14 le pont ne contenant que deux atomes de carbone
A61K 31/4353 - 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
A61P 29/00 - Agents analgésiques, antipyrétiques ou anti-inflammatoires non centraux, p. ex. agents antirhumatismauxMédicaments anti-inflammatoires non stéroïdiens [AINS]
63.
USE OF OPIOID ANTAGONISTS FOR TREATING URINARY RETENTION
USE OF A COMBINATION OF AN OPIOID AGONIST AND AN OPIOID ANTAGONIST FOR THE TREATMENT OF CROHN´S DISEASE AND THE SYMPTOMS ASSOCIATED WITH CROHN´S DISEASE
The invention relates to amide compounds of Formula I: (I) and pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein: Y is CO or SOm; Z is each optionally substituted lower alkyl, lower alkenyl, cycloalkyl, aryl, heterocyclyl, etc.; R1 and R2 are each independently hydrogen, halogen, cyano, optionally substituted lower alky, optionally substituted cycloalkyl, optionally substituted aryl or optionally substituted heterocyclyl etc. R3 and R4 are hydrogen, each optionally substituted lower alkyl, cycloalkyl, aryl or heterocyclyl etc.; X is =O, optionally substituted lower alkyl, halogen, cyano, nitro etc., n is 0-5, m is 1 or 2 and p is 0- 2. The invention is also directed to the use compounds of Formula I to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.
A01N 43/40 - Biocides, produits repoussant ou attirant les animaux nuisibles, ou régulateurs de croissance des végétaux, contenant des composés hétérocycliques comportant des cycles avec un atome d'azote comme unique hétéro-atome du cycle des cycles à six chaînons
A61K 31/445 - Pipéridines non condensées, p. ex. pipérocaïne
67.
USE OF OPIOID FORMULATIONS IN NEEDLE-LESS DRUG DELIVERY DEVICES
The present invention concerns a needle- less drug delivery device being suitable for delivering drugs through a skin surface into a human or animal body comprising a pharmaceutical composition with at least one analgesic agent preferably being an opioid. The present invention also relates to the use of at least one analgesic agent, preferably being at least one opioid in a needle-less drug delivery device being suitable for injecting medication through a skin surface into the human or animal body. Further, the invention is concerned with a method of treating breakthrough pain by injecting at least one analgesic agent preferably being an opioid into the human or animal body using a needle- less drug delivery device.
A61K 31/485 - Dérivés du morphinane, p. ex. morphine, codéine
A61K 31/135 - Amines, p. ex. amantadine ayant des cycles aromatiques, p. ex. méthadone
A61K 31/4468 - Pipéridines non condensées, p. ex. pipérocaïne ayant un atome d'azote lié directement en position 4, p. ex. clébopride, fentanyl
A61M 5/30 - Seringues pour injection par projection, sans aiguille, p. ex. utilisables avec des ampoules ou des cartouches échangeables
A61M 5/20 - Seringues automatiques, p. ex. avec tige de piston actionnée automatiquement, avec injection automatique de l'aiguille, à remplissage automatique
A61M 37/00 - Autres appareils pour introduire des agents dans le corpsPercutanisation, c.-à-d. introduction de médicaments dans le corps par diffusion à travers la peau
A61P 25/04 - Analgésiques centraux, p. ex. opioïdes
A61M 5/19 - Seringues avec plusieurs compartiments
The present invention relates to oral pharmaceutical dosage forms comprising buprenorphine with the dosage form releasing buprenorphine instantly upon oral, preferably sublingual, application of the dosage form. The present invention also relates to the use of such dosage forms for treating pain in a human or animal or for drug substitution therapy in drug- dependent human subjects.
A device for inserting medication into a cavity of a body comprising a syringe having a barrel member and a plunger, the plunger having an end for movable interaction with the barrel member, the end comprising a seat configured to allow seating of the medication therein.
The invention relates to oxime compounds of Formula (I) and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein X is hydrogen, optionally substituted aryl, optionally substituted heteroaryl or the like; Y is CO, SO2, CR3R4 or the like; Z is optionally substituted lower alkyl, optionally substituted aryl or the like; W is optionally substituted lower alkylene or optionally substituted lower alkenylene, R3 and R4 are each independently hydrogen, lower alkyl or the like; p is 0, 1, or 2 and q is O, 1 or 2. The invention is also directed to the use compounds of Formula I to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.
A61K 31/40 - 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
C07D 207/14 - Atomes d'azote ne faisant pas partie d'un radical nitro
71.
BENZENESULFONAMIDE COMPOUNDS AND THEIR USE AS BLOCKERS OF CALCIUM CHANNELS
The invention relates to piperidinyl and hexahydroazepinyl compounds of Formula (I): and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein R1-R3, Z and q are defined as set forth in the specification. The invention is also directed to the use compounds of Formula (I) to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.
The invention relates to azetidinyl, pyrrolidinyl, piperidinyl, and hexahydroazepinyl compounds of Formula (I): and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein R1-R3, Z, p and q are defined as set forth in the specification. The invention is also directed to the use compounds of Formula (I) to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.
A61K 31/4468 - Pipéridines non condensées, p. ex. pipérocaïne ayant un atome d'azote lié directement en position 4, p. ex. clébopride, fentanyl
A61P 29/02 - Agents analgésiques, antipyrétiques ou anti-inflammatoires non centraux, p. ex. agents antirhumatismauxMédicaments anti-inflammatoires non stéroïdiens [AINS] sans effet anti-inflammatoire
The invention relates to azetidinyl, pyrrolidinyl, piperidinyl, and hexahydroazepinyl compounds of Formula I and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein R1-R3 and Z are defined as set forth in the specification. The invention is also directed to the use compounds of Formula I to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.
C07D 207/14 - Atomes d'azote ne faisant pas partie d'un radical nitro
C07D 211/42 - Atomes d'oxygène liés en position 3 ou 5
C07D 401/12 - Composés hétérocycliques contenant plusieurs hétérocycles comportant des atomes d'azote comme uniques hétéro-atomes du cycle, au moins un cycle étant un cycle à six chaînons avec un unique atome d'azote contenant deux hétérocycles liés par une chaîne contenant des hétéro-atomes comme chaînons
A61K 31/445 - Pipéridines non condensées, p. ex. pipérocaïne
A61P 25/00 - Médicaments pour le traitement des troubles du système nerveux
According to the invention glyceryl monostearate and a polymeric binder are employed as a spheronising aid in the manufacture of pharmaceutical spheroids containing no or substantially no microcrystalline cellulose. The spheroids can contain one or more therapeutically active agent which undergoes no or substantially no degradation when stored under accelerated temperature and humidity conditions. A coating may be applied to the spheroids; when present, the coating is preferably a controlled release coating.
The invention is related to gel preparations capable of absorbing as well as releasing liquid, and the use of such gel preparations in the treatment of wounds.
The invention relates to cyclourea compounds of Formula I: or a pharmaceutically acceptable salt or solvate thereof, wherein R1-R3 and Z are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.
C07D 235/02 - Composés hétérocycliques contenant des cycles diazole-1, 3 ou diazole-1, 3 hydrogéné, condensés avec d'autres cycles condensés avec des carbocycles ou avec des systèmes carbocycliques
C07D 401/06 - Composés hétérocycliques contenant plusieurs hétérocycles comportant des atomes d'azote comme uniques hétéro-atomes du cycle, au moins un cycle étant un cycle à six chaînons avec un unique atome d'azote contenant deux hétérocycles liés par une chaîne carbonée contenant uniquement des atomes de carbone aliphatiques
A61K 31/41 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à cinq chaînons avec plusieurs hétéro-atomes cycliques, l'un au moins étant l'azote, p. ex. tétrazole
A61P 29/00 - Agents analgésiques, antipyrétiques ou anti-inflammatoires non centraux, p. ex. agents antirhumatismauxMédicaments anti-inflammatoires non stéroïdiens [AINS]
A61P 25/00 - Médicaments pour le traitement des troubles du système nerveux
Methods for making trans-(-)-.DELTA.9-tetrahydrocannabinoI and trans-(+)- .DELTA.9-tetrahydrocannabinol are disclosed herein. In one embodiment, a trans-(-)-.DELTA.9-tetrahydrocannabinoI composition is prepared by allowing a composition comprising (+)-.DELTA.9- tetrahydrocannabinol to separate on a chiral stationary phase to provide a trans-(-)-.DELTA.9-tetrahydrocannabinoI composition comprising at least about 99% by weight of trans-(-)-.DELTA.9-tetrahydrocannabinol based on the total amount of trans-(-)-.DELTA.9-tetrahydrocannabinol and trans-(+)-.DELTA.9- tetrahydrocannabinol. The invention also relates to methods for treating or preventing a condition such as pain comprising administering to a patient in need thereof an effective amount of a trans-(-)-.DELTA.9- tetrahydrocannabinoI having a purity of at least about 98% based on the total weight of cannabinoids.
A61K 9/48 - Préparations en capsules, p. ex. de gélatine, de chocolat
A61K 31/352 - Composés hétérocycliques ayant l'oxygène comme seul hétéro-atome d'un cycle, p. ex. fungichromine ayant des cycles à six chaînons avec un oxygène comme seul hétéro-atome d'un cycle condensés avec des carbocycles, p. ex. cannabinols, méthanthéline
A61P 1/08 - Médicaments pour le traitement des troubles du tractus alimentaire ou de l'appareil digestif des nausées, du mal des transports ou des vertigesAntiémétiques
ABSTRACT The present invention is directed to a pharmaceutical combination comprising a
glucocorticoid and a dual function alkylating-HDACi fusion molecule which functions as an alkylating agent and also potently inhibits the HDAC pathway, and to the use thereof in the treatment of cancers including breast cancer and hematologic cancers (such as multiple myeloma, lymphoma and leukemia). Also provided are pharmaceutical compositions and kits/commercial packages that may be used in combination therapies according to the present invention. The dual function alkylating-HDACi fusion molecule is a compound of formula l or a pharmaceutically acceptable salt thereof. i ciTh,..1% - k.10H 1 Date Recue/Date Received 2021-09-16
A61K 31/4184 - 1,3-Diazoles condensés avec des carbocycles, p. ex. benzimidazoles
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 31/58 - Composés contenant des systèmes cycliques du cyclopenta[a]hydrophénanthrèneLeurs dérivés, p. ex. stéroïdes contenant des hétérocycles, p. ex. danazol, stanozolol, pancuronium ou digitogénine
There is provided tinostamustine or a pharmaceutically acceptable salt thereof for use in the treatment of ovarian cancer in a patient in need thereof.
A61K 31/337 - Composés hétérocycliques ayant l'oxygène comme seul hétéro-atome d'un cycle, p. ex. fungichromine ayant des cycles à quatre chaînons, p. ex. taxol
A61K 31/4184 - 1,3-Diazoles condensés avec des carbocycles, p. ex. benzimidazoles
A61K 41/00 - Préparations médicinales obtenues par traitement de substances par énergie ondulatoire ou par rayonnement corpusculaire
A61K 45/06 - Mélanges d'ingrédients actifs sans caractérisation chimique, p. ex. composés antiphlogistiques et pour le cœur
T-PLLTherapy There is provided tinostamustine or a pharmaceutically acceptable salt thereof for use in the treatment of T-cell prolymphocytic leukemia (T-PLL) in a patient in need thereof.
The present invention relates to co-extruded pharmaceutical compositions and dosage forms including an active agent, such as an opioid agonist, and an adverse agent, such as an opioid antagonist. Such compositions and dosage forms are useful for preventing or discouraging tampering, abuse, misuse or diversion of a dosage form containing an active pharmaceutical agent, such as an opioid. The present invention also relates to methods of treating a patient with such a dosage form, as well as kits containing such a dosage form with instructions for using the dosage form to treat a patient.
A61J 3/06 - Dispositifs ou procédés spécialement conçus pour donner à des produits pharmaceutiques une forme physique déterminée ou une forme propre à leur administration la forme de pilules, tablettes ou pastilles
A61J 3/07 - Dispositifs ou procédés spécialement conçus pour donner à des produits pharmaceutiques une forme physique déterminée ou une forme propre à leur administration la forme de capsules ou de petits conteneurs similaires à absorber par voie buccale
A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
A61K 9/24 - Pilules, pastilles ou comprimés du type à libération prolongée ou discontinue en doses unitaires constituées de couches ou feuilletées
A61K 45/06 - Mélanges d'ingrédients actifs sans caractérisation chimique, p. ex. composés antiphlogistiques et pour le cœur
A61K 47/32 - Composés macromoléculaires obtenus par des réactions faisant intervenir uniquement des liaisons non saturées carbone-carbone, p. ex. carbomères
A61P 25/04 - Analgésiques centraux, p. ex. opioïdes
83.
METHODS FOR MAKING 3-O-PROTECTED MORPHINONES AND 3-O-PROTECTED MORPHINONE DIENOL CARBOXYLATES
Disclosed are methods for making aldehydes and ketones comprising allowing the corresponding primary or secondary alcohol to react in the presence of trichoroisocyanuric acid, a compound of formula R1SR2 and a base. In one embodiment, the alcohol is a compound of formula (I) wherein R3 is a protecting group. Also disclosed are methods for making 3-O-protected morphine dienol carboxylates comprising allowing a compound of formula (I) to oxidize in the presence of a chlorine-containing compound and a compound of formula R1SR2; and allowing the product of the oxidation step to react with an acylating agent.
C07B 41/06 - Formation ou introduction de groupes fonctionnels contenant de l'oxygène de groupes carbonyle
C07C 45/29 - Préparation de composés comportant des groupes C=O liés uniquement à des atomes de carbone ou d'hydrogènePréparation des chélates de ces composés par oxydation de groupes hydroxyle
C07D 489/02 - Composés hétérocycliques contenant des systèmes cycliques 4 aH-8, 9 c-imino-éthano-phénantro [4, 5-b, c, d] furanne, p. ex. dérivés d'époxy-4, 5 morphinane de formule avec des atomes d'oxygène liés en position 3 et 6, p. ex. morphine, morphinone
C07F 7/10 - Composés comportant une ou plusieurs liaisons C—Si azotés
The present invention provides abuse-resistant transdermal delivery devices containing an opioid agonist intended for analgesic purposes in pain patients.
85.
RESOLUTION AND PURIFICATION OF TRANS-(-)-DELTA-9-TETRAHYDROCANNABINOL AND TRANS-(+)-DELTA-9-TETRAHYDROCANNABINOL BY CHIRAL CHROMATOGRAPHY
Methods for making trans-(-)-.DELTA.9-tetrahydrocannabinoI and trans-(+)- .DELTA.9-tetrahydrocannabinol are disclosed herein. In one embodiment, a trans- (-)-.DELTA.9-tetrahydrocannabinoI composition is prepared by allowing a composition comprising (~)-.DELTA.9-tetrahydrocannabinol to separate on a chiral stationary phase to provide a trans-(-)-.DELTA.9-tetrahydrocannabinoI composition comprising at least about 99% by weight of trans-(-)-.DELTA.9- tetrahydrocannabinol based on the total amount of trans-(-)-.DELTA.9- tetrahydrocannabinol and trans-(+)-.DELTA.9-tetrahydrocannabinol. The invention also relates to methods for treating or preventing a condition such as pain comprising administering to a patient in need thereof an effective amount of a trans-(-)-.DELTA.9-tetrahydrocannabinoI having a purity of at least about 98% based on the total weight of cannabinoids.
A61K 31/352 - Composés hétérocycliques ayant l'oxygène comme seul hétéro-atome d'un cycle, p. ex. fungichromine ayant des cycles à six chaînons avec un oxygène comme seul hétéro-atome d'un cycle condensés avec des carbocycles, p. ex. cannabinols, méthanthéline
A61P 1/08 - Médicaments pour le traitement des troubles du tractus alimentaire ou de l'appareil digestif des nausées, du mal des transports ou des vertigesAntiémétiques
A61P 3/00 - Médicaments pour le traitement des troubles du métabolisme
A61P 29/00 - Agents analgésiques, antipyrétiques ou anti-inflammatoires non centraux, p. ex. agents antirhumatismauxMédicaments anti-inflammatoires non stéroïdiens [AINS]
(VI)The present invention provides a process for the preparation of a compound of formula (VI), or a salt or derivative thereof, wherein R1 and R2 are independently C1-8 alkyl and * represents a stereocentre.
A61K 31/4353 - 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
A61P 29/00 - Agents analgésiques, antipyrétiques ou anti-inflammatoires non centraux, p. ex. agents antirhumatismauxMédicaments anti-inflammatoires non stéroïdiens [AINS]
C07D 489/12 - Composés hétérocycliques contenant des systèmes cycliques 4 aH-8, 9 c-imino-éthano-phénantro [4, 5-b, c, d] furanne, p. ex. dérivés d'époxy-4, 5 morphinane de formule contenant des systèmes cycliques 4 aH-8, 9 c-imino-éthano-phénantro [4, 5-b, c, d] furanne condensés avec des carbocycles ou avec des systèmes carbocycliques avec un pont entre les positions 6 et 14 le pont ne contenant que deux atomes de carbone
87.
PROCESS FOR PREPARING OXYCODONE HYDROCHLORIDE HAVING LESS THAN 25 PPM 14-HYDROXYCODEINONE
In certain embodiments the invention is directed to a process for preparing an oxycodone hydrochloride composition having less than 25 ppm of 14-hydroxycodeinone.
The present invention relates to storage stable prolonged release pharmaceutical dosage forms comprising oxycodone or a pharmaceutically acceptable salt thereof and naloxone or a pharmaceutically acceptable salt thereof, the manufacture thereof as well as their use for administration to human beings.
The present invention relates to an intranasal pharmaceutical dosage form comprising a dosing unit comprising naloxone or a pharmaceutically acceptable salt thereof in an amount of equivalent to = 0.5 mg naloxone HCl dissolved in an application fluid of a volume of = 250 µl. Furthermore, the present invention relates to such an intranasal pharmaceutical dosage form for use in the treatment of opioid overdosing and/or at least one symptom thereof.
It is possible to effectively treat moderate to severe visceral pain by administering analgesic medications comprising the opioid oxycodone or pharmaceutically acceptable salts thereof. Visceral pain and especially acute (i.e. non-chronic) visceral pain can be effectively treated by administering oxycodone at a dosage which is lower than the corresponding dosage of other opioids like morphine.
The present invention is directed to a process for reducing the level of .alpha., .beta.- unsaturated ketone in an opioid analgesic composition by hydrogentation with diimide or a diimide progenitor.
In certain embodiments the invention is directed to a process for preparing an oxycodone salt composition having less than 25 ppm of 14-hydroxycodeinone, and to an oxycodone salt composition and a pharmaceutical dosage form thereof, having less than 25 ppm 14-hydroxycodeinone.
The present invention relates to prolonged release pharmaceutical dosage forms comprising hydromorphone or a pharmaceutically acceptable salt thereof and naloxone or a pharmaceutically acceptable salt thereof for use in the treatment of pain.
A61K 31/485 - Dérivés du morphinane, p. ex. morphine, codéine
A61K 45/06 - Mélanges d'ingrédients actifs sans caractérisation chimique, p. ex. composés antiphlogistiques et pour le cœur
A61P 1/00 - Médicaments pour le traitement des troubles du tractus alimentaire ou de l'appareil digestif
A61P 29/00 - Agents analgésiques, antipyrétiques ou anti-inflammatoires non centraux, p. ex. agents antirhumatismauxMédicaments anti-inflammatoires non stéroïdiens [AINS]
94.
USE OF A BENZIMIDAZOLE ALKYLATING HDAC INHIBITOR IN COMBINATION WITH A PROTEOSOME INHIBITOR IN THE TREATMENT OF CANCER
The present invention is directed to a combination comprising a proteasome inhibitor and a compound of formula (I), or a pharmaceutically acceptable salt thereof: to a pharmaceutical composition and to a kit both comprising said combination, to the combination, composition or kit for use in the treatment of cancer, and to a method of treatment of cancer in a patient in need thereof comprising administering to said patient an effective amount of said combination, composition or kit.
There is provided a compound of formula I or a pharmacologically acceptable salt thereof: for use in the treatment of a brain cancer selected from a MGMT positive astrocytic brain tumour, a metastatic brain cancer and primary CNS lymphoma and a method of treating said brain cancers in a patient in need thereof comprising administering to the patient said compound of formula I or a pharmacologically acceptable salt thereof.
Compound for Use in the Treatment of Hodgkin LymphomaThere is provided a compound of formula l or a pharmacologically acceptable salt thereof for use in a method of treating Hodgkin lymphoma in a patient in need thereof comprising administering to said patient an effective amount of said compound of formula l or a pharmacologically acceptable salt thereof:(see formula I)a combination of said compound of formula l or a pharmaceutically acceptable salt thereof with Brentuximab Vedotin and said combination for use in a method of treating Hodgkin lymphoma in a patient in need thereof comprising administering to said patient an effective amount of said combination.
A61K 31/4184 - 1,3-Diazoles condensés avec des carbocycles, p. ex. benzimidazoles
A61K 47/68 - 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 anticorps, une immunoglobuline ou son fragment, p. ex. un fragment Fc
In certain embodiments the invention is directed to a process for preparing an
oxycodone salt composition having less than 25 ppm of 14-hydroxycodeinone, and to an oxycodone salt composition and a pharmaceutical dosage form thereof, having less than 25 ppm 14-hydroxycodeinone .
Disclosed are methods for making aldehydes and ketones comprising allowing the corresponding primary or secondary alcohol to react in the presence of trichoroisocyanuric acid, a compound of formula R1SR2 and a base. In one embodiment, the alcohol is a compound of formula (I) wherein R3 is a protecting group. Also disclosed are methods for making 3-0-protected morphine dienol carboxylates comprising allowing a compound of formula (I) to oxidize in the presence of a chlorine-containing compound and a compound of formula R1SR2; and allowing the product of the oxidation step to react with an acylating agent.
C07B 41/06 - Formation ou introduction de groupes fonctionnels contenant de l'oxygène de groupes carbonyle
C07C 45/29 - Préparation de composés comportant des groupes C=O liés uniquement à des atomes de carbone ou d'hydrogènePréparation des chélates de ces composés par oxydation de groupes hydroxyle
C07D 489/02 - Composés hétérocycliques contenant des systèmes cycliques 4 aH-8, 9 c-imino-éthano-phénantro [4, 5-b, c, d] furanne, p. ex. dérivés d'époxy-4, 5 morphinane de formule avec des atomes d'oxygène liés en position 3 et 6, p. ex. morphine, morphinone
C07F 7/10 - Composés comportant une ou plusieurs liaisons C—Si azotés
The present invention is directed to pharmaceutical compositions comprising: (a) a cyclopolysaccharide and (b) a compound of Formula (I) or its pharmaceutical acceptable salt: wherein X1, X2, Q, Z, and m are defined herein. Also disclosed is a method for treating a neoplastic disease or an immune disease with these compositions.
The disclosure includes compounds of Formula (1): wherein X1, X2, Q, Z, R1, and R2 are defined herein. Also disclosed is a method for treating a neoplastic disease or an immune disease with these compounds.
C07D 417/12 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes de soufre et d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant deux hétérocycles liés par une chaîne contenant des hétéro-atomes comme chaînons
C07D 417/14 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes de soufre et d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant au moins trois hétérocycles
brevets
