The present disclosure relates to: a) a crystalline composition of essentially pure Form IV of N—((R)-2,3-dihydroxypropoxy)-3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-benzamide; b) pharmaceutical compositions comprising the crystalline composition of essentially pure Form IV of N—((R)-2,3-dihvdroxypropoxy)-3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-benzamide, and, optionally, a pharmaceutically acceptable carrier; and c) methods of treating a tumor, a cancer, or a Rasopathy disorder by administering the crystalline composition of essentially pure Form IV of N—((R)-2,3-dihydroxypropoxy)-3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-benzamide to a subject in need thereof.
C07C 237/28 - Amides d'acides carboxyliques, le squelette carboné de la partie acide étant substitué de plus par des groupes amino ayant l'atome de carbone d'au moins un des groupes carboxamide lié à un atome de carbone d'un cycle aromatique à six chaînons non condensé du squelette carboné
2.
COMPOSITIONS OF ESSENTIALLY PURE FORM IV OF N-((R)-2,3- DIHYDROXYPROPOXY)-3,4-DIFLUORO-2- (2-FLUORO-4-IODOPHENYLAMINO)- BENZAMIDE AND USES THEREOF
The present disclosure relates to: a) a crystalline composition of essentially pure Form IV of N-((R)-2,3-dihydroxypropoxy)-3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-benzamide; b) pharmaceutical compositions comprising the crystalline composition of essentially pure Form IV of N-((R)-2,3-dihydroxypropoxy)-3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-benzamide, and, optionally, a pharmaceutically acceptable carrier; and c) methods of treating a tumor, a cancer, or a Rasopathy disorder by administering the crystalline composition of essentially pure Form IV of N-((R)-2,3-dihydroxypropoxy)-3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-benzamide to a subject in need thereof.
C07C 259/10 - Composés contenant des groupes carboxyle, un atome d'oxygène d'un groupe carboxyle étant remplacé par un atome d'azote, cet atome d'azote étant lié de plus à un atome d'oxygène et ne faisant pas partie de groupes nitro ou nitroso sans remplacement de l'autre atome d'oxygène du groupe carboxyle, p. ex. acides hydroxamiques ayant des atomes de carbone de groupes hydroxamique liés à des atomes de carbone de cycles aromatiques à six chaînons
A61K 31/166 - Amides, p. ex. acides hydroxamiques ayant des cycles aromatiques, p. ex. colchicine, aténolol, progabide ayant l'atome de carbone d'un groupe carboxamide lié directement au cycle aromatique, p. ex. procaïnamide, procarbazine, métoclopramide, labétalol
The present disclosure relates to: a) a crystalline composition of essentially pure Form IV of N-((R)-2,3-dihydroxypropoxy)-3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-benzamide; b) pharmaceutical compositions comprising the crystalline composition of essentially pure Form IV of N-((R)-2,3-dihydroxypropoxy)-3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-benzamide, and, optionally, a pharmaceutically acceptable carrier; and c) methods of treating a tumor, a cancer, or a Rasopathy disorder by administering the crystalline composition of essentially pure Form IV of N-((R)-2,3-dihydroxypropoxy)-3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-benzamide to a subject in need thereof.
C07C 237/28 - Amides d'acides carboxyliques, le squelette carboné de la partie acide étant substitué de plus par des groupes amino ayant l'atome de carbone d'au moins un des groupes carboxamide lié à un atome de carbone d'un cycle aromatique à six chaînons non condensé du squelette carboné
A61K 9/48 - Préparations en capsules, p. ex. de gélatine, de chocolat
The present disclosure relates to: a) a crystalline composition of essentially pure Form IV of N—((R)-2,3-dihydroxypropoxy)-3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-benzamide; b) pharmaceutical compositions comprising the crystalline composition of essentially pure Form IV of N—((R)-2,3-dihydroxypropoxy)-3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-benzamide, and, optionally, a pharmaceutically acceptable carrier; and c) methods of treating a tumor, a cancer, or a Rasopathy disorder by administering the crystalline composition of essentially pure Form IV of N—((R)-2,3-dihydroxypropoxy)-3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-benzamide to a subject in need thereof.
C07C 237/28 - Amides d'acides carboxyliques, le squelette carboné de la partie acide étant substitué de plus par des groupes amino ayant l'atome de carbone d'au moins un des groupes carboxamide lié à un atome de carbone d'un cycle aromatique à six chaînons non condensé du squelette carboné
A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
A61K 9/48 - Préparations en capsules, p. ex. de gélatine, de chocolat
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
(1) Pharmaceutical preparations for the prevention and treatment of psychiatric diseases, degenerative nerve diseases and brain disorders, namely, mood, anxiety and cognitive disorders, Alzheimer's disease, cerebral palsy, Parkinson's disease, Huntington's disease and multiple sclerosis; Pharmaceutical preparations for the prevention and treatment of cranial and facial nerve disorders, connective tissue injuries, diseases and disorders, bone and cartilage injuries, diseases and disorders; Pharmaceutical preparations for the prevention and treatment of neuromuscular and neurological diseases and disorders, namely, central nervous system diseases and disorders, namely central nervous system infections, brain diseases, central nervous system movement disorders, muscle diseases and disorders, namely inflammatory muscle diseases and disorders and muscular dystrophy, ocular motility and spinal cord infections, injuries and diseases, and seizure disorders; Pharmaceutical preparations for the prevention and treatment of genitourinary diseases, namely, inflammatory pelvic, vaginitis, dysmenorrhea, cervix erosion, cervicitis, trachelitis, uterine cervicitis, endomitriosis, sexually transmitted diseases, erectile and sexual dysfunction, infertility and incontinence; Pharmaceutical preparations for the prevention and treatment of cardiovascular, gastrointestinal, hematologic, oncological, ophthalmological and respiratory system diseases and disorders; Pharmaceutical preparations for the prevention and treatment of auto-immune diseases and disorders, namely collagen disease, rheumatoid arthritis, systemic lupus erythematosus, alopecia areata, and systemic sclerosis; Pharmaceutical preparations for the prevention and treatment of allergies, hypertension, menopause, diabetic neuropathy, arthritis, and pain; Antibiotics, anti-infectives, anti-inflammatories, anti-fungals, antivirals, oral and injectable pharmaceutical contraceptives, human vaccines; Pharmaceutical preparations for the prevention and treatment of smoking habits and addictions; Pharmaceutical preparations for the prevention and treatment of renal disease and disorders; Pharmaceutical preparations for the prevention and treatment of diseases, disorders and infections of the endocrine system, namely growth and thyroid disorders; Pharmaceutical preparations for the prevention and treatment of muscular atrophy; Pharmaceutical preparations for the prevention and treatment of inflammatory diseases, namely inflammatory bowel diseases, inflammatory joint diseases, inflammatory connective tissue diseases, inflammatory muscle diseases and disorders; Pharmaceutical preparations for the prevention and treatment of metabolic diseases and disorders, namely diabetes, hypoglycemia, muscular dystrophy, sickle cell disease, non-alcoholic steatohepatitis and anemia; Pharmaceutical preparations for the prevention and treatment of dermatological diseases and conditions, namely eczema, atopic dermatitis, psoriasis, bacterial skin infections, fungal skin infections, viral skin infections, parasitic skin infections, acne, pyoderma, skin erosion, ulcer, skin wounds, burned skin, pain and inflammation.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
(1) Pharmaceutical preparations for the prevention and treatment of psychiatric diseases, degenerative nerve diseases and brain disorders, namely, mood, anxiety and cognitive disorders, Alzheimer's disease, cerebral palsy, Parkinson's disease, Huntington's disease and multiple sclerosis; Pharmaceutical preparations for the prevention and treatment of cranial and facial nerve disorders, connective tissue injuries, diseases and disorders, bone and cartilage injuries, diseases and disorders; Pharmaceutical preparations for the prevention and treatment of neuromuscular and neurological diseases and disorders, namely, central nervous system diseases and disorders, namely central nervous system infections, brain diseases, central nervous system movement disorders, muscle diseases and disorders, namely inflammatory muscle diseases and disorders and muscular dystrophy, ocular motility and spinal cord infections, injuries and diseases, and seizure disorders; Pharmaceutical preparations for the prevention and treatment of genitourinary diseases, namely, inflammatory pelvic, vaginitis, dysmenorrhea, cervix erosion, cervicitis, trachelitis, uterine cervicitis, endomitriosis, sexually transmitted diseases, erectile and sexual dysfunction, infertility and incontinence; Pharmaceutical preparations for the prevention and treatment of cardiovascular, gastrointestinal, hematologic, oncological, ophthalmological and respiratory system diseases and disorders; Pharmaceutical preparations for the prevention and treatment of auto-immune diseases and disorders, namely collagen disease, rheumatoid arthritis, systemic lupus erythematosus, alopecia areata, and systemic sclerosis; Pharmaceutical preparations for the prevention and treatment of allergies, hypertension, menopause, diabetic neuropathy, arthritis, and pain; Antibiotics, anti-infectives, anti-inflammatories, antifungal medication, anti-virals, oral and injectable pharmaceutical contraceptives, human vaccines; Pharmaceutical preparations for the prevention and treatment of smoking habits and addictions; Pharmaceutical preparations for the prevention and treatment of renal disease and disorders; Pharmaceutical preparations for the prevention and treatment of diseases, disorders and infections of the endocrine system, namely growth and thyroid disorders; Pharmaceutical preparations for the prevention and treatment of muscular atrophy; Pharmaceutical preparations for the prevention and treatment of inflammatory diseases, namely inflammatory bowel diseases, inflammatory joint diseases, inflammatory connective tissue diseases, inflammatory muscle diseases and disorders; Pharmaceutical preparations for the prevention and treatment of metabolic diseases and disorders, namely diabetes, hypoglycemia, muscular dystrophy, sickle cell disease, non-alcoholic steatohepatitis and anemia; Pharmaceutical preparations for the prevention and treatment of dermatological diseases and conditions, namely eczema, atopic dermatitis, psoriasis, bacterial skin infections, fungal skin infections, viral skin infections, parasitic skin infections, acne, pyoderma, skin erosion, ulcer, skin wounds, burned skin, pain and inflammation
This invention provides quinazoline compounds of the formula:
2; m is 1-3; and X is O, S or NH; or a pharmaceutically acceptable salt thereof, as well as processes and intermediate compounds for making them, useful pharmaceutical compositions and methods of using the compounds in the treatment of proliferative diseases.
A61K 31/517 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des systèmes carbocycliques, p. ex. quinazoline, périmidine
A01N 43/90 - Biocides, produits repoussant ou attirant les animaux nuisibles, ou régulateurs de croissance des végétaux, contenant des composés hétérocycliques comportant plusieurs hétérocycles déterminants condensés entre eux ou avec un système carbocyclique commun
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Pharmaceutical and veterinary preparations; sanitary preparations for medical purposes; dietetic substances adapted for medical use.
14.
NOVEL FORMS OF ⏧R-(R*,R*)]-2-(4-FLUOROPHENYL)-B,B-DIHYDROXY-5-(1-METHYLETHYL)-3-PHENYL-4-⏧(PHENYLAMINO)CARBONYL]-1H-PYRROLE-1-HEPT ANOIC ACID MAGNESIUM
Novel forms of atorvastatin magnesium salt designated Form A, Form B, Form C, Form D, Form E, and Form F, pharmaceutical compositions containing such compounds, methods for their preparation and methods utilizing the compounds for treatment of hyperlipidemia, hypercholesterolemia, osteoporosis, benign prostatic hyperplasia (BPH) and Alzheimer's disease are described.
C07D 207/34 - 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 comportant deux liaisons doubles entre chaînons cycliques ou entre chaînons cycliques et chaînons non cycliques 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 aux atomes de carbone du cycle
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
A61P 19/10 - Médicaments pour le traitement des troubles du squelette des maladies osseuses, p. ex. rachitisme, maladie de Paget de l'ostéoporose
A61P 25/28 - Médicaments pour le traitement des troubles du système nerveux des troubles dégénératifs du système nerveux central, p. ex. agents nootropes, activateurs de la cognition, médicaments pour traiter la maladie d'Alzheimer ou d'autres formes de démence
This invention provides quinazoline compounds of the formula:
2; m is 1-3; and X is O, S or NH; or a pharmaceutically acceptable salt thereof, as well as processes and intermediate compounds for making them, useful pharmaceutical compositions and methods of using the compounds in the treatment of proliferative diseases.
A61K 31/517 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des systèmes carbocycliques, p. ex. quinazoline, périmidine
C07D 413/12 - 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 contenant des hétéro-atomes comme chaînons
Disclosed are polymorphs of the isethionate salt of 6-acetyl-8-cyclopentyl-5-methyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-8H-pyrido[2,3-d]pyrimidin-7-one,
which is a selective cyclin-dependent kinase 4 (CDK4) inhibitor useful for treating inflammation and cell proliferative diseases such as cancer and restenosis.
Disclosed are polymorphs of the isethionate salt of 6-acetyl-8-cyclopentyl-5- methyl-2~(5-piperazin-1-yl-pyridin-2-ylamino)-8H-pyrido[2,3-d]pyrimidin-7-one, which is a selective cyclin-dependent kinase 4 (CDK4) inhibitor useful for treating inflammation and cell proliferative diseases such as cancer and restenosis.
The present disclosure relates to: a) a crystalline composition of essentially pure Form IV of N-((R)-2,3-dihydroxypropoxy)-3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-benzamide; b) pharmaceutical compositions comprising the crystalline composition of essentially pure Form IV of N-((R)-2,3-dihydroxypropoxy)-3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-benzamide, and, optionally, a pharmaceutically acceptable carrier; and c) methods of treating a tumor, a cancer, or a Rasopathy disorder by administering the crystalline composition of essentially pure Form IV of N-((R)-2,3-dihydroxypropoxy)-3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-benzamide to a subject in need thereof.
A61K 31/166 - Amides, p. ex. acides hydroxamiques ayant des cycles aromatiques, p. ex. colchicine, aténolol, progabide ayant l'atome de carbone d'un groupe carboxamide lié directement au cycle aromatique, p. ex. procaïnamide, procarbazine, métoclopramide, labétalol
A61P 17/00 - Médicaments pour le traitement des troubles dermatologiques
The invention provides quinazoline compounds of the formula: wherein R1 is halo; R2 is H or halo; R3 is a) C1-C3 alkyl, optionally substituted by halo; or b) -(CH2)n-morpholino, -(CH2)n-piperidine, -(CH2)n-piperazine, -(CH2)n- piperazine-N(C1-C3 alkyl), -(CH2)n-pyrrolidine, or -(CH2)n imidazole; n is 1 to 4; R4 is -(CH2)m-Het; Het is morpholine,piperidine, piperazine, piperazine- N(C1-C3 alkyl), imidazole,pyrrolidine, azepane, 3,4-dihydro-2H-pyridine, or 3,6-dihydro-2H-pyridine, each optionally substituted by alkyl, halo, OH, NH2, NH(C1-C3 alkyl) or N (C1-C3 alkyl)2; m is 1-3; and X is O, S or NH; or a pharmaceutically acceptable salt thereof, as well as processes and intermediate compounds for making them, useful pharmaceutical compositions and methods of using the compounds in the treatment of proliferative diseases.
A61K 31/517 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime condensées en ortho ou en péri avec des systèmes carbocycliques, p. ex. quinazoline, périmidine
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
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 403/12 - 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 413/12 - 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 contenant des hétéro-atomes comme chaînons
C07D 413/14 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes d'azote et d'oxygène comme uniques hétéro-atomes du cycle contenant au moins trois hétérocycles
A dispensing device for dispensing a liquid desired by a user is disclosed. The device includes a cover having an aperture, and a dispensing assembly coupled to the cover. The dispensing assembly includes a container for storing the liquid, and a liquid transport mechanism for drawing the liquid out of the container and dispensing through a nozzle, the nozzle being provided within the cover. The nozzle is in alignment with the aperture in a dispensing position, and the nozzle is out of alignment with the aperture in a storage position.
A dispensing device for a material to be activated by a user is disclosed. The device includes a container for storing an amount of material, a material dispensing assembly coupled to the container for dispensing an amount of material through an orifice, and a cover coupled to the container. The cover includes a member provided above the liquid dispensing assembly forming an opening. The user activates the liquid dispensing assembly by inserting a finger into the opening and applying pressure to the liquid dispensing assembly.