Disclosed are a minoxidil-containing suspension, a preparation method therefor, and a use thereof. The suspension comprises, by total weight: about 2% to about 15% of minoxidil; about 0.05% to about 2% of an ionic stabilizer; about 0.1% to about 10% of a steric stabilizer; about 0% to about 80% of a solubilizer; and about 10% to about 97% of water.
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 47/28 - Stéroïdes, p. ex. cholestérol, acides biliaires ou acide glycyrrhétinique
A61K 47/20 - Composés organiques, p. ex. hydrocarbures naturels ou synthétiques, polyoléfines, huile minérale, gelée de pétrole ou ozocérite contenant du soufre, p. ex. sulfoxyde de diméthyle [DMSO], docusate, laurylsulfate de sodium ou acides aminosulfoniques
A61P 17/14 - Médicaments pour le traitement des troubles dermatologiques pour le traitement de la calvitie ou de l'alopécie
2.
CRYSTAL FORM OF SELECTIVE PARP-1 INHIBITOR HYDROCHLORIDE, PREPARATION METHOD THEREFOR AND USE THEREOF
The present disclosure relates to the field of pharmaceutical chemistry. Specifically, the present invention relates to a crystal form of a selective PARP-1 inhibitor hydrochloride, i.e., a crystal form of a hydrochloride of compound A having a structure of 2-(1-cyclohexylpiperidin-4-yl)-3-oxo-2,3-dihydro-1H-isoindole-4-carboxylic acid amide, a preparation method therefor, and a use thereof. The crystal form of the hydrochloride of compound A provided by the present disclosure has at least one of the following excellent characteristics: good stability, high purity, good solubility, good dissolution, high bioavailability, low hygroscopicity, high melting point, good fluidity, good mechanical stress stability, good machinability such as good compressibility, good crystal morphology, good compression resistance, stable storage, avoiding crystal transformation of a drug during development and storage, simple and reliable preparation method, and great development value.
C07D 401/04 - 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 liaison directe de chaînon cyclique à chaînon cyclique
The present disclosure belongs to the field of pharmaceutical formulations, and particularly relates to a compound composition of adapalene and dapsone for topical dermal use, a preparation method therefor, and use thereof. The composition of the present disclosure has at least one of the following excellent characteristics: high solubility of drug active ingredients in a carrier, small particle size of drug particles, stable particle size, good skin absorption, high in-vitro release efficiency, small particle size of composition oil drops, good stability, good therapeutic effect, small skin irritation, and good placement stability. The composition of the present disclosure can be directly used as a formulation, or can be further prepared into formulations of different dosage forms after other carriers are added.
A61K 31/192 - Acides carboxyliques, p. ex. acide valproïque ayant des groupes aromatiques, p. ex. sulindac, acides 2-aryl-propioniques, acide éthacrynique
A61K 31/136 - Amines, p. ex. amantadine ayant des cycles aromatiques, p. ex. méthadone ayant le groupe amino lié directement au cycle aromatique, p. ex. benzène-amine
A61K 31/145 - Amines, p. ex. amantadine ayant des atomes de soufre, p. ex. thiurames (N-C(S)-S-C(S)-N ou N-C(S)-S-S-C(S)-N)Sulfinylamines (-N=SO)Sulfonylamines (-N=SO2)
The present disclosure belongs to the field of pharmaceutical formulations and particularly relates to a composition with a synergistic therapeutic effect on acne lesions and a preparation method therefor and use thereof. The composition provided by the present disclosure comprises active ingredients adapalene and dapsone, which exhibit a synergistic therapeutic effect on inflammatory acne lesions when used in combination. Compared with corresponding single drugs, the composition can significantly reduce the number of inflammatory lesions; meanwhile, relative to the topical use of adapalene alone, the composition of the present disclosure can mitigate skin irritation reactions caused by adapalene and exhibits good safety.
A61K 31/145 - Amines, p. ex. amantadine ayant des atomes de soufre, p. ex. thiurames (N-C(S)-S-C(S)-N ou N-C(S)-S-S-C(S)-N)Sulfinylamines (-N=SO)Sulfonylamines (-N=SO2)
A61K 31/136 - Amines, p. ex. amantadine ayant des cycles aromatiques, p. ex. méthadone ayant le groupe amino lié directement au cycle aromatique, p. ex. benzène-amine
A61K 31/192 - Acides carboxyliques, p. ex. acide valproïque ayant des groupes aromatiques, p. ex. sulindac, acides 2-aryl-propioniques, acide éthacrynique
A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
The present disclosure relates to the field of pharmaceutical chemistry, and specifically relates to a crystal form of a selective PARP-1 inhibitor, i.e. a crystal form of a compound represented by formula (I), a preparation method therefor and the use thereof. The crystal form of the compound represented by formula (I) provided by the present disclosure has at least one of the following excellent characteristics: good stability, high purity, good solubility, good dissolution, high bioavailability, low hygroscopicity, good fluidity, good mechanical stress stability, good processability, such as good compressibility, good crystal morphology, good pressure resistance, capability of stable storage, capability of avoiding crystal transformation of a drug during development and storage processes, a simple and reliable preparation method and high development value.
C07D 401/04 - 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 liaison directe de chaînon cyclique à chaînon cyclique
A61K 31/454 - Pipéridines non condensées, p. ex. pipérocaïne contenant d'autres systèmes hétérocycliques contenant un cycle à cinq chaînons avec l'azote comme hétéro-atome du cycle, p. ex. pimozide, dompéridone
05 - Produits pharmaceutiques, vétérinaires et hygièniques
Produits et services
Medicated dermatological preparations and substances; Gels, creams and solutions for dermatological use; Medicated creams for treating dermatological conditions; Analgesic and anti-inflammatory preparations; Haemorrhoid preparations; Acne treatment preparations; Preparations for the treatment of burns; Medicated ointments for treating dermatological conditions; Dermatological preparations; Balsamic preparations for medical purposes; Preparations for treating colds; Antibiotic ointments; Anti-itch ointment; Pain relief medication; Medicinal preparations for stimulating hair growth
7.
CRYSTAL FORM OF RP-6306, AND PREPARATION METHOD THEREFOR AND USE THEREOF
A crystal form of Lunresertib (also referred to as RP-6306), and a preparation method therefor and the use thereof. The crystal form has at least one of the following excellent characteristics: good stability, high purity, good solubility, good dissolution, low hygroscopicity, good fluidity, good processibility, for example, good compressibility, more stable pressed tablets, good crystal morphology and good pressure resistance, and can be stably stored and prevent the drug from undergoing crystal transformation during the development process and storage, and the preparation method is simple and reliable. Therefore, the crystal form has a high development value.
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 31/495 - 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
This application relates to the field of chemistry of drugs. It relates to a lazertinib monomethanesulfonate hydrate crystal form, its preparation method thereof and uses. The crystal form of lazertinib monomethanesulfonate hydrate provided in this application has at least one of the following advantageous properties: good stability, high solubility, good dissolution, low hygroscopicity, uniform particle size distribution, favorable morphology, good flowability, and high crystallinity. These characteristics contribute to stable storage, preventing degradation, increased impurities, changes in appearance, and crystallization during development and storage. The preparation method is simple and reliable, offering significant development value.
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
A61K 31/5377 - 1,4-Oxazines, p. ex. morpholine non condensées et contenant d'autres hétérocycles, p. ex. timolol
9.
Crystal and amorphous form of tolebrutinib, preparation method therefor, and use thereof
The present application provides a crystalline form of tolebrutinib, an amorphous form, and a method of preparation thereof and a use thereof, and the crystalline form of tolebrutinib provided in the present application has at least one of the following advantages: good stability, low moisture attraction, uniform particle size distribution, solubility meeting the requirements for medicinal use, stable storage, avoiding phase transformation of the drug in the process of development and in storage, and a reliable method for the preparation thereof, which has a great development value. The amorphous form of tolebrutinib provided in this application, while possessing better solubility than that of tolebrutinib in the crystalline state, still possesses good stability of placement and acceptable hygroscopicity, and has high medicinal value.
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
10.
CRYSTAL FORM OF AZD5305, PREPARATION METHOD THEREFOR, AND USE THEREFOR
The present application relates to the field of chemical synthesis of pharmaceutics. Specifically, the present application relates to a crystal form of AZD5305, a preparation method therefor, and use thereof. The crystal form provided by the present application has at least one of the following improved features: good stability, low hygroscopicity, good solubility, good dissolution performance, high purity, good fluidity, good druggability such as good compressibility and higher stability in tablet formulations after tableting, good crystal morphology, good stress resistance, and stability in storage that can avoid the crystal transition of drugs in the development process and storage. The prevent invention features a simple and reliable preparation method and has great development value.
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
A61K 31/4375 - 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 six chaînons ayant l'azote comme hétéro-atome du cycle, p. ex. quinolizines, naphtyridines, berbérine, vincamine
The present application relates to the field of drug synthesis, in particular to a crystal form of ARV-110 and a preparation method therefor and a use thereof. The crystal form of the ARV-110 at least has one of the following improved characteristics: the stability is good, the hygroscopicity is low, the solubility is good, the melting point is high, stable storage can be achieved, crystal transformation of a drug in a development process and storage is avoided, the preparation method is simple and reliable, and great development values are achieved.
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
A61K 31/501 - PyridazinesPyridazines hydrogénées non condensées et contenant d'autres hétérocycles
Disclosed are a crystal form of Evobrutinib, a crystal form of a succinate thereof, and a preparation method therefor and the use thereof. The crystal form of Evobrutinib has good stability, low hygroscopicity, good solubility, good dissolution and good crystal morphology, is basically pure, and can be stably stored, thereby preventing crystal transformation of a drug in a development process and storage. The preparation method is simple and reliable, and the crystal form has great development value. The crystal form of a succinate of Evobrutinib also has good stability, low hygroscopicity, good solubility, good dissolution and good crystal morphology, is basically pure, and can be stably stored, thereby preventing crystal transformation of the drug in the development process and storage. The preparation method is simple and reliable, and the crystal form has great development value.
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
A61K 31/506 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime non condensées et contenant d'autres hétérocycles
The present application relates to the field of medicinal chemistry. The present application relates to a hydrate crystal form of lazertinib monomethanesulfonate, a preparation method therefor and an application thereof. The hydrate crystal form of lazertinib monomethanesulfonate provided by the present application has at least one of the following advantages: good stability, good solubility, good dissolution, low hygroscopicity, uniform particle size distribution, good morphology, good fluidity, good crystallinity, and being capable of stable storage, which prevent the degradation, impurity increase, and appearance change of a drug during development and storage, and prevent crystal transformation during storage. The preparation method is simple and reliable, and has great development value.
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
A61K 31/5377 - 1,4-Oxazines, p. ex. morpholine non condensées et contenant d'autres hétérocycles, p. ex. timolol
The present invention relates to the field of pharmaceutical chemistry, and specifically to a tolebrutinib salt and a crystal form thereof, a preparation method therefor, a pharmaceutical composition thereof, and a use thereof. Tolebrutinib hydrochloride and the crystal form thereof have at least one of the following advantages: good stability, low hygroscopicity, solubility satisfying medicinal requirements, uniform particle size distribution, good morphology, good fluidity, good compressibility, good crystallinity, stability during storage, avoidance of crystal transformation during drug development and storage, a simple and reliable preparation method, and great development values. Tolebrutinib maleate and the crystal form thereof have at least one of the following advantages: good stability, uniform distribution, good fluidity, solubility satisfying medicinal requirements, stability during storage, avoidance of crystal transformation during drug development and storage, and a simple and reliable preparation method.
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
A61P 37/00 - Médicaments pour le traitement des troubles immunologiques ou allergiques
A61P 29/00 - Agents analgésiques, antipyrétiques ou anti-inflammatoires non centraux, p. ex. agents antirhumatismauxMédicaments anti-inflammatoires non stéroïdiens [AINS]
Provided are a crystal form, an amorphous form of tolebrutinib, a preparation method therefor and use thereof. The crystal form of tolebrutinib has at least one of the following advantages: good stability, low hygroscopicity, uniform particle size distribution, solubility that meets medicinal requirements, stable storage, avoids the occurrence of crystal transformation during development and storage, a reliable preparation method, and has a great development value. The amorphous form of tolebrutinib has better solubility than the crystal form of tolebrutinib, while still having good storage stability and acceptable hygroscopicity; in addition, same has a high medicinal value.
A61K 31/4545 - Pipéridines non condensées, p. ex. pipérocaïne contenant d'autres systèmes hétérocycliques contenant un cycle à six chaînons avec l'azote comme hétéro-atome du cycle, p. ex. pipampérone, anabasine
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
Disclosed are a Resmetirom crystal form, a preparation method therefor, and a use thereof, as well as a pharmaceutical composition containing the crystal form.
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
A61K 31/501 - PyridazinesPyridazines hydrogénées non condensées et contenant d'autres hétérocycles
A61P 1/16 - Médicaments pour le traitement des troubles du tractus alimentaire ou de l'appareil digestif des troubles de la vésicule biliaire ou du foie, p. ex. protecteurs hépatiques, cholagogues, cholélitholytiques
17.
CRYSTAL FORM OF BREPOCITINIB TOSYLATE, AND PREPARATION METHOD AND USE THEREFOR
A61K 31/506 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime non condensées et contenant d'autres hétérocycles
A61P 37/00 - Médicaments pour le traitement des troubles immunologiques ou allergiques
A61P 29/00 - Agents analgésiques, antipyrétiques ou anti-inflammatoires non centraux, p. ex. agents antirhumatismauxMédicaments anti-inflammatoires non stéroïdiens [AINS]
A61P 17/14 - Médicaments pour le traitement des troubles dermatologiques pour le traitement de la calvitie ou de l'alopécie
A61P 17/00 - Médicaments pour le traitement des troubles dermatologiques
18.
CRYSTAL FORM OF TAS-116, AND PREPARATION METHOD THEREFOR, PHARMACEUTICAL COMPOSITION, AND USE THEREFOR
A61K 31/4439 - Pyridines non condenséesLeurs dérivés hydrogénés contenant d'autres systèmes hétérocycliques contenant un cycle à cinq chaînons avec l'azote comme hétéro-atome du cycle, p. ex. oméprazole
Disclosed are a crystal form I of a compound as shown in formula (I) and a crystal form II of a compound as shown in formula (II), wherein the compound as shown in formula (I) and the compound as shown in formula (II) are as described in the present disclosure.
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
A61K 31/501 - PyridazinesPyridazines hydrogénées non condensées et contenant d'autres hétérocycles
A61P 29/00 - Agents analgésiques, antipyrétiques ou anti-inflammatoires non centraux, p. ex. agents antirhumatismauxMédicaments anti-inflammatoires non stéroïdiens [AINS]
20.
Crystal form of tipifarnib and method of treatment thereof
The present invention relates to novel crystal forms of tipifarnib. Compared with the prior art, the crystal forms of tipifarnib have advantages in crystallinity, hygroscopicity, morphology, form stability and chemical stability. The present invention also relates to the preparation methods of crystal forms of tipifarnib, pharmaceutical composition thereof and their use in preparation for treating and/or preventing abnormal cell growth diseases.
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
21.
Crystal form of ACP-196 and method of treatment thereof
Crystalline forms of ACP-196, preparation methods, pharmaceutical compositions and uses thereof in the preparation of drugs for treatment and/or prevention of Bruton's tyrosine kinase (BTK)-mediated disorders such as autoimmune diseases or disorders, heteroimmune diseases or disorders, cancers including lymphoma and inflammatory diseases or disorders. As compared with the known solid form of ACP-196, the crystalline forms of the present invention have advantages in crystallinity.
Provided are a fruquintinib and a saccharin salt or eutectic crystal, a fruquintinib and a malonic acid eutectic crystal or a fruquintinib and a maleic eutectic crystal, a preparation method therefor, a pharmaceutical composition containing thereof, and uses thereof in preparing drugs for treating and/or preventing diseases related to abnormal angiogenesis, such as cancer, tumors, macular degeneration, chronic inflammation and the like.
C07D 407/12 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes d'oxygène 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 275/03 - Composés hétérocycliques contenant des cycles thiazole-1, 2 ou thiazole-1, 2 hydrogéné non condensés avec d'autres cycles 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
23.
Crystal form of 2-(6-methyl-pyridin-2-yl)-3-yl-[6-amido-quinolin-4-yl]-5,6-dihydro-4H-pyrrolo[1,2-B]pyrazole, preparation method therefor and pharmaceutical composition thereof
The present invention relates to a crystal form of 2-(6-methyl-pyridin-2-yl)-3-(6-amido-quinolin-4-yl)-5,6-dihydro-4h-pyrrolo[1,2-b]pyrazole (Galunisertib or LY2157299), represented by formula (I). Compared with the known solid form of Galunisertib, the crystal form of the present invention has advantages in terms of solubility, hygroscopicity, crystal stability, morphology and the like. The present invention also relates to a process of preparing the crystal forms of Galunisertib, a pharmaceutical composition thereof and a use thereof in the preparation of a medicament for the prevention and/or treatment of diseases associated with TGF-beta.
The present invention relates to a compound formed by entinostat as shown in formula (I) and acidic counterion. Compared with the known solid form of entinostat, the compound involved has advantages in terms of solubility, stability, etc. The present invention also relates to a crystalline form of the compound and a preparation method therefor, a pharmaceutical composition thereof and the use thereof in the preparation of a drug for preventing and/or treating a disease associated with differentiation or proliferation.
05 - Produits pharmaceutiques, vétérinaires et hygièniques
35 - Publicité; Affaires commerciales
42 - Services scientifiques, technologiques et industriels, recherche et conception
Produits et services
(1) Antibiotics; collyrium; food supplements consisting of trace elements; anti-infectives; pharmaceutical preparations for regulating the immune system; pharmaceutical preparations for the treatment of autoimmune diseases; pharmaceutical preparations for the treatment of the respiratory system; pharmaceutical preparations for the treatment of allergies; pharmaceutical preparations for the treatment of chronic pain; preparations for the relief of pain; pharmaceutical preparations for the treatment of gastro-intestinal diseases; pharmaceutical preparations for the treatment of genitourinary diseases, namely, urological diseases, infertility, sexually transmitted diseases, inflammatory pelvic diseases; pharmaceutical preparations for the treatment of vascular diseases; pharmaceutical preparations for use in oncology; pharmaceutical preparations for the treatment of blood disorders; pharmaceutical preparations for the treatment of metabolic disorders, namely diabetes, bulimia nervosa, anorexia, obesity and hypothyroidism; pharmaceutical preparations for the treatment of bacterial skin infections, fungal skin infections, viral skin infections and parasitic skin infections; pharmaceutical preparations for the treatment of acne; homeopathic remedies for treatment of skin conditions, namely, dermatitis, eczema, psoriasis; pharmaceutical preparations for the treatment of diseases, disorders and infections of the endocrine system, namely growth and thyroid disorders; pharmaceutical preparations for the treatment of diabetes; vaccines for human use; adjuvants for use with vaccines; tumor suppressing agents; pharmaceutical products for the treatment of cancer; pharmaceutical preparations for treating gastrointestinal disorders; preparations for treating haemorrhoids; topical anesthetics; chemotherapeutics; pharmaceutical preparations for the treatment of brain diseases and disorders, namely, epilepsy, alzheimer's, cerebral palsy, parkinson's disease, multiple sclerosis (1) Business management consultancy; conducting business and market research surveys for others; consultancy and advisory services in the field of business strategy; import-export agency services; publication of publicity texts; advice and information concerning commercial business management; market analysis; advice and information about customer services and product management and prices on Internet sites in connection with purchases made over the Internet; online department store services; wholesale services for pharmaceutical, veterinary and sanitary preparations and medical supplies; advertising agencies; business organisation and management consulting services; product demonstration services in shop windows by live models; arranging and conducting craft trade show exhibitions; market analysis and research services
(2) Research and development of new products for others; chemical analysis; chemical research; biochemical research; cosmetic research; medical research; clinical trials; providing medical and scientific research information in the field of pharmaceuticals and clinical trials; food safety auditing; chemist services; laboratory research in the field of chemistry; pharmaceutical evaluation services; pharmaceutical research and development; pharmaceutical research services; research and development of vaccines and medicines
26.
Co-crystals of ribociclib and co-crystals of ribociclib monosuccinate, preparation method therefor, compositions thereof, and uses thereof
The present invention relates to co-crystals of ribociclib and co-crystals of ribociclib monosuccinate, comprising the co-crystal of ribociclib and saccharin, the co-crystal of ribociclib and cholic acid, the co-crystal of ribociclib and orotic acid, and the co-crystal of ribociclib monosuccinate and citric acid. Compared with the prior art, the co-crystals have one or more improved properties. The present invention also relates to methods of preparing the co-crystal of ribociclib and saccharin, the co-crystal of ribociclib and cholic acid, the co-crystal of ribociclib and orotic acid, and the co-crystal of ribociclib monosuccinate and citric acid, pharmaceutical compositions, and uses thereof in the preparation of medicines for treating and/or preventing diseases involving one or more symptoms of protein kinase related dysfunctions, cancers, transplant rejection and autoimmune diseases.
The present invention relates to a crystalline form of N-((s)-1-(3-(3-chloro-4-cyanophenyl)-1H-pyrazol-1-yl)prop-2-yl)-5-(1-hydroxylethyl)-1H-pyrazole-3-carboxamide (namely, ODM-201). The ODM-201 crystalline form of the present invention has one or more improved properties compared to known ODM-201. The present invention further relates to a method for preparing the ODM-201 crystalline form, a pharmaceutical composition thereof, and a use thereof in the preparation of a medicament for the treatment of nuclear receptor, specifically steroid receptor, and more specifically androgen receptor (AR)-dependent diseases and conditions.
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
A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
28.
Cocrystal of 2-(6-methyl-pyridine-2-yl)-3-yl-[6-amide-quinoline-4-yl]-5,6-dihydro-4H-pyrrole[1,2-b]pyrazole, preparation method therefor, and pharmaceutical composition
The present invention relates to a cocrystal of 2-(6-methyl-pyridine-2-yl)-3-yl-[6-amide-quinoline-4-yl]-5,6-dihydro-4H-pyrrole[1,2-b]pyrazole (Galunisertib or LY2157299) represented by formula (I) and a cocrystal former. Compared with the known solid form of Galunisertib, the cocrystal of the present invention has advantages in terms of stability, solubility, etc. The present invention also relates to a crystal form of the cocrystal, a preparation method therefor, a pharmaceutical composition thereof, and an application thereof in preparation of drugs for preventing and/or treating diseases relevant to TGF-β.
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
29.
Crystal form of ACP-196, preparation method therefor and pharmaceutical composition thereof
Crystalline forms of ACP-196, preparation methods, pharmaceutical compositions and uses thereof in the preparation of drugs for treatment and/or prevention of Bruton's tyrosine kinase (BTK)-mediated disorders such as autoimmune diseases or disorders, heteroimmune diseases or disorders, cancers including lymphoma and inflammatory diseases or disorders. As compared with the known solid form of ACP-196, the crystalline forms of the present invention have advantages in crystallinity.
The present invention relates to novel crystalline forms of ACP-196 (acalabrutinib) salts, compared with the known solid form of ACP-196, the crystalline forms of ACP-196 salts of the present invention have advantages in crystallinity, solubility and hygroscopicity. The present invention also relates to the preparation methods for the preparation of the crystalline forms of ACP-196 salts, pharmaceutical compositions thereof and their uses in the preparation of methods for treating and/or preventing diseases mediated by Bruton tyrosine kinase (BTK), such as autoimmune diseases or disorders, xenoimmune diseases or disorders, cancer, including lymphoma and inflammatory diseases or disorders.
The present invention relates to novel crystal forms of tipifarnib. Compared with the prior art, the crystal forms of tipifarnib have advantages in crystallinity, hygroscopicity, morphology, form stability and chemical stability. The present invention also relates to the preparation methods of crystal forms of tipifarnib, pharmaceutical composition thereof and their use in preparation for treating and/or preventing abnormal cell growth diseases.
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
32.
CRYSTAL FORM OF ABEMACICLIB MESYLATE, PREPARATION METHOD THEREFOR AND PHARMACEUTICAL COMPOSITION THEREOF
Disclosed is a crystal form of abemaciclib mesylate, which has one or more improved properties compared with the known abemaciclib mesylate. Also involved are a method for preparing the crystal form of abemaciclib mesylate, a pharmaceutical composition and the use of same in the preparation of a drug for treating cancer diseases such as colorectal cancer, breast cancer, lung cancer, prostate cancer, glioblastoma, mantle cell lymphoma, chronic granulocytic leukemia and acute granulocytic leukemia.
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
A61K 31/506 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime non condensées et contenant d'autres hétérocycles
The present invention relates to canagliflozin Monohydrate and its crystalline forms, which as compared to the prior art, have higher stability in water or aqueous system, are more suitable for wet granulation processes or suspension preparations and have good storage stability; the present invention also relates to preparation methods of canagliflozin Monohydrate and its crystalline forms, pharmaceutical compositions thereof and uses thereof in preparation of drugs for treating diseases such as diabetes, diabetes complications, obesity and so on.
C07D 409/10 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes de soufre comme uniques hétéro-atomes du cycle contenant deux hétérocycles liés par une chaîne carbonée contenant des cycles aromatiques
A61K 31/7042 - Composés ayant des radicaux saccharide et des hétérocycles
A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
Provided are a fruquintinib and a saccharin salt or eutectic crystal, a fruqintinib and a malonic acid eutectic crystal or a fruquintinib and a maleic euctectic crystal, a preparation method therefor, a pharmaceutical composition containing thereof, and uses thereof in preparing drugs for treating and/or preventing diseases abnormally related to angiogenesis, such as cancer, tumors, macular degeneration, chronic inflammation and the like.
C07D 405/12 - Composés hétérocycliques contenant à la fois un ou plusieurs hétérocycles comportant des atomes d'oxygène comme uniques hétéro-atomes du cycle et un ou plusieurs hétérocycles comportant des atomes d'azote comme uniques hétéro-atomes du cycle contenant deux hétérocycles liés par une chaîne contenant des hétéro-atomes comme chaînons
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
A61P 29/00 - Agents analgésiques, antipyrétiques ou anti-inflammatoires non centraux, p. ex. agents antirhumatismauxMédicaments anti-inflammatoires non stéroïdiens [AINS]
A61P 43/00 - Médicaments pour des utilisations spécifiques, non prévus dans les groupes
35.
Fenofibrate crystalline form and manufacturing method thereof
The present invention relates to Form IV of fenofibrate and its preparation methods thereof. Its X-ray powder diffraction pattern expressed as 2θ angle has characteristic peaks at 14.15±0.2°, 15.94±0.2°, 16.49±0.2°, 17.45±0.2°, 20.21±0.2°, and 22.87±0.2°. The present invention also provides preparation methods of Form IV. The preparation methods are simple, easy to operate, short, and have good repeatability. The methods are also non-toxic and non-polluting by using water as a medium and using a pharmaceutically accepted excipient, such as polyvinylpyrrolidone or polyvinyl alcohol as an inducer. The results of stability experiments (light exposure, high humidity and grinding) and solubility tests show that Form IV is stable and has a higher solubility than the prior art crystal form.
C07C 67/52 - SéparationPurificationStabilisationEmploi d'additifs par modification de l'état physique, p. ex. par cristallisation
C07C 69/712 - Éthers le groupe hydroxyle de l'ester étant éthérifié par un composé hydroxylé dont le groupe hydroxyle est lié à un atome de carbone d'un cycle aromatique à six chaînons
36.
ABT-199 addition salt and crystal form thereof, preparation method thereof, and pharmaceutical composition thereof
Crystalline forms, preparation methods and pharmaceutical compositions of ABT-199 monohydrochloride and ABT-199 dihydrochloride are disclosed. Compared with known ABT-199, they have one or more improved properties. They can be used to prepare drugs for the treatment and/or prevention of one or more diseases associated with overexpression of an anti-apoptotic BCL-2 family protein.
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
The present invention relates to novel crystal forms of ozanimod. Compared with the prior art, the crystal forms of the present invention have one or more improved properties. The present invention also relates to preparation methods of the crystal forms, pharmaceutical compositions thereof and uses thereof for the manufacture of medicament for treating and/or preventing diseases or adverse conditions associated with modulation, activation, stimulation, inhibition or antagonization of selective sphingosine-1-phosphate (S1P) receptor.
A61K 47/10 - AlcoolsPhénolsLeurs sels, p. ex. glycérolPolyéthylène glycols [PEG]PoloxamèresAlkyléthers de PEG/POE
A61K 47/16 - Composés organiques, p. ex. hydrocarbures naturels ou synthétiques, polyoléfines, huile minérale, gelée de pétrole ou ozocérite contenant de l'azote
A61K 47/08 - Composés organiques, p. ex. hydrocarbures naturels ou synthétiques, polyoléfines, huile minérale, gelée de pétrole ou ozocérite contenant de l'oxygène
A61K 9/19 - Préparations médicinales caractérisées par un aspect particulier à l'état particulaire, p. ex. poudres lyophilisées
A61P 37/06 - Immunosuppresseurs, p. ex. médicaments pour le traitement du rejet de greffe
A61P 11/00 - Médicaments pour le traitement des troubles du système respiratoire
A61P 1/00 - Médicaments pour le traitement des troubles du tractus alimentaire ou de l'appareil digestif
A61P 19/02 - Médicaments pour le traitement des troubles du squelette des troubles articulaires, p. ex. arthrites, arthroses
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
The present invention relates to canagliflozin Monohydrate and its crystalline forms, which as compared to the prior art, have higher stability in water or aqueous system, are more suitable for wet granulation processes or suspension preparations and have good storage stability; the present invention also relates to preparation methods of canagliflozin Monohydrate and its crystalline forms, pharmaceutical compositions thereof and uses thereof in preparation of drugs for treating diseases such as diabetes, diabetes complications, obesity and so on.
C07D 409/10 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes de soufre comme uniques hétéro-atomes du cycle contenant deux hétérocycles liés par une chaîne carbonée contenant des cycles aromatiques
A61K 31/7042 - Composés ayant des radicaux saccharide et des hétérocycles
A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
The present invention involves novel crystal forms of Dabrafenib mesylate and preparation method thereof, wherein the novel crystal forms are more stable in water or an aqueous system, and have greater solubility and dissolution rate in water, thus having better stability and bioavailability compared with the existing crystal forms.
C07D 239/02 - Composés hétérocycliques contenant des cycles diazine-1, 3 ou diazine-1, 3 hydrogéné non condensés avec d'autres cycles
C07D 277/04 - Composés hétérocycliques contenant des cycles thiazole-1, 3 ou thiazole-1, 3 hydrogénés non condensés avec d'autres cycles ne comportant pas de liaison double entre chaînons cycliques ou entre chaînons cycliques et chaînons non cycliques
A61K 31/505 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime
C07D 417/04 - 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 liaison directe de chaînon cyclique à chaînon cyclique
40.
Crystal form of dabrafenib and preparation method and use thereof
The invention relates to Crystal Form VII of dabrafenib and preparation method thereof, wherein Crystal Form VII has the advantage of being more stable at room temperature or in aqueous systems, and has low hygroscopicity, and thus is more suitable for a wet granulation process or being prepared into a suspension; and the present invention also relates to a pharmaceutical composition and formulations comprising Crystal Form VII, and their use in the treatment of Raf family kinase-related diseases.
C07D 417/04 - 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 liaison directe de chaînon cyclique à chaînon cyclique
C30B 7/06 - Croissance des monocristaux à partir de solutions en utilisant des solvants liquides à la température ordinaire, p. ex. à partir de solutions aqueuses par évaporation du solvant en utilisant des solvants non aqueux
C30B 7/14 - Croissance des monocristaux à partir de solutions en utilisant des solvants liquides à la température ordinaire, p. ex. à partir de solutions aqueuses le matériau à cristalliser étant produit dans la solution par des réactions chimiques
The present invention relates to new crystalline forms of the inhibitor, 5-fluoro-3-phenyl-2-[(S)-1-(9H-purin-6-ylamino)-propyl]-3H-quinazoline-4-one; the present invention also relates to methods for preparing the new crystalline forms of 5-fluoro-3-phenyl-2-[(S)-1-(9H-purin-6-ylamino)-propyl]-3H-quinazolin-4-one, pharmaceutical compositions containing the new crystalline forms thereof, and uses thereof for the treatment and/or prevention of diseases such as chronic lymphocytic leukemia and indolent non-Hodgkin's lymphoma.
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
The present invention involves novel crystal forms of Dabrafenib mesylate and preparation method thereof, wherein the novel crystal forms are more stable in water or an aqueous system, and have greater solubility and dissolution rate in water, thus having better stability and bioavailability compared with the existing crystal forms.
C07D 239/02 - Composés hétérocycliques contenant des cycles diazine-1, 3 ou diazine-1, 3 hydrogéné non condensés avec d'autres cycles
C07D 277/04 - Composés hétérocycliques contenant des cycles thiazole-1, 3 ou thiazole-1, 3 hydrogénés non condensés avec d'autres cycles ne comportant pas de liaison double entre chaînons cycliques ou entre chaînons cycliques et chaînons non cycliques
A61K 31/505 - PyrimidinesPyrimidines hydrogénées, p. ex. triméthoprime
C07D 417/04 - 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 liaison directe de chaînon cyclique à chaînon cyclique
