The present invention relates to a crystal of a nitrogen-bridged heterocyclic compound and a preparation method therefor. Specifically, the present invention relates to a crystal form of a fumarate of a compound represented by formula (I). The crystal provided by the present invention has excellent flowability, and is better for use in production and clinical treatment.
C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 401/02 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
A61P 37/00 - Drugs for immunological or allergic disorders
A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
A61K 31/439 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
A61P 11/00 - Drugs for disorders of the respiratory system
A61P 13/00 - Drugs for disorders of the urinary system
The present disclosure relates to a pyrrolo benzodiazepine derivative and a conjugate, preparation method and use thereof. In particular, the present disclosure relates to a compound of formula (DL) and a antibody-drug conjugate thereof, a pharmaceutical composition containing same, and a use thereof in the preparation of a medicament for the treatment of cancer. The definitions of groups in the general formula (DL) are as defined in the description.
C12N 5/10 - Cells modified by introduction of foreign genetic material, e.g. virus-transformed cells
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
The present invention relates to a MOR receptor agonist pharmaceutical composition. In particular, the MOR receptor agonist pharmaceutical composition comprises (1S,4S)-4-methoxy-N-(2-((R)-9-(pyridin-2-yl)-6-oxaspiro[4.5]decane-9-yl)ethyl)-1,2,3,4-tetrahydronaphthalen-1-amine or a pharmaceutically acceptable salt thereof, and a phosphate buffer solution. The pharmaceutical composition of the present invention exhibits good stability after months of storage.
A61K 31/4433 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
4.
PHARMACEUTICAL COMPOSITION OF KOR RECEPTOR AGONIST
Disclosed in the present invention is a pharmaceutical composition of a KOR receptor agonist, which comprises 4-amino-N-[N2-[N-[N-[N-((R)-2-phenyl propyl)glycyl]-D-phenylalanyl]-D-leucyl]-D-lysyl]piperidine-4-carboxylic acid or available salts thereof, and an acetate buffer solution.
Provided are a crystalline form of a GnRH receptor antagonist and a preparation method therefor. Specifically, provided are a crystalline form I of 1-(4-(7-(2,6-difluorobenzyl)-3-((dimethylamino)methyl)-5-(6-methoxypyridazin-3-yl)-4,6-dicarbonyl-4,5,6,7-tetrahydro-2H-pyrazolo[3,4-d]pyrimidin-2-yl)phenyl)-3-methoxy urea (a compound of formula I) and a preparation method, the use of same in a pharmaceutical composition and the use of the crystalline form I and the composition in the preparation of a drug for treating diseases associated with a GnRH receptor antagonist.
Provided are a crystalline form of a GnRH receptor antagonist and a preparation method therefor. Specifically, provided are a crystalline form I of 1-(4-(7-(2,6-difluorobenzyl)-3-((dimethylamino)methyl)-5-(6-methoxypyridazin-3-yl)-4,6-dicarbonyl-4,5,6,7-tetrahydro-2H-pyrazolo[3,4-d]pyrimidin-2-yl)phenyl)-3-methoxyurea (a compound of formula I) and a preparation method, the use of same in a pharmaceutical composition and the use of the crystalline form I and the composition in the preparation of a drug for treating diseases associated with a GnRH receptor antagonist.
The present invention relates to a crystalline form of a free base of an imidazo isoindole derivative and a preparation method therefor. Specifically, the present invention relates to the A, B, C, D, E, and F crystal forms of the compound represented by formula (I), the chemical name being (S)-2-(4-(4-(4-(6-fluoro-5H-imidazo[5,1-a]isoindol-5-yl)piperidine-1-yl)phenyl)-1H-pyrazol-1-yl)ethanol. The present invention also relates to a preparation method for the A, B, C, D, E, and F crystal forms, the use thereof in a pharmaceutical composition, and the application of the A, B, C, D, E, and F crystal forms and the pharmaceutical composition in the treatment of diseases having an IDO-mediated tryptophan metabolic pathway pathological feature; the A, B, C, D, E, and F crystal forms of formula (I) obtained in the present invention have good stability, and the crystallisation solvent used has low toxicity and low residue, and can be better used for clinical treatment.
A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
A61P 35/02 - Antineoplastic agents specific for leukemia
A61P 35/04 - Antineoplastic agents specific for metastasis
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
The present invention relates to an opioid receptor antagonist derivative, a preparation method thereof and a use thereof in medicine. In particular, the present invention relates to a naloxone derivative as shown by general formula (I) and a pharmaceutically acceptable salt thereof, a preparation method thereof, and a use of thereof as a therapeutic agent for treating diseases such as constipation caused by long-term use of opioid receptor agonists such as morphine. The drug acts on peripheral nerves, wherein the definitions of the substituents in general formula (I) are the same as those defined in the description.
C07D 489/00 - Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula:
A61K 31/439 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
A61P 25/02 - Drugs for disorders of the nervous system for peripheral neuropathies
A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
METHOD FOR PREPARING (2R,3S,4R,5R)-2-(HYDROXYMETHYL)-5-(6-((2-(METHYLTHIO)ETHYL)AMINO)-2-((3,3,3-TRIFLUOROPROPYL)THIO)-9H-PURIN-9-YL)TETRAHYDROFURAN-3,4-DIOL
The present invention relates to a method for preparing (2R,3S,4R,5R)-2-(hydroxymethyl)-5-(6-((2-(methylthio)ethyl)amino)-2-((3,3,3-trifluoropropyl)thio)-9H-purin-9-yl)tetrahydrofuran-3,4-diol. Specifically, the present invention relates to a method for preparing (2R,3S,4R,5R)-2-(hydroxymethyl)-5-(6-((2-(methylthio)ethyl)amino)-2-((3,3,3-trifluoropropyl)thio)-9H-purin-9-yl)tetrahydrofuran-3,4-diol (I). The method comprises the step of enabling 2-halogenated adenosine (XI) to react with 3,3,3-trifluoropropyl sulfide (VI). The preparation method is low in cost, simple in operation, easy in separation and purification and high in yield, thus being suitable for large-scale production.
C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
Provided is a method for preparing an intermediate of formula II for odanacatib, comprising a step of reducing the compound of formula II to a compound of formula IA, wherein the reduction is performed by adding a metal chloride and a metal borohydride to a solvent in which the compound of formula II is dissolved. The preparation method is cost-effective, simple to operate, and easy for separation and purification of the product.
C07C 303/30 - Preparation of esters or amides of sulfuric acidsPreparation of sulfonic acids or of their esters, halides, anhydrides or amides of esters of sulfonic acids by reactions not involving the formation of esterified sulfo groups
C07C 309/76 - Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing nitrogen atoms, not being part of nitro or nitroso groups, bound to the carbon skeleton
C07C 253/30 - Preparation of carboxylic acid nitriles by reactions not involving the formation of cyano groups
C07C 255/46 - Carboxylic acid nitriles having cyano groups bound to carbon atoms of rings other than six-membered aromatic rings to carbon atoms of non-condensed rings
12.
TICAGRELOR SOLID DISPERSION AND PREPARATION METHOD THEREOF
A ticagrelor solid dispersion and preparation method thereof; the solid dispersion is prepared via dispersing the ticagrelor into a carrier material, the carrier material comprising one or more of polyvinylpyrrolidone, copovidone and crospovidone.
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
A61P 9/14 - VasoprotectivesAntihaemorrhoidalsDrugs for varicose therapyCapillary stabilisers
13.
MIDBODY OF TICAGRELOR AND PREPARATION METHOD THEREFOR, AND PREPARATION METHOD FOR TICAGRELOR
Disclosed are a midbody of ticagrelor and a preparation method therefor, and a preparation method for ticagrelor. Specifically, disclosed is a midbody, namely, compound of formula (VI), for preparing ticagrelor. Further disclosed are a method for preparing the midbody and a method for preparing ticagrelor by using the midbody. Ticagrelor is prepared by using the midbody, so that the synthesis process is simple, and a defect that longtime reaction under high temperature is required in the existing method is avoided. This preparation method is suitable for mass production in the industry, energy consumption is reduced, pollution to the environment is reduced, and discharge of the three wastes is reduced.
C07D 317/44 - Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems
C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
patents
