Disclosed are a salt of diazacycloheptane compound and a crystal form and an amorphous substance thereof, which have improved features in the aspects of solubility, stability, dissolution of solid preparations and the like. Also disclosed are methods for preparing the salt and the crystal form and amorphous substance thereof, a pharmaceutical composition thereof and uses of preparing medicaments for treating and preventing neurological and psychiatric disorders and diseases relevant to hypocretin receptors.
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
A61K 31/551 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
A61P 25/00 - Drugs for disorders of the nervous system
A61P 5/00 - Drugs for disorders of the endocrine system
A61P 9/00 - Drugs for disorders of the cardiovascular system
A61P 13/00 - Drugs for disorders of the urinary system
2.
CRYSTALLINE FORM OF ANTI-HEPATITIS C VIRUS DRUG, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF
A new crystalline form of an anti-hepatitis C virus (HCV) drug TMC435, a preparation method therefor, a pharmaceutical composition thereof, and a use thereof in preparing drugs for treating and/or preventing HCV infection.
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
The present invention relates to a new type of eutectic crystal of lorcaserin hydrochloride and benzoic acid. Compared with the prior art, the eutectic crystal has the improved properties of good stability, low solubility, and being suitable for the application of controlled-release preparation. The present invention also relates to a method for preparing the eutectic crystal, a pharmaceutical composition thereof and the use thereof in the preparation of drugs for treating and/or preventing diseases associated with 5HT2c.
A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
The present invention relates to a novel crystal form of oxazolidinone antibiotics. The new crystal form has advantages in the aspects of solubility, hygroscopicity, crystallinity and stability. The present invention also relates to a method for preparing the new crystal form, a pharmaceutical composition thereof and the use thereof in the preparation of drugs for treating and/or preventing diseases caused by microbial infection.
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
C07F 9/06 - Phosphorus compounds without P—C bonds
A DPP-IV inhibitor trelagliptin semi-succinate and crystals thereof, preparation method for trelagliptin semi-succinate and crystals thereof, pharmaceutical composition thereof and use thereof in preparation of drugs treating diseases such as diabetes and the like.
C07D 239/54 - Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
C07D 401/12 - 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 chain containing hetero atoms as chain links
C07D 401/04 - 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 directly linked by a ring-member-to-ring- member bond
A61K 31/56 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids
A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
The present invention relates to Canagliflozin monohydrate and crystal form thereof. Compared with the prior art, the Canagliflozin monohydrate and crystal form has higher stability in water or an aqueous system, is more suitable for a wet granulation process or suspension preparation, and has good storage stability. The present invention also relates to a preparation method of the Canagliflozin monohydrate and crystal form thereof, pharmaceutical composition thereof and uses thereof in the preparation of drugs for treating diseases such as diabetes, diabetes complications, obesity and the like.
C07D 409/10 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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 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
A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
A61P 17/02 - Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
A61P 5/50 - Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
The present invention relates to a new crystalline form of a Dolutegravir sodium salt. Compared with a known crystalline form of the Dolutegravir sodium salt, the new crystalline form according to the present invention has one or more beneficial properties, such as desirable stability in water, high solubility, low hygroscopicity, desirable storage stability, and excellent particle appearance. The present invention further relates to a preparation method of the Dolutegravir sodium salt in the new crystalline form, a pharmaceutical composition thereof, and uses thereof in preparing a medicine for treating and/or preventing HIV-1 infection.
The present invention relates to a crystalline form of a hepatitis C drug (2R,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropyl sulphonyl)-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydro-2-[[7-methoxyl-8-methyl-2-[4-(1-methylethyl)-2-thiazolyl]-4-quinolinyl] oxyl]-5-methyl-4,14-dioxocyclopentano[c]cyclopropo[g][1,6] diazacyclotetradecene-12a(1H)-methanamine(TMC435) sodium salt, the crystalline form having good crystallinity and stability compared with known crystalline forms. The present invention further relates to a preparation method, pharmaceutical composition and use of the crystalline form, the use in preparing drugs for treating and/or preventing hepatitis C viral infection or liver disease related to hepatitis C viral infection.
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
A61K 31/4725 - Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
SALT OF COMPOUND AND CRYSTALLINE OR AMORPHOUS SUBSTANCE THEREOF, PREPARATION METHOD THEREFOR, PHARMACEUTICAL COMPOSITION CONTAINING SAME AND USE THEREOF
Provided are a salt of a compound ((1S)-1-(((2S)-2-(5-(4'-(2-((2S)-1-((2S)-2-((methoxycarbonyl)amino)-3-methylbutyryl)-2-pyrrolidyl)-1H-imidazol-5-yl)-4-biphenyl)-1H-imidazol-2-yl)-1-pyrrolidyl)carbonyl)-2-methylpropyl)methyl carbamate, and a crystalline or amorphous substance thereof. Also provided are a preparation method for the salt and the crystalline and amorphous substances thereof, a pharmaceutical composition and the pharmaceutical use thereof.
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
A61K 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
The present invention relates to a crystal form 1 of anacetrapib. Compared with the prior art, the crystal form 1 of anacetrapib of the present invention has a better crystal form stability, is easily stored, and is suitable for use as a solid preparation. The present invention also relates to a method for preparing the crystal form 1, a pharmaceutical composition thereof and the use thereof in the preparation of drugs for treating and/or preventing diseases such as atherosclerosis, hyperlipidemia, and the like.
A61K 31/4174 - Arylalkylimidazoles, e.g. oxymetazolin, naphazoline, miconazole
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
Disclosed in the present application are the following crystals of Lorcaserin: sulfamate, stearate, cholate, 4-aminobenzene sulfonate, or terephthalate, and the preparation methods and pharmaceutical compositions thereof, and the uses thereof in the preparation of drugs for treating and/or preventing diseases associated with 5HT2c, such as obesity. The release rate index in water of sustained release tablets of the crystals has improved properties.
A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
The present invention relates to crystalline forms of trametinib and solvate thereof, preparation method therefor, pharmaceutical compositions comprising the crystalline form and use thereof in preparing related medicines. In comparison with the prior art, the crystalline forms of the trametinib and solvate thereof of the present invention has good crystalline state, good crystalline stability, low moisture absorption, improved solubility in water, higher amount of active components, lower solvent toxicity, and is more beneficial to meet the strict requirements for pharmaceutical preparation. The crystalline forms can be prepared at room temperature or low temperature, and is beneficial to industrial production of the products.
A61K 31/4353 - 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 ortho- or peri-condensed with heterocyclic ring systems
The present application relates to rigosertib salt and a crystal form thereof. Compared with existing rigosertib salt, the rigosertib salt and the crystal form thereof in the present application has advantages on crystallinity, crystal habit, hygroscopicity, and stability. In addition, the present application further relates to a preparation method for the rigosertib salt and the crystal form thereof, pharmaceutical compositions, and their applications in preparing drugs for treating solid tumor disease.
C07C 317/28 - SulfonesSulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to acyclic carbon atoms of the carbon skeleton
14.
SOLID FORM OF ENZALUTAMIDE, PREPARATION METHOD AND USE THEREOF
The present invention relates to a novel solid form of Enzalutamide. In comparison with the prior art, the new solid form of Enzalutamide in the present invention has one or more improved properties, such as good solubility and dissolution rate, good stability, favorable processing properties, and suitability for solid preparation application. The present invention also relates to a preparation method for the new solid form of Enzalutamide, pharmaceutical compositions thereof and uses thereof in preparing drugs for treating diseases such as metastatic castration-tolerant prostate cancer.
The present invention relates to novel vortioxetine salt, a solvate and a crystal form thereof, specifically, vortioxetine hemi-hydrobromide and a crystal form thereof, and a vortioxetine hydrobromide isopropanol solvate and a crystal form thereof. Compared with known vortioxetine hydrobromide, the vortioxetine salt, the solvate and the crystal form thereof in the present invention have an improved feature in stability, hygroscopicity, and purity. The present invention also relates to a preparation method of the vortioxetine salt, the solvate and the crystal form thereof, pharmaceutical compositions thereof, and usage thereof in preparing antidepressant drugs.
C07D 295/096 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
A61P 25/00 - Drugs for disorders of the nervous system
16.
CRYSTAL FORM OF REGORAFENIB SALT AND PREPARATION METHOD AND APPLICATION THEREOF
This application relates to a novel regorafenib salt and a crystal form thereof. Compared with an existing regorafenib monohydrate and a crystal form thereof, the regorafenib salt and the crystal form thereof in this application have one or more modification features. This application further relates to preparation methods of the regorafenib salt and the crystal form thereof, a pharmaceutical composition thereof, and application thereof in preparing medicine for treating metastatic colorectal cancer.
The present invention relates to a new crystalline form of the inhibitor 5-fluoro-3-phenyl-2-[(S)-1-(9H-purin-6-ylamino)-propyl]-3H-quinazolin-4-one; the new crystalline form, as compared to known forms, has one or more improved properties. The present invention also relates to a method for preparing a new crystalline form of 5-fluoro-3-phenyl-2-[(S)-1-(9H-purin-6-ylamino) -propyl]-3H-quinazolin-4-one, a pharmaceutical composition thereof, and a use thereof in preparation of a pharmaceutical for the treatment and/or prevention of diseases such as chronic lymphocytic leukemia and indolent non-Hodgkin's lymphoma.
The present invention relates to novel afatinib acid addition salts and crystal forms thereof. Compared with the prior art, the afatinib acid addition salts and crystal forms thereof of the present invention have one or more improved properties. The present invention also relates to a preparation method of the novel afatinib acid addition salts and crystal forms thereof, a pharmaceutical composition thereof, and the use thereof in preparing drugs for treating and/or preventing advanced non-small cell lung cancer and HER2-positive advanced breast cancer.
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
C07C 309/05 - Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing at least two sulfo groups bound to the carbon skeleton
C07C 303/32 - Preparation of esters or amides of sulfuric acidsPreparation of sulfonic acids or of their esters, halides, anhydrides or amides of salts of sulfonic acids
C07C 51/41 - Preparation of salts of carboxylic acids by conversion of the acids or their salts into salts with the same carboxylic acid part
C07C 59/105 - Polyhydroxy carboxylic acids having five or more carbon atoms, e.g. aldonic acids
C07C 307/02 - Monoamides of sulfuric acids or esters thereof, e.g. sulfamic acids
C07C 303/34 - Preparation of esters or amides of sulfuric acidsPreparation of sulfonic acids or of their esters, halides, anhydrides or amides of amides of sulfuric acids
C07C 309/46 - Sulfonic acids having 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 having the sulfo groups bound to carbon atoms of non-condensed six-membered aromatic rings
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
Disclosed are a novel crystal form of Dabrafenib mesylate and preparation method thereof. The novel crystal form of the present invention is more stable in water or an aqueous system, and has greater solubility and dissolution in water, thus having better stability and bioavailability compared with the existing crystal forms.
C07D 417/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
The present invention relates to a new crystalline form of macitentan. The new crystalline form has advantages in terms of solubility. The present invention also relates to a preparation method of the new crystalline form, pharmaceutical composition thereof and use thereof in the manufacture of a medicament for the treatment of hypertension and pulmonary arterial hypertension.
The invention relates to a new crystal form of dabrafenib and preparation method thereof. With respect to known crystal forms, the new crystal form 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. The present invention also relates to a pharmaceutical composition and formulations comprising the new crystal form, and their use in the treatment of Raf family kinase-related diseases.
C07D 417/10 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing aromatic rings
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
patents