The present disclosure relates to a novel crystalline form of a tosylate of diazadicyclic compound of formula (I), preparation method therefor, a pharmaceutical composition containing the crystal form, and the use of the crystal form in the preparation of a drug for treating alopecia areata, psoriasis and ulcerative colitis.
Provided are a crystal form D, a crystal form AJ, a crystal form AL, a crystal form AZ, a crystal form AF, a crystal form Z and a crystal form AE of a compound of formula (I), a process for preparing the same and the use thereof. The crystal forms have advantages in at least one aspect of solubility, melting point, stability, dissolution, hygroscopicity, adhesiveness, fluidity, biological effectiveness, processability, purification effect, preparation production, safety, etc., thus providing a new better choice for the preparation of pharmaceutical preparations containing the compound of formula (I), and having important significance for drug development.
The present invention relates to a crystal form of a substituted oxopyridine derivative and to a preparation method therefor. The invention provides a crystal form A of a compound shown in formula (I), as well as a preparation method therefor and a use thereof. The crystal form A of the formula (I) compound provided by the present invention has at least one of the advantages of: solubility, melting point, stability, degree of dissolution, hygroscopicity, adhesiveness, fluidity, bioavailability, processability, purification effect, preparation production, safety, etc.; a new better choice is provided for preparing a pharmaceutical preparation containing the formula (I) compound, with very important significance for drug development.
C07D 401/10 - 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 aromatic rings
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61P 9/00 - Drugs for disorders of the cardiovascular system
A61K 31/4412 - Non-condensed pyridinesHydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
4.
CRYSTALLINE FORMS OF BENZAMIDE COMPOUND AND PROCESS FOR PREPARING THE SAME
The present disclosure relates to crystalline forms of benzamide compound and processes for preparing the same. Provided are crystalline Form J and an amorphous form of a compound of formula (I), a process for preparing the same, and use thereof. The crystalline Form J has the advantages in at least one of solubility, melting point, stability, dissolution, hygroscopicity, adhesion, fluidity, biological effectiveness, processing performance, purification, formulation production, safety, and the like, which provides a new and better choice for the preparation of pharmaceutical formulations containing the compound of formula (I), and has a very important significance for the drug development.
The present invention relates to a crystal form of an azacyclobutyl nicotinic acid compound and a preparation method therefor. The present invention provides crystal forms B, D, E and K of a compound of formula (I) as well as preparation methods therefor and applications thereof. The crystal forms B, D, E and K of the compound of formula (I) provided by the present invention have advantages in at least one of the following aspects such as solubility, melting point, stability, dissolution rate, hygroscopicity, adhesiveness, fluidity, bioavailability, processability, purification, preparation production, and safety, provide a new and better option for the preparation of a pharmaceutical preparation comprising the compound of formula (I), and are of great significance for pharmaceutical development.
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 31/4427 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems
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
A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
6.
CRYSTALLINE FORMS OF A SULFONAMIDE COMPOUND AND PROCESSES FOR PREPARING THE SAME
The present invention relates to crystalline forms of a sulfonamide compound and processes for preparing the same. The present invention provides five Crystalline Forms B, C, D, E, and F of the compound of formula (I), and processes for preparing the same and uses thereof. The prevent invention also provides processes for preparing the Crystalline Form A. Crystalline Forms B, C, D, E, and F of the compound of formula (I) provided by the present invention have the advantages in at least one of solubility, melting point, stability, dissolution, hygroscopicity, adhesion, fluidity, biological effectiveness, processing performance, purification, formulation production, safety, and the like, which provides a new and better choice for the preparation of pharmaceutical formulations containing the compound of formula (I), and has a very important significance for the drug development.
The present invention relates to crystalline forms of a sulfonamide compound and processes for preparing the same. The present invention provides five Crystalline Forms B, C, D, E, and F of the compound of formula (I), and processes for preparing the same and uses thereof. The prevent invention also provides processes for preparing the Crystalline Form A. Crystalline Forms B, C, D, E, and F of the compound of formula (I) provided by the present invention have the advantages in at least one of solubility, melting point, stability, dissolution, hygroscopicity, adhesion, fluidity, biological effectiveness, processing performance, purification, formulation production, safety, and the like, which provides a new and better choice for the preparation of pharmaceutical formulations containing the compound of formula (I), and has a very important significance for the drug development.
A crystal form A of a compound as shown in formula (I), and a preparation method and use therefor. The crystal form A of the compound as shown in formula (I) has an advantage in at least one of solubility, melting point, stability, dissolution rate, hygroscopicity, adhesiveness, fluidity, biological effectiveness, processability, purification effect, preparation production, and safety. A new and better choice is provided for the preparation of the pharmaceutical formulation containing the compound as shown in formula (I), and the method has very important significance for drug development.
Crystal forms B, M, P, S, E and A of a compound of formula (I), a preparation method therefor and a use thereof. The crystal forms have advantages in at least one of solubility, melting point, stability, dissolution, hygroscopicity, adhesion, fluidity, biological availability and processing performance, purification, preparation production, safety, etc., provide better options for the preparation of pharmaceutical preparations containing the compound of formula (I), and have significance for drug development.
C07D 401/14 - 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 three or more hetero rings
A61K 31/501 - PyridazinesHydrogenated pyridazines not condensed and containing further heterocyclic rings
42 - Scientific, technological and industrial services, research and design
Goods & Services
Chemical analysis; Chemical research; Chemical research services; Conducting of feasibility studies in the field of new technologies; Material testing; Product quality evaluation; Research and development of new products for others; Research in the field of physics; Scientific laboratory services; Technological research in the field of medicine
42 - Scientific, technological and industrial services, research and design
Goods & Services
Chemical analysis; Chemical research; Chemical research services; Conducting of feasibility studies in the field of new technologies; Material testing; Product quality evaluation; Research and development of new products for others; Research in the field of physics; Scientific laboratory services; Technological research in the field of medicine
11.
CRYSTAL FORM OF OXODIHYDROIMIDAZOPYRIDINE COMPOUND AND PREPARATION METHOD THEREFOR
The present invention relates to a crystal form of an oxodihydroimidazopyridine compound and a preparation method therefor. Provided are crystal forms B, C, and E of a compound of formula (I) and a preparation method therefor and a use thereof. The provided crystal forms B, C, and E of the compound of formula (I) have advantages in at least one of solubility, melting point, stability, dissolution, hygroscopicity, adhesion, fluidity, bioavailability and processability, purification, preparation production, safety, and the like, provide a new better option for preparation of a pharmaceutical preparation containing the compound of formula (I), and are very important for drug development.
A61K 31/437 - 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 heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
A61P 37/00 - Drugs for immunological or allergic disorders
A61P 37/06 - Immunosuppressants, e.g. drugs for graft rejection
A61P 25/00 - Drugs for disorders of the nervous system
12.
CRYSTAL FORMS OF SULFAMOYL PYRROLE AMIDE COMPOUNDS AND PREPARATION METHODS THEREFOR
Provided are crystal forms relating to sulfamoyl pyrrole amide compounds and preparation methods therefor. Specifically, two crystal forms A and B of compounds of formula (I) and preparation methods and uses therefor are provided. The provided crystal forms A and B of the compounds of formula (I) have advantages in at least one aspect regarding solubility, melting point, stability, dissolution, hygroscopicity, adhesion, fluidity, bioavailability, processability, purification effect, preparation production, safety, etc., provide a new and better choice for the preparation of pharmaceutical formulations comprising the compounds of formula (I), and are of great significance for drug development.
A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
Provided are a new crystal form of hydrochloride of (R)-N-(4-(chlorodifluoromethoxy)phenyl)-6-(3-hydroxypyrrolidin-1-yl)-5-(1H-pyrazol-5-yl)nicotinamide, a preparation method therefor, a pharmaceutical composition containing the compound, and the use thereof in the preparation of a drug. The compound is a selective Abl1 allosteric inhibitor, and can be used for preventing and/or treating Bcr-Abl tyrosine kinase-mediated diseases.
C07D 401/14 - 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 three or more hetero rings
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
Provided are a crystal form 2, a crystal form 8, a crystal form 10, and a crystal form 16 of a hemifumarate salt of formula (I), preparation methods therefor, and uses thereof. The crystal form 2, crystal form 8, crystal form 10, and crystal form 16 of the hemifumarate salt of a compound of formula (I) have advantages in at least one of solubility, melting point, stability, dissolution, hygroscopicity, adhesiveness, fluidity, biological effectiveness, processability, purification effect, formulation production, safety and the like, thus providing a new better choice for the preparation of pharmaceutical preparations containing the hemifumarate salt of the compound of formula (I), and having very important significance for drug development.
C07D 205/04 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
A61K 31/397 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
A61P 37/00 - Drugs for immunological or allergic disorders
15.
CRYSTAL FORMS OF PYRROLE DERIVATIVE COMPOUND AND PREPARATION METHOD THEREFOR
The present invention relates to crystal forms of a pyrrole derivative compound and a preparation method therefor. Provided are three crystal forms, crystal form A, crystal form C, and crystal form D, of a compound represented by formula (I), a preparation method therefor and a use thereof. The provided crystal form A, crystal form C, and crystal form D of the compound represented by formula (I) have advantages in at least one aspect among solubility, melting point, stability, dissolution, hygroscopicity, adhesion, fluidity, bioavailability and processability, purification, preparation production, safety, and so on. The present invention provides a new and better option for the preparation of pharmaceutical preparations containing the compound represented by formula (I), and is very important for drug development.
Provided are a crystal form D, a crystal form AJ, a crystal form AL, a crystal form AZ, a crystal form AF, a crystal form Z and a crystal form AE of a compound of formula (I), a preparation method therefor and use thereof. The crystal forms have advantages in at least one aspect of solubility, melting point, stability, dissolution, hygroscopicity, adhesiveness, fluidity, biological effectiveness, processability, purification effect, preparation production, safety and the like, thus providing a new better choice for the preparation of pharmaceutical preparations containing the compound of formula (I), and having important significance for drug development.
C07D 239/91 - Oxygen atoms with aryl or aralkyl radicals attached in position 2 or 3
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
17.
NEW CRYSTAL FORMS OF INDOLE CARBOXAMIDE COMPOUND AND PREPARATION METHOD THEREFOR
New crystal forms of an indole carboxamide compound and a preparation method therefor. Provided are preparation methods and uses for crystal form C, crystal form A, crystal form Y, crystal form V, crystal form AE, and crystal form AA of formula (I), the provided crystal form C, crystal form A, crystal form Y, crystal form V, crystal form AE, and crystal form AA of a compound of formula (I) are advantageous in at least one aspect among solubility, melting point, stability, dissolution, hygroscopicity, adhesiveness, flowability, bioavailability, as well as processability, a purification effect, production of a formulation, safety, etc., providing new, better choices for preparation of a pharmaceutical formulation containing a compound of formula (I), and having great significance for pharmaceutical development.
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
C07D 401/10 - 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 aromatic rings
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 209/18 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
A61K 31/4045 - Indole-alkylaminesAmides thereof, e.g. serotonin, melatonin
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
A61P 37/00 - Drugs for immunological or allergic disorders
18.
NEW CRYSTAL FORM OF BENZOIC ACID DERIVATIVE AND PREPARATION METHOD THEREFOR
Provided are three crystal forms A, B and C of the compound of formula (I), and a preparation method therefor and the use thereof. Crystal forms A, B and C of the compound of formula (I) have an improved solubility, melting point, stability, dissolution, hygroscopicity, adhesion, fluidity, biological effectiveness and processing performance, purification effect, preparation production, safety etc., and provide better choices for drug preparation.
C07D 491/052 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered
A61K 31/4162 - 1,2-Diazoles condensed with heterocyclic ring systems
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
19.
CRYSTAL FORMS OF BENZAMIDE COMPOUNDS AND PREPARATION METHOD THEREFOR
The present invention relates to crystal forms of benzamide compounds and a preparation method therefor. Provided are a crystal form J and an amorphous form of a compound of formula (I), and a preparation method and use thereof. The provided crystal form J of the compound of formula (I) has advantages in at least one of the aspects such as the solubility, melting point, stability, dissolution, hygroscopicity, adhesion, fluidity, biological effectiveness, processing performance, purification effect, preparation production, and safety, and provide a new and better choice for the preparation of a pharmaceutical preparation containing the compound of formula (I), thus achieving very important significance for drug development.
A crystal form of a propenone compound, and a preparation method therefor. Provided in the present invention are two crystal forms A and B of a malonate of the compound of formula (I), and a preparation method therefor and a use thereof. The malonate crystal forms A and B of the compound of formula (I) provided in the present invention have advantages in at least one aspect among solubility, melting point, stability, dissolution, hygroscopicity, processability, purification effect, preparation production, and safety, thus providing a new and better choice for the preparation of pharmaceutical preparations containing the compound of formula (I), and having very important significance for drug development.
A61K 31/4375 - 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 heterocyclic ring system containing a six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
21.
NEW CRYSTAL FORM OF BENZAMIDE COMPOUND AND DIHYDROCHLORIDE THEREOF, AND PREPARATION METHOD THEREFOR
The present invention relates to the field of chemical medicines, and particularly to a new crystal form of a free base and dihydrochloride of benzamide compounds, and a preparation method therefor. Provided in the present invention are a method for preparing dihydrochloride crystal form J, dihydrochloride crystal form M, dihydrochloride crystal form E, dihydrochloride crystal form F, dihydrochloride crystal form H, dihydrochloride crystal form N, dihydrochloride crystal form Q, dihydrochloride crystal form S, dihydrochloride crystal form T, dihydrochloride crystal form K and free base crystal form A, free base crystal form B and free base crystal form C of a compound of formula (I), and the use thereof. Dihydrochloride crystal form J, dihydrochloride crystal form M, dihydrochloride crystal form E, dihydrochloride crystal form F, dihydrochloride crystal form H, dihydrochloride crystal form N, dihydrochloride crystal form Q, dihydrochloride crystal form S, dihydrochloride crystal form T, dihydrochloride crystal form K and free base crystal form A, free base crystal form B and free base crystal form C of the compound of formula (I) provided in the present invention have advantages in terms of at least one of the following aspects: solubility, melting point, stability, dissolution rate, hygroscopicity, adhesion, fluidity, bioavailability, processing performance, purification effect, preparation production, safety etc., which provides a new better choice for the preparation of a pharmaceutical preparation containing a free base of the compound of formula (I) and the dihydrochloride thereof, and is of great significance to drug development.
C07D 401/10 - 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 aromatic rings
C07D 253/07 - 1,2,4-Triazines having three double bonds between ring members or between ring members and non-ring members with hetero atoms, or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
Disclosed are crystal form A of a p-toluenesulfonate salt of a diazabicyclic compound as represented by formula (I) and a preparation method therefor. The crystal form A of the p-toluenesulfonate salt of the compound as represented by formula (I) has advantages in at least one aspect from among solubility, melting point, stability, dissolution, hygroscopicity, adhesion, fluidity, bioequivalence, processing performance, purification, preparation production, safety etc. and can be used for preventing or treating alopecia areata, psoriasis and ulcerative colitis.
The present invention relates to a crystal form C of (2E)-N-[4-[(3-chloro-4-fluorophenyl)amino]-7-methoxy-6-quinazolinyl]-4-(1-piperidinyl)-2-butenamide, and a preparation method therefor and a drug containing same. The crystal form C is an anhydrous substance; and by means of Cu-Kα radiation, the X-ray powder diffraction pattern of the crystal form C has characteristic peaks where the diffraction angle 2θ is 5.6° ± 0.2°, 10.5° ± 0.2°, and 12.8° ± 0.2°. The crystal form C of the present invention is an anhydrous substance, and has obvious advantages in drug development in comparison with existing solvates. In addition, while maintaining good stability, the crystal form C of the present invention has a significantly improved solubility compared with existing solvates.
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
The present invention relates to a novel crystal form of a benzothiazole compound and a preparation method therefor. Provided in the present invention are a crystal form A of a compound of formula (I) and a preparation method therefor and a use thereof. The crystal form A of the compound of formula (I) provided in the present invention has advantages in at least one aspect of solubility, melting point, stability, dissolution, hygroscopicity, adhesiveness, fluidity, biological effectiveness, processability, purification effect, preparation production, safety and the like, thus providing a new better choice for the preparation of pharmaceutical preparations containing the compound of formula (I), and having very important significance for drug development.
The present invention relates to crystal forms of a sulfonamide compound and a preparation method therefor. Provided in the present invention are five crystal forms B, C, D, E and F of a compound of formula (I), and a preparation method therefor and the use thereof. Also provided in the present invention is a method for preparing crystal form A. The crystal forms B, C, D, E and F of the compound of formula (I) provided in the present invention have advantages in at least one of solubility, melting point, stability, dissolution, hygroscopicity, adhesion, fluidity, biological effectiveness, processing performance, purification effect, preparation production, safety and so on, and provide a new and better choice for the preparation of a pharmaceutical preparation containing the compound of formula (I), which has very important implications for drug development.
Provided are crystal forms X, III, and V of a monosuccinate of ribociclib as a compound shown in formula (I) and preparation methods thereof. Also provided are pharmaceutical compositions containing the crystal forms. Also provided are uses of the crystal forms in preparing a cyclin-dependent kinase 4/6 inhibitor or a pharmaceutic preparation for treating breast cancer.
The present invention relates to novel crystalline forms of 7-cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide (compound I), its salts, and process for preparation thereof. Crystalline forms in the present invention have good stability, low hygroscopicity, good processability, easy treatability and other favorable properties. In addition, the process is simple, low cost, and has an important value for future optimization and development of the drug.
C07D 401/14 - 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 three or more hetero rings
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 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
Novel crystalline forms of trisodium [3-((1S,3R)-1-biphenyl-4-ylmethyl-3-ethoxycarbonyl-1-butylcarbamoyl) propionate-(S)-3′-methyl-2′-(pentanoyl{2″-(tetrazol-5-ylate)biphenyl-4′-ylmethyl}amino)butyrate] hydrate, methods for their preparation, pharmaceutical compositions comprising these new forms, and use of them for treating or delaying progression or onset of diseases or disorders related to activity of angiotensin receptor 1 (AT1) blockage and neprilysin (NEP) inhibition, such as heart failure, are disclosed.
A61K 31/41 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
C07C 233/47 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton
29.
Crystal form of lenvatinib methanesulfonate salt and preparation method thereof
The present disclosure relates to a novel crystalline form of lenvatinib mesylate and the preparation method thereof. The novel crystalline form of mesylate of the present disclosure can be used for treating invasive and differentiated thyroid cancer. The novel crystalline form of mesylate of the present disclosure has good solubility, stability, and remarkable purification effect in process. The preparation method of this novel crystalline form is simple, low cost, and has an important value for future optimization and development of the drug.
The present invention relates to two AP26113 crystals and a preparation method therefor. Provided in the present invention, crystal CS1 and crystal CS2 of AP26113 have advantages in terms of solubility and stability, are suitable for process development, provide improved options for preparing a pharmaceutical preparation containing AP26113, and are of great significance to the development of a medicament.
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
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A crystal form of an adenosine A2A receptor antagonist drug, tozadenant, and a preparation method and use thereof. The prepared tozadenant has crystal form CS1, can be used to prepare an adenosine A2A receptor antagonist drug formulation, provides a new option for the preparation of a drug formulation containing tozadenant, and has a crucial value for drug development.
C07D 417/12 - 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 chain containing hetero atoms as chain links
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 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
Novel crystalline Forms of trisodium [3-((1S,3R)-1-biphenyl-4-ylmethyl-3-ethoxycarbonyl-1-butyl carbamoyl) propionate-(S)-3′-methyl-T-(pentanoyl{2″-(tetrazol-5-ylate)biphenyl-4′-ylmethyl}amino)butyrate] hydrate, methods for their preparation, pharmaceutical compositions comprising these new forms, and use of them for treating or delaying progression or onset of diseases or disorders related to activity of angiotensin receptor 1 (AT1) blockage and neprilysin (NEP) inhibition, such as heart failure, are disclosed.
The present invention relates to novel crystalline forms of 7-cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-car boxylic acid dimethylamide(compound I), its salts, and process for preparation thereof. Crystalline forms in the present invention have good stability, low hygroscopicity, good processability, easy treatability and other favorable properties. In addition, the process is simple, low cost, and has an important value for future optimization and development of the drug.
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
C07D 401/14 - 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 three or more hetero rings
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
34.
CRYSTALLINE FORM E OF TAFAMIDIS METHYLGLUCAMINE SALT, AND PREPARATION METHOD AND APPLICATION THEREOF
The present invention discloses a novel crystalline form E of a tafamidis methylglucamine salt, and a preparation method and application thereof. When compared to other known crystalline forms, the new crystalline form provided in the invention has the advantages of easy preparation, low technical requirements, and low hygroscopicity. The invention therefore provides a new and better option for preparing a pharmaceutical product comprising a tafamidis methylglucamine salt, and is very important for pharmaceutical product development.
The present invention relates to AHU377 crystal forms, and a preparation method therefor and the use thereof. Provided are AHU377 crystal forms III and IV, and the crystal forms III and IV have a good stability, a low hygroscopicity, a high impurity removal capacity, and a good purifying effect, and have a very high economic value.
C07C 233/47 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton
A61K 31/216 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acids having aromatic rings, e.g. benactizyne, clofibrate
A61K 31/41 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
A61P 9/04 - Inotropic agents, i.e. stimulants of cardiac contractionDrugs for heart failure
A61P 9/00 - Drugs for disorders of the cardiovascular system
A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
36.
HYDROCHLORIDE SALT CRYSTAL OF DRUG FOR TREATING OR PREVENTING JAK-ASSOCIATED DISEASE AND PREPARATION METHOD THEREOF
Disclosed are a hydrochloride salt crystal of a drug (Filgotinib) for treating or preventing a JAK-associated disease and a preparation method, pharmaceutical composition, and formulation thereof, and an application of the hydrochloride salt crystal, the pharmaceutical composition, and the formulation in the prevention and/or treatment of a disease associated with a JAK family kinase. In comparison to a known crystal, the crystal provided in the invention shows more favorable properties in terms of pharmaceutical engineering, such as higher stability under low water activity conditions, simplicity in the preparation process and/or higher solubility.
A61K 31/437 - 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 heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
37.
CRYSTAL FORM A OF 2-[(2R)-2-METHYL-2-PYRROLIDYL]-1H-BENZIMIDAZOLE-7-CARBOXAMIDE DIHYDROCHLORIDE AND PREPARATION METHOD THEREOF
Provided are a crystal form A of 2-[(2R)-2-methyl-2-pyrrolidyl]-1H-benzimidazole-7-carboxamide dihydrochloride and the preparation method and use thereof. An X-ray powder diffractogram of crystal form A has a characteristic peak at the following 2θ-diffraction angles: 8.3°±0.2°, 26.7°±0.2° and 16.1°±0.2°. Crystal form A, compared with the existing crystal form, has a surprisingly excellent solubility, mechanical and storage stabilities and particle size distribution, is a more ideal crystal form compared with the reported crystal forms, better satisfies medicinal requirements, and has an important value for the optimization and development of the drug in the future.
C07D 403/04 - 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 directly linked by a ring-member-to-ring- member bond
A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
The present invention relates to crystal form II of 5-chlorine-N2-(2-isopropoxy-5-methyl-4-piperidine-4-yl-phenyl)-N4-[2-(propane-2-sulfonyl)-phenyl]-pyrimidine-2,4-diamine (ceritinib), and the present invention also relates to the method for preparing the crystal form, the pharmaceutical composition comprising the crystal form and the method for treating diseases with the crystal form and the pharmaceutical composition. The crystal form provided by the present invention has advantageous performances, such as a good stability, relatively low hygroscopicity, exploitability and strong treatability of process, and the preparation method is simple, is low cost, and has an important value for the optimization and development of the drug in the future.
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
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
The present invention relates to new crystalline forms I, II and III of 6-(1H-indazol-6-yl)-N-[4-(4-morpholinyl)phenyl]imidazo[1,2-a]pyrazin-8-amine methanesulfonate, and a preparation method and use for the crystalline forms. Crystalline form I is a dimethanesulfonate, and has characteristic peaks at 2theta values of 5.9° ±0.2°, 13.5° ±0.2° and 21.8° ±0.2° in an X-ray powder diffraction pattern. Crystalline form II is a dimethanesulfonate, and has characteristic peaks at 2theta values of 15.8° ±0.2°, 17.2° ±0.2° and 19.5° ±0.2° in an X-ray powder diffraction pattern. Crystalline form III is a monomethanesulfonate, and has characteristic peaks at 2theta values of 7.4° ±0.2°, 12.9° ±0.2° and 19.2° ±0.2° in an X-ray powder diffraction pattern. The crystalline forms meet medicinal requirements better than existing crystalline forms, and the preparation method for the crystalline forms is simple and has good reproducibility and significant value for future drug optimisation and development.
The present invention relates to a new crystal form B and crystal form C of eluxadoline and the preparation method and use thereof, wherein the X-Ray powder diffractogram of crystal form B has characteristic peaks at the following 2 θ-diffraction angles: 6.3°±0.2°, 15.0°±0.2° and 17.8°±0.2°, and the crystal form B can be obtained through adding the free form of eluxadoline into two ketonic solvents or a mixed solvent of ketonic or ester solvents, and stirring for crystallization; and the X-Ray powder diffractogram of crystal form C has characteristic peaks at the following 2 θ-diffraction angles: 11.6°±0.2°, 13.0°±0.2°, 6.6°±0.2° and 16.2°±0.2°, and the crystal form C can be obtained through adding the free form of eluxadoline into a mixed solvent of an amide solvent and ketonic solvent or a mixed solvent of an alcohol solvent or alkane solvent, and stirring for crystallization. The fluidity of the particles of crystal forms B and C in the present invention has been improved significantly compared with the existing β crystal form, and the purity is higher and the new crystal forms can be stably and controllably prepared.
C07D 233/64 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
Disclosed are crystalline forms 1, 2, and 3 of a selective S1P1 receptor agonist, namely Ponesimod, and a method for preparing the same. An X-ray powder diffraction pattern of the crystalline form 1 has characteristic peaks at 2 theta values of 18.1° ± 0.2°, 14.6° ± 0.2°, and 11.3° ± 0.2°. An X-ray powder diffraction pattern of the crystalline form 2 has characteristic peaks at 2 theta values of 3.8° ± 0.2°, 10.8° ± 0.2°, and 6.1° ± 0.2°. An X-ray powder diffraction pattern of the crystalline form 3 has characteristic peaks at 2 theta values of 12.2° ± 0.2°, 6.2° ± 0.2°, and 5.6° ± 0.2°. Compared with existing crystalline forms, the present invention has better stability and a greatly increased solubility, and is more suitable for development of a pharmaceutical preparation containing Ponesimod
Disclosed is a preparation method for a eutectic hydrate crystal form II of AHU-377 and diovan trisodium salt, comprising: firstly, obtaining a clear solution of an AHU-377 and diovan trisodium salt compound, a solvent of the clear solution consisting of an anti-solvent and an n-solvent of a target product crystal form II, and the boiling point of the n-solvent being lower than that of the anti-solvent; secondly, removing the n-solvent and water from a system by evaporation under closed conditions; and finally, selectively adding a seed crystal of the crystal form II, and additionally adding a mixture of water and a carrier solvent to perform stirring crystallization. The method in the present invention can prepare a crystal form II, and has a stable and controllable technological process. The prepared crystal form II product is high in chemical purity, crystal form purity and fluidity, the process can be amplified, and demands for large-scale production are met.
C07C 233/47 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton
The present invention relates to a composition and eutectic of saxagliptin and metformin, and a preparation method and use thereof. In particular, provided in the present invention are a composition and a eutectic form in which the molar ratio of saxagliptin and metformin is 1:1, wherein the X-ray powder diffraction pattern (CuK α radiation) of eutectic crystal form I thereof has characteristic peaks at 2 theta values of 17.8° ± 0.2°, 6.6° ± 0.2° and 22.4° ± 0.2° at 25ºC. The composition and eutectic provided in the present invention have good stability, low wettability, and a solubility meeting the medicinal requirements, all of which are of great value for the optimization and development of the drug in the future.
A61K 31/403 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
Disclosed are a novel crystal form of Flibaserin, and a preparation method therefor. The novel crystal form of Flibaserin of the present invention is named a crystal form I and a crystal form II. Compared with an existing crystal form, the novel crystal form is high in stability, solubility, and bioavailability. The crystal form I, the crystal form II, or a mixture of the crystal form I and the crystal form II of the present invention can be used for preparing pharmaceutical preparations for treating depression, schizophrenia, anxiety disorders, sleep disorders, sexual and mental disorders, and age-related memory disorders, and particularly used for preparing pharmaceutical preparations for treating a hypoactive sexual desire disorder (HSDD).
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 25/00 - Drugs for disorders of the nervous system
45.
NEW CRYSTAL FORM OF IMIDAZOLYL BIPHENYL COMPOUND SALT AND PREPARATION METHOD THEREOF
The present invention provides a new crystal form of a dihydrochloride of the compound of formula (I) and a preparation method thereof. The new crystal forms provided in the present invention are named crystal form A and crystal form B, and compared with the prior art, have improved stability and flowability and the dissolution rate meets the requirements of medicinal use. In particular, crystal form A under specific conditions has better stability than an existing N-2 crystal form. The preparation process of crystal forms A and B have convenient operations, a solvent is easily obtained, and the invention thus has great value for the optimization and development of future medicaments. The present invention provides crystal forms A and B of a dihydrochloride of the compound of formula (I) or a combination thereof for use in the preparation of pharmaceutical preparations for treating liver diseases such as hepatitis and in particular hepatitis C.
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
Disclosed in the present invention are novel crystalline form IX, crystalline form X and crystalline form XII of palbociclib and preparation method therefor and uses thereof. An X-ray powder diffraction pattern of the crystalline form IX has characteristic peaks expressed in degrees 2-theta at 16.8 ± 0.2, 8.4 ± 0.2 and 24.3 ± 0.2. An X-ray powder diffraction pattern of the crystalline form X has characteristic peaks expressed in degrees 2-theta at 21.5 ± 0.2, 17.0 ± 0.2, 17.5 ± 0.2. An X-ray powder diffraction pattern of the crystalline form XII has characteristic peaks expressed in degrees 2-theta at 21.4 ± 0.2, 22.4 ± 0.2, 20.5 ± 0.2. Compared to the existing crystalline forms, the crystalline forms of the present invention have higher solubility and particle size distribution and morphology more suitable for pharmaceutical use, provide new and better options in preparing pharmaceutical preparations comprising palbociclib and are important for drug development.
The present invention relates to novel crystalline forms of a cell apoptosis inducing agent and a preparation method therefor, the structural formula whereof is shown in formula (I). The crystalline forms are obtained directly from the solvent by crystallization, and have a good stability, low wetting and uniform particle size distribution, and provide a new and improved choice for the preparation of pharmaceutical preparations containing ABT199, and are of great significance for drug development.
The invention relates to a crystal form H and a preparation method of a 5-[2,6-Di(4-morpholinyl)-4-pyrimidinyl]-4-(trifluoromethyl)-2-pyridinamine monohydrochloride. An x-ray powder diffraction pattern of the crystal form H in 25°C comprises characteristic peaks of a 2theta value at 16.6°±0.2°, 15.8°±0.2°, and 18.5°±0.2°. In comparison to a conventional crystal form, the crystal form H has favorable stability and low hygroscopicity, and is significant in drug development.
C07D 401/14 - 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 three or more hetero rings
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
C07D 239/28 - Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
Provided are novel crystal forms of panobinostat lactate, named a crystal form G, a crystal form H, and a crystal form I, respectively. An X-ray powder diffraction pattern of the crystal form G has a characteristic peak at a 2theta value 7.7°±0.2°, 20.0°±0.2°, and 10.3°±0.2°. An X-ray powder diffraction pattern of the crystal form H has a characteristic peak at a 2theta value 11.8°±0.2°, 21.0°±0.2°, and 15.0°±0.2°. An X-ray powder diffraction pattern of the crystal form I has a characteristic peak at a 2theta value 10.2°±0.2°, 25.0°±0.2°, and 22.9°±0.2°. The provided three novel crystal forms of panobinostat lactate can assist a researcher in understanding and controlling heteromorphism of the panobinostat lactate, thereby facilitating preparation of a medicine which is more effective or more stable.
The invention relates to a crystal salt of a 5-[2,6-Di(4-morpholinyl)-4-pyrimidinyl]-4-(trifluoromethyl)-2-pyridinamine dihydrochloride and a preparation method thereof, and specifically, to a dihydrochloride having Crystal form I or Crystal form II. The crystal forms have favorable stability, increased solubility, and decreased hygroscopicity, possessing a significant value in future drug development and optimization.
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 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
NOVEL CRYSTAL FORM OF 3-(6-(1-(2,2-DIFLUOROBENZO[D][1,3]DIOXOLE-5-YL)CYCLOPROPANE FORMAMIDO)-3-METHYLPYRIDINE-2-YL)BENZOIC ACID AND PREPARATION METHOD THEREOF
A crystal form A of 3-(6-(1-(2,2-difluorobenzo[D][1,3]dioxole-5-yl)cyclopropane formamido)-3-methylpyridine-2-yl)benzoic acid and preparation method thereof. The crystal form A has a low hygroscopicity, convenience for storage, good stability, and higher solubility than the prior art, and therefore plays an important role in future optimization and development of the drug.
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
A61K 31/443 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
A61P 11/00 - Drugs for disorders of the respiratory system
52.
B CRYSTAL FORM OF 2-[(2R)-2-METHYL-2-PYRROLIDINYL]-1H-BENZIMIDAZOLE-7-CARBOXAMIDE, PREPARATION METHOD AND USE
A B crystal form of 2-[(2R)-2-methyl-2-pyrrolidinyl]-1H-benzimidazole-7-carboxamide (ABT-888), a preparation method thereof and use are provided. The X-ray powder diffraction pattern (CuKα radiation) of B crystal form at 25 ℃ has characteristic peaks at 2 theta values of 9.40 ° ± 0.20 °, 17.30 ° ± 0.20 °, 22.80 ° ± 0.2 °. The B crystal form is prepared by dissolving ABT-888 free alkali in methanol and volatilizing the same at room temperature into a B crystal form. Compared with existing crystal forms, the B crystal form has a higher solubility and a simpler preparation process, and has good stability. The B crystal form is of great significance for improving the efficacy of and for reducing the drug load for treating metastatic breast cancer, colon cancer, metastatic melanoma and brain tumor.
C07D 403/04 - 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 directly linked by a ring-member-to-ring- member bond
A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
The present invention provides a crystalline form A of masitinib mesylate, a preparation method therefor and a medical use thereof. The hygroscopicity of crystalline form A is remarkably reduced. Therefore, it is convenient for medicaments preparation and long-term storage.
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
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
54.
NOVEL CRYSTALLINE FORMS OF VOLASERTIB AND TRIHYDROCHLORIDE THEREOF
The present invention provides novel crystalline forms of Volasertib and Volasertib trihydrochloride, preparation methods therefor, medical uses thereof and compositions comprising same. Compared with the known crystalline forms, the novel crystalline forms of the present invention have significantly improved fluidity. Furthermore, the crystalline forms of the present invention have relatively good storage stability, are good supplements for the known crystalline forms and have important application values. The preparation methods of the present novel crystalline forms are simple, low-cost and adaptable to industrialization.
Novel salts and cocrystals of lesinurad, processes for their preparation, pharmaceutical compositions comprising these new salt forms and co-crystals, and use of them for treating or delaying progression or onset of diseases or disorders related to activity of uric acid transport 1 (URAT1) proteins are disclosed. These novel forms were characterized by X-ray powder diffraction, differential scanning calorimetry, and other techniques. They can be readily prepared and are suitable for preparation of solid dosage forms owing to their ease of handling and superior pharmacological properties.
The present invention relates to a new crystal form of a Lenvatinib methanesulfonate salt and a preparation method thereof. The new crystal form of the Lenvatinib methanesulfonate salt provided in the present invention can be used for treating invasive and differentiated thyroid cancer. The new crystal form of the Lenvatinib methanesulfonate salt provided in the present invention has a good solubility and stability, significant effects in the purification process, a simple preparation method and low cost, and has an important value for the optimization and development of this drug in future.
Disclosed are a co-crystal of olaparib and urea and a preparation method therefor. Specifically disclosed is a co-crystal form A, and an X-ray powder diffraction pattern of this crystal form has characteristic peaks at points where 2theta value is 17.4°±0.2°, 20.7°±0.2°, 10.5°±0.2°. The disclosed co-crystal has better stability, lower hygroscopicity and higher solubility as compared to existing olaparib free alkali crystal forms.
C07D 237/32 - Phthalazines with oxygen atoms directly attached to carbon atoms of the nitrogen-containing ring
C07C 273/02 - Preparation of urea or its derivatives, i.e. compounds containing any of the groups the nitrogen atoms not being part of nitro or nitroso groups of urea, its salts, complexes or addition compounds
A61K 31/502 - PyridazinesHydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
The present invention relates to a crystal form I of Dapagliflozin which is a medicine for treating type II diabetes, and a preparation method therefor. The crystal form I is characterized in that an x-ray powder diffraction pattern has characteristic peaks when 2theta values are 15.8°±0.2°, 19.8°±0.2° and 28.7°±0.2°. Compared with the prior art, the crystal form I has better stability, facilitates the long-term storage of a medicine, and avoids crystal transformation during medicine development and storage. The preparation method is simple, facilitates cost control in technological production, and has very high economic value.
A61K 31/351 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom not condensed with another ring
A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
59.
CRYSTAL FORM OF N-[6-(CIS FORM-2,6-DIMETHYLMORPHOLINE-4-GROUP)PYRIDINE-3- GROUP]-2-METHYL-4'-(TRIFLUOROMETHOXY)[1,1'-BIPHENYL]-3- FORMAMIDE MONOPHOSPHATE, AND PREPARATION METHOD THEREFOR
The present invention relates to a crystal form of N-[6-(cis form-2,6-dimethylmorpholine-4-group) pyridine-3- group]-2-methyl-4'-(trifluoromethoxy)[1,1'-biphenyl]-3- formamide monophosphate, and a preparation method therefor. The crystal form of the monophosphate of a compound represented by formula (I) has low hygroscopicity, is convenient to store, has better stability than that of diphosphate in the prior art, can avoid the risk of crystal transformation in the development and production of a drug. The preparation method is simple, has low cost, and has important value for further optimization and development of the drug.
C07D 413/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
The present invention relates to a CDK inhibitor, a eutectic crystal of an MEK inhibitor, and a preparation method therefor. Specifically, the present invention provides hydrates or anhydrous substance crystal forms which are named as a crystal form I, a crystal form II and a crystal form III. The eutectic crystal provided in the present invention has good stability, low hygroscopicity and high solubility, and has important value for further optimization and development of the drug.
C07D 235/06 - BenzimidazolesHydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
The present invention relates to a new crystal form of 5-(2-cyan-4-pyridyl)-3-(4-pyridyl)-1,2,4-triazole, and a preparation method therefor. The new crystal form provided in the present invention can be used for treating gout and hyperuricemia. The new crystal form provided in the present invention has good stability, an obvious refinement effect in process, and has a solubility and hygroscopicity satisfying drug use requirements. The crystal form A provided in the present invention has favorable performance facilitating industrial production, and has important value for further optimization and development of the drug.
C07D 401/14 - 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 three or more hetero rings
A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
A61P 19/06 - Antigout agents, e.g. antihyperuricemic or uricosuric agents
A61P 43/00 - Drugs for specific purposes, not provided for in groups
62.
AHU377 CRYSTAL FORM, PREPARATION METHOD AND USE THEREOF
The present invention relates to a new crystal form of a compound of formula (I), a preparation method and a use thereof. The new crystal form provided in the present invention is stable and has a low hygroscopicity, and a purification process has a remarkable effect on the new crystal form. The new crystal form of the compound of formula (I) provided in the present invention can be used to prepare a medicine treating heart failure.
C07C 233/47 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton
A preparation method of a PCI-32765 crystal form A. The preparation method comprises the following steps: 1) dissolving free alkali solid of PCI-32765 into a positive solvent; 2) adding a solution in the step 1) in an anti solvent dropwise, stirring after dropwise adding is completed, and adding a crystal seed of the PCI-32765 crystal form A, or adding the solution in the step 1) in suspension liquid containing the crystal seed of the PCI-32765 crystal form A; 3) controlling a solution system obtained in the step 2) to continuously stir, and ageing to obtain crystal magma; and 4) filtering, washing and drying the crystal magma to obtain powder of the PCI-32765 crystal form A. The preparation method has the characteristics of simpleness in process operation, stable and controllable process, high yield, environmental protection, good impurity removing capacity and suitability for industrial production. In addition, the prepared crystal form A can be stably stored, and the hygroscopicity and the solubility of the prepared crystal form A meet the requirements for medicinal use.
The present invention relates to a new crystal form of a JAK inhibitor and a preparation method thereof. The new crystal form provided in the present invention can be used to treat autoimmunity disease and particularly rheumatoid arthritis. The new crystal form provided in the present invention is stable, a purification process has a remarkable effect on the new crystal form, and the solubility and hygroscopicity thereof meet the medicinal requirement. The new crystal form is simple to prepare, has low costs and has an important value to future optimization and development of the medicine.
The present invention relates to a crystal form for treating melanoma and ovarian cancer and a preparation method thereof. The crystal form A and the crystal form B provided by the present invention have a good stability, the process purification effect thereof is significant, and the solubility and hygroscopicity thereof meet medicinal requirements. The preparation method of the crystal form is simple, the cost is low, and the future optimization and development of the drug has significant value.
C07D 235/06 - BenzimidazolesHydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
The present invention relates to an α crystal form of a formula (I) compound used for preparing a leukemia treatment drug and preparation method thereof. The α crystal form provided in the present invention has a better stability, solubility and hygroscopicity comply with pharmaceutical requirements. The α crystal form has a simple preparation method and a low manufacturing cost, and provides a significant value to future optimization and development of the drug.
The present invention relates to a new crystalline form of (R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide hydrochloride and a preparation method for the new crystalline form. The crystalline form has advantageous properties such as good stability, low hygroscopicity, a developable process and tractability. The preparation method is simple and low-cost, and has significant value for the future optimisation and development of the drug.
C07D 453/02 - Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
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 25/28 - 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 25/18 - Antipsychotics, i.e. neurolepticsDrugs for mania or schizophrenia
68.
PHOSPHATE OF EPIDERMAL GROWTH FACTOR RECEPTOR INHIBITOR, CRYSTALLINE FORM OF PHOSPHATE, AND PREPARATION METHOD
The present invention relates to a phosphate crystalline form A of the compound of formula (I), and a preparation method for the phosphate crystalline form A. The phosphate crystalline form A has advantageous properties such as good solubility, low hygroscopicity and process developability. The preparation method is simple and low-cost, and has significant value for the future optimisation and development of the drug.
C07D 403/04 - 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 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
Provided are a new crystalline form of an antiandrogen drug which treats prostate cancer, said drug being represented by formula I, and a preparation method for the new crystalline form. The crystalline form has good stability, and the solubility and hygroscopicity meet pharmaceutical requirements. The preparation method is simple and low-cost.
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 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
The present invention relates to crystalline forms of (3β)-17-(1H-benzimidazole-1-yl)androstane-5, and 16-diene-3-ol phosphate, tartrate, and citrate and preparation methods therefor. Crystalline forms of phosphate, tartrate, and citrate of a compound of formula (I) in the present invention have advantageous performance such as high solubility, low hygroscopicity, good stability, a simple process, and being easy to operate, are suitable for storage and industrialized production, and have an important value in future optimization and development of the drug.
C07J 43/00 - Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta[a]hydrophenanthrene skeleton
A61K 31/58 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
The present invention relates to a new crystal form of neratinib maleate and a preparation method therefor. A new crystal form of the maleate of a compound as represented by formula (I) of the present invention has advantageous properties of high solubility, good stability, technological availability and tractability, and the preparation method is simple and requires low costs, which is of important value for the optimization and development of the drug in the future.
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
A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
The present invention relates to a crystal form A of obeticholic acid and a preparation method therefor. The crystal form A provided by the present invention has characteristic peaks at 2theta having values of 4.9º±0.2º, 5.2º±0.2º and 9.9º±0.2º. The present invention provides a new crystal form of the obeticholic acid. The crystal form has advantageous properties of being stable, exploitable in technology and treatable, and is suitable for being stored and used as a final product. In addition, the preparation method for the crystal form is simple and has low costs, and has important value in optimization and development of the medicine in the future.
C07J 9/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
A61K 31/575 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
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
73.
CRYSTAL FORM OF SALT OF EPIDERMAL GROWTH FACTOR RECEPTOR KINASE INHIBITOR AND PREPARATION METHOD THEREOF
Disclosed are a crystal form of a salt of an epidermal growth factor receptor kinase inhibitor and a preparation method thereof, and in particular, the crystal forms of a hydrobromide and a phosphate of a compound of formula (I).
The present invention relates to a salt of a pyrrolo[2,3-D]pyrimidine compound and a novel polymorph of the salt and specifically relates to a salt of a compound as represented by formula (I), a novel polymorph of the salt, and a preparation method. The salt of the compound as represent by formula (I) and the novel polymorph of the salt of the present invention have the advantageous properties of great stability, reduced hygroscopicity, process developability, and tractability, while the preparation method is simple and inexpensive, thus providing great value for future optimization and development of the medicament.
New salts and crystalline Forms of palbociclib, processes for their preparation, pharmaceutical compositions comprising the new salts or crystalline Forms, and use of the new salts and crystalline Forms of palbociclib for treating or delaying diseases or disorders related to activity of cyclin-dependent kinase (CDK) 4/6 are disclosed.
The present invention relates to crystal form I of ceritinib and preparation method therefor. The crystal form provided by the present invention has advantageous properties of good stability, lower hygroscopicity, technological exploitablity and tractability etc. The preparation method is simple and the cost is low. The crystal form has important value on the optimization and exploitation of the drug in the future.
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
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
The present invention relates to Lu AE58054 hydrochloride crystalline form A, and preparation method and application thereof, Lu AE58054 hydrochloride crystalline form A having a characteristic peak at a point where 2theta value is 17.1°±0.2°、17.8°±0.2°、21.4°±0.2° in an X-ray powder diffraction pattern (Cu-Kα radiation) under 25°C. Having a simple preparation process, a low cost, a good stability, a low moisture absorbance property, a high solubility, Crystalline form A is beneficial to absorption of drugs, and has a great significance in reducing drug load and preparing pharmaceutical formulation for curing Alzheimer disease.
C07D 209/14 - Radicals substituted by nitrogen atoms, not forming part of a nitro radical
A61K 31/4045 - Indole-alkylaminesAmides thereof, e.g. serotonin, melatonin
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
78.
CRYSTALLINE FORM IV OF TRISODIUM SUPRAMOLECULAR COMPLEX COMPRISING VALSARTAN AND AHU-377 AND METHODS THEREOF
A novel crystalline Form of trisodium [3-((1S,3R)-1-biphenyl-4-ylmethyl-3- ethoxycarbonyl-1-butylcarbamoyl)propionate-(S)-3'-methyl-2'-(pentanoyl{2''-(tetrazol-5- ylate)biphenyl-4'-ylmethyl}amino)butyrate] hydrate, process for its preparation, pharmaceutical composition comprising the new form, and use of it for treating or delaying progression or onset of diseases or disorders related to activity of angiotensin receptor 1 (AT1) blockage and neprilysin (NEP) inhibition is disclosed. The novel form was characterized by X-ray powder diffraction, differential scanning calorimetry, and other techniques.
A61K 31/41 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
79.
CRYSTALLINE FORMS OF TRISODIUM SUPRAMOLECULAR COMPLEX COMPRISING VALSARTAN AND AHU-377 AND METHODS THEREOF
Novel crystalline Forms of trisodium [3-((1S,3R)-l-biphenyl-4-ylmethyl-3-ethoxycarbonyl-1-butyl carbamoyl) propionate-(S)-3'-methyl-2'-(pentanoyl{2"-(tetrazol-5-ylate)biphenyl-4'-ylmethyl}amino)butyrate] hydrate, methods for their preparation, pharmaceutical compositions comprising these new forms, and use of them for treating or delaying progression or onset of diseases or disorders related to activity of angiotensin receptor 1 (AT1) blockage and neprilysin (NEP) inhibition, such as heart failure, are disclosed.
A61K 31/41 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
C07C 233/47 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton
80.
CRYSTALLINE FORMS OF TRISODIUM SUPRAMOLECULAR COMPLEX COMPRISING VALSARTAN AND AHU-377 AND METHODS THEREOF
Novel crystalline Forms of trisodium [3-((1S,3R)-l-biphenyl-4-ylmethyl-3-ethoxycarbonyl-1-butyl carbamoyl) propionate-(S)-3'-methyl-2'-(pentanoyl{2"-(tetrazol-5-ylate)biphenyl-4'-ylmethyl}amino)butyrate] hydrate, methods for their preparation, pharmaceutical compositions comprising these new forms, and use of them for treating or delaying progression or onset of diseases or disorders related to activity of angiotensin receptor 1 (AT1) blockage and neprilysin (NEP) inhibition, such as heart failure, are disclosed.
A61K 31/216 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acids having aromatic rings, e.g. benactizyne, clofibrate
A61K 31/41 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
C07C 233/47 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton
Novel salts and cocrystals of lesinurad, processes for their preparation, pharmaceutical compositions comprising these new salt forms and co-crystals, and use of them for treating or delaying progression or onset of diseases or disorders related to activity of uric acid transport 1 (URAT1) proteins are disclosed. These novel forms were characterized by X-ray powder diffraction, differential scanning calorimetry, and other techniques. They can be readily prepared and are suitable for preparation of solid dosage forms owing to their ease of handling and superior pharmacological properties.
Crystalline Form I of ibrutinib, processes for its preparation, pharmaceutical compositions comprising the new Form, and use of Form I of ibrutinib for treating or delaying diseases or disorders related to activity of Bruton's tyrosine kinase (BTK) proteins are disclosed. The novel Form was characterized by X-ray powder diffraction, differential scanning calorimetry, and other techniques. It can be readily prepared and is suitable for use in the preparation of solid dosage forms.
Novel crystalline forms of lesinurad and its sodium salt, processes for their preparation, pharmaceutical compositions comprising these new forms, and use of them for treating or delaying progression or onset of diseases or disorders related to activity of uric acid transporter 1 (URAT1) proteins are disclosed. These novel forms were characterized by X-ray powder diffraction, differential scanning calorimetry, and other techniques. They can be readily prepared and are suitable for preparation of solid dosage forms owing to their ease of handling and superior pharmacological properties.
Novel crystalline Forms B, C, and D of canagliflozin, processes for their preparation, pharmaceutical compositions comprising these new Forms, and use of them for treating or delaying progression or onset of diseases or disorders related to activity of sodium-glucose transport proteins are disclosed. These novel Forms were characterized by powder X-ray diffraction, differential scanning calorimetry, and other techniques. They can be readily prepared and are suitable for preparation of solid dosage forms owing to their ease of handling and superior pharmacological properties.
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
