A new route for preparing an oxopyridine compound as represented by formula (I) and a key intermediate thereof. The new route can greatly reduce the generation of isomer impurities, improve the selectivity of the reaction chirality and the selectivity of N/O-alkylation, increase the yield, avoid re-purification of a crude product, and reduce the cost, has a short production period, and is energy-saving and environmentally-friendly, and suitable for preparing a drug for treating and/or preventing diseases related to FXIa receptors, and particularly provides a new idea for preparing a drug for treating and/or preventing cerebrovascular artery diseases and/or peripheral artery diseases.
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
C07C 303/28 - Preparation of esters or amides of sulfuric acidsPreparation of sulfonic acids or of their esters, halides, anhydrides or amides of esters of sulfonic acids by reaction of hydroxy compounds with sulfonic acids or derivatives thereof
C07C 309/73 - Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton to carbon atoms of non-condensed six-membered aromatic rings
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
Disclosed are a dihydropyrimidine based compound, a preparation method therefor and an application thereof, belonging to the technical field of pharmaceutical chemistry. The present disclosure relates to a dihydropyrimidine based compound, the structure of which is shown in formula I. Also provided in the present disclosure is an application of the compound represented by formula I, or a salt, solvate, isomer, metabolite, nitrogen oxide and prodrug thereof, in the preparation of a medicament for treating or preventing P2X3 and/or P2X2/3 receptor-related diseases. The dihydropyrimidine based compound of the present disclosure has good P2X3 receptor antagonist activity and improved safety.
Disclosed are a dihydropyrimidine based compound, a preparation method therefor and an application thereof, belonging to the technical field of pharmaceutical chemistry. The present disclosure relates to a dihydropyrimidine based compound, the structure of which is shown in formula I. Also provided in the present disclosure is an application of the compound represented by formula I, or a salt, solvate, isomer, metabolite, nitrogen oxide and prodrug thereof, in the preparation of a medicament for treating or preventing P2X3 and/or P2X2/3 receptor-related diseases. The dihydropyrimidine based compound of the present disclosure has good P2X3 receptor antagonist activity and improved safety.
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
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
C07D 239/545 - Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other 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
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
3.
NOVEL 2-(1-HYDROXYPENTYL) BENZOIC ACID CYCLOALKYL AMINE SALT
A 2-(1-hydroxypentyl) benzoic acid cycloalkyl amine salt having a structure as represented by formula I, a preparation method therefor, a pharmaceutical composition having the compound as an active ingredient, and an application of the compound in the treatment and/or prevention of ischemic heart and cerebrovascular diseases, especially mild, moderate, and severe acute ischemic stroke, etc.
C07C 65/01 - Compounds having carboxyl groups bound to carbon atoms of six-membered aromatic rings and containing any of the groups OH, O-metal, —CHO, keto, ether, groups, groups, or groups containing hydroxy or O-metal groups
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 211/38 - Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of rings other than six-membered aromatic rings of a saturated carbon skeleton containing condensed ring systems
C07C 209/00 - Preparation of compounds containing amino groups bound to a carbon skeleton
A61P 9/00 - Drugs for disorders of the cardiovascular system
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
A61K 31/205 - Amine addition salts of organic acidsInner quaternary ammonium salts, e.g. betaine, carnitine
4.
SULFONAMIDES, METHOD FOR PREPARATION THEREOF, AND USE THEREOF
The present disclosure discloses sulfonamides, methods for preparation thereof and uses thereof, belonging to the technical field of medicinal chemistry. The structure of the sulfonamides of the present disclosure is shown in Formula I. The present disclosure also provides use of the compound of Formula I or a salt, solvate, isomer, metabolite, nitrogen-oxide, or prodrug thereof in the manufacture of a medicament for the treatment or prevention of P2X3 and/or P2X2/3 receptor-associated diseases. The sulfonamides of the present disclosure have a potent cough suppressing effect and a significantly prolonged action. Their inhibitory activity against P2X3 is superior to that of Comparative compound 1 and the positive control Gefapixant.
The present disclosure discloses sulfonamides, methods for preparation thereof and uses thereof, belonging to the technical field of medicinal chemistry. The structure of the sulfonamides of the present disclosure is shown in Formula I. The present disclosure also provides use of the compound of Formula I or a salt, solvate, isomer, metabolite, nitrogen-oxide, or prodrug thereof in the manufacture of a medicament for the treatment or prevention of P2X3 and/or P2X2/3 receptor-associated diseases. The sulfonamides of the present disclosure have a potent cough suppressing effect and a significantly prolonged action. Their inhibitory activity against P2X3 is superior to that of Comparative compound 1 and the positive control Gefapixant.
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 31/53 - 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
C07D 251/26 - Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with only hetero atoms directly attached to ring carbon atoms
5.
CRYSTAL FORM AND AMORPHOUS FORM OF CAREBASTINE P-TOLUENESULFONATE
Provided are a crystal form and amorphous form of carebastine p-toluenesulfonate, and a preparation method therefor, relating to the field of medicinal chemistry, for use in solving the problems in the prior art that carebastine is unstable, not easy to scale up for synthesis, and difficult to make into a drug and the like. The crystal form and amorphous form of carebastine p-toluenesulfonate have the characteristics of high purity, high stability, high bioavailability, easy scale-up synthesis, and industrial production and the like, and have excellent hygroscopicity for easy storage.
Disclosed in the present invention are a compound as represented by formula (I), a stereoisomer or pharmaceutically acceptable salt thereof, and a key intermediate thereof. The present invention also provides a use of the compound, and the stereoisomer or pharmaceutically acceptable salt thereof in preparation of drugs for treating and/or preventing FXIa receptor-related diseases, especially a use in preparation of drugs for treating and/or preventing cerebrovascular arterial diseases and/or peripheral arterial diseases.
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 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
A61P 9/00 - Drugs for disorders of the cardiovascular system
The present invention provides a solid preparation containing (7aS,2'S)-2-oxo-clopidogrel and a preparation method therefor. The solid preparation is an oral tablet containing (7aS,2'S)-2-oxo-clopidogrel and pharmaceutically acceptable excipients, the excipients comprising a filler, a disintegrant, a binder, and a lubricant.
A61K 31/4365 - 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 having sulfur as a ring hetero atom, e.g. ticlopidine
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
A61P 9/00 - Drugs for disorders of the cardiovascular system
Provided are an anti-platelet aggregation medicament and use thereof. The medicament is a compound having a structure of formula I, or a pharmaceutically acceptable salt thereof, a solvate thereof, or a deuterated substance thereof. The compound has a remarkable anti-platelet aggregation effect, relatively suitable water solubility and good stability, and thus is expected to become a new type of injectable anti-platelet aggregation medicament.
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/4365 - 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 having sulfur as a ring hetero atom, e.g. ticlopidine
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
9.
PHARMACEUTICAL COMPOSITION FOR TREATING AND RESISTING BLOOD COAGULATION AND USE THEREOF
max(0-t)(0-∞)(0-∞) of a metabolically produced compound A and an active metabolite H4, thereby ensuring the effectiveness and safety of usage of medication.
A61K 31/4365 - 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 having sulfur as a ring hetero atom, e.g. ticlopidine
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 25/00 - Drugs for disorders of the nervous system
The present invention relates to the field of pharmaceutical chemistry, and in particular, to a carebastine salt and use thereof. The present invention solves the problems of solid carebastine in the prior art such as poor form, excessive impurities, instability, difficulties in purification, scale-up and synthesis, and low druggability. The carebastine salt of the present invention includes, but is not limited to, an acid addition salt or a base addition salt, and particularly includes a potassium salt, a sodium salt, a methanesulfonate, and a p-toluenesulfonate. The carebastine salt of the present invention possesses use in preparing a medicament as a histamine H1 receptor antagonist. The carebastine salt of the present invention has characteristics such as ease of purification, high stability, simple process, ease of industrial production and the like, and has good hygroscopicity and convenience in storage. Also, the salt of the present invention can quickly enter a body to exert its efficacy, features good oral absorption performance and superior safety and individual difference to ebastine, and is a very promising antiallergic.
Disclosed are a dihydropyrimidine compound, a preparation method therefor and an application thereof, belonging to the technical field of pharmaceutical chemistry. The present invention relates to a dihydropyrimidine compound, the structure of which is shown in formula I. Also provided in the present invention is an application of the compound represented by formula I, or a salt, solvate, isomer, metabolite, nitrogen oxide and prodrug thereof, in the preparation of a medicament for treating or preventing P2X3 and/or P2X2/3 receptor-related diseases. The dihydropyrimidine compound of the present invention has good P2X3 receptor antagonist activity and better safety.
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 239/545 - Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other 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
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 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
C07D 413/12 - 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 linked by a chain containing hetero atoms as chain links
A61P 11/00 - Drugs for disorders of the respiratory system
Disclosed are a sulfonamide compound, a preparation method therefor and a use thereof, belonging to the technical field of pharmaceutical chemistry. The structure of the sulfonamide compound of the present invention is as shown in formula I. Also provided in the present invention also are applications of the compound represented by formula I or a salt, a solvate, an isomer, a metabolite, a nitrogen oxide, and a prodrug thereof in the preparation of a medicament for the treatment or prevention of P2X3 and/or P2X2/3 receptor-related diseases. The sulfonamide compound of the present invention has a strong antitussive effect and can significantly prolong drug effect duration, and P2X3 inhibitory activity thereof is better than that of the compound of Comparative Example 1 and a positive control drug gefapixant.
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 31/53 - 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 is a method for treating a blood plasma sample containing (7aS,2'S)-2-oxo-clopidogrel, and a measurement method, which belong to the technical field of pharmaceutical analysis, and solve the problem in the prior art whereby there is not yet a method for measuring the concentration of (7aS,2'S)-2-oxo-clopidogrel in blood plasma. The method for treating a blood plasma sample containing (7aS,2'S)-2-oxo-clopidogrel comprises: taking whole blood containing (7aS,2'S)-2-oxo-clopidogrel, adding a reducing agent solution to same, and collecting blood plasma to obtain a blood plasma sample. The method for measuring (7aS,2'S)-2-oxo-clopidogrel in blood plasma involves treating, by using the treatment method, a sample to be measured, and comprises the following steps: S1, treatment of whole blood, involving: taking whole blood, adding a reducing agent solution to same, centrifuging same, and collecting blood plasma; S2, pretreatment of a blood plasma sample, involving: adding a protein precipitant and an internal standard working solution to the blood plasma, swirling and then centrifuging same, and taking the supernatant; and S3, measurement using LC/MS/MS. The method of the present invention is simple, easy to operate, has good stability, specificity and sensitivity, and provides accurate measurement results.
The present invention belongs to the technical field of medicinal chemistry, and disclosed are a trans-amantadine derivative or a salt thereof, and a preparation method therefor, a composition thereof and the use thereof. Provided in the present invention is a trans-amantadine derivative having a structure as represented by formula I or a pharmaceutically acceptable salt thereof. The preparation method of the present invention comprises a two-step reaction: step 1, performing a condensation reaction by means of taking a compound as shown in formula III, a compound as shown in formula IV or a salt thereof as a starting raw material to prepare a compound as shown in formula II; and step 2, performing a reduction reaction on the compound of formula II and a reducing agent to obtain the trans-amantadine derivative as represented by formula I. The trans-amantadine derivative of the present invention has better drug efficacy in treating lung injury and coughing relative to ambroxol hydrochloride, and can be used for the preparation of a drug for treating lung injury and coughing, especially for the preparation of a drug for treating acute lung injury and refractory cough.
C07C 211/52 - Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton having amino groups bound to only one six-membered aromatic ring the carbon skeleton being further substituted by halogen atoms or by nitro or nitroso groups
C07C 215/44 - Compounds containing amino and hydroxy groups bound to the same carbon skeleton having amino groups or hydroxy groups bound to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton bound to carbon atoms of the same ring or condensed ring system
C07C 249/02 - Preparation of compounds containing nitrogen atoms doubly-bound to a carbon skeleton of compounds containing imino groups
C07C 251/24 - Compounds containing nitrogen atoms doubly- bound to a carbon skeleton containing imino groups having carbon atoms of imino groups bound to carbon atoms of six-membered aromatic rings
C07C 209/52 - Preparation of compounds containing amino groups bound to a carbon skeleton by reduction of carboxylic acids or esters thereof in presence of ammonia or amines, or by reduction of nitriles, carboxylic acid amides, imines or imino-ethers by reduction of imines or imino-ethers
C07C 213/02 - Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton by reactions involving the formation of amino groups from compounds containing hydroxy groups or etherified or esterified hydroxy groups
A61K 31/137 - Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine
The present invention relates to the technical field of pharmaceutical chemistry. Disclosed is a use of a trans amantadine derivative having a structure as represented by formula I or a pharmaceutically acceptable salt thereof in the preparation of drugs for preventing or/and treating respiratory diseases. The trans amantadine derivative of the present invention and the salt thereof have better efficacy with respect to ambroxol hydrochloride and an amantadine hydrochloride derivative mixture (an isomer mixture). By means of an acute lung injury test in a mouse and a mouse cough model induced by ammonia, it is shown that the drug has an excellent effect of treating lung injury and cough, the effect is better than that of ambroxol hydrochloride and the amantadine hydrochloride derivative mixture, and drug has statistical significance. Compared with ambroxol hydrochloride, the trans adamantane derivative and hydrochloride thereof can significantly increase the sputum excretion of a rat, and can significantly increase the phenolsulfonphthalein excretion of the mouse, and the effects are better than those of ambroxol hydrochloride and the amantadine hydrochloride derivative mixture.
C07C 211/52 - Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton having amino groups bound to only one six-membered aromatic ring the carbon skeleton being further substituted by halogen atoms or by nitro or nitroso groups
C07C 215/44 - Compounds containing amino and hydroxy groups bound to the same carbon skeleton having amino groups or hydroxy groups bound to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton bound to carbon atoms of the same ring or condensed ring system
C07C 249/02 - Preparation of compounds containing nitrogen atoms doubly-bound to a carbon skeleton of compounds containing imino groups
C07C 251/24 - Compounds containing nitrogen atoms doubly- bound to a carbon skeleton containing imino groups having carbon atoms of imino groups bound to carbon atoms of six-membered aromatic rings
C07C 209/52 - Preparation of compounds containing amino groups bound to a carbon skeleton by reduction of carboxylic acids or esters thereof in presence of ammonia or amines, or by reduction of nitriles, carboxylic acid amides, imines or imino-ethers by reduction of imines or imino-ethers
C07C 213/02 - Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton by reactions involving the formation of amino groups from compounds containing hydroxy groups or etherified or esterified hydroxy groups
A61K 31/137 - Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine
A61P 11/00 - Drugs for disorders of the respiratory system
Disclosed in the present invention are a crystalline form B of a tetrahydrothienopyridine compound having a structure as represented by Compound I, a preparation method, a composition and an application thereof, for use in solving the problems in the prior art of lots of impurities, low content, bad crystalline form stability, and inability to form a drug. The crystalline form B uses Cu-Kα radiation, and X-ray powder diffraction expressed at a 2θ angle has characteristic peaks at 11.21±0.2°, 12.61±0.2°, 14.69±0.2°, 16.14±0.2°, 17.81±0.2°, 20.22±0.2°, and 22.10±0.2°. The crystalline form B of the present invention has few of impurities, good stability, good crystallinity, and reproducibility, and is suitable for industrial production. Moreover, the crystalline form B has an unexpectedly stronger anti-ADP-induced platelet aggregation effect and better fluidity.
Disclosed in the present invention are a crystalline form B of a tetrahydrothienopyridine compound having a structure as represented by Compound I, a preparation method, a composition and an application thereof, for use in solving the problems in the prior art of lots of impurities, low content, bad crystalline form stability, and inability to form a drug. The crystalline form B uses Cu-Kα radiation, and X-ray powder diffraction expressed at a 2θ angle has characteristic peaks at 11.21±0.2°, 12.61±0.2°, 14.69±0.2°, 16.14±0.2°, 17.81±0.2°, 20.22±0.2°, and 22.10±0.2°. The crystalline form B of the present invention has few of impurities, good stability, good crystallinity, and reproducibility, and is suitable for industrial production. Moreover, the crystalline form B has an unexpectedly stronger anti-ADP-induced platelet aggregation effect and better fluidity.
A dibromobenzyl derivative with a structure shown as formula I, a stereoisomer or a pharmaceutically acceptable salt thereof and a preparation method and an application of the dibromobenzyl derivative are provided. The dibromobenzyl derivative or the stereoisomer thereof is superior in in-vivo pharmacokinetic stability and drug efficacy, and capable of being used for preparing respiratory drugs, in particular the apophlegmatic drugs.
C07C 215/44 - Compounds containing amino and hydroxy groups bound to the same carbon skeleton having amino groups or hydroxy groups bound to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton bound to carbon atoms of the same ring or condensed ring system
A61K 31/137 - Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine
C07C 209/52 - Preparation of compounds containing amino groups bound to a carbon skeleton by reduction of carboxylic acids or esters thereof in presence of ammonia or amines, or by reduction of nitriles, carboxylic acid amides, imines or imino-ethers by reduction of imines or imino-ethers
C07C 213/02 - Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton by reactions involving the formation of amino groups from compounds containing hydroxy groups or etherified or esterified hydroxy groups
C07C 249/02 - Preparation of compounds containing nitrogen atoms doubly-bound to a carbon skeleton of compounds containing imino groups
18.
DIBROMOBENZYL DERIVATIVE, STEREOISOMER OR SALT THEREOF, AND PREPARATION METHOD THEREFOR AND USE THEREOF
Disclosed is a dibromobenzyl derivative having a structure represented by formula I, a stereoisomer or a pharmaceutically acceptable salt thereof, and the preparation method therefor and use thereof. The dibromobenzyl derivative and the stereoisomer of same of the present invention possess improved pharmacokinetic stability in vivo and improved drug efficacy, can be used for drugs for treating the respiratory system, particularly for preparing expectorants.
C07C 211/52 - Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton having amino groups bound to only one six-membered aromatic ring the carbon skeleton being further substituted by halogen atoms or by nitro or nitroso groups
A61K 31/137 - Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine
Disclosed in the present invention are a B crystal form of a tetrahydrothienopyridine compound having a structure as represented by formula I, a preparation method therefor, a composition and an application, for use in solving the problems in the prior art of lots of impurities, low content, bad crystal form stability, and inability to form a drug. The B crystal form uses Cu-Kα radiation, and X-ray powder diffraction expressed at a 2θ angle has characteristic peaks at 11.21±0.2°, 12.61±0.2°, 14.69±0.2°, 16.14±0.2°, 17.81±0.2°, 20.22±0.2°, and 22.10±0.2°. The B crystal form of the present invention has few of impurities, good stability, good crystallinity, and reproducibility, and is suitable for industrial production; moreover, the B crystal form has an unexpectedly stronger anti-ADP-induced platelet aggregation effect and better fluidity.
A61K 31/4365 - 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 having sulfur as a ring hetero atom, e.g. ticlopidine
patents
