Abstract

The present invention relates to the use of a class of 1,4-dihydro-naphthyridine derivatives in the treatment of tumors.

IPC Classes  ?

• A61K 31/4745 - QuinolinesIsoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenanthrolines
• A61K 31/4188 - 1,3-Diazoles condensed with heterocyclic ring systems, e.g. biotin, sorbinil
• A61P 35/00 - Antineoplastic agents

Abstract

The present invention relates to a composition of (S)-3-aminomethyl-5-methylhexanoic acid or a pharmaceutically acceptable salt thereof, and riluzole. The composition has broad application prospects in the manufacture of a medicament for treating neuropathic pain.

IPC Classes  ?

• A61K 31/197 - Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
• A61K 31/428 - Thiazoles condensed with carbocyclic rings
• A61P 25/04 - Centrally acting analgesics, e.g. opioids

Abstract

A composition applied to preparation of a medicament for treating cerebrovascular diseases, in particular ischemic cerebrovascular diseases. The composition contains 2-amino-6-trifluoromethoxybenzothiazole or a pharmaceutically acceptable salt thereof and borneol. By means of the compatibility between 2-amino-6-trifluoromethoxybenzothiazole and d-borneol, according to non-clinical cell test and animal efficacy test results, for cerebrovascular diseases, 2-amino-6-trifluoromethoxybenzothiazole and d-borneol have the effect of synergistically increasing efficacy.

IPC Classes  ?

• A61K 31/428 - Thiazoles condensed with carbocyclic rings
• A61K 31/045 - Hydroxy compounds, e.g. alcoholsSalts thereof, e.g. alcoholates
• 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

Abstract

Disclosed is the use of a composition containing cilostazol or a pharmaceutically acceptable salt thereof and edaravone in the preparation of a drug for treating cerebrovascular diseases, especially ischemic cerebrovascular diseases. The experiment result shows that the tail vein administration of 1-15 mg/kg of cilostazol or 1.67-8.33 mg/kg of edaravone on rats with a focal cerebral ischemia-reperfusion injury can significantly ameliorate neurological defects in rats with an MCAO and reduce a cerebral infarction area; and performing compound combination within the dosage range (the mass ratio of cilostazol:edaravone is 1:5 to 5:1) can be synergistic. The tail vein administration of 3.33-16.67 mg/kg of cilostazol or 3.33-16.67 mg/kg of edaravone on mice with a focal cerebral ischemia-reperfusion injury can significantly ameliorate neurological defects in mice with an MCAO and reduce a cerebral infarction area.

IPC Classes  ?

• A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
• A61K 31/4152 - 1,2-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. antipyrine, phenylbutazone, sulfinpyrazone
• 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

Abstract

The present invention belongs to the pharmaceutical field, and relates to an application of a cilostazol and d-borneol composition in preparing a drug for treating cerebrovascular disease, in particular ischemic cerebrovascular disease. The present invention specifically relates to a composition containing cilostazol or a pharmaceutically acceptable salt thereof and d-borneol, and an application of the composition in preparing a drug for treating cerebrovascular disease, in particular ischemic cerebrovascular disease.

IPC Classes  ?

• A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
• A61K 31/045 - Hydroxy compounds, e.g. alcoholsSalts thereof, e.g. alcoholates
• 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

Abstract

The present invention relates to the use of a class of 1,4-dihydro-naphthyridine derivatives in the treatment of tumors.

IPC Classes  ?

• 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
• A61P 35/00 - Antineoplastic agents

Abstract

An application of a composition in improving or treating cognitive impairment. The composition contains 3-methyl-1-phenyl-2-pyrazolin-5-one or a pharmaceutically acceptable salt thereof and borneol or dexborneol. The cognitive impairment comprises Alzheimer's disease (AD), vascular dementia (VD), mild cognitive impairment (MCI), and other types of dementia.

IPC Classes  ?

• A61K 31/4152 - 1,2-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. antipyrine, phenylbutazone, sulfinpyrazone
• A61K 31/045 - Hydroxy compounds, e.g. alcoholsSalts thereof, e.g. alcoholates
• 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

Abstract

The present invention relates to a composition of (S)-3-aminomethyl-5-methylhexanoic acid or a pharmaceutically acceptable salt thereof, and riluzole. The composition has broad application prospects in the preparation of a drug for treating neuropathic pain.

IPC Classes  ?

• A61K 31/428 - Thiazoles condensed with carbocyclic rings
• A61K 31/197 - Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
• A61P 25/04 - Centrally acting analgesics, e.g. opioids

Abstract

A composition applied to preparation of a medicament for treating cerebrovascular diseases, in particular ischemic cerebrovascular diseases. The composition contains 2-amino-6-trifluoromethoxybenzothiazole or a pharmaceutically acceptable salt thereof and borneol. By means of the compatibility between 2-amino-6-trifluoromethoxybenzothiazole and d-borneol, according to non-clinical cell test and animal efficacy test results, for cerebrovascular diseases, 2-amino-6-trifluoromethoxybenzothiazole and d-borneol have the effect of synergistically increasing efficacy.

IPC Classes  ?

• A61K 31/428 - Thiazoles condensed with carbocyclic rings
• A61K 31/045 - Hydroxy compounds, e.g. alcoholsSalts thereof, e.g. alcoholates
• 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

Abstract

Disclosed is the use of a composition containing vinpocetine or a pharmaceutically acceptable salt thereof and edaravone in the preparation of a drug for treating cerebrovascular diseases, especially ischemic cerebrovascular diseases. The experiment result shows that the tail vein administration of 1-15 mg/kg of vinpocetine or 1.67-8.33 mg/kg of edaravone on rats with a focal cerebral ischemia-reperfusion injury can significantly ameliorate neurological defects in rats with an MCAO and reduce a cerebral infarction area; and performing compound combination within the dosage range (the mass ratio of vinpocetine : edaravone is 1 : 5 to 5 : 1) can be synergistic. The tail vein administration of 3.33-16.67 mg/kg of vinpocetine or 3.33-16.67 mg/kg of edaravone on mice with a focal cerebral ischemia-reperfusion injury can significantly ameliorate neurological defects in mice with an MCAO and reduce a cerebral infarction area.

IPC Classes  ?

• A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
• A61K 31/4152 - 1,2-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. antipyrine, phenylbutazone, sulfinpyrazone
• 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

Abstract

The present invention belongs to the pharmaceutical field, and relates to an application of a cilostazol and d-borneol composition in preparing a drug for treating cerebrovascular disease, in particular ischemic cerebrovascular disease. The present invention specifically relates to a composition containing cilostazol or a pharmaceutically acceptable salt thereof and d-borneol, and an application of the composition in preparing a drug for treating cerebrovascular disease, in particular ischemic cerebrovascular disease.

IPC Classes  ?

• A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
• A61K 31/045 - Hydroxy compounds, e.g. alcoholsSalts thereof, e.g. alcoholates
• 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

Abstract

A sublingual tablet pharmaceutical composition containing edaravone and (+)-2-borneol, and a preparation method thereof. The sublingual tablet pharmaceutical composition includes edaravone, (+)-2-camphanol, an excipient, a filler, a binder, a disintegrant, and a lubricant. The excipient is selected from one or more of mannitol, lactose, dextran, cysteine, glycine, copovidone, and beta-cyclodextrin.

IPC Classes  ?

• A61K 31/4152 - 1,2-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. antipyrine, phenylbutazone, sulfinpyrazone
• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61K 9/20 - Pills, lozenges or tablets
• A61K 47/26 - Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharidesDerivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
• A61K 47/32 - Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers
• A61K 31/045 - Hydroxy compounds, e.g. alcoholsSalts thereof, e.g. alcoholates

Abstract

Disclosed are 1,4-dihydro-naphthyridine derivatives and pharmaceutical composition and uses thereof. The 1,4-dihydro-naphthyridine derivatives are a compound capable of inhibiting acetylcholinesterase activity and preventing extracellular calcium from flowing into a cell via a calcium channel, i.e., having a dual-activity, which are of potential importance as a pharmaceutical and can be used to prepare the drugs for treating cardiovascular diseases, cerebrovascular diseases and dementia.

IPC Classes  ?

• C07D 495/14 - Ortho-condensed systems
• C07D 471/14 - Ortho-condensed systems
• C07D 471/04 - Ortho-condensed systems
• C07D 471/12 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups in which the condensed system contains three hetero rings
• C07D 491/14 - Ortho-condensed systems

Abstract

A N-benzylaniline derivative and uses thereof. The derivative is a compound represented by formula I or a pharmaceutically acceptable salt thereof. The compound protects against cerebral ischemia/reperfusion injury and has analgesic action for chronic pathologic pain, and may be used to treat cerebral apoplexy, neuropathic pain, and inflammatory pain. Moreover, because of the unique mechanism of action of the compound, the compound can be used to treat epilepsy, affective disorder, and neurodegenerative diseases.

IPC Classes  ?

• C07C 229/00 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton
• C07C 229/60 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton with amino and carboxyl groups bound to carbon atoms of the same non-condensed six-membered aromatic ring with amino and carboxyl groups bound in meta- or para- positions
• A61K 31/196 - Carboxylic acids, e.g. valproic acid having an amino group the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
• A61K 31/245 - Amino benzoic acid types, e.g. procaine, novocaine
• C07C 233/54 - 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 a carbon atom of a six-membered aromatic ring having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of a saturated carbon skeleton
• C07C 229/54 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton with amino and carboxyl groups bound to carbon atoms of the same non-condensed six-membered aromatic ring

Abstract

A sublingual tablet pharmaceutical composition containing edaravone and (+)-2-borneol, and a preparation method thereof. The sublingual tablet pharmaceutical composition includes edaravone, (+)-2-camphanol, an excipient, a filler, a binder, a disintegrant, and a lubricant. The excipient is selected from one or more of mannitol, lactose, dextran, cysteine, glycine, copovidone, and beta-cyclodextrin.

IPC Classes  ?

• A61K 9/20 - Pills, lozenges or tablets
• A61K 31/045 - Hydroxy compounds, e.g. alcoholsSalts thereof, e.g. alcoholates
• A61K 31/4152 - 1,2-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. antipyrine, phenylbutazone, sulfinpyrazone
• A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof
• A61K 47/26 - Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharidesDerivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
• A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
• A61K 47/40 - CyclodextrinsDerivatives thereof
• 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

Abstract

The present invention belongs to the pharmaceutical field, and relates to an application of a cilostazol and d-borneol composition in preparing a drug for treating cerebrovascular disease, in particular ischemic cerebrovascular disease. The present invention specifically relates to a composition containing cilostazol or a pharmaceutically acceptable salt thereof and d-borneol, and an application of the composition in preparing a drug for treating cerebrovascular disease, in particular ischemic cerebrovascular disease.

IPC Classes  ?

• A61K 31/045 - Hydroxy compounds, e.g. alcoholsSalts thereof, e.g. alcoholates
• A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
• A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Abstract

The present invention relates to a composition of (S)-3-aminomethyl-5-
methylhexanoic acid
or a pharmaceutically acceptable salt thereof, and riluzole. The composition
has broad application
prospects in the manufacture of a medicament for treating neuropathic pain.

IPC Classes  ?

• A61K 31/197 - Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
• A61K 31/428 - Thiazoles condensed with carbocyclic rings
• A61P 25/04 - Centrally acting analgesics, e.g. opioids

Abstract

An application of a composition in improving or treating cognitive impairment. The composition contains 3-methyl-1-phenyl-2-pyrazolin-5-one or a pharmaceutically acceptable salt thereof and borneol or dexborneol. The cognitive impairment comprises Alzheimer's disease (AD), vascular dementia (VD), mild cognitive impairment (MCI), and other types of dementia.

IPC Classes  ?

• A61K 31/045 - Hydroxy compounds, e.g. alcoholsSalts thereof, e.g. alcoholates
• A61K 31/4152 - 1,2-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. antipyrine, phenylbutazone, sulfinpyrazone
• 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

Abstract

The present invention relates to the use of a class of 1,4-dihydro-naphthyridine derivatives in the treatment of tumors.

IPC Classes  ?

• 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