摘要:
The present invention relates to: micellar aqueous compositions formed by chitosan derivatives in which carboxy-C 1-5 alkyl groups have been introduced as the hydrophilic groups and alkyl groups of 9 to 21 carbon atoms or aliphatic acyl groups of 9 to 21 carbon atoms have been introduced as the hydrophobic groups, and hydrophobic drugs; and a method of solubilizing hydrophobic drugs by adding the chitosan derivatives and hydrophobic drugs into an aqueous solvent to form micellar aqueous compositions. According to the present invention, drugs that could not be used for injection due to their insolubility in water can be formulated into injections, and also the effect of promoting absorptivity of drugs that were poorly absorbed orally etc. due to its poor solubility can be expected.
摘要:
The present invention provides an amino compound represented by Formula: wherein X is CH 2 NH or CONH, Y is CH 2 NH or CONH with the proviso that X and Y are not CONH at the same time; Z is CH=C(R 4 )R 5 , CH 2 CH(R 4 )R 5 or an alkoxycarbonyl group, R 1 is a hydrogen atom; a lower alkyl group, a cycloalkyl group, a cycloalkyl-substituted alkyl group, an aralkyl group or an aryl group, each group of which is substituted or unsubstituted, R 2 and R 3 are each independently a lower alkyl group or an aralkyl group, each group of which is substituted or unsubstituted, and R 4 and R 5 are each independently a hydrogen atom; an alkyl group, an aralkyl group, an aryl group or a heteroaryl group, each group of which is substituted or unsubstituted, or a pharmaceutically acceptable salt thereof; a medicine comprising the amino compound of Formula (1) or a pharmaceutically acceptable salt; and an angiotensin IV receptor agonist containing the same as an effective component, which are useful, in particular, as a therapeutical drug (antagonist or agonist) for various diseases in which angiotensin IV participates, for example, acceleration of renal blood flow, cerebral vasodilation, inhibition of cell proliferation and hypermnesia.
摘要:
The present invention relates to a thiazole derivative represented by formula (I) wherein Ar 1 represents a substituted or unsubstituted phenyl or thienyl group, Y 1 and Y 2 are different and each represents a nitrogen atom or a sulfur atom, R 1 represents a hydrogen atom, a C 1 to C 5 alkyl group, a phenyl group, or an amino group unsubstituted or mono- or di-substituted with a C 1 to C 5 alkyl group, and R 2 represents a substituted or unsubstituted nitrogen heterocycle group, or a pharmaceutically acceptable salt thereof. The compound of the present invention are a dopamine D 4 receptor antagonist which has an antipsychotic effect without causing any extrapyramidal disorder.
摘要:
A pyridine derivative represented by the following formula: , where R 1 is a methyl group or a functional group represented by any one of the following formulae:
―CONHCH 2 CH 2 N(CH 3 ) 2
―CONHCH 2 CH 2 CH 2 N(CH 3 ) 2
―COOCH 2 CH 2 N(CH 3 ) 2
―COOCH 2 CH 2 N(CH 2 CH 3 ) 2
―NHCOCH 2 N(CH 3 ) 2
―NHCOCH 2 N(CH 2 CH 3 ) 2
and R 2 is a hydrogen atom, an amino group or a functional group represented by any one of the following formulae:
―CONHCH 2 CH 2 N(CH 3 ) 2
―COOCH 2 CH 2 N(CH 3 ) 2
―NHCOCH 2 N(CH 3 ) 2
―NHCOCH 2 N(CH 2 CH 3 ) 2
or a salt thereof directly or indirectly acts on neuronal cells in vivo and is expected to show an effect on amelioration and curing of nerve disorders due to neuronal degeneration, with application as a drug for ameliorating and curing, for example, traumatic symptoms and maladies, those induced by drugs such as alcohol, antineoplastic agents, etc., inflammatory ones, metabolic ones as observed in diabetes, etc., and furthermore those due to idiopathic degeneration of peripheral nerves, and also with application as drugs for ameliorating and curing symptoms and maladies due to degeneration of central nerves, for example, Alzheimer's disease and cerebrovascular ischemia, Down syndrome, Parkinson's disease, Huntington chorea, diseases secondary to cerebral ischemia, cerebral infarction, intracerebral bleeding, head injuries, etc., amnesia, spinal neuropathy, etc.
摘要:
Endo-(8-methyl-8-azabicyclo[3.2.1]oct-3-yl) 1-isopropyl-2(1H)-quinolone-3-carboxylate represented by Formula (I): or an acid addition salt thereof acts on a serotonin 4 receptor thereby to have a serotonin-like receptor stimulating activity, therefore has an action on activating gastrointestinal motor functions and thus is effective for the improvement of gastrointestinal conditions such as heartburn, anorexia, bowel pain or abdominal distension accompanied by chronic gastritis or postoperative gastroparesis, and further for the treatment of gastro-esophagal reflux, intestinal pseudo-obstruction or constipation.
摘要:
Epoxysuccinamic acid derivative represented by general formula (I), which is useful for treating myolysis, pharmaceutically acceptable salt thereof, and intermediate therefor, wherein R1 represents C¿1? to C10 alkyl, phenyl or benzyl.
摘要:
A 5-amino-2-phenoxysulfonanilide compound represented by formula (I) and a salt thereof, having excellent anti-inflammatory, antipyretic, analgesic and antirheumatic effects, thus being useful as anti-inflammatory, antipyretic, analgesic and antirheumatic agents.
摘要:
OBJECT: To provide compounds having an excellent inhibitory action of blood platelet aggregation and a good stability when formulated. CONSTITUTION: A thiazoline derivative represented by the formula: wherein R 1 is an alkyl group having 1 to 4 carbon atoms and R 2 is a hydrogen atom or an alkyl group having 1 to 4 carbon atoms, or a pharmaceutically acceptable salt thereof.
摘要:
A terpyridine derivative represented by general formula (I) (wherein R represents hydrogen, (un)substituted phenyl, pyridyl, etc.), which has the effect of promoting the production of nerve growth factors or a neurotrophic factor activity. Hence it can be used as an ameliorant or remedy for the symptoms and diseases accompanying peripheral nerve degeneration which is idiopathic or caused by trauma, chemicals such as alcohol or anticancer drug, inflammation, or metabolism as observed in, for example, diabetes. In addition, it can be used as an ameliorant or remedy for the symptoms and diseases accompanying central nerve degeneration, such as senile dementia of Alzheimer type, cerebrovascular dementia, Down's syndrome, Parkinson's disease or Hantington's chorea, mental and motor function incompetences caused by cerebral ischemia, cerebral infarction, cerebral hemorrhage or head injury, spinal neuroparalysis, and so forth.
摘要:
An N-t-butylaniline analog represented by general formula (I) or a salt thereof, and a lipid level depressant containing the same as the active ingredient. In said formula, R¹ and R², which may be the same or different from each other, represent each hydrogen, halogen, amino, nitro, acetamide, lower alkyl, lower alkoxy, halogenated lower alkyl, halogenated lower alkoxy or lower alkanoyl; R³ represents hydrogen, halogen, lower alkoxy or halogenated lower alkyl; and Z represents S, SO or SO₂. This compound has a remarkably excellent effect of depressing the lipid level as compared with clofibrate and 4-(N-t-butyl)methanesulfonylaminodiphenyl ether and is extremely reduced in toxicity.
摘要翻译:由通式(I)表示的N-叔丁基苯胺类似物或其盐,以及含有与活性成分相同的脂质降低剂。 在所述式中,R 1和R 2可以彼此相同或不同,表示氢,卤素,氨基,硝基,乙酰胺,低级烷基,低级烷氧基,卤代低级烷基,卤代低级烷氧基 或低级烷酰基; R 3表示氢,卤素,低级烷氧基或卤代低级烷基; Z表示S,SO或SO 2。 与氯贝特和4-(N-叔丁基)甲磺酰氨基二苯醚相比,该化合物具有显着优异的抑制脂质水平的作用,毒性极度降低。