Patent classifications
C07C309/04
SALT OF ARYLAMINOPURINE DERIVATIVE, PREPARATION METHOD THEREFOR AND USE THEREOF
Provided in the present invention are a salt of an arylaminopurine derivative represented by Formula (2), a preparation method therefor and the use thereof. The salt obtained in the present invention has good crystallinity and significantly improved solubility relative to that in the free form, and the preferred salt and crystal form have low hygroscopicity and can exist stably. Therefore, compared with the free form of arylaminopurine derivatives or other salts, it is easier to prepare same into a medicine.
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MITOCHONDRIAL DYSFUNCTION IMPROVING AGENT
The object of the present invention is to provide a mitochondrial dysfunction improving agent comprising a vitamin K derivative having a high deliverability to mitochondria.
A mitochondrial dysfunction improving agent, neurodegeneration improving agent, amyotrophic lateral sclerosis improving agent, Alzheimer's disease improving agent, and Parkinson's disease improving agent comprising at least one of a carboxylic acid ester of an active vitamin K represented by a general formula (1) or a salt thereof, and
##STR00001##
(wherein, R.sub.1 and R.sub.2 are a hydrogen atom, respectively, or a substituent selected from glycine, N-acyl glycine, N-alkyl glycine, N,N-dialkyl glycine, N,N,N-trialkyl glycine, acyl, dicarboxylic acid hemiester, and salts thereof; and at least either of R.sub.1 and R.sub.2 is glycine, N-acyl glycine, N-alkyl glycine, N,N-dialkyl glycine, N,N,N-trialkyl glycine, acyl, dicarboxylic acid hemiester, and salts thereof. R.sub.3 is a group represented by a general formula (2), or a general formula (3). n is an integer of 1 to 7)
##STR00002##
a mitochondrial dysfunction improving agent, neurodegeneration improving agent, amyotrophic lateral sclerosis improving agent, Alzheimer's disease improving agent, and Parkinson's disease improving agent comprising a carboxylic acid ester of an active vitamin K or a salt thereof (in the general formula (1), R.sub.1 and R.sub.2 is a carboxylic acid residue selected from a group consisting of R.sub.4OOCCH.sub.2CH.sub.2CO— and R.sub.4OOCCH.sub.2CH.sub.2CH.sub.2CO—. R.sub.3 represents the above general formula (2) or (3). R.sub.4 is a C1-C3 alkyl group.).
MITOCHONDRIAL DYSFUNCTION IMPROVING AGENT
The object of the present invention is to provide a mitochondrial dysfunction improving agent comprising a vitamin K derivative having a high deliverability to mitochondria.
A mitochondrial dysfunction improving agent, neurodegeneration improving agent, amyotrophic lateral sclerosis improving agent, Alzheimer's disease improving agent, and Parkinson's disease improving agent comprising at least one of a carboxylic acid ester of an active vitamin K represented by a general formula (1) or a salt thereof, and
##STR00001##
(wherein, R.sub.1 and R.sub.2 are a hydrogen atom, respectively, or a substituent selected from glycine, N-acyl glycine, N-alkyl glycine, N,N-dialkyl glycine, N,N,N-trialkyl glycine, acyl, dicarboxylic acid hemiester, and salts thereof; and at least either of R.sub.1 and R.sub.2 is glycine, N-acyl glycine, N-alkyl glycine, N,N-dialkyl glycine, N,N,N-trialkyl glycine, acyl, dicarboxylic acid hemiester, and salts thereof. R.sub.3 is a group represented by a general formula (2), or a general formula (3). n is an integer of 1 to 7)
##STR00002##
a mitochondrial dysfunction improving agent, neurodegeneration improving agent, amyotrophic lateral sclerosis improving agent, Alzheimer's disease improving agent, and Parkinson's disease improving agent comprising a carboxylic acid ester of an active vitamin K or a salt thereof (in the general formula (1), R.sub.1 and R.sub.2 is a carboxylic acid residue selected from a group consisting of R.sub.4OOCCH.sub.2CH.sub.2CO— and R.sub.4OOCCH.sub.2CH.sub.2CH.sub.2CO—. R.sub.3 represents the above general formula (2) or (3). R.sub.4 is a C1-C3 alkyl group.).
CYTISINE SALTS
Salts of cytisine have been prepared and incorporated in stable pharmaceutical compositions, including compositions comprising lactose. The salts are prepared by adding acid stock solutions to solutions of cytisine with heating, followed by cooling to ambient temperature. The salts and compositions are indicated in the treatment of nicotine addiction.
CYTISINE SALTS
Salts of cytisine have been prepared and incorporated in stable pharmaceutical compositions, including compositions comprising lactose. The salts are prepared by adding acid stock solutions to solutions of cytisine with heating, followed by cooling to ambient temperature. The salts and compositions are indicated in the treatment of nicotine addiction.
Pyrimidinone compounds as human neutrophil elastase inhibitors
Pyrimidone compounds defined herein exhibit human neutrophil elastase inhibitory properties and are useful for treating diseases and condition in which HNE is implicated.
Pyrimidinone compounds as human neutrophil elastase inhibitors
Pyrimidone compounds defined herein exhibit human neutrophil elastase inhibitory properties and are useful for treating diseases and condition in which HNE is implicated.
FORMS AND COMPOSITIONS OF INHIBITORS OF PLASMA KALLIKREIN
The present invention provides solid forms of compound (1) and compositions thereof which are useful as inhibitors of Plasma Kallikrein (pKal) and which exhibit desirable characteristics for the same.
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FORMS AND COMPOSITIONS OF INHIBITORS OF PLASMA KALLIKREIN
The present invention provides solid forms of compound (1) and compositions thereof which are useful as inhibitors of Plasma Kallikrein (pKal) and which exhibit desirable characteristics for the same.
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COMPOSITIONS FOR TREATING NEURODEGENERATIVE DISEASES
The present disclosure relates to novel compounds, pharmaceutical compositions containing the compounds and methods of using the compounds and pharmaceutical compositions for treating neurodegerative diseases, including Alzheimer's disease and cognitive decline. Methods for inhibiting synapse number decline or membrane trafficking abnormalities associated with exposure of a neuronal cell to Abeta species are also disclosed.