Patent classifications
C07D295/096
COMPOUND FOR TREATING ALZHEIMERS DISEASE
Provided in the present invention are a compound as shown in formula I, various crystal forms thereof, a hydrate, a solvate or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition. The compound of the present invention can effectively treat Alzheimer's disease or Down's syndrome, especially cognitive function impairment caused by Alzheimer's disease or Down's syndrome. Also disclosed in the present invention is use of a ubiquitin specific protease USP25 encoded and expressed by chromosome 21 for preventing, treating or ameliorating Alzheimer's disease or Down's syndrome.
##STR00001##
COMPOUND FOR TREATING ALZHEIMERS DISEASE
Provided in the present invention are a compound as shown in formula I, various crystal forms thereof, a hydrate, a solvate or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition. The compound of the present invention can effectively treat Alzheimer's disease or Down's syndrome, especially cognitive function impairment caused by Alzheimer's disease or Down's syndrome. Also disclosed in the present invention is use of a ubiquitin specific protease USP25 encoded and expressed by chromosome 21 for preventing, treating or ameliorating Alzheimer's disease or Down's syndrome.
##STR00001##
NON-ATP/CATALYTIC SITE P38 MITOGEN ACTIVATED PROTEIN KINASE INHIBITORS
Compounds that inhibit p38a MAPK protein, and methods of using the same, are provided for treating or preventing diseases such as cancer or inflammatory diseases.
GLP-1 receptor agonist and use thereof
- Hong Chul Yoon ,
- Kyung Mi An ,
- myong Jae Lee ,
- Jin Hee Lee ,
- Jeong-Geun Kim ,
- A-rang Im ,
- Woo Jin Jeon ,
- Jin Ah Jeong ,
- Jaeho Heo ,
- Changhee Hong ,
- Kyeojin Kim ,
- Jung-Eun Park ,
- Te-ik Sohn ,
- Changmok Oh ,
- Da Hae Hong ,
- Sung Wook Kwon ,
- Jung Ho Kim ,
- Jae Eui Shin ,
- Yeongran Yoo ,
- Min Whan Chang ,
- Eun Hye Jang ,
- In-gyu Je ,
- Ji Hye Choi ,
- Gunhee Kim ,
- Yearin Jun
Disclosed are novel compounds of Chemical Formula 1, optical isomers of the compounds, and pharmaceutically acceptable salts of the compounds or the optical isomers. The compounds, isomers, and salts exhibit excellent activity as GLP-1 receptor agonists. In particular, they, as GLP-1 receptor agonists, exhibit excellent glucose tolerance, thus having a great potential to be used as therapeutic agents for metabolic diseases. Moreover, they exhibit excellent pharmacological safety for cardiovascular systems.
Complexes
The present invention provides a palladium(II) complex of formula (1). ##STR00001## R.sub.12, m, and X are described in the specification. The invention also provides a process for the preparation of the complex, and its use in carbon-carbon and carbon-heteroatom coupling reactions.
Complexes
The present invention provides a palladium(II) complex of formula (1). ##STR00001## R.sub.12, m, and X are described in the specification. The invention also provides a process for the preparation of the complex, and its use in carbon-carbon and carbon-heteroatom coupling reactions.
1-[2-(2,4-DIMETHYLPHENYLSULFANYL)-PHENYL]PIPERAZINE AS A COMPOUND With COMBINED SEROTONIN REUPTAKE, 5-HT3 AND 5-HT1A ACTIVITY FOR THE TREATMENT OF COGNITIVE IMPAIRMENT
1-[2-(2,4-dimethylphenylsulphanyl)phenyl)]piperazine exhibits potent activity on SERT, 5-HT.sub.3 and 5-HT.sub.1A and may as such be useful for the treatment of cognitive impairment, especially in depressed patients.
1-[2-(2,4-DIMETHYLPHENYLSULFANYL)-PHENYL]PIPERAZINE AS A COMPOUND With COMBINED SEROTONIN REUPTAKE, 5-HT3 AND 5-HT1A ACTIVITY FOR THE TREATMENT OF COGNITIVE IMPAIRMENT
1-[2-(2,4-dimethylphenylsulphanyl)phenyl)]piperazine exhibits potent activity on SERT, 5-HT.sub.3 and 5-HT.sub.1A and may as such be useful for the treatment of cognitive impairment, especially in depressed patients.
Aromatic amino acid derivative and positron emission topography (PET) probe using the same
A compound having a structure represented by the general formula (I): ##STR00001##
(wherein n is 0 or 1;
R.sup.1 represents a hydrogen atom (only if n=0), a halogen atom, a C1-C6 alkyl group, a C1-C6 haloalkyl group, an optionally substituted amino group, an optionally substituted phenyl group, a C1-C6 alkylthio group, a C1-C6 alkoxy group, a C1-C6 haloalkoxy group or a C7-C12 aralkyloxy group;
R.sup.2 represents —(CH.sub.2).sub.p—[O(CH.sub.2).sub.q].sub.r—X (wherein X is a halogen atom, p is an integer of 1 to 6, q is an integer of 1 to 4, and r is an integer of 0 to 4);
R.sup.3 represents a hydrogen atom, a C1-C6 alkyl group, a C7-C16 aralkyl group or a C6-C14 aryl group; and
R.sup.4 represents a hydrogen atom or a C1-C6 alkyl group), or a pharmaceutically acceptable salt thereof excels FAMT in terms of the tendency to accumulate intensively in cancer, the affinity for LAT1 and the selectivity for cancer, and can be labeled using an automated synthesizer in clinical settings, and therefore is useful as a highly versatile PET imaging agent.
Aromatic amino acid derivative and positron emission topography (PET) probe using the same
A compound having a structure represented by the general formula (I): ##STR00001##
(wherein n is 0 or 1;
R.sup.1 represents a hydrogen atom (only if n=0), a halogen atom, a C1-C6 alkyl group, a C1-C6 haloalkyl group, an optionally substituted amino group, an optionally substituted phenyl group, a C1-C6 alkylthio group, a C1-C6 alkoxy group, a C1-C6 haloalkoxy group or a C7-C12 aralkyloxy group;
R.sup.2 represents —(CH.sub.2).sub.p—[O(CH.sub.2).sub.q].sub.r—X (wherein X is a halogen atom, p is an integer of 1 to 6, q is an integer of 1 to 4, and r is an integer of 0 to 4);
R.sup.3 represents a hydrogen atom, a C1-C6 alkyl group, a C7-C16 aralkyl group or a C6-C14 aryl group; and
R.sup.4 represents a hydrogen atom or a C1-C6 alkyl group), or a pharmaceutically acceptable salt thereof excels FAMT in terms of the tendency to accumulate intensively in cancer, the affinity for LAT1 and the selectivity for cancer, and can be labeled using an automated synthesizer in clinical settings, and therefore is useful as a highly versatile PET imaging agent.