123014-46-0

Upstream product

• 91-16-7 1,2-dimethoxybenzene 
• 22809-37-6 6-bromohexanoyl chloride 
• 4224-70-8 6-bromohexanoic acid 

Downstream Products

• 123015-00-9 4-[[6-(3,4-dimethoxyphenyl)-6-oxohexyl]oxy]-2-hydroxy-3-propylbenzoic acid methyl ester 

Relevant academic research and scientific papers

Synthesis and pharmacological properties of benzamide derivatives as selective serotonin 4 receptor agonists

A series of 4-amino-5-chloro-2-methoxy-N-(piperidin-4-ylmethyl)benzamides with a polar substituent group at the 1-position of the piperidine ring was synthesized and evaluated for its effect on gastrointestinal motility. The benzoyl, phenylsulfonyl, and benzylsulfonyl derivatives accelerated gastric emptying and increased the frequency of defecation. One of them, 4-amino-N-[1-[3-(benzylsulfonyl)propyl]piperidin-4-ylmethyl]-5-chloro-2- methoxybenzamide (13a, Y-36912), was a selective 5-HT4 receptor agonist offering potential as a novel prokinetic with reduced side effects derived from 5-HT3- and dopamine D2 receptor-binding affinity. In the oral route of administration, this compound enhanced gastric emptying and defecation in mice, and has a possibility as a prokinetic agent, which is effective on both the upper and the lower gastrointestinal tract.

Novel derivatives and analogues of galanthamin

New compounds of general formula I 1

BENZOIC ACID COMPOUNDS AND USE THEREOF AS MEDICAMENTS

Benzoic acid compounds of the formula STR1 wherein each symbol is as defined in the specification, optical isomers thereof and pharmaceutically acceptable salts thereof; pharmaceutical composition comprising this compound and pharmaceutically acceptable additive; and serotonin 4 receptor agonists, gastrointestinal prokinetic agents and therapeutic agents for various gastrointestinal diseases, which comprise this compound as active ingredient. The compounds of the present invention have high and selective affinity for serotonin 4 receptor, and show agonistic effects thereon. Accordingly, they are useful medications for the prophylaxis and treatment of various gastrointestinal diseases, central nervous disorders, cardiac function disorders, urinary diseases, and the like, as well as useful anti-nociceptors for analgesic use which increase threshold of pain.

BENZOIC ACID COMPOUNDS AND MEDICINAL USE THEREOF

A benzoic acid compound of the formula wherein each symbol is as defined in the specification, an optical isomer thereof and a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprising this compound and a pharmaceutically acceptable additive, a serotonin 4 receptor agonist comprising this compound as an active ingredient, a gastrointestinal prokinetic agent and a therapeutic agent for gastrointestinal diseases. The compound of the present invention shows selective and high affinity for serotonin 4 receptors, activates same, is useful as a pharmaceutical agent for the prophylaxis and treatment of gastrointestinal diseases (e.g., reflux esophagitis; gastroesophageal reflux such as that accompanying cystic fibrosis; Barrett syndrome; intestinal pseudoileus; acute or chronic gastritis; gastric or duodenal ulcer; Crohn's disease; non-ulcer dyspepsia; ulcerative colitis; postgastrectomy syndrome; postoperative digestive function failure; delayed gastric emptying caused by gastric neurosis, gastroptosis, diabetes, and the like; gastrointestinal disorders such as indigestion, meteorism, abdominal indefinite complaint, and the like; constipation such as atonic constipation, chronic constipation, and that caused by spinal cord injury, pelvic diaphragm failure and the like; and irritable bowel syndrome), central nervous disorders (e.g., schizophrenia, depression, anxiety, disturbance of memory and dementia), cardiac function disorders (e.g., cardiac failure and myocardial ischemia), urinary diseases (e.g., dysuria caused by urinary obstruction, ureterolith, prostatomegaly, spinal cord injury, pelvic diaphragm failure, etc.), and shows superior absorption.

Catechol carboxylic acids

The invention relates to catechol carboxylic acid derivatives of the formula STR1 wherein, R1 is STR2 acetyl, hydrogen, hydroxy or alkanoyloxy, R2 is STR3 hydroxy, hydrogen or alkanoyloxy, wherein R is hydrogen, lower alkyl or --(CH2)n --N--(lower alkyl)2, R3 is hydrogen, lower alkyl or amino, R4 is hydrogen, lower alkyl, halogen or amino A is STR4 wherein, R5 is hydrogen or acyl, R6 is hydrogen, halogen, lower alkyl, aryl or cycloalkyl, and R7 and R8, independently, are hydrogen, lower alkyl or halogen, or A is STR5 wherein, R5 is hydrogen or acyl, R9 is hydrogen, lower alkyl, R10 is hydrogen, lower alkyl or halogen, R11 is hydrogen, lower alkyl, cycloalkyl or halogen, m is 0 or 1, n is an integer of 2-10, provided, that no more than one of R1 or R2 can be hydroxy, alkanoyloxy or STR6 and when R is hydrogen, salts thereof with pharmaceutically acceptable bases or when R is --(CH2)n --N--(lower alkyl)2, salts thereof with pharmaceutically acceptable acids. The compounds of formula I are useful as agents for the treatment of inflammatory diseases such as arthritis, inflammatory bowel disease such as colitis, cardiovascular diseases such as myocardial ischemia, skin diseases such as psoriasis by topical administration, and bronchopulmonary diseases such as asthma.

Substituted naphthalene carboxylic acids

The invention relates to substituted naphthalene carboxylic acid derivatives of the formula STR1 wherein one of R1 and R2 is STR2 and the other is hydrogen, wherein R is hydrogen or lower alkyl, R10 is hydrogen or lower al