- Synthesis of α-Cyano and α-Sulfonyl Cyclic Ethers via Intramolecular Reactions of Peroxides with Sulfone- And Nitrile-Stabilized Carbanions
-
The intramolecular reaction of carbon nucleophiles with oxygen-centered electrophiles has been little explored outside of nucleophilic epoxidation. We now report the synthesis of sulfonyl- and cyano-substituted oxacycles via intramolecular reaction of sul
- Horn, Alissa,Dussault, Patrick H.
-
p. 14611 - 14626
(2019/11/13)
-
- NR2B SELECTIVE NMDA-RECEPTOR ANTAGONISTS FOR TREATMENT OF IMMUNE-MEDIATED INFLAMMATORY DISEASES
-
The present invention provides novel means and methods for treatment auf immunemediated inflammatory diseases.
- -
-
-
- Fluorine-18 Radiolabeling and Radiopharmacological Characterization of a Benzodioxolylpyrimidine-based Radiotracer Targeting the Receptor Tyrosine Kinase EphB4
-
Members of the Eph receptor tyrosine kinase family play essential roles in the pathogenesis of cancer and are therefore promising candidates for molecular imaging by positron emission tomography (PET), for example. In this regard, radiochemical access to
- Mamat, Constantin,Mosch, Birgit,Neuber, Christin,K?ckerling, Martin,Bergmann, Ralf,Pietzsch, Jens
-
p. 1991 - 2003
(2013/01/15)
-
- NR2B-SELECTIVE NMDA-RECEPTOR ANTAGONISTS
-
The present invention relates to compounds according to general formula (I) and pharmaceutical compositions comprising compounds according to general formula (I).
- -
-
Page/Page column 53-54
(2010/11/05)
-
- 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.
- Sonda, Shuji,Katayama, Kenichi,Kawahara, Toshio,Sato, Noriko,Asano, Kiyoshi
-
p. 2737 - 2747
(2007/10/03)
-
- 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.
- -
-
-
- N-substituted imidazol derivative
-
The present invention is to provide novel imidazole derivatives effectual as an antihyperlipemic agent and therapeutic and preventive drugs for arteriosclerosis, and to provide methods for manufacturing the said derivatives. More particularly, the present invention is directed to the compounds represented by the following general formula [I]; STR1 wherein R1 is hydrogen or lower alkyl, n is 0 or 1, X is N-r1 wherein r1 is hydrogen or lower alkyl, O, S, SO, SO2, CH2, CH(CH3), CONH or C(r2)=NO wherein r2 is hydrogen or lower alkyl, m is 0 or an integer of from 1 to 12, and A is methyl or a group represented by the following general formula; STR2 wherein Y is N-r3 wherein r3 is hydrogen or lower alkyl, N(r4)SO2 wherein r4 is hydrogen or lower alkyl, O, S, SO, SO2, CH2, CH(CH3), CONH or C(r5)=NO wherein r5 is hydrogen or lower alkyl, R2 is a halogen, a lower alkyl, a lower alkoxy, a cycloalkyl or COOr6 wherein r6 is hydrogen or a lower alkyl, and l is 0, 1, 2 or 3, however, m denotes an integer of from 6 to 9 when A is methyl, or m denotes 0 or an integer of from 1 to 6 when A is a group represented by the following general formula; STR3 and X and Y are each independently CH2 when m is 0, the pharmaceutically-acceptable salts thereof and methods for manufacturing the said compounds and the pharmaceutically-acceptable salts thereof.
- -
-
-
- 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.
- -
-
-
- The sily-durst chlorination of hydroxy sulfoxides
-
Treatment by sulfuryl chloride of the bis-O-TES derivative of a γ,ε-bis-hydroxy phenylsulfoxide resulted in the selective formation of the corresponding γ-chloro-ε-hydroxy phenylsulfone.
- Oddon,Uguen
-
p. 4407 - 4410
(2007/10/03)
-
- α-Fluorination of methyl phenyl sulfoxide and related compounds by molecular fluorine: A novel method for the introduction of fluorine into sulfoxides bearing α-H atoms
-
Direct formation of α-fluorosulfones from sulfoxides bearing α-H atoms merely by reaction with molecular fluorine (5% F2/N2) is reported, and a novel non-Pummerer-type mechanism is proposed for this α-fluorination reaction.
- Toyota, Akemi,Ono, Yoshinori,Chiba, Jun,Sugihara, Takumichi,Kaneko, Chikara
-
p. 703 - 708
(2007/10/03)
-
- Piperazine derivatives of theophylline and theobromine
-
New compounds of formulas I and II STR1 and the pharmaceutically acceptable acid addition salts thereof, wherein M is selected from the group consisting of hydrogen, morpholino, benzylamino, di-n-lower alkylamino, n-lower alkylamino and STR2 wherein Ar is
- -
-
-
- MODERN FRIEDEL-CRAFTS CHEMISTRY. XI. CYCLIZATION OF ARYL HALOALKYL SULFONES, ARYLSULFONYLACYL CHLORIDES AND THEIR CORRESPONDING SULFIDES
-
The sulfone group deactivation for cyclialkylation and cycliacylation reactions in the presence of Friedel-Crafts catalysts was demonstrated in a number of aryl chloroalkylsulfones (1-8) and arylsulfonylacyl chlorides (17a-22a), respectively.As expected, the corresponding arylchloroalkyl sulfides (9-16) and arylmercaptoacyl chlorides (13a-28a) underwent ring-closure reaction in most cases under the same conditions.The ease of cyclization was governed by the ring size, the stability of the attacking carbocation and the nucleophilicity of the aryl moiety.Also, the behaviour of benzyl sulfones (29, 31a, and 32a) and sulfides (33, 34a and 36a) was inconsistent.Noteworthy, the Friedel-Crafts cyclization reaction is thus considered an accessible method for the synthesis of compounds 37-41 and 45, 51.
- Abdel-Wahab, Aboel-Magd A.,El-Khawaga, Ahmed M.,El-Zohry, Maher F.,Khalaf, Ali A.
-
-