151389-25-2Relevant articles and documents
20-HETE FORMATION INHIBITORS
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Paragraph 0357-0360; 0361; 0362, (2020/08/23)
This disclosure provides novel heterocyclic compounds and methods for inhibiting the enzyme CYP4. Further disclosed methods include: a method of inhibiting the biosynthesis of 20-hydroxyeicosatetraenoic acid (20-HETE) in a subject in need thereof and a method of producing neuroprotection and decreased brain damage by preventing cerebral microvascular blood flow impairment and anti-oxidant mechanisms in a subject experiencing or having experienced an ischemic event.
Potent heteroarylpiperidine and carboxyphenylpiperidine 1-alkyl-cyclopentane carboxamide CCR2 antagonists
Pasternak, Alexander,Goble, Stephen D.,Vicario, Pasquale P.,Di Salvo, Jerry,Ayala, Julia M.,Struthers, Mary,DeMartino, Julie A.,Mills, Sander G.,Yang, Lihu
, p. 994 - 998 (2008/09/19)
This report describes replacement of the 4-(4-fluorophenyl)piperidine moiety in our CCR2 antagonists with 4-heteroaryl piperidine and 4-(carboxyphenyl)-piperidine subunits. Some of the resulting analogs retained potency in our CCR2 binding assay and had i
Synthesis, SAR studies, and evaluation of 1,4-benzoxazepine derivatives as selective 5-HT1A receptor agonists with neuroprotective effect: Discovery of Piclozotan
Kamei, Katsuhide,Maeda, Noriko,Nomura, Kayoko,Shibata, Makoto,Katsuragi-Ogino, Ryoko,Koyama, Makoto,Nakajima, Mika,Inoue, Teruyoshi,Ohno, Tomochika,Tatsuoka, Toshio
, p. 1978 - 1992 (2007/10/03)
A new series of 1,4-benzoxazepine derivatives was designed, synthesized, and evaluated for binding to 5-HT1A receptor and cerebral anti-ischemic effect. A lot of compounds exhibited nanomolar affinity for 5-HT1A receptor with good selectivity over both dopamine D 2 and α1-adrenergic receptors. Among these compounds, 3-chloro-4-[4-[4-(2-pyridinyl)-1,2,3,6-tetrahydropyridin-1-yl]butyl]- 1, 4-benzoxazepin-5(4H)-one (50: SUN N4057 (Piclozotan) as 2HCl salt) showed remarkable neuroprotective activity in a transient middle cerebral artery occlusion (t-MCAO) model.
New piperidinyl- and 1,2,3,6-tetrahydropyridinyl-pyrimidine derivatives as selective 5-HT1A receptor agonists with highly potent anti-ischemic effects
Kamei, Katsuhide,Maeda, Noriko,Katsuragi-Ogino, Ryoko,Koyama, Makoto,Nakajima, Mika,Tatsuoka, Toshio,Ohno, Tomochika,Inoue, Teruyoshi
, p. 2990 - 2993 (2007/10/03)
A series of new piperidinyl- and 1,2,3,6-tetrahydropyridinyl-pyrimidine derivatives were synthesized. Among these compounds, 4-methyl-2-(1,2,3,6- tetrahydropyridin-4-yl)pyrimidine derivative 23 (SUN N5147) exhibited sub-nanomolar affinity for 5-HT1A receptor with 1000-fold selectivity over both dopamine D2 and α1-adrenergic receptors and remarkable neuroprotective activity in a transient middle cerebral artery occlusion (t-MCAO) model.
PROLINE DERIVATIVES AND USE THEREOF AS DRUGS
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, (2008/06/13)
The present invention aims at providing compounds having therapeutic effects due to a DPP-IV inhibitory action, and satisfactory as pharmaceutical products. The present inventors have found that derivatives having a substituent introduced into the γ-position of proline represented by the formula (I) wherein each symbol is as defined in the specification, have a potent DPP-IV inhibitory activity, and completed the present invention by increasing the stability.
Pyrimidine derivatives and their salts, useful for making benzoxazepine derivatives
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Example 26, (2010/11/29)
A benzoxazepine derivative having the general formula (I) and its salts and medicaments containing the same as effective ingredients: wherein, n is an integer of 2 to 5, R1indicates a hydrogen atom, halogen atom, C1to C4lo
Benzoxazepine derivatives and their salts and medicaments containing the same
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, (2008/06/13)
A benzoxazepine derivative having the general formula (I) and its salts and medicaments containing the same as effective ingredients: wherein, n is an integer of 2 to 5, R1indicates a hydrogen atom, halogen atom, C1to C4lower alkyl group, C1to C4lower alkoxyalkyl group, C1to C4halogenoalkyl group, cyano group, or ester group, R2indicates a hydrogen atom, halogen atom, C1to C4lower alkyl group, C1to C4lower alkoxy group, or hydroxy group, a dotted line indicates the presence or absence of a binding bond, W indicates C, CH, or CH2or a nitrogen atom, provided that, when W is a nitrogen atom, Z is bonded to W and the dotted line indicates the absence of a bond, and Z indicates an unsubstituted or substituted aromatic hydrocarbon ring group or an unsubstituted or substituted heterocyclic group). This benzoxazepine derivative and its salts are useful as medicaments for the treatment of anxiety neurosis, phobias, obsessive-compulsive disorders, schizophrenia, post-cardiac trauma stress, depression, psychosomatic and other psychoneurotic disorders, eating disorders, menopausal disorders, infantile autism and also emesis or disorders involving the cerebral circulatory system accompanying cerebral infarction and cerebral hemorrhage.
Process of production of 4-substituted-3-halogeno-1,4-benzoxazepine derivative and salts thereof
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, (2008/06/13)
A process for producing 4-substituted-3-halogeno-1,4-benzoxazepin derivative or the salt thereof comprising: deprotonizing a benzoxazepine derivative having the formula (II): STR1 with a base; and then, reacting the deprotonized product with a phosphate halide to produce an intermediate having the formula (IV): STR2 and then, reacting the resultant intermediate (IV) with a reagent selected from (i) a complex of a phosphine with chlorine or bromine, (ii) a phosphine and a chlorine gas or liquid bromine, (iii) a phosphine and tetrachloromethane or tetrabromomethane, or (iv) a halogenated phosphite ester to produce a 4-substituted-3-halogeno-1,4-benzoxazepine derivative having the formula (I) STR3 wherein X indicates a chlorine atom or a bromine atom, or its salt.