28945-95-1Relevant academic research and scientific papers
PREVENTIVE AND / OR THERAPEUTIC AGENTS FOR SIP-MEDIATED DISEASES
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Paragraph 0214, (2021/04/22)
本發明之課題係提供一種將S1P5受體作動活性相對於S1P1受體作動活性之平衡經改善的化合物作為有效成份的醫藥組成物，以及將該醫藥組成物用於S1P5媒介疾病(例如，神經退化性疾病、多系統萎縮症、巴金森氏病)等之預防及/或治療的醫藥。 包含通式(V)(式中，各基的定義如說明書所載)所示之化合物或其藥學上可容許之鹽、及藥學上可容許之載體的醫藥組成物，係由於改善了S1P5受體作動活性相對於S1P1受體作動活性的平衡，故作為S1P5媒介疾病之預防及/或治療劑有用。 (式中，所有記號如說明書記載) An object
COMPOUND HAVING S1P5 RECEPTOR AGONIST ACTIVITY
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Paragraph 0174, (2021/01/14)
Provided is a compound in which the balance of the agonist activity against the S1P5 receptor relative to the S1P1 receptor has been improved in order to develop a pharmaceutical useful for the treatment of SIPs-mediated diseases such as schizophrenia and Binswanger's disease and other neurodegenerative diseases. A compound represented by the general formula (V) (wherein, all the symbols are as defined in the specification) has an improved balance of the agonist activity against the S1P5 receptor relative to the S1P1 receptor, and can thus serve as a therapeutic agent for S1P5-mediated diseases such as schizophrenia and Binswanger's disease and other neurodegenerative diseases.
SUBSTITUTED 3,4-DIHYDRONAPHTHALENES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND PREPARATION PROCESSES
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, (2008/06/13)
Substituted 3,4-dihydronaphthalenes of the formula I wherein R1 is a methyl or an amino group, R2 represents a hydrogen atom or a methyl group, and R3 is a linear or branched chain alkyl residue having 1 to 4 carbon atoms, an allyl or a crotyl group or a cyclopentyl group are disclosed which specifically inhibit 5-lipoxygenase and are useful in pharmaceutical compositions for prophylaxis and treatment of disorders attributable to the action of leucotrienes. The dihydronaphthalenes may be prepared by reacting a compound of formula II. with hydroxylamine or a salt thereof to form the corresponding oxime, reducing the oxime to a hydroxylamine of formula III and introducing a -CO-R1 group.
Synthesis of 2-(N-substituted amino)-6-hydroxy-1,2,3,4-tetrahydronaphthalen-1-ol derivatives
Miyake,Itoh,Tada,Tanabe,Hirata,Oka
, p. 2329 - 2348 (2007/10/02)
trans-6-Hydroxy-2-(1-methyl-3-phenylpropyl)amino-1,2,3,4-tetrahydronaphth alen-1-ol (8a), trans-6-hydroxy-2-(1-methyl-2-phenoxyethyl)amino-1,2,3,4-tetrahydronaphtha len-1-ol (8b) and trans-1,6-dihydroxy-2-(1-methyl-3-phenylpropyl)amino-1,2,3,4-tetrahydronap hthalene-5-carboxamide (9a) were synthesized as a part of our search for useful cardiovascular agents. 2-(N-Substituted amino)-6-alkoxy-1,2,3,4-tetrahydronaphthalen-1-ols (10-31) having various substituents at the 5-, 6- and 7-positions of the naphthalene ring were prepared by a five-step sequence of reactions starting from 3,4-dihydro-1(2H)-naphthalenone derivatives (36). Furthermore 2-(N-substituted amino)-1-indanol derivatives (33) and 6-(N-substituted amino)-2-hydroxy-6,7,8,9-tetrahydro-5H-benzocyclohepten-5-ols (34, 35) were obtained by the reductive alkylation of the corresponding amino alcohols with carbonyl compounds. These N-substituted amino alcohols (8-35) were tested for vasodilating activity in anesthetized dogs and for β-blocking activity using isolated guinea pig atrial preparations.
