847585-91-5

Upstream product

• 3470-50-6 6-Hydroxy-1-tetralone 
• 32263-70-0 6-benzyloxy-3,4-dihydro-2H-naphthalen-1-one 
• 100-39-0 benzyl bromide 
• 847585-90-4 7-(benzyloxy)-4-methyl-1,2-dihydronaphthalene 
• 68-12-2 N,N-dimethyl-formamide 

Downstream Products

• 847585-84-6 1-{[6-(2,2-dimethyl-3-phenylpropoxy)-1-methyl-3,4-dihydronaphthalen-2-yl]methyl}azetidine-3-carboxylic acid hydrochloride 
• 847585-93-7 6-[3-(4-fluorophenyl)propoxy]-1-methyl-3,4-dihydronaphthalene-2-carboaldehyde 
• 1355088-68-4 C₂₁H₂₁FO₂ 
• 1355088-70-8 C₂₁H₂₁FO₂ 
• 1355088-72-0 C₂₂H₂₄O₂ 
• 1355088-74-2 C₂₂H₂₄O₂ 
• 1355088-76-4 C₂₂H₂₄O₂ 
• 1355088-77-5 C₂₃H₂₆O₂ 
• 872710-02-6 6-{[(2R)-3-(4-fluorophenyl)-2-methylpropyl]oxy}-1-methyl-3,4-dihydro-2-naphthalenecarbaldehyde 
• 872709-90-5 6-{[(2S)-3-(4-fluorophenyl)-2-methylpropyl]oxy}-1-methyl-3,4-dihydro-2-naphthalenecarbaldehyde 
• 1355088-80-0 C₂₃H₂₅FO₂ 
• 1355088-82-2 C₂₄H₂₇FO₂ 
• 872709-83-6 6-{[(2S)-3-(4-chlorophenyl)-2-methylpropyl]oxy}-1-methyl-3,4-dihydro-2-naphthalenecarbaldehyde 
• 847736-94-1 C₂₅H₂₈FNO₃ 

Relevant academic research and scientific papers

PREVENTIVE AND / OR THERAPEUTIC AGENTS FOR SIP-MEDIATED DISEASES

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

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.

DIHYDRONAPHTHALENE DERIVATIVE

A compound shown by general formula (I) (in the formula, all of the symbols are as defined in the specification) has selective S1P5 receptor agonist activity due to having a linker from a phenyl group to a cyclic substituent in a dihydronaphthalene skelet

Structure-activity relationship studies of S1P agonists with a dihydronaphthalene scaffold

Structure-activity relationship (SAR) of sphingosine-1-phosphate receptor agonists with a dihydronaphthalene scaffold was investigated. Compound 1 was modified to improve S1P1 agonistic activity and in vivo peripheral lymphocyte lowering (PLL) activity without impairing selectivity over S1P 3 agonistic activity. A detailed SAR study of the terminal lipophilic part revealed that the introduction of substituents on the propylene linker and the terminal benzene ring influences in vitro and PLL activities. Compound 6n bearing a (S)-methyl group at the 2-position on the propylene linker and chlorine at the para-position on the terminal benzene ring showed potent hS1P1 agonistic activity with excellent selectivity over hS1P 3 and in vivo PLL activity in mice.

AMINOCARBOXYLIC ACID DERIVATIVE AND MEDICINAL USE THEREOF

The present invention relates to a compound represented by the formula (I), a salt thereof, an N-oxide form thereof, a solvate thereof, or a prodrug thereof, and a medicament containing the same. The compound represented by the formula (I) has an ability to bind to an S1P receptor (particularly, EDG-1, EDG-6, and/or EDG-8) and is useful for preventing and/or treating for rejection to transplantation, graft-versus-host disease, autoimmune diseases, allergic diseases, neurodegenerating diseases, and the like. wherein all symbols are described in the specification.

COMPOUND HAVING S1P RECEPTOR BINDING POTENCY AND USE THEREOF

Provided are: a compound represented by formula (I): (wherein ring A and ring D each represent a cyclic group which may have a substituent(s); E and G each represent a bond or a spacer having 1 to 8 atoms in its main chain; L represents a hydrogen atom or a substituent; X represents amino which may have a substituent(s), or a heterocylcic group which contains at least one nitrogen atom and which may have a substituent(s); n represents 0 to 3, in which when n is 2 or more, a plurality of ring A's may be the same or different from one another); a salt thereof; an N-oxide form thereof; a solvate thereof; a prodrug thereof; and a medicament which includes those. The compound represented by formula (I) is capable of binding S1P receptors (in particular, EDG-1 and/or EDG-6), and useful for preventing and/or treating rejection in transplantation, autoimmune diseases, allergic diseases, etc.

COMPOUND CAPABLE OF BINDING S1P RECEPTOR AND PHARMACEUTICAL USE THEREOF

A compound having an ability to bind to an S1P receptor (particularly EDG-6, preferably EDG-1 and EDG-6), for example, the compound represented by formula (I) of the present invention, a salt thereof, a solvate thereof or a prodrug thereof is useful for prevention and/or treatment of rejection of transplantation, graft-versus-host disease, autoimmune disease, allergic disease and the like. wherein ring A is a cyclic group; ring B is a cyclic group which may have substituent(s); X is a spacer having 1 to 8 atoms in its main chain, etc.; Y is a spacer having 1 to 10 atoms in its main chain, etc.; n is 0 or 1, wherein when n is 0, m is 1 and R1 is a hydrogen atom or a substituent, and wherein when n is 1, m is 0 or an integer of 1 to 7 and R1 is a substituent, and wherein m is 2 or more, R1s are the same or different.

AMINOCARBOXYLIC ACID DERIVATIVE AND MEDICINAL USE THEREOF

A compound represented by the general formula (I), a salt thereof, an N-oxide form thereof, a solvate thereof, or a prodrug of any of these; and a drug containing any of these. (I) (In the formula, all the symbols are as defined in the description.) The compound represented by the general formula (I) has the ability to combine with an S1P receptor (especially EDG-1, EDG-6, and/or EDG-8). It is useful for the prevention and/or treatment of rejection reactions to transplantation, graft versus host diseases, autoimmune diseases, allergic diseases, neurodegenerative diseases, etc.