1048962-91-9

Upstream product

• 186581-53-3 diazomethane 
• 127956-19-8 methyl 5-oxotetrahydro-2H-pyran-3-carboxylate 
• 61363-56-2 2H-pyran-3,5(4H,6H)-dione 
• 57595-23-0 methyl 4-oxotetrahydrofuran-3-carboxylate 
• 127956-17-6 methyl 4-(phenylamino)-2,5-dihydrofuran-3-carboxylate 
• 127956-18-7 methyl 3-(iodomethyl)-4-(phenylimino)tetrahydrofuran-3-carboxylate 
• 1048962-91-9 (±)-cis-methyl 5-hydroxytetrahydro-2H-pyran-3-carboxylate 

Relevant academic research and scientific papers

ISOXAZOLE CARBOXYLIC ACIDS AS LPA ANTAGONISTS

The present invention provides compounds of Formula (I) or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein all the variables are as defined herein. These compounds are selective LPA receptor inhibitors.

TRIAZOLE CARBOXYLIC ACIDS AS LPA ANTAGONISTS

The present invention provides compounds of Formula (I), or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein all the variables are as defined herein. These compounds are selective LPA receptor inhibitors.

Key intermediate of 5-oxo-tetrahydropyrane-3-carboxylate and preparation method of key intermediate

The invention discloses a key intermediate of 5-oxo-tetrahydropyrane-3-carboxylate and a preparation method of the key intermediate. The preparation method of the key intermediate comprises the following steps: carrying out halogenating reaction by taking 2H-pyran-3,5(4H, 6H)-diketone (compound II) as a raw material to obtain a compound III; carrying out reduction reaction on the compound III to obtain a compound IV; carrying out halogen carbonyl insertion reaction on the compound IV to obtain a compound V; carrying out reduction on double bonds in a structure of the compound V to obtain a compound VI; and carrying out oxidation of hydroxy on the compound VI to obtain carbonyl and 5-oxo-tetrahydropyrane-3-carboxylate (compound I).

Heterocyclic-substituted alkanamides as therapeutic compounds

Use of compounds of the general formula (I) and pharmaceutically acceptable salt thereof, in which R1 and R2 have the definitions illustrated in detail in the description, as beta-secretase, cathepsin D, plasmepsin II and/or HIV protease inhibitors.

5-AMINO-4-HYDROXY-7- (IMIDAZO [1,2-A] PYRIDIN-6- YLMETHYL)-8-METHYL-NONAMIDE DERIVATIVES AND RELATED COMPOUNDS AS RENIN INHIBITORS FOR THE TREATMENT OF HYPERTENSION

Compounds of the general formula (I) or its salt or a compound in which one or more atoms are replaced by their stable, nonradio-active isotopes, in particular its pharmaceutically acceptable salt; in which X is -CH2-; R1 is a mono- to tetrasubstituted, mono- or bicyclic, unsaturated heterocyclic radical having 1 to 4 nitrogen atoms, R2 is C1-6alkyl or C3-6cycloalkyl; R3 is independently of one another H, C1-6alkyl, C1-6alkoxycarbonyl or C1-6alkanoyl; R4 is C2-6alkenyl, C1-6alkyl, unsubstituted or substituted aryl- C1-6alkyl or C3-8cycloalkyl; R5 is -Lm-R6; L is C1-6alkylene which is optionally substituted by 1-4 halogen, or a linker: formula (II) n = 0, 1 or 2; m = 0 or 1; R6 is a radical composed of 2 cyclic systems selected from bicyclo[x.y.z]alkyl, spiro[o.p]alkyl, mono- or bioxabicyclo[x.y.z]alkyl or mono- or bioxaspiro[o.p]alkyl, all of which may be substituted by 1-3 substituents selected from C1-6alkyl, C1-6alkoxy, cyano, halogen, C1-6alkoxy- C1-6alkyl, hydroxy-C1-6alkyl or dialkylamino, or if m = 0: is also saturated C3-8heterocyclyl which comprises 1-2 oxygen atoms, substituted by 1-3 substituents selected from C1-6alkyl, C1-6alkoxy, cyano, halogen, C1-6alkoxy- C1-6alkyl, hydroxy- C1-6alkyl or dialkylamino, or if m = 1: is also saturated C3-8heterocyclyl which comprises 1-2 oxygen atoms, optionally substituted by 1-3 substituents selected from C1-6alkyl, C1-6alkoxy, cyano, halogen, C1-6-alkoxy-C1-6alkyl, hydroxy-C1-6alkyl or dialkylamino; have renin- inhibiting properties and can be used as medicines for the treatment of hypertension.

HETEROCYCLIC-SUBSTITUTED ALKANAMIDES USEFUL AS RENIN INHIBITORS

Compounds of the general formula (I) in which the meanings of the substituents R1 and R2 are as stated in claim 1, have renin-inhibiting properties and can be used as medicines.