697739-27-8Relevant academic research and scientific papers
NOVEL NITROGEN-CONTAINING AROMATIC HETEROCYCLIC COMPOUND
-
Paragraph 0136, (2018/10/15)
A compound represented by general formula [1] wherein X represents N or the like, Y represents CH or the like; RA represents a cycloalkyl group which may be substituted or the like, R1 represents an alkyl group or the like, R2 represents an alkyl group which may be substituted or the like, R3 represents a hydrogen atom or an alkyl group, or a pharmaceutically acceptable salt thereof has an inhibitory activity on aldosterone synthetase, and is useful as a prophylactic and/or therapeutic agent for various diseases or symptoms associated with aldosterone.
HETEROCYCLIC SULFONAMIDE DERIVATIVE AND MEDICINE COMPRISING SAME
-
Paragraph 0623; 0624; 0625, (2016/12/01)
The present invention provides a compound represented by the formula (I): wherein each symbol is as defined in the DESCRIPTION, or a pharmaceutically acceptable salt thereof. The compound has a superior TRPA1 antagonist activity, and can provide a medicament useful for the prophylaxis or treatment of diseases involving TRPA1 antagonist and TRPA1.
AZA PYRIDONE ANALOGS USEFUL AS MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS
-
Page/Page column 92, (2010/10/03)
MCHR1 antagonists are provided having the following Formula (I): A 1 and A 2 are independently C or N, E is C or N, Q 1 , Q 2 , and Q 3 are independently C or N provided that at least one of Q 1 , Q 2 , and Q 3 is N but not more than one of Q 1 , Q 2 , and Q 3 is N, D 1 is a bond, -CR 8 R 9 X-, -XCR 8 R 9 -, -CHR 8 CHR 9 -, -CR 10 =CR 10' -, -C-C-, or 1,2-cyclopropyl; X is O, S or NR 11, R 1 , R 2 , and R 3 are ,independently selected from the group consisting of hydrogen, halogen, lower alkyl, lower cycloalkyl, -CF 3 , -OCF 3 , -OR 12 and -SR 12, G is O, S or -NR 15, D 2 is lower alkyl, lower cycloalkyl, lower alkylcycloalkyl, lower cycloalkylalkyl, lower cycloalkoxyalkyl or lower alkylcycloalkoxy or when G is NR 15 , G and D 2 together may optionally form an azetidine, pyrrolidine or piperidine ring; Z 1 and Z 2 are independently hydrogen, lower alkyl, lower cycloalkyl, lower alkoxy, lower cycloalkoxy, halo, -CF 3 , -OCONR 14 R 14' , -CN, -CONR 14 R 14' , -SOR 12 , -SO 2 R 12 , -NR 14 COR 14' , -NR 14 CO 2 R 14' , -CO 2 R 12 , NR 14 SO 2 R 12 or COR 12 ; R 5 , R 6 , and R 7 are independently selected from the group consisting of hydrogen lower alkyl, lower cycloalkyl, -CF 3 , -SR 12 , lower alkoxy, lower cycloalkoxy, -CN, -CONR 14 R 14' , SOR 12 , SO 2 R 12 , NR 14 COR 14' , NR 14 CO 2 R 12 , CO 2 R 12 , NR 14 SO 2 R 12 and -COR 12 ; R 8 , R 9 , R 10 , R 10' , R 11 are independently hydrogen or lower alkyl; R 12 is lower alkyl or lower cycloalkyl; R 14 and R 14' are independently H, lower alkyl, lower cycloalkyl or R 14 and R 14' together with the N to which they are attached form a ring having 4 to 7 atoms; and R 15 is independently selected from the group consisting of hydrogen and lower alkyl. Such compounds are useful for the treatment of MCHR1 mediated diseases, such as obesity, diabetes, IBD, depression, and anxiety
(1-AZINONE) -SUBSTITUTED PYRIDOINDOLES AS MCH ANTAGONISTS
-
Page/Page column 143, (2009/09/04)
Substituted pyridoindoles for incorporation in pharmaceutical compositions employed in the treatment of various diseases correspond to formula (I) wherein R1 is H or optionally substituted alkyl; R2, R3, R4 are
AMINO-HETEROCYCLES AS VR-1 ANTAGONISTS FOR TREATING PAIN
-
Page 36, (2010/02/07)
the present invention provides a compound of formula (I): wherein V represents NR5, O, S, SO or S(O)2; W and X each independently represent CH or N; Y represents N, CH or C-Ar2, with the proviso that at least one, but no more than two, of W, X and Y are N; Z represents CH or C-Ar2, with the proviso that when Y is N or CH then Z is C-Ar2, and with the further proviso that when Y is C-Ar2 then Z is CH; Ar1 represents a fused 9 or 10 membered heterobicyclic ring system containing one, two, three or four heteroatoms selected from nitrogen, oxygen and sulfur, wherein at least one of the rings in said ring system is aromatic; Ar2 represents an aromatic ring selected from phenyl, pyridyl, pyrimidinyl and pyridazinyl which is optionally fused and substituted; R1 represents halogen, hydroxy, oxo, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, haloC1-6alkyl, hydroxyC1-6alkyl, C1-6alkoxy, haloC1-6alkoxy, hydroxyC1-6alkoxy, C3-7cycloalkyl, C3-7cycloalkoxy, C3-5cycloalkylC1-4alkyl, cyano, nitro, SR6, SOR6, SO2R6, COR6, NR3COR6, CONR3R4, NR3SO2R6, SO2NR3R4, -(CH2)mcarboxy, esterified -(CH2)mcarboxy or -(CH2)mNR3R4; R2 represents hydrogen, halogen, hydroxy, C1-6alkyl, haloC1-6alkyl, C3-7cycloalkyl, C1-6alkoxy, haloC1-6alkoxy, unsubstituted phenyl or phenyl substituted with one or two groups selected from halogen, C1-6alkyl, haloC1-6alkyl, C3-7cycloalkyl, C1-6alkoxy or haloC1-6alkoxy; R3 and R4 are each independently hydrogen, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-7cycloalkyl or fluoroC1-6alkyl; or R3 and R4 and the nitrogen atom to which they are attached together form a heteroaliphatic ring of 4 to 7 ring atoms, optionally substituted by one or two groups selected from hydroxy or C1-4alkoxy, which ring may optionally contain as one of the said ring atoms an oxygen or a sulfur atom, S(O), S(O)2, or NR5; R5 represents hydrogen, C1-4alkyl, hydroxyC1-4alkyl or C1-4alkoxyC1-4alkyl; R6 represents hydrogen, C1-6alkyl, fluoroC1-6alkyl, C3-7cycloalkyl, unsubstituted phenyl, or phenyl substituted with one or two groups selected from halogen, C1-6alkyl, haloC1-6alkyl, C3-7cycloalkyl, C1-6alkoxy or haloC1-6alkoxy; m is either zero or an integer from 1 to 4; n is either zero or an integer from 1 to 3; or a pharmaceutically acceptable salt, N-oxide or a prodrug thereof; a pharmaceutical composition comprising it; its use in methods of treatment; use of it for the manufacture of a medicament for treating VR-1 related conditions such as those in which pain and/or inflammation predominate; and methods of treatment using it.
