Category: 1159811-32-1

On January 26, 2017, Schwink, Lothar; Buning, Christian; Glombik, Heiner; Gossel, Matthias; Kadereit, Dieter; Halland, Nis; Lohmann, Matthias; Poeverlein, Christoph; Ritter, Kurt published a patent.Product Details of 1159811-32-1 The title of the patent was Preparation of substituted fused heterocycles as GPR119 modulators for the treatment of diabetes, obesity, dyslipidemia and related disorders. And the patent contained the following:

The title compounds I [A = N or C; B = CO, N or CH; E = N or C; G = N or CR30 (wherein at least one of the groups A, B, E or G = N); R30 = H or (CR11R12)nR32; R11, R12 = (independently) H or alkyl; n = 0-3; R32 = alkyl, COOR13, CONR14R15, etc.; R13 = H or alkyl; R14, R15 = (independently) H, alkyl, cycloalkyl, etc.; or R14 and R15 form together with the N-atom to which they are attached, (un)substituted 4-6 membered heterocycle, optionally containing an addnl. heteroatom selected from the list O, S and NR18 (R18 = H or alkyl); R1a, R1b, R1c = (independently) H, F, Cl, Br, alkyl or CN; R2a, R2b, R2c = (independently) H, F, Cl, Br, alkyl or CN; Y = N or CH; Z = a bond, O, C(O), etc.; R3 = a bond or (CR7R71)p (wherein p = 0-4; R7, R71 = (independently) H or alkyl); R4 = alkyl, (un)substituted cycloalkyl, Ph, etc.] that are GPR119 modulators and useful for the prevention and/or treatment of diabetes, obesity, dyslipidemia and related disorders, were prepared For example, reacting 6-bromo-2-cyclopropyl-[1,2,4]triazolo[1,5-a]pyridine with (R)-3-{[6-(cyclopropylmethoxy)pyridin-3-yl]oxy}pyrrolidin-2-one in the presence of N,N’-dimethylethane-1,2-diamine and cesium carbonate in 1,4-dioxane afforded the isoindolinone II. Exemplified compounds I were tested for their biol. activity using the cell line expressing human GPR119 (data given). The invention furthermore relates to the use of the compounds I as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them. The experimental process involved the reaction of Methyl 6-bromo-[1,2,4]triazolo[1,5-a]pyridine-2-carboxylate(cas: 1159811-32-1).Product Details of 1159811-32-1

The Article related to fused heterocycle preparation gpr119 modulator antidiabetic antiobesity dyslipidemia, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Product Details of 1159811-32-1

Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

On August 26, 2021, Wiles, Jason Allan; Gadhachanda, Venkat Rao published a patent.Application In Synthesis of Methyl 6-bromo-[1,2,4]triazolo[1,5-a]pyridine-2-carboxylate The title of the patent was Preparation of pyrimidine-containing compounds for the treatment of Complement factor D – mediated disorders. And the patent contained the following:

The invention relates to preparation of pyrimidine-containing compounds of formulas (I) and (II) or pharmaceutically acceptable salts thereof, as inhibitors of complement factor D. Compounds I and II wherein R1 is halo or C1-2 haloalkyl; R2 is H, halo, C1-3 haloalkyl, etc.; R3 is halo, C1-3 alkyl, or C1-3 haloalkyl; R4 and R5 each independently is H, halo, CN, etc., are claimed. Compds I and II are targeting complement factor D, and inhibit or regulate the complement cascade. The example compound III was prepared via 3-step synthesis using (1R,2S,5S)-3-(tert-butoxycarbonyl)-3-azabicyclo[3.1.0]hexane-2-carboxylic acid as starting material (procedure given). Compounds I and II are inhibitors of factor D, and reducers of the excessive activation of complement (data given). Compounds I and II can be useful in treatment of Complement factor D – mediated disorders. The experimental process involved the reaction of Methyl 6-bromo-[1,2,4]triazolo[1,5-a]pyridine-2-carboxylate(cas: 1159811-32-1).Application In Synthesis of Methyl 6-bromo-[1,2,4]triazolo[1,5-a]pyridine-2-carboxylate

The Article related to pyrimidine preparation complement d disease treatment, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Application In Synthesis of Methyl 6-bromo-[1,2,4]triazolo[1,5-a]pyridine-2-carboxylate

Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

On October 8, 2015, Schwink, Lothar; Buning, Christian; Glombik, Heiner; Gossel, Matthias; Kadereit, Dieter; Halland, Nis; Lohmann, Matthias; Poeverlein, Christoph; Ritter, Kurt published a patent.HPLC of Formula: 1159811-32-1 The title of the patent was Preparation of fused heterocycles as GPR119 modulators for the treatment of diabetes, obesity, dyslipidemia and related disorders. And the patent contained the following:

Disclosed are fused heterocyclic compounds of formula I as GPR119 modulators useful for the prevention and/or treatment of diabetes, obesity, dyslipidemia and related disorders. The invention furthermore relates to the use of I as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them. I [wherein R1a, R1b, R1c, R2a, R2b, and R2c are independently H, Cl, F, alkyl, etc.; R3 is a bond or (CR7R7′)p; R7R7′ wherein each R is independently H or alkyl; p is 0, 1, 2, 3, or 4; R4 is alkyl, cycloalkyl, Ph, etc.; R30 is H, alkyl, hydroxyalkyl, etc.; A and E are independently N or C; B is CO, N, or CH; G is N or (un)substituted C; Y is N or CH; Z is bond, O, C=O, etc.] or any stereoisomeric forms or physiol. acceptable salts thereof, are claimed and exemplified. For example, (R)-II was prepared by coupling dimethylamine with the corresponding acid. I were evaluated for GPR agonistic activity using a HTRF assay from which (R)-II was determined to exhibit an EC50 value of 0.126 μM. The experimental process involved the reaction of Methyl 6-bromo-[1,2,4]triazolo[1,5-a]pyridine-2-carboxylate(cas: 1159811-32-1).HPLC of Formula: 1159811-32-1

The Article related to fused heterocycle preparation gpr119 diabetes obesity dyslipidemia, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.HPLC of Formula: 1159811-32-1

Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics