180253-65-0

Upstream product

• 1990-90-5 4-amino-3-methylpyridine 
• 1074-98-2 3-methyl-4-nitropyridine N-oxide 
• 24424-99-5 di-tert-butyl dicarbonate 
• 98400-69-2 N-(4-pyridyl) t-butyl carbamate 
• 74-88-4 methyl iodide 

Downstream Products

• 264883-49-0 2-[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]-5-azaindole 
• 849777-09-9 [2-(5-chloro-2-fluoro-phenyl)-pyrido[2,3-d]pyrimidin-4-yl]-(3-methyl-pyridin-4-yl)-carbamic acid tert-butyl ester 
• 800401-64-3 ethyl 1H-pyrrolo[3,2-c]pyridine-2-carboxylate 

Relevant academic research and scientific papers

HTT MODULATORS FOR TREATING HUNTINGTON'S DISEASE

Provided herein are certain compounds useful as HTT modulators. Such compound are useful in the treatment of Huntington's disease.

AUTOTAXIN INHIBITORS AND USES THEREOF

Described herein are methods and compositions for the treatment of conditions, diseases, or disorders associated with autotaxin activity. The methods and compositions disclosed herein include the use of at least one autotaxin inhibitor compound.

TETRAHYDROISOQUINOLINE DERIVATIVES

The present invention relates to tetrahydroisoquinoline derivatives according to formula (I), wherein G represents a fused heterocyclic system selected from the groups represented by formula (G1), (G2), (G3), (G4/sup

Asymmetric Hydrogenation of Azaindoles: Chemo- and Enantioselective Reduction of Fused Aromatic Ring Systems Consisting of Two Heteroarenes

High enantioselectivity was achieved for the hydrogenation of azaindoles by using the chiral catalyst, which was prepared from [Ru(η3-methallyl)2(cod)] and a trans-chelating bis(phosphine) ligand (PhTRAP). The dearomative reaction exclusively occurred on the five-membered ring, thus giving the corresponding azaindolines with up to 97:3 enantiomer ratio.

ANNELATED PYRROLES AND THEIR USE AS CRAC INHIBITORS

The invention relates to substituted bicyclic pyrroloheterocyclyl compounds of general formula (I), wherein A1 and A2 represent direct bond or C(=O), with the proviso that 0 or 1 of A1 and A2 represents C(=O); m and n independently denote 0, 1, 2 or 3, with the proviso that the sum [n + m] is 1, 2, 3 or 4; R1 denotes H, F, CI, Br, I, CN, CF3, CF2H, CFH2, CO2H, CO2R13, R13, OH. O-R13, NH2, N(H)R13, N(R13)2, R2 represents 0 to 4 substituents, each independently selected from F, CI, Br, CN. CF3, CF2H, CFH2, R13, OH, O-R13, NH2, N(H)R13 and N(R13)2; Ar1 represents phenyl or 5- or 6-membered heteroaryl, in each case unsubstituted or substituted with one, two, three or four substituents, independently selected from F, CI, Br, CN, CF3. CF2H, CFH2, R13 and O- R13; or C3-6-cycloalkyl or 3 to 7 membered heterocycloalkyl, in each case unsubstituted or mono- or polysubstituted; Ar2 represents phenyl or 5- or 6-membered heteroaryl, wherein said phenyl or said heteroaryl may be unsubstituted or mono- or polysubstituted and may be condensed with a 4-, 5-, 6-or 7- membered ring, being carbocyclic or heterocyclic, wherein said condensed ring may be saturated, partially unsaturated or aromatic and may be unsubstituted or mono- or polysubstituted; useful as ICRAC inhibitors, to pharmaceutical compositions containing these compounds and to these compounds for the use in the treatment and/or prophylaxis of diseases and/or disorders, in particular inflammatory diseases and/or inflammatory disorders.

TETRACYCLIC INHIBITORS OF JANUS KINASES

The present invention provides compounds that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.

QUINAZOLINE DERIVATIVES AS MEDICAMENTS

Quinazoline derivatives have the formula (I) or the pharmaceutically acceptable salts thereof; wherein each of Z5, Z6, Z7 and Z8 is N or CH and wherein one or two Z5, Z6, Z7 and Z8 are N and wherein two adjacent Z positions cannot be N; wherein m and n are each independently 0-3; wherein R1 is independently OH, SH, NH2, OR, SR, NHR, halo or R-halide; wherein two adjacent R1 groups may be joined to form an aliphatic hetero cycle ring of 5-6 members; wherein R2 is independently R, halo, R-halide, OR-halide, NH2, CONH2 or CONHR; wherein R is optionally substituted C1-C12 alkyl, C1-C12 alkenyl, C1-C12 alkynyl, or aryl C1-C12 alkyl, containing 0-4 heteroatoms in place of a carbon in the carbon backbone, where the optional substituents are =O, =N, or OH; and wherein R3 is H or CH3. Such compounds are useful in pharmaceutical compositions and methods of treating conditions characterized by enhanced TGFβ activity.

PYRROLOPYRIDINE-2-CARBOXYLIC ACID AMIDE INHIBITORS OF GLYCOGEN PHOSHORYLASE

Compounds represented by Formula (I): or pharmaceutically acceptable salts thereof, are inhibitors of glycogen phosphorylase and are useful in the prophylactic or therapeutic treatment of diabetes, hyperglycemia, hypercholesterolemia, hyperinsulinemia, hyperlipidemia, hypertension, atherosclerosis or tissue ischemia e.g. myocardial ischemia, and as cardioprotectants.

A convenient method for the preparation of 5-, 6- and 7-azaindoles and their derivatives

The directed ortho lithiation of 2-tert-butoxycarbonylamino-3-methylpyridine (6a) has provided a convenient method for the preparation of 1H-pyrrolo[2,3-b]pyridine (4a, 7-azaindole). This procedure has been used to prepare a range of 3-substituted 2-tert-butoxycarbonylaminopyridines 6, 2- and 3-substituted and 2,3-disubstituted 1H-pyrrolo[2,3-b]pyridines 4 and shown to be of value in the preparation of 1H-pyrrolo[3,2-c]pyridine (15, 5-azaindole) and 1H-pyrrolo[2,3-c]pyridine (18, 6-azaindole) and derivatives.