807620-95-7

Upstream product

• 60-35-5 acetamide 
• 1435-51-4 1,3-dibromo-5-fluorobenzene 

Downstream Products

• 134168-98-2 3-bromo-5-fluoroaniline hydrochloride 
• 807620-97-9 2-{2-[3-fluoro-5-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-phenyl]-2H-tetrazol-5-yl}-pyridine 
• 807620-96-8 2-[2-(3-bromo-5-fluoro-phenyl)-2H-tetrazol-5-yl]-pyridine 
• 710348-95-1 3-fluoro-5-(tetramethyl-1,3,2-dioxaborolan-2-yl)aniline 
• 507269-27-4 3-fluoro-5-(5-pyridin-2-yl-2H-tetrazol-2-yl)benzonitrile 
• 210992-28-2 3-amino-5-fluoro-benzonitrile 
• 134168-97-1 3-bromo-5-fluoroaniline 

Relevant academic research and scientific papers

3-[Substituted]-5-(5-pyridin-2-yl-2H-tetrazol-2-yl)benzonitriles: Identification of highly potent and selective metabotropic glutamate subtype 5 receptor antagonists

Structure-activity relationship studies on the phenyl ring of 3-(5-pyridin-2-yl-2H-tetrazol-2-yl)benzonitrile 2 led to the discovery that small, non-hydrogen bond donor substituents at the 3-position led to a substantial increase in in vitro potency. In particular, 3-fluoro-5-(5-pyridin- 2-yl-2H-tetrazol-2-yl)benzonitrile (7) is a highly potent and selective mGlu5 receptor antagonist with good rat pharmacokinetics, brain penetration, and in vivo receptor occupancy.

SUBSTITUTED TRICYCLIC COMPOUNDS

Disclosed are compounds of the general formula (I), its tautomeric form, its stereoisomer, its pharmaceutically acceptable salt, its polymorph, or solvate thereof, Formula (I) wherein, ring A, R1 to R5, X, Y, m, and n are as defined herein, for use as SOS1 inhibitors in the treatment of proliferative, infectious and RASopathy diseases or disorders. Also disclosed are methods of synthesizing the compound of formula I, pharmaceutical compositions containing the compound of formula I, method of treatment of proliferative, infectious and RASopathy diseases or disorder, for example, a cancer, by administering the said compound and combinations of the compound of formula I with other active ingredients.

INHIBITORS OF JUN N-TERMINAL KINASE

The present disclosure provides inhibitors of c-Jun N-terminal kinases (JNK) having a structure according to the following formula (I): or a salt or solvate thereof, wherein ring A, Ca, Cb, Z, R5, W and Cy are defined herein. The disclosure further provides pharmaceutical compositions including the compounds of the present disclosure and methods of making and using the compounds and compositions of the present disclosure, e.g., in the treatment and prevention of various disorders, such as Alzheimer's disease.

COMPOUNDS FOR THE TREATMENT OF MULTI-DRUG RESISTANT BACTERIAL INFECTIONS

The present invention relates to compounds that demonstrate antibacterial activity, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment of bacterial infections in warm-blooded animals such as humans. In particular this invention relates to compounds useful for the treatment of bacterial infections in warm-blooded animals such as humans, more particularly to the use of these compounds in the manufacture of medicaments for use in the treatment of bacterial infections in warm-blooded animals such as humans.

3-[3-Fluoro-5-(5-pyridin-2-yl-2H-tetrazol-2-yl)phenyl]-4-methylpyridine: A highly potent and orally bioavailable metabotropic glutamate subtype 5 (mGlu5) receptor antagonist

Structure-activity relationship studies performed around 3-fluoro-5-(5-pyridin-2-yl-2H-tetrazol-2-yl)benzonitrile for the purposes of developing novel mGlu5 receptor antagonists are described. Synthesis of a series of four-ring tetrazoles led to the discovery of 3-[3-fluoro-5-(5-pyridin-2-yl- 2H-tetrazol-2-yl)phenyl]-4-methylpyridine (26), a highly potent, brain penetrant, tetrazole-based mGlu5 receptor antagonist. Structure-activity relationship studies performed around 3-fluoro-5-(5-pyridin-2-yl-2H-tetrazol-2- yl)benzonitrile for the purpose of developing novel mGlu5 receptor antagonists are described. Synthesis of a series of four-ring tetrazoles led to the discovery of 3-[3-fluoro-5-(5-pyridin-2-yl-2H-tetrazol-2-yl)phenyl]-4- methylpyridine, a highly potent, brain penetrant, azole-based mGlu5 receptor antagonist.