915016-52-3

Upstream product

• 4333-56-6 cyclopropyl bromide 
• 123-08-0 4-hydroxy-benzaldehyde 
• 38380-85-7 1-bromo-4-(cyclopropyloxy)benzene 
• 68-12-2 N,N-dimethyl-formamide 

Downstream Products

• 1400701-35-0 (4-cyclopropoxyphenyl)methanol 
• 1345507-42-7 C₂₄H₁₈BrNO 
• 1345507-41-6 C₂₄H₁₉NO 

Relevant academic research and scientific papers

COMPOUNDS, SALTS THEREOF AND METHODS FOR TREATMENT OF DISEASES

The present disclosure relates to compounds according to Formulae (I), (II) and (VIII), useful for treating diseases.

Discovery of novel 2-[(4-hydroxy-6-oxo-2,3-dihydro-1H-pyridine-5-carbonyl)amino]acetic acid derivatives as HIF prolyl hydroxylase inhibitors for treatment of renal anemia

Prolyl hydroxylase domain-containing protein (PHD) inhibitors are useful as orally administered agents for the treatment of renal anemia. Based on the common structures of known PHD inhibitors, we found novel PHD inhibitor 1 with a 2-[(4-hydroxy-6-oxo-2,3

COMBINATION TREATMENTS COMPRISING IMIDAZOPYRAZINONES FOR THE TREATMENT OF PSYCHIATRIC AND/OR COGNITIVE DISORDERS

The present invention provides combination treatments comprising administration of compounds that are PDE1 enzyme inhibitors and other compounds useful in the treatment of psychiatric and/or cognitive disorders such as for example Attention Deficit Hyperactivity Disorder (ADHD), depression, anxiety, narcolepsy, schizophrenia, cognitive impairment or cognitive impairment associated with schizophrenia (CIAS). Separate aspects of the invention are directed to the combined use of said compounds for the treatment of psychiatric and/or cognitive disorders. The present invention also provides pharmaceutical compositions comprising said PDE1 enzyme inhibitors together with other compounds useful in the treatment of psychiatric and/or cognitive disorders.

COMBINATION TREATMENTS COMPRISING ADMINISTRATION OF IMIDAZOPYRAZINONES

The present invention provides combination treatments comprising administration of compounds that are PDE1 enzyme inhibitors and other compounds useful in the treatment of neurodegenerative disorders such as for example Alzheimer's Disease, Parkinson's Disease or Huntington's Disease. Separate aspects of the invention are directed to the combined use of said compounds for the treatment of neurodegenerative and/or cognitive disorders. The present invention also provides pharmaceutical compositions comprising said PDE1 enzyme inhibitors together with other compounds useful in the treatment of neurodegenerative disorders.

Targeting quinolone- and aminocoumarin-resistant bacteria with new gyramide analogs that inhibit DNA gyrase

Bacterial DNA gyrase is an essential type II topoisomerase that enables cells to overcome topological barriers encountered during replication, transcription, recombination, and repair. This enzyme is ubiquitous in bacteria and represents an important clinical target for antibacterial therapy. In this paper we report the characterization of three exciting new gyramide analogs - from a library of 183 derivatives - that are potent inhibitors of DNA gyrase and are active against clinical strains of Gram-negative bacteria (Escherichia coli, Shigella flexneri, and Salmonella enterica; 3 of 10 wild-type strains tested) and Gram-positive bacteria (Bacillus spp., Enterococcus spp., Staphylococcus spp., and Streptococcus spp.; all 9 of the wild-type strains tested). E. coli strains resistant to the DNA gyrase inhibitors ciprofloxacin and novobiocin display very little cross-resistance to these new gyramides. In vitro studies demonstrate that the new analogs are potent inhibitors of the DNA supercoiling activity of DNA gyrase (IC50s of 47-170 nM) but do not alter the enzyme's ATPase activity. Although mutations that confer bacterial cells resistant to these new gyramides map to the genes encoding the subunits of the DNA gyrase (gyrA and gyrB genes), overexpression of GyrA, GyrB, or GyrA and GyrB together does not suppress the inhibitory effect of the gyramides. These observations support the hypothesis that the gyramides inhibit DNA gyrase using a mechanism that is unique from other known inhibitors.

IMIDAZOPYRAZINONES AS PDE1 INHIBITORS

The present invention provides imidazopyrazinones as PDE1 inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders.

PARTIALLY SATURATED NITROGEN-CONTAINING HETEROCYCLIC COMPOUND

There are provided compounds having a superior PHD2 inhibitory effect that are represented by general formula (I'): (in the above-mentioned general formula (I'), W, Y, R2, R3, R4, and Y4 are as described hereinabove), or pharmaceutically acceptable salts thereof.

SULFONAMIDE COMPOUNDS HAVING TRPM8 ANTAGONISTIC ACTIVITY

Sulfonamide compounds having TRPM8 antagonistic activity are provided. A sulfonamide compound of formula (I) or a pharmaceutically acceptable salt thereof, or a prodrug thereof: (I) wherein Ring A is bicyclic aromatic heterocycle comprised of (a) pyridine is condensed with benzene; or (b) pyridine is condensed with monocyclic aromatic heterocycle, and Ring A binds to a sulfonylamino moiety on a carbon atom adjacent to a nitrogen atom of the pyridine ring constituting Ring A, Ring B is (a) monocyclic or bicyclic aromatic hydrocarbon; (b) monocyclic or bicyclic alicyclic hydrocarbon; (c) monocyclic or bicyclic aromatic heterocycle; or (d) monocyclic or bicyclic non-aromatic heterocycle, Ring C is (a) benzene; or (b) monocyclic aromatic heterocycle, and other symbols are the same as defined in the specification.

SUBSTITUTED ACRYLAMIDE DERIVATIVE AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME

A pharmaceutical composition comprising a compound having Formula (I) or a pharmacologically acceptable salt thereof as an active ingredient: [wherein, R1 is, for example, a C6-C10 aryl group which may be substituted with one group or more than one group selected from substituent group α; R2 is, for example, a C6-C10 aryl group which may be substituted with one group or more than one group selected from substituent group α; and X is, for example, a hydroxyl group or a C1-C6 alkoxy group].

SUBSTITUTED PROPANAMIDE DERIVATIVE AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME

It is an object of the present invention to provide a substituted propanamide derivative or a pharmacologically acceptable salt thereof that is useful as a prophylactic or therapeutic agent for a bone metabolic disease. The present invention relates to a pharmaceutical composition comprising a compound having General Formula (I) or a pharmacologically acceptable salt thereof as an active ingredient: [wherein, R1 represents a C6-C10 aryl group that may be substituted by a group selected from Substituent Group α, for example; R2 represents a C6-C10aryl group that may be substituted by a group selected from Substituent Group α, for example; and X represents a hydroxyl group or a C1-C6 alkoxy group, for example].