682804-05-3

Upstream product

• 34036-07-2 3,4 difluorobenzaldehyde 
• 141-82-2 malonic acid 
• 1393363-64-8 tert-butyl (3S,αR)-3-[N-benzyl-N-(α-methylbenzyl)amino]-3-(3',4'-difluorophenyl)propanoate 
• 447416-67-3 tert-butyl (3S,αR)-3-(3,4-difluorophenyl)-3-(N-benzyl-N-α-methyl-4-methoxybenzylamino)propanoate 
• 181517-78-2 tert-butyl (E)-3-(3',4'-difluorophenyl)prop-2-enoate 
• 181517-91-9 tert-butyl (S)-3-amino-3-(3',4'-difluorophenyl)propanoate 

Relevant academic research and scientific papers

1-PHENYLPYRROLIDIN-2-ONE DERIVATIVES AS PERK INHIBITORS

The invention is directed to substituted pyrrolidinone and imidazolidinone derivatives. Specifically, the invention is directed to compounds according to Formula I: (I) wherein R1, R2, R3, R4, R5, R6, R7, X and Y are as defined herein. The compounds of the invention are inhibitors of PERK and can be useful in the treatment of cancer, pre-cancerous syndromes and diseases/injuries associated with activated unfolded protein response pathways, such as Alzheimer's disease, neuropathic pain, spinal cord injury, traumatic brain injury, ischemic stroke, stroke, Parkinson's disease, diabetes, metabolic syndrome, metabolic disorders, Huntington's disease, Creutzfeldt- Jakob Disease, fatal familial insomnia, Gerstmann-Str?ussler-Scheinker syndrome, and related prion diseases, amyotrophic lateral sclerosis, progressive supranuclear palsy, myocardial infarction, cardiovascular disease, inflammation, organ fibrosis, chronic and acute diseases of the liver, fatty liver disease, liver steatosis, liver fibrosis, chronic and acute diseases of the lung, lung fibrosis, chronic and acute diseases of the kidney, kidney fibrosis, chronic traumatic encephalopathy (CTE), neurodegeneration, dementias, frontotemporal dementias, tauopathies, Pick's disease, Neimann-Pick's disease, amyloidosis, cognitive impairment, atherosclerosis, ocular diseases, arrhythmias, in organ transplantation and in the transportation of organs for transplantation. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PERK activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

SUBSTITUTED PYRAZOLO[1,5-A]PYRIDINE-3-CARBOXAMIDES AND USE THEREOF

The present application relates to novel pyrazolo[1,5-a] pyridine-3-carboxamides, to processes for preparation thereof, to the use thereof, alone or in combinations, for treatment and/or prophylaxis of diseases, and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially for treatment and/or prophylaxis of cardiovascular disorders.

3-(PYRIMIDINE-2-YL)IMIDAZO[1,2-A]PYRIDINES

The present application relates to novel 3-(pyrimidin-2-yl)imidazo[1,2-a]pyridines, to processes for preparation thereof, to the use thereof, alone or in combinations, for the treatment and/or prophylaxis of diseases, and to the use thereof for production of medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prophylaxis of cardiovascular disorders.

BICYCLIC-PYRIMIDINEDIONE COMPOUNDS

The present invention provides novel bicyclic pyrimidinedione compounds that are useful for the treatment of hypertrophic cardiomyopathy (HCM) and conditions associated with left ventricular hypertrophy or diastolic dysfunction. The synthesis and characterization of the compounds is described, as well as methods for treating HCM and other forms of heart disease.

Amino-substituted imidazo[1,2-a]pyridinecarboxamides and their use

The present application relates to novel substituted imidazo[1,2-a]pyridine-3-carboxamides, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.

Asymmetric synthesis of β-fluoroaryl-β-amino acids

The conjugate addition of lithium (R)-N-benzyl-N-(α-methylbenzyl) amide to a range of β-fluoroaryl-α,β-unsaturated esters gave the corresponding β-amino esters with high diastereoselectivity and in good isolated yields. Sequential treatment of the resulta

Asymmetric synthesis of β-haloaryl β-amino acid derivatives

Lithium N-benzyl-N-α-methyl-4-methoxybenzylamide may be employed as a homochiral ammonia equivalent for the synthesis of homochiral β-haloaryl β-amino acid derivatives via a strategy involving its conjugate addition to α,β-unsaturated β-haloaryl acceptors and subsequent oxidative deprotection with ceric ammonium nitrate.

Lactam and cyclic urea derivatives useful as alpha 1a adrenoceptor antagonists

Lactam and cyclic urea derivatives and their pharmaceutically acceptable salts are disclosed. The synthesis of these compounds and their use as alpha 1aadrenergic receptor antagonists is also described. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are typically selective in their ability to relax smooth muscle tissue enriched in the alpha 1areceptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia can be achieved.