59595-94-7

Upstream product

• 3964-58-7 3-chloro-4-hydroxybenzoic acid 
• 99-96-7 4-hydroxy-benzoic acid 

Downstream Products

• 888730-46-9 (3-chloro-4-hydroxyphenyl)-(2,3-dihydrobenzo[1,4]oxazin-4-yl)-methanone 
• 2420-16-8 4-hydroxy-3-chlorobenzaldehyde 
• 105960-29-0 2-chloro-4-(hydroxymethyl)phenol 
• 1608147-62-1 tert-butyl N-[5-(5-{5-[4-(benzyloxy)-3-chlorophenyl]-1,2,4-oxadiazol-3-yl}-1-benzofuran-2-yl)-2,2-dimethyl-1,3-dioxan-5-yl]carbamate 
• 1608144-51-9 2-amino-2-(5-(5-(4-isopropoxy-3-chlorophenyl)-1,2,4-oxadiazol-3-yl)benzofuran-2-yl)propane-1,3-diol methanesulfonic acid 
• 1608147-60-9 tert-butyl N-[5-(5-{5-[3-chloro-4-isopropoxyphenyl]-1,2,4-oxadiazol-3-yl}-1-benzofuran-2-yl)-2,2-dimethyl-1,3-dioxan-5-yl]carbamate 
• 1608147-58-5 tert-butyl N-(5-{5-[5-(3-chloro-4-hydroxyphenyl)-1,2,4-oxadiazol-3-yl]-1-benzofuran-2-yl}-2,2-dimethyl-1,3-dioxan-5-yl)carbamate 
• 1608147-56-3 2-chloro-4-(3-(4-hydroxy-3-iodophenyl)-1,2,4-oxadiazol-5-yl)phenol 
• 1608147-54-1 2-chloro-4-(3-(3-iodo-4-isopropoxyphenyl)-1,2,4-oxadiazol-5-yl)phenol 
• 1608144-50-8 2-amino-2-(5-(5-(3-chloro-4-isopropoxyphenyl)-1,2,4-oxadiazol-3-yl)benzofuran-2-yl)propane-1,3-diol 
• 1608147-52-9 N-(3-chloro-4-hydroxybenzoyloxy)-3-iodo-4-isopropoxybenzimidamide 
• 1163142-27-5 ethyl 2-(7-(5-(3-chloro-4-hydroxyphenyl)-1,2,4-oxadiazol-3-yl)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetate 
• 932019-91-5 C₁₄H₉ClF₃NO₂ 

Relevant academic research and scientific papers

PRODRUGS OF FUSED-BICYCLIC C5aR ANTAGONISTS

The present disclosure provides, inter alia, Compounds of Formulae IA, IB, IC, IIA, IIB and IIC or pharmaceutically acceptable salts thereof that are modulators of the C5a receptor. Also provided are pharmaceutical compositions and methods of use including the treatment of diseases or disorders involving pathologic activation from C5a and non-pharmaceutical applications.

ORGANIC COMPOUNDS

Novel benzofuran derivatives are disclosed. The derivatives have S1P1 receptor activity and/or disease modifying activity and find use in the treatment of conditions or diseases associated with the immune, vascular and nervous systems in animals and/or humans

Theramutein modulators

This invention relates to agents that are inhibitors or activators of variant forms of endogenous proteins and novel methods of identifying such variants. Of particular interest are inhibitors and activators of endogenous protein variants, encoded by genes which have mutated, which variants often arise or are at least first identified as having arisen following exposure to a chemical agent which is known to be an inhibitor or activator of the corresponding unmutated endogenous protein.

Fragment-based drug discovery applied to Hsp90. Discovery of two lead series with high ligand efficiency

Inhibitors of the chaperone Hsp90 are potentially useful as chemotherapeutic agents in cancer. This paper describes an application of fragment screening to Hsp90 using a combination of NMR and high throughput X-ray crystallography. The screening identified an aminopyrimidine with affinity in the high micromolar range and subsequent structure-based design allowed its optimization into a low nanomolar series with good ligand efficiency. A phenolic chemotype was also identified in fragment screening and was found to bind with affinity close to 1 mM. This fragment was optimized using structure based design into a resorcinol lead which has subnanomolar affinity for Hsp90, excellent cell potency, and good ligand efficiency. This fragment to lead campaign improved affinity for Hsp90 by over 1000000-fold with the addition of only six heavy atoms. The companion paper (DOI: 10.1021/jm100060b) describes how the resorcinol lead was optimized into a compound that is now in clinical trials for the treatment of cancer.

TETRAHYDROCYCLOPENTA[B]INDOL-3-YL CARBOXYLIC ACID DERIVATIVES USEFUL IN THE TREATMENT OF AUTOIMMUNE AND INFLAMMATORY DISORDERS

The present invention relates to certain (1,2,4-oxadiazol-3-yl)-1,2,3,4-tetrahydrocyclo-penta[b]indol-3-yl carboxylic acid derivatives of Formula (Ia) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the S1P1 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of S1P1 associated disorders, for example, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, acne, microbial infections or diseases and viral infections or diseases.

THERAMUTEIN MODULATORS

This invention relates to agents that are inhibitors or activators of variant forms of endogenous proteins and novel methods of identifying such variants. Of particular interest are inhibitors and activators of endogenous protein variants, encoded by genes which have mutated, which variants often arise or are at least first identified as having arisen following exposure to a chemical agent which is known to be an inhibitor or activator of the corresponding unmutated endogenous protein.

Production Method of Nitrogen-Containing Fused Ring Compounds

[Problems] The present invention provides a superior production method and a superior purification method of compounds effective for the treatment or prophylaxis of pathology showing involvement of uric acid, such as hyperuricemia, gouty tophus, acute gouty arthritis, chronic gouty arthritis, gouty kidney, urolithiasis, renal function disorder, coronary artery disease, ischemic heart disease and the like. [Means] A compound represented by the following formula [2] or a pharmaceutically acceptable salt thereof can be produced by reacting a compound represented by the following formula [3] or a salt thereof with a compound represented by the following formula [4], a salt thereof or a reactive derivative thereof. Moreover, crystallization of a compound represented by the formula [2] can be performed with industrially superior workability, and high quality crystals of a compound represented by the formula [2] can be obtained. wherein each symbol is as defined in the description.