20532-39-2

Upstream product

• 1266327-49-4 2-trimethylsilylethynylthiophene-3-carbaldehyde 
• 2365-48-2 Methyl thioglycolate 
• 2060-63-1 benzo[b]thiophene-5-carbonitrile 
• 4923-87-9 5-bromobenzo[b]thiophene 
• 2060-64-2 benzo[b]thiophene-5-carboxylic acid 
• 67-56-1 methanol 
• 112101-59-4 methyl 6,7-dihydrobenzothiophene-5-carboxylate 

Downstream Products

• 1005206-97-2 methyl 3-bromo-1-benzothiophene-5-carboxylate 

Relevant academic research and scientific papers

NEW ANALOGS AS ANDROGEN RECEPTOR AND GLUCOCORTICOID RECEPTOR MODULATORS

The present invention relates to novel dihydropyridine derivatives of formula (I): as modulators of nuclear receptors selected from androgen receptor and glucocorticoid receptor, to processes for their preparation, to pharmaceutical compositions comprising said compounds and to the use of said for manufacturing a medicament for the treatment of pathological conditions or diseases that can improve by modulation of androgen receptor and/or glucocorticoid receptor, selected from cancer, metastasizing cancers, benign prostate hyperplasia, polycystic ovary syndrome (PCOS), hair loss, hirsutism, acne, hypogonadism, muscle wasting diseases, cachexia, Cushing's syndrome, anti-psychotic drug induced weight gain, obesity, post-traumatic stress disorder and alcoholism.

TRICYCLIC COMPOUND AS CRTH2 INHIBITOR

Provided are a tricyclic compound as shown in formula (I) as a CRTH2 inhibitor, or a pharmaceutically acceptable salt, a tautomer, a stereoisomer or a solvate thereof, and the use thereof in treating diseases related to CRTH2 receptors.

INDOLE DERIVATIVE USED AS CRTH2 INHIBITOR

The present application discloses an indole as represented by formula (I) used as a CRTH2 inhibitor, and a pharmaceutically acceptable salt or tautomer of the indole, and an application of same in treating a disease related to a CRTH2 receptor.

Indole derivatives with CRTH2 inhibitor activity

The invention discloses indole derivatives having CRTH2 inhibitor activity and shown as formula (I) in the description or pharmaceutically acceptable salts of the indole derivatives and an applicationof the indole derivatives to treatment of CRTH2 recepto

Imidazole-containing condensed tricyclic compound and application thereof

The invention discloses an imidazole-containing condensed tricyclic compound adopting the structure as shown in the formula (I) or pharmaceutically acceptable salts, stereisomers or prodrug molecules thereof. The imidazole-containing condensed tricyclic compound has the IDO1 activity regulation function, can enhance T-cell activation through blocking immune checkpoints IDO1, is used for treating IDO1-mediated immunosuppression, and therefore, can become an effective medicine for treating malignant tumors. When used together with checkpoint protein anti-body drugs or other anti-cancer drugs, the imidazole-containing condensed tricyclic compound can enhance the anti-cancer effect. Meanwhile, the imidazole-containing condensed tricyclic compound has the potential of effectively treating IDO1 abnormity related immunosuppressive diseases and has a high application value.

BICYCLIC HYDROXAMIC ACIDS USEFUL AS INHIBITORS OF MAMMALIAN HISTONE DEACETYLASE ACTIVITY

A compound of formula (Ia) or (Ib) or a pharmaceutically acceptable salt thereof. The compound is an inhibitor of a histone deacetylase, and as such is useful in terepy, e.g. in the treatment of autoimmune disorders, mental disorders, neurodegenerative disorders, and hyperproliferative disorders.

METHOD FOR PROMOTING PLANT GROWTH

The present invention provides a method for promoting plant growth, which comprises treating a plant with a compound represented by the following Formula (1): provided that a method for promoting plant growth which comprises treating plants with a compoun

Rapid access to benzo-annelated heterocycles, naphthalenes, and polysubstituted benzenes through a novel benzannulation reaction

A novel, efficient, and powerful methyl mercaptoacetate triggered benzannulation reaction is described. The precursors are heterocyclic, aromatic or acyclic compounds bearing a carbonyl group at ortho position to an internal alkyne. The methodology does not require transition-metal catalysts and moreover it is general for the preparation of wide range of benzo-annelated heterocycles, naphthalenes and benzenes.

Synthesis of substituted benzenes and phenols by ring-closing olefin metathesis

New synthetic approaches to substituted aromatic compounds are reported. Ring-closing olefin metathesis (RCM)/dehydration and RCM/tautomerization are the key processes in the synthesis of substituted benzenes 3 and phenols 6, respectively. Readily accessible 1,5,7-trien-4-ols 7, which are the precursors of benzenes, were prepared from β-halo-α, β-unsaturated aldehydes 11 or β-halo-α,β-unsaturated esters 19 by utilizing reliable transformations in which cross-coupling with vinylic metal reagents 12 and allylation with allylic metal reagents 13 were employed as carbon-carbon bond forming reactions. RCM of 7, followed by dehydration, afforded a wide variety of substituted benzenes 3. In addition, RCM of 1,5,7trien-4-ones 9, which were prepared by oxidation of 7, furnished various substituted phenols 6 by automatic tautomerization.

NOVEL BENSOPHENONE DERIVATIVES OR SALTS THEREOF

A benzophenone derivative represented by the following formula: whereinR1 represents, for example, an optionally substituted heterocyclic group, or a substituted phenyl group; Z represents, for example, an alkylene group; R2 represents, for example, a carboxyl group optionally protected with alkyl;R3 represents, for example, an optionally protected hydroxyl group; R4 represents, for example, an optionally substituted cycloalkyloxy group; and R5 represents, for example, a hydrogen atom, ???or a salt thereof has anti-arthritic activity, inhibits bone destruction caused by arthritis, and provides high safety and excellent pharmacokinetics and thus is useful as therapeutic agent for arthritis. These compounds have inhibitory effect on AP-1 activity and are useful as preventive or therapeutic agent for diseases in which excessive expression of AP-1 is involved.