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Bicyclic compounds, compositions and medicinal applications thereof

A technology for compounds and solvates, applied in the field of preparing these bicyclic compounds, can solve the problem that RORγt inhibitors have not reached the market stage.

Inactive Publication Date: 2017-09-26
ADVINUS THERAPEUTICS PVT LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] RORγt inhibitors have not yet reached the market stage

Method used

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  • Bicyclic compounds, compositions and medicinal applications thereof
  • Bicyclic compounds, compositions and medicinal applications thereof
  • Bicyclic compounds, compositions and medicinal applications thereof

Examples

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example

[0274] The present disclosure is further illustrated by the following examples, which in no way constitute a further limitation of the present disclosure. Those skilled in the art will readily understand that the specific methods and results described are illustrative only.

[0275] Synthesis of INT-1-III: phenacyl bromide

[0276]

[0277] Step I: INT-1-II: Aryl ketones:

[0278] Aryl ketones were either synthesized as described (Vicha, Robert et al., Tetrahedron, 2005, 61:83-88 and WO2006094840) or were purchased commercially.

[0279] Step II: INT-1-III: General procedure for the preparation of phenacyl bromide

[0280] To a cold solution of aryl ketone INT-1-II (10 mmol) in chloroform (20 mL) was slowly added a solution of bromine (0.51 mL, 10 mmol) in chloroform (20 mL). After completion of the reaction (monitored by LCMS), the mixture was extracted with dichloromethane. The extract was washed with water and dried over anhydrous sodium sulfate. The solvent was eva...

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Abstract

The present disclosure relates to a class of substituted bicyclic compounds of formula (I), their tautomers, polymorphs, stereoisomers, prodrugs, solvates, hydrates, N-oxides, co-crystals, pharmaceutically acceptable salts and pharmaceutical compositions containing them. The disclosure also relates to the process of preparation of compounds of Formula (I). These compounds are useful in the treatment, prevention, prophylaxis, management, or adjunct treatment of all medical conditions related to inhibition of retinoic acid-related orphan receptor [gamma] (ROR[gamma]) such as inflammatory and / or autoimmune disorder, rheumatoid arthritis, psoriasis, psoriatic arthritis, multiple sclerosis, inflammatory bowel disease, allergic diseases, asthma, COPD, cancer, cell proliferation, type 1 diabetes, myasthenia gravis, hematopoetic disfunction, systemic lupus, erythematosus or other disorders.

Description

technical field [0001] The present invention relates to: a series of bicyclic compounds, their stereoisomers, tautomers, prodrugs, pharmaceutically acceptable salts, polymorphs, solvates, hydrates, N-oxides, co- Crystals, and preparations thereof. The present disclosure also relates to processes for preparing these bicyclic compounds (I). The compounds of the present invention were identified as inhibitors / modulators of retinoic acid-related orphan receptor gamma (RORy). More particularly, the disclosed compounds are useful for preventing, treating or ameliorating RORγ-mediated diseases. Background technique [0002] RORγ is a member of the nuclear receptor (NR) superfamily of transcription factors. The NR superfamily contains 48 members in humans and includes steroid hormone receptors, thyroid hormone receptors, various lipid receptors, and oxysterol receptors. Various nuclear receptors act as ligand-dependent transcription factors and share a modular domain (Mangelsd o...

Claims

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Application Information

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IPC IPC(8): C07D471/04A61K31/437A61K31/444A61P19/02A61P17/06A61P13/12A61P37/06A61P11/00A61P11/06A61P11/02A61P37/08A61P17/00A61P25/28A61P3/10A61P1/00A61P19/08A61P1/04A61P29/00A61P25/04A61P25/00A61P13/10A61P31/12A61P31/04A61P27/02A61P33/00A61P1/02A61P25/06
CPCC07D471/04A61P1/00A61P1/02A61P1/04A61P1/12A61P3/10A61P9/10A61P11/00A61P11/02A61P11/06A61P13/10A61P13/12A61P15/00A61P17/00A61P17/02A61P17/06A61P19/02A61P19/08A61P25/00A61P25/04A61P25/06A61P25/28A61P27/02A61P29/00A61P31/04A61P31/12A61P33/00A61P37/02A61P37/06A61P37/08A61P39/02A61P43/00A61K31/437A61K31/5377
Inventor 帕萨·穆霍帕迪亚尤盖希·穆努特纳迪姆·沙科赫贝梅尚卡尔·A·库尔卡尼卡西姆·穆克蒂亚
Owner ADVINUS THERAPEUTICS PVT LTD
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