Sulfonylureas and related compounds and use of same
What is Al technical title?
Al technical title is built by PatSnap Al team. It summarizes the technical point description of the patent document.
A technology of compounds and solvates used in the field of medical treatment and diagnosis of diseases
Active Publication Date: 2018-12-21
THE UNIV OF QUEENSLAND +1
View PDF9 Cites 4 Cited by
Summary
Abstract
Description
Claims
Application Information
AI Technical Summary
This helps you quickly interpret patents by identifying the three key elements:
Problems solved by technology
Method used
Benefits of technology
Problems solved by technology
Other previously characterized NLRP3 inhibitors include parthenolide, 3,4-methylenedioxy-β-nitrostyrene, and dimethylsulfoxide (DMSO), although these agents have limited potency and are nonspecific of
Method used
the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more
Image
Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
Click on the blue label to locate the original text in one second.
Reading with bidirectional positioning of images and text.
Smart Image
Examples
Experimental program
Comparison scheme
Effect test
Embodiment 1
[0448] Example 1: N-((1,2,3,5,6,7-hexahydro-s-indacene-4-yl)carbamoyl)morpholine-4-sulfonamide
[0449]
[0450] Using 4-isocyanato-1,2,3,5,6,7-hexahydro s-indacene (prepared using general method A2) and morpholine-4-sulfonamide in general method C2 gives The title compound, as a white solid (25 mg, 24%). 1 H NMR (400MHz, DMSO-d6): δ=7.98(bs,1H),6.94(s,1H),3.63(t,J=4.0Hz,4H),3.18(t,J=4.0Hz,4H), 2.81 (t, J = 8.0Hz, 4H), 2.68 (t, J = 8.0Hz, 4H), 2.02-1.95 (m, 4H); LCMS purity: >95%; LCMS (m / z): 366 [M +H] + .
Embodiment 2
[0451] Example 2: N-((1,2,3,5,6,7-hexahydro-s-indacene-4-yl)carbamoyl)-4-methylpiperazine-1-sulfonamide
[0452]
[0453] Using 4-isocyanato-1,2,3,5,6,7-hexahydro-s-indacene (prepared using general method A2) and 4-methylpiperazine-1 in general method C3 -sulfonamide The title compound was obtained as a white solid (60 mg, 55%). 1 H NMR (600MHz, DMSO-d 6 ):δ=7.96(bs,1H),6.94(s,1H),3.20(t,J=6.0Hz,4H),2.80(t,J=6.0Hz,4H),2.69(t,J=6.0Hz , 4H), 2.37(t, J=6.0Hz, 4H), 2.19(s, 3H), 2.00-1.95(m, 4H). 13 C NMR (150MHz, DMSO-d 6 ): δ=150.6, 143.5, 137.4, 129.6, 118.1, 54.3, 46.5, 45.9, 32.9, 30.7, 25.5. LCMS purity: >95%; LCMS (m / z): 379[M+H] + . C 18 h 27 N 4 o 3 S 1 (M+H) + HRMS calculated: 379.1798, found: 379.1795.
[0456] 4-Isocyanato-1,2,3,5,6,7-hexahydro-s-indacene (prepared using General Method A2) and N,N-dimethyl Sulfonamide afforded the title compound as a white solid (29 mg, 31%). 1 H NMR (400MHz, DMSO-d 6 ):δ=7.96(s,1H),6.94(s,1H),2.81(t,J=8Hz,4H),2.79(s,6H),2.70(t,J=8Hz,4H),2.02-1.96 (m,4H). 13 C NMR (150MHz, DMSO-d 6 ): δ=143.4, 142.9, 137.4, 125.1 117.9, 38.6, 32.9, 30.7, 25.5; LCMS (m / z): 324[M+H] + ;C 15 h 21 N 3 o 3 S 1 (M+H) + , HRMS calculated value: 324.13764, measured value: 324.13891.
the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more
PUM
Login to view more
Abstract
The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts, solvates and prodrugs thereof: Formula (I) wherein Q is selected from O, S and Se; J is S or Se; W1 and W2, when present, are independently selected from N and C; R1 and R2 are independently selected from the group consisting of hydrogen, C1-C12alkyl, C2-C12alkenyl, C2-C12alkynyl, aryl, heterocyclyl,heteroaryl, cycloalkyl, cycloalkenyl, amino, amido, alkylthio, acyl, arylalkyl and acylamido, all of which may be optionally substituted; and wherein at least one of W1 and W2 is present and is a nitrogen atom and when R1 and R2 are cyclic then the respective W1 or W2 may form part of the ring structure. The present invention also relates to pharmaceutical compositions including such compounds, tomethods of treatment using such compounds, in particular in relation to NLRP3 inflammasome mediated disorders, and to associated diagnostic uses.
Description
technical field [0001] The present invention relates to the field of medical treatment and diagnosis of diseases. More specifically, the present invention relates to novel sulfonylureas and related compounds and their use in the treatment or identification of diseases or conditions responsive to inhibition of NLRP3 or activation of NLRP3 or related components of the inflammatory process. Background technique [0002] Any reference herein to background art is not to be construed as an admission that such art forms common general knowledge, in Australia or elsewhere. [0003] The NOD-like receptor (NLR) family, pyridine domain-containing protein 3 (NLRP3) inflammasome is a component of the inflammatory process and its aberrant activation in genetic disorders such as cryopyrin-associated periodic syndrome (CAPS) and complex diseases such as multiple sclerosis, type 2 diabetes, Alzheimer's disease and atherosclerosis. [0004] NLRP3 is an intracellular signaling molecule that ...
Claims
the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more
Application Information
Patent Timeline
Application Date:The date an application was filed.
Publication Date:The date a patent or application was officially published.
First Publication Date:The earliest publication date of a patent with the same application number.
Issue Date:Publication date of the patent grant document.
PCT Entry Date:The Entry date of PCT National Phase.
Estimated Expiry Date:The statutory expiry date of a patent right according to the Patent Law, and it is the longest term of protection that the patent right can achieve without the termination of the patent right due to other reasons(Term extension factor has been taken into account ).
Invalid Date:Actual expiry date is based on effective date or publication date of legal transaction data of invalid patent.
Login to view more 
Login to view more