Unlock instant, AI-driven research and patent intelligence for your innovation.
Broadspectrum 2-(substituted-amino)-benzothiazole sulfonamide HIV protease inhibitors
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 for preparing medicine and pharmacy, applied in the field of combination of AIDS treatment, broad-spectrum HIV protease inhibitor, and antiretroviral agent
Inactive Publication Date: 2011-06-15
TIBOTEC PHARMA
View PDF3 Cites 0 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
[0008] It is also important to find compounds with high potency against both the natural form and the various variants, since the pill dose will be reduced if therapeutic concentrations are kept to a minimum
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
[0223] Embodiment 1: the preparation of compound 29
[0224]
[0225] 1.56 g of intermediate a-3 (R 2 = H, R 4 =-CH 2 -CH 2 -NH-(2-pyridyl)), a mixture of 0.59 g of triethylamine and 50 ml of dichloromethane, then add 1.25 g of 2-(acetylamino)-6-benzothiazolesulfonyl chloride, and place the reaction mixture at room temperature Stir overnight. After washing with water, the organic layer was separated, dried and the solvent was evaporated. The resulting brown solid was redissolved in methanol at 70 °C, cooled and filtered to yield 1.9 g (75%) of intermediate a-4 (R 2 = H, R 4 =-CH 2 -CH 2 -NH-(2-pyridyl),-A-R 6 =H).
[0226] To 6 grams of intermediate a-4 in 50 milliliters of dichloromethane (R 2 = H, R 4 =-CH 2 -CH 2 -NH-(2-pyridyl),-A-R 6 =H) to the mixture was added 7.3 ml of trifluoroacetic acid. The reaction mixture was stirred at room temperature for 6 hours. Add additional dichloromethane and wash with NaHCO 3 Solution wash. The organic layer was dri...
Embodiment 2
[0228] Embodiment 2: the preparation of compound 31
[0229]
[0230] 540 mg of intermediate a-5 (R 2 = H, R 4 =-CH 2 -(2-pyridyl),-A-R 6 =H), a mixture of 135 mg tert-butanol, 192 mg EDC, 101 mg triethylamine in 5 ml dichloromethane was stirred overnight at room temperature. Then use Na 2 CO 3 solution and brine to wash the reaction mixture. The organic layer was separated, dried and the solvent was evaporated. The residue was purified by prep-HPLC to afford 184 mg (26%) of compound 31 . Mass spectral data: m / z=702 (M+H)
Embodiment 3
[0231] Embodiment 3: the preparation of compound 33
[0232]
[0233] 540 mg of intermediate a-5 (R 2 = H, R 4 =-CH 2 -(2-pyridyl),-A-R 6 =H), 271 mg 1-[[[[(3S,3aR,6aS)+(3R,3aS,6aR)-hexahydrofuroyl (furo)[2,3-b]furan-3-yl]oxy] A mixture of carbonyl]oxy]-2,5-pyrrolidinedione, 101 mg of triethylamine in 5 ml of dichloromethane was stirred at room temperature for 24 hours. Then use Na 2 CO 3 solution and brine to wash the reaction mixture. The organic layer was separated, dried and the solvent was evaporated. The residue was purified by preparative HPLC to afford 161 mg (23%) of compound 33. Mass spectral data: m / z = 696 (M+H).
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
Property
Measurement
Unit
shear viscosity
aaaaa
aaaaa
Login to View More
Abstract
The present invention concerns broad spectrum 2-(substituted-amino)-benzothiazole sulfonamide hiv protease inhibitors. The invention provides the following compounds. It further relates to their use as broadspectrum HIV protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. It also concerns combinations thereof with anotheranti-retroviral agent, and to their use in assays as reference compounds or as reagents.
Description
[0001] This application is a Chinese patent application (national application number is No. 02804982.9, a divisional application with international application number PCT / EP02 / 01788). technical field [0002] The present invention relates to 2-(substituted-amino)-benzothiazole sulfonamides, their use as aspartic protease inhibitors, in particular as broad-spectrum HIV protease inhibitors, their preparation and medicaments containing them Compositions and diagnostic kits. The present invention also relates to the combination of said 2-(substituted-amino)-benzothiazolesulfonamides with another antiretroviral agent. The invention also relates to their use in assays as reference compounds or reactants. Background technique [0003] As we all know, the virus that causes AIDS (AIDS) has many names, including T-lymphotropic virus III (HTLV-III), or lymphadenopathy-associated virus (LAV), or AIDS-related virus (ARV), or human immunodeficiency virus (HIV). Until now, two disti...
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