The Article related to allergy, allergy inhibitors, antiasthmatics, antirheumatic agents, antitumor agents, asthma, atopic dermatitis, autoimmune disease, b cell, crohn disease, homo sapiens, human, interleukin 2 role: bsu (biological study, unclassified), biol (biological study) (production inhibitors), leukemia, neoplasm (hematol.), psoriasis, rheumatoid arthritis, systemic lupus erythematosus, transplant rejection (inhibitors), ulcerative colitis and other aspects.Recommanded Product: 1-(Cyclopropanecarbonyl)indoline-5-sulfonyl chloride
On August 19, 2010, Takahashi, Fumie; Imada, Sunao; Shiwaku, Masahiko; Kato, Koji; Fukahori, Hidehiko published a patent.Recommanded Product: 1-(Cyclopropanecarbonyl)indoline-5-sulfonyl chloride The title of the patent was Preparation of 2-(difluoromethyl)-1-(morpholinoheterocyclyl)benzimidazole derivatives as selective phosphatidyl inositol-3-kinase (PI3Kδ) inhibitors. And the patent contained the following:
The title compounds [I; R1 = A1, A2, A3 = CH or N, provided that at least 2 of A1-A3 are N; W = NH, O; R1 = Q, Q1; R2 = H, lower alkyl, hydroxy-lower alkyl; R3 = H, halo; B1, B2 = bond, C1-4 alkylene; B3 = O, S, NR0; B4 = (un)substituted CH, N; R0 = H, lower alkyl; R10 = H, (un)substituted lower alkenyl, lower alkynyl, optionally alkoxy-substituted phenyl-lower alkyl, phenyl-lower alkoxy-lower alkyl; R11 = H, R100, C(O)R101, C(O)O R102, (un)substituted CONH2, SO2R105; or NR10R11 = (un)substituted 3- to 8-membered monocyclic heterocyclyl containing 1-4 heteroatoms selected from O, S, and N; R100 = (un)substituted lower alkyl, lower alkynyl, each ring-(un)substituted cycloalkyl, cycloalkylalkyl, heterocyclyl, or heterocyclylalkyl, (un)substituted NH2; R101 = each (un)substituted lower alkyl, CONH2, or piperadinylcarbonyl, cyano, HO, lower alkoxy, etc.; R102 = lower alkyl; R105 = (un)substituted lower alkyl, lower alkenyl, etc.] or salts thereof were prepared It is found that these tri-substituted triazine derivative or tri-substituted pyrimidine derivatives have a selective inhibitory activity on PI3Kδ over PI3Kα and/or an inhibitory activity on the production of IL-2 and/or an inhibitory activity on the proliferation of B cells (including an inhibitory activity on the activation of B cells) and can be used as prophylactic or therapeutic agents for rejections in various types of organ transplantation, allergic diseases (e.g., asthma, atopic dermatitis), autoimmune diseases (e.g., rheumatoid arthritis, psoriasis, ulcerative colitis, Crohn diseases, systemic lupus erythematosus), hematol. tumors (e.g., leukemia) and others. Thus, a solution of 2.27 g 2-(difluoromethyl)-1-[2-(methylsulfonyl)-6-(morpholin-4-yl)pyrimidin-4-yl]-1H-benzimidazole in 57 mL N,N-dimethylacetamide was treated with 5.45 g trans-cyclohexane-1,4-diamine and 1.15 g K2CO3 and stirred at 100° for 1 h to give, after workup and silica gel chromatog., 2.21 g trans-N-[4-[2-(difluoromethyl)-1H-benzimidazol-1-yl]-6-(morpholin-4-yl)pyrimidin-2-yl]cyclohexane-1,4-diamine (II). A mixture of 100 mg II, 0.04 mL pyridine, and 1 mL CH2Cl2 was treated with 0.04 mL 3-chloropropane-1-sulfonyl chloride under ice-cooling, stirred at room temperature overnight, and concentrated to give, after silica gel chromatog., the precursor. Th precursor was dissolved in 1 mL N,N-dimethylformamide, treated with 27 mg 60% NaH, stirred at 0° for 1 h and at room temperature for 2 h to give, after workup and silica gel chromatog., 6-[2-(difluoromethyl)-1H-benzimidazol-1-yl]-N-[trans-4-(1,1-dioxoisothiazolidin-2-yl)cyclohexyl]-2-(morpholin-4-yl)pyrimidin-4-amine (III). III and urea derivative (IV) showed IC50 of 5.0 and 0.85 nM, resp., against human PI3Kδ and IC50 of 2,900 and 460 nM, resp., against human PI3Kα, resp. The experimental process involved the reaction of 1-(Cyclopropanecarbonyl)indoline-5-sulfonyl chloride(cas: 879562-21-7).Recommanded Product: 1-(Cyclopropanecarbonyl)indoline-5-sulfonyl chloride
The Article related to allergy, allergy inhibitors, antiasthmatics, antirheumatic agents, antitumor agents, asthma, atopic dermatitis, autoimmune disease, b cell, crohn disease, homo sapiens, human, interleukin 2 role: bsu (biological study, unclassified), biol (biological study) (production inhibitors), leukemia, neoplasm (hematol.), psoriasis, rheumatoid arthritis, systemic lupus erythematosus, transplant rejection (inhibitors), ulcerative colitis and other aspects.Recommanded Product: 1-(Cyclopropanecarbonyl)indoline-5-sulfonyl chloride
Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles