Khan, Pasha M. et al. published their research in ACS Medicinal Chemistry Letters in 2011 |CAS: 879562-21-7

The Article related to indoline tetrahydroisoquinoline aminobenzimidazole preparation, structure activity relationship pharmacokinetics nod1 induced nfkappab activation inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.Category: indole-building-block

On October 13, 2011, Khan, Pasha M.; Correa, Ricardo G.; Divlianska, Daniela B.; Peddibhotla, Satyamaheshwar; Sessions, E. Hampton; Magnuson, Gavin; Brown, Brock; Suyama, Eigo; Yuan, Hongbin; Mangravita-Novo, Arianna; Vicchiarelli, Michael; Su, Ying; Vasile, Stefan; Smith, Layton H.; Diaz, Paul W.; Reed, John C.; Roth, Gregory P. published an article.Category: indole-building-block The title of the article was Identification of Inhibitors of NOD1-Induced Nuclear Factor-κB Activation. And the article contained the following:

NOD1 (nucleotide-binding oligomerization domain 1) protein is a member of the NLR (NACHT and leucine rich repeat domain containing proteins) protein family, which plays a key role in innate immunity as a sensor of specific microbial components derived from bacterial peptidoglycans and induction of inflammatory responses. Mutations in NOD proteins have been associated with various inflammatory diseases that affect NF-κB (nuclear factor κB) activity, a major signaling pathway involved in apoptosis, inflammation, and immune response. A luciferase-based reporter gene assay was utilized in a high-throughput screening program conducted under the NIH-sponsored Mol. Libraries Probe Production Center Network program to identify the active scaffolds. Herein, we report the chem. synthesis, structure-activity relationship studies, downstream counterscreens, secondary assay data, and pharmacol. profiling of the 2-aminobenzimidazole lead, I, as a potent and selective inhibitor of NOD1-induced NF-κB activation. The experimental process involved the reaction of 1-(Cyclopropanecarbonyl)indoline-5-sulfonyl chloride(cas: 879562-21-7).Category: indole-building-block

The Article related to indoline tetrahydroisoquinoline aminobenzimidazole preparation, structure activity relationship pharmacokinetics nod1 induced nfkappab activation inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.Category: indole-building-block

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

Shalygina, E. E. et al. published their research in Izvestiya Vysshikh Uchebnykh Zavedenii, Khimiya i Khimicheskaya Tekhnologiya in 2004 |CAS: 879562-21-7

The Article related to combinatorial library acylindolinesulfonamide preparation pharmacol potential, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.COA of Formula: C12H12ClNO3S

Shalygina, E. E.; Kobylinskii, D. V.; Ivanovskii, S. A.; Balakin, K. V.; Dorogov, M. V.; Toporova, T. A. published an article in 2004, the title of the article was Synthesis and properties of 1-acylindolinesulfonamides.COA of Formula: C12H12ClNO3S And the article contains the following content:

Title compounds I and II were prepared by N-acylation of indoline, bromination and chlorosulfonylation (or just chlorosulfonylation), and amidation. Several properties indicative of potential pharmacol. activities were determined The experimental process involved the reaction of 1-(Cyclopropanecarbonyl)indoline-5-sulfonyl chloride(cas: 879562-21-7).COA of Formula: C12H12ClNO3S

The Article related to combinatorial library acylindolinesulfonamide preparation pharmacol potential, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.COA of Formula: C12H12ClNO3S

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

Shalygina, E. E. et al. published their research in Izvestiya Vysshikh Uchebnykh Zavedenii, Khimiya i Khimicheskaya Tekhnologiya in 2004 |CAS: 879562-21-7

The Article related to combinatorial library acylindolinesulfonamide preparation pharmacol potential, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.COA of Formula: C12H12ClNO3S

Shalygina, E. E.; Kobylinskii, D. V.; Ivanovskii, S. A.; Balakin, K. V.; Dorogov, M. V.; Toporova, T. A. published an article in 2004, the title of the article was Synthesis and properties of 1-acylindolinesulfonamides.COA of Formula: C12H12ClNO3S And the article contains the following content:

Title compounds I and II were prepared by N-acylation of indoline, bromination and chlorosulfonylation (or just chlorosulfonylation), and amidation. Several properties indicative of potential pharmacol. activities were determined The experimental process involved the reaction of 1-(Cyclopropanecarbonyl)indoline-5-sulfonyl chloride(cas: 879562-21-7).COA of Formula: C12H12ClNO3S

The Article related to combinatorial library acylindolinesulfonamide preparation pharmacol potential, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.COA of Formula: C12H12ClNO3S

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

Prime, Michael et al. published their patent in 2012 |CAS: 879562-21-7

The Article related to piperidinyl acrylamide preparation transglutaminase tg2 inhibitor combination chemotherapy, neurodegenerative disorder huntington’s disease treatment piperidinyl acrylamide preparation and other aspects.Application In Synthesis of 1-(Cyclopropanecarbonyl)indoline-5-sulfonyl chloride

On November 29, 2012, Prime, Michael; Courtney, Stephen Martin; Marston, Richard; Dominguez, Celia; MacDonald, Douglas; Wityak, John published a patent.Application In Synthesis of 1-(Cyclopropanecarbonyl)indoline-5-sulfonyl chloride The title of the patent was Preparation of piperidin-4-yl substituted acrylamides as transglutaminase TG2 inhibitors. And the patent contained the following:

The title compounds I [A = (un)substituted (hetero)aryl, heterocycloalkyl; B = (un)substituted mono- or bicyclic heterocycloalkyl; R1 = H, NO2, COR (wherein R = H, alkyl, cycloalkyl, etc.), etc.; R2 = H or alkyl; R3-R5 = H, F, Cl, alkyl; p = 0-3; q = 0-1], were prepared E.g., a multi-step synthesis of the acrylamide II, starting from tert-Bu piperidin-4-ylcarbamate and 6-chloropyridine-3-sulfonyl chloride, was described. Exemplified compounds I were tested for human TG2 activity. Certain compounds I were found to have IC50 value less than 100 nM (no specific data given). Also provided are pharmaceutical compositions comprising at least one compound or pharmaceutically acceptable salt therein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain disease states responsive to the inhibition of transglutaminase TG2 activity are described. These disease states include neurodegenerative disorders such as Huntington’s disease. Also described are methods of treatment which include administering at least one compound or pharmaceutically acceptable salt thereof as a single active agent or administering at least one compound or pharmaceutically acceptable salt thereof in combination with one or more other therapeutic agents. The experimental process involved the reaction of 1-(Cyclopropanecarbonyl)indoline-5-sulfonyl chloride(cas: 879562-21-7).Application In Synthesis of 1-(Cyclopropanecarbonyl)indoline-5-sulfonyl chloride

The Article related to piperidinyl acrylamide preparation transglutaminase tg2 inhibitor combination chemotherapy, neurodegenerative disorder huntington’s disease treatment piperidinyl acrylamide preparation and other aspects.Application In Synthesis of 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

Takahashi, Fumie et al. published their patent in 2010 |CAS: 879562-21-7

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