Category: 1609131-18-1

On May 8, 2014, Tanaka, Tadashi; Konishi, Yoshitake; Kubo, Daisuke; Fujino, Masataka; Doi, Issei; Nakagawa, Daisuke; Murakami, Tatsuya; Yamakawa, Takayuki published a patent.Name: 6-Fluoro-5-nitro-1H-indole The title of the patent was Preparation of (hetero)arylamines having keratinocyte proliferation inhibitory activity. And the patent contained the following:

A novel amine derivative expressed by general formula (I) (in the formula: G1, G2, and G3 are the same or different and represent CH or a nitrogen atom; R1 represents a chlorine atom, an optionally-substituted C3-8 cycloalkyl group, or the like; R2 represents -COOR5 (in the formula, R5 represents a hydrogen atom or a carboxyl protective group), or the like; R3 represents a hydrogen atom, or the like; and R4 represents an optionally-substituted condensed bicyclic hydrocarbon group, an optionally-substituted bicyclic heterocyclic group, or the like), or a salt thereof is useful in procedures such as the treatment or prevention of conditions related to excessive keratinocyte proliferation. Thus, heteroarylamines, prepared by several steps, inhibited the proliferation of human neonatal epidermal keratinocytes and TNFα formation in LPS-stimulated Raw264.7 cells. The compounds also inhibited TPA-induced ear thickening in mice. The experimental process involved the reaction of 6-Fluoro-5-nitro-1H-indole(cas: 1609131-18-1).Name: 6-Fluoro-5-nitro-1H-indole

The Article related to heteroarylamine preparation keratinocyte proliferation tnfalpha inhibitor, tumor necrosis factor alpha inhibitor heteroarylamine preparation, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Name: 6-Fluoro-5-nitro-1H-indole

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

On May 8, 2014, Tanaka, Tadashi; Konishi, Yoshitake; Kubo, Daisuke; Fujino, Masataka; Doi, Issei; Nakagawa, Daisuke; Murakami, Tatsuya; Yamakawa, Takayuki published a patent.Name: 6-Fluoro-5-nitro-1H-indole The title of the patent was Preparation of (hetero)arylamines having keratinocyte proliferation inhibitory activity. And the patent contained the following:

A novel amine derivative expressed by general formula (I) (in the formula: G1, G2, and G3 are the same or different and represent CH or a nitrogen atom; R1 represents a chlorine atom, an optionally-substituted C3-8 cycloalkyl group, or the like; R2 represents -COOR5 (in the formula, R5 represents a hydrogen atom or a carboxyl protective group), or the like; R3 represents a hydrogen atom, or the like; and R4 represents an optionally-substituted condensed bicyclic hydrocarbon group, an optionally-substituted bicyclic heterocyclic group, or the like), or a salt thereof is useful in procedures such as the treatment or prevention of conditions related to excessive keratinocyte proliferation. Thus, heteroarylamines, prepared by several steps, inhibited the proliferation of human neonatal epidermal keratinocytes and TNFα formation in LPS-stimulated Raw264.7 cells. The compounds also inhibited TPA-induced ear thickening in mice. The experimental process involved the reaction of 6-Fluoro-5-nitro-1H-indole(cas: 1609131-18-1).Name: 6-Fluoro-5-nitro-1H-indole

The Article related to heteroarylamine preparation keratinocyte proliferation tnfalpha inhibitor, tumor necrosis factor alpha inhibitor heteroarylamine preparation, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Name: 6-Fluoro-5-nitro-1H-indole

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

On January 3, 2020, Ma, Dawei; Wang, Kailiang; Xia, Shanghua; Li, Zheng; Zhao, Jinlong; Li, Ying published a patent.Category: indole-building-block The title of the patent was Preparation of triazole derivatives as cell necrosis inhibitors for treatment of inflammatory diseases. And the patent contained the following:

Provided by the present application are cell necrosis inhibitors with general formula I [wherein X = O, S or CH2; ring m = (un)substituted 5-6 membered heteroaryl or 5-6 membered hetero-cyclo ring fused Ph group; ring B = (un)substituted 5-12 membered aryl, 5-12 membered heteroaryl or 5-12 membered heterocyclic; R = (un)substituted (C3-C12)cycloalkyl, 5-12 membered aryl group, 5-12 membered heteroaryl group, or 5-12 membered heterocyclic group; L = O, S, NH, N(CH3)2, etc.; R1 = H or (un)substituted C1-C6 alkyl; R2 = H, halogen, hydroxy, cyano, benzyl, etc.; m = 0, 1, 2 or 3; n = 1, 2 or 3] or pharmaceutically acceptable salts thereof, the preparation method and the use thereof; in particular, provided by the present application is an inhibitor of cell necrosis and/or human receptor-interacting protein 1 kinase (RIP1). For example, compound II was prepared in a multi-step synthesis. The title compounds may be used to prevent or treat diseases involving cell death or inflammation. (assay data given). The experimental process involved the reaction of 6-Fluoro-5-nitro-1H-indole(cas: 1609131-18-1).Category: indole-building-block

The Article related to preparation triazole cell necrosis inhibitor treatment inflammatory disease human, Heterocyclic Compounds (More Than One Hetero Atom): Other 7-Membered Rings 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

On January 2, 2020, Ma, Dawei; Ji, Yuhua; He, Weiming; Fang, Chao; Zhao, Jinlong; Wang, Kailiang; Xia, Shanghua; Li, Zheng; Li, Ying published a patent.Name: 6-Fluoro-5-nitro-1H-indole The title of the patent was Preparation of triazole derivatives as cell necrosis inhibitors for treatment of inflammatory diseases. And the patent contained the following:

Provided by the present application are cell necrosis inhibitors with general formula I [wherein X = O, S or CH2; ring m = (un)substituted 5-6 membered heteroaryl or 5-6 membered hetero-cyclo ring fused Ph group; ring B = (un)substituted 5-12 membered aryl, 5-12 membered heteroaryl or 5-12 membered heterocyclic; R = (un)substituted (C3-C12)cycloalkyl, 5-12 membered aryl group, 5-12 membered heteroaryl group, or 5-12 membered heterocyclic group; L = O, S, NH, N(CH3)2, etc.; R1 = H or (un)substituted C1-C6 alkyl; R2 = H, halogen, hydroxy, cyano, benzyl, etc.; m = 0, 1, 2 or 3; n = 1, 2 or 3] or pharmaceutically acceptable salts thereof, the preparation method and the use thereof; in particular, provided by the present application is an inhibitor of cell necrosis and/or human receptor-interacting protein 1 kinase (RIP1). For example, compound II was prepared in a multi-step synthesis. The title compounds may be used to prevent or treat diseases involving cell death or inflammation. (assay data given). The experimental process involved the reaction of 6-Fluoro-5-nitro-1H-indole(cas: 1609131-18-1).Name: 6-Fluoro-5-nitro-1H-indole

The Article related to preparation triazole cell necrosis inhibitor treatment inflammatory disease human, Heterocyclic Compounds (More Than One Hetero Atom): Other 7-Membered Rings and other aspects.Name: 6-Fluoro-5-nitro-1H-indole

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

On January 3, 2020, Ma, Dawei; Wang, Kailiang; Xia, Shanghua; Li, Zheng; Zhao, Jinlong; Li, Ying published a patent.Category: indole-building-block The title of the patent was Preparation of triazole derivatives as cell necrosis inhibitors for treatment of inflammatory diseases. And the patent contained the following:

Provided by the present application are cell necrosis inhibitors with general formula I [wherein X = O, S or CH2; ring m = (un)substituted 5-6 membered heteroaryl or 5-6 membered hetero-cyclo ring fused Ph group; ring B = (un)substituted 5-12 membered aryl, 5-12 membered heteroaryl or 5-12 membered heterocyclic; R = (un)substituted (C3-C12)cycloalkyl, 5-12 membered aryl group, 5-12 membered heteroaryl group, or 5-12 membered heterocyclic group; L = O, S, NH, N(CH3)2, etc.; R1 = H or (un)substituted C1-C6 alkyl; R2 = H, halogen, hydroxy, cyano, benzyl, etc.; m = 0, 1, 2 or 3; n = 1, 2 or 3] or pharmaceutically acceptable salts thereof, the preparation method and the use thereof; in particular, provided by the present application is an inhibitor of cell necrosis and/or human receptor-interacting protein 1 kinase (RIP1). For example, compound II was prepared in a multi-step synthesis. The title compounds may be used to prevent or treat diseases involving cell death or inflammation. (assay data given). The experimental process involved the reaction of 6-Fluoro-5-nitro-1H-indole(cas: 1609131-18-1).Category: indole-building-block

The Article related to preparation triazole cell necrosis inhibitor treatment inflammatory disease human, Heterocyclic Compounds (More Than One Hetero Atom): Other 7-Membered Rings 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

On January 2, 2020, Ma, Dawei; Ji, Yuhua; He, Weiming; Fang, Chao; Zhao, Jinlong; Wang, Kailiang; Xia, Shanghua; Li, Zheng; Li, Ying published a patent.Name: 6-Fluoro-5-nitro-1H-indole The title of the patent was Preparation of triazole derivatives as cell necrosis inhibitors for treatment of inflammatory diseases. And the patent contained the following:

Provided by the present application are cell necrosis inhibitors with general formula I [wherein X = O, S or CH2; ring m = (un)substituted 5-6 membered heteroaryl or 5-6 membered hetero-cyclo ring fused Ph group; ring B = (un)substituted 5-12 membered aryl, 5-12 membered heteroaryl or 5-12 membered heterocyclic; R = (un)substituted (C3-C12)cycloalkyl, 5-12 membered aryl group, 5-12 membered heteroaryl group, or 5-12 membered heterocyclic group; L = O, S, NH, N(CH3)2, etc.; R1 = H or (un)substituted C1-C6 alkyl; R2 = H, halogen, hydroxy, cyano, benzyl, etc.; m = 0, 1, 2 or 3; n = 1, 2 or 3] or pharmaceutically acceptable salts thereof, the preparation method and the use thereof; in particular, provided by the present application is an inhibitor of cell necrosis and/or human receptor-interacting protein 1 kinase (RIP1). For example, compound II was prepared in a multi-step synthesis. The title compounds may be used to prevent or treat diseases involving cell death or inflammation. (assay data given). The experimental process involved the reaction of 6-Fluoro-5-nitro-1H-indole(cas: 1609131-18-1).Name: 6-Fluoro-5-nitro-1H-indole

The Article related to preparation triazole cell necrosis inhibitor treatment inflammatory disease human, Heterocyclic Compounds (More Than One Hetero Atom): Other 7-Membered Rings and other aspects.Name: 6-Fluoro-5-nitro-1H-indole

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

On October 14, 2021, Fett, Eykmar; Venier, Olivier published a patent.Application of 1609131-18-1 The title of the patent was Preparation of (1H-indol-5-yl)acrylamide derivatives as inhibitors of TEAD proteins and the HIPPO-YAP1/TAZ signaling cascade for the treatment of cancer. And the patent contained the following:

The invention relates to 1H-indolyl-acrylamide derivatives I [n = 0-1; R1 = a single bond, alkenyl; R2 = (fluoro)alkyl, (fluoro)alkoxy, (un)substituted Ph, etc.; R4 = H, alkyl; R7 = H, CN, (un)substituted alkyl, etc.; R8 = H, (un)substituted alkyl; R11 = H, F, Cl] or pharmaceutically acceptable salts thereof, useful as inhibitors of the TEAD-dependent gene transcription and the HIPPO-YAP1/TAZ signaling cascade for use in methods of treatment of cancer, such as e.g. breast, ovarian, uterine, prostate, lung, gastric, colorectal, bladder, pancreatic and liver cancers, sarcomas, esophageal, head and neck cancers, uveal melanoma or glioma, and in particular in the treatment of patients who have exhibited resistance to prior anti-cancer therapy. E.g., a multi-step synthesis of II, starting from 5-nitroindole and 3-(trifluoromethyl)benzyl bromide, was disclosed. Exemplified compounds I underwent biochem. studies in order to determine their capacity to inhibit YAP1/TAZ-TEAD or TEAD-dependent gene transcription (data given). Pharmaceutical composition comprising compound I was disclosed. The experimental process involved the reaction of 6-Fluoro-5-nitro-1H-indole(cas: 1609131-18-1).Application of 1609131-18-1

The Article related to indolylacrylamide preparation tead protein hippo yap1 taz signaling cascade, antitumor breast ovarian uterine prostate lung cancer indolylacrylamide preparation, gastric colorectal bladder pancreatic liver cancer treatment indolylacrylamide preparation, sarcoma esophageal head neck cancer glioma treatment indolylacrylamide preparation and other aspects.Application of 1609131-18-1

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

On October 13, 2021, there was a patent about antitumor agents.Name: 6-Fluoro-5-nitro-1H-indole The title of the patent was Preparation of (1H-indol-5-yl)acrylamide derivatives as inhibitors of TEAD proteins and the HIPPO-YAP1/TAZ signaling cascade for the treatment of cancer. And the patent contained the following:

The invention relates to 1H-indolyl-acrylamide derivatives I [n = 0-1; R1 = a single bond, alkenyl; R2 = (fluoro)alkyl, (fluoro)alkoxy, (un)substituted Ph, etc.; R4 = H, alkyl; R7 = H, CN, alkyl; R8 = H, (un)substituted alkyl] or pharmaceutically acceptable salts thereof, useful as inhibitors of the TEAD-dependent gene transcription and the HIPPO-YAP1/TAZ signaling cascade for use in methods of treatment of cancer, such as e.g. breast, ovarian, uterine, prostate, lung, gastric, colorectal, bladder, pancreatic and liver cancers, sarcomas, esophageal, head and neck cancers, uveal melanoma or glioma, and in particular in the treatment of patients who have exhibited resistance to prior anti-cancer therapy. E.g., a multi-step synthesis of II, starting from 5-nitroindole and 3-(trifluoromethyl)benzyl bromide, was disclosed. Exemplified compounds I underwent biochem. studies in order to determine their capacity to inhibit YAP1/TAZ-TEAD or TEAD-dependent gene transcription (data given). Pharmaceutical composition comprising compound I was disclosed. The experimental process involved the reaction of 6-Fluoro-5-nitro-1H-indole(cas: 1609131-18-1).Name: 6-Fluoro-5-nitro-1H-indole

The Article related to indolylacrylamide preparation tead protein hippo yap1 taz signaling cascade, antitumor breast ovarian uterine prostate lung cancer indolylacrylamide preparation, gastric colorectal bladder pancreatic liver cancer treatment indolylacrylamide preparation, sarcoma esophageal head neck cancer glioma treatment indolylacrylamide preparation and other aspects.Name: 6-Fluoro-5-nitro-1H-indole

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

On October 15, 2021, Ledneczki, Istvan; Horvath, Anita; Tapolcsanyi, Pal; Eles, Janos; Molnar, Katalin Dudas; Vago, Istvan; Visegrady, Andras; Kiss, Laszlo; Szigetvari, Aron; Koti, Janos; Kramos, Balazs; Maho, Sandor; Holm, Patrik; Kolok, Sandor; Fodor, Laszlo; Than, Marta; Kostyalik, Diana; Balazs, Ottilia; Vastag, Monika; Greiner, Istvan; Levay, Gyorgy; Lendvai, Balazs; Nemethy, Zsolt published an article.Product Details of 1609131-18-1 The title of the article was HTS-based discovery and optimization of novel positive allosteric modulators of the α7 nicotinic acetylcholine receptor. And the article contained the following:

HTS campaign of the corporate compound collection resulted in a novel, oxalic acid diamide scaffold of α7 nACh receptor pos. allosteric modulators. During the hit expansion, several derivatives, such as I-III demonstrated not only high in vitro potency, but also in vivo efficacy in the mouse place recognition test. The advanced hit mol. II was further optimized by the elimination of the putatively mutagenic aromatic-amine building block that resulted in a novel, aminomethylindole compound family. The most balanced physico-chem. and pharmacol. profile was found in case of compound IV. Docking study revealed an inter-subunit binding site to be the most probable for our compounds IV demonstrated favorable cognitive enhancing profile not only in scopolamine-induced amnesia (place recognition test in mice) but also in natural forgetting (novel object recognition test in rats). IV was, furthermore, active in a cognitive paradigm of high translational value, namely in the rat touch screen visual discrimination test. Therefore, IV was selected as a lead compound for further optimization. Based on the obtained favorable results, the invented aminomethylindole cluster may provide a viable approach for cognitive enhancement through pos. allosteric modulation of α7 nAChRs. The experimental process involved the reaction of 6-Fluoro-5-nitro-1H-indole(cas: 1609131-18-1).Product Details of 1609131-18-1

The Article related to indole allosteric modulator preparation nicotinic acetylcholine receptor cognitive enhancement, highthroughput screening indole allosteric modulator preparation drug discovery, alpha 7 nicotinic acetylcholine receptor, cognitive enhancement, high-throughput screening, positive allosteric modulation, structure-activity relationship and other aspects.Product Details of 1609131-18-1

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