Category: 386704-04-7

On December 17, 2020, Hiscox, Afton; Stenne, Brice; Chrovian, Christa; Gelin, Christine; Samant, Andrew; Letavic, Michael A.; Dvorak, Curt published a patent.Related Products of 386704-04-7 The title of the patent was Substituted heteroaromatic pyrazolo-pyridines and their use as glun2b receptor modulators. And the patent contained the following:

Substituted Pyrazolo-pyridines as GluN2B receptor ligands. Such compounds may be used in GluN2B receptor modulation and in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by GluN2B receptor activity. The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).Related Products of 386704-04-7

The Article related to pyrazolopyridine glun2b receptor therapy, Pharmacology: Effects Of Nervous System- and Behavior-Affecting Drugs and Neuromuscular Agents and other aspects.Related Products of 386704-04-7

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On December 3, 2020, Castro, Alfredo C. published a patent.Application of 386704-04-7 The title of the patent was Sulfamides as TEAD inhibitors and their preparation, pharmaceutical compositions and use in the treatment of cancer. And the patent contained the following:

The invention provides sulfamide compounds I, compositions thereof, and methods of using the same. Compounds of formula I wherein L1 is (un)substituted (un)branched C1-6 alkylene, etc.; ring A is Ph, (un)substituted 5- to 6-membered heteroaryl, etc.; R2 is H, (un)substituted 4- to 6-membered heteroaryl, etc.; R4 is H, halo, -SO2NH2 and derivatives, -CONH2 and derivatives; R6 is H, (un)substituted C1-6 alkyl, etc.; and their pharmaceutically acceptable salts as TEAD inhibitors in the treatment of cancer thereof, are claimed. Example compound II was prepared by using etherification and cross-coupling as the key steps. All the invention compounds were evaluated for their TEAD inhibitory activity. The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).Application of 386704-04-7

The Article related to sulfamide preparation tead inhibitor treatment cancer, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.Application of 386704-04-7

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On March 15, 2018, Sato, Takahiro; Nagayama, Yukiho; Yoshino, Yasuhiro; Inoue, Tsutomu; Kato, Hiroshige; Amata, Junichiro; Inaba, Masato; Yamoto, Noriko; Taniguchi, Tetsuya published a patent.HPLC of Formula: 386704-04-7 The title of the patent was Preparation of heterocyclic compounds having erythropoietin-production acceleration activity. And the patent contained the following:

Disclosed are compounds I [X = oxygen atom, nitrogen atom, sulfur atom, etc.; R1-R3 = independently H or alkyl; R4 = H, alkyl or aryl-alkyl; R5 = alkyl, alkenyl, alkynyl, etc. (wherein alkyl, alkenyl and alkynyl are optionally substituted with halo, methoxy, trifluoromethoxy, etc.); or pharmaceutically acceptable salts thereof] and pharmaceutical composition Thus, compound II was prepared via reaction of 2,4-dimethylbenzyl alc. with methanesulfonyl chloride followed by in-situ treatment with [(7-benzyloxy-5-mercapto[1,2,4]triazolo[1,5-a]pyridine-8-carbonyl)amino]acetic acid tert-Bu ester and de-esterification. The invention compounds, e.g., II, promoted erythropoietin (EPO) production in Hep3B cells. Of note, compounds I are useful for the treatment of anemia. The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).HPLC of Formula: 386704-04-7

The Article related to heterocycle preparation erythropoietin production promoter, antianemic agent triazolopyridine erythropoietin production acceleration, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.HPLC of Formula: 386704-04-7

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On July 11, 2019, Qian, Wenyuan; Yang, Chundao; Xu, Guanghai; Li, Jie; Li, Jian; Chen, Shuhui published a patent.SDS of cas: 386704-04-7 The title of the patent was Preparation of isoindolinone and derivatives thereof as CSF-1R inhibitors. And the patent contained the following:

The present invention relates to a type of isoindolinone derivatives and use thereof in the preparation of a medicament for treating diseases associated with a novel colony stimulating factor 1 receptor (CSF-1R) inhibitor. The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).SDS of cas: 386704-04-7

The Article related to isoindolinone preparation colony stimulating factor receptor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.SDS of cas: 386704-04-7

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On February 11, 2016, Claremon, David A.; Dong, Chengguo; Fan, Yi; Leftheris, Katerina; Lotesta, Stephen D.; Singh, Suresh B.; Tice, Colin M.; Zhao, Wei; Zheng, Yajun; Zhuang, Linghang published a patent.Application of 386704-04-7 The title of the patent was Preparation of piperazine derivatives as liver X receptor modulators. And the patent contained the following:

Provided are novel compounds of formula I, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are liver X receptor modulators, and which are useful in the treatment of diseases and disorders associated with the liver X receptor. Also provided are the compounds of formula I and pharmaceutical compositions thereof for treating atherosclerosis, cardiovascular disease, Alzheimer’s disease, dermatitis, dyslipidemia, cancer and other diseases or disorders. Title compounds I [Q = alkyl-OC(O), heteroaryl, aryl-alkyl-OC(O), etc.; R1 = alkyl, cycloalkyl, aryl-alkyl, etc.; R2 = H, halo, cyano, etc.; R3 = alkyl, halo-alkyl, cycloalkyl, etc.; R4 = H or alkyl], and their pharmaceutically acceptable salts, are prepared Thus, e.g., II was prepared by reaction of (R)-tert-Bu 2-isopropylpiperazine-1-carboxylate with [3-(methylsulfonyl)phenyl]boronic acid. Compounds of the invention were evaluated for their LXr α/β binding ad agonist activity, e.g., II showed Ki value of 1690 nM and 157 nM on LXRα and LXRβ, resp. The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).Application of 386704-04-7

The Article related to piperazine derivative preparation liver receptor lxr modulator, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Application of 386704-04-7

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On December 11, 2008, Bernasconi, Giovanni; Bromidge, Steven Mark; Carpenter, Andrew James; D’Adamo, Lucilla; Di Fabio, Romano; Guery, Sebastien; Pavone, Francesca; Pozzan, Alfonso; Rinaldi, Marilisa; Sabbatini, Fabio Maria; St-Denis, Yves published a patent.SDS of cas: 386704-04-7 The title of the patent was Preparation of N-phenyl piperidinyl- and piperazinylacetohydrazides as modulators of the ghrelin receptor. And the patent contained the following:

Title compounds [I; R1 = Cl, Br, Me, CF3; X = C, N; R1a = H, alkyl; R2a = H, Me; R2 = alkyl, H, (CH2)n, wherein n = 3, 4 and the terminal C of the chain is bonded to the C atom adjacent to the N bearing the R2 group, such that a fused 6,5 or 6,6-bicyclic ring is formed; Y = (substituted) Ph pyridyl, naphthyl, pyrimidinyl, imidazo[1,2-a]pyridine-6-yl, benzothiophen-2-yl, benzothiophen-5-yl, benzofuran-2-yl, dibenzo[b,d]furan-3-yl, dibenzo[b,d]thiophen-2-yl, dibenzo[b,d]thiophen-4-yl, 1,3-benzodioxol-5-yl, 2,3-dihydro-1,4-benzodioxin-5-yl, 2,3-dihydro-1,4-benzodioxin-6-yl, 2,3-dihydro-1-benzofuran-4-yl, 2,2-difluoro-1,3-benzodiox-4-yl, pyridazinyl, imidazolyl, oxazolyl, pyrazolyl, thiazolyl, triazolyl; when Y = 2,3-dihydro-1,4-benzodioxin-6-yl, R1 ≠ Cl], were prepared Thus, dibenzo[b,d]thien-4-ylboronic acid, glyoxylic acid hydrate, and 1-methylpiperazine were microwaved together in MeCN at 120° for 20 min. to give 53% dibenzo[b,d]thien-4-yl(4-methyl-1-piperazinyl)acetic acid hydrochloride. This was stirred with TBTU, PL-DIPAM, and 3,5-dichlorophenylhydrazine in DMF for 24 h at room temperature to give 31% 2-dibenzo[b,d]thien-4-yl-N’-(3,5-dichlorophenyl)-2-(4-methyl-1-piperazinyl)acetohydrazide formate. The latter and other I showed pIC50 values of >5.5 in the GHSR antagonist BACMAM FLIPR assay. The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).SDS of cas: 386704-04-7

The Article related to piperazinylacetohydrazide preparation ghrelin receptor modulator, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.SDS of cas: 386704-04-7

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On October 24, 2019, Lauffer, David J.; Bemis, Guy; Boyd, Michael; Deininger, David; Deng, Hongbo; Dorsch, Warren; Gu, Wenxin; Hoover, Russell R.; Johnson, Jr., Mac Arthur; Ledeboer, Mark Willem; Ledford, Brian; Maltais, Francois; Penney, Marina; Takemoto, Darin; Waal, Nathan D.; Weng, Tiansheng published a patent.Application of 386704-04-7 The title of the patent was Preparation of pteridinone compounds for the treatment of cellular proliferative disorders. And the patent contained the following:

The invention provides compounds of formula I, or pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof, and methods of use thereof for treating cellular proliferative disorders (e.g., cancer). Compounds of formula I wherein A is (un)saturated 3- to 8-membered carbocyclic ring, indanyl, Ph, (un)saturated 4- to 8-membered monocyclic heterocyclic ring; L is a bond, (un)branched C1-6 hydrocarbyl and (un)branched C1-6 heterohydrocarbyl; R1 is H, (un)substituted C1-4 aliphatic, R’, etc.; R2 and R2′ are independently H, R’, (un)substituted C1-4 aliphatic, etc.; R3 is H, R’, and (un)substituted C1-6 aliphatic; R4 is H, R’, CH2OH, etc.; R5 is H, acyl, CO2H and derivatives, etc.;each R6 is independently halo, CN, NO2, acyl, etc.; R’ is C1-4 deuterioaliph.; X is N and CH; n is 0, 1, 2, 3, 4 and 5; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by a general procedure (procedure given). The invention compounds were evaluated for their PLK1 inhibitory activity. From the assay, it was determined that compound II exhibited IC50 value of < 0.3 μM. The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).Application of 386704-04-7

The Article related to pteridinone preparation treatment cellular proliferative disorder, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Application of 386704-04-7

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On January 26, 2017, Kane, John L., Jr.; Barberis, Claude; Czekaj, Mark; Erdman, Paul; Giese, Barret; Kothe, Michael; Le, Tieu-Binh; Liu, Jinyu; Ma, Liang; Metz, Markus; Patel, Vinod; Scholte, Andrew; Shum, Patrick; Wei, Limli published a patent.Formula: C7H6F3NO The title of the patent was Preparation of nitrogen heterocycles as colony stimulating factor-1 receptor (CSF-1R) inhibitors. And the patent contained the following:

Compounds I [A = (CR1R2)n; M = (CR4R5)m; n is 0, 1, 2, 3, 4 or 5; m is 1, 2, 3 or 4; X1 is C, N or CR7, X2, X3, X4, X5, X6 and X7 are each independently selected from N, NR7 or CR7;]. [Wherein: each R7 is independently selected from the group consisting of H, C1-10-alkyl, C3-10-cycloalkyl, C2-9-heterocycloalkyl, C6-14-aryl, C2-9-heteroaryl, C2-10-alkylnyl, (C1-10-alkyl)NH, (C1-0-alkyl)2N, (C2-10-alkynyl)NH, C(:O), (C1-10-alkyl)-CO2-, (C1-10-alkyl)-CO2H, (C3-10-cycloalkyl)-CO2H, C1-10-alkoxy, R8-(C1-10-alkyl), R8-(C3-10-cycloalkyl), NR8R9, etc.;]. [Wherein: R8 and R9 are each independently selected from the group consisting of H, C1-10-alkyl, C3-10-cycloalkyl, C2-9-heterocycloalkyl, C6-14-aryl, C2-9-heteroaryl, (C1-10-alkyl)NH, (C1-10-alkyl)2N, (C1-3-alkynyl)NH, (C1-10-alkyl)-CO2-, COOH, (C1-10-alkyl)CO2H, etc.; or, R8 and R9 are taken together to form a 3 to 10 member cycloalkyl, heterocycloalkyl, aryl or heteroaryl ring;]. [X8 and X9 are each independently selected from N or C; T1, T2 and T3 is each independently selected from are each independently selected from N or CR10; wherein: each R10 is independently selected from the group consisting of H, C1-10-alkyl, C3-10-cycloalkyl, C2-9-heterocycloalkyl, C6-14-aryl, C2-9-heteroaryl, C2-10-alkylnyl, (C1-10-alkyl)NH, (C1-10-alkyl)2N, (C2-10-alkynyl)NH, C(:O), (C1-10-alkyl)-CO2-, (C1-10-alkyl)-CO2H, (C3-10-cycloalkyl)-CO2H, C1-10-alkoxy, etc.;]. [Y1 is O, S, NR12 or CR12R13; wherein: R12 is absent or R12 and R13 are each independently selected from the group consisting of H, C1-10-alkyl, C3-10-cycloalkyl, C2-9-heterocycloalkyl, C6-14-aryl, C2-9-heteroaryl, (C1-10-alkyl)NH, (C1-10-alkyl)2N, (C1-3-alkynyl)NH, (C1-10-alkyl)-CO2-, (C1-10-alkyl)CO2H, (C3-10-cycloalkyl)CO2H, C1-10-alkoxy, etc,;]. [R1 together with the carbon to which it is attached to form a carbonyl and R2 is absent; or, R1 and R2 are each independently selected from the group consisting of H, C1-10-alkyl, C3-10-cycloalkyl, C2-9-heterocycloalkyl, C6-14-aryl, C2-9-heteroaryl, (C1-10-alkyl)NH, (C1-10-alkyl)2N, (C1-3-alkynyl)NH, C1-10-alkoxy, etc.;]. [R4 is selected from the group consisting of H, C1-10-alkyl, C3-10-cycloalkyl, C2-9-heterocycloalkyl, C6-14-aryl, C2-9-heteroaryl, (C1-10-alkyl)NH, (C1-10-alkyl)2N, (C1-3-alkynyl)NH, C1-10-alkoxy, etc.; or, R4 and R5 can be taken together with the carbon to which they are attached to form a 3 to 10 member ring;]. [R5 is absent or selected from the group consisting of H, C1-10-alkyl, C3-10-cycloalkyl, C2-9-heterocycloalkyl, C6-14-aryl, C2-9-heteroaryl, (C1-10-alkyl)NH, (C1-10-alkyl)2N, (C1-3-alkynyl)NH, C1-10-alkoxy, etc.;]. [R6 is selected from the group consisting of H, C1-10-alkyl, C3-10-cycloalkyl, C2-9-heterocycloalkyl, C6-14-aryl, C2-9-heteroaryl, C2-10-alkynyl, (C1-10-alkyl)NH, (C1-10-alkyl)2N, (C2-10-alkynyl)NH, C(:O), etc.;]. [R3 is N or CR16; wherein: R16 is selected from the group consisting of H, C1-10-alkyl, C3-10-cycloalkyl, C2-9-heterocycloalkyl, C6-14-aryl, C2-9-heteroaryl, (C1-10-alkyl)NH, (C1-10-alkyl)2N, (C1-3-alkynyl)NH, (C1-10-alkyl)-CO2-, (C1-10-alkyl)-CO2H,(C3-10-cycloalkyl)-CO2H, C1-10-alkoxy, etc.;]. [When m is 1, R16 and R4 are taken together with the carbons to which they are attached to form a compound; wherein the dashed lines represent optional double bonds;] and II [p is 0, 1, 2, 3, 4 or 5; Z = (CZ1)p; Z1 is each independently selected from H, halogen, C1-10-alkyl, C2-9-heteroalkyl, (C1-10-alkyl)NH, (C1-10-alkyl)2N, (C2-10-alkynyl)NH, C1-10-alkoxy or NH2;]. [Y2 is O, S, NR17, or CR17R18, wherein R17 is absent, or R17 and R18 are each independently selected from H, C1-10-alkyl, C3-10-cycloalkyl, C2-9-heterocycloalkyl, C6-14-aryl, C2-9-heteroaryl, (C1-10-alkyl)NH, (C1-10-alkyl)2N, (C1-3-alkynyl)NH, (C1-10-alkyl)-CO2-, etc.;], or the pharmaceutically acceptable salt thereof, are described. Compounds I and II are useful as colony stimulating factor-1 receptor inhibitors (“”CSF-1R inhibitors””). Thus, 4-(1-((2-(4-methoxyphenyl)-2,3-dihydrobenzo[b][1,4]dioxin-6-yl)methyl)-1H-benzo[d]imidazol-5-yl)-2-methylbut-3-yn-2-amine (III) was prepared and tested for CSF-1R inhibition [c-FMS IC50 = 0.005 μM; Phospho c-FMS IC50 = 0,053 μM]. The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).Formula: C7H6F3NO

The Article related to colony stimulating factor receptor inhibitors heterocyclic compound preparation, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Formula: C7H6F3NO

Referemce:
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On August 6, 2015, Kobayashi, Kaori; Suzuki, Tamotsu; Kawahira, Mizuki; Fujii, Tomohiro; Sugiki, Masayuki; Ohsumi, Koji; Okuzumi, Tatsuya published a patent.HPLC of Formula: 386704-04-7 The title of the patent was Preparation of heterocyclic sulfonamide derivatives as TRPA1 antagonists for treating pain, digestive diseases, and inflammatory diseases. And the patent contained the following:

The heterocyclic sulfonamide derivatives are represented by formula I [Q = O, S; A = 6-membered aromatic or heterocyclic ring, bicyclic aromatic or heterocyclic ring; A1 = C(Ra), N; A2 = C(Rb), N; A3 = C(Rc), N; A4 = C(Rd), N; Ra-Rd = H, halo, cyano, OH, C1-6 alkyl, etc.; least two of A1-A4 are not N; R1 = H, (un)substituted C1-6 alkyl; R2 = H, (un)substituted C1-6 alkyl or C2-6 alkenyl; R3-R5 = H, C1-6 alkyl; R1 and R2 may form (un)substituted heterocycle; R4 and R5 may form cycloalkane; X = (un)substitued C, (un)substited N, or S-containing Cy; Cy = (un)substituted and hetero-(un)containing saturated or unsaturated cyclic group; R6 = (un)substituted C1-6 alkyl, C2-6 alkenyl, halo, OH, amino, etc.; m = 0-3], excluding II. Thus, Mitsunobu reaction of (2S)-1-(benzofuran-2-ylsulfonyl)-N-[(3-hydroxyphenyl)methyl]pyrrolidine-2-carboxamide (preparation given) and 4-hydroxybenzonitrile (sic) gave (2S)-1-(benzofuran-2-ylsulfonyl)-N-[[3-[(4-cyanophenyl)methoxy]phenyl]methyl]pyrrolidine-2-carboxamide showing human transient receptor potential ankyrin 1 antagonistic activity (IC50) 0.0030 μM. The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).HPLC of Formula: 386704-04-7

The Article related to heterocyclic sulfonamide preparation trpa1 antagonist pain digestive inflammatory, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.HPLC of Formula: 386704-04-7

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On June 21, 2012, Surman, Matthew D.; Guzzo, Peter R.; Freeman, Emily; Henderson, Alan J. published a patent.Name: (6-(Trifluoromethyl)pyridin-3-yl)methanol The title of the patent was Preparation of tetrahydro-azacarboline MCH-1 antagonists. And the patent contained the following:

The present invention relates to tetrahydro-azacarboline derivatives I [G = NR8CR9C10 or CR9R10NR8; X = CR16, C(R16)2, N, NR16; Y = CR16, C, N; W = C or N; Q = C or N; Z = C, CH or N; L = (CH2)pO, (CH2)p, CH:CH, a bond; A = C, CH, CH2, N; B = (un)substituted (hetero)aryl, heterocyclyl, cycloalkyl; R1 = H, alkyl, cycloalkyl, etc.; R2-R5, R9-R10 = H, halo, alkyl, etc.; R6 = H, halo, aryl, etc.; R7 = H, halo, CN, etc.; R8 = H, alkyl, cycloalkyl, etc.; n = 0-3; p = 1-4] which are melanin-concentrating hormone (MCH-1) receptor antagonists. Twenty-eight compounds I were prepared E.g., a multi-step synthesis of II.HCl, starting from 2,6-dibromopyridine, was described. Exemplified compounds I were tested in the human MCH-1 binding assay (data given). The present invention also relates to pharmaceutical compositions including these compounds, and methods of preparation and use thereof. The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).Name: (6-(Trifluoromethyl)pyridin-3-yl)methanol

The Article related to azacarboline preparation melanin concentrating hormone mch1 receptor antagonist, Heterocyclic Compounds (More Than One Hetero Atom): Fused-Ring Systems With Two Or More Hetero Atoms, No More Than One Hetero Atom Per Ring and other aspects.Name: (6-(Trifluoromethyl)pyridin-3-yl)methanol

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