Category: 386704-04-7

On April 12, 2018, Chrovian, Christa C.; Letavic, Michael A.; Rech, Jason C.; Rudolph, Dale A.; Johnson, Akinola Soyode; Stenne, Brice M.; Wall, Jessica L. published a patent.Application of 386704-04-7 The title of the patent was Preparation of substituted 1H-imidazo[4,5-b]pyridin-2(3H)-ones and their use as GluN2B receptor modulators. And the patent contained the following:

Provided are substituted 1H-imidazo[4,5-b]pyridin-2(3H)-ones of formula I as NR2B receptor modulators useful for the treatment of diseases, disorders, and conditions mediated by NR2B receptor activity. Compounds of formula I [wherein R1 = H, CH2F, or CH3; R2 = (un)substituted Ph, (un)substituted pyridinyl,(un)substituted thienyl, etc.; R3 = H; R4 = for example, pyrazin-2-ylmethyl, oxetan-2-ylmethyl, pyridazin-3-ylmethyl, etc.] or pharmaceutically acceptable salts, solvates, stereoisomers, isotopic variants, or N-oxides or pharmaceutical compositions thereof, are claimed and exemplified. Example compound II was prepared from a multistep procedure (preparation given). Exemplified I were evaluated for NMDA receptor antagonistic activity using human NR1/NR2B ion channel expressing mammalian cells from which II demonstrated an IC50 value of 2.740 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 imidazopyridinone preparation glun2b receptor modulator, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Application of 386704-04-7

Referemce:
Alcohol – Wikipedia,
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On July 27, 2020, Kato, Mikiya; Imazu, Takuya published a patent.Electric Literature of 386704-04-7 The title of the patent was Preparation of indazole derivatives as RORγt inhibitors. And the patent contained the following:

Provided are compounds I [R1 = H, halo, alkyl, etc.; R2 = H, halo or alkyl; R3a, R3b = independently H, halo, alkyl, etc.; R4a, R4b = independently H, halo or alkyl; R5 = CO2H or CO2R21; R21 = alkyl or alkenyl; R6a, R6b = independently H or alkyl; R7 = H, halo, cyano, etc.; R8 = H, halo, cyano, etc.; R9 = halo, alkyl, alkoxy, etc.; R10 = halo; Xa = single bond, cycloalkylene or alkynylene; n = 1 or 2; p = 0-2; q = 0-3; ring A = aryl, heteroaryl, cycloalkyl, etc.; or their pharmaceutically acceptable sats]. Thus, compound II was prepared via DIAD-mediated reaction of 7-chloro-1H-indazole-4-carboxylic acid Me ester with (trans-4-(trifluoromethyl)cyclohexyl)methanol, hydrolysis, amidation with 2-(trans-4-(aminomethyl)cyclohexyl)acetic acid Me ester·HCl in the presence of HATU, and hydrolysis. In RORγt (retinoic acid receptor-related orphan receptor-γt) inhibition assay, the invention compounds, e.g., II, showed IC50 value of <300 nM. Compounds I are claimed useful for the treatment of autoimmune diseases or allergic diseases. The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).Electric Literature of 386704-04-7

The Article related to indazole preparation ror gamma t inhibitor, autoimmune allergic disease treatment indazole ror gamma t inhibition, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Electric Literature of 386704-04-7

Referemce:
Alcohol – Wikipedia,
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On October 4, 2018, Kato, Masaya; Imazu, Takuya published a patent.HPLC of Formula: 386704-04-7 The title of the patent was Preparation of indazole derivatives as RORγt inhibitors. And the patent contained the following:

Provided are compounds I [R1 = H, halo, alkyl, etc.; R2 = H, halo or alkyl; R3a, R3b = independently H, halo, alkyl, etc.; R4a, R4b = independently H, halo or alkyl; R5 = CO2H or CO2R21; R21 = alkyl or alkenyl; R6a, R6b = independently H or alkyl; R7 = H, halo, cyano, etc.; R8 = H, halo, cyano, etc,; R9 = halo, alkyl, alkoxy, etc.; R10 = halo; Xa = single bond, cycloalkylene or alkynylene; n = 1 or 2; p = 0-2; q = 0-3; ring A = aryl, heteroaryl, cycloalkyl, etc.; or their pharmaceutically acceptable sats]. Thus, compound II was prepared via DIAD-mediated reaction of 7-chloro-1H-indazole-4-carboxylic acid Me ester with (trans-4-(trifluoromethyl)cyclohexyl)methanol, hydrolysis, amidation with 2-(trans-4-(aminomethyl)cyclohexyl)acetic acid Me ester·HCl in the presence of HATU, and hydrolysis. In RORγt (retinoic acid receptor-related orphan receptor-γt) inhibition assay, the invention compounds, e.g., II, showed IC50 value of <300 nM. Compounds I are claimed useful for the treatment of autoimmune diseases or allergic diseases. 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 indazole preparation ror gamma t inhibitor, autoimmune allergic disease treatment indazole ror gamma t inhibition, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.HPLC of Formula: 386704-04-7

Referemce:
Alcohol – Wikipedia,
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On December 8, 2011, Barnes, Michael Christopher Stratton; Flack, Stephen Sean; Fraser, Ian; Lumley, James Andrew; Pang, Pui Shan; Spencer, Keith Charles; Tiberghien, Nathalie Anne Laure; Tomkinson, Gary Peter published a patent.Safety of (6-(Trifluoromethyl)pyridin-3-yl)methanol The title of the patent was Preparation of benzodiazepine compounds useful for the treatment of hepatitis C. And the patent contained the following:

The invention concerns benzodiazepine derivatives of Formula I (L1 is O or NR8, wherein R8 is H, C1-6 alkyl, etc.; L2 is -(CR9R10)n-, wherein n = 1-6 and R9 and R10 independently are H, C1-6 alkyl, or cyclopropyl; A is aryl, a 5-6 membered monocyclic heteroaryl ring, etc.; R1 is H or fluoro; R2 is H, halo, C1-6 alkyl, etc.; R3 is H, C1-6 alkyl or halo; R4 is H, halo, C1-6 alkyl, etc.; R5 is H, halo, or C1-6 alkyl; R6 is H, halo, C1-6 alkyl, etc.; and R7 is H, C1-6 alkyl, halo, etc.; X is CH or N). The present invention also relates to processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the treatment or prophylaxis of hepatitis C virus infection. Example compound II was prepared by reacting 3-amino-5-(2,4,6-trichlorophenyl)-1,3-dihydrobenzo[e][1,4]diazepin-2-one hydrochloride and 2-(3-(2H-tetrazol-5-yl)propoxy)-5-chlorobenzoic acid. When tested in assays that measured HCV polymerase inhibitory activity and/or reduction of HCV replicon levels, all of the exemplified compounds of the invention had IC50 values < 10 μM, indicating that they are expected to possess useful therapeutic properties. The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).Safety of (6-(Trifluoromethyl)pyridin-3-yl)methanol

The Article related to benzodiazepine compound preparation treatment hepatitis c, Heterocyclic Compounds (More Than One Hetero Atom): Diazepines and other aspects.Safety of (6-(Trifluoromethyl)pyridin-3-yl)methanol

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

On October 15, 2020, Zhong, Wenge; Guo, Wei published a patent.Quality Control of (6-(Trifluoromethyl)pyridin-3-yl)methanol The title of the patent was Benzimidazole derivatives as Glp-1R agonists and their preparation, pharmaceutical compositions and use in the treatment of diseases. And the patent contained the following:

Provided herein are benzimidazole compounds of formula I and pharmaceutical compositions thereof, for use in, e.g. treating type 2 diabetes mellitus, pre-diabetes, obesity, non-alc. fatty liver disease, non-alc. steatohepatitis, and cardiovascular disease. Compounds of formula I wherein dashed double bond is either as single bond or a double bond; EE is COOH, -COCF3, -CH(OH)CF3, -CO-NH-CN, -CO-NH-OH, etc.; X1-X5 are independently N, CH; W is O, S, (un)substituted CH, NH and derivatives; ring B is 6-membered heteroaryl, 6-membered monocyclic ring, Ph; Y1 and Y3-Y4 are independently N, CH; T6-T8 are independently N, (un)substituted VH; ring C is cyclohexyl, Ph, pyridinyl; L is (un)substituted CH2, S, O, NH and derivatives; ring D is bicyclic heteroaryl; EE is COOH, -COCF3, -CH(OH)CF3, -CONH-CN, -CONH-OH, -CO-NH-OMe, etc.; Rb is H, C1-6 alkyl, C1-6 alkoxy, etc.; R1 is H, halo, CN, OH, C1-6 alkyl, C1-6 alkoxy, etc.; R2 is H, D, halo, CN, OH, oxo, C1-6 alkyl, etc.; R3 is H, D, CN, OH, oxo, C1-6 alkyl, C1-6 alkoxy, etc.; and their pharmaceutically acceptable salts, stereoisomers, solvates, hydrates as Glp-1R agonists in the treatment of diseases thereof, are claimed. Example compound II was prepared starting from 4-bromo-3-fluorobenzeneacetonitrile by using alcoholysis, heterocyclization, cross-coupling, and hydrolysis as the key steps. All the invention compounds were evaluated for their Glp-1R agonistic activity. The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).Quality Control of (6-(Trifluoromethyl)pyridin-3-yl)methanol

The Article related to benzimidazole derivative preparation glp1r agonist treatment disease, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.Quality Control of (6-(Trifluoromethyl)pyridin-3-yl)methanol

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

On June 11, 2015, Kane, John L., Jr.; Matthews, Gloria; Metz, Markus; Kothe, Michael; Liu, Jinyu; Scholte, Andrew published a patent.Category: alcohols-buliding-blocks The title of the patent was Benzimidazole and imidazopyridine derivatives as tropomyosin-related kinase (Trk) inhibitors and their preparation and use for the treatment of diseases. And the patent contained the following:

The invention relates to benzimidazole and imidazopyridine derivatives of formula I, which are tropomyosin-related kinase (Trk) inhibitors and which are useful in the treatment of diseases. Compounds of formula I wherein Q1 is H, halo, (un)substituted C6-14 aryl, etc.; Q2 is (un)substituted C6-14 aryl, (un)substituted C2-9 heteroaryl, etc.; R1 is H, halo, C1-10 alkyl, etc.; R2 is H, halo, C1-10 alkyl, C1-10 alkoxy, etc.; L is (CR3R4)1-5; R3 and R4 are independently H, NH2, C1-10 alkyl, etc.; Z is (CR5R6)0-4; R5 and R6 are independently H, NH2, C1-10 alkyl, etc.; X is CH, halo, NH, etc.; and pharmaceutically acceptable salts thereof, are disclosed. Example compound II was prepared by a multistep procedure (procedure given). All the invention compounds were evaluated for their Trk inhibitory activity. From the assay, it was determined that compound II exhibited IC50 values of 0.001 μM and 0.0005 μM towards TrkA and TrkB, resp. The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).Category: alcohols-buliding-blocks

The Article related to imidazopyridine preparation trk inhibitor treatment disease, benzimidazole preparation trk inhibitor treatment disease, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.Category: alcohols-buliding-blocks

Referemce:
Alcohol – Wikipedia,
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On June 21, 2012, Yamamoto, Shuji; Ohta, Hiroshi; Abe, Kumi; Araki, Yuko; Moriya, Minoru; Sun, Xiang-Min; Yasuhara, Akito published a patent.Recommanded Product: 386704-04-7 The title of the patent was Preparation of imidazolidin-2-one derivatives for inhibiting glycine transporter. And the patent contained the following:

Title compounds I [R1 = Ph, pyridyl, pyridazyl, etc. (herein, Ph, pyridyl and pyridazyl are optionally substituted with group 1); group 1 = alkyl, haloalkyl, alkoxy, etc.; R2 = Ph (optionally substituted with group 2) or mono- or bi-cyclic heteroaryl (optionally substituted with group 2); group 2 = Ph, alkyl, haloalkyl, etc.; R3, R4 = H, alkyl, cycloalkyl, etc.; R3 and R4, together with the carbon atom to which they are attached, may combine to form a cycloalkane, THF or tetrahydropyran; with a proviso that R3 and R4 cannot be hydrogen atom simultaneously; R5, R6 = H or alkyl; or pharmaceutically acceptable salts thereof] were prepared For example, to a solution of 3-(6-methoxypyridin-3-yl)-1,3-diazaspiro[4.5]decan-2-one (100 mg) in DMF (2 mL) was added NaH (23 mg), the resulting mixture was stirred for 30 min and treated with 5-(chloromethyl)-3-phenyl-1,2-oxazole (110 mg) at room temperature overnight to give, after work-up, compound II (109 mg). In glycine uptake inhibition assay, IC50 of III was 0.038 μM. Compounds I are claimed useful for the treatment of schizophrenia, Alzheimer disease, depression, etc. The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).Recommanded Product: 386704-04-7

The Article related to imidazolidinone preparation glycine transporter inhibitor, schizophrenia alzheimer disease depression treatment imidazolidinone glycine transporter inhibition, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.Recommanded Product: 386704-04-7

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

On December 18, 2014, Ikegami, Satoru; Watanabe, Atsushi; Hirano, Kimio; Ohyama, Tadashi published a patent.Application of 386704-04-7 The title of the patent was Preparation of 4-alkynyl imidazole derivatives for the treatment of EP4 receptor-related diseases. And the patent contained the following:

The present invention provides 4-alkynyl imidazole derivatives I [ring A = (un)substituted cycloalkyl, aryl or heteroaryl; ring B = cycloalkyl, aryl or heteroaryl; m = 0-2; n = 1-3; R1 = H, alkyl, alkoxy, etc.; R2 and R3 = independently H, halogen, alkyl or carbocyclic ring when taken together; R4 and R5 = independently H, alkyl or carbocyclic ring when taken together; R6 and R7 = independently H, alkyl, alkoxy, etc.; X = OR8, NR9R10 or halogen; R8 = H, alkyl or haloalkyl; R9 and R10 = independently H, alkyl or heterocycle when taken together; Y = single bond, O or S; E = CO2H, CO2P or biol. equivalent of carboxyl group; CO2P = pharmacol. acceptable ester prodrug] and their pharmaceutically acceptable salts. Thus, compound II (preparation given) was subjected to a coupling reaction with 4-(1-aminocyclopropyl)benzoic acid Me ester followed by O-methylation and hydrolysis to provide compound III. Compound III exhibited antagonistic activity against rat EP4 receptor with an IC50 value of 1.7 nmol/L. The invention compounds have excellent EP4 receptor antagonist effects and are useful as medicines for treating diseases associated with EP4 receptors, for example, anti-inflammatory agents and/or analgesics for inflammatory diseases and diseases associated with various kinds of pain, and also as medicines for treating immune diseases that occur as a result of Th1 cell and/or Th17 cell activation, which causes tissue destruction and gives rise to inflammation. 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 alkynyl imidazole derivative preparation ep4 receptor antagonist, inflammatory disease pain immune disease treatment antiinflammatory agent, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.Application of 386704-04-7

Referemce:
Alcohol – Wikipedia,
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On July 5, 2007, Buettelmann, Bernd; Han, Bo; Knust, Henner; Thomas, Andrew published a patent.SDS of cas: 386704-04-7 The title of the patent was Preparation of arylisoxazolyl imidazoles as GABAA α5 receptor ligands for the treatment of cognitive disorder and Alzheimer’s disease. And the patent contained the following:

Title compounds I [wherein R1, R2, R3 = H or halo; R4 = H, alkyl, cycloalkyl, etc.; R5 = (un)substituted (CH2)m-(hetero)aryl; m = 0-1; R6 = H, CHO, cycloalkyl, etc.] and pharmaceutically acceptable acid addition salts thereof were prepared as GABAA α5 receptor ligands. For instance, II was synthesized in 43% yield by N-alkylation of the corresponding imidazole with 4-fluoroacetophenone. This compound has a Ki value of 4.7 nM for displacement of [3H]flumazenil from GABAA α5 subunits. I and their pharmaceutical compositions are useful for the treatment of diseases related to the GABAA a5 subunits, such as cognitive disorder and Alzheimer’s disease. 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 arylisoxazolyl imidazole preparation gabaa receptor ligand cognitive enhancer antialzheimer, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.SDS of cas: 386704-04-7

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

On March 23, 2017, Axten, Jeffrey Michael; Faucher, Nicolas Eric; Daugan, Alain Claude-Marie published a patent.Product Details of 386704-04-7 The title of the patent was Preparation of imidazolidinone derivatives as inhibitors of PERK. And the patent contained the following:

The title imidazolidinones I [R1 = (un)substituted bicycloheteroaryl, heteroaryl; R2 = alkyl, (un)substituted aryl, heteroaryl, etc.; R3 = H, NH2, NH(alkyl), etc.; R4 and R5 = (independently) H and alkyl; R4 and R5 taken together with the carbon atoms to which they are attached form 3-4 membered cycloalkyl, optionally substituted with 1-3 alkyl; R6 = H, alkyl, CF3, etc.; R7 = H, alkyl, CF3, etc.; X = N or (un)substituted CH; Y1 and Y2 = (independently) H, CF3, alkyl; or Y1 and Y2 are taken together with the carbon to which they are attached to form C3-6 cycloalkyl; z = 0-1] or salts thereof including a pharmaceutically acceptable salts thereof, which are inhibitors of PERK and can be useful in the treatment of cancer, pre-cancerous syndromes, Alzheimer’s disease, neuropathic pain, etc., were prepared and formulated. E.g., a multi-step synthesis of II, starting from 4-bromo-3-fluoroaniline and 1-chloro-2-isocyanatoethane, was described. Exemplified compounds I were tested for activity against PERK (data given). Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound I. The invention is still further directed to methods of inhibiting PERK activity and treatment of disorders associated therewith using a compound I or a pharmaceutical composition comprising I. The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).Product Details of 386704-04-7

The Article related to imidazolidinone preparation perk inhibitor antitumor analgesic alzheimer’s disease, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.Product Details of 386704-04-7

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts