pyrazoles-derivatives

On January 16, 2020, Brace, Gareth Neil; Brookings, Daniel Christopher; Foulkes, Gregory; Lecomte, Fabien Claude published a patent.Name: 1-(Tetrahydro-2H-pyran-4-yl)-1H-pyrazole-4-carboxylic acid The title of the patent was Spirocyclic indane analogs as IL-17 modulators and their preparation. And the patent contained the following:

A series of substituted spirocyclic indane derivatives of formula I, and analogs thereof, being potent modulators of human IL-17 activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including inflammatory and autoimmune disorders. Compounds of formula I wherein ring A is C3-9 cycloalkyl, C3-7 heterocycloalkyl and C4-9 heterobicycloalkyl; B is CR2 and N; D is CR3 and N; E is CR4 and N; XY is OCY1Y2, NHSO2 and derivatives, CO2, etc.; R1 is (un)substituted C1-6 alkyl, (un)substituted C3-9 cycloalkyl, (un)substituted aryl, (un)substituted heteroaryl, etc.; R2, R3 and R4 H, halo, CN, C1-6 alkyl, etc.; Y1 is H, halo, CN, CF3, etc.; Y2 is H, halo and C1-6 alkyl; and N-oxides as pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by amidation of lithium 2-cyclooctyl-2-(3-methylisoxazole-4-carboxamido)acetate with spiro[indene-1,4′-oxane]-5-amine. The invention compounds were evaluated for their IL-17 modulatory activity (some data given). The experimental process involved the reaction of 1-(Tetrahydro-2H-pyran-4-yl)-1H-pyrazole-4-carboxylic acid(cas: 1340372-11-3).Name: 1-(Tetrahydro-2H-pyran-4-yl)-1H-pyrazole-4-carboxylic acid

The Article related to spirocyclic indane preparation il17 modulator, Heterocyclic Compounds (One Hetero Atom): Spiro Compounds With One Hetero Atom In Each Ring and other aspects.Name: 1-(Tetrahydro-2H-pyran-4-yl)-1H-pyrazole-4-carboxylic acid

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On December 24, 2008, Sprott, Kevin; Talley, John Jeffrey; Pearson, James Philip; Milne, Todd G. published a patent.Formula: C9H7N3O2 The title of the patent was Indole derivatives as FAAH inhibitors and their preparation and use in the treatment of diseases. And the patent contained the following:

Indole derivatives of formula I that are useful for treating pain, inflammation and other conditions are described. Certain of the compounds are benzyl derivatives and others are benzoyl derivatives The compounds are substituted at least at the 3 position of the indole. Compounds of formula I wherein each V, W, X, Y, Z, J, K, L and M are independently N and C; each P1 – P6 are independently N and C; each Q1 – Q6 are independently N and C; A and A’ are independently OH, and (un)substituted C1-3 alkoxy; AA’ taken together to form =O, =NOH, and =NOMe, etc.; dashed bonds indicated single and double bonds; R2 is halo, OH, NO2, (un)substituted C1-5 alkyl, (un)substituted C1-5 alkoxy, etc.; each of R4 – R17 is absent when bonded to N; each one of R4 – R17 is H, halo, NO2, CN, CO2H, OH, etc.; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was tested for its FAAH inhibitory activity. From the assay, it was determined that compound II exhibited IC50 valued of < 1 μM. The experimental process involved the reaction of 1-(Pyridin-3-yl)-1H-pyrazole-4-carboxylic acid(cas: 1014631-89-0).Formula: C9H7N3O2

The Article related to indole preparation faah inhibitor treatment disease, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Formula: C9H7N3O2

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Xu, Juan; Zhao, Xinyu; Kang, Congmin published an article in 2018, the title of the article was Improved synthesis of pyrazolo[1,5-a]pyridine-3-carboxylic acid derivatives.Product Details of 143803-93-4 And the article contains the following content:

Pyrazolo[1,5-a]pyridine-3-carboxylate derivatives were obtained from 1,3-dipolar cycloaddition reaction with Et propynoate and N-aminopyridine sulfate synthesized by the reactions of substituted pyridines and hydroxyamine-O-sulfonic acid. They were further treated with 30% NaOH aqueous solution to give corresponding substituted pyrazolo[1,5-a]pyridine-3-carboxylic acid derivatives In this method, N-aminopyridine sulfate was directly put into the next reaction, which eliminated the step of converting sulfate into iodine salt in the traditional method and solved the problem that the iodine salt was difficult to precipitate N-aminopyridine sulfate and Et propynoate were dissolved in water and N,N-dimethylformamide, resp., and then mixed to increase the solubility of reactants. Six compounds (4a∼4f) were successfully synthesized with yields of 88%∼93%. The method is mild and easy to process and has low cost as a new process for mass production The experimental process involved the reaction of 4-Methylpyrazolo[1,5-a]pyridine-3-carboxylic acid(cas: 143803-93-4).Product Details of 143803-93-4

The Article related to pyrazolopyridine carboxylic acid derivative synthesis, Industrial Organic Chemicals, Leather, Fats, and Waxes: Manufacture Of Industrial Organic Chemicals and other aspects.Product Details of 143803-93-4

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On February 14, 2008, Talley, John Jeffrey; Sprott, Kevin; Pearson, James Philip; Milne, G. Todd; Schairer, Wayne; Yang, Jing Jing; Kim, Charles; Barden, Timothy; Lundigran, Regina; Mermerian, Ara; Currie, Mark G. published a patent.Synthetic Route of 1014631-89-0 The title of the patent was Indole compounds for treating pain, inflammation and other conditions. And the patent contained the following:

The title indoles such as I [V, W, X, Y, Z, J, K, L and M = N or C; P1-P6 = N or C; Q1-Q5 = N or C; A and A1 = OH or (un)substituted alkoxy; or A and A1 taken together = O, N(OH), N(OMe); or A and A1 together with the carbon atom to which they are attached form a cyclic ketal containing a total of 4 or 5 carbon atoms which can be optionally substituted; R2 = halo, OH, NO2, etc.; R4-R17 = absent, H, halo, NO2, etc.; with the provisos] that are useful for treating pain, inflammation and other conditions are described. Certain of the compounds I are benzyl derivatives and others are benzoyl derivatives The compounds I are substituted at least at the 3 position of the indole. General synthetic methods for the preparation of compounds I are described. E.g., a multistep synthesis of {1-[(5-chlorothien-2-yl)carbonyl]-6-fluoro-5-hydroxy-2-methyl-1H-indole-3-yl}acetic acid, starting from 3-fluoro-4-methoxyaniline, was given. Pharmaceutical composition comprising the compound I is disclosed. The experimental process involved the reaction of 1-(Pyridin-3-yl)-1H-pyrazole-4-carboxylic acid(cas: 1014631-89-0).Synthetic Route of 1014631-89-0

The Article related to indole preparation analgesic antiinflammatory faah dao related disorder treatment, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Synthetic Route of 1014631-89-0

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On April 3, 2014, Eskildsen, Joergen published a patent.Recommanded Product: 1-(Tetrahydro-2H-pyran-4-yl)-1H-pyrazole-4-carboxylic acid The title of the patent was Preparation of indolylalkylamide derivatives for use as positive allosteric modulators of nicotinic acetylcholine receptor. And the patent contained the following:

Title compounds I [R1, R2, R4, and R5 independently = H, F, CN, (un)substituted alkyl, alkenyl, or alkynyl; R3 = H, CN, (un)substituted alkyl, alkenyl, or alkynyl; R6 = H or Me; Q = substituted isoxazolyl, isothiazolyl, or pyrazolyl], and their pharmaceutically acceptable salts, are prepared and disclosed as pos. allosteric modulators (PAMs) of the nicotinic acetylcholine α7 receptor. Thus, e.g., II was prepared by a multistep procedure (preparation given). I were evaluated in α7 NNR receptor PAM flux activity assays, e.g., II demonstrated an EC50 value of 2200 nM. The experimental process involved the reaction of 1-(Tetrahydro-2H-pyran-4-yl)-1H-pyrazole-4-carboxylic acid(cas: 1340372-11-3).Recommanded Product: 1-(Tetrahydro-2H-pyran-4-yl)-1H-pyrazole-4-carboxylic acid

The Article related to indolylalkylamide preparation pos allosteric modulators nicotinic acetylcholine receptor, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Recommanded Product: 1-(Tetrahydro-2H-pyran-4-yl)-1H-pyrazole-4-carboxylic acid

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On August 7, 2014, Okura, Hironari; Kitajima, Kazuki; Kawahara, Atsuko; Wakita, Takeo; Kawase, Ayumi; Nomura, Michikazu published a patent.Electric Literature of 1014631-89-0 The title of the patent was Preparation of heterocyclic compounds as pest control agents. And the patent contained the following:

Disclosed are compounds I [G1 = nitrogen, carbon atom or CH; R1 = H, halo, cyano, etc.; m = 1-3; n = 0 or 1; Hy = 5- or 6-membered aromatic ring represented by Q1 (*2 is connection position to G2); A1 = carbon or nitrogen atom; A2 = carbon or sulfur atom; A3 = carbon or nitrogen atom; A4 = carbon or nitrogen atom; with a proviso that A1 and A2 cannot be carbon atom simultaneously; p = 0-2; q = 0 or 1; R2 = H, halo, alkyl, etc.; G2 = Q2 (*1 is connection position to Hy); Q = oxygen atom or NR5; R5 = H, alkyl, cycloalkyl, etc.; R3 = H, alkyl, cycloalkyl, etc.; R4 = alkyl, cycloalkyl, alkenyl, etc.; or salts thereof]. For example, compound II was prepared via reaction of thionicotinamide with chloroacetylacetone, condensation reaction with NH2OH and carbamoylation with ethylisocyanate. The invention compounds, e.g., II, showed ≥70% pesticidal activities for Laodelphax striatellus and Myzus persicae. The experimental process involved the reaction of 1-(Pyridin-3-yl)-1H-pyrazole-4-carboxylic acid(cas: 1014631-89-0).Electric Literature of 1014631-89-0

The Article related to heterocycle preparation pest control agent, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.Electric Literature of 1014631-89-0

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On January 17, 2019, Hoffman, Thomas James; Stierli, Daniel; Pitterna, Thomas; Rajan, Ramya published a patent.Application of 215610-30-3 The title of the patent was Preparation of oxadiazole derivatives as microbicides. And the patent contained the following:

Compounds of the formula I useful as pesticides, especially as fungicides. Compounds of formula I wherein Z is substituted pyrazolyl; R1, R2, R3 and R4 are independently H and F, provided that 0 – 2 of R1 – R4 are F; R5 and R6 are independently H and Me; and salts and N-oxides thereof, are claimed. Example compound II was prepared by amidation of 1-[[4-[5-(trifluoromethyl)-1,2,4-oxadiazol-3-yl]phenyl]methyl]pyrazole-4-carboxylic acid with N-cyclopropylethylamine. The invention compounds were evaluated for their fungicidal activity (data given). The experimental process involved the reaction of 5-Methoxy-1H-pyrazole(cas: 215610-30-3).Application of 215610-30-3

The Article related to oxadiazole preparation fungicide microbicide, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.Application of 215610-30-3

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On September 6, 2019, Tang, Haifeng; Boyce, Sarah; Hanson, Michael; Nie, Zhe published a patent.Name: 5-Methoxy-1H-pyrazole The title of the patent was Compounds and compositions for treating conditions associated with APJ receptor activity. And the patent contained the following:

The invention relates to substituted triazoles of formula I and pharmaceutically acceptable salts thereof (wherein R1 is (Y1)0-1Y2; Y1 is (un)substituted C1-6 alkylene; Y2 is (un)substituted C3-10 cycloalkyl, (un)substituted C6-10 aryl, (un)substituted heteroaryl, etc.; R2 is (un)substituted C6-10 aryl, (un)substituted heteroaryl; R3 is (Y3)0-1Y4; Y3 is (un)substituted C1-6 alkylene; Y4 is (un)substituted C3-6 cycloalkyl, (un)substituted C6-10 aryl, (un)substituted 5- to 10-membered heteroaryl; R4 is H and C1-3 alkyl;) as apelin receptor modulators; their preparation and use in the treatment of pulmonary arterial hypertension. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their APJ modulatory activities. From the assay, it was determined that compound II exhibited EC50 value of less than 1 nM. The experimental process involved the reaction of 5-Methoxy-1H-pyrazole(cas: 215610-30-3).Name: 5-Methoxy-1H-pyrazole

The Article related to triazole preparation apj receptor modulator treatment pulmonary arterial hypertension, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.Name: 5-Methoxy-1H-pyrazole

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Kamal, Raj; Kumar, Vipan; Kumar, Ravinder; Kumar, Vikas; Sharma, Prabodh C.; Bansal, Kushal K. published an article in 2019, the title of the article was Chloramine-T Mediated Facile One Pot Synthesis of Pyrazolyltriazolobenzothiazole Hybrids as Potent Anti-Infective Agents.Reference of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde And the article contains the following content:

An expedient and facile one pot synthesis of 3-(3-aryl-1-phenyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[3,4-b]-1,3-benzothiazole derivatives I (R = 4-methoxyphenyl, 3-nitrophenyl, 2-naphthyl, etc.) through in situ oxidative cyclization of corresponding N-heteroarylhydrazone promoted by environmentally benign chloramines-T trihydrate at room temperature has been accomplished. All synthesized pyrazolyltriazolobenzothiazole hybrids I were also evaluated for their antibacterial and anthelmintic potentials and found to be moderate to significant anti-infective agents. The experimental process involved the reaction of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde(cas: 36640-53-6).Reference of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde

The Article related to pyrazolyl triazolobenzothiazole preparation green chem antibacterial anthelmintic activity, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.Reference of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Vlasenko, Yulia A.; Kuczmera, Thomas J.; Antonkin, Nikita S.; Postnikov, Pavel S.; Nachtsheim, Boris J. published an article in 2022, the title of the article was Site selective nucleophilic aromatic substitutions of azole-ligated diaryliodonium salts.SDS of cas: 57446-04-5 And the article contains the following content:

Herein the application of azole-stabilized diaryliodonium salts with addnl. thiophen-2-yl-ligands as substrates for metal-free nucleophilic arylations was presented. Besides their synthesis, their application in chemoselective nitrations, oxygenations, aminations as well as thiolations under umpolung conditions was demonstrated. Convenient one-pot procedures that are based on their in situ formation are also discussed. The experimental process involved the reaction of Methyl 3-(2-nitrophenyl)-1H-pyrazole-5-carboxylate(cas: 57446-04-5).SDS of cas: 57446-04-5

The Article related to diaryliodonium triflate regioselective nucleophilic aromatic nitration reaction, nitro biaryle preparation, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.SDS of cas: 57446-04-5

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics