Tag: 100-200

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

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 August 31, 2017, Chappie, Thomas Allen; Patel, Nandini Chaturbhai; Verhoest, Patrick Robert; Helal, Christopher John; Sciabola, Simone; Lachapelle, Erik Alphie; Wager, Travis T.; Hayward, Matthew Merrill published a patent.Reference of Ethyl 6,7-dihydro-5H-pyrazolo[5,1-b][1,3]oxazine-2-carboxylate The title of the patent was 6,7-Dihydro-5H-pyrazolo[5,1-b][1,3]oxazine-2-carboxamide compounds as PDE4 inhibitors and their preparation. And the patent contained the following:

The invention is directed to PDE4B inhibitors of formula Ior a pharmaceutically acceptable salt thereof. The invention is also directed to pharmaceutical compositions comprising the compounds, methods of treatment using the compounds, and methods of preparing the compounds Compounds of formula I wherein R1 is (un)substituted C3-8 cycloalkyl, (un)substituted C6-10 aryl, (un)substituted 5- to 10-membered heteroaryl, etc.; R2 and R3 are independently H, (un)substituted C1-6 alkyl, (un)substituted C3-8 cycloalkyl, (un)substituted C6-10 aryl, etc.; n is 0, 1, 2 and 3; each R4 is independently halo, CN, OH, SF5, NO2, etc.; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by cross-coupling of azetidin-1-yl(3-bromo-6,7-dihydro-5H-pyrazolo[5,1-b]oxazin-2-yl)methanol with 4-chloro-2-methylphenylboronic acid. The invention compounds were evaluated for their PDE4 inhibitory activity. From the assay, it was determined that compound II exhibited IC50 values of 211 nM, 241 nM and 653 nM towards PDE4B1, PDE4A3 and PDE4C1, resp. The experimental process involved the reaction of Ethyl 6,7-dihydro-5H-pyrazolo[5,1-b][1,3]oxazine-2-carboxylate(cas: 153597-59-2).Reference of Ethyl 6,7-dihydro-5H-pyrazolo[5,1-b][1,3]oxazine-2-carboxylate

The Article related to pyrazolooxazinecarboxamide preparation pde4 inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Oxazines (Including Morpholine) and other aspects.Reference of Ethyl 6,7-dihydro-5H-pyrazolo[5,1-b][1,3]oxazine-2-carboxylate

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

On July 8, 2010, Chuaqui, Claudio; Cossrow, Jennifer; Dowling, James; Guan, Bing; Hoemann, Michael; Ishchenko, Alexey; Jones, John Howard; Kabigting, Lori; Kumaravel, Gnanasambandam; Peng, Hairuo; Powell, Noel; Raimundo, Brian; Tanaka, Hiroko; Van Vloten, Kurt; Vessels, Jeffrey; Xin, Zhili published a patent.Product Details of 1014631-89-0 The title of the patent was Preparation of heteroaryl compounds useful as Raf kinase inhibitors. And the patent contained the following:

The present invention provides compounds I [Cy1 = (un)substituted phenylene, 5-6 membered saturated or partially unsaturated carbocyclylene, 7-10 membered saturated or partially unsaturated bicyclic carbocyclylene, etc.; Cy2 = (un)substituted Ph, 5-8 membered saturated or partially unsaturated carbocyclic ring, 7-10 membered saturated or partially unsaturated bicyclic carbocyclic ring, etc.; L1 = (un)substituted alkylene; L2 = NR1 or C(O)NR1; R, R1 = H, (un)substituted alkyl; ring A = (un)substituted imidazopyridinyl, imidazopyrazinyl; pyrazolopyridinyl, imidazolyl, thiazolyl, etc.] which are useful as inhibitors of Raf protein kinase. Over three-hundred-fifty compounds I were prepared E.g., a multi-step synthesis of the amide II, starting from III, was given. Exemplified compounds were assayed for Raf kinase activity and were found to be inhibitors of Raf kinase (data given). The present invention also provides compositions comprising I, and methods of treating Raf-mediated diseases. The experimental process involved the reaction of 1-(Pyridin-3-yl)-1H-pyrazole-4-carboxylic acid(cas: 1014631-89-0).Product Details of 1014631-89-0

The Article related to heteroaryl imidazopyridine imidazopyrazine pyrazolopyridine imidazole preparation raf kinase inhibitor, amide carboxamide thiazole pyridine preparation raf kinase inhibitor and other aspects.Product Details of 1014631-89-0

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

On May 6, 1992, Higashino, Takeo; Suzuki, Yukio; Sasahara, Takehiko; Saito, Tetsu; Mochizuki, Daisuke published a patent.COA of Formula: C9H8N2O2 The title of the patent was Preparation of pyrazolo[1,5-a]pyridine-3-carboxylic acid as serotonin 3-receptor binding antagonists. And the patent contained the following:

The title compounds (I; R1, R2 = H, alkyl; R3 = azabicyclo groups Q, Q1; Y = O, NH; Z = alkyl; n = 2, 3) or their salts, useful as antianxietics and antiemetics, especially for reducing nausea and vomiting due to side effects of an carcinostatic agent, were prepared, e.g., by amidation of pyrazolo[1,5-a]pyridinecarboxylic acids by azabicycloalkanamines. Thus, 7-methyl-3-pyrazolo[1,5-a]pyridinecarboxylic acid [J. Organic Chem. 33(5), 2062-4 (1968)] was refluxed in SOCl2 for 30 min., distilled, and the residue refluxed for 24 h with endo-8-methyl-8-azabicyclo[3.2.1]oct-3-yl-7-methylpyrazolo[1,5-a]pyridine-3-carboxamide (II). The latter in a 3H-quipazine binding assay in vitro had IC50 = 19.1 nM. II at 0.1 mg/kg i.v. in beagles prevented vomiting following administration of 3 mg/kg i.v. cisplatin. The experimental process involved the reaction of 4-Methylpyrazolo[1,5-a]pyridine-3-carboxylic acid(cas: 143803-93-4).COA of Formula: C9H8N2O2

The Article related to pyrazolopyridine preparation antiemetic antianxietic, nausea cisplatin prevention pyrazolopyridine preparation, vomiting cisplatin prevention pyrazolopyridine preparation and other aspects.COA of Formula: C9H8N2O2

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

On September 23, 2021, Holson, Edward; Blum, Charles published a patent.Electric Literature of 1014631-89-0 The title of the patent was Preparation of benzenesulfonamide derivatives as TRAP1 modulators and uses thereof. And the patent contained the following:

The disclosure provides compounds of formula I and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled compounds, and prodrugs thereof. The provided compounds may be tumor necrosis factor (“”TNF””) receptor associated protein 1 (“”TRAP1″”) modulators (e.g., TRAP1 activators). The provided compounds of formula I may also rescue the activity in PTEN-induced kinase 1 (“”PINK1″”) loss of function contexts. The provided compounds of formula I may also improve mitochondrial health, function, quality, quantity, and/or activity, and/or reduce the production of reactive oxygen species. The provided compounds of formula I may also refold or solubilize aggregated or misfolded proteins such as α-synuclein. The disclosure also provides pharmaceutical compositions comprising the provided compounds; kits comprising the provided compounds or pharmaceutical compositions; and methods of using the provided compounds and pharmaceutical compositions (e.g., for treating a disease in a subject in need thereof). Compounds of formula I wherein A and E are independently aryl and heteroaryl; dashed bonds are single and double bonds are valency permits; m is 0, 1 and 2; n and p are independently 0 – 13; each R1 is independently halo, (un)substituted alkyl, (un)substituted alkenyl, (un)substituted alkynyl, etc.; R3 and R6 are independently H, (un)substituted alkyl and nitrogen protecting group; R1R3 may be taken together to form (un)substituted heterocyclyl; each R4 is independently halo, (un)substituted alkyl, (un)substituted alkenyl, (un)substituted aryl, etc.; R5 and R9 are independently H, halo, (un)substituted alkyl, (un)substituted alkenyl, (un)substituted alkynyl, etc.; each R7 is independently (un)substituted alkyl, (un)substituted alkenyl, (un)substituted alkynyl, (un)substituted aryl, etc.; and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled compounds, and prodrugs thereof, are claimed. Example compound II was prepared by amidation of oxazole-5-carboxylic acid with 5-amino-N-(4-bromophenyl)-2-methoxybenzenesulfonamide. The invention compounds were evaluated for their TRAP1 modulatory activity. From the assay, it was determined that compound II exhibited an EC50 value in the range of 20μM to 100μM and an Emax value in the range of 160 – 199%. 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 benzenesulfonamide preparation trap1 modulator, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Amides, Amidines, Imidic Esters, Hydrazides, and Hydrazonic Esters and other aspects.Electric Literature of 1014631-89-0

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

On July 29, 2022, Perma Tenzin, Puno; Sun, Handong; Zhou, Yuanfei; Yan, Bingchao; Yang, Qian; Du, Xue; Hu, Kun published a patent.Related Products of 1014631-89-0 The title of the patent was Preparation of ent-kauranoid derivatives as antitumor drugs. And the patent contained the following:

The invention discloses a preparation of ent-kauranoid derivatives I [wherein R=(un)substituted C3-C8 alkyl and cycloalkyl, heterocyclic group containing N, O, S, substituted Ph, etc.] as antitumor drugs, which has the advantages of easy availability of raw materials, high yield and good anti-tumor effect. For example, (3aS,5aR,6S,7aR,10S,12aS,12bR,13R)-6-hydroxy-5,5-dimethyl-9-methylene-3,7,8-trioxododecahydro-1H,3H-7a,10-methanocyclohepta[6,7]indeno[1,7a-c]furan-13-yl butyrate was prepared by the following steps: oxidation of oridonin; selective reduction; diazotization; oxidation; rearrangement reaction; cyclization to obtain calyx lactone B; esterification. The title compound is used to prepare anti-tumor drugs, and tumors include cervical cancer, colon cancer, ovarian cancer, lung cancer, prostate cancer, breast cancer and liver cancer. The experimental process involved the reaction of 1-(Pyridin-3-yl)-1H-pyrazole-4-carboxylic acid(cas: 1014631-89-0).Related Products of 1014631-89-0

The Article related to preparation ent kauranoid antitumor oxidation reduction diazotization cyclization esterification, Terpenes and Terpenoids: Diterpenes (C20), Including Gibberellins, Retinoids, Quassinoids, and Tocopherols and other aspects.Related Products of 1014631-89-0

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

On April 1, 2021, Xie, Yinong; Babiss, Lee E. published a patent.SDS of cas: 98138-75-1 The title of the patent was Preparation of SHP2 inhibitors for treatment of cancer. And the patent contained the following:

Disclosed are compounds of formula I, useful as inhibitors of protein tyrosine phosphatase SHP2 for the treatment of cancer. Compounds of formula I [wherein X = S; Ring A = (un)substituted aryl having 6-10 carbons, (un)substituted 5- to 6-membered mono-cyclic heteroaryl, or (un)substituted bicyclic ring system having 5-10 ring carbons; RA and RB independently = H or C1-12 hydrocarbyl, or N(RA)(RB) optionally = substituted heterocyclic ring system] or pharmaceutically acceptable salts thereof, are claimed and exemplified. Thus, disubstituted 1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one II was prepared from a multistep synthesis (preparation given). Exemplified I were evaluated for inhibition of SHP2 from which II demonstrated an IC50 = ≤ 50 nM. The pharmaceutical compositions comprising compounds of Formula I, methods of synthesis of these compounds, methods of treatment for diseases associated with the aberrant activity of SHP2 such as cancer using these compounds or compositions containing these compounds are also disclosed. The experimental process involved the reaction of 6-Chloro-4-methoxy-1H-pyrazolo[3,4-d]pyrimidine(cas: 98138-75-1).SDS of cas: 98138-75-1

The Article related to dihydropyrazolopyrimidinone preparation shp2 inhibitor preparation inhibitor cancer, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.SDS of cas: 98138-75-1

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

On September 26, 2019, Xie, Yinong; Babiss, Lee E. published a patent.Category: pyrazoles-derivatives The title of the patent was Preparation of SHP2 inhibitors and uses thereof. And the patent contained the following:

The invention relates to compounds of formula I and their preparation, useful as inhibitors of protein tyrosine phosphatase SHP2 in the treatment of diseases such as cancer. Compounds of formula I are claimed, in which ring A is (un)substituted aryl, heteroaryl, and bicyclic ring system; X is S, O, NRa, CHRa, S(O), SO2, C(O), or bond; Ra is H and C1-6 hydrocarbyl; ring B is (un)substituted mono-, bi-, tri-, or tetracyclic heterocyclic ring system containing heteroaryl and at least two ring N atoms; and pharmaceutically acceptable salts thereof. Example compound II was prepared via a multistep process with key step of coupling tert-Bu ((1-(5-chloro-4-cyano-1-methyl-6-oxo-1,6-dihydropyrimidin-2-yl)-4-methylpiperidin-4-yl)methyl)carbamate with 2,3-dichlorophenylboronic acid followed by deprotection. Invention compounds were evaluated for their SHP2 inhibitory activity (data given). The experimental process involved the reaction of 6-Chloro-4-methoxy-1H-pyrazolo[3,4-d]pyrimidine(cas: 98138-75-1).Category: pyrazoles-derivatives

The Article related to shp2 inhibition treatment cancer, heteroaromatic preparation, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Category: pyrazoles-derivatives

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

On August 29, 2019, Walters, W. Patrick; Lescarbeau, Andre; Kelley, Elizabeth H.; Shortsleeves, Kelley C.; Taylor, Alexander M.; Pierce, Levi Charles Thomas; Murcko, Mark Andrew; Giordanetto, Fabrizio; Greisman, Jack Benjamin; Maragakis, Paul; Bhat, Sathesh; Konze, Kyle; Dahlgren, Markus Kristofer; Therrien, Eric published a patent.Quality Control of 6-Chloro-4-methoxy-1H-pyrazolo[3,4-d]pyrimidine The title of the patent was Preparation of heterocyclic compounds as SHP2 phosphatase inhibitors. And the patent contained the following:

The present disclosure relates to novel compounds and pharmaceutical compositions thereof, and methods for inhibiting the activity SHP2 phosphatase with the compounds and compositions of the disclosure. The present disclosure further relates to, but is not limited to, methods for treating disorders associated with SHP2 deregulation with the compounds and compositions of the disclosure. Example compound I•formate was prepared by cyclocondensation of tert-Bu (1-(5-amino-1,3,4-thiadiazol-2-yl)-3-methylpiperidin-3-yl)carbamate with 2,3-dichlorobenzaldehyde and 2-isocyano-2,4,4-trimethylpentane followed by deprotection. The invention compounds were evaluated for their SHP2 phosphatase inhibitory activity. From the assay, it was determined that compound I•formate exhibited IC50 value less than 5 μM. The experimental process involved the reaction of 6-Chloro-4-methoxy-1H-pyrazolo[3,4-d]pyrimidine(cas: 98138-75-1).Quality Control of 6-Chloro-4-methoxy-1H-pyrazolo[3,4-d]pyrimidine

The Article related to heterocycle preparation shp2 phosphatase inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Quality Control of 6-Chloro-4-methoxy-1H-pyrazolo[3,4-d]pyrimidine

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