Tag: 200-300

Naumchuk, V. M.; Volynets, G. P.; Gorbatiuk, O. B.; Lukashov, S. S.; Bdzhola, V. G.; Yarmoluk, S. M. published an article in 2015, the title of the article was Investigation of inhibitory activity of imidazolone derivatives and their precursors toward human protein kinase CK2.Formula: C12H9N3O And the article contains the following content:

We have investigated inhibitory activity of imidazolone derivatives and their precursors toward protein kinase CK2. As a result, we have found seven inhibitors with IC50 values in the range from 8 to 30 μM. The experimental process involved the reaction of 3-Phenyl-1H-imidazo[4,5-b]pyridin-2(3H)-one(cas: 41010-50-8).Formula: C12H9N3O

The Article related to protein kinase imidazolone derivative non cyclic precursor inhibition, Enzymes: Other and other aspects.Formula: C12H9N3O

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On October 31, 2012, WOJTASIAK-WYPART, M.; Soma, L. R.; Rudy, J. A.; Uboh, C. E.; Boston, R. C.; Driessen, B. published an article.Safety of N-(2-Bromo-6-fluorophenyl)-4,5-dihydro-1H-imidazol-2-amine hydrochloride The title of the article was Pharmacokinetic profile and pharmacodynamic effects of romifidine hydrochloride in the horse. And the article contained the following:

Romifidine HCl (romifidine) is an α2-agonist commonly used in horses. This study was undertaken to investigate the pharmacokinetics (PK) of romifidine following i.v. (i.v.) administration and describe the relationship between PK parameters and simultaneously recorded pharmacodynamic (PD) parameters. Romifidine (80 μg/kg) was administered by i.v. infusion over 2 min to six adult Thoroughbred horses, and plasma samples were collected and analyzed using liquid chromatog.-mass spectrometry. Limit of quantification was <0.1 ng/mL. PD parameters and arterial blood gases were measured for 300 min following romifidine administration. Statistical PD data anal. included mixed-effect modeling. After i.v. administration of romifidine, the plasma concentration-vs.-time curve was best described by a two-compartmental model. Terminal elimination half-life (t1/2β) was 138.2 (104.6-171.0) min and volumes for central (Vc) and peripheral (V2) compartments were 1.89 (0.93-2.39) and 2.57 (1.71-4.19) L/kg, resp. Maximum plasma concentration (Cmax) was 51.9 ± 13.1 ng/mL measured at 4 min following commencement of drug administration. Systemic clearance (Cl) was 32.4 (25.5-38.4) mL·min/kg. Romifidine caused a significant reduction in heart rate and cardiac index and an increase in mean arterial pressure (P < 0.05). Sedation score and head height values were significantly different from the baseline values for 120 min (P < 0.05). The decline in cardiovascular and sedative effects correlated with the decline in plasma romifidine concentration (P < 0.05). In conclusion, a highly sensitive anal. technique for the detection of romifidine in equine plasma allowed detailed description of its PK profile. The drug produces long-lasting sedation in horses that corresponds with the long terminal elimination half-life of the drug. The experimental process involved the reaction of N-(2-Bromo-6-fluorophenyl)-4,5-dihydro-1H-imidazol-2-amine hydrochloride(cas: 65896-14-2).Safety of N-(2-Bromo-6-fluorophenyl)-4,5-dihydro-1H-imidazol-2-amine hydrochloride

The Article related to sedivet pharmacodynamics pharmacokinetics sedative equus heart rate blood pressure, Pharmacology: Drug Metabolism and other aspects.Safety of N-(2-Bromo-6-fluorophenyl)-4,5-dihydro-1H-imidazol-2-amine hydrochloride

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On August 5, 2004, Food and Drug Administration published an article.HPLC of Formula: 65896-14-2 The title of the article was Implantation or injectable dosage form new animal drugs; romifidine. And the article contained the following:

The Food and Drug Administration (FDA) is amending the animal drug regulations to reflect approval of a new animal drug application (NADA) field by Boehringer Ingelheim Vetmedica, Inc. The NADA provides for the veterinary prescription use of romifidine hydrochloride injectable solution in horses as a sedative and analgesic, and as a preanesthetic agent. The experimental process involved the reaction of N-(2-Bromo-6-fluorophenyl)-4,5-dihydro-1H-imidazol-2-amine hydrochloride(cas: 65896-14-2).HPLC of Formula: 65896-14-2

The Article related to romifidine standard injection horse, Pharmaceuticals: Drug Standards and other aspects.HPLC of Formula: 65896-14-2

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On February 11, 2021, Pennington, Lewis D.; Woods, James R.; Huynh, Hoan; Aquila, Brian M.; Mugge, Ingo Andreas; Hu, Yuan; Choi, Younggi; Wynn, Thomas Andrew; Gerard, Baudouin; Bosanac, Todd; Vantangoli, Nicholas J. published a patent.Application of 40644-16-4 The title of the patent was Lactam-containing compounds for the treatment of pain. And the patent contained the following:

Provided herein are compounds I (R1= (halogen-substituted) C1-6 alkyl, C1-4 alkoxy; R2, R3, R4= H, (halogen-substituted) C1-4 alkyl, C1-4 alkoxy, OH, halogen; R5= H, C1-4 alkyl; X and R6 as defined in text) that are useful in the treatment of pain in a subject. Also provided herein is a pharmaceutical composition comprising compounds or pharmaceutically acceptable salts thereof, and a pharmaceutically acceptable carrier and methods of treating pain in a subject in need thereof. The experimental process involved the reaction of 4-Bromo-1H-benzo[d]imidazol-2(3H)-one(cas: 40644-16-4).Application of 40644-16-4

The Article related to pharmaceutical composition pain, Pharmaceuticals: Pharmaceutics and other aspects.Application of 40644-16-4

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On December 27, 2018, Davoren, Jennifer E.; Nason, Deane; Coe, Jotham; Dlugolenski, Keith; Helal, Christopher; Harris, Anthony R.; LaChapelle, Erik; Liang, Sidney; Liu, Yue; OConnor, Rebecca; Orozco, Christine C.; Rai, Brajesh K.; Salafia, Michelle; Samas, Brian; Xu, Wenjian; Kozak, Rouba; Gray, David published an article.Recommanded Product: 5-Bromo-6-methylimidazo[1,2-a]pyridine The title of the article was Discovery and Lead Optimization of Atropisomer D1 Agonists with Reduced Desensitization. And the article contained the following:

The discovery of D1 subtype-selective agonists with drug-like properties has been an enduring challenge for the greater part of 40 years. All known D1-selective agonists are catecholamines that bring about receptor desensitization and undergo rapid metabolism, thus limiting their utility as a therapeutic for chronic illness such as schizophrenia and Parkinson’s disease. Our high-throughput screening efforts on D1 yielded a single non-catecholamine hit PF-4211 (6) that was developed into a series of potent D1 receptor agonist leads with high oral bioavailability and CNS penetration. An important structural feature of this series is the locked biaryl ring system resulting in atropisomerism. Disclosed herein is a summary of our hit-to-lead efforts on this series of D1 activators culminating in the discovery of atropisomer 31 (PF-06256142), a potent and selective orthosteric agonist of the D1 receptor that has reduced receptor desensitization relative to dopamine and other catechol-containing agonists. The experimental process involved the reaction of 5-Bromo-6-methylimidazo[1,2-a]pyridine(cas: 1346157-13-8).Recommanded Product: 5-Bromo-6-methylimidazo[1,2-a]pyridine

The Article related to preparation atropisomer dopamine d1 agonist receptor desensitization, schizophrenia parkinson’s dopamine d1 agonist structure, Pharmacology: Structure-Activity and other aspects.Recommanded Product: 5-Bromo-6-methylimidazo[1,2-a]pyridine

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On June 17, 2021, Pade, Remi; Charpentier, Gael; Villard, Isabelle published a patent.Synthetic Route of 65896-14-2 The title of the patent was Mite infestation treatment. And the patent contained the following:

The invention relates to a compound of the invention, a salt thereof or a composition containing same as an acaricide, to a method for reducing or preventing an infestation of an animal by a mite, comprising exposing the mite to a compound of invention, to a composition comprising a compound of invention and a polymer, to a strap or a beehive comprising a compound such as detomidine. The experimental process involved the reaction of N-(2-Bromo-6-fluorophenyl)-4,5-dihydro-1H-imidazol-2-amine hydrochloride(cas: 65896-14-2).Synthetic Route of 65896-14-2

The Article related to miticides beehives cat collars dog, Agrochemical Bioregulators: Invertebrate and other aspects.Synthetic Route of 65896-14-2

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On October 14, 2021, Liu, Tao; Zhou, Shubao; Wang, Shaomeng; Zhang, Meng; Xu, Fuming; Zhou, Haibin; Aguilar, Angelo; Huang, Liyue published a patent.Safety of 4-Bromo-1H-benzo[d]imidazol-2(3H)-one The title of the patent was Preparation of piperidine derivatives as menin inhibitors and methods of use for treating cancer. And the patent contained the following:

The present disclosure provides compounds represented by Formula (I): or a pharmaceutically acceptable salt thereof, wherein Ra, Rb, Rc, Rd, L1, R2 B, Q and E are as defined as set forth in the specification. The present disclosure also provides compounds of Formula (I) for use to treat cancer or any other disease, condition, or disorder that is responsive to inhibition of menin. :. The disclosure provides compounds represented by formula I, or a pharmaceutically acceptable salt thereof. The disclosure also provides compounds of formula I for use to treat cancer or any other disease, condition, or disorder that is responsive to inhibition of menin. Compounds of formula I wherein n is 0, 1 and 2; each Ra and each Rb are independently H and C1-4 alkyl; Rc is H and halo; each R4 is independently halo; Q is NHCO2R; R is C1-4 alkyl, C1-4 haloalkyl and CD3; B is imidazolylmethyl, pyrazolylmethyl, CH2OH, etc.; E is (un)substituted sulfonylphenyl, (un)substituted Ph, (un)substituted pyrimidinyl, etc.; L1 is CH2; and pharmaceutically acceptable salt thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their menin inhibitory activity. From the assay, it was determined that compound II exhibited IC50 values of less than 50 nM. The experimental process involved the reaction of 4-Bromo-1H-benzo[d]imidazol-2(3H)-one(cas: 40644-16-4).Safety of 4-Bromo-1H-benzo[d]imidazol-2(3H)-one

The Article related to piperidine preparation menin inhibitor treatment cancer, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Safety of 4-Bromo-1H-benzo[d]imidazol-2(3H)-one

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Bollenbach, Maud; Nemska, Simona; Wagner, Patrick; Camelin, Guillaume; Daubeuf, Francois; Obrecht, Adeline; Villa, Pascal; Rognan, Didier; Bihel, Frederic; Bourguignon, Jean-Jacques; Schmitt, Martine; Frossard, Nelly published an article in 2021, the title of the article was Design, synthesis and biological evaluation of arylpyridin-2-yl guanidine derivatives and cyclic mimetics as novel MSK1 inhibitors. An application in an asthma model.Category: imidazoles-derivatives And the article contains the following content:

In order to identify new MSK1 inhibitors, a screening of a library of low mol. weight compounds was performed, and the results highlighted the I [R = phenyl] ( IC50~18μM) as a starting hit for structure-activity relationship study. Derivatives, homologues and rigid mimetics of I [R = Ph, 2-furanyl, 3-pyridine, etc.] were designed, and all synthesized compounds were evaluated for their inhibitory activity towards MSK1. Among them, the non-cytotoxic 2-aminobenzimidazole was the most potent at inhibiting significantly: (i) MSK1 activity, (ii) the release of IL-6 in inflammatory conditions in vitro (IC50~2μM) and (iii) the inflammatory cell recruitment to the airways in a mouse model of asthma. The experimental process involved the reaction of 4-Bromo-1H-benzo[d]imidazol-2(3H)-one(cas: 40644-16-4).Category: imidazoles-derivatives

The Article related to arylpyridinyl guanidine preparation msk1 inhibitor antiasthmatic cytotoxicity sar, msk1, pyridine-2-yl guanidine, asthma, inflammation, kinase inhibitors, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Category: imidazoles-derivatives

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On September 30, 2011, Kruger, Karin; Stegmann, George F.; Becker, Piet J. published an article.Reference of N-(2-Bromo-6-fluorophenyl)-4,5-dihydro-1H-imidazol-2-amine hydrochloride The title of the article was Preliminary investigation of concurrent administration of phenylbutazone and romifidine in healthy horses. And the article contained the following:

To characterize the cardiorespiratory and electrocardiog. effects of the combined administration of phenylbutazone and romifidine. Prospective four-period, four-treatment, blinded, randomized, crossover trial. Five, healthy, mixed breed horses. Prior to treatment administration, a catheter was introduced into the intra-thoracic cranial vena cava via the jugular vein and a s.c. located carotid artery was catheterised. All treatments were administered i.v. and consisted of saline placebo (PLC), phenylbutazone (PBZ, 4.4 mg/kg-1) romifidine (ROM, 80 μg/kg-1) and a combination of phenylbutazone (4.4 mg/kg-1) and romifidine (80 μg/kg-1). There was at least a 1 wk washout period between treatments. Heart rate (HR), respiratory rate (fR), systolic (SAP), diastolic (DAP) and mean (MAP) arterial pressures and central venous pressure (CVP) were recorded for baseline (prior to drug administration) and at 5 min intervals thereafter for 30 min. Electrocardiog. abnormalities were recorded. Data were analyzed by ANOVA. For the cardiovascular variables there were no statistically significant (p > 0.05) differences between horses treated with ROM and PBZ_ROM. Statistically significant (p < 0.05) differences only occurred between treatments with romifidine (ROM and PBZ_ROM) and without romifidine (PLC and PBZ). Within treatments, for ROM, changes over time were statistically significant (p < 0.05) for HR, SAP, DAP, MAP and CVP. For PBZ_ROM, changes over time were statistically significant (p < 0.05) for CVP. Sino-atrial and atrio-ventricular blocks occurred in horses treated with ROM and PBZ_ROM. The combined i.v. administration of phenylbutazone and romifidine had no statistically significant effect on cardiorespiratory variables. These limited data suggest no evidence why both agents should not be included in a preoperative medication protocol for healthy horses but do not exclude the possibility of interactions occurring in a larger population. The experimental process involved the reaction of N-(2-Bromo-6-fluorophenyl)-4,5-dihydro-1H-imidazol-2-amine hydrochloride(cas: 65896-14-2).Reference of N-(2-Bromo-6-fluorophenyl)-4,5-dihydro-1H-imidazol-2-amine hydrochloride

The Article related to phenylarthrite sedivet anesthetic combination therapy heart rate respiration horse, Pharmacology: Drug Interactions and General Pharmacology and other aspects.Reference of N-(2-Bromo-6-fluorophenyl)-4,5-dihydro-1H-imidazol-2-amine hydrochloride

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On November 3, 1977, Schweisguth, Bernard published a patent.Safety of 3-Phenyl-1H-imidazo[4,5-b]pyridin-2(3H)-one The title of the patent was (Morpholinylmethyl)benzimidazolinones. And the patent contained the following:

Antidepressant morpholine derivatives I (R = Me, Me2CH, Ph, PhCH2; R1 = H, 6-Cl, 5-MeO; R2 = H, PhCH2; X = N, CH) (12 compounds) were prepared Thus, 1-methyl-2,3-dihydro-2-benzimidazolone reacted with NaH and 2-(chloromethyl)-4-benzylmorpholine to give I (R = Me, R1 = H, R2 = PhCH2), which was hydrogenated to I (R2 = H). I are useful as antidepressants at 50-150 mg/day for humans. The experimental process involved the reaction of 3-Phenyl-1H-imidazo[4,5-b]pyridin-2(3H)-one(cas: 41010-50-8).Safety of 3-Phenyl-1H-imidazo[4,5-b]pyridin-2(3H)-one

The Article related to morpholinylmethylbenzimidazolone, antidepressant morpholinylmethylbenzimidazolone, benzimidazolone morpholinylmethyl, Heterocyclic Compounds (More Than One Hetero Atom): Oxazines and other aspects.Safety of 3-Phenyl-1H-imidazo[4,5-b]pyridin-2(3H)-one

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem