Tag: 200-300

On November 15, 2018, Kettle, Jason Grant; Bagal, Sharanjeet Kaur; Boyd, Scott; Eatherton, Andrew John; Fillery, Shaun Michael; Robb, Graeme Richard; Raubo, Piotr Antoni published a patent.Category: imidazoles-derivatives The title of the patent was Preparation of heteroaryl compounds as inhibitors as G12C mutant RAS proteins. And the patent contained the following:

The invention relates to compounds of formula I and pharmaceutically acceptable salts thereof; their preparation, pharmaceutical compositions containing them and their use in the treatment of cell proliferative disorders. Compounds of formula I wherein ring A is aryl, monocyclic heteroaryl and bicyclic heteroaryl; R1 is C1-4 alkyl, halo, OH, etc.; n is 0 – 3; W is N and CR13; X is O and NR14; Y is CR15R16, CO, COCR21R22; R2 is H, CN, halo, etc.; R3 is H, C1-3 fluoroalkyl, OH and derivatives, etc.; R4 is H and Me, R5 is H and Me; R6 is H and CH2NMe2; R13 is H, C1-4 alkyl, halo, etc.; R15, R16 are independently H and C1-3 alkyl; R21 and R22 are independently H, C1-3 alkyl, and F; 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 KRas protein inhibitory activity (some data given). 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 pyrazinooxazepinoquinazoline preparation g12c mutant ras protein inhibitor anticancer, Heterocyclic Compounds (More Than One Hetero Atom): Other 7-Membered Rings and other aspects.Category: imidazoles-derivatives

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On September 3, 2009, Levin, Jeremy Ian; Hopper, Darrin William; Torres, Nancy; Dutia, Minu Dhanjish; Berger, Dan Maarten; Wang, Xiaolun; Di Grandi, Martin Joseph; Zhang, Chunchun; Dunnick, Alejandro Lee published a patent.Synthetic Route of 40644-16-4 The title of the patent was Preparation of bridged, bicyclic heterocyclic or spiro bicyclic heterocyclic derivatives of pyrazolo[1,5-a]pyrimidines as Raf kinase inhibitors.. And the patent contained the following:

Title compounds [I; R1 = (substituted) 5-7 membered heterocyclyl, heteroaryl; R2 = (substituted) (bicyclic) aryl, heteroaryl; R3-R5 = H, cyano, (substituted) alkyl, cycloalkyl aryl, heterocyclyl, heteroaryl, etc.], were prepared Thus, title compound 3-[7-[6-[(1-azabicyclo[2.2.2]oct-4-ylmethyl)amino]pyridin-3-yl]-2-pyridin-4-ylpyrazolo[1,5-a]pyrimidin-3-yl]phenol [multistep preparation from 5-acetyl-2-bromopyridine, DMF di-Me acetal, 3-methoxyphenylacetonitrile, Me isonicotinate, and 1-(1-azabicyclo[2.2.2]oct-4-yl)methylamine given] inhibited B-Raf kinase with IC50 = 0.002 μM. The experimental process involved the reaction of 4-Bromo-1H-benzo[d]imidazol-2(3H)-one(cas: 40644-16-4).Synthetic Route of 40644-16-4

The Article related to pyrazolopyrimidine preparation raf kinase inhibitor, cancer inflammation treatment azabicyclooctylmethylaminopyridinylpyridin4ylpyrazolopyrimidinylphenol preparation, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Synthetic Route of 40644-16-4

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On September 11, 2009, Berger, Dan Maarten; Levin, Jeremy Ian; Dutia, Minu Dhanjisha; Norton, Emily Boucher; Diamantidis, George published a patent.Application of 40644-16-4 The title of the patent was Preparation of aminosulfonylphenyl pyrazolo[1,5-a]pyrimidines as Raf kinase inhibitors.. And the patent contained the following:

Title compounds [I; R = H, halo, NO2, N3, cyano, CHO, CF3, OCF3, R5, OR5, N(R5)2, etc.; R1 = (substituted) heteroaryl, heterocyclyl; R2 = (substituted) aryl, heteroaryl, heterocyclyl; R3, R4 = H, (substituted) alkyl, cycloalkyl, heteroaryl; R5 = H, alkyl, alkenyl, alkynyl, cycloalkyl; N(R5)2 = atoms to form a substituted ring containing 2-7 C atoms], were prepared Thus, N-[2-(diethylamino)ethyl]-N-ethyl-3-[3-(3-hydroxyphenyl)-2-pyridin-4-ylpyrazolo[1,5-a]pyrimidin-7-yl]benzenesulfonamide (multistep preparation given) inhibited B-Raf kinase with IC50 <0.0003 μM. 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 phenylsulfonamide pyrazolopyrimidine preparation raf kinase inhibitor, cancer inflammation treatment aminosulfonylphenylpyrazolopyrimidine preparation, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Application of 40644-16-4

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On January 20, 2022, Venkatraman, Shankar; Katz, Jason; Roush, William R.; Seidel, Hans Martin published a patent.Category: imidazoles-derivatives The title of the patent was Preparation of indoles, imidazopyridines, pyrazolopyrimidines and related heterocycles useful alone or in compositions in treatment of diseases associated with STING activity. And the patent contained the following:

The invention relates to preparation of indoles, imidazopyridines, pyrazolopyrimidines and related heterocycles(I) or a pharmaceutically acceptable salt, hydrate, cocrystal, or drug combination that inhibit (e.g., antagonize) Stimulator of Interferon Genes (STING). Compounds I wherein X1 and X2 each independently is O, S, N, etc.; Z and Y1-Y3 each independently is heteroaryl; ring B is bicyclic or polycyclic C5-15 cycloalkyl or C5-15 cycloalkenyl, etc.; etc., are claimed. The example compound II was prepared via 4-steps synthesis using 5-bromo-1H-indole as starting material (procedure given). Compounds I were evaluated for their biol. activity (data given). Compounds I are useful, e.g., for treating a diseases in which increased (e.g., excessive) STING activation (e.g., STING signaling) contributes to the pathol. and/or symptoms and/or progression of the disease (e.g., cancer) in a subject (e.g., a human). The experimental process involved the reaction of 6-(Trifluoromethyl)-5,6,7,8-tetrahydroimidazo[1,2-a]pyridine-2-carboxylic acid(cas: 1774893-22-9).Category: imidazoles-derivatives

The Article related to pyrazolopyrimidine preparation sting activation inhibitor cancer disease treatment, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Category: imidazoles-derivatives

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On September 30, 2010, Devisscher, Lindsey; Schauvliege, Stijn; Dewulf, Jeroen; Gasthuys, Frank published an article.Electric Literature of 65896-14-2 The title of the article was Romifidine as a constant rate infusion in isoflurance anaesthetized horses: a clinical study. And the article contained the following:

Objective: To evaluate the effects of a constant rate infusion (CRI) of romifidine on the requirement of isoflurane, cardiovascular performance and recovery in anesthetized horses undergoing arthroscopic surgery. Study design: Randomized blinded prospective clin. trial. Animals Thirty horses scheduled for routine arthroscopy. Methods: After premedication (acepromazine 0.02 mg kg-1, romifidine 80 渭g kg-1, methadone 0.1 mg kg-1) and induction (midazolam 0.06 mg kg-1 ketamine 2.2 mg kg-1), anesthesia was maintained with isoflurane in oxygen. Horses were assigned randomly to receive a CRI of saline (group S) or 40 渭g kg-1 hour-1 romifidine (group R). The influences of time and treatment on anesthetic and cardiovascular parameters were evaluated using an anal. of variance. Body weight (t-test), duration of anesthesia (t-test) and recovery score (Wilcoxon Rank Sum Test) were compared between groups. Significance was set at p < 0.05. Results All but one horse were positioned in the dorsal recumbent position and ventilated from the start of anesthesia. End tidal isoflurane concentrations were similar in both groups at similar time points and over the whole anesthetic period. Cardiac output was significantly lower in horses of the R group, but there were no significant differences between groups in cardiac index, body weight or age. All other cardiovascular parameters were similar in both groups. Quality of recovery did not differ significantly between groups, but more horses in group R stood without ataxia at the first attempt. One horse from group S had a problematic recovery. Conclusions and clin. relevance: No inhalation anesthetic sparing effect or side effects were observed by using a 40 渭g kg-1 hour-1 romifidine CRI in isoflurane anesthetized horses under clin. conditions. Cardiovascular performance remained acceptable. Further studies are needed to identify the ED of romifidine that will induce an inhalation anesthetic sparing effect in anesthetized horses. The experimental process involved the reaction of N-(2-Bromo-6-fluorophenyl)-4,5-dihydro-1H-imidazol-2-amine hydrochloride(cas: 65896-14-2).Electric Literature of 65896-14-2

The Article related to sedivet infusion isoflurane anesthesia horse, Pharmacology: Effects Of Nervous System- and Behavior-Affecting Drugs and Neuromuscular Agents and other aspects.Electric Literature of 65896-14-2

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On February 15, 2013, Woodhouse, Kerry J.; Brosnan, Robert J.; Nguyen, Kyvan Q.; Moniz, Gale W.; Galuppo, Larry D. published an article.Safety of N-(2-Bromo-6-fluorophenyl)-4,5-dihydro-1H-imidazol-2-amine hydrochloride The title of the article was Effects of postanesthetic sedation with romifidine or xylazine on quality of recovery from isoflurane anesthesia in horses. And the article contained the following:

Objective-To test the hypothesis that postanesthetic sedation with romifidine would dose-dependently improve recovery quality of recovery from isoflurane anesthesia in horses more than postanesthetic sedation with xylazine. Design-Prospective, randomized, blinded clin. trial. Animals-101 healthy adult horses examined at the University of California-Davis Veterinary Medical Teaching Hospital from 2007 to 2009. Procedures-Horses were sedated with xylazine, and anesthesia was induced with guaifenesin, diazepam, and ketamine via a standardized drug protocol. Anesthesia for surgical or diagnostic procedures was maintained with isoflurane in oxygen for 1 to 4 h. At the end of anesthesia, horses were moved to a padded stall for recovery. Once the breathing circuit was disconnected and the patient was spontaneously breathing, either xylazine (100 or 200 渭g/kg [45 or 91 渭g/lb]) or romifidine (10 or 20 渭g/kg [4.5 or 9.1 渭g/lb]) was administered IV. Objective patient, surgical, and anesthesia data were recorded. Subjective visual analog scale (VAS) scores of recovery quality were assigned by a single individual who was unaware of the treatment received. A stepwise linear regression model was used to correlate patient and procedure factors with the VAS score. Results-Painful procedures, longer anesthesia times, and the Arabian horse breed were associated with poorer VAS scores. Adjustment for these factors revealed an improved VAS recovery score associated with the use of a romifidine dose of 20 渭g/kg. Conclusions and Clin. Relevance-In healthy adult horses anesthetized with isoflurane for > 1 h, the results of this study supported the use of 20 渭g of romifidine/kg, IV, rather than lower romifidine doses or xylazine, for postanesthetic sedation to improve recovery quality. 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 horse sedivet sedation isoflurane anesthetic, Pharmacology: Effects Of Nervous System- and Behavior-Affecting Drugs and Neuromuscular Agents 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 December 31, 2001, Saxena, Apra; Sharma, A. K.; Kumar, Naveen published an article.Electric Literature of 65896-14-2 The title of the article was Sedivet as a premedicant in barbiturate and nonbarbiturate anaesthesia in goats. And the article contained the following:

Sedivet (12.5 渭g/kg) was administered i.v. Behavioral changes were observed on after sedivet administration in atropine (0.5 mg/kg,s.c.) pre-medicated goats. Increased salivation was noticed during experimentation. Corneal palpebral, pharyngeal and laryngeal reflexes were mildly depressed (++) in group B while they were absent in group A during anesthesia. Analgesia in flank in group B persisted for 80.39卤31.85 min and in group A for 50.83卤20.30 min. Polyurea occurred in both the groups. Marked reduction in rectal temperature, heart rate and respiration rate was noticed in sedivet ketamine group. ABP and CVP increased significantly at 2 min of sedivet injection. TEC, TLC, PCV, HB altered nonsignificantly. Serum glucose, bilirubin, urea, SUN and OCT exhibited significant rise (P<0.05) at different intervals while total proteins, albumin, globulin and A:G ratio were slightly lower at 1 h. Hematobiochem. parameters were recorded close to base value at 72 h. Recovery was smooth and uncomplicated. The experimental process involved the reaction of N-(2-Bromo-6-fluorophenyl)-4,5-dihydro-1H-imidazol-2-amine hydrochloride(cas: 65896-14-2).Electric Literature of 65896-14-2

The Article related to sedivet premedicant anesthesia goat, Pharmacology: Effects Of Nervous System- and Behavior-Affecting Drugs and Neuromuscular Agents and other aspects.Electric Literature of 65896-14-2

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On July 31, 2009, Marzok, Mohamed; El-Khodery, Sabry published an article.Related Products of 65896-14-2 The title of the article was Sedative and analgesic effects of romifidine in camels (Camelus dromedarius). And the article contained the following:

To evaluate the clin. effectiveness and the sedative and analgesic effects of i.v. romifidine in camels. Randomized prospective study. Eighteen healthy adult Dromedary camels. Romifidine was administered i.v. to camels (n = 6) at three different doses (40, 80 or 120 渭g/kg-1). Time of onset, degree and duration of sedation and analgesia were recorded immediately after drug administration. Heart rate, respiratory rate, ruminal contractions, muscle relaxation, response to auditory and tactile stimulation, distance between ears, distance from lower lip to the ground, and degree of ataxia were also recorded pre-administration and at 5, 15, 30, 45, 60, 90, 120, and 180 min post-administration. Plasma glucose, blood urea nitrogen and creatinine were measured. Romifidine produced dose dependent sedation and analgesia. Significant decreases in heart rate (p < 0.001), ruminal contractions (p < 0.05), distance from lower lip to the ground (p < 0.001), response to auditory and tactile stimuli (p < 0.01), and significant increases in the degree of ataxia (p < 0.01), distance between the ear tips (p < 0.001) and blood glucose (p < 0.01) concentration were recorded after administration of romifidine until recovery. However, no significant changes in rectal temperature and respiratory rate were recorded. I.v. administration of romifidine at three different doses appeared to be an effective sedative and analgesic agent for camels. Bradycardia, ruminal atony, and hyperglycemia were the most important adverse effects after i.v. administration of romifidine. The i.v. administration of romifidine at a dose rate of 120 渭g/kg-1 caused profound sedation and analgesia. Romifidine could be used for chem. restraint for a variety of diagnostic and minor surgical procedures in camels. The experimental process involved the reaction of N-(2-Bromo-6-fluorophenyl)-4,5-dihydro-1H-imidazol-2-amine hydrochloride(cas: 65896-14-2).Related Products of 65896-14-2

The Article related to camelus sedative analgesic sedivet, Pharmacology: Effects Of Nervous System- and Behavior-Affecting Drugs and Neuromuscular Agents and other aspects.Related Products of 65896-14-2

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On April 17, 1986, Kern, Otto; Wilhelm, Franz published a patent.Safety of N-(2-Bromo-6-fluorophenyl)-4,5-dihydro-1H-imidazol-2-amine hydrochloride The title of the patent was Sedative. And the patent contained the following:

2-[(2-Bromo-6-fluorophenyl)imino]imidazolidine and its salts are veterinary sedatives with analgesic and bradycardiac activity. 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 bromofluorophenyliminoimidazolidine sedative analgesic, imidazolidine bromofluorophenylimino sedative analgesic, bradycardiac bromofluorophenyliminoimidazolidine, Pharmacology: Effects Of Nervous System- and Behavior-Affecting Drugs and Neuromuscular Agents 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 December 31, 2013, Ringer, S. K.; Schwarzwald, C. C.; Portier, K.; Mauch, J.; Ritter, A.; Bettschart-Wolfensberger, R. published an article.Quality Control of N-(2-Bromo-6-fluorophenyl)-4,5-dihydro-1H-imidazol-2-amine hydrochloride The title of the article was Blood glucose, acid-base and electrolyte changes during loading doses of alpha2-adrenergic agonists followed by constant rate infusions in horses. And the article contained the following:

The aim of the present study was to investigate changes in blood glucose concentration ([Glu]B), acid-base status and electrolyte concentrations during constant rate infusions (CRI) of two alpha2-adrenergic agonists in seven horses treated in a blinded, randomized, crossover design with xylazine or romifidine. An i.v. (IV) bolus of xylazine (1 mg/kg) or romifidine (80 渭g/kg) was administered followed by an IV CRI of xylazine (0.69 mg/kg/h) or romifidine (30 渭g/kg/h) for 2 h. Blood samples were collected from the pulmonary artery before and after loading doses, during the CRI, and for 1 h after discontinuing drugs.Blood glucose, base excess (BE), pH, partial pressure of carbon dioxide (PvCO2), strong ion difference (SIDest) and bicarbonate concentration ([HCO3std-]B) increased significantly during the CRI with both alpha2-adrenergic agonists. Chloride concentration ([Cl-]B) and anion-gap (AG) decreased significantly compared to baseline. The decrease in sodium concentration ([Na+]B) was only significant with xylazine. From 1 h after starting the CRI onwards, [Glu]B was significantly higher with romifidine compared to xylazine. Except [Glu]B, SIDest, and PvCO2, all variables returned to normal values 1 h after discontinuing xylazine. After stopping romifidine, all variables except pH remained altered for at least 1 h.It was concluded that loading doses of alpha2-adrenergic agonists followed by CRIs produce [Glu]B, acid-base and electrolyte changes. The clin. significance of the reported changes remains to be investigated and absolute values should be interpreted with caution, as fluid boli were used for cardiac output measurements, but may become important during prolonged infusion and in critically ill patients. The experimental process involved the reaction of N-(2-Bromo-6-fluorophenyl)-4,5-dihydro-1H-imidazol-2-amine hydrochloride(cas: 65896-14-2).Quality Control of N-(2-Bromo-6-fluorophenyl)-4,5-dihydro-1H-imidazol-2-amine hydrochloride

The Article related to anesthetic adrenergic agonist glucose base excess electrolyte horse, acid-base, electrolytes, glucose, romifidine, xylazine, Pharmacology: Effects Of Nervous System- and Behavior-Affecting Drugs and Neuromuscular Agents and other aspects.Quality Control of N-(2-Bromo-6-fluorophenyl)-4,5-dihydro-1H-imidazol-2-amine hydrochloride

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem