Tag: 200-300

On March 19, 2020, Akahoshi, Issei; Sumikawa, Yoshitake; Furuta, Sadayoshi; Fukushima, Keiichiro; Imazu, Takuya; Kotaka, Ryota published a patent.Recommanded Product: 6-(Trifluoromethyl)-5,6,7,8-tetrahydroimidazo[1,2-a]pyridine-2-carboxylic acid The title of the patent was Preparation of heteroaromatic amide derivative for inhibiting Nav1.7. And the patent contained the following:

The present invention relates to a compound I [X-Y = N-C or C-N; Y1-Y4 = independently single bond, -CH2-, -CH2CH2-, etc.; Z1 = single bond, -O-, -S-, etc.; ring A = monocyclic aromatic ring or bicyclic aromatic ring; R1a, R1b = independently H, halo, hydroxy, etc.; R2 = H, halo, hydroxy, etc.; R3a, R3b, R3c = independently H, halo, cyano, etc.; combination of R5a, R5b, R5c, R6a, R6b and n is selected from (1), (2), (3), etc.; (1) R5b and R5c combine to form a single bond, -CH2-, -OCH2-, etc., R5a is H, alkyl, haloalkyl, etc., R6a and R6b each is H, halo, hydroxy, etc., and n is 1 or 2 (2) R5a and R6a combine to form -CH2-, -CH2CH2-, -CH2CH2O-, etc., R5b is H, alkyl or haloalkyl, R5c and R6b each is H, halo, hydroxy, etc. (or R5c and R6b may combine to form -(CH2)p-, -O(CH2)p-, -(CH2)pO-, etc. (p = 0-3)), and n is 1 (3) R5a is H, alkyl, haloalkyl, etc., R5b is H or alkyl, R5c is H, alkyl or halo, R6a and R6b each is H, halo, alkyl, etc. (or R6a and R6b, together with the carbon atom to which they are attached, may combine to form a monocyclic ring) and n is 1 or 2; or a salt thereof]. For example, compound II was prepared via cyclization of 5-(trifluoromethyl)pyridin-2-amine with Et bromopyruvate, hydrogenation, hydrolysis and HATU-mediated amidation with 6-fluorochroman-3-amine·HCl. Compound I shows selective inhibition of Nav1.7 over Nav1.5, and is useful for the treatment of pain and various Nav1.7-related disease. 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).Recommanded Product: 6-(Trifluoromethyl)-5,6,7,8-tetrahydroimidazo[1,2-a]pyridine-2-carboxylic acid

The Article related to heteroaromatic amide preparation voltage gated sodium channel blocker, analgesic heteroaromatic amide, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.Recommanded Product: 6-(Trifluoromethyl)-5,6,7,8-tetrahydroimidazo[1,2-a]pyridine-2-carboxylic acid

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On January 12, 1978, Staehle, Helmut; Koeppe, Herbert; Kummer, Werner; Hoefke, Wolfgang published a patent.Product Details of 65896-14-2 The title of the patent was 2-Bromo-6-fluoro-N-2-imidazolidinylideneaniline. And the patent contained the following:

The title compound (I) and its pharmaceutically acceptable salts were prepared by the cyclization of 2,6-FBrC6H3NHC(SR):NH.HX (II; R = alkyl, X = halogen) with H2NCH2CH2NH2. Thus, II (R = Me, X = iodo) was refluxed with H2NCH2CH2NH2 in BuOH and the mixture treated with HCl to give 56.3% I HCl, which has antihypertensive activity comparable to that of clonidine, with fewer side effects, e.g., inhibition of gastric juice secretion. The experimental process involved the reaction of N-(2-Bromo-6-fluorophenyl)-4,5-dihydro-1H-imidazol-2-amine hydrochloride(cas: 65896-14-2).Product Details of 65896-14-2

The Article related to antihypertensive phenyliminoimidazolidine, phenyliminoimidazolidine, imidazolidine phenylimino, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.Product Details of 65896-14-2

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On October 31, 1983, Kovac, T.; Oklobdzija, M.; Comisso, G.; Decorte, E.; Fajdiga, T.; Moimas, F.; Angeli, C.; Zonno, F.; Toso, R.; Sunjic, V. published an article.Safety of 3-Phenyl-1H-imidazo[4,5-b]pyridin-2(3H)-one The title of the article was New synthesis of 11-acyl-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-ones and related studies. And the article contained the following:

11-Acyl-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-ones I (R = 4-methylpiperazino, imidazolo, 2-methylimidazolo) were prepared via N-α-chloroacetylation and aminolysis. Other attempts at cyclization to form I are also reported. 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 aminoacetylpyridobenzodiazepinone, pyridobenzodiazepinone aminoacetyl, benzodiazepinone pyrido, Heterocyclic Compounds (More Than One Hetero Atom): Diazepines and other aspects.Safety of 3-Phenyl-1H-imidazo[4,5-b]pyridin-2(3H)-one

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On November 5, 2020, Rosen, Yael; Dangoor, David; Fisher, Richard published a patent.HPLC of Formula: 65896-14-2 The title of the patent was Methods of treating pruritus by topically administering an α-2 adrenoreceptor agonist. And the patent contained the following:

The present disclosure related to methods of treating pruritus in a subject by topically administering an α-2 adrenoreceptor agonist to a subject. 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 pruritus treatment topical alpha2 adrenoreceptor agonist, Pharmacology: Other (All Agents and Effects Not Otherwise Assignable) and other aspects.HPLC of Formula: 65896-14-2

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On June 24, 2021, Machacek, Michelle; Altman, Michael D.; Huang, Chunhui; Reutershan, Michael H.; Sloman, David L.; Siliphaivanh, Phieng; Schneider, Sebastian E.; Yeung, Charles S.; Witter, David J.; Gibeau, Craig R.; Ye, Yingchun published a patent.Safety of 6-(Trifluoromethyl)-5,6,7,8-tetrahydroimidazo[1,2-a]pyridine-2-carboxylic acid The title of the patent was Protein-arginine N-methyltransferase PRMT5 inhibitors for therapy. And the patent contained the following:

The present invention provides compounds and pharmaceutically acceptable salts, esters, and prodrugs thereof, which are PRMT5 inhibitors. These compounds can treat cancer, sickle cell, and hereditary persistence of fetal Hb mutations. 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).Safety of 6-(Trifluoromethyl)-5,6,7,8-tetrahydroimidazo[1,2-a]pyridine-2-carboxylic acid

The Article related to methyltransferase prmt5 inhibitor pharmaceutical, Pharmacology: Other (All Agents and Effects Not Otherwise Assignable) and other aspects.Safety of 6-(Trifluoromethyl)-5,6,7,8-tetrahydroimidazo[1,2-a]pyridine-2-carboxylic acid

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On September 30, 2009, Leece, Elizabeth A.; Girard, Nicolas M.; Maddern, Kieren published an article.Application In Synthesis of N-(2-Bromo-6-fluorophenyl)-4,5-dihydro-1H-imidazol-2-amine hydrochloride The title of the article was Alfaxalone in cyclodextrin for induction and maintenance of anesthesia in ponies undergoing field castration. And the article contained the following:

To evaluate the induction and maintenance of anesthesia using alfaxalone following pre-anesthetic medication with romifidine and butorphanol in ponies undergoing castration in the field. Prospective clin. study. Seventeen male ponies weighing 169 ± 29 kg. The ponies were sedated with romifidine and butorphanol i.v. Induction time was recorded following administration of alfaxalone 1 mg/kg-1 and diazepam 0.02 mg/kg-1 i.v. If movement during surgery occurred, alfaxalone 0.2 mg/kg-1 was administered i.v. The quality of anesthetic induction, and recovery were scored on a subjective scale of 1 (good) to 5 (poor). The number of attempts to attain sternal recumbency and standing, quality of recovery and times from induction to end of surgery, first head lift, sternal recumbency and standing were recorded. Induction quality was good [median score (range) 1 (1-3)] with a mean ±SD time of 29 ± 6 s taken to achieve lateral recumbency. Ten ponies required incremental doses of alfaxalone during surgery. Mean times to the end of surgery, first head lift, sternal recumbency and standing were 26 ± 9 min, 31 ± 9 min, 33 ± 9 min and 34 ± 9 min resp. The number of attempts to attain sternal recumbency was 1(1-1) and to attain standing was 1(1-2). Quality of recovery was good, with a recovery score of 1(1-2). Alfaxalone provided smooth induction and recovery characteristics and was considered suitable for maintenance of anesthesia for castration in ponies. The experimental process involved the reaction of N-(2-Bromo-6-fluorophenyl)-4,5-dihydro-1H-imidazol-2-amine hydrochloride(cas: 65896-14-2).Application In Synthesis of N-(2-Bromo-6-fluorophenyl)-4,5-dihydro-1H-imidazol-2-amine hydrochloride

The Article related to alfaxan cyclodextrin anesthesia horse anesthetic, Mammalian Hormones: Corticosteroid, Gonadal, and Placental Hormones and other aspects.Application In Synthesis of N-(2-Bromo-6-fluorophenyl)-4,5-dihydro-1H-imidazol-2-amine hydrochloride

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On February 28, 1979, Svertilova, I. A.; Yutilov, Yu M. published an article.Recommanded Product: 3-Phenyl-1H-imidazo[4,5-b]pyridin-2(3H)-one The title of the article was Condensed imidazolones. And the article contained the following:

Eight imidazolones I (X, Y = CH, N; R = H, Me, Ph, benzyl; R1 = H, Me, Et, Ph, benzyl) were prepared in 90-9% yield by cyclocondensation of diamines II with (EtO2C)2O. The experimental process involved the reaction of 3-Phenyl-1H-imidazo[4,5-b]pyridin-2(3H)-one(cas: 41010-50-8).Recommanded Product: 3-Phenyl-1H-imidazo[4,5-b]pyridin-2(3H)-one

The Article related to cyclocondensation pyrocarbonate pyridinediamine, phenylenediamine pyrocarbonate cyclocondensation, imidazolone condensed, benzimidazolone, imidazopyridinone, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.Recommanded Product: 3-Phenyl-1H-imidazo[4,5-b]pyridin-2(3H)-one

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On July 31, 2014, Stine, Jessica M.; Michau, Tammy M.; Williams, Megan K.; Kuebelbeck, Karen Leann; Stengard, Michele E. published an article.SDS of cas: 65896-14-2 The title of the article was The effects of intravenous romifidine on intraocular pressure in clinically normal horses and horses with incidental ophthalmic findings. And the article contained the following:

Design : Original study. Objective : To evaluate the effect of sedation with romifidine hydrochloride 1% (Sedivet: Boehringer-Ingelheim) on intraocular pressure (IOP) in the normal horse and horses with incidental ophthalmic findings as measured by applanation tonometry. Animals : Nineteen clin. normal horses (13 geldings, six mares) and eight horses (three geldings, five mares) with incidental ophthalmic findings were included in this study. Procedures : All horses underwent complete ophthalmic examination with pharmacol. mydriasis a min. of 2 wk prior to IOP evaluation. Baseline intraocular pressure values were obtained following auriculopalpebral nerve block and topical anesthetic. Immediately thereafter, romifidine was administered i.v. (75 μg/kg) and the IOP recorded at 5, 15, 30, 45 and 60 min postsedation in both eyes. Five successive readings were obtained at each time point, the low and high value discarded, and three remaining readings averaged for a mean. Results : The changes with time were consistent between eyes and OD and OS results were pooled. The mean IOP at baseline was 26.35 ± 5.57 mmHg. Mean IOP values were significantly lower than baseline at 5 (P < 0.0001), 15 (P < 0.0001), 30 (P = 0.0003), 45 (P < 0.0001) and 60 (P = 0.0005) minutes. The largest change from baseline (16.7%) was noted at t = 15 min. Conclusions and clin. relevance : Administration of romifidine significantly decreased the IOP from baseline at all time points measured. The greatest decline in IOP was noted at 15 min postsedation. Results are consistent with other studies noting a decline in IOP with administration of α-2 agonists. The experimental process involved the reaction of N-(2-Bromo-6-fluorophenyl)-4,5-dihydro-1H-imidazol-2-amine hydrochloride(cas: 65896-14-2).SDS of cas: 65896-14-2

The Article related to sedivet alpha2 agonist intravenous drug delivery intraocular pressure horse, alpha-2 agonist, equine, intraocular pressure, romifidine, sedation, tonometry, Pharmacology: Other (All Agents and Effects Not Otherwise Assignable) and other aspects.SDS of cas: 65896-14-2

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On July 31, 2014, Marzok, Mohamed A.; El-khodery, Sabry A.; Oheida, Aiman H. published an article.Category: imidazoles-derivatives The title of the article was Effect of intravenous administration of romifidine on intraocular pressure in clinically normal horses. And the article contained the following:

Objective : To evaluate the effect of i.v. administration of romifidine on the intraocular pressure (IOP) in horses. Animals studied : Twenty-four horses with no ocular abnormalities. Procedure : Horses were randomly assigned into two equal groups (treatment and control). All horses in the treatment group received an i.v. (IV) injection of romifidine (40 μg/kg). The horses in the control group were administrated an i.v. injection of 0.9% saline (0.4 mL/100 kg). In both groups, the IOP values were measured immediately (T0) pre-administration and at 5 (T5), 15 (T15), 30 (T30), 45 (T45), 60 (T60), 90 (T90), and 120 (T120) min after drug administration. Results : The pre-treatment values (T0) of IOP for right and left eyes were 24.25 ± 3.5 and 25.16 ± 3.4 mmHg, resp. A significant decrease in IOP values was observed in both right and left eyes of the horses in treatment group at T5, T15, T30, T45, T60, and T90 in comparison with the baseline values (P < 0.05). The lowest level of IOP in romifidine-treated groups was recorded at T45 for the right and left eyes (10.25 ± 2.3 and 11.25 ± 3.5 mmHg, resp.). Conclusion : Romifidine significantly decreased IOP in clin. normal horses and may be used safely for surgery or diagnostic ocular procedures in horses when specific control of IOP is required. The experimental process involved the reaction of N-(2-Bromo-6-fluorophenyl)-4,5-dihydro-1H-imidazol-2-amine hydrochloride(cas: 65896-14-2).Category: imidazoles-derivatives

The Article related to sedivet alpha2 adrenoceptor agonist intraocular pressure horse antiglaucoma, applanation tonometry, horse, intraocular pressure, romifidine, Pharmacology: Other (All Agents and Effects Not Otherwise Assignable) and other aspects.Category: imidazoles-derivatives

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On January 31, 2007, Buhl, Rikke; Ersboell, Annette K.; Larsen, Nanna H.; Eriksen, Lis; Koch, Joergen published an article.Application In Synthesis of N-(2-Bromo-6-fluorophenyl)-4,5-dihydro-1H-imidazol-2-amine hydrochloride The title of the article was The effects of detomidine, romifidine or acepromazine on echocardiographic measurements and cardiac function in normal horses. And the article contained the following:

To evaluate by echo- and electrocardiog. the cardiac effects of sedation with detomidine hydrochloride, romifidine hydrochloride or acepromazine maleate in horses. An exptl. study using a crossover design without randomization. Animals Eight clin. normal Standardbred trotters. Echocardiog. examinations (two-dimensional, guided M-mode and color Doppler) were recorded on five different days. Heart rate (HR) and standard limb lead electrocardiograms were also obtained. Subsequently, horses were sedated with detomidine (0.01 mg kg-1), romifidine (0.04 mg kg-1) or acepromazine (0.1 mg kg-1) administered i.v. and all examinations repeated. Heart rate before treatment with the three drugs did not differ significantly (p = 0.98). Both detomidine and romifidine induced a significant decrease (p < 0.001) in HR during the first 25 min after sedation; while acepromazine had a varying effect on HR. For detomidine, there was a significant increase in LVIDd (left ventricular internal diameter in diastole; p = 0.034) and LVIDs (left ventricular internal diameter in systole; p < 0.001). In addition, a significant decrease was found in IVSs (the interventricular septum in systole; p < 0.001), LVFWs (the left ventricular free wall in systole; p = 0.002) and FS% (fractional shortening; p < 0.001). The frequency of pulmonary regurgitation was increased significantly (p < 0.001). Romifidine induced a significant increase in LVIDs (p < 0.001) and a significant decrease in IVSs (p < 0.001) and FS% (p = 0.002). Acepromazine had no significant effect upon any of the measured values. The results indicate that sedation of horses with detomidine and to a lesser extent romifidine at the doses given in this study has a significant effect on heart function, echocardiog. measurements of heart dimensions and the occurrence of valvular regurgitation. Although the clin. significance of these results may be minimal, the potential effects of sedative drugs should be taken into account when echocardiog. variables are interpreted in clin. cases. The experimental process involved the reaction of N-(2-Bromo-6-fluorophenyl)-4,5-dihydro-1H-imidazol-2-amine hydrochloride(cas: 65896-14-2).Application In Synthesis of N-(2-Bromo-6-fluorophenyl)-4,5-dihydro-1H-imidazol-2-amine hydrochloride

The Article related to horse heart rate electrocardiog echocardiog domosedan sedivet plegicil sedative, Pharmacology: Effects Of Cardiovascular, Hematologic, and Renal Drugs and other aspects.Application In Synthesis of N-(2-Bromo-6-fluorophenyl)-4,5-dihydro-1H-imidazol-2-amine hydrochloride

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem