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Olmesartan medoxomil

Olmesartan medoxomil structure

CAS No:
144689-63-4
Formula:
C29H30N6O6
Chemical Name:
Olmesartan medoxomil
Synonyms:
1H-Imidazole-5-carboxylic acid,4-(1-hydroxy-1-methylethyl)-2-propyl-1-[[2′-(2H-tetrazol-5-yl)[1,1′-biphenyl]-4-yl]methyl]-,(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl ester;1H-Imidazole-5-carboxylic acid,4-(1-hydroxy-1-methylethyl)-2-propyl-1-[[2′-(1H-tetrazol-5-yl)[1,1′-biphenyl]-4-yl]methyl]-,(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl ester;1,3-Dioxole,1H-imidazole-5-carboxylic acid deriv.;CS 866;Olmesartan medoxomil;Benicar;Olmetec;Olsertain;Angiosartan;(5-Methyl-2-oxo-2H-1,3-dioxol-4-yl)methyl 4-(2-hydroxypropan-2-yl)-2-propyl-1-([4-[2-(1H-1,2,3,4-tetrazol-5-yl)phenyl]phenyl]methyl)-1H-imidazole-5-carboxylate;(5-Methyl-2-oxo-1,3-dioxol-4-yl)methyl 4-(1-hydroxy-1-methylethyl)-2-propyl-1-[[2′-(2H-tetrazol-5-yl)[1,1′-biphenyl]-4-yl]methyl]-1H-imidazole-5-carboxylate
Categories:
Active Pharmaceutical Ingredients > Circulatory System Drugs

Description

White to off-white crystalline powderOlmesartan medoxomil was launched in the US as benicar@, an orallyadministered treatment for hypertension. This ester prodrug of olmesartan can besynthesized in 8 steps from diaminomaleonitrile by successive reactions withtrialkylorthopropanoate to access 2-propyl-imidazole-45dicarbonitrile, conversion of thetwo nitrile functions to the corresponding ethyl esters, followed by methylmagnesiumbromide addition to give the corresponding 4-(1-hydroxyalk

Olmesartan medoxomil is a member of biphenyls.|Olmesartan Medoxomil is a synthetic imidazole derivative prodrug with an antihypertensive property. Upon hydrolysis, olmesartan medoxomil is converted to olmesartan. Olmesartan selectively binds to the angiotensin type 1 (AT1) receptor of angiotensin II in vascular smooth muscle and adrenal gland, thereby competing angiotensin II binding to the receptor. This prevents angiotensin II-induced vasoconstriction and decreases aldosterone production, thereby preventing aldosterone-stimulated sodium retention and potassium excretion.|An ANGIOTENSIN II TYPE 1 RECEPTOR BLOCKER that is used to manage HYPERTENSION.

Olmesartan medoxomil Basic Attributes

Molecular Weight：

558.585

Exact Mass：

558.59

EC Number：

1308068-626-2

UNII：

6M97XTV3HD

NSC Number：

758924

DSSTox ID：

DTXSID9045924

NCI Thesaurus Code：

C47640

ATC Code：

C09CA08|C - Cardiovascular system

HScode：

2934990002

Characteristics

PSA：

154

XLogP3：

3.8

Appearance：

white to beige

Density：

1.38±0.1 g/cm3(Predicted)

Melting Point：

180-182 °C @ Solvent: Acetone

Boiling Point：

804.2±75.0 °C(Predicted)

Flash Point：

180°C

Refractive Index：

1.666

Water Solubility：

DMSO: soluble20mg/mL, clear

Storage Conditions：

-20°C Freezer

Vapor Pressure：

0mmHg at 25°C

Collision Cross Section：

225 Å² [M+H]+ [CCS Type: TW, Method: calibrated with polyalanine and drug standards]

Safety Information

hazard class code：

R36/38; R41; R38

safety instructions：

S37/39; S26; S39

RTECS Number：

NI4014200

Marks：

GHS Classification：

|Danger|H302 (94.85%): Harmful if swallowed [Warning Acute toxicity, oral]|P201, P202, P261, P264, P270, P271, P280, P281, P301+P312, P302+P352, P304+P312, P304+P340, P305+P351+P338, P308+P313, P312, P322, P330, P337+P313, P363, P405, and P501|Aggregated GHS information provided by 97 companies from 10 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Drug Information

Drug Indication：

Treatment of hypertension|Treatment of essential hypertension|Essential hypertension|Prevention of cardiovascular events, Treatment of dyslipidaemia, Treatment of hypertension

MeSH：

Agents that antagonize ANGIOTENSIN II TYPE 1 RECEPTOR. Included are ANGIOTENSIN II analogs such as SARALASIN and biphenylimidazoles such as LOSARTAN. Some are used as ANTIHYPERTENSIVE AGENTS. (See all compounds classified as Angiotensin II Type 1 Receptor Blockers.)|Drugs used in the treatment of acute or chronic vascular HYPERTENSION regardless of pharmacological mechanism. Among the antihypertensive agents are DIURETICS; (especially DIURETICS, THIAZIDE); ADRENERGIC BETA-ANTAGONISTS; ADRENERGIC ALPHA-ANTAGONISTS; ANGIOTENSIN-CONVERTING ENZYME INHIBITORS; CALCIUM CHANNEL BLOCKERS; GANGLIONIC BLOCKERS; and VASODILATOR AGENTS. (See all compounds classified as Antihypertensive Agents.)

MeSH Entry Terms：

5-Methyl-2-oxo-1,3-dioxolen-4-yl)methoxy-4-(1-hydroxy-1-methylethyl)-2-propyl-1-(4-(2-(tetrazol-5-yl)phenyl)phenyl)methylimidazol-5-carboxylate - T287346

Olmesartan medoxomil Use and Manufacturing

Uses

An angiotensin II receptor antagonist.Used as an anti-hypertensiveraw material intermediates for dyes, spices, food colors, medicines, pesticides, and building materials.

Use Classification：

Human Drugs -> EU pediatric investigation plans|Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients|Pharmaceuticals

Computed Properties

Molecular Weight:558.6
XLogP3:3.8
Hydrogen Bond Donor Count:2
Hydrogen Bond Acceptor Count:10
Rotatable Bond Count:11
Exact Mass:558.22268270
Monoisotopic Mass:558.22268270
Topological Polar Surface Area:154
Heavy Atom Count:41
Complexity:969
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

Drug Function and Efficacy

No specific description provided

This ingredient has been used in drugs with the following functions (note: it does not mean that the ingredient itself has the following health functions)

Related Drugs

Olmesartan Medoxomil

Olmesartan Medoxomil Tablets
Ingredients	Olmesartan medoxomil.
Indication	Olmesartan medoxomil is not metabolized by the hepatic cytochrome P450 system and has no effect on P450 enzymes. Therefore, drug interactions related to inhibition, induction or metabolism of these enzymes will not occur. There were no significant drug interactions with the concomitant use of digoxin or warfarin in healthy subjects, and the concomitant use of antacids [Al(OH)3/Mg(OH)2] did not significantly change the bioavailability of Olmesartan medoxomil.
Specifications	20mg
Manufacturer	Shanghai Sine Promod Pharmaceutical Co., Ltd.

Olmesartan Medoxomil Tablets
Specifications	20mg
Manufacturer	Nanjing Chia Tai-tianqing Pharmaceutical Co., Ltd.

See More Related Drugs

Registered Holders

CHROMO LABORATORIES INDIA PRIVATE LTD

United States
Active
MICRO LABS LTD

United States
Active
ZHUHAI RUNDU PHARMACEUTICAL CO LTD

United States
Active

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