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Details

Stereochemistry ABSOLUTE
Molecular Formula C17H26N4O6S
Molecular Weight 414.477
Optical Activity UNSPECIFIED
Defined Stereocenters 1 / 1
E/Z Centers 1
Charge 0

SHOW SMILES / InChI
Structure of TIMOLOL MALEATE ESTER

SMILES

CC(C)(C)NC[C@@H](COC1=NSN=C1N2CCOCC2)OC(=O)\C=C/C(O)=O

InChI

InChIKey=MGIAXRFZDNBKRF-RXNFCKPNSA-N
InChI=1S/C17H26N4O6S/c1-17(2,3)18-10-12(27-14(24)5-4-13(22)23)11-26-16-15(19-28-20-16)21-6-8-25-9-7-21/h4-5,12,18H,6-11H2,1-3H3,(H,22,23)/b5-4-/t12-/m0/s1

HIDE SMILES / InChI

Molecular Formula C17H26N4O6S
Molecular Weight 414.477
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 1 / 1
E/Z Centers 1
Optical Activity UNSPECIFIED

Timolol maleate (ISTALOL) is a non-selective beta-adrenergic receptor blocking agent. Timolol maleate is a beta1 and beta2 (non-selective) adrenergic receptor blocking agent that does not have significant intrinsic sympathomimetic, direct myocardial depressant, or local anesthetic (membrane-stabilizing) activity. In its opthalmic form, Timolol maleate, is used to treat open-angle and occasionally secondary glaucoma. Timolol maleate, when applied topically to the eye, has the action of reducing elevated, as well as normal, intraocular pressure, whether or not accompanied by glaucoma. Elevated intraocular pressure is a major risk factor in the pathogenesis of glaucomatous visual field loss and optic nerve damage. Timolol maleate ester is a Timolol maleate specified impurity E [EP]. Timolol impurities are used for ANDA filling/DMF filling and genotoxic study.

Originator

Approval Year

Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
ISTALOL

Approved Use

ISTALOL ophthalmic solution is indicated in the treatment of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma.

Launch Date

2.52460794E11
Patents

Sample Use Guides

Timolol maleate (ISTALOL) ophthalmic solution is available in a concentration of 0.5 percent. The starting dose is one drop of 0.5 percent ISTALOL in the affected eye(s) once a day in the AM.
Route of Administration: Topical
In Vitro Use Guide
Unknown
Substance Class Chemical
Created
by admin
on Sat Dec 16 10:07:08 UTC 2023
Edited
by admin
on Sat Dec 16 10:07:08 UTC 2023
Record UNII
J2V3WF497E
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
TIMOLOL MALEATE ESTER
Common Name English
TIMOLOL MALEATE IMPURITY E [EP IMPURITY]
Common Name English
2-BUTENEDIOIC ACID (2Z)-, 1-((1S)-1-(((1,1-DIMETHYLETHYL)AMINO)METHYL)-2-((4-(4-MORPHOLINYL)-1,2,5-THIADIAZOL-3-YL)OXY)ETHYL) ESTER
Systematic Name English
(2Z)-4-((1S)-1-(((1,1-DIMETHYLETHYL)AMINO)METHYL)-2-((4-(MORPHOLIN-4-YL)-1,2,5-THIADIAZOL-3-YL)OXY)ETHOXY)-4-OXOBUT-2-ENOIC ACID
Systematic Name English
Code System Code Type Description
PUBCHEM
10112466
Created by admin on Sat Dec 16 10:07:08 UTC 2023 , Edited by admin on Sat Dec 16 10:07:08 UTC 2023
PRIMARY
FDA UNII
J2V3WF497E
Created by admin on Sat Dec 16 10:07:08 UTC 2023 , Edited by admin on Sat Dec 16 10:07:08 UTC 2023
PRIMARY
CAS
1026075-53-5
Created by admin on Sat Dec 16 10:07:08 UTC 2023 , Edited by admin on Sat Dec 16 10:07:08 UTC 2023
PRIMARY
Related Record Type Details
PARENT -> IMPURITY
not more than twice the area of the principal peak in the chromatogram obtained with reference solution (a)
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP