95722-07-9

Usage

InChI:InChI=1/C22H30O5/c1-3-4-5-6-15(2)20(23)8-7-18-19-12-16(9-10-27-14-22(25)26)11-17(19)13-21(18)24/h9,15,17-21,23-24H,3,6,10-14H2,1-2H3,(H,25,26)/b16-9+/t15-,17-,18+,19-,20+,21+/m0/s1

Upstream product

• 112741-42-1 (1S,5S,6S,7R)-6-(2-bromo-3(S)-hydroxy-4(S)-methyl-1-nonen-6-ynyl)-7-hydroxy-(E)-3-<(4-tert-butoxycarbonyl)-3-oxabutylidene>bicyclo<3.3.0>octane 
• 112741-46-5 (S)-2-Methyl-hept-4-yn-1-ol 
• 112741-45-4 2-((S)-2-Methyl-hept-4-ynyloxy)-tetrahydro-pyran 
• 106937-29-5 {2-[(3aS,4S,5R,6aS)-4-((Z)-(S)-2-Bromo-3-hydroxy-4-methyl-non-1-en-6-ynyl)-5-(tetrahydro-pyran-2-yloxy)-hexahydro-pentalen-(2E)-ylidene]-ethoxy}-acetic acid tert-butyl ester 
• 112741-13-6 2-methyl-4-heptynal 
• 112741-11-4 1,1-dibromo-3-methyl-5-octyn-2-ol 
• 112741-16-9 1,1-dibromo-3-methyl-5-octyn-2-one 
• 99828-10-1 C₂₇H₃₃BrO₅ 
• 99783-78-5 2-[(3aS,5R,6aS)-5-(tert-Butyl-dimethyl-silanyloxy)-4-[(3S,4S)-3-(tert-butyl-dimethyl-silanyloxy)-4-methyl-nona-1,6-diynyl]-hexahydro-pentalen-(2E)-ylidene]-ethanol 
• 99783-73-0 (S)-2-Methyl-hept-4-ynoic acid ((R)-2-hydroxy-1-phenyl-ethyl)-amide 
• 99828-09-8 C₂₇H₃₁BrO₅ 
• 99783-76-3 (3aS,5R,6aR)-5-(tert-Butyl-dimethyl-silanyloxy)-4-[(3S,4S)-3-(tert-butyl-dimethyl-silanyloxy)-4-methyl-nona-1,6-diynyl]-hexahydro-pentalen-2-one 
• 95639-59-1 (3aS,5R,6aR)-5-Hydroxy-4-((3S,4S)-3-hydroxy-4-methyl-nona-1,6-diynyl)-hexahydro-pentalen-2-one 
• 99783-74-1 (S)-2-methyl-4-heptynoic acid methyl ester 

Relevant academic research and scientific papers

THERAPY FOR COMPLICATIONS OF DIABETES

A method for enhancing glycemic control and/or insulin sensitivity in a human subject having diabetic nephropathy and/or metabolic syndrome comprises administering to the subject a selective endothelin A (ETA) receptor antagonist in a glycemic control and/or insulin sensitivity enhancing effective amount. A method for treating a complex of comorbidities in an elderly diabetic human subject comprises administering to the subject a selective ETA receptor antagonist in combination or as adjunctive therapy with at least one additional agent that is (i) other than a selective ETA receptor antagonist and (ii) effective in treatment of diabetes and/or at least one of said comorbidities other than hypertension. A therapeutic combination useful in such a method comprises a selective ETA receptor antagonist and at least one antidiabetic, anti-obesity or antidyslipidemic agent other than a selective ETA receptor antagonist.

ANTIHYPERTENSIVE THERAPY

A new use of darusentan is provided in preparation of a pharmaceutical composition for lowering blood pressure in a patient exhibiting resistance to a baseline antihypertensive therapy with one or more drugs. The composition comprises darusentan in an amount providing a therapeutically effective daily dose; wherein (a) the composition is orally deliverable and/or (b) the daily dose of darusentan is effective to provide a reduction of at least about 3 mmHg in one or more blood pressure parameters selected from trough sitting systolic, trough sitting diastolic, 24-hour ambulatory systolic, 24-hour ambulatory diastolic, maximum diurnal systolic and maximum diurnal diastolic blood pressures. Further provided is a new use of darusentan in preparation of a pharmaceutical composition for lowering blood pressure in a patient exhibiting resistance to a baseline antihypertensive therapy, wherein the composition is administered adjunctively with at least one diuretic and at least one antihypertensive drug selected from ACE inhibitors, angiotensin II receptor blockers, beta-adrenergic receptor blockers and calcium channel blockers.

Method for treating resistant hypertension

A method is provided for lowering blood pressure in a patient having clinically diagnosed resistant hypertension. The method comprises administering darusentan to the patient adjunctively with a baseline antihypertensive regimen that comprises administration of at least one diuretic and at least two antihypertensive drugs selected from at least two of (a) ACE inhibitors and angiotensin II receptor blockers, (b) beta-adrenergic receptor blockers and (c) calcium channel blockers. The darusentan is orally administered at a dose and frequency effective, in combination with the baseline regimen, to provide a reduction of at least about 3 mmHg in one or more blood pressure parameters selected from trough sitting systolic, trough sitting diastolic, 24-hour ambulatory systolic, 24-hour ambulatory diastolic, maximum diurnal systolic and maximum diurnal diastolic blood pressures.

Asymmetric synthesis of the highly potent anti-metastatic prostacyclin analogue cicaprost and its isomer isocicaprost

An asymmetric synthesis of the anti-metastatic prostacyclin analogue cicaprost and a formal one of its isomer isocicaprost by a new route are described. A key step of these syntheses is the coupling of a chiral bicyclic C6-C14 ethynyl building block with

A New Method for the Introduction of Carbon-Carbon Triple Bond at C-13 in PG Synthesis. A Stereocontrolled Synthesis of ZK 96 480

ZK 96 480, a chemically and metabolically stable prostacyclin analogue, has been synthesized from the Corey lactone in a stereocontrolled manner by a route utilizing a newlyeveloped method for introduction of the carbon-carbon triple bond at C-13 (PG numb