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242478-38-2,MFCD09952287
Catalog No.:AA003911

242478-38-2 | 1-Azabicyclo[2.2.2]octan-8-yl (1S)-1-phenyl-3,4-dihydro-1H-isoquinoline-2-carboxylate butanedioic acid

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10mg
≥98%
in stock  
$46.00   $32.00
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25mg
≥98%
in stock  
$69.00   $48.00
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50mg
≥98%
in stock  
$123.00   $86.00
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1g
98%(HPLC)
in stock  
$158.00   $110.00
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5g
98%(HPLC)
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$475.00   $333.00
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  • Technical Information
  • Properties
  • Downstream Synthesis Route
  • Literature
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  • Technical Information
  • Properties
  • Downstream Synthesis Route
  • Literature
Technical Information
Catalog Number:
AA003911
Chemical Name:
1-Azabicyclo[2.2.2]octan-8-yl (1S)-1-phenyl-3,4-dihydro-1H-isoquinoline-2-carboxylate butanedioic acid
CAS Number:
242478-38-2
Molecular Formula:
C27H32N2O6
Molecular Weight:
480.5528
MDL Number:
MFCD09952287
SMILES:
O=C(N1CCc2c([C@@H]1c1ccccc1)cccc2)O[C@H]1CN2CCC1CC2.OC(=O)CCC(=O)O
Properties
Computed Properties
 
Complexity:
617  
Covalently-Bonded Unit Count:
2  
Defined Atom Stereocenter Count:
2  
Heavy Atom Count:
35  
Hydrogen Bond Acceptor Count:
7  
Hydrogen Bond Donor Count:
2  
Rotatable Bond Count:
6  

Downstream Synthesis Route

[1]CurrentPatentAssignee:DRREDDY'SLABORATORIESLIMITED-WO2008/11462,2008,A2Locationinpatent:Page/Pagecolumn25;26

110-15-6    242478-37-1   
solifenacinsuccinate 

[1]CurrentPatentAssignee:TEVAPHARMACEUTICALINDUSTRIESLTD.-US2008/114028,2008,A1Locationinpatent:Page/Pagecolumn11

[2]CurrentPatentAssignee:BEIJINGLABWORLDBIOMEDICALTECHNOLOGYCOLTD-CN108314681,2018,ALocationinpatent:Paragraph0012;0014

[3]CurrentPatentAssignee:WEIHAIDISUPHARM;DISHAPHARMACEUTICALGROUP;SHANDONGDISHAPHARMACEUTICALDISHAPHAMACEUTICAL-CN103450183,2017,BLocationinpatent:Paragraph0018;0037-0039

[4]CurrentPatentAssignee:ZAKLADYFARMACEUTYCZNEPOLPHARMAS.A.-WO2009/142522,2009,A1Locationinpatent:Page/Pagecolumn12

[5]CurrentPatentAssignee:MEDICHEM,S.A.-US2010/29944,2010,A1Locationinpatent:Page/Pagecolumn7

[6]CurrentPatentAssignee:CHONGQINGKERUIPHARMACEUTICALGROUP-CN103896938,2016,BLocationinpatent:Paragraph0071

[7]CurrentPatentAssignee:KYUNGDONGPHARM.CO.,LTD.-US2015/112072,2015,A1Locationinpatent:Paragraph0084-0108

[8]CurrentPatentAssignee:TEVAPHARMACEUTICALINDUSTRIESLTD.-US2008/114028,2008,A1Locationinpatent:Page/Pagecolumn13

[9]CurrentPatentAssignee:TEVAPHARMACEUTICALINDUSTRIESLTD.-US2008/114028,2008,A1Locationinpatent:Page/Pagecolumn11

[10]CurrentPatentAssignee:TEVAPHARMACEUTICALINDUSTRIESLTD.-US2008/114028,2008,A1Locationinpatent:Page/Pagecolumn11

[11]CurrentPatentAssignee:TEVAPHARMACEUTICALINDUSTRIESLTD.-US2008/114028,2008,A1Locationinpatent:Page/Pagecolumn13

[12]CurrentPatentAssignee:TEVAPHARMACEUTICALINDUSTRIESLTD.-US2008/114028,2008,A1Locationinpatent:Page/Pagecolumn10;11

[13]CurrentPatentAssignee:TEVAPHARMACEUTICALINDUSTRIESLTD.-US2008/114028,2008,A1Locationinpatent:Page/Pagecolumn11

[14]CurrentPatentAssignee:TEVAPHARMACEUTICALINDUSTRIESLTD.-US2008/114028,2008,A1Locationinpatent:Page/Pagecolumn111

[15]CurrentPatentAssignee:TEVAPHARMACEUTICALINDUSTRIESLTD.-US2008/114028,2008,A1Locationinpatent:Page/Pagecolumn11

[16]CurrentPatentAssignee:TEVAPHARMACEUTICALINDUSTRIESLTD.-US2008/114028,2008,A1Locationinpatent:Page/Pagecolumn11

[17]CurrentPatentAssignee:TEVAPHARMACEUTICALINDUSTRIESLTD.-US2008/114028,2008,A1Locationinpatent:Page/Pagecolumn12

[18]CurrentPatentAssignee:TEVAPHARMACEUTICALINDUSTRIESLTD.-US2008/114028,2008,A1Locationinpatent:Page/Pagecolumn11

[19]CurrentPatentAssignee:TEVAPHARMACEUTICALINDUSTRIESLTD.-US2008/114028,2008,A1Locationinpatent:Page/Pagecolumn10

[20]CurrentPatentAssignee:TEVAPHARMACEUTICALINDUSTRIESLTD.-US2008/114028,2008,A1Locationinpatent:Page/Pagecolumn12

[21]CurrentPatentAssignee:TEVAPHARMACEUTICALINDUSTRIESLTD.-US2008/114028,2008,A1Locationinpatent:Page/Pagecolumn9-10;11

[22]CurrentPatentAssignee:TEVAPHARMACEUTICALINDUSTRIESLTD.-US2008/114028,2008,A1Locationinpatent:Page/Pagecolumn12

[23]CurrentPatentAssignee:TEVAPHARMACEUTICALINDUSTRIESLTD.-US2008/114028,2008,A1Locationinpatent:Page/Pagecolumn10

[24]CurrentPatentAssignee:ASTELLASPHARMAINC.-EP1714965,2006,A1Locationinpatent:Page/Pagecolumn10

[25]CurrentPatentAssignee:DRREDDY'SLABORATORIESLIMITED-WO2008/11462,2008,A2Locationinpatent:Page/Pagecolumn24

[26]CurrentPatentAssignee:DRREDDY'SLABORATORIESLIMITED-WO2008/11462,2008,A2Locationinpatent:Page/Pagecolumn26;27

[27]CurrentPatentAssignee:DRREDDY'SLABORATORIESLIMITED-WO2008/11462,2008,A2Locationinpatent:Page/Pagecolumn24;25

[28]CurrentPatentAssignee:MEDICHEM,S.A.-US2008/242697,2008,A1Locationinpatent:Page/Pagecolumn4

[29]CurrentPatentAssignee:TEVAPHARMACEUTICALINDUSTRIESLTD.-WO2009/11844,2009,A1Locationinpatent:Page/Pagecolumn16

[30]CurrentPatentAssignee:TEVAPHARMACEUTICALINDUSTRIESLTD.-WO2009/11844,2009,A1Locationinpatent:Page/Pagecolumn16-17;21;21-22;22-23

[31]CurrentPatentAssignee:DIPHARMAFRANCISS.R.L.-US2009/203915,2009,A1Locationinpatent:Page/Pagecolumn3-4

[32]CurrentPatentAssignee:TEVAPHARMACEUTICALINDUSTRIESLTD.-US2008/114028,2008,A1Locationinpatent:Page/Pagecolumn9

[33]CurrentPatentAssignee:TEVAPHARMACEUTICALINDUSTRIESLTD.-US2008/114028,2008,A1Locationinpatent:Page/Pagecolumn12

[34]CurrentPatentAssignee:TEVAPHARMACEUTICALINDUSTRIESLTD.-WO2007/76116,2007,A2Locationinpatent:Page/Pagecolumn13-14

[35]CurrentPatentAssignee:KRKADDNOVOMESTO-WO2011/3624,2011,A1Locationinpatent:Page/Pagecolumn22

[36]CurrentPatentAssignee:ZAKLFARMACEUTYCZNEPOLPHARMASPOLKAAKCYJNA;ZAKLADYFARMACEUTYCZNEPOLPHARMAS.A.-WO2011/86003,2011,A1Locationinpatent:Page/Pagecolumn13

[37]Locationinpatent:experimentalpartNiphade,NavnathC.;Jagtap,KunalM.;Mali,AnilC.;Solanki,PavankumarV.;Jachak,MadhukarN.;Mathad,VijayavitthalT.[MonatsheftefurChemie,2011,vol.142,#11,p.1181-1186]

[38]CurrentPatentAssignee:CHENGDUHUAYUPHARMACEUTICAL-CN105566315,2016,ALocationinpatent:Paragraph0062;0063

[39]CurrentPatentAssignee:DRREDDY'SLABORATORIESLIMITED-WO2008/128028,2008,A2Locationinpatent:Page/Pagecolumn30-31

110-15-6    242478-37-1    862207-71-4    862207-70-3   
solifenacinsuccinate 

[1]CurrentPatentAssignee:ASTELLASPHARMAINC.-EP1714965,2006,A1Locationinpatent:Page/Pagecolumn11

732228-02-3    740780-79-4    110-15-6   
(S)-1-phenyl-1,2,3,4-tetrahydroisoquinoline 
  242478-37-1    862207-71-4    862207-70-3   
1-(S)-phenyl-1,2,3,4-tetrahydroisoquinolinesuccinate 
 
solifenacinsuccinate 

[1]CurrentPatentAssignee:ADVENTINTERNATIONALCORPORATION-WO2008/77357,2008,A2Locationinpatent:Page/Pagecolumn7-8

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Journal: Urology 20060801

Title: [Comment on the STAR study: Comparison of the efficacy and tolerance of solifenacin and tolterodine retard in the treatment of overactive bladder].

Journal: Der Urologe. Ausg. A 20060701

Title: Comparative evaluation of exocrine muscarinic receptor binding characteristics and inhibition of salivation of solifenacin in mice.

Journal: Biological & pharmaceutical bulletin 20060701

Title: Pharmacokinetic effect of ketoconazole on solifenacin in healthy volunteers.

Journal: Basic & clinical pharmacology & toxicology 20060701

Title: Solifenacin: as effective in mixed urinary incontinence as in urge urinary incontinence.

Journal: International urogynecology journal and pelvic floor dysfunction 20060601

Title: Short- and long-term efficacy of solifenacin treatment in patients with symptoms of mixed urinary incontinence.

Journal: BJU international 20060601

Title: Using anticholinergics to treat overactive bladder: the issue of treatment tolerability.

Journal: The American journal of medicine 20060301

Title: The emergence of new drugs for overactive bladder.

Journal: Expert opinion on emerging drugs 20060301

Title: Efficacy and tolerability of solifenacin in elderly subjects with overactive bladder syndrome: a pooled analysis.

Journal: The American journal of geriatric pharmacotherapy 20060301

Title: New drugs 06, part I.

Journal: Nursing 20060201

Title: Re: Chapple CR, Martinez-Garcia R, Selvaggi L, Toozs-Hobson P, Warnack W, Drogendijk T, Wright DM, Bolodeoku J. A comparison of the efficacy and tolerability of solifenacin succinate and extended release tolterodine at treating overactive bladder syndrome: results of the STAR trial. Eur Urol 2005;48:464-70.

Journal: European urology 20060101

Title: Efficacy of solifenacin in patients with severe symptoms of overactive bladder: a pooled analysis.

Journal: Current medical research and opinion 20060101

Title: Solifenacin in overactive bladder syndrome.

Journal: Drugs 20060101

Title: Solifenacin versus tolterodine--a head-to-head study: finally! But not final?

Journal: Current urology reports 20051101

Title: [Drug discovery in the fields of urology: tamsulosin and solifenacin].

Journal: Nihon yakurigaku zasshi. Folia pharmacologica Japonica 20051101

Title: Synthesis and antimuscarinic properties of quinuclidin-3-yl 1,2,3,4-tetrahydroisoquinoline-2-carboxylate derivatives as novel muscarinic receptor antagonists.

Journal: Journal of medicinal chemistry 20051020

Title: Solifenacin in the management of the overactive bladder syndrome.

Journal: International journal of clinical practice 20051001

Title: A comparison of the efficacy and tolerability of solifenacin succinate and extended release tolterodine at treating overactive bladder syndrome: results of the STAR trial.

Journal: European urology 20050901

Title: Solifenacin is effective for the treatment of OAB dry patients: a pooled analysis.

Journal: European urology 20050901

Title: Pharmacokinetic interaction of solifenacin with an oral contraceptive containing ethinyl estradiol and levonorgestrel in healthy women: a double-blind, placebo-controlled study.

Journal: Clinical therapeutics 20050901

Title: Solifenacin and darifenacin for overactive bladder.

Journal: Obstetrics and gynecology 20050801

Title: New treatment options for overactive bladder.

Journal: South Dakota journal of medicine 20050601

Title: Muscarinic receptor binding, plasma concentration and inhibition of salivation after oral administration of a novel antimuscarinic agent, solifenacin succinate in mice.

Journal: British journal of pharmacology 20050501

Title: Effect of age on the pharmacokinetics of solifenacin in men and women.

Journal: International journal of clinical pharmacology and therapeutics 20050501

Title: Effects of solifenacin succinate (YM905) on detrusor overactivity in conscious cerebral infarcted rats.

Journal: European journal of pharmacology 20050404

Title: Solifenacin and darifenacin for overactive bladder.

Journal: The Medical letter on drugs and therapeutics 20050314

Title: Long-term open-label solifenacin treatment associated with persistence with therapy in patients with overactive bladder syndrome.

Journal: European urology 20050301

Title: Improved quality of life in patients with overactive bladder symptoms treated with solifenacin.

Journal: BJU international 20050101

Title: New molecular entity: Vesicare, Yamanouchi/GlaxoSmithKline solifenacin.

Journal: Geriatrics 20050101

Title: New drugs: acamprosate calcium and solifenacin succinate.

Journal: Journal of the American Pharmacists Association : JAPhA 20050101

Title: Recent developments in the management of overactive bladder: focus on the efficacy and tolerability of once daily solifenacin succinate 5 mg.

Journal: Current medical research and opinion 20050101

Title: [Neurological aspect of the hyperactive urinary bladder syndrome].

Journal: Zhurnal nevrologii i psikhiatrii imeni S.S. Korsakova 20050101

Title: Solifenacin in overactive bladder syndrome.

Journal: Drugs & aging 20050101

Title: Solifenacin in overactive bladder syndrome: a viewpoint by Scott Serels.

Journal: Drugs & aging 20050101

Title: Solifenacin in overactive bladder: a viewpoint by Hashim Hashim.

Journal: Drugs & aging 20050101

Title: Randomized, double-blind placebo controlled trial of the once daily antimuscarinic agent solifenacin succinate in patients with overactive bladder.

Journal: The Journal of urology 20041101

Title: The emerging role of solifenacin in the treatment of overactive bladder.

Journal: Expert opinion on investigational drugs 20041001

Title: Preview of new drugs for overactive bladder and incontinence: darifenacin, solifenacin, trospium, and duloxetine.

Journal: Current urology reports 20041001

Title: Elevating our therapeutic expectations in overactive bladder.

Journal: Journal of the American Academy of Nurse Practitioners 20041001

Title: Pharmacokinetics and safety of solifenacin succinate in healthy young men.

Journal: Journal of clinical pharmacology 20040901

Title: [Overactive bladder. New anticholinergic drug controls urinary urge].

Journal: MMW Fortschritte der Medizin 20040708

Title: Food does not affect the pharmacokinetics of solifenacin, a new muscarinic receptor antagonist: results of a randomized crossover trial.

Journal: British journal of clinical pharmacology 20040701

Title: [In overactive bladder, above all urgency is stressful. The patients know the site of each toilet].

Journal: MMW Fortschritte der Medizin 20040527

Title: In vitro and in vivo tissue selectivity profile of solifenacin succinate (YM905) for urinary bladder over salivary gland in rats.

Journal: European journal of pharmacology 20040525

Title: Solifenacin: treatment of overactive bladder.

Journal: Drugs of today (Barcelona, Spain : 1998) 20040401

Title: Randomized, double-blind placebo- and tolterodine-controlled trial of the once-daily antimuscarinic agent solifenacin in patients with symptomatic overactive bladder.

Journal: BJU international 20040201

Title: Comparison of in vitro selectivity profiles of solifenacin succinate (YM905) and current antimuscarinic drugs in bladder and salivary glands: a Ca2+ mobilization study in monkey cells.

Journal: Life sciences 20040102

Title: Solifenacin appears effective and well tolerated in patients with symptomatic idiopathic detrusor overactivity in a placebo- and tolterodine-controlled phase 2 dose-finding study.

Journal: BJU international 20040101

Title: Solifenacin demonstrates high absolute bioavailability in healthy men.

Journal: Drugs in R&D 20040101

Title: [Urinary incontinence: new pharmacologic therapies].

Journal: Revista de medicina de la Universidad de Navarra 20040101

Title: M(3) receptor antagonism by the novel antimuscarinic agent solifenacin in the urinary bladder and salivary gland.

Journal: Naunyn-Schmiedeberg's archives of pharmacology 20020801

Title: Effects of YM905, a novel muscarinic M3-receptor antagonist, on experimental models of bowel dysfunction in vivo.

Journal: Japanese journal of pharmacology 20010701

Title: Krishna SR, Rao BM, Rao NS.A validated rapid stability-indicating method for the determination of related substances in solifenacin succinate by ultra-fast liquid chromatography.J Chromatogr Sci. 2010 Nov;48(10):807-10.

Title: Ohtake A, Sato S, Sasamata M, Miyata K.The forefront for novel therapeutic agents based on the pathophysiology of lower urinary tract dysfunction: ameliorative effect of solifenacin succinate (Vesicare), a bladder-selective antimuscarinic agent, on overactive bladder symptoms, especially urgency episodes.J Pharmacol Sci. 2010;112(2):135-41. Epub 2010 Feb 4.

Title: Hoffstetter S, Leong FC.Solifenacin succinate for the treatment of overactive bladder.Expert Opin Drug Metab Toxicol. 2009 Mar;5(3):345-50.

Title: Choo MS, Lee JZ, Lee JB, Kim YH, Jung HC, Lee KS, Kim JC, Seo JT, Paick JS, Kim HJ, Na YG, Lee JG.Efficacy and safety of solifenacin succinate in Korean patients with overactive bladder: a randomised, prospective, double-blind, multicentre study.Int J Clin Pract. 2008 Nov;62(11):1675-83.

Title: Imamura T, et al.Combined treatment with a β3 -adrenergic receptor agonist and a muscarinic receptor antagonist inhibits detrusor overactivity induced by cold stress in spontaneously hypertensive rats. Neurourol Urodyn. 2017 Apr;36(4):1026-1033.

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SDS
Tags:242478-38-2 Molecular Formula|242478-38-2 MDL|242478-38-2 SMILES|242478-38-2 1-Azabicyclo[2.2.2]octan-8-yl (1S)-1-phenyl-3,4-dihydro-1H-isoquinoline-2-carboxylate butanedioic acid