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Novel lead compounds in pre-clinical development against African sleeping sickness

It’s only fair to share… Novel lead compounds in pre-clinical development against African sleeping sickness Med. Chem. Commun., 2017, 8,1872-1890 DOI: 10.1039/C7MD00280G, Review Article Michael Berninger, Ines Schmidt, Alicia Ponte-Sucre, Ulrike Holzgrabe This article reviews the recent progress in drug development against the African sleeping sickness. Novel lead compounds in pre-clinical development against African sleeping sickness …

NNC 45-0781

It’s only fair to share… NNC 45-0781 Molecular Formula C27H29NO3 Molecular Weight 415.5241 CAS 207277-66-5 2H-1-Benzopyran-7-ol, 3,4-dihydro-3-phenyl-4-[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]-, cis-(-)- (3S,4R)-3,4-Dihydro-3-phenyl-4-[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]-2H-1-benzopyran-7-ol 2H-1-Benzopyran-7-ol, 3,4-dihydro-3-phenyl-4-(4-(2-(1-pyrrolidinyl)ethoxy)phenyl)-, (3S,4R)- OriginatorNovo Nordisk ClassOsteoporosis therapies; Pyrrolidines; Small molecules Mechanism of ActionSelective estrogen receptor modulators PATENT WO 9818776 WO 9818771 WO 2003063859 A quantitative structure activity relationship study on cis-3,4-diaryl hydroxy chromones as high affinity partial agonists for the estrogen …

(R)-(–)-Baclofen, Arbaclofen, STX 209, AGI 006

It’s only fair to share… (R)-(–)-Baclofen, Arbaclofen, STX 209, AGI 006 Chemical Names: (R)-Baclofen; Arbaclofen; 69308-37-8; (R)-4-Amino-3-(4-chlorophenyl)butanoic acid; (-)-Baclofen; D-Baclofen Molecular Formula: C10H12ClNO2 Molecular Weight: 213.661 g/mol  A GAMMA-AMINOBUTYRIC ACID derivative that is a specific agonist of GABA-B RECEPTORS. It is used in the treatment of MUSCLE SPASTICITY, especially that due to SPINAL CORD INJURIES. Its therapeutic …

ESCITALOPRAM, S-(+)-Citalopram, эсциталопрам , إيسكيتالوبرام , 艾司西酞普兰 ,

It’s only fair to share… Escitalopram (+)-Citalopram (1S)-1-[3-(Dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-2-benzofuran-5-carbonitrile [ACD/IUPAC Name] (S)-citalopram 128196-01-0 [RN] 5-Isobenzofurancarbonitrile, 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-, (1S)- [ACD/Index Name] Molecular FormulaC20H21FN2O Average mass324.392 Da S-(+)-Citalopram эсциталопрам [Russian] [INN] إيسكيتالوبرام [Arabic] [INN] 艾司西酞普兰 [Chinese] [INN] Lexapro® (escitalopram oxalate) is an orally administered selective serotonin reuptake inhibitor (SSRI). Escitalopram is the pure Senantiomer (single isomer) of the racemic bicyclic phthalane derivative citalopram. Escitalopram oxalate is designated S-(+)-1-[3(dimethyl-amino)propyl]-1-(p-fluorophenyl)-5-phthalancarbonitrile oxalate with the …

(+)-(S,S)-Reboxetine succinate, Esreboxetine succinate

It’s only fair to share… Esreboxetine succinate (2S)-2-[(S)-(2-ethoxyphenoxy)(phenyl)methyl]morpholine butanedioate (1:1) (2S)-2-[(S)-(2-Ethoxyphenoxy)(phenyl)methyl]morpholine succinate (1:1) (S,S)-reboxetine succinate 635724-55-9 [RN] Esreboxetine succinate [USAN] Morpholine, 2-[(S)-(2-ethoxyphenoxy)phenylmethyl]-, (2S)-, butanedioate (1:1) Succinic acid – (2S)-2-[(S)-(2-ethoxyphenoxy)(phenyl)methyl]morpholine (1:1) UNII:XQO13W6OCH Esreboxetine is a selective norepinephrine reuptake inhibitor which was under development by Pfizer for the treatment of neuropathic pain and fibromyalgia but failed to show significant benefit over currently available medications and was discontinued.[1][2][3][4] It is the …

Amantadine Hydrochloride, アダマンタン-1-アミン

It’s only fair to share… Amantadine Molecular Formula C10H17N Average mass 151.249 Da [768-94-5] 1-ADAMANTAMINE 1-adamantanamine; 1-adamantylamine; 1-aminoadamantane; Amantidine; Aminoadamantane 1-Adamantylamine 1-Aminotricyclo(3.3.1.1(sup 3,7))decane 2204333 [Beilstein] 31377-23-8 [RN] 40933-03-7 [RN] 4-pyridinecarboxylic acid, compd. with tricyclo[3.3.1.13,7]decan-1-amine (1:1) Journal of the American Chemical Society, 91, p. 6457, 1969 DOI: 10.1021/ja01051a047 Synthesis, p. 457, 1976 AMANTADINE HYDROCHLORIDE Molecular FormulaC10H18ClN Average mass187.710 Da CAS 665-66-7 SPECTROSCOPY BASE 13 …

JTV 519, K 201

It’s only fair to share… JTV-519 Molecular FormulaC25H32N2O2S Average mass424.599 Da 145903-06-6 CAS   JTV-519 hydrochloride salt Molecular FormulaC25H33ClN2O2S Average mass461.060 Da 3-(4-Benzyl-1-piperidinyl)-1-(7-methoxy-2,3-dihydro-1,4-benzothiazepin-4(5H)-yl)-1-propanonhydrochlorid (1:1) 4-[3-(4-benzylpiperidin-1-yl)propanoyl]-7-methoxy-2,3,4,5-tetrahydro-1,4-benzothiazepine hydrochloride JTV-519 hydrochloride salt 1038410-88-6 [RN] UNII-0I621Y6R4Q K201 1038410-88-6 K 201 SCHEMBL194018 CHEMBL2440857 DTXSID90146108 0I621Y6R4Q LS-193564 JAPAN TOBACCO Acute Myocardial Infarction, Treatment of Cardiovascular Diseases (Not Specified) Antiarrhythmic Drugs JTV-519 (K201) is a 1,4-benzothiazepine derivative …

Phytomenadione, Phytonadione, фитоменадион ,فيتوميناديون ,

It’s only fair to share… Phytomenadione, PHYTONADIONE, Phylloquinone Molecular Formula: C31H46O2 Molecular Weight: 450.707 g/mol [R-[R*,R*-(E)]]-2-Methyl-3-(3,7,11,15-tetramethyl-2-hexadecenyl)-1,4-naphthalenedione 1,4-Naphthalenedione, 2-methyl-3-((2E,7R,11R)-3,7,11,15-tetramethyl-2-hexadecenyl)- 2′,3′-trans-Vitamin K1 фитоменадион [Russian] [INN] فيتوميناديون [Arabic] [INN] 2-methyl-3-[(2E,7R,11R)-3,7,11,15-tetramethylhexadec-2-en-1-yl]naphthalene-1,4-dione  CAS 84-80-0[RN] Antihemorrhagic vitamin Aqua mephyton AQUAMEPHYTON Combinal K1 Kativ N Kephton Kinadion K-Ject KONAKION Mono-kay Phyllochinonum Phylloquinone (8CI) Optical Rotatory Power -0.28 ° Solv: 1,4-dioxane (123-91-1); Wavlen: 589.3 nm; Temp: 25 °C Karrer, …

ELAMIPRETIDE

It’s only fair to share… Elamipretide H-D-Arg-Tyr(2,6-diMe)-Lys-Phe-NH2 D-arginyl-2,6-dimethyl-L-tyrosyl-L-lysyl-L-phenylalaninamide (2S)-6-amino-2-[[(2S)-2-[[(2R)-2-amino-5-(diaminomethylideneamino)pentanoyl]amino]-3-(4-hydroxy-2,6-dimethylphenyl)propanoyl]amino]-N-[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]hexanamide CAS 736992-21-5 Chemical Formula: C32H49N9O5 Molecular Weight: 639.8 A free radical scavenger and antioxidant that localizes in the inner mitochondrial membrane. Mitochondrial Protective Agent to Improve Cell Viability Elamipretide bendavia UNII-87GWG91S09 736992-21-5 MTP 131 RX 31 SS 31 87GWG91S09 L-Phenylalaninamide, D-arginyl-2,6-dimethyl-L-tyrosyl-L-lysyl- SS-31 peptide Arg-Dmt-Lys-Phe-NH2 D-Arg-Dmt-Lys-Phe-NH2 SS31 peptide …

A highly efficient Suzuki-Miyaura methylation of pyridines leading to the drug pirfenidone and its CD3 version (SD-560)

It’s only fair to share…   A highly efficient Suzuki-Miyaura methylation of pyridines leading to the drug pirfenidone and its CD3 version (SD-560) Green Chem., 2017, Advance Article DOI: 10.1039/C7GC01740E, Communication Eliezer Falb, Konstantin Ulanenko, Andrey Tor, Ronen Gottesfeld, Michal Weitman, Michal Afri, Hugo Gottlieb, Alfred Hassner The first methylation/deuteromethylation in green and nearly quantitative …