Category «PHASE 3»

(+)-(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 …

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 …

TOZADENANT

It’s only fair to share… Tozadenant RO-449351 SYN-115 Molecular Formula C19H26N4O4S Average mass 406.499 Da A2 (3); A2a-(3); RO4494351; RO4494351-000; RO4494351-002; SYN-115 Phase III clinical trials at Biotie Therapies for the treatment of Parkinson’s disease as an adjunctive therapy with levodopa 1-Piperidinecarboxamide, 4-hydroxy-N-[4-methoxy-7-(4-morpholinyl)-2-benzothiazolyl]-4-methyl- 4-Hydroxy-N-[4-methoxy-7-(4-morpholinyl)-1,3-benzothiazol-2-yl]-4-methyl-1-piperidinecarboxamide 4-Hydroxy-N-[4-methoxy-7-(4-morpholinyl)-2-benzothiazolyl]-4-methyl-1-piperidinecarboxamide 4-Hydroxy-4-methyl-piperidine-1-carboxylic acid(4-methoxy-7-morpholin-4-yl-benzothiazol-2-yl)-amide CAS 870070-55-6 Originator Roche Developer Acorda Therapeutics Class Amides; Antiparkinsonians; Benzothiazoles; Carboxylic acids; …

RAPASTINEL рапастинел , راباستينيل , 雷帕替奈

It’s only fair to share… RAPASTINEL Molecular Formula C18H31N5O6 Average mass 413.469 Da L-threonyl-L-prolyl-L-prolyl-L-threoninamide (2S)-1-[(2S)-1-[(2S,3R)-2-amino-3-hydroxybutanoyl]pyrrolidine-2-carbonyl]-N-[(2S,3R)-1-amino-3-hydroxy-1-oxobutan-2-yl]pyrrolidine-2-carboxamide 117928-94-6 [RN] L-Threoninamide, L-threonyl-L-prolyl-L-prolyl- рапастинел [Russian] راباستينيل [Arabic] 雷帕替奈 [Chinese] (S)-N-((2S,3R)-1-amino-3-hydroxy-1-oxobutan-2-yl)-1-((S)-1-((2S,3R)-2-amino-3-hydroxybutanoyl)pyrrolidine-2-carbonyl)pyrrolidine-2-carboxamide UNII-6A1X56B95E; 117928-94-6; 6A1X56B95E (S)-N-((2S,3R)-1-amino-3-hydroxy-1-oxobutan-2-yl)-1-((S)-1-((2S,3R)-2-amino-3-hydroxybutanoyl)pyrrolidine-2-carbonyl)pyrrolidine-2-carboxamide [117928-94-6] GLYX-13 trifluoroacetate GLYX-13;GLYX13;GLYX 13;Thr-Pro-Pro-Thr-NH2 L-Threonyl-L-prolyl-L-prolyl-L-threoninamide trifluoroacetate MFCD20527320 Thr-Pro-Pro-Thr-NH2 trifluoroacetate TPPT-amide trifluoroacetate UNII:6A1X56B95E BV-102; GLYX13, GLYX-13, in phase 3 clinical trials Originator Northwestern University Developer Allergan; Naurex Class Amides; Antidepressants; Neuropsychotherapeutics; Oligopeptides; Small molecules Mechanism of …

Rosiptor acetate

It’s only fair to share… Rosiptor acetate CAS: 782487-29-0 (acetate)  782487-28-9 (free base) Chemical Formula: C22H39NO4 Molecular Weight: 381.557 AQX-1125; AQX 1125; AQX1125; AQX-1125 acetate; Rosiptor acetate PHASE 3 …..a SH2-containing inositol 5-phosphatase 1 (SHIP1) modulator for treating cancer, inflammatory disorders and immune disorders. (1S,3S,4R)-4-((3aS,4R,5S,7aS)-4-(Aminomethyl)-7a-methyl-1- methyleneoctahydro -1H – inden-5-yl)-3-(hydroxymethyl)-4-methylcyclohexanol, acetate IUPAC/Chemical Name: (1S,3S,4R)-4-((3aS,4R,5S,7aS)-4-(aminomethyl)-7a-methyl-1-methyleneoctahydro-1H-inden-5-yl)-3-(hydroxymethyl)-4-methylcyclohexan-1-ol acetate Originator Aquinox Pharmaceuticals Class Anti-inflammatories; …

Lanabecestat (formerly known as AZD3293 or LY3314814)

It’s only fair to share… Lanabecestat Molecular FormulaC26H28N4O Average mass412.527 Da Dispiro[cyclohexane-1,2′-[2H]indene-1′(3′H),2”-[2H]imidazol]-4”-amine, 4-methoxy-5”-methyl-6′-[5-(1-propyn-1-yl)-3-pyridinyl]-, (1α,1′R,4β)- (1r,1’R,4R)-4-Methoxy-5”-methyl-6′-[5-(1-propin-1-yl)-3-pyridinyl]-3’H-dispiro[cyclohexane-1,2‘-indene-1’,2”-imidazol]-4”-amin (1r,1’R,4R)-4-Methoxy-5”-methyl-6′-[5-(1-propyn-1-yl)-3-pyridinyl]-3’H-dispiro[cyclohexane-1,2‘-indene-1’,2”-imidazol]-4”-amine (lr,l’R,4R)- 4-methoxy-5″-methyl-6′-[5-(prop-l-yn-l-yl)pyridin-3-yl]-3’H- dispiro[cyclohexane-l,2′-inden-l’2′-imidazole]-4″-amine (lr,4r)-4-Methoxy-5″-methyl-6′-(5-prop-l-yn-l-ylpyridin-3-yl)-3’H-dispiro[cyclohexane- l,2′-indene-l’,2″-imidazol]- “-amine CAS 1383982-64-6 AZD3293 Dispiro[cyclohexane-1,2′-[1H]indene-1′(3’H),2”-[2H]imidazol]-4”-amine, 4-methoxy-5”-methyl-6‘-[5-(1-propyn-1-yl)-3-pyridinyl]-, (1‘R)- Lanabecestat LY3314814 UNII:X8SPJ492VF, AZ-12304146 Beta amyloid antagonist; Beta secretase 1 inhibitor; Beta secretase 2 inhibitor Fast Track (1α,1’R,4β)-4-Methoxy-5”-methyl-6′-[5-(1-propyn-1-yl)-3-pyridinyl]dispiro[cyclohexane-1,2′-[2H]indene-1′(3’H),2”-[2H]imidazol]-4”-amine (1,4-trans,1’R)-4-methoxy-5”-methyl-6′-[5-(prop-1-yn-1-yl)pyridin-3-yl]-3’H-dispiro[cyclohexane-1,2′-indene-1′,2”-imidazol]-4”-amine (1r,1’R,4R)-4-methoxy-5”-methyl-6′-[5-(prop-1-yn-1-yl)pyridin-3-yl]-3’H-dispiro[cyclohexane-1,2′-indene-1′,2”-imidazol]-4”-amine Lanabecestat (formerly known as AZD3293 or LY3314814) is …

Pridopidine

It’s only fair to share… Pridopidine Molecular Formula C15H23NO2S Average mass 281.414 Da 346688-38-8  CAS FREE FORM 882737-42-0 (hydrochloride) 1440284-30-9 HBr 4-[3-(Methylsulfonyl)phenyl]-1-propylpiperidin 4- (3 -Methanesulfonyl-phenyl ) – 1-propyl -piperidine ACR16 Huntexil UNII-HD4TW8S2VK; 4-[3-(Methylsulfonyl)phenyl]-1-propylpiperidine ACR 16 ASP 2314 FR 310826 Huntingtons chorea Dopamine D2 receptor antagonist; Opioid receptor sigma agonist 1 Neurosearch INNOVATORS, In 2012, the product was acquired by …

Plinabulin

It’s only fair to share… Plinabulin Molecular FormulaC19H20N4O2 Average mass336.388 Da (3Z,6Z)-3-Benzylidène-6-{[4-(2-méthyl-2-propanyl)-1H-imidazol-5-yl]méthylène}-2,5-pipérazinedione 2,5-Piperazinedione, 3-[[5-(1,1-dimethylethyl)-1H-imidazol-4-yl]methylene]-6-(phenylmethylene)-, (3Z,6Z)- CAS 714272-27-2 NPI 2358 NPI-2358; NPI 2358 UNII:986FY7F8XR Phase 3 Clinical Tubulin antagonist Cancer; Febrile neutropenia; Non-small-cell lung cancer Plinabulin (chemical structure, BPI-2358, formerly NPI-2358) is a small molecule under development by BeyondSpring Pharmaceuticals, and is in a world-wide Phase …

Pexidartinib, PLX-3397

It’s only fair to share… Pexidartinib PLX-3397 5-((5-chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)methyl)-N-((6-(trifluoromethyl)pyridin-3-yl)methyl)pyridin-2-amine N-[5-[(5-Chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)methyl]-2-pyridinyl]-6-(trifluoromethyl)-3-pyridinemethanamine 5-[(5-Chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)methyl]-N-[[6-(trifluoromethyl)pyridin-3-yl]methyl]pyridin-2-amine hydrochloride Phase III A Multi-targeted tyrosine kinase inhibitor potentially for the treatment of tenosynovial giant cell tumor (TGCT). CAS 1029044-16-3 C20H15ClF3N5, 417.81 Pexidartinib; 1029044-16-3; PLX-3397; 5-((5-chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)methyl)-N-((6-(trifluoromethyl)pyridin-3-yl)methyl)pyridin-2-amine; 5-[(5-chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)methyl]-N-[[6-(trifluoromethyl)pyridin-3-yl]methyl]pyridin-2-amine; 5-[(5-Chloro-1h-Pyrrolo[2,3-B]pyridin-3-Yl)methyl]-N-{[6-(Trifluoromethyl)pyridin-3-Yl]methyl}pyridin-2-Amine; Originator Plexxikon Developer Barbara Ann Karmanos Cancer Institute; Columbia University; Merck & Co; National Cancer Institute (USA); Plexxikon; University …

Pibrentasvir, ABT-530, A 1325912.0

It’s only fair to share… Pibrentasvir ABT-530, Pibrentasvir, A 1325912.0 Dimethyl N,N’-([(2R,5R)-1-{3,5-difluoro-4-[4-(4-fluorophenyl)piperidin-1-yl]phenyl}pyrrolidine-2,5-diyl]bis{(6-fluoro-1H-benzimidazole-5,2-diyl)[(2S)-pyrrolidine-2,1-diyl][(2S,3R)-3-methoxy-1-oxobutane-1,2-diyl]})biscarbamate Methyl {(2S,3R)-1-[(2S)-2-{5-[(2R,5R)-1-{3,5-difluoro-4-[4-(4-fluorophenyl)piperidin-1-yl]phenyl}-5-(6-fluoro-2-{(2S)-1-[N-(methoxycarbonyl)-O-methyl-L-threonyl]pyrrolidin-2-yl}-1H-benzimidazol-5-yl)pyrrolidin-2-yl]-6-fluoro-1H-benzimidazol-2-yl}pyrrolidin-1-yl]-3-methoxy-1-oxobutan-2-yl}carbamate Dimethyl N,N’-(((2R,5R)-1-(3,5-difluoro-4-(4-(4-fluorophenyl)piperidin-1-yl)phenyl)pyrrolidine-2,5-diyl)bis((6-fluoro-1H-benzimidazole-5,2-diyl)((2S)-pyrrolidine-2,1-diyl)((2S,3R)-3-methoxy-1-oxobutane-1,2-diyl)))biscarbamate Methyl ((2S,3R)-1-((2S)-2-(5-((2R,5R)-1-(3,5-difluoro-4-(4-(4-fluorophenyl)piperidin-1-yl)phenyl)-5-(6-fluoro-2-((2S)-1-(N-(methoxycarbonyl)-O-methyl-L-threonyl)pyrrolidin-2-yl)-1H-benzimidazol-5-yl)pyrrolidin-2-yl)-6-fluoro-1H-benzimidazol-2-yl)pyrrolidin-1-yl)-3-methoxy-1-oxobutan-2-yl)carbamate Phase III Abbott Laboratories  INNOVATOR A protease inhibitor potentially for the treatment of HCV infection. Hepatitis C virus NS 5 protein inhibitors CAS No. 1353900-92-1 MF C57H65F5N10O8 MW 1113.1925 MW Pibrentasvir UNII-2WU922TK3L CLINICAL https://clinicaltrials.gov/search/intervention=A-1325912.0%20OR%20ABT-530%20OR%20Pibrentasvir Pibrentasvir SYNTHESIS PATENT WO 2012051361 http://www.google.com/patents/WO2012051361A1?cl=en Example …