DR ANTHONY MELVIN CRASTO Ph.D

Pinnick oxidation

The Pinnick oxidation is also known as Lindgren oxidation. It is an organic reaction by which aldehydes can be oxidized into its corresponding carboxylic acid, originally developed by Lindgren and Nilsson.ref1 The typical reaction condition used today was modified by G. A. Kraus even before Pinnick.ref2,3 Pinnick proved this condition as general. There are number of ways to oxidize the aldehydes however, only… Continue reading Pinnick oxidation

US 6894199, Process for the production of xylitol

(2R,4S)-Pentane-1,2,3,4,5-pentol Xylitol used to denote sugar alcohols) is a sugar alcohol sweetener used as a sugar substitute. Xylitol has the formula (CHOH)3(CH2OH)2 and is an achiral isomer of pentane-1,2,3,4,5-pentol. Xylitol is roughly as sweet as sucrose with 33% fewer calories. Unlike other sweeteners, xylitol is actively beneficial for dental health, reducing caries to a third in regular use, and has been shown to reduce… Continue reading US 6894199, Process for the production of xylitol

AVANAFIL, NEW DRUG FOR ERECTILE DYSFUNCTION, FDA APRIL 2012

Avanafil is a PDE5 inhibitor approved for erectile dysfunction on April 27, 2012.[1] Avanafil is known by the trademark name Stendra and was developed by Vivus Inc. It acts by inhibiting a specific phosphodiesterase type 5 enzyme which is found in various body tissues, but primarily in the corpus cavernosum penis, as well as the retina. Other similar drugs are sildenafil, tadalafil and vardenafil. The advantage of avanafil is that… Continue reading AVANAFIL, NEW DRUG FOR ERECTILE DYSFUNCTION, FDA APRIL 2012

New Data for Jakafi® (Ruxolitinib) to Be Presented at the 2012 American Society of Hematology Annual Meeting

Ruxolitinib (3R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]propanenitrile, CAS number 941678-49-5 Incyte Corporation (Nasdaq: INCY) announced today that several analyses from clinical studies of Jakafi® (ruxolitinib) will be presented at the 2012 American Society of Hematology (ASH) Annual Meeting from Dec. 8 to 11 , 2012 at the Georgia World Congress Center in Atlanta. Jakafi, an oral Janus kinase (JAK) inhibitor,… Continue reading New Data for Jakafi® (Ruxolitinib) to Be Presented at the 2012 American Society of Hematology Annual Meeting

FDA accepts AVEO-Astellas tivozanib NDA filing for renal cell carcinoma, 29 nov 2012

1-{2-Chloro-4-[(6,7-dimethoxyquinolin-4-yl)oxy]phenyl}-3-(5-methylisoxazol-3-yl)urea AV-951 Tivozanib (AV-951) is an oral VEGF receptor tyrosine kinase inhibitor. It is undergoing clinical trial investigation for the treatment of renal cell carcinomas.[1] An oral quinoline urea derivative, tivozanib suppresses angiogenesis by being selectively inhibitory against vascular endothelial growth factor.[2] It was developed by AVEO Pharmaceuticals.[3] It is designed to inhibit all three VEGF receptors.[4] Phase III results on advanced renal cell carcinoma suggest a 30%… Continue reading FDA accepts AVEO-Astellas tivozanib NDA filing for renal cell carcinoma, 29 nov 2012

Substituted indole derivatives for the treatment of immunological disorders,WO 2012156936, Novartis AG, Protein kinase C theta inhibitor

TITLE-Substituted indole derivatives for the treatment of immunological disorders Protein kinase C theta inhibitor WO 2012156936, 22.11.2012, Novartis AG GENERAL STRUCTURE DESCRIBED IS Phosphoric acid mono-[3-[3-(4,7-diaza-spiro[2.5]oct-7-yl)-isoquinolin-1 -yl]-4-(7-methyl-1 H-indol-3-yl)-2,5-dioxo-2,5-dihydro-pyrrol-1 -ylmethyl] ester 1H-NMR (400 MHz, DMSO-d6): 12.10 (s, 1 H), 8.08 (d, 1 H), 7.65-7.61 (m, 2H), 7.44 (f, 1 H), 7.20 (s, 1 H), 7.06 (f, 1… Continue reading Substituted indole derivatives for the treatment of immunological disorders,WO 2012156936, Novartis AG, Protein kinase C theta inhibitor

cis z jasmone

Jasmone is a natural organic compound extracted from the volatile portion of the oil fromjasmine flowers. It is a colorless to pale yellow liquid that has the odor of jasmine. Jasmone can exist in two isomeric forms with differing geometry around the pentenyl double bond, cis-jasmone and trans-jasmone. The natural extract contains only the cis form, while synthetic material is often… Continue reading cis z jasmone

WO 2012130821, BENZOIC ACID SALT OF OTAMIXABAN (SANOFI)

Otamixaban (INN) is a direct factor Xa inhibitor,[1] currently being developed by the French pharmaceutical company Sanofi-Aventis as a treatment for acute coronary syndrome. Methyl (2R,3R)-2-{3-[amino(imino)methyl]benzyl}-3-{[4-(1-oxidopyridin-4-yl)benzoyl]amino}butanoate Guertin KR, Choi YM (2007). “The discovery of the Factor Xa inhibitor otamixaban: from lead identification to clinical development”. Curr. Med. Chem. 14 (23): 2471–81.doi:10.2174/092986707782023659. PMID 17979700. Methyl (2R,3R)-2-{3-[amino(imino)methyl]benzyl}-3-{[4-(1 -oxidopyridin-4-yl)benzoyl]amino}butanoate, (CAS number 193153-04-7) has the International Nonproprietary Name Otamixaban The present… Continue reading WO 2012130821, BENZOIC ACID SALT OF OTAMIXABAN (SANOFI)

Sucampo and Abbott Announce Launch of AMITIZA in Japan, 26 nov 2012

Sucampo and Abbott Announce Launch of AMITIZA in Japan Product is Japan’s Only Prescription Medicine for Chronic Constipation Lubiprostone CAS number 136790-76-6 Sucampo Pharmaceuticals, Inc. and Abbott today announced the availability of AMITIZA® (lubiprostone) in Japan, a prescription medicine for the treatment of chronic constipation not caused by organic diseases. AMITIZA was approved by the Ministry of Health,… Continue reading Sucampo and Abbott Announce Launch of AMITIZA in Japan, 26 nov 2012

Total synthesis of artemisinin, WO 2012154906 (A1) 15th nov 2012

Total synthesis of artemisinin, WO2012154906 (A1) 15th nov 2012 link at espacenet http://worldwide.espacenet.com/publicationDetails/biblio?DB=EPODOC&II=0&ND=3&adjacent=true&locale=en_EP&FT=D&date=20121115&CC=WO&NR=2012154906A1&KC=A1 Indiana University Research And Technology Corporation Inventors Cook, Silas; Zhu, Chun-Yin Application number: WO2012US37214 2012 05 10 Priority number(s): US201161484317P 2011 05 10 Oxidative synthesis; Rearrangement synthesis, The present invention provides a method for manufacturing artemisinin and its congeners from cyclohexenone as… Continue reading Total synthesis of artemisinin, WO 2012154906 (A1) 15th nov 2012