Sirolimus (INN/USAN), also known as rapamycin, is an immunosuppressant drug used to prevent rejection in organ transplantation; it is especially useful in kidneytransplants. It prevents activation of T cells and B cells by inhibiting their response tointerleukin-2 (IL-2). A macrolide, sirolimus was discovered by Brazilian researchers as a product of the bacterium Streptomyces hygroscopicus in a soil sample from Easter Island[1] — an island also known as Rapa Nui.[2] It was approved by the… Continue reading Immunosuppressant Drug Rapamycin Helps Preserving Female Fertility
Category: DRUGS
AT13148, Drug Blocks Multiple Cancer Causes
AT13148 AT13148 is a multi-AGC kinase, ATP-competitive inhibitor, identified utilizing high-throughput X-ray crystallography and fragment-based lead discovery techniques. AT13148 caused substantial blockade of AKT, p70S6K, PKA, ROCK and SGK substrate phosphorylation and induction of apoptosis in both a concentration and time-dependent manner in cancer cells with clinically relevant genetic defects both in vitro and in… Continue reading AT13148, Drug Blocks Multiple Cancer Causes
Bedaquiline(Sirturo, TMC207 or R207910) FDA approves 1st new tuberculosis drug in 40 years
(1R,2S)-1-(6-Bromo-2-methoxy-3-quinolyl)-4-dimethylamino-2-(1-naphthyl)-1-phenyl-butan-2-ol, cas no 654653-81-3 Bedaquiline FDA approves 1st new tuberculosis drug in 40 years The Food and Drug Administration on Monday approved a Johnson & Johnson tuberculosis drug that is the first new medicine to fight the deadly infection in more than four decades. Bedaquiline (also known as Sirturo, TMC207 or R207910) is an diarylquinoline anti-tuberculosis drug, which was discovered… Continue reading Bedaquiline(Sirturo, TMC207 or R207910) FDA approves 1st new tuberculosis drug in 40 years
LM11A-31, New drug can help paralyzed people walk again
LM11A-31, C12 H25 N3 O2, Pentanamide, 2-amino-3-methyl-N–[2-(4-morpholinyl)ethyl]– WO 2010102212 TO LONGO FRANK, PUB 10.09.2010 THE UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL PATENT LINK http://patentscope.wipo.int/search/en/WO2010102212 Scientists have developed a pill which they claim could help paralyzed people walk again. The new drug allowed mice with no movement in their lower limbs to walk… Continue reading LM11A-31, New drug can help paralyzed people walk again
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
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)