Formulation development of insoluble drugs has always been a challenge in pharmaceutical development. This presentation reviews some current options to old problem.
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Keryx Biopharmaceuticals has announced that its new drug application (NDA) for Zerenex (ferric citrate coordination complex) has been accepted for filing by the US FDA.
Keryx’s NDA for kidney drug accepted for filing by US FDA
Zerenex aims to lower blood levels of phosphorous in patients undergoing kidney dialysis.
sumanirole
179386-43-7
179386-44-8 (maleate)
Sumanirole maleate, U-95666 (free base), U-95666E, PNU-95666E
| Process for synthesis of chiral 3-substituted tetrahydroquinoline derivatives | |
| Council Of Scientific & Industrial Research | |
| The present invention relates to novel and concise process for the construction of chiral 3-substituted tetrahydroquinoline derivatives based on proline catalyzed asymmetric α-functionalization of aldehyde, followed by in situ reductive cyclization of nitro group under catalytic hydrogenation condition with high optical purities. Further the invention relates to conversion of derived chiral 3-substituted tetrahydroquinoline derivatives into therapeutic agents namely (-)-sumanirole (96% ee) and 1-[(S)-3-(dimethylamino)-3,4-dihydro-6,7-dimethoxy-quinolin-1(2H)-yl]propanone[(S)-903] (92% ee). | |
| Process,sumanirole | |
| Indications | Restless legs syndrome; Parkinsons disease |
| Target-based Actions | Dopamine D2 receptor agonist |
| Other Actions | Anxiolytic; Antiparkinsonian |
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| Inventors | Boopathi, Senthil, Kumar; Arumugam, Sudalai; Rawat, Varun |
| IPC Codes | C07D 215/20; C07D 471/06; C07D 215/38 |
| DRUG | sumanirole |
| Publication Date | 26-Sep-2013 WO-2013140419-A1 |
Sumanirole (PNU-95,666) is a highly selective D2 receptor full agonist, the first of its kind to be discovered. It was developed for the treatment of Parkinson’s disease andrestless leg syndrome. While it has never been approved for medical use it is a highly valuable tool compound for basic research to identify neurobiological mechanisms that are based on a dopamine D2-linked (vs. D1, D3, D4, and D5-linked) mechanism of action
sumanirole
OTHER INFO
D-Phenylalanine (I) was protected as the methyl carbamate (II) by acylation with methyl chloroformate under Schotten-Baumann conditions. The N-methoxy amide (III) was then prepared by coupling of (II) with O-methyl hydroxylamine in the presence of EDC. Cyclization of (III) to the N-methoxy quinolinone (IV) was accomplished by treatment with bis(trifluoroacetoxy)iodobenzene in the presence of trifluoroacetic acid. Simultaneous reduction of the N-methoxy lactam and carbamate functions of (IV) by means of borane-methyl sulfide complex provided diamine (V). The aliphatic amino group of (V) was then selectively protected as the benzyl carbamate (VI) by using N-(benzyloxycarbonyloxy)succinimide at -40 C. Reaction of (VI) with phosgene, followed by treatment of the intermediate carbamoyl chloride with O-methyl hydroxylamine gave rise to the N-methoxy urea derivative (VII). This was cyclized with bis(trifluoroacetoxy)iodobenzene to the imidazoquinolinone (VIII). The N-methoxy and N-benzyloxycarbonyl groups of (VIII) were then removed by hydrogenolysis in the presence of Pearlman’s catalyst, and the title compound was finally converted to the corresponding maleate salt.
JOC 1997,62,(19):6582
http://www.intechopen.com/books/advances-in-prostate-cancer
Edited by Gerhard Hamilton, ISBN 978-953-51-0932-7, Hard cover, 690 pages, Publisher: InTech, Chapters published January 16, 2013 under CC BY 3.0 license
DOI: 10.5772/45948
Prostate cancer is one of the most common types of cancer in men and its treatment was constricted to surgery for confined state and androgen ablation for advanced disease until new options have become available. The present book covers a broad range of novel aspects of prostate cancer diagnosis, treatment and patient care, as well as new research on relevant cell biology. In detail, this special volume focusses on supportive modalities for prostate cancer patients, appropriate selection of novel therapeutic regimens, including inhibitors of steroidal synthesis, cytotoxic agents, as well as intermittent androgen suppression and the roles of prostate cancer stem cells and inflammatory processes.
Epidemiology of Prostate Cancerby Martin Dörr, Anne Schlesinger-Raab and Jutta EngelIs There an Infectious Agent Behind Prostate Cancer?by Ugo RovigattiPsychological and Social Factors influencing Patients’ Treatment Selection for Localised Prostate Cancerby Luke A Robles, Shihning Chou, Owen J Cole, Akhlil Hamid, Amanda Griffiths and Kavita VedharaThe Role of Physiotherapy in the Pre and Post Treatment Interventions in Prostate Cancer Patientsby Mario Bernardo Filho and Mauro Luis Barbosa JúniorAbdominoperineal Resection: Consideration and Limitations of Prostate Cancer Screening and Prostate Biopsyby Zachary Klaassen, Ray S. King, Kelvin A. Moses, Rabii Madi and Martha K. TerrisRadiation Therapy for Prostate Cancerby Shinji KariyaHigh-Dose-Rate Interstitial Brachytherapy as Monotherapy in One Fraction for the Treatment of Favorable Stage Prostate Cancerby Pedro J. PradaTestosterone Measurement and Prostate Cancerby Tine HajdinjakDescribing Prostate Cancer Dynamics: Second Look at PSA- Doubling Time and PSA-Specific Growth Rateby Glenn TismanRational Categorization of the Pipeline of New Treatments for Advanced Cancer – Prostate Cancer as an Exampleby Sarah M. Rudman, Peter G. Harper and Christopher J. SweeneyNovel Therapeutic Settings in the Treatment of Castration- Resistant Prostate Cancerby Miguel Álvarez Múgica, Jesús M. Fernández Gómez, Antonio Jalón Monzón, Erasmo Miguelez García and Francisco Valle GonzálezSteroidal CYP17 Inhibitors for Prostate Cancer Treatment: From Concept to Clinicby Jorge A. R. Salvador, Vânia M. Moreira and Samuel M. SilvestreIntermittent Androgen Suppression Therapy for Prostate Cancer Patients: An Updateby Gerhard Hamilton and Gerhard TheyerStem Cells and Prostate Cancerby Vildan Bozok Çetintaş, Burçin Tezcanlı Kaymaz and Buket KosovaSalinomycin-Induced Apoptosis in Human Prostate Cancer Cellsby Hak-Jong Choi, Kwang-Youn Kim, Sun-Nyoung Yu, Sang-Hun Kim, Sung-Sik Chun, Hak-Sun Yu, Yeong-Min Park and Soon-Cheol AhnNatural Compounds, Antioxidant and Antiandrogens in the Prevention of Prostate Cancer: In vivo Evidences from Murine Models and Human Clinical Studiesby Rossano Lattanzio, Alessia Lamolinara, Mauro Piantelli and Manuela IezziProstate Cancer, Inflammation and Antioxidantsby Marika Crohns, Tuomas Westermarck and Faik AtroshiInflammatory Microenvironment in Prostate Carcinogenesisby Geraldine Gueron, Javier Cotignola and Elba VazquezExpression and Function of Stromal Androgen Receptor in Prostate Cancerby Mandeep Singh, Garrett Daniels, Yirong Li and Pen g LeeProstate Cancer Progression to Androgen Independent Disease: The Role of the PI3K/AKT Pathwayby Jacqueline R Ha, Yu Hao D Huang, Amit Persad and Sujata PersadNon-Androgen Regulated Transcription Factors as Novel Potential Targets for Prostate Cancer Therapyby J. Nathan Davis, Adam H. Greer, Thomas Yong and Shari MeyersTrithorax Genes in Prostate Cancerby Pier-Luc Clermont, Francesco Crea and Cheryl D. HelgasonThe Function of YY1 and Its Oncogenic Role in Prostate Cancerby Daniel B. Stovall and Guangchao SuiThe Role of PARP Activation in Prostate Cancerby Luis A. EspinozaIntegrins in Prostate Cancer Invasion and Metastasisby Paulynn Chin Suyin, Joanne Louise Dickinson and Adele Frances HollowayThe Role of E-Cadherin-Catenin Complex in Prostate Cancer Progressionby Anuradha K. Murali and James S. Norrishttp://www.intechopen.com/books/advances-in-prostate-cancer
http://www.intechopen.com/books/advances-in-prostate-cancer
WORLDDRUGTRACKER
ANNOUNCING ONE LAKH PLUS VIEWS ON ALL BLOGS- DR ANTHONY CRASTO
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DR ANTHONY MELVIN CRASTO, Worlddrugtracker, Born in Mumbai in 1964 and graduated from Mumbai University, Completed his PhD from ICT ,1991, Mumbai, India, in Organic chemistry, The thesis topic was Synthesis of Novel Pyrethroid Analogues, Currently he is working with GLENMARK- GENERICS LTD, Research centre as Principal Scientist, Process Research (bulk actives) at Mahape, Navi Mumbai, India. Prior to joining Glenmark, he worked with major multinationals like Hoechst Marion Roussel, now sSanofi, Searle India ltd, now Rpg lifesciences, etc. he is now helping millions, has million hits on google on all organic chemistry websites. His New Drug Approvals, Green Chemistry International, Eurekamoments in organic chemistry are some most read blogs He has hands on experience in initiation and developing novel routes for drug molecules and implementation them on commercial scale over a 25 year tenure, good knowledge of IPM, GMP, Regulatory aspects, he has several international drug patents published worldwide . He gas good proficiency in Technology transfer, Spectroscopy, Stereochemistry, Synthesis, polymorphism etc He suffered a paralytic stroke in dec 2007 and is bound to a wheelchair, this seems to have injected feul in him to help chemists around the world, he is more active than before and is pushing boundaries, he has one lakh connections on all networking sites, He makes himself available to all, contact him on +91 9323115463, amcrasto@gmail.com
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READ THIS FANTASTIC CHAPTER
By J. Sarek, M. Kvasnica, M. Vlk, M. Urban, P. Dzubak and M. Hajduch
DOI: 10.5772/19582
[1] Dept. of Org. Chem., IMTM, Faculty of Sciences, Palacky University, Olomouc, Czech Republic
[2] Betulinines – Chemical group, Stribrna Skalice, Czech Republic
[3] IOCB, Academy of Sciences, Prague, Czech Republic
[4] Dept. of Nuclear Chemistry, Faculty of Nuclear Sciences and Physical Engineering, CTU, Prague, Czech Republic
[5] Dept. of Chem. and Bioch., Univ. of Colorado at Boulder, Colorado, USA
[6] Lab. of Exp. Medicine, IMTM, Faculty of Medicine and Dentistry, Palacky University and University Hospital in Olomouc, Olomouc, Czech Republic
ALL THE THUMBNAILS FOR READER
Takeda Receives Simultaneous European Marketing Authorization for Three New Type 2 Diabetes Therapies, VipidiaTM (alogliptin) and Fixed-Dose Combinations VipdometTM (alogliptin and metformin) and IncresyncTM (alogliptin and pioglitazone)
Osaka, Japan, September 24, 2013 – Takeda Pharmaceutical Company Limited (Takeda) today announced that the European Commission has granted Marketing Authorization (MA) for VipidiaTM (alogliptin), a dipeptidyl peptidase IV (DPP-4) inhibitor, for the treatment of type 2 diabetes patients who are uncontrolled on existing therapies1-3and for the fixed-dose combination (FDC) therapies VipdometTM (alogliptin with metformin) and IncresyncTM (alogliptin with pioglitazone). The Committee for Medicinal Products for Human Use (CHMP), of the European Medicines Agency (EMA), issued a positive opinion for these products on July 26, 2013.http://www.pharmalive.com/takeda-gets-simultaneous-eu-oks-for-three-new-type-2-diabetes-therapies
