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DRUG APPROVALS BY DR ANTHONY MELVIN CRASTO
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Supervision of Chinese-Made Drug Substances by Philippe André
Why source drug substances from China?
Large markets, economies of scale and cheaper labor;An industrial ecosystem supplying raw materials and equipment;Developed infrastructure and industry friendly policies;About 5,000 manufacturers;
Thousands of chemists and students across China looking for novel synthesis routes for generic drug substances and intermediates.
read all at
http://www.allfordrugs.com/2013/06/21/supervision-of-chinese-made-drug-substances-by-philippe-andre/
Pharmaceutical Industry In Global Market: Issues To Be Handled For Better Growth
In the global market, the position of the pharmaceutical industry is not parallel as compared to other information and technology based industries.
Among the Leading industries, the pharmaceutical industry lacks behind in the growth rate as far as innovative research, capital investment and
government regulations are concern. Most of the countries simply depends on bulk production of the generic drugs and not focused on core research. In
comparison with the growth rate of the electronic and IT industry stands first where as the pharmaceutical comes at the 9th position.
read all at
Vivus has presented data on its already-approved but not-yet-marketed erectile dysfunction drug Stendra which shows that the treatment is effective for sexual activity within 15 minutes.
Stendra (avanafil) was given the green light by the US Food and Drug Administration over a year ago, but there has been no launch yet as Vivus has been seeking a partner. The latest data should be attractive to potential suitors and could help Stendra take on other phosphodiesterase type 5 (PDE5) inhibitors, notably Pfizer’s Viagra (sildenafil) but also Eli Lilly’s Cialis (tadalafil) and Bayer’s Levitra (vardenafil).
read all at
http://www.pharmatimes.com/Article/13-06-20/Vivus_ED_drug_gets_to_work_in_less_than_15_mins.aspx
Avanafil can be synthesized from a benzylamine derivative and a pyrimidine derivative:Yamada, K.; Matsuki, K.; Omori, K.; Kikkawa, K.; 2004, U.S. Patent 6,797,709
- A cutting that phenanthrene by a methylthio urea ( a ) and ethoxy methylene malonate ( 2 ) cyclization of 3 , chloride, phosphorus oxychloride get 4 , 4 with benzyl amine 5 occurred SNAr the reaction product after oxidation with mCPBA 6 . In pyrimidine, if the 2 – and 4 – positions are active simultaneously the same leaving group in the case, SNAr reaction occurs preferentially at 4 – position, but does not guarantee the 2 – side reaction does not occur. Here is an activity of the poor leaving group sulfide spans 2 – bit, and a good leaving group active chlorine occupy four – position, thus ensuring a high regioselectivity of the reaction. 4 – position after completion of the reaction, then the 2 – position of the group activation, where sulfide sulfoxide better than the leaving group. Amino alcohols 7 and 6 recurrence SNAr reaction 8 , 8 after alkaline hydrolysis and acid alpha amidation get that phenanthrene.
HPV Vaccine Halves Infection Rate in Teen Girls
A vaccine against a cervical cancer virus has cut infections in teen girls by half, according to a study released.
read all at
A vaccine against a cervical cancer virus has cut infections in teen girls by half, according to a study released. The study confirms research done before the HPV vaccine came on the market in 2006. But this is the first evidence of how well it works now that it is in general use.
ALMIRALL-Product development pipeline
| Preclin. | Phase I | Phase II | Phase III | Registr. | Registration application | |||
|---|---|---|---|---|---|---|---|---|
    |
||||||||
| LAS190792 |  |
MABA |  |
>2014 | ||||
| Aclidinium bromide | |
Antimuscarinic |  |
Approved by the FDA & EMA | ||||
| AB + Formoterol (LAS40464) | |
Antimuscarinic + LABA |  |
Undisclosed | ||||
| Abediterol (LAS100977) + ICS | |
OD LABA + ICS |  |
>2014 | ||||
| LAS186323 | |
DHODH inhibitor |  |
Undisclosed | ||||
| Sativex® | |
CB agonist |  |
Undisclosed | ||||
| LAS189913 | |
S1P1 |  |
Undisclosed | ||||
| LAS41002 | |
Topical anti-inflamatory |  |
Registration application in EU | ||||
| LAS41004 | |
Combination |  |
2014 | ||||
| LAS41008 | |
Psoriaris |  |
Undisclosed | ||||
| Linaclotide | |
Guanylate cyclase type-C agonist |  |
Approved by the EMA | ||||
AB: Aclidinium Bromide | ICS: Inhaled Corticoesteroid | RA: Reumatoid Artritis | MS: Multiple Sclerosis
IBS-C: Irritable Bowel Syndrome with associated Constipation
http://www.almirall.com/webcorp2/cda/ImD_03_02.jsp?langSuscripcion=3
Amgen In Focus
Amgen In Focus
Seeking Alpha
According to Amgen, they have 45 drugs in development from Phase 1 to Phase 3. Conversely, Gilead has 32 drugs in development and Pfizer has 64. Meanwhile, Gilead only has 8 drugs in Phase 3, Pfizer has 25, and Amgen has 14. 7 of those Phase 3 …
http://seekingalpha.com/article/1510002-amgen-in-focus?source=google_news
Amgen has the second deepest pipeline of drugs of the three large cap biotechs. According to Amgen, they have 45 drugs in development from Phase 1 to Phase 3. Conversely, Gilead has 32 drugs in development and Pfizer has 64. Meanwhile, Gilead only has 8 drugs in Phase 3, Pfizer has 25, and Amgen has 14. 7 of those Phase 3 drugs are focused on cancer treatments for Amgen, more than either Pfizer or Gilead. Keep in mind that 12.4 million people learn they have cancer each year, while 7.6 million people lose that battle each year. The CDC predicts that the global number of cancer related deaths will increase by 80% by 2030. It doesn’t take a rocket scientist to know that cancer treating drugs presents the largest opportunity for any drug maker considering those statistics. Amgen has the inside track versus Gilead and Pfizer as far as quantity of drugs in late stage development.
Modality
Tocilizumab Impresses in Polyarticular Juvenile Arthritis
tocilizumab
Tocilizumab Impresses in Polyarticular Juvenile Arthritis
Medscape
MADRID, Spain — Children with polyarticular juvenile idiopathic arthritis treated with tocilizumab (Actemra, Genentech) achieved high response rates with sustained improvement in the phase 3 CHERISH trial.
The results prompted the US Food and Drug Administration toapprove tocilizumab for this indication. The drug is already approved for systemic juvenile idiopathic arthritis and for adults with moderate to severe rheumatoid arthritis.
read all at
http://www.medscape.com/viewarticle/806572
Tocilizumab (INN, or atlizumab, developed by Hoffmann–La Roche and Chugai and sold under the trade names Actemra and RoActemra) is an immunosuppressive drug, mainly for the treatment of rheumatoid arthritis (RA) and systemic juvenile idiopathic arthritis, a severe form of RA in children. It is a humanized monoclonal antibody against the interleukin-6 receptor (IL-6R). Interleukin 6 (IL-6) is a cytokine that plays an important role in immune response and is implicated in the pathogenesis of many diseases, such asautoimmune diseases, multiple myeloma and prostate cancer.
Adamas claims success with new and improved Parkinson’s drug
amantadine
Adamas claims success with new and improved Parkinson’s drug
Amantadine (trade name Symmetrel, by Endo Pharmaceuticals) is a drug that has US Food and Drug Administration approval for use both as an antiviral and an antiparkinsonian drug. It is the organic compound 1-adamantylamine or 1-aminoadamantane, meaning it consists of an adamantane backbone that has an amino group substituted at one of the four methyne positions. Rimantadine is a closely related derivative of adamantane with similar biological properties.
Apart from medical uses, this compound is useful as a building block, allowing the insertion of an adamantyl group.
According to the US Centers for Disease Control and Prevention, 100% of seasonal H3N2 and 2009 pandemic flu samples tested have shown resistance to adamantanes, and amantadine is no longer recommended for treatment of influenza in the United States. Additionally, its effectiveness as an antiparkinsonian drug is undetermined, with a 2003 Cochrane Review concluding that there was insufficient evidence in support or against its efficacy and safety.
Synthesis
Amantadine may be prepared by reacting adamantane with bromine or nitric acid to give the bromide or nitroester at position one. Reaction of either compound with acetonitrile affords the acetamide, which is hydrolyzed to give 1-adamantylamine:
Celgene saw the firm get European approval for Revlimid as a treatment for a rare form of blood disease
lenalidomide
European Commission has expanded approval on Revlimid (lenalidomide) to allow treatment of patients with transfusion-dependent anaemia due to low or intermediate-1 risk myelodysplastic syndromes (MDS) with an isolated chromosomal abnormality called deletion 5q when other options do not work. MDS is a type of cancer where the production of blood cells and platelets by the bone marrow is disrupted, which can often lead to severe anemia, infections and bleeding.
Patent of Fresenius Kabi Oncology Ltd.Novel intermediates and process for the preparation of lapatinib and…….
LAPATINIB
Lapatinib (INN), used in the form of lapatinib ditosylate, (USAN) (Tykerb/Tyverb, GSK) is an orally active drug for breast cancer and other solid tumours. It is a dual tyrosine kinase inhibitor which interrupts the HER2/neu and epidermal growth factor receptor (EGFR) pathways. It is used in combination therapy for HER2-positive breast cancer. It is used for the treatment of patients with advanced or metastatic breast cancer whose tumors overexpress HER2 (ErbB2).
………………………………………………………..
Beilstein J. Org. Chem. 2013, 9, 2265–2319.
http://www.beilstein-journals.org/bjoc/single/articleFullText.htm?publicId=1860-5397-9-265
GlaxoSmithKline’s lapatinib (3.38, Tykerb) is a novel dual kinase inhibitor used in the treatment of solid tumors such as those found in breast cancer and contains a quinazoline core structure. It consists of a 2,5-disubstituted furan ring, which is directly linked to the aminoquinazoline unit (Scheme 41). The quinazoline heterocycle was prepared starting from 5-iodoanthranilic acid (3.72) via initial condensation with formamidine acetate (3.73) followed by chlorination using oxalyl chloride or phosphorous oxychloride [101]. Performing a nucleophilic aromatic substitution on the chloride 3.74 with aniline 3.75 renders the extended core of lapatinib. This intermediate (3.76) was then coupled with 5-formyl-2-furanoboronic acid (3.77) using standard Suzuki cross-coupling conditions. Finally, a reductive amination of the pendant aldehyde of 3.78 with 2-(methylsulfonyl)ethylamine (3.79) furnishes the desired product lapatinib (Scheme 41).
![[1860-5397-9-265-i41]](http://www.beilstein-journals.org/bjoc/content/inline/1860-5397-9-265-i41.png?scale=2.0&max-width=1024&background=FFFFFF)
http://www.beilstein-journals.org/bjoc/single/articleFullText.htm?publicId=1860-5397-9-265
……………………………………………..
Fresenius Kabi Oncology Ltd.WO 2013080218
Lahiri, Saswata; Gupta, Nitin; Singh, Hemant Kumar; Handa, Vishal; Sanghani, Sunil
6 JUNE 2013, http://www.google.com/patents/WO2013080218A1?cl=en
Literature References: Reversible dual inhibitor of ErbB1 and ErbB2 tyrosine kinases. Prepn: M. C. Carter et al., WO 9935146(1999 to Glaxo); eidem, US 6727256 (2004 to SmithKline Beecham). Mechanism of action study: W. Xia et al., Oncogene 21, 6255 (2002); and crystal structure in complex with epidermal growth factor receptor (EGFR, ErbB1): E. R. Wood et al., Cancer Res. 64, 6652 (2004). In vitro antitumor activity in combination with anti-ErbB2 antibodies: W. Xia et al., Oncogene 24, 6213 (2005). Biologic effects on tumor growth: N. L. Spector et al., J. Clin. Oncol. 23, 2502 (2005). Pharmacokinetics and clinical activity in metastatic carcinomas: H. A. Burris III et al., ibid. 5305. Review of clinical development: T. E. Kim, J. R. Murren, IDrugs6, 886-893 (2003); H. A. Burris III, Oncologist 9, Suppl. 3, 10-15 (2004).
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