Endocrinology Compound Library (96-Well)
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Endothelin System and Therapeutic Application of Endothelin Receptor
xperim ACCESS Freely available online & E en OPEN l ta a l ic P in h l a C r m f o a c l a o n l o r g u y o J Journal of ISSN: 2161-1459 Clinical & Experimental Pharmacology Research Article Endothelin System and Therapeutic Application of Endothelin Receptor Antagonists Abebe Basazn Mekuria, Zemene Demelash Kifle*, Mohammedbrhan Abdelwuhab Department of Pharmacology, School of Pharmacy, College of Medicine and Health Sciences, University of Gondar, Gondar, Ethiopia ABSTRACT Endothelin is a 21 amino acid molecule endogenous potent vasoconstrictor peptide. Endothelin is synthesized in vascular endothelial and smooth muscle cells, as well as in neural, renal, pulmonic, and inflammatory cells. It acts through a seven transmembrane endothelin receptor A (ETA) and endothelin receptor B (ETB) receptors belongs to G protein-coupled rhodopsin-type receptor superfamily. This peptide involved in pathogenesis of cardiovascular disorder like (heart failure, arterial hypertension, myocardial infraction and atherosclerosis), renal failure, pulmonary arterial hypertension and it also involved in pathogenesis of cancer. Potentially endothelin receptor antagonist helps the treatment of the above disorder. Currently, there are a lot of trails both per-clinical and clinical on endothelin antagonist for various cardiovascular, pulmonary and cancer disorder. Some are approved by FAD for the treatment. These agents are including both selective and non-selective endothelin receptor antagonist (ETA/B). Currently, Bosentan, Ambrisentan, and Macitentan approved -
Corporate Release No 485 12 December 2012 FDA Accepts
H. Lundbeck A/S Ottiliavej 9 Tel +45 36 30 13 11 E-mail [email protected] DK-2500 Valby, Copenhagen Fax +45 36 43 82 62 www.lundbeck.com CVR number: 56759913 Corporate Release No 485 12 December 2012 FDA accepts Takeda and Lundbeck’s filing for review of Brintellix (vortioxetine) for the treatment of major depression FDA has determined that the New Drug Application filed in October 2012 is sufficiently complete to permit a substantive review Upon the acceptance of the filing by the FDA, Lundbeck is to receive a milestone of USD 50 million (approximately DKK 285 million) from Takeda H. Lundbeck A/S (Lundbeck) announced today that the U.S. Food and Drug Administration (FDA) has accepted the submission of a New Drug Application (NDA) for BrintellixTM (vortioxetine) for the treatment of major depressive disorder (MDD) in adult patients. Brintellix (pronounced “brin′-tel-ix”) is the proposed global trade name for vortioxetine. According to the timelines established by the Prescription Drug User Fee Act (PDUFA), the review of the NDA is targeted for completion by 2 October, 2013. The NDA includes positive data from six short-term studies and one long-term maintenance study. The vortioxetine global clinical development program included more than 7,500 individuals aged 18 to 88 years old exposed to the drug. Major depression, often referred to as depression, is a common, debilitating illness affecting around 15 million Americans and 121 million people worldwide. Depression was the third leading contributor to the global burden of disease in 2004 and is projected to be the leading contributor to the worldwide burden of disease by 2030. -
(12) Patent Application Publication (10) Pub. No.: US 2017/0152273 A1 Merchant Et Al
US 20170152273A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2017/0152273 A1 Merchant et al. (43) Pub. Date: Jun. 1, 2017 (54) TOPCAL PHARMACEUTICAL Publication Classification FORMULATIONS FOR TREATING (51) Int. Cl. NFLAMMLATORY-RELATED CONDITIONS C07F 5/02 (2006.01) Applicant: A6II 47/06 (2006.01) (71) Anacor Pharmaceuticals Inc., New A69/06 (2006.01) York, NY (US) A6IR 9/00 (2006.01) (72) Inventors: Tejal Merchant, Cupertino, CA (US); A6II 47/8 (2006.01) Dina Jean Coronado, Danville, CA A6II 45/06 (2006.01) (US); Charles Edward Lee, Union A6II 47/10 (2006.01) City, CA (US); Delphine Caroline A6II 3/69 (2006.01) Imbert, Cupertino, CA (US); Sylvia (52) U.S. Cl. Zarela Yep, Milpitas, CA (US) CPC .............. C07F 5/025 (2013.01); A61K 47/10 (2013.01); A61K 47/06 (2013.01); A61K3I/69 (73) Assignee: Anacor Pharmaceuticals Inc., New (2013.01); A61K 9/0014 (2013.01); A61 K York, NY (US) 47/183 (2013.01); A61K 45/06 (2013.01); A61K 9/06 (2013.01); C07B 2.200/13 (21) Appl. No.: 15/364,347 (2013.01) (22) Filed: Nov. 30, 2016 (57) ABSTRACT Related U.S. Application Data (60) Provisional application No. 62/420,987, filed on Nov. Topical pharmaceutical formulations, and methods of treat 11, 2016, provisional application No. 62/260,716. ing inflammatory conditions with these formulations, are filed on Nov. 30, 2015. disclosed. Patent Application Publication Jun. 1, 2017. Sheet 1 of 4 US 2017/0152273 A1 ?zzzzzzzzzzzzzzzzzzzzzzzzzzzz ????????????????????????????????????????????????????????????????????? S&S&S Šx&N Sssssssssssssssssssssssssssssssssssssss (r) eqn. O. peppy jeeNA go eunO/A Patent Application Publication Jun. -
Cyclohexyl Amide Derivatives As Crf Receptor
(19) TZZ ¥_Z_T (11) EP 2 531 490 B1 (12) EUROPEAN PATENT SPECIFICATION (45) Date of publication and mention (51) Int Cl.: of the grant of the patent: A61K 31/4155 (2006.01) A61P 25/24 (2006.01) 15.10.2014 Bulletin 2014/42 C07D 213/82 (2006.01) C07D 231/12 (2006.01) C07D 231/14 (2006.01) C07D 231/16 (2006.01) (2006.01) (2006.01) (21) Application number: 11701824.2 C07D 231/20 C07D 231/38 C07D 231/54 (2006.01) C07D 231/56 (2006.01) C07D 249/08 (2006.01) C07D 401/04 (2006.01) (22) Date of filing: 31.01.2011 C07D 401/12 (2006.01) C07D 401/14 (2006.01) C07D 405/04 (2006.01) C07D 471/04 (2006.01) C07D 473/00 (2006.01) C07D 491/052 (2006.01) C07C 233/79 (2006.01) (86) International application number: PCT/EP2011/051293 (87) International publication number: WO 2011/095450 (11.08.2011 Gazette 2011/32) (54) CYCLOHEXYL AMIDE DERIVATIVES AS CRF RECEPTOR ANTAGONISTS CYCLOHEXYLAMIDDERIVATE ALS CRF-REZEPTORANTAGONISTEN DÉRIVÉS DE CYCLOHEXYLAMIDE À TITRE D’ANTAGONISTES DU RÉCEPTEUR CRF (84) Designated Contracting States: • COLSON, Anny-Odile AL AT BE BG CH CY CZ DE DK EE ES FI FR GB Horsham GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO Sussex RH12 5AB (GB) PL PT RO RS SE SI SK SM TR • CULSHAW, Andrew James Horsham (30) Priority: 17.12.2010 US 424258 P Sussex RH12 5AB (GB) 02.02.2010 US 300576 P • SHARP, Thomas Horsham (43) Date of publication of application: Sussex RH12 5AB (GB) 12.12.2012 Bulletin 2012/50 (74) Representative: Woodcock-Bourne, Heather (73) Proprietor: Novartis AG Novartis Pharma AG 4056 Basel (CH) Patent Department Postfach (72) Inventors: 4002 Basel (CH) •BEATTIE,David Horsham (56) References cited: Sussex RH12 5AB (GB) WO-A1-2010/015655 • BRUCE, Ian Horsham • GILLIGAN, P. -
(12) Patent Application Publication (10) Pub. No.: US 2004/0116357 A1 Fushimi Et Al
US 2004O116357A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2004/0116357 A1 Fushimi et al. (43) Pub. Date: Jun. 17, 2004 (54) GLUCOPYRANOSYLOXYPYRAZOLE DERVATIVES AND MEDICINAL USE THEREOF (I) (76) Inventors: Nobuhiko Fushimi, Matsumoto-shi (JP); Hideki Fujikura, Matsumoto-shi (JP); Toshihiro Nishimura, Minamiazumi-gun (JP); Kenji Katsuno, Kamiina-gun (JP); Masayuki Isaji, Shiojiri-shi (JP) Correspondence Address: SUGHRUE MION, PLLC 2100 PENNSYLVANIAAVENUE, N.W. SUTE 800 WASHINGTON, DC 20037 (US) (21) Appl. No.: 10/469,140 (22) PCT Filed: Feb. 26, 2002 (86) PCT No.: PCT/JP02/01708 wherein R', R and R represent a hydrogen atom or a (30) Foreign Application Priority Data halogen atom; R" represents a lower alkyl group or a halo(lower alkyl) group; and R represents a hydrogen atom, Feb. 27, 2001 (JP)...................................... 2001-053085 a lower alkyl group, a lower alkoxy group, a lower alkylthio group, etc., a pharmaceutically acceptable Salt thereof or a Publication Classification prodrug thereof., which exert an excellent inhibitory activity (51) Int. Cl. ................................................ A61K 31/7056 in human SGLT2, and therefore are useful as drugs for the (52) U.S. Cl. ............................................. 514/23: 536/17.4 prevention or treatment of a disease associated with hyper glycemia Such as diabetes, diabetic complications or obesity, (57) ABSTRACT pharmaceutically acceptable Salts thereof or prodrugs The present invention provides glucopyranosyloxypyrazole thereof, production intermediates thereof and pharmaceuti derivatives represented by the general formula: cal uses thereof. US 2004/0116357 A1 Jun. 17, 2004 GLUCOPYRANOSYLOXYPYRAZOLE 0005. In recent years, development of new type antidia DERVATIVES AND MEDICINAL USE THEREOF betic agents has been progressing, which promote urinary glucose excretion and lower blood glucose level by prevent TECHNICAL FIELD ing excess glucose reabsorption at the kidney (J. -
Minilap: a MIGS Approach to the Benign Large Adnexal Mass Surgical Technique Video
MDEDGE.COM/OBGYN | VOL 31, NO 4 | APRIL 2019 Society of Gynecologic Surgeons Annual Meeting Highlights Issue Peripartum depression: New counseling guidelines Robert L. Barbieri, MD Update on prenatal exome sequencing AAnnenne H.H. Mardy,Mardy, MD;MD; MaryMary E.E. Norton,Norton, MDMD A member of the Network Minilap: A MIGS approach to the benign large adnexal mass Surgical technique video Beyond ERAS Sean C. Dowdy, MD HT and Alzheimer disease: An association? Andrew M. Kaunitz, MD Vaginal anatomy for the gyn surgeon p. SS4 FoFollowllow us on FFacebookacebook aandnd Twitter C1 0419.indd 1 4/2/19 11:59 AM TAKE A NEXT STEP IN MODERATE TO SEVERE ENDOMETRIOSIS PAIN1 Clinical study design: Two robust, similar, multicenter, Dysmenorrhea double-blind, prospective, placebo-controlled phase 3 (150 mg or 200 mg) trials of 6-month treatment at 2 doses as compared with placebo in premenopausal women (18 to 49 years of age) Non-menstrual with surgically diagnosed endometriosis and moderate or Pelvic Pain (NMPP) severe endometriosis-associated pain (N=1686).1,2 (150 mg or 200 mg) • Co-primary efficacy endpoints (independently evaluated): proportion of responders for dysmenorrhea at month 3 1 Dyspareunia* and proportion of responders for NMPP at month 3 (200 mg only) *Statistical significance for dyspareunia was not achieved with the 150 mg QD dose of ORILISSA. INDICATION Change in Menstrual Bleeding Pattern and Reduced Ability to ORILISSA® (elagolix) is indicated for the management of Recognize Pregnancy moderate to severe pain associated with endometriosis. • Women who take ORILISSA may experience a reduction in the IMPORTANT SAFETY INFORMATION amount, intensity, or duration of menstrual bleeding, which may reduce the ability to recognize the occurrence of pregnancy CONTRAINDICATIONS in a timely manner. -
A Randomized, Double-Blind, Placebo-Controlled Study
medRxiv preprint doi: https://doi.org/10.1101/2020.04.06.20055715; this version posted April 11, 2020. The copyright holder for this preprint (which was not certified by peer review) is the author/funder, who has granted medRxiv a license to display the preprint in perpetuity. It is made available under a CC-BY-NC-ND 4.0 International license . 1 Mo%on Sifnos: A randomized, double-blind, placebo-controlled study demonstra%ng the effec%veness of tradipitant in the treatment of mo%on sickness Vasilios M. Polymeropoulos*1, Mark É. Czeisler1#a, Mary M. Gibson1¶, Aus%n A. Anderson1¶, Jane Miglo1#b, Jingyuan Wang1, Changfu Xiao1, Christos M. Polymeropoulos1, Gunther Birznieks1, Mihael H. Polymeropoulos1 1 Vanda Pharmaceu%cals, Washington, District of Columbia, United States of America #a The Ins%tute for Breathing and Sleeping, Aus%n Health, Heidelberg, Victoria, Australia #b College of Pharmacy, University of Illinois at Chicago, Chicago, Illinois, United States of America *Corresponding author Email: [email protected] (VMP) ¶These authors contributed equally to this work. NOTE: This preprint reports new research that has not been certified by peer review and should not be used to guide clinical practice. medRxiv preprint doi: https://doi.org/10.1101/2020.04.06.20055715; this version posted April 11, 2020. The copyright holder for this preprint (which was not certified by peer review) is the author/funder, who has granted medRxiv a license to display the preprint in perpetuity. It is made available under a CC-BY-NC-ND 4.0 International license . 2 Abstract Background Novel therapies are needed for the treatment of mo%on sickness given the inadequate relief, and bothersome and dangerous adverse effects of currently approved therapies. -
Modifications to the Harmonized Tariff Schedule of the United States to Implement Changes to the Pharmaceutical Appendix
United States International Trade Commission Modifications to the Harmonized Tariff Schedule of the United States to Implement Changes to the Pharmaceutical Appendix USITC Publication 4208 December 2010 U.S. International Trade Commission COMMISSIONERS Deanna Tanner Okun, Chairman Irving A. Williamson, Vice Chairman Charlotte R. Lane Daniel R. Pearson Shara L. Aranoff Dean A. Pinkert Address all communications to Secretary to the Commission United States International Trade Commission Washington, DC 20436 U.S. International Trade Commission Washington, DC 20436 www.usitc.gov Modifications to the Harmonized Tariff Schedule of the United States to Implement Changes to the Pharmaceutical Appendix Publication 4208 December 2010 (This page is intentionally blank) Pursuant to the letter of request from the United States Trade Representative of December 15, 2010, set forth at the end of this publication, and pursuant to section 1207(a) of the Omnibus Trade and Competitiveness Act, the United States International Trade Commission is publishing the following modifications to the Harmonized Tariff Schedule of the United States (HTS) to implement changes to the Pharmaceutical Appendix, effective on January 1, 2011. Table 1 International Nonproprietary Name (INN) products proposed for addition to the Pharmaceutical Appendix to the Harmonized Tariff Schedule INN CAS Number Abagovomab 792921-10-9 Aclidinium Bromide 320345-99-1 Aderbasib 791828-58-5 Adipiplon 840486-93-3 Adoprazine 222551-17-9 Afimoxifene 68392-35-8 Aflibercept 862111-32-8 Agatolimod -
204569Orig1s000
CENTER FOR DRUG EVALUATION AND RESEARCH APPLICATION NUMBER: 204569Orig1s000 MEDICAL REVIEW(S) Cross Discipline Team Leader Review 3. CMC/Device Dr. Khairuzzaman found the drug product portion of the NDA to be acceptable, and without need for phase 4 commitments. Dr. Sapru’s review stated that with the exception of a pending issue concerning the control of potential genotoxic impurity (b) (4) the NDA was approvable in terms of drug substance. Dr. Suarez found that the NDA was acceptable from a biopharmaceutics perspective. The Office of Compliance issuance of an acceptable recommendation for drug substance manufacturing and testing facilities was pending at the time of this review. 4. Nonclinical Pharmacology/Toxicology Dr. Richard Siarey completed the primary nonclinical review, and Dr. Lois Freed completed a supervisory memo. Dr. Siarey’s overall conclusion was that from a nonclinical perspective, approval of the suvorexant NDA was recommended. However, he found evidence that catapelxy was observed in dogs exposed to MK-4305 (suvorexant) near Tmax, although he concluded that additional information could have been gained by studying the drug in an experimental model that has been used for diagnosing cataplexy in dogs. Dr. Siarey suggested that since cataplexy occurred in dogs near Tmax, a time at which if used for insomnia patients would ordinarily be in bed, safety concern for humans was reduced. Dr. Siarey also found that the neurobehavioral assessment in the pre- and post-natal developmental study was not complete, as the passive avoidance tests was performed too early in development, while learning/acquisition tests and retention/memory tests were not conducted. -
Anti-Infectives Industry Over the Next 5 Years and Beyond
Bridging the innovation gap... New Drug Futures: Products that could change the pharma market to 2013 and beyond Over 70 pipeline prospects This new major and insightful 450 page in 8 major therapy areas analysis evaluates, compares and contrasts the are analysed in this report prospects for the development compounds that could revolutionise the pharmaceutical Anti-infectives industry over the next 5 years and beyond. Cardiovascular CNS The report provides: Gastrointestinal Detailed background and market context for Metabolic each therapy area covered: Musculoskeletal Addressable patient population Oncology Current treatments Sales drivers Respiratory Sales breakers Future treatments Market dynamics – winners and losers Key drug launches by 2013 Unique sales forecasts by major product to 2013 Over 70 key products assessed Unique evaluation scores for key areas such as novelty of mechanism, clinical data and competition Critical and detailed appraisal of each product‟s research and development Extensive pipeline listings, putting the profiled products into their competitive context The search – and need – for new products has never been greater and what’s in the development pipeline has never generated more interest. That is why this analysis is so important! GLOBAL PHARMA MARKET IN CONTEXT THE Are there too many prophets of doom ready to write-off the research-based pharma industry in the future? Too few novel There is plenty on which to base such anxiety. The research-based industry products and an must achieve a fair price in the face of greater cost control, while the aggressive generic burden of regulation is setting the bar high for successful product sector are taking introduction. -
Are Supplements Supplemented? Evaluating the Composition of Complementary and Alternative Medicines Using Mass Spectrometry and Metabolomics
Are supplements supplemented? Evaluating the composition of complementary and alternative medicines using mass spectrometry and metabolomics By Elly Gwyn Crighton BForensics in Forensic Biology & Toxicology (First Class Honours) BSc in Molecular Biology & Biomedical Science This thesis is presented for the degree of Doctor of Philosophy Perth, Western Australia at Murdoch University 2020 Declaration I declare that: i. The thesis is my own account of my research, except where other sources are acknowledged. ii. The extent to which the work of others has been used is clearly stated in each chapter and certified by my supervisors. iii. The thesis contains as its main content, work that has not been previously submitted for a degree at any other university. i Abstract The complementary and alternative medicines (CAM) industry is worth over US$110 billion globally. Products are available to consumers with little medical advice; with many assuming that such products are ‘natural’ and therefore safe. However, with adulterated, contaminated and fraudulent products reported on overseas markets, consumers may be placing their health at risk. Previous studies into product content have reported undeclared plant materials, ingredient substitution, adulteration and contamination. However, no large-scale, independent audit of CAM has been undertaken to demonstrate these problems in Australia. This study aimed to investigate the content and quality of CAM products on the Australian market. 135 products were analysed using a combination of next-generation DNA sequencing and liquid chromatography-mass spectrometry. Nearly 50% of products tested had contamination issues, in terms of DNA, chemical composition or both. 5% of the samples contained undeclared pharmaceuticals. -
United States Patent (19) (11) 4,310,524 Wiech Et Al
United States Patent (19) (11) 4,310,524 Wiech et al. 45 Jan. 12, 1982 (54) TCA COMPOSITION AND METHOD FOR McMillen et al., Fed. Proc., 38,592 (1979). RAPD ONSET ANTDEPRESSANT Sellinger et al., Fed. Proc., 38,592 (1979). THERAPY Pandey et al., Fed. Proc., 38,592 (1979). 75) Inventors: Norbert L. Wiech; Richard C. Ursillo, Primary Examiner-Stanley J. Friedman both of Cincinnati, Ohio Attorney, Agent, or Firm-Millen & White 73) Assignee: Richardson-Merrell, Inc., Wilton, Conn. (57 ABSTRACT A method is provided for treating depression in a pa (21) Appl. No.: 139,498 tient therefrom and requiring rapid symptomatic relief, (22 Filed: Apr. 11, 1980 which comprises administering to said patient concur 51) Int. Cl. .................... A61K 31/33; A61K 31/135 rently (a) an effective antidepressant amount of a tricy clic antidepressant or a pharmaceutically effective acid (52) ...... 424/244; 424/330 addition salt thereof, and (b) an amount of an a-adrener 58) Field of Search ................................ 424/244, 330 gic receptor blocking agent effective to achieve rapid (56) References Cited onset of the antidepressant action of (a), whereby the PUBLICATIONS onset of said antidepressant action is achieved within Chemical Abst., vol. 66-72828m, (1967), Kellett. from 1 to 7 days. Chemical Abst, vol. 68-94371a, (1968), Martelli et al. A pharmaceutical composition is also provided which is Chemical Abst., vol. 74-86.048j, (1971), Dixit et al. especially adapted for use with the foregoing method. Holmberg et al., Psychopharm., 2,93 (1961). Svensson, Symp. Med. Hoechst., 13, 245 (1978). 17 Claims, No Drawings 4,310,524 1.