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Nitrate Prodrugs Able to Release Nitric Oxide in a Controlled and Selective
Europäisches Patentamt *EP001336602A1* (19) European Patent Office Office européen des brevets (11) EP 1 336 602 A1 (12) EUROPEAN PATENT APPLICATION (43) Date of publication: (51) Int Cl.7: C07C 205/00, A61K 31/00 20.08.2003 Bulletin 2003/34 (21) Application number: 02425075.5 (22) Date of filing: 13.02.2002 (84) Designated Contracting States: (71) Applicant: Scaramuzzino, Giovanni AT BE CH CY DE DK ES FI FR GB GR IE IT LI LU 20052 Monza (Milano) (IT) MC NL PT SE TR Designated Extension States: (72) Inventor: Scaramuzzino, Giovanni AL LT LV MK RO SI 20052 Monza (Milano) (IT) (54) Nitrate prodrugs able to release nitric oxide in a controlled and selective way and their use for prevention and treatment of inflammatory, ischemic and proliferative diseases (57) New pharmaceutical compounds of general effects and for this reason they are useful for the prep- formula (I): F-(X)q where q is an integer from 1 to 5, pref- aration of medicines for prevention and treatment of in- erably 1; -F is chosen among drugs described in the text, flammatory, ischemic, degenerative and proliferative -X is chosen among 4 groups -M, -T, -V and -Y as de- diseases of musculoskeletal, tegumental, respiratory, scribed in the text. gastrointestinal, genito-urinary and central nervous sys- The compounds of general formula (I) are nitrate tems. prodrugs which can release nitric oxide in vivo in a con- trolled and selective way and without hypotensive side EP 1 336 602 A1 Printed by Jouve, 75001 PARIS (FR) EP 1 336 602 A1 Description [0001] The present invention relates to new nitrate prodrugs which can release nitric oxide in vivo in a controlled and selective way and without the side effects typical of nitrate vasodilators drugs. -
Daily Lifestyle Modifications to Improve Quality of Life And
brain sciences Review Daily Lifestyle Modifications to Improve Quality of Life and Survival in Glioblastoma: A Review Sarah Travers and N. Scott Litofsky * Division of Neurosurgery, University of Missouri School of Medicine, Columbia, MO 65212, USA; [email protected] * Correspondence: [email protected] Abstract: Survival in glioblastoma remains poor despite advancements in standard-of-care treatment. Some patients wish to take a more active role in their cancer treatment by adopting daily lifestyle changes to improve their quality of life or overall survival. We review the available literature through PubMed and Google Scholar to identify laboratory animal studies, human studies, and ongoing clinical trials. We discuss which health habits patients adopt and which have the most promise in glioblastoma. While results of clinical trials available on these topics are limited, dietary restrictions, exercise, use of supplements and cannabis, and smoking cessation all show some benefit in the comprehensive treatment of glioblastoma. Marital status also has an impact on survival. Further clinical trials combining standard treatments with lifestyle modifications are necessary to quantify their survival advantages. Keywords: survival in glioblastoma; dietary restriction in glioblastoma; cannabis use in glioblastoma; supplementation in glioblastoma; glioblastoma health modifications Citation: Travers, S.; Litofsky, N.S. Daily Lifestyle Modifications to 1. Introduction Improve Quality of Life and Survival Glioblastoma remains the most aggressive and deadly form of primary brain tumor, in Glioblastoma: A Review. Brain Sci. with average survival rates ranging from 7.8 to 23.4 months after diagnosis [1]. Maximal 2021, 11, 533. https://doi.org/ surgical resection followed by radiation and temozolomide have become standard of 10.3390/brainsci11050533 care [2,3]. -
Acne Vulgaris and Intake of Selected Dietary Nutrients—A Summary of Information
healthcare Review Acne Vulgaris and Intake of Selected Dietary Nutrients—A Summary of Information Aleksandra Podgórska †, Anna Pu´scion-Jakubik*,† , Renata Markiewicz-Zukowska˙ , Krystyna Joanna Gromkowska-K˛epkaand Katarzyna Socha Department of Bromatology, Faculty of Pharmacy with the Division of Laboratory Medicine, Medical University of Białystok, Mickiewicza 2D Street, 15-222 Białystok, Poland; [email protected] (A.P.); [email protected] (R.M.-Z.);˙ [email protected] (K.J.G.-K.); [email protected] (K.S.) * Correspondence: [email protected]; Tel.: +48-8574-854-69 † Contributed equally. Abstract: Acne vulgaris (AV) is a chronic disease that affects a significant percentage of the world’s population. Its development is influenced by both external and internal factors. The purpose of this review is to demonstrate the effect of basic nutrient intake on the exacerbation or alleviation of AV lesions. A retrospective review of publications in PubMed regarding diet therapy and the impact of individual nutrient intake on the skin condition of patients was conducted. Ingestion of products with a high glycaemic index may indirectly lead to sebum overproduction, which promotes infection with Cutibacterium acnes and causes inflammation. Consumption of certain dairy products may result Citation: Podgórska, A.; in skin deterioration caused by the presence of hormones in these products, i.e., progesterone and Pu´scion-Jakubik,A.; testosterone precursors. The beneficial effect of fatty acids on the skin is manifested by the reduction Markiewicz-Zukowska,˙ R.; Gromkowska-K˛epka,K.J.; Socha, K. in inflammation. Of significance in AV treatment are vitamins A, C, D, E and B, as well as mineral Acne Vulgaris and Intake of Selected elements zinc and selenium. -
Pp375-430-Annex 1.Qxd
ANNEX 1 CHEMICAL AND PHYSICAL DATA ON COMPOUNDS USED IN COMBINED ESTROGEN–PROGESTOGEN CONTRACEPTIVES AND HORMONAL MENOPAUSAL THERAPY Annex 1 describes the chemical and physical data, technical products, trends in produc- tion by region and uses of estrogens and progestogens in combined estrogen–progestogen contraceptives and hormonal menopausal therapy. Estrogens and progestogens are listed separately in alphabetical order. Trade names for these compounds alone and in combination are given in Annexes 2–4. Sales are listed according to the regions designated by WHO. These are: Africa: Algeria, Angola, Benin, Botswana, Burkina Faso, Burundi, Cameroon, Cape Verde, Central African Republic, Chad, Comoros, Congo, Côte d'Ivoire, Democratic Republic of the Congo, Equatorial Guinea, Eritrea, Ethiopia, Gabon, Gambia, Ghana, Guinea, Guinea-Bissau, Kenya, Lesotho, Liberia, Madagascar, Malawi, Mali, Mauritania, Mauritius, Mozambique, Namibia, Niger, Nigeria, Rwanda, Sao Tome and Principe, Senegal, Seychelles, Sierra Leone, South Africa, Swaziland, Togo, Uganda, United Republic of Tanzania, Zambia and Zimbabwe America (North): Canada, Central America (Antigua and Barbuda, Bahamas, Barbados, Belize, Costa Rica, Cuba, Dominica, El Salvador, Grenada, Guatemala, Haiti, Honduras, Jamaica, Mexico, Nicaragua, Panama, Puerto Rico, Saint Kitts and Nevis, Saint Lucia, Saint Vincent and the Grenadines, Suriname, Trinidad and Tobago), United States of America America (South): Argentina, Bolivia, Brazil, Chile, Colombia, Dominican Republic, Ecuador, Guyana, Paraguay, -
Enzyme Mediated Inflammation: Epidemiology and Therapeutic Implications Parteek Prasher*
Available online www.jocpr.com Journal of Chemical and Pharmaceutical Research, 2016, 8(9):89-100 ISSN : 0975-7384 Review Article CODEN(USA) : JCPRC5 Enzyme Mediated Inflammation: Epidemiology and Therapeutic implications Parteek Prasher* Assistant Professor of Chemistry, University of Petroleum and Energy Study, Energy acres, Uttrakhand, India ___________________________________________________________________________________ ABSTRACT The identification of various enzymes participating in the arachidonic acid metabolism and recognition of inflammatory metabolites led to systematic studies for the development of anti-inflammatory drugs. Starting with the stimulatory role of phospholipases to release arachidonic acid from phospholipids, over-expression of cyclooxygenase-2 (COX-2) and lipoxygenase (LOX) enzymes cause more than normal production of the respective metabolites. Excessive production of prostaglandins and leukotrienes leads to the manifestation of acute to chronic inflammation in humans. The consequent ailments are expressed in the form of asthma, atherosclerosis, irritable bowel syndrome, arthritis and cancer. Targeting the induced isoform of cyclooxygenase viz. cyclooxygenase-2 (COX-2) and 5-LOX enzyme has opened new aspects for capping the enzyme mediated inflammation. A number of such aspects have been discussed in this comprehensive review. Keywords: COX; Cyclooxygenase; LOX; Lipoxygenase; Arachidonic acid ___________________________________________________________________________________ INTRODUCTION According to a recent survey of the World Health Organization (WHO), cancer causes around 13% of the total deaths worldwide and if it continues rising, it is estimated to cause 13.1 million deaths in 2030 [1]. Moreover, the reason for about 15% of the total cancer deaths has been reported [2] to be associated with chronic inflammation. Hence, an obvious way out to minimize cancer deaths is to put control over the inflammatory conditions. -
Vitamin D and Its Analogues Decrease Amyloid- (A) Formation
International Journal of Molecular Sciences Article Vitamin D and Its Analogues Decrease Amyloid-β (Aβ) Formation and Increase Aβ-Degradation Marcus O. W. Grimm 1,2,3,*,† ID , Andrea Thiel 1,† ID , Anna A. Lauer 1 ID , Jakob Winkler 1, Johannes Lehmann 1,4, Liesa Regner 1, Christopher Nelke 1, Daniel Janitschke 1,Céline Benoist 1, Olga Streidenberger 1, Hannah Stötzel 1, Kristina Endres 5, Christian Herr 6 ID , Christoph Beisswenger 6, Heike S. Grimm 1 ID , Robert Bals 6, Frank Lammert 4 and Tobias Hartmann 1,2,3 1 Experimental Neurology, Saarland University, Kirrberger Str. 1, 66421 Homburg/Saar, Germany; [email protected] (A.T.); [email protected] (A.A.L.); [email protected] (J.W.); [email protected] (J.L.); [email protected] (L.R.); [email protected] (C.N.); [email protected] (D.J.); [email protected] (C.B.); [email protected] (O.S.); [email protected] (H.S.); [email protected] (H.S.G.); [email protected] (T.H.) 2 Neurodegeneration and Neurobiology, Saarland University, Kirrberger Str. 1, 66421 Homburg/Saar, Germany 3 Deutsches Institut für DemenzPrävention (DIDP), Saarland University, Kirrberger Str. 1, 66421 Homburg/Saar, Germany 4 Department of Internal Medicine II–Gastroenterology, Saarland University Hospital, Saarland University, Kirrberger Str. 100, 66421 Homburg/Saar, Germany; [email protected] 5 Department of Psychiatry and Psychotherapy, Clinical Research Group, University Medical Centre Johannes Gutenberg, University of Mainz, Untere Zahlbacher Str. 8, 55131 Mainz, Germany; [email protected] 6 Department of Internal Medicine V–Pulmonology, Allergology, Respiratory Intensive Care Medicine, Saarland University Hospital, Kirrberger Str. -
MMC International BV
M.M.C. International Steroid Substances Steroid Test A Colour Steroid Test B Colour Steroid Test B Colour with UV Light Stanozolol/ Oxandrolone Test Clenbuterol/ Oxymetholone Test Ephedrine Test Alfadolone Orange Yellow Nil - - - Androsterone Orange Yellow White - - - Beclometasone Brown–yellow Orange Nil - - - Betamethasone Orange–brown Pink–Orange Nil - - - Boldenone Base (Equipoise, Ganabol) (pure powder) Warm red after 2 min. Dark Orange after 2 min. Bright Light Orange - - - Boldenone Undecanoate (oil) Dark brownish-red Dark Red Bright Light Orange - - - Boldenone Undecylenate (oil) Orange - Light Brown Dark Orange → Brown Bright Light Orange-Yellow - - - Carbenoxolone (CBX) Orange Yellow Yellow - - - Cholesterol Violet Orange White - - - Clenbuterol (Spiropent, Ventipulmin) - - - - Purple - Dark brown with yellow-green on the Dark brown with yellow-green on the Clomiphene (Androxal, Clomid, Omifin) Nil Dark brown to black No reaction Dark brown to black sides of the ampoule sides of the ampoule Cortisone Orange Yellow Green - - - Desoxycortone Blue–black Yellow Yellow - - - Dexamethasone Yellow Orange–pink Nil - - - Dienestrol Yellow Orange–red Nil - - - Diethylstilbestrol (DES) Orange (→yellow–green) Nil - - - Dimethisterone Brown–green Orange–red Yellow - - - Drostanolone Propionate (Masteron) (oil) Bright green Yellow-Orange Orange - - - Dydrogesterone (Duphaston) - Orange Green-Yellow - - - Enoxolone Orange Yellow Green-Yellow - - - Ephedrine (also for Pseudo- and Nor-Ephedrine) - - - - - Orange Estradiol (Oestradiol) Orange -
(12) Patent Application Publication (10) Pub. No.: US 2014/0296.191 A1 PATEL Et Al
US 20140296.191A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2014/0296.191 A1 PATEL et al. (43) Pub. Date: Oct. 2, 2014 (54) COMPOSITIONS OF PHARMACEUTICAL (52) U.S. Cl. ACTIVES CONTAINING DETHYLENE CPC ............... A61K 47/10 (2013.01); A61 K9/0019 GLYCOL MONOETHYLETHER OR OTHER (2013.01); A61 K9/0048 (2013.01); A61 K ALKYL DERVATIVES 45/06 (2013.01) USPC ........... 514/167: 514/177; 514/178: 514/450; (71) Applicant: THEMIS MEDICARE LIMITED, 514/334: 514/226.5: 514/449; 514/338; Mumbai (IN) 514/256; 514/570; 514/179; 514/174: 514/533; (72) Inventors: Dinesh Shantilal PATEL, Mumbai (IN); 514/629; 514/619 Sachin Dinesh PATEL, Mumbai (IN); Shashikant Prabhudas KURANI, Mumbai (IN); Madhavlal Govindlal (57) ABSTRACT PATEL, Mumbai (IN) (73) Assignee: THEMIS MEDICARE LIMITED, The present invention relates to pharmaceutical compositions Mumbai (IN) of various pharmaceutical actives, especially lyophilic and hydrophilic actives containing Diethylene glycol monoethyl (21) Appl. No.: 14/242,973 ether or other alkyl derivatives thereofas a primary vehicle and/or to pharmaceutical compositions utilizing Diethylene (22) Filed: Apr. 2, 2014 glycol monoethyl ether or other alkyl derivatives thereofas a primary vehicle or as a solvent system in preparation of Such (30) Foreign Application Priority Data pharmaceutical compositions. The pharmaceutical composi Apr. 2, 2013 (IN) ......................... 1287/MUMA2013 tions of the present invention are safe, non-toxic, exhibits enhanced physical stability compared to conventional formu Publication Classification lations containing such pharmaceutical actives and are Suit able for use as injectables for intravenous and intramuscular (51) Int. Cl. administration, as well as for use as a preformed solution/ A647/ (2006.01) liquid for filling in and preparation of capsules, tablets, nasal A6 IK 45/06 (2006.01) sprays, gargles, dermal applications, gels, topicals, liquid oral A6 IK9/00 (2006.01) dosage forms and other dosage forms. -
Combined Estrogen–Progestogen Menopausal Therapy
COMBINED ESTROGEN–PROGESTOGEN MENOPAUSAL THERAPY Combined estrogen–progestogen menopausal therapy was considered by previous IARC Working Groups in 1998 and 2005 (IARC, 1999, 2007). Since that time, new data have become available, these have been incorporated into the Monograph, and taken into consideration in the present evaluation. 1. Exposure Data 1.1.2 Progestogens (a) Chlormadinone acetate Combined estrogen–progestogen meno- Chem. Abstr. Serv. Reg. No.: 302-22-7 pausal therapy involves the co-administration Chem. Abstr. Name: 17-(Acetyloxy)-6-chlo- of an estrogen and a progestogen to peri- or ropregna-4,6-diene-3,20-dione menopausal women. The use of estrogens with IUPAC Systematic Name: 6-Chloro-17-hy- progestogens has been recommended to prevent droxypregna-4,6-diene-3,20-dione, acetate the estrogen-associated risk of endometrial Synonyms: 17α-Acetoxy-6-chloro-4,6- cancer. Evidence from the Women’s Health pregnadiene-3,20-dione; 6-chloro-Δ6-17- Initiative (WHI) of adverse effects from the use acetoxyprogesterone; 6-chloro-Δ6-[17α] of a continuous combined estrogen–progestogen acetoxyprogesterone has affected prescribing. Patterns of exposure Structural and molecular formulae, and relative are also changing rapidly as the use of hormonal molecular mass therapy declines, the indications are restricted, O CH and the duration of the therapy is reduced (IARC, 3 C 2007). CH3 CH3 O C 1.1 Identification of the agents CH3 H O 1.1.1 Estrogens HH For Estrogens, see the Monograph on O Estrogen-only Menopausal Therapy in this Cl volume. C23H29ClO4 Relative molecular mass: 404.9 249 IARC MONOGRAPHS – 100A (b) Cyproterone acetate Structural and molecular formulae, and relative Chem. -
Simulation of Physicochemical and Pharmacokinetic Properties of Vitamin D3 and Its Natural Derivatives
pharmaceuticals Article Simulation of Physicochemical and Pharmacokinetic Properties of Vitamin D3 and Its Natural Derivatives Subrata Deb * , Anthony Allen Reeves and Suki Lafortune Department of Pharmaceutical Sciences, College of Pharmacy, Larkin University, Miami, FL 33169, USA; [email protected] (A.A.R.); [email protected] (S.L.) * Correspondence: [email protected] or [email protected]; Tel.: +1-224-310-7870 or +1-305-760-7479 Received: 9 June 2020; Accepted: 20 July 2020; Published: 23 July 2020 Abstract: Vitamin D3 is an endogenous fat-soluble secosteroid, either biosynthesized in human skin or absorbed from diet and health supplements. Multiple hydroxylation reactions in several tissues including liver and small intestine produce different forms of vitamin D3. Low serum vitamin D levels is a global problem which may origin from differential absorption following supplementation. The objective of the present study was to estimate the physicochemical properties, metabolism, transport and pharmacokinetic behavior of vitamin D3 derivatives following oral ingestion. GastroPlus software, which is an in silico mechanistically-constructed simulation tool, was used to simulate the physicochemical and pharmacokinetic behavior for twelve vitamin D3 derivatives. The Absorption, Distribution, Metabolism, Excretion and Toxicity (ADMET) Predictor and PKPlus modules were employed to derive the relevant parameters from the structural features of the compounds. The majority of the vitamin D3 derivatives are lipophilic (log P values > 5) with poor water solubility which are reflected in the poor predicted bioavailability. The fraction absorbed values for the vitamin D3 derivatives were low except for calcitroic acid, 1,23S,25-trihydroxy-24-oxo-vitamin D3, and (23S,25R)-1,25-dihydroxyvitamin D3-26,23-lactone each being greater than 90% fraction absorbed. -
SEAC) Held on 01/10/2019 at Committee Room, Gujarat Pollution Control Board, Sector 10A,Gandhinagar
Minutes of the 554 th meeting ofthe State Level Expert Appraisal Committee (SEAC) held on 01/10/2019 at Committee Room, Gujarat Pollution Control Board, Sector 10A,Gandhinagar. The 554 th meeting of the State Level Expert Appraisal Committee (SEAC) was held on 1st October 2019 at Committee Room, Gujarat Pollution Control Board, Sector 10A, Gandhinagar. Following members attended the meeting: 1. Dr. Dinesh Misra, Chairman, SEAC 2. Shri S. C. Srivastav, Vice Chairman, SEAC 3. Shri Rajesh. I. Shah, Member, SEAC 4. Shri V. N. Patel, Member, SEAC 5. Dr. V. K. Jain, Member, SEAC 6. Shri A. K. Mule, Member, SEAC The regular agenda of Appraisal, Screening & Scoping/ToR, Reconsideration cases were taken up. The Committee considered the applications made by project proponents, additional details submitted as required by the SEAC/SEIAA and details furnished in the Form-1, PFR, EIA-EMP reports. Proposal No. Name and Address of the Unit Remarks 04 SIA/GJ/IND2/29059/2017 M/s. Dev Dyechem Industries EC – Plot No. C-1/324, Phase-I & II GIDC – Reconsideration Naroda, Ahmedabad. • PP remained absent in the EC – Appraisal presentation held on 01/10/2019. • After detailed discussion, Committee decided to defer the proposal and consider the same in one of the upcoming meeting of SEAC. 05 SIA/GJ/IND2/29678/2018 M/s. Apex Pharma EC – C-298/2/4, Saykha Industrial Estate, Reconsideration Saykha, Ta- Vagra, Dist -Bharuch. Category of the unit: 5(f) Project status: New • Project proponent (PP) submitted online application vide no. SIA/GJ/IND2/29678/2018 dated 30/04/19 for obtaining Environmental Clearance. -
The Use of Stems in the Selection of International Nonproprietary Names (INN) for Pharmaceutical Substances
WHO/PSM/QSM/2006.3 The use of stems in the selection of International Nonproprietary Names (INN) for pharmaceutical substances 2006 Programme on International Nonproprietary Names (INN) Quality Assurance and Safety: Medicines Medicines Policy and Standards The use of stems in the selection of International Nonproprietary Names (INN) for pharmaceutical substances FORMER DOCUMENT NUMBER: WHO/PHARM S/NOM 15 © World Health Organization 2006 All rights reserved. Publications of the World Health Organization can be obtained from WHO Press, World Health Organization, 20 Avenue Appia, 1211 Geneva 27, Switzerland (tel.: +41 22 791 3264; fax: +41 22 791 4857; e-mail: [email protected]). Requests for permission to reproduce or translate WHO publications – whether for sale or for noncommercial distribution – should be addressed to WHO Press, at the above address (fax: +41 22 791 4806; e-mail: [email protected]). The designations employed and the presentation of the material in this publication do not imply the expression of any opinion whatsoever on the part of the World Health Organization concerning the legal status of any country, territory, city or area or of its authorities, or concerning the delimitation of its frontiers or boundaries. Dotted lines on maps represent approximate border lines for which there may not yet be full agreement. The mention of specific companies or of certain manufacturers’ products does not imply that they are endorsed or recommended by the World Health Organization in preference to others of a similar nature that are not mentioned. Errors and omissions excepted, the names of proprietary products are distinguished by initial capital letters.