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(12) Patent Application Publication (10) Pub. No.: US 2006/0110428A1 De Juan Et Al
US 200601 10428A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2006/0110428A1 de Juan et al. (43) Pub. Date: May 25, 2006 (54) METHODS AND DEVICES FOR THE Publication Classification TREATMENT OF OCULAR CONDITIONS (51) Int. Cl. (76) Inventors: Eugene de Juan, LaCanada, CA (US); A6F 2/00 (2006.01) Signe E. Varner, Los Angeles, CA (52) U.S. Cl. .............................................................. 424/427 (US); Laurie R. Lawin, New Brighton, MN (US) (57) ABSTRACT Correspondence Address: Featured is a method for instilling one or more bioactive SCOTT PRIBNOW agents into ocular tissue within an eye of a patient for the Kagan Binder, PLLC treatment of an ocular condition, the method comprising Suite 200 concurrently using at least two of the following bioactive 221 Main Street North agent delivery methods (A)-(C): Stillwater, MN 55082 (US) (A) implanting a Sustained release delivery device com (21) Appl. No.: 11/175,850 prising one or more bioactive agents in a posterior region of the eye so that it delivers the one or more (22) Filed: Jul. 5, 2005 bioactive agents into the vitreous humor of the eye; (B) instilling (e.g., injecting or implanting) one or more Related U.S. Application Data bioactive agents Subretinally; and (60) Provisional application No. 60/585,236, filed on Jul. (C) instilling (e.g., injecting or delivering by ocular ion 2, 2004. Provisional application No. 60/669,701, filed tophoresis) one or more bioactive agents into the Vit on Apr. 8, 2005. reous humor of the eye. Patent Application Publication May 25, 2006 Sheet 1 of 22 US 2006/0110428A1 R 2 2 C.6 Fig. -
Labeling and Synthesis of Estrogens and Their Metabolites
Labeling and Synthesis of Estrogens and Their Metabolites Paula Kiuru University of Helsinki Faculty of Science Department of Chemistry Laboratory of Organic Chemistry P.O. Box 55, 00014 University of Helsinki, Finland ACADEMIC DISSERTATION To be presented with the permission of the Faculty of Science of the University of Helsinki, for public criticism in Auditorium A110 of the Department of Chemistry, A. I. Virtasen Aukio 1, Helsinki, on June 18th, 2005 at 12 o'clock noon Helsinki 2005 ISBN 952-91-8812-9 (paperback) ISBN 952-10-2507-7 (PDF) Helsinki 2005 Valopaino Oy. 1 ABSTRACT 3 ACKNOWLEDGMENTS 4 LIST OF ORIGINAL PUBLICATIONS 5 LIST OF ABBREVIATIONS 6 1. INTRODUCTION 7 1.1 Nomenclature of estrogens 8 1.2 Estrogen biosynthesis 10 1.3 Estrogen metabolism and cancer 10 1.3.1 Estrogen metabolism 11 1.3.2 Ratio of 2-hydroxylation and 16α-hydroxylation 12 1.3.3 4-Hydroxyestrogens and cancer 12 1.3.4 2-Methoxyestradiol 13 1.4 Structural and quantitative analysis of estrogens 13 1.4.1 Structural elucidation 13 1.4.2 Analytical techniques 15 1.4.2.1 GC/MS 16 1.4.2.2 LC/MS 17 1.4.2.3 Immunoassays 18 1.4.3 Deuterium labeled internal standards for GC/MS and LC/MS 19 1.4.4 Isotopic purity 20 1.5 Labeling of estrogens with isotopes of hydrogen 20 1.5.1 Deuterium-labeling 21 1.5.1.1 Mineral acid catalysts 21 1.5.1.2 CF3COOD as deuterating reagent 22 1.5.1.3 Base-catalyzed deuterations 24 1.5.1.4 Transition metal-catalyzed deuterations 25 1.5.1.5 Deuteration without catalyst 27 1.5.1.6 Halogen-deuterium exchange 27 1.5.1.7 Multistep labelings 28 1.5.1.8 Summary of deuterations 30 1.5.2 Enhancement of deuteration 30 1.5.2.1 Microwave irradiation 30 1.5.2.2 Ultrasound 31 1.5.3 Tritium labeling 32 1.6 Deuteration estrogen fatty acid esters 34 1.7 Synthesis of 2-methoxyestradiol 35 1.7.1 Halogenation 35 1.7.2 Nitration of estrogens 37 1.7.3 Formylation 38 1.7.4 Fries rearrangement 39 1.7.5 Other syntheses of 2-methoxyestradiol 39 1.7.6 Synthesis of 4-methoxyestrone 40 1.8 Synthesis of 2- and 4-hydroxyestrogens 41 2. -
Effects of Chronic Treatment with Testosterone Propionate on Aggression and Hormonal Levels in Intact Male Mice
Psychoneuroendocrinology, Vol. 23, No. 3, pp. 275–293, 1998 © 1998 Elsevier Science Ltd. All rights reserved Printed in Great Britain 0306-4530/98 $19.00+.00 PII: S0306-4530(97)00005-5 EFFECTS OF CHRONIC TREATMENT WITH TESTOSTERONE PROPIONATE ON AGGRESSION AND HORMONAL LEVELS IN INTACT MALE MICE S. Martı´nez-Sanchis, A. Salvador, L. Moya-Albiol, E. Gonza´lez-Bono and V. M. Simo´n Area de Psicobiologı´a, Facultad de Psicologı´a, Universitat de Vale`ncia, Avenida Blasco Iban˜ez n° 21, Apartado 22109, 46071 Valencia, Spain (Recei6ed 31 January 1997; in final form 22 No6ember 1997) SUMMARY Effects of testosterone propionate, an anabolic-androgenic steroid (AAS), on aggression in gonadally intact male mice were examined. Animals were given weekly injections of 3.75, 7.5, 15, and 30 mg/kg of drug or sesame oil for 10 weeks. During the last 3 weeks, behavioral tests were conducted and at the end of the experiment, body, liver and testes weight and hormonal data were collected. The treatment had minimal behavioral and endocrine effects. It resulted in shorter latencies of ‘threat’ only in the last agonistic encounter, increases in testosterone levels and decreases in testes weight in a non-linear dose-dependant way. The action of the treatment was different on threat and attack, the latter being unaffected. The behavioral effects in the total sample were only found in aggressive animals selected on the basis of their latency of attack in the first encounter. © 1998 Elsevier Science Ltd. All rights reserved. Keywords—AAS; Testosterone; Corticosterone; Aggression; Intact male mice; Individual differences. -
Pharmaceutical Appendix to the Tariff Schedule 2
Harmonized Tariff Schedule of the United States (2007) (Rev. 2) Annotated for Statistical Reporting Purposes PHARMACEUTICAL APPENDIX TO THE HARMONIZED TARIFF SCHEDULE Harmonized Tariff Schedule of the United States (2007) (Rev. 2) Annotated for Statistical Reporting Purposes PHARMACEUTICAL APPENDIX TO THE TARIFF SCHEDULE 2 Table 1. This table enumerates products described by International Non-proprietary Names (INN) which shall be entered free of duty under general note 13 to the tariff schedule. The Chemical Abstracts Service (CAS) registry numbers also set forth in this table are included to assist in the identification of the products concerned. For purposes of the tariff schedule, any references to a product enumerated in this table includes such product by whatever name known. ABACAVIR 136470-78-5 ACIDUM LIDADRONICUM 63132-38-7 ABAFUNGIN 129639-79-8 ACIDUM SALCAPROZICUM 183990-46-7 ABAMECTIN 65195-55-3 ACIDUM SALCLOBUZICUM 387825-03-8 ABANOQUIL 90402-40-7 ACIFRAN 72420-38-3 ABAPERIDONUM 183849-43-6 ACIPIMOX 51037-30-0 ABARELIX 183552-38-7 ACITAZANOLAST 114607-46-4 ABATACEPTUM 332348-12-6 ACITEMATE 101197-99-3 ABCIXIMAB 143653-53-6 ACITRETIN 55079-83-9 ABECARNIL 111841-85-1 ACIVICIN 42228-92-2 ABETIMUSUM 167362-48-3 ACLANTATE 39633-62-0 ABIRATERONE 154229-19-3 ACLARUBICIN 57576-44-0 ABITESARTAN 137882-98-5 ACLATONIUM NAPADISILATE 55077-30-0 ABLUKAST 96566-25-5 ACODAZOLE 79152-85-5 ABRINEURINUM 178535-93-8 ACOLBIFENUM 182167-02-8 ABUNIDAZOLE 91017-58-2 ACONIAZIDE 13410-86-1 ACADESINE 2627-69-2 ACOTIAMIDUM 185106-16-5 ACAMPROSATE 77337-76-9 -
Directory of Suppliers
Directory of Suppliers The directory lists the major suppliers of instruments and acces sories. A more complete list can be found in J. Gas Chromatog., June 1965. Suppliers are generally listed under one heading only although many of the large instrument manufacturers supply most of the listed accessories and supplies. INSTRUMENTS AMERICAN INSTRUMENT CO., INC. MICRO-TEK INSTRUMENTS, INC. 8030 Georgia Avenue P. O. Box 15409 Silver Spring, Maryland 20910 Baton Rouge. Louisiana BARBER-COLMAN COMPANY NESTER/FAUST Rockford. Illinois 2401 Ogletown Road Newark, Delaware BECKMAN INSTRUMENTS. INC. 2500 Harbor Boulevard PACKARD INSTRUMENT CO .. INC. Fullerton. California 92634 2200 Warrenville Road Downers Grove, Illinois 60515 BURRELL CORPORATION 2223 Fifth Avenue THE PERKIN-ELMER CORP. Pittsburgh 19, Pennsylvania 870 Main Avenue Norwalk, Connecticut CARY INSTRUMENTS Applied Physics Corporation 2724 South Peck Road WARNER-CHILCOTT LABORATORIES Monrovia, California Instrument Division 200 South Garrard Boulevard F & M SCIENTIFIC CORP. Richmond, California Route 41 and Starr Road Avondale, Pennsyl vania WILKENS INSTRUMENT & RESEARCH INC. 2700 Mitchell Drive, Box 313 GLOWALL CORPORATION Walnut Creek. California 2530 Wyandotte Road Willow Grove, Pennsylvania BECKER-DELFT (Julian H. Becker N.V.) JARRELL-ASH COMPANY Vulcanusweg 113, P. O. Box 219 590 Lincoln Street Delft, Holland Waltham, Massachusetts 02154 BODENSEEWERK PERKIN ELMER & CO. LOENCO, INC. GmbH 2092 North Lincoln Avenue 777 Uberlingen/Bodensee Altadena, California 91002 West Germany 267 268 Directory of Suppliers CARLO ERBA S.p.A. JOHNS-MANVILLE PRODUCTS CORP. Via Carlo Imbonati, 24 Celite Division Milano, Italy 22 East 40th Street New York, New York GAS CHROMATOGRAPHY LIMITED Boyn Valley Road, Maidenhead MAY & BAKER LIMITED Berkshire, England Dagenham Essex, England W. -
Relationship Between Prenatal Characteristics and Body Condition and Endocrine Profile in Rabbits
animals Article Relationship between Prenatal Characteristics and Body Condition and Endocrine Profile in Rabbits María-Luz García 1,* , Raquel Muelas 1, María-José Argente 1 and Rosa Peiró 2 1 Departamento de Tecnología Agroalimentaria, Universidad Miguel Hernández de Elche, Ctra de Beniel km 3.2, 03312 Orihuela, Spain; [email protected] (R.M.); [email protected] (M.-J.A.) 2 Instituto de Conservación y Mejora de la Agrodiversidad Valenciana, Universitat Politècnica de València, P.O. Box 22012, 46071 Valencia, Spain; [email protected] * Correspondence: [email protected] Simple Summary: Litter size is an essential trait in rabbit production, and it depends on ovulation rate and embryonic and foetal survival. The period between 8 and 18 d of gestation is critical for foetal survival, as the placenta controls foetal nutrition during this period. Ovulation rate and foetal survival at 12 d of gestation are affected by body condition and metabolic and hormonal profile. Higher foetal survival is related to a higher number of vessels arriving at the implantation site, and may be due to higher available space for the foetus. Abstract: This study evaluated the relationship between prenatal characteristics and body condition and endocrine profile. A total of 25 non-lactating multiparous females were used. Body condition, measured as body weight and perirenal fat thickness, non-esterified fatty acids (NEFA), leptin, progesterone and 17β-estradiol were recorded at mating and 12 d of gestation. Ovulation rate, number of foetuses, ovary and foetal weight, length and weight of uterine horn, available space per foetus and maternal and foetal placental morphometry were recorded at 12 d of gestation. -
Expression of Progesterone Receptor Related to the Polymorphism in the PGR Gene in the Rabbit Reproductive Tract1
Expression of progesterone receptor related to the polymorphism in the PGR gene in the rabbit reproductive tract1 R. Peiró,*2 A. Herrler,† M. A. Santacreu,* M. Merchán,‡ M. J. Argente,§ M. L. García,§ J. M. Folch,‡ and A. Blasco* *Instituto de Ciencia y Tecnología Animal, Universidad Politécnica de Valencia, PO Box 22012, 46071 Valencia, Spain; †Department of Anatomy and Reproductive Biology, Medical School, RWTH University of Aachen, Wendlingweg 2, 52057 Aachen, Germany; ‡Departament de Ciència Animal i dels Aliments, Universitat Autònoma de Barcelona, 08193 Bellaterra, Spain; and §Departamento de Tecnología Agroalimentaria, Universidad Miguel Hernández de Elche, 03312 Orihuela, Spain ABSTRACT: The association of the 2464G > A SNP AA genotype in the oviduct (GG/AAPR-B = 0.81 and found in the promoter region of the rabbit progester- GG/AAPR-A = 0.73) and uterus (around 0.70 in both one receptor gene with progesterone receptor (PR) ex- isoforms). The GA genotype showed similar PR-A ex- pression was evaluated by Western blot analysis. This pression in both tissues and also similar PR-B expres- SNP was associated with 2 lines divergently selected sion in the oviduct to the GG genotype. Conversely, for uterine capacity, the high line selected to increase the GG genotype showed less PR-B expression than uterine capacity and the low line selected to decrease the GA genotype in the uterus (GG/GAPR-B = 0.79). uterine capacity. Two progesterone isoforms were ob- Similar expression of both PR isoforms was found in tained using a commercial monoclonal antibody: the the uterus at d 2 and 3 of gestation; meanwhile, an PR-B isoform described previously in rabbits, and the increase of both isoforms was observed in the oviduct. -
Synthetic Modifications of Estrogens and Androgens
Synthetic Modifications of Estrogens and Androgens Somdatta Deb University of Helsinki Faculty of Science Department of Chemistry Laboratory of Organic Chemistry Finland ACADEMIC DISSERTATION To be presented with the permission of the Faculty of Scienec of the University of Helsinki for public criticism in Auditorium A110, Department of Chemistry on June 23rd, 2011, at 12 o’clock. Helsinki 2011 Supervisor Professor Kristiina Wähälä Laboratory of Organic Chemistry Department of Chemistry University of Helsinki Finland Reviewers Professor Erkki Kolehmainen Department of Chemistry University of Jyväskyla Finland Docent Salme Koskimies Adjunct. Professor University of Helsinki Opponent Professor Maria Christina das Neves Oliveira Unidade de Ciências Químicas e Radiofarmacêuticas Portugal ISBN 978-952-92-9174-8 (paperback) ISBN 978-952-10-7051-8 (PDF) Helsinki 2011 Unigrafia Acknowledgements This thesis work was carried out at the Laboratory of Organic Chemistry, Department of Chemistry, University of Helsinki. I would like to express my deep gratitude to my supervisor Prof. Kristiina Wähälä for introducing me to the fascinating field of steroid chemistry and for providing the facilities to do this work. I warmly thank emeritus professor Tapio Hase for his helpful, invaluable scientific advice during my work. Prof. Matti J. Tikkananen and his group are gratefully acknowledged for pleasant collaboration. My warmest thanks are due to all personnel in the Laboratory of Organic Chemistry, specially the members (former and present) of Phyto-Syn group for their support. They have been always there when needed. In particular I would like to thank Gudrun Silvennoinen for technical assistance and friendship. I am thankful to Dr. Ullastiina Hakala for introducing me to the field of ionic liquid. -
United States Patent (19) 11 Patent Number: 6,068,830 Diamandis Et Al
US00606883OA United States Patent (19) 11 Patent Number: 6,068,830 Diamandis et al. (45) Date of Patent: May 30, 2000 54) LOCALIZATION AND THERAPY OF FOREIGN PATENT DOCUMENTS NON-PROSTATIC ENDOCRINE CANCER 0217577 4/1987 European Pat. Off.. WITH AGENTS DIRECTED AGAINST 0453082 10/1991 European Pat. Off.. PROSTATE SPECIFIC ANTIGEN WO 92/O1936 2/1992 European Pat. Off.. WO 93/O1831 2/1993 European Pat. Off.. 75 Inventors: Eleftherios P. Diamandis, Toronto; Russell Redshaw, Nepean, both of OTHER PUBLICATIONS Canada Clinical BioChemistry vol. 27, No. 2, (Yu, He et al), pp. 73 Assignee: Nordion International Inc., Canada 75-79, dated Apr. 27, 1994. Database Biosis BioSciences Information Service, AN 21 Appl. No.: 08/569,206 94:393008 & Journal of Clinical Laboratory Analysis, vol. 8, No. 4, (Yu, He et al), pp. 251-253, dated 1994. 22 PCT Filed: Jul. 14, 1994 Bas. Appl. Histochem, Vol. 33, No. 1, (Papotti, M. et al), 86 PCT No.: PCT/CA94/00392 Pavia pp. 25–29 dated 1989. S371 Date: Apr. 11, 1996 Primary Examiner Yvonne Eyler S 102(e) Date: Apr. 11, 1996 Attorney, Agent, or Firm-Banner & Witcoff, Ltd. 87 PCT Pub. No.: WO95/02424 57 ABSTRACT It was discovered that prostate-specific antigen is produced PCT Pub. Date:Jan. 26, 1995 by non-proStatic endocrine cancers. It was further discov 30 Foreign Application Priority Data ered that non-prostatic endocrine cancers with Steroid recep tors can be stimulated with Steroids to cause them to produce Jul. 14, 1993 GB United Kingdom ................... 93.14623 PSA either initially or at increased levels. -
Stembook 2018.Pdf
The use of stems in the selection of International Nonproprietary Names (INN) for pharmaceutical substances FORMER DOCUMENT NUMBER: WHO/PHARM S/NOM 15 WHO/EMP/RHT/TSN/2018.1 © World Health Organization 2018 Some rights reserved. This work is available under the Creative Commons Attribution-NonCommercial-ShareAlike 3.0 IGO licence (CC BY-NC-SA 3.0 IGO; https://creativecommons.org/licenses/by-nc-sa/3.0/igo). Under the terms of this licence, you may copy, redistribute and adapt the work for non-commercial purposes, provided the work is appropriately cited, as indicated below. In any use of this work, there should be no suggestion that WHO endorses any specific organization, products or services. The use of the WHO logo is not permitted. If you adapt the work, then you must license your work under the same or equivalent Creative Commons licence. If you create a translation of this work, you should add the following disclaimer along with the suggested citation: “This translation was not created by the World Health Organization (WHO). WHO is not responsible for the content or accuracy of this translation. The original English edition shall be the binding and authentic edition”. Any mediation relating to disputes arising under the licence shall be conducted in accordance with the mediation rules of the World Intellectual Property Organization. Suggested citation. The use of stems in the selection of International Nonproprietary Names (INN) for pharmaceutical substances. Geneva: World Health Organization; 2018 (WHO/EMP/RHT/TSN/2018.1). Licence: CC BY-NC-SA 3.0 IGO. Cataloguing-in-Publication (CIP) data. -
Wo 2009/132050 A2
(12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (10) International Publication Number (43) International Publication Date 29 October 2009 (29.10.2009) WO 2009/132050 A2 (51) International Patent Classification: 61/101,1 12 29 September 2008 (29.09.2008) US A61K 39/395 (2006.01) A61K 47/34 (2006.01) 61/140,033 22 December 2008 (22. 12.2008) US A61P 27/16 (2006.01) A61K 9/06 (2006.01) 61/160,233 13 March 2009 (13.03.2009) US (21) International Application Number: (71) Applicants (for all designated States except US): OTON- PCT/US2009/041320 OMY, INC. [US/US]; 5626 Oberlin Drive, Suite 100, San Diego, CA 92121 (US). THE REGENTS OF THE (22) International Filing Date: UNIVERSITY OF CALIFORNIA [US/US]; 1111 2 1 April 2009 (21 .04.2009) Franklin Street, 12th Floor, Oakland, CA 94607 (US). (25) Filing Language: English (72) Inventors; and (26) Publication Language: English (75) Inventors/Applicants (for US only): LICHTER, Jay [US/US]; P.O. Box 676244, Rancho Santa Fe, CA 92067 (30) Priority Data: (US). VOLLRATH, Benedikt [DE/US]; 4704 Niagara 61/046,543 2 1 April 2008 (21 .04.2008) US Avenue, San Diego, CA 92107 (US). TRAMMEL, An¬ 61/048,878 29 April 2008 (29.04.2008) US drew, M. [US/US]; 12485 South Alden Circle, Olathe, 61/127,7 13 14 May 2008 (14.05.2008) us KS 66062 (US). DURON, Sergio, G. [US/US]; 1605 61/055,625 23 May 2008 (23.05.2008) us Neale Street, San Diego, CA 92103 (US). -
Développement De Modèles Prédictifs De La Toxicocinétique De Substances Organiques
Université de Montréal Développement de modèles prédictifs de la toxicocinétique de substances organiques par Thomas Peyret Département de santé environnementale et santé au travail Faculté de Médecine Thèse présentée à la Faculté de Médecine en vue de l’obtention du grade de Ph.D. en Santé Publique option Toxicologie et analyse du risque Février, 2013 © Peyret, 2013 Université de Montréal Faculté des études supérieures et postdoctorales Cette thèse intitulée : Développement de modèles prédictifs de la toxicocinétique de substances organiques Présentée par : Thomas Peyret a été évaluée par un jury composé des personnes suivantes : Marc Baril, président-rapporteur Kannan Krishnan, directeur de recherche Ginette Truchon, membre du jury Yumei Cecilia Tan, examinateur externe Patrick du Souich, représentant du doyen de la FESP Résumé Les modèles pharmacocinétiques à base physiologique (PBPK) permettent de simuler la dose interne de substances chimiques sur la base de paramètres spécifiques à l’espèce et à la substance. Les modèles de relation quantitative structure-propriété (QSPR) existants permettent d’estimer les paramètres spécifiques au produit (coefficients de partage (PC) et constantes de métabolisme) mais leur domaine d’application est limité par leur manque de considération de la variabilité de leurs paramètres d’entrée ainsi que par leur domaine d’application restreint (c. à d., substances contenant CH3, CH2, CH, C, C=C, H, Cl, F, Br, cycle benzénique et H sur le cycle benzénique). L’objectif de cette étude est de développer de nouvelles connaissances et des outils afin d’élargir le domaine d’application des modèles QSPR-PBPK pour prédire la toxicocinétique de substances organiques inhalées chez l’humain.