Astrazeneca Exhibit 2013 (PTAB Nov. 5, 2015)
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E30 SEM. O.C. Disclosed Is a Compound Represented by the Formula (1) (51) Int
USOO9453000B2 (12) United States Patent (10) Patent No.: US 9.453,000 B2 Kimura et al. (45) Date of Patent: *Sep. 27, 2016 (54) POLYCYCLIC COMPOUND (56) References Cited (75) Inventors: Teiji Kimura, Tsukuba (JP); Noritaka U.S. PATENT DOCUMENTS Kitazawa, Tsukuba (JP); Toshihiko 3,470,167 A 9, 1969 Sarkar Kaneko, Tsukuba (JP); Nobuaki Sato, 3,989,816 A 1 1/1976 Rajadhyaksha Tsukuba (JP); Koki Kawano, Tsukuba 4,910,200 A 3, 1990 Curtze et al. (JP): Koichi Ito, Tsukuba (JP); 5,281,626 A 1/1994 Oinuma et al. M s Tak ishi Tsukub JP 5,563,162 A 10, 1996 Oku et al. amoru Takaishi Tsukuba (JP); 5,804,577 A 9, 1998 Hebeisen et al. Takeo Sasaki, Tsukuba (JP); Yu 5,985,856 A 11/1999 Stella et al. Yoshida, Tsukuba (JP); Toshiyuki 6,235,728 B1 5, 2001 Golik et al. Uemura, Tsukuba (JP); Takashi Doko, g R 1939. E. al. Its SE E. Shinmyo, 7,138.414 B2 11/2006 Schoenafingereatch et al. et al. sukuba (JP); Daiju Hasegawa, 7,300,936 B2 11/2007 Parker et al. Tsukuba (JP); Takehiko Miyagawa, 7,314,940 B2 1/2008 Graczyk et al. Hatfield (GB); Hiroaki Hagiwara, 7,618,960 B2 11/2009 Kimura et al. Tsukuba (JP) 7,667,041 B2 2/2010 Kimura et al. 7,687,640 B2 3/2010 Kimura et al. 7,713,993 B2 5/2010 Kimura et al. (73) Assignee: EISAI R&D MANAGEMENT CO., 7,737,141 B2 6/2010 Kimura et al. LTD., Tokyo (JP) 7,880,009 B2 2/2011 Kimura et al. -
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 -
WO 2011/089216 Al
(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 t 28 July 2011 (28.07.2011) WO 2011/089216 Al (51) International Patent Classification: (81) Designated States (unless otherwise indicated, for every A61K 47/48 (2006.01) C07K 1/13 (2006.01) kind of national protection available): AE, AG, AL, AM, C07K 1/1 07 (2006.01) AO, AT, AU, AZ, BA, BB, BG, BH, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, (21) Number: International Application DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, PCT/EP201 1/050821 HN, HR, HU, ID, J , IN, IS, JP, KE, KG, KM, KN, KP, (22) International Filing Date: KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, 2 1 January 201 1 (21 .01 .201 1) ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PE, PG, PH, PL, PT, RO, RS, RU, SC, SD, (25) Filing Language: English SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, (26) Publication Language: English TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (30) Priority Data: (84) Designated States (unless otherwise indicated, for every 1015 1465. 1 22 January 2010 (22.01 .2010) EP kind of regional protection available): ARIPO (BW, GH, GM, KE, LR, LS, MW, MZ, NA, SD, SL, SZ, TZ, UG, (71) Applicant (for all designated States except US): AS- ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, MD, RU, TJ, CENDIS PHARMA AS [DK/DK]; Tuborg Boulevard TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, 12, DK-2900 Hellerup (DK). -
I Regulations
23.2.2007 EN Official Journal of the European Union L 56/1 I (Acts adopted under the EC Treaty/Euratom Treaty whose publication is obligatory) REGULATIONS COUNCIL REGULATION (EC) No 129/2007 of 12 February 2007 providing for duty-free treatment for specified pharmaceutical active ingredients bearing an ‘international non-proprietary name’ (INN) from the World Health Organisation and specified products used for the manufacture of finished pharmaceuticals and amending Annex I to Regulation (EEC) No 2658/87 THE COUNCIL OF THE EUROPEAN UNION, (4) In the course of three such reviews it was concluded that a certain number of additional INNs and intermediates used for production and manufacture of finished pharmaceu- ticals should be granted duty-free treatment, that certain of Having regard to the Treaty establishing the European Commu- these intermediates should be transferred to the list of INNs, nity, and in particular Article 133 thereof, and that the list of specified prefixes and suffixes for salts, esters or hydrates of INNs should be expanded. Having regard to the proposal from the Commission, (5) Council Regulation (EEC) No 2658/87 of 23 July 1987 on the tariff and statistical nomenclature and on the Common Customs Tariff (1) established the Combined Nomenclature Whereas: (CN) and set out the conventional duty rates of the Common Customs Tariff. (1) In the course of the Uruguay Round negotiations, the Community and a number of countries agreed that duty- (6) Regulation (EEC) No 2658/87 should therefore be amended free treatment should be granted to pharmaceutical accordingly, products falling within the Harmonised System (HS) Chapter 30 and HS headings 2936, 2937, 2939 and 2941 as well as to designated pharmaceutical active HAS ADOPTED THIS REGULATION: ingredients bearing an ‘international non-proprietary name’ (INN) from the World Health Organisation, specified salts, esters or hydrates of such INNs, and designated inter- Article 1 mediates used for the production and manufacture of finished products. -
Recent Advances on the Progressive Mechanism and Therapy in Castration-Resistant Prostate Cancer
Journal name: OncoTargets and Therapy Article Designation: Review Year: 2018 Volume: 11 OncoTargets and Therapy Dovepress Running head verso: Wang et al Running head recto: Novel research advancement on mechanism and therapy in CRPC open access to scientific and medical research DOI: 159777 Open Access Full Text Article REVIEW Recent advances on the progressive mechanism and therapy in castration-resistant prostate cancer Keshan Wang1 Background: Although there have been great advances in mechanisms and therapeutic methods Hailong Ruan1 of prostate cancer, the mortality rate of prostate cancer remains high. The castration-resistant Tianbo Xu1 prostate cancer (CRPC), which develops from hormone-sensitive prostate cancer, foreshadows a Lei Liu1 more dismal outcome. Concomitant with the researches in the mechanism of CRPC and therapy Di Liu1 for CRPC, more and more landmark progress has been made in recent years. Hongmei Yang2 Methods: A number of clinical and experimental studies were reviewed to indicate the novel advancement in the progressive mechanism and therapy of CRPC. Xiaoping Zhang1 Results: The androgen receptor (AR) is still a vital driver in the progression of CRPC, while other Ke Chen1 multiple mechanisms also contribute to this progression, such as tumor immunity, cancer stem 1Department of Urology, Union cells, epithelial–mesenchymal transition and DNA repair disorder. In terms of the therapeutic Hospital, Tongji Medical College, Huazhong University of Science and methods of CRPC, chemotherapy with drugs, such as docetaxel, has been the first-line therapy Technology, Wuhan 430022, China; for CRPC for many years. Besides, newer agents, which target some of the above mechanisms, For personal use only. -
GABA Receptor Gamma-Aminobutyric Acid Receptor; Γ-Aminobutyric Acid Receptor
GABA Receptor Gamma-aminobutyric acid Receptor; γ-Aminobutyric acid Receptor GABA receptors are a class of receptors that respond to the neurotransmitter gamma-aminobutyric acid (GABA), the chief inhibitory neurotransmitter in the vertebrate central nervous system. There are two classes of GABA receptors: GABAA and GABAB. GABAA receptors are ligand-gated ion channels (also known as ionotropic receptors), whereas GABAB receptors are G protein-coupled receptors (also known asmetabotropic receptors). It has long been recognized that the fast response of neurons to GABA that is blocked by bicuculline and picrotoxin is due to direct activation of an anion channel. This channel was subsequently termed the GABAA receptor. Fast-responding GABA receptors are members of family of Cys-loop ligand-gated ion channels. A slow response to GABA is mediated by GABAB receptors, originally defined on the basis of pharmacological properties. www.MedChemExpress.com 1 GABA Receptor Agonists, Antagonists, Inhibitors, Activators & Modulators (+)-Bicuculline (+)-Kavain (d-Bicuculline) Cat. No.: HY-N0219 Cat. No.: HY-B1671 (+)-Bicuculline is a light-sensitive competitive (+)-Kavain, a main kavalactone extracted from Piper antagonist of GABA-A receptor. methysticum, has anticonvulsive properties, attenuating vascular smooth muscle contraction through interactions with voltage-dependent Na+ and Ca2+ channels. Purity: 99.97% Purity: 99.98% Clinical Data: No Development Reported Clinical Data: Launched Size: 10 mM × 1 mL, 50 mg, 100 mg Size: 10 mM × 1 mL, 5 mg, 10 mg (-)-Bicuculline methobromide (-)-Bicuculline methochloride (l-Bicuculline methobromide) Cat. No.: HY-100783 (l-Bicuculline methochloride) Cat. No.: HY-100783A (-)-Bicuculline methobromide (l-Bicuculline (-)-Bicuculline methochloride (l-Bicuculline methobromide) is a potent GABAA receptor methochloride) is a potent GABAA receptor antagonist. -
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. -
A Abacavir Abacavirum Abakaviiri Abagovomab Abagovomabum
A abacavir abacavirum abakaviiri abagovomab abagovomabum abagovomabi abamectin abamectinum abamektiini abametapir abametapirum abametapiiri abanoquil abanoquilum abanokiili abaperidone abaperidonum abaperidoni abarelix abarelixum abareliksi abatacept abataceptum abatasepti abciximab abciximabum absiksimabi abecarnil abecarnilum abekarniili abediterol abediterolum abediteroli abetimus abetimusum abetimuusi abexinostat abexinostatum abeksinostaatti abicipar pegol abiciparum pegolum abisipaaripegoli abiraterone abirateronum abirateroni abitesartan abitesartanum abitesartaani ablukast ablukastum ablukasti abrilumab abrilumabum abrilumabi abrineurin abrineurinum abrineuriini abunidazol abunidazolum abunidatsoli acadesine acadesinum akadesiini acamprosate acamprosatum akamprosaatti acarbose acarbosum akarboosi acebrochol acebrocholum asebrokoli aceburic acid acidum aceburicum asebuurihappo acebutolol acebutololum asebutololi acecainide acecainidum asekainidi acecarbromal acecarbromalum asekarbromaali aceclidine aceclidinum aseklidiini aceclofenac aceclofenacum aseklofenaakki acedapsone acedapsonum asedapsoni acediasulfone sodium acediasulfonum natricum asediasulfoninatrium acefluranol acefluranolum asefluranoli acefurtiamine acefurtiaminum asefurtiamiini acefylline clofibrol acefyllinum clofibrolum asefylliiniklofibroli acefylline piperazine acefyllinum piperazinum asefylliinipiperatsiini aceglatone aceglatonum aseglatoni aceglutamide aceglutamidum aseglutamidi acemannan acemannanum asemannaani acemetacin acemetacinum asemetasiini aceneuramic -
Androgen/Androgen Receptor Signaling in Ovarian Cancer: Molecular Regulation and Therapeutic Potentials
International Journal of Molecular Sciences Review Androgen/Androgen Receptor Signaling in Ovarian Cancer: Molecular Regulation and Therapeutic Potentials Wei-Min Chung 1,2,†, Lumin Chen 1,†, Wei-Chun Chang 2, Sheng-Yuan Su 1, Yao-Ching Hung 2,3,* and Wen-Lung Ma 2,4,5,* 1 Department of Obstetrics and Gynecology, China Medical University Hsinchu Hospital, Hsinchu 30272, Taiwan; [email protected] (W.-M.C.); [email protected] (L.C.); [email protected] (S.-Y.S.) 2 Sex Hormone Research Center, Department of Obstetrics and Gynecology, China Medical University Hospital, Taichung 40403, Taiwan; [email protected] 3 Department of Obstetrics and Gynecology, Asia University Hospital, Taichung 41354, Taiwan 4 Graduate Institute of Biomedical Sciences, School of Medicine, China Medical University, Taichung 40403, Taiwan 5 Department of Nursing, Asia University, Taichung 41354, Taiwan * Correspondence: [email protected] (Y.-C.H.); [email protected] (W.-L.M.); Tel.: +886-975681032 (Y.-C.H. & W.-L.M.) † These authors contributed equally as first author. Abstract: Ovarian cancer (OVCA) arises from three cellular origins, namely surface epithelial cells, germ cells, and stromal cells. More than 85% of OVCAs are EOCs (epithelial ovarian carcinomas), which are the most lethal gynecological malignancies. Cancer stem/progenitor cells (CSPCs) are considered to be cancer promoters due to their capacity for unlimited self-renewal and drug resistance. Androgen receptor (AR) belongs to the nuclear receptor superfamily and can be activated through Citation: Chung, W.-M.; Chen, L.; Chang, W.-C.; Su, S.-Y.; Hung, Y.-C.; binding to its ligand androgens. Studies have reported an association between AR expression and Ma, W.-L. -
Oxidative Stress and Redox Signaling in CRPC Progression: Therapeutic Potential of Clinically- Tested Nrf2-Activators
Mondal et al. Cancer Drug Resist 2021;4:96-124 Cancer DOI: 10.20517/cdr.2020.71 Drug Resistance Review Open Access Oxidative stress and redox signaling in CRPC progression: therapeutic potential of clinically- tested Nrf2-activators Debasis Mondal, Devin Narwani, Shahnawaz Notta, Dawood Ghaffar, Nikhil Mardhekar, Syed S. A. Quadri Debusk College of Osteopathic Medicine, Lincoln Memorial University, Knoxville, TN 37932, USA. Correspondence to: Dr. Debasis Mondal, Associate Professor of Microbiology, Debusk College of Osteopathic Medicine, Lincoln Memorial University, 9737 Cogdill Road, Rm. #238, Knoxville, TN 37932, USA. E-mail: [email protected] How to cite this article: Mondal D, Narwani D, Notta S, Ghaffar D, Mardhekar N, Quadri SSA. Oxidative stress and redox signaling in CRPC progression: therapeutic potential of clinically-tested Nrf2-activators. Cancer Drug Resist 2021;4:96-124. http://dx.doi.org/10.20517/cdr.2020.71 Received: 31 Aug 2020 First Decision: 23 Oct 2020 Revised: 6 Nov 2020 Accepted: 11 Nov 2020 Available online: 19 Mar 2021 Academic Editor: Godefridus J. Peters Copy Editor: Cai-Hong Wang Production Editor: Jing Yu Abstract Androgen deprivation therapy (ADT) is the mainstay regimen in patients with androgen-dependent prostate cancer (PCa). However, the selection of androgen-independent cancer cells leads to castrate resistant prostate cancer (CRPC). The aggressive phenotype of CRPC cells underscores the need to elucidate mechanisms and therapeutic strategies to suppress CRPC outgrowth. Despite ADT, the activation of androgen receptor (AR) transcription factor continues via crosstalk with parallel signaling pathways. Understanding of how these signaling cascades are initiated and amplified post-ADT is lacking. -
MEMBRANE ANDROGEN RECEPTOR-INDUCED OXIDATIVE STRESS: MECHANISM INVOLVED in NEURODEGENERATION DISSERTATION Presented to the Gradu
MEMBRANE ANDROGEN RECEPTOR-INDUCED OXIDATIVE STRESS: MECHANISM INVOLVED IN NEURODEGENERATION DISSERTATION Presented to the Graduate Council of the Graduate School of Biomedical Sciences University of North Texas Health Science Center at Fort Worth in Partial Fulfillment of the Requirements For the Degree of DOCTOR OF PHILOSOPHY By Mavis A. A. Tenkorang, B (Pharm) Fort Worth, Texas April 2019 i Copyright by Mavis A. A. Tenkorang 2019 ii MEMBRANE ANDROGEN RECEPTOR-INDUCED OXIDATIVE STRESS: MECHANISM INVOLVED IN NEURODEGENERATION Mavis A.A. Tenkorang APPROVED: ……………………………………………………………………………………………………… Major Professor, Rebecca L. Cunningham, Ph.D ……………………………………………………………………………………………………… Committee Member, Sid O’Bryant, Ph.D ……………………………………………………………………………………………………… Committee Member, Derek Schreihofer, Ph.D ……………………………………………………………………………………………………… Committee Member, Robert Barber, Ph.D ……………………………………………………………………………………………………… University Member, YiQiang (Eric) Cheng, Ph.D ……………………………………………………………………………………………………… Chair, Department of Pharmacology & Neuroscience, Michael Forster, Ph.D ……………………………………………………………………………………………………… Dean, J. Michael Mathis, Ph.D, EdD), Graduate School of Biomedical Sciences iii ABSTRACT Oxidative stress-associated neurodegenerative diseases, such as Parkinson’s disease (PD), affect millions of people worldwide. Although aging is the greatest risk factor for PD, other significant factors may be implicated, such as sex hormones that can mediate sex differences. Men have a higher incidence and prevalence of PD than women. Therefore, testosterone, a primary male sex hormone and a known oxidative stressor, is implicated in PD pathophysiology. Since androgens can have negative effects on dopaminergic cells, it is imperative to understand the underlying mechanisms in order to determine what mediates the observed sex differences in PD prevalence. NADPH Oxidase 1 and 2 are major oxidative stress generators in the brain, thus potential targets for testosterone-induced oxidative stress and cell death. -
― D03 - 1 ― 医学中央雑誌刊行会・医学用語シソーラス 第9版（ 2019） カテゴリー別リスト
医学中央雑誌刊行会・医学用語シソーラス 第9版（ 2019） カテゴリー別リスト 複素環式化合物 D03+ Alkaloids D03-10+ Aconitine D03-10-10 # Acridones D03-10-20+ # Acronine D03-10-20-10 # Amaryllidaceae Alkaloids D03-10-30+ Galantamine D03-10-30-10 # Anabasine D03-10-40 # Arecoline D03-10-50 # Benzophenanthridines D03-10-60 # Benzylisoquinolines D03-10-70+ # Aporphines D03-10-70-10+ # Apomorphine D03-10-70-10-10 # Berberine Alkaloids D03-10-70-20+ # Berberine D03-10-70-20-10 # Bicuculline D03-10-70-30 # * Cepharanthine D03-10-70-40 # Papaverine D03-10-70-50+ # Drotaverin D03-10-70-50-10 # Ethaverine D03-10-70-50-20 # Tetrahydropapaveroline D03-10-70-50-30 # Toxiferine D03-10-70-60+ # Alcuronium D03-10-70-60-10 # Tubocurarine D03-10-70-70+ # Dimethyltubocurarinium Chloride D03-10-70-70-10 # Betalains D03-10-80+ # Betacyanins D03-10-80-10 # Betaxanthins D03-10-80-20 # Camptothecin D03-10-90+ # Belotecan D03-10-90-10 # Diflomotecan D03-10-90-20 # Exatecan D03-10-90-30 # Irinotecan D03-10-90-40 # Rubitecan D03-10-90-50 # Topotecan D03-10-90-60+ # Delimotecan D03-10-90-60-10 # Cinchona Alkaloids D03-10-100+ Quinidine D03-10-100-10 # Quinine D03-10-100-20 # Colchicine D03-10-110+ # Demecolcine D03-10-110-10 # Lumicolchicines D03-10-110-20 1-Deoxynojirimycin D03-10-120+ # Emiglitate D03-10-120-10 # * Migalastat D03-10-120-20 # Miglitol D03-10-120-30 # Miglustat D03-10-120-40 # Dihydro-Beta-Erythroidine D03-10-130 # Emetine D03-10-140+ # Dehydroemetine D03-10-140-10 # Ergot Alkaloids D03-10-150+ Ergolines D03-10-150-10+ # Cabergoline D03-10-150-10-10 # Ergonovine D03-10-150-10-20+ # Methylergometrine