Fagin-Event-Laurahaas.Pdf
Total Page:16
File Type:pdf, Size:1020Kb
Load more
Recommended publications
-
Chemical Ligand Space of Cereblon Iuliia Boichenko,† Kerstin Bar,̈ Silvia Deiss, Christopher Heim, Reinhard Albrecht, Andrei N
This is an open access article published under a Creative Commons Attribution (CC-BY) License, which permits unrestricted use, distribution and reproduction in any medium, provided the author and source are cited. Article Cite This: ACS Omega 2018, 3, 11163−11171 http://pubs.acs.org/journal/acsodf Chemical Ligand Space of Cereblon Iuliia Boichenko,† Kerstin Bar,̈ Silvia Deiss, Christopher Heim, Reinhard Albrecht, Andrei N. Lupas, Birte Hernandez Alvarez,* and Marcus D. Hartmann* Department of Protein Evolution, Max Planck Institute for Developmental Biology, Max-Planck-Ring 5, 72076 Tübingen, Germany *S Supporting Information ABSTRACT: The protein cereblon serves as a substrate receptor of a ubiquitin ligase complex that can be tuned toward different target proteins by cereblon-binding agents. This approach to targeted protein degradation is exploited in different clinical settings and has sparked the development of a growing number of thalidomide derivatives. Here, we probe the chemical space of cereblon binding beyond such derivatives and work out a simple set of chemical requirements, delineating the metaclass of cereblon effectors. We report co-crystal structures for a diverse set of compounds, including commonly used pharmaceuticals, but also find that already minimalistic cereblon-binding moieties might exert teratogenic effects in zebrafish. Our results may guide the design of a post-thalidomide generation of therapeutic cereblon effectors and provide a framework for the circumvention of unintended cereblon binding by negative design -
Ep 1553091 A1
Europäisches Patentamt *EP001553091A1* (19) European Patent Office Office européen des brevets (11) EP 1 553 091 A1 (12) EUROPEAN PATENT APPLICATION published in accordance with Art. 158(3) EPC (43) Date of publication: (51) Int Cl.7: C07D 263/32, C07D 417/14, 13.07.2005 Bulletin 2005/28 C07D 333/20, C07D 413/12, C07D 417/06 (21) Application number: 04726765.3 (86) International application number: (22) Date of filing: 09.04.2004 PCT/JP2004/005119 (87) International publication number: WO 2004/089918 (21.10.2004 Gazette 2004/43) (84) Designated Contracting States: • SAKAMOTO, Johei AT BE BG CH CY CZ DE DK EE ES FI FR GB GR Takatsuki-shi, Osaka 569-1125 (JP) HU IE IT LI LU MC NL PL PT RO SE SI SK TR • NAKANISHI, Hiroyuki Designated Extension States: Takatsuki-shi, Osaka 569-1125 (JP) AL HR LT LV MK • NAKAGAWA, Yuichi Takatsuki-shi, Osaka 569-1125 (JP) (30) Priority: 09.04.2003 JP 2003105267 • OHTA, Takeshi 03.06.2003 JP 2003157590 Takatsuki-shi, Osaka 569-1125 (JP) • SAKATA, Shohei (71) Applicant: Japan Tobacco Inc. Takatsuki-shi, Osaka 569-1125 (JP) Tokyo 105-8422 (JP) • MORINAGA, Hisayo Takatsuki-shi, Osaka 569-1125 (JP) (72) Inventors: • IKEMOTO, Tomoyuki (74) Representative: Takatsuki-shi, Osaka 569-1125 (JP) von Kreisler, Alek, Dipl.-Chem. et al • TANAKA, Masahiro Deichmannhaus am Dom, Takatsuki-shi, Osaka 569-1125 (JP) Postfach 10 22 41 • YUNO, Takeo 50462 Köln (DE) Takatsuki-shi, Osaka 569-1125 (JP) (54) HETEROAROMATIC PENTACYCLIC COMPOUND AND MEDICINAL USE THEREOF (57) A 5-membered heteroaromatic ring compound represented by the formula [I] 1 2 4 5 7 wherein V is CH or N; W is S or O; R and R are each H etc.; X is -N(R )-, -O-, -S-, -SO2-N(R )-, -CO-N(R )- etc.; L is EP 1 553 091 A1 Printed by Jouve, 75001 PARIS (FR) (Cont. -
GPCR/G Protein
Inhibitors, Agonists, Screening Libraries www.MedChemExpress.com GPCR/G Protein G Protein Coupled Receptors (GPCRs) perceive many extracellular signals and transduce them to heterotrimeric G proteins, which further transduce these signals intracellular to appropriate downstream effectors and thereby play an important role in various signaling pathways. G proteins are specialized proteins with the ability to bind the nucleotides guanosine triphosphate (GTP) and guanosine diphosphate (GDP). In unstimulated cells, the state of G alpha is defined by its interaction with GDP, G beta-gamma, and a GPCR. Upon receptor stimulation by a ligand, G alpha dissociates from the receptor and G beta-gamma, and GTP is exchanged for the bound GDP, which leads to G alpha activation. G alpha then goes on to activate other molecules in the cell. These effects include activating the MAPK and PI3K pathways, as well as inhibition of the Na+/H+ exchanger in the plasma membrane, and the lowering of intracellular Ca2+ levels. Most human GPCRs can be grouped into five main families named; Glutamate, Rhodopsin, Adhesion, Frizzled/Taste2, and Secretin, forming the GRAFS classification system. A series of studies showed that aberrant GPCR Signaling including those for GPCR-PCa, PSGR2, CaSR, GPR30, and GPR39 are associated with tumorigenesis or metastasis, thus interfering with these receptors and their downstream targets might provide an opportunity for the development of new strategies for cancer diagnosis, prevention and treatment. At present, modulators of GPCRs form a key area for the pharmaceutical industry, representing approximately 27% of all FDA-approved drugs. References: [1] Moreira IS. Biochim Biophys Acta. 2014 Jan;1840(1):16-33. -
Federal Register / Vol. 60, No. 80 / Wednesday, April 26, 1995 / Notices DIX to the HTSUS—Continued
20558 Federal Register / Vol. 60, No. 80 / Wednesday, April 26, 1995 / Notices DEPARMENT OF THE TREASURY Services, U.S. Customs Service, 1301 TABLE 1.ÐPHARMACEUTICAL APPEN- Constitution Avenue NW, Washington, DIX TO THE HTSUSÐContinued Customs Service D.C. 20229 at (202) 927±1060. CAS No. Pharmaceutical [T.D. 95±33] Dated: April 14, 1995. 52±78±8 ..................... NORETHANDROLONE. A. W. Tennant, 52±86±8 ..................... HALOPERIDOL. Pharmaceutical Tables 1 and 3 of the Director, Office of Laboratories and Scientific 52±88±0 ..................... ATROPINE METHONITRATE. HTSUS 52±90±4 ..................... CYSTEINE. Services. 53±03±2 ..................... PREDNISONE. 53±06±5 ..................... CORTISONE. AGENCY: Customs Service, Department TABLE 1.ÐPHARMACEUTICAL 53±10±1 ..................... HYDROXYDIONE SODIUM SUCCI- of the Treasury. NATE. APPENDIX TO THE HTSUS 53±16±7 ..................... ESTRONE. ACTION: Listing of the products found in 53±18±9 ..................... BIETASERPINE. Table 1 and Table 3 of the CAS No. Pharmaceutical 53±19±0 ..................... MITOTANE. 53±31±6 ..................... MEDIBAZINE. Pharmaceutical Appendix to the N/A ............................. ACTAGARDIN. 53±33±8 ..................... PARAMETHASONE. Harmonized Tariff Schedule of the N/A ............................. ARDACIN. 53±34±9 ..................... FLUPREDNISOLONE. N/A ............................. BICIROMAB. 53±39±4 ..................... OXANDROLONE. United States of America in Chemical N/A ............................. CELUCLORAL. 53±43±0 -
(12) United States Patent (10) Patent No.: US 8,158,152 B2 Palepu (45) Date of Patent: Apr
US008158152B2 (12) United States Patent (10) Patent No.: US 8,158,152 B2 Palepu (45) Date of Patent: Apr. 17, 2012 (54) LYOPHILIZATION PROCESS AND 6,884,422 B1 4/2005 Liu et al. PRODUCTS OBTANED THEREBY 6,900, 184 B2 5/2005 Cohen et al. 2002fOO 10357 A1 1/2002 Stogniew etal. 2002/009 1270 A1 7, 2002 Wu et al. (75) Inventor: Nageswara R. Palepu. Mill Creek, WA 2002/0143038 A1 10/2002 Bandyopadhyay et al. (US) 2002fO155097 A1 10, 2002 Te 2003, OO68416 A1 4/2003 Burgess et al. 2003/0077321 A1 4/2003 Kiel et al. (73) Assignee: SciDose LLC, Amherst, MA (US) 2003, OO82236 A1 5/2003 Mathiowitz et al. 2003/0096378 A1 5/2003 Qiu et al. (*) Notice: Subject to any disclaimer, the term of this 2003/OO96797 A1 5/2003 Stogniew et al. patent is extended or adjusted under 35 2003.01.1331.6 A1 6/2003 Kaisheva et al. U.S.C. 154(b) by 1560 days. 2003. O191157 A1 10, 2003 Doen 2003/0202978 A1 10, 2003 Maa et al. 2003/0211042 A1 11/2003 Evans (21) Appl. No.: 11/282,507 2003/0229027 A1 12/2003 Eissens et al. 2004.0005351 A1 1/2004 Kwon (22) Filed: Nov. 18, 2005 2004/0042971 A1 3/2004 Truong-Le et al. 2004/0042972 A1 3/2004 Truong-Le et al. (65) Prior Publication Data 2004.0043042 A1 3/2004 Johnson et al. 2004/OO57927 A1 3/2004 Warne et al. US 2007/O116729 A1 May 24, 2007 2004, OO63792 A1 4/2004 Khera et al. -
WHO Drug Information Vol. 03, No. 4, 1989
WHO DRUG INFORMATION VOLUME 3 • NUMBER 4 • 1989 PROPOSED INN LIST 62 INTERNATIONAL NONPROPRIETARY NAMES FOR PHARMACEUTICAL SUBSTANCES WORLD HEALTH ORGANIZATION • GENEVA WHO Drug Information WHO Drug Information provides an cerned with the rational use of overview of topics relating to drug drugs. In effect, the journal seeks development and regulation that to relate regulatory activity to are of current relevance and im therapeutic practice. It also aims to portance, and will include the lists provide an open forum for debate. of proposed and recommended In Invited contributions will portray a ternational Nonproprietary Names variety of viewpoints on matters of for Pharmaceutical Substances general policy with the aim of (INN). Its contents reflect, but do stimulating discussion not only not present, WHO policies and ac in these columns but wherever tivities and they embrace socio relevant decisions on this subject economic as well as technical mat have to be taken. ters. WHO Drug Information is pub The objective is to bring issues that lished 4 times a year in English and are of primary concern to drug French. regulators and pharmaceutical manufacturers to the attention of a Annual subscription: Sw.fr. 50.— wide audience of health profes Airmail rate: Sw.fr. 60.— sionals and policy-makers con Price per copy: Sw.fr. 15.— © World Health Organization 1989 Authors alone are responsible for views expressed Publications of the World Health Organization in signed contributions. enjoy copyright protection in accordance with the provisions of Protocol 2 of the Universal The mention of specific companies or of certain Copyright Convention. For rights of reproduc manufacturers' products does not imply that they are tion or translation, in part or In toto, applica endorsed or recommended by the World Health tion should be made to: Chief, Office of Organization in preference to others of a similar na Publications, World Health Organization, ture which are not mentioned. -
(12) Patent Application Publication (10) Pub. No.: US 2009/0053329 A1 Peters Et Al
US 2009.0053329A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2009/0053329 A1 Peters et al. (43) Pub. Date: Feb. 26, 2009 (54) COMBINATIONS OF 5-HT2A INVERSE 61/012,771, filed on Dec. 10, 2007, provisional appli AGONSTS AND ANTAGONSTS WITH cation No. 61/026,092, filed on Feb. 4, 2008. ANTIPSYCHOTICS Publication Classification (75) Inventors: Perry Peters, San Diego, CA (US); (51) Int. Cl. David Furlano, San Diego, CA A633/00 (2006.01) (US); Daun Bahr, San Diego, CA A6II 3/445 (2006.01) (US); Daniel Van Kammen, San A 6LX 3/59 (2006.01) Diego, CA (US); Mark Brann, A6II 3/438 (2006.01) Rye, NH (US) A6IP 25/18 (2006.01) Correspondence Address: A 6LX 3L/2197 (2006.01) KNOBBE MARTENS OLSON & BEAR LLP A6II 3/54 (2006.01) 2040 MAINSTREET, FOURTEENTH FLOOR A6II 3/55 (2006.01) IRVINE, CA 92.614 (US) (52) U.S. Cl. .................... 424/722:514/329; 514/259.41: 514/278; 514/254.06; 514/222.2: 514/212.01 (73) Assignee: Acadia Pharmaceuticals, Inc., San Diego, CA (US) (57) ABSTRACT Combinations of 5-HT2A inverse agonists or antagonists (21) Appl. No.: 12/051,807 Such as pimavanserin with antipsychotics Such as risperidone are shown to induce a rapid onset of antipsychotic action and (22) Filed: Mar. 19, 2008 increase the number of responders when compared to therapy with the antipsychotic alone. These effects can be achieved at Related U.S. Application Data a low dose of the antipsychotic, thereby reducing the inci (60) Provisional application No. -
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. -
Combinations of 5-Ht2a Inverse Agonists And
(19) TZZ _¥¥¥Z_T (11) EP 2 134 330 B1 (12) EUROPEAN PATENT SPECIFICATION (45) Date of publication and mention (51) Int Cl.: of the grant of the patent: A61K 31/00 (2006.01) 08.05.2013 Bulletin 2013/19 (86) International application number: (21) Application number: 08744091.3 PCT/US2008/057557 (22) Date of filing: 19.03.2008 (87) International publication number: WO 2008/116024 (25.09.2008 Gazette 2008/39) (54) COMBINATIONS OF 5-HT2A INVERSE AGONISTS AND ANTAGONISTS WITH ANTIPSYCHOTICS KOMBINATIONEN AUS 5-HT2A-INVERSAGONISTEN UND -ANTAGONISTEN MIT ANTIPSYCHOTIKA COMBINAISONS D’AGONISTES INVERSES OU ANTAGONISTES DE 5-HT2A AVEC ANTIPSYCHOTIQUES (84) Designated Contracting States: (74) Representative: Weber, Martin AT BE BG CH CY CZ DE DK EE ES FI FR GB GR Jones Day HR HU IE IS IT LI LT LU LV MC MT NL NO PL PT Prinzregentenstraße 11 RO SE SI SK TR 80538 München (DE) Designated Extension States: AL BA MK RS (56) References cited: WO-A-2004/064738 WO-A-2007/133802 (30) Priority: 19.03.2007 US 895735 P US-A1- 2006 204 486 29.03.2007 US 908921 P 10.12.2007 US 12771 • "ACP-103" DRUGS OF THE FUTURE, PROUS 04.02.2008 US 26092 SCIENCE, ES, vol. 31, no. 11, 1 January 2006 (2006-01-01), pages 939-943, XP002446571 ISSN: (43) Date of publication of application: 0377-8282 23.12.2009 Bulletin 2009/52 • GRAHNEN A E ET AL: "Reduction of haloperidol- induced side effects by ACP-103 in healthy (73) Proprietor: Acadia Pharmaceuticals Inc. volunteers" CLINICAL PHARMACOLOGY & San Diego, CA 92121-1402 (US) THERAPEUTICS, MOSBY-YEAR BOOK, ST LOUIS, MO, US, vol. -
Harmonized Tariff Schedule of the United States (2004) -- Supplement 1 Annotated for Statistical Reporting Purposes
Harmonized Tariff Schedule of the United States (2004) -- Supplement 1 Annotated for Statistical Reporting Purposes PHARMACEUTICAL APPENDIX TO THE HARMONIZED TARIFF SCHEDULE Harmonized Tariff Schedule of the United States (2004) -- Supplement 1 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. Product CAS No. Product CAS No. ABACAVIR 136470-78-5 ACEXAMIC ACID 57-08-9 ABAFUNGIN 129639-79-8 ACICLOVIR 59277-89-3 ABAMECTIN 65195-55-3 ACIFRAN 72420-38-3 ABANOQUIL 90402-40-7 ACIPIMOX 51037-30-0 ABARELIX 183552-38-7 ACITAZANOLAST 114607-46-4 ABCIXIMAB 143653-53-6 ACITEMATE 101197-99-3 ABECARNIL 111841-85-1 ACITRETIN 55079-83-9 ABIRATERONE 154229-19-3 ACIVICIN 42228-92-2 ABITESARTAN 137882-98-5 ACLANTATE 39633-62-0 ABLUKAST 96566-25-5 ACLARUBICIN 57576-44-0 ABUNIDAZOLE 91017-58-2 ACLATONIUM NAPADISILATE 55077-30-0 ACADESINE 2627-69-2 ACODAZOLE 79152-85-5 ACAMPROSATE 77337-76-9 ACONIAZIDE 13410-86-1 ACAPRAZINE 55485-20-6 ACOXATRINE 748-44-7 ACARBOSE 56180-94-0 ACREOZAST 123548-56-1 ACEBROCHOL 514-50-1 ACRIDOREX 47487-22-9 ACEBURIC ACID 26976-72-7 -
(19) United States (12) Reissued Patent (10) Patent Number: US RE41,998 E Campbell (45) Date of Reissued Patent: Dec
USOORE41998E (19) United States (12) Reissued Patent (10) Patent Number: US RE41,998 E Campbell (45) Date of Reissued Patent: Dec. 14, 2010 (54) COMPOSITIONS AND METHODS OF 6,534,048 B1 3/2003 Borgman TREATMENT OF SYMPATHETICALLY 6,559,186 B1 5/2003 Campbell MANTAINED PAN 2004/0101582 A1 5, 2004 Wolicki 2004/0132824 A1 7, 2004 Gil et al. (75) Inventor: James N. Campbell, Lutherville, MD FOREIGN PATENT DOCUMENTS (US) DE 2920500 11, 1980 (73) Assignee: Arclon Therapeutics, Inc., Baltimore, EP O 241 050 10, 1987 JP 1216928 8, 1989 MD (US) WO WO92,14453 9, 1992 WO WO 2007/O25613 3, 2007 (21) Appl. No.: 11/123,257 OTHER PUBLICATIONS (22) Filed: May 5, 2005 Indoramin: http://www.netdoctor.co.uk/medicines/ Related U.S. Patent Documents 100000841.html.online retrieved from the internet on Dec. Reissue of: 11, 2008; Jun. 11, 2007: 5 pages. * (64) Patent No.: 6,559, 186 Labetalol: http://www.answers.com/labetalol; online Issued: May 6, 2003 retrieved from the internet on Dec. 11, 2008: Jul. 1, 2002; 7 Appl. No.: 08/286.404 pages. Filed: Aug. 5, 1994 Phenoxybenzamine: http://www.nlm.nih.gov/medlineplus/ druginfo/meds/a882059.html; online retrieved from the U.S. Applications: internet on Dec. 11, 2008; Apr. 1, 2003: 3 pages.* (63) Continuation of application No. 07/747,635, filed on Aug. Medetomidine: http://www.answers.com/topic/medetomi 20, 1991, now abandoned, which is a continuation-in-part of dine-1; online retrieved from the internet on Dec. 11, application No. 07/661.554, filed on Feb. -
Chemical Structure-Related Drug-Like Criteria of Global Approved Drugs
Molecules 2016, 21, 75; doi:10.3390/molecules21010075 S1 of S110 Supplementary Materials: Chemical Structure-Related Drug-Like Criteria of Global Approved Drugs Fei Mao 1, Wei Ni 1, Xiang Xu 1, Hui Wang 1, Jing Wang 1, Min Ji 1 and Jian Li * Table S1. Common names, indications, CAS Registry Numbers and molecular formulas of 6891 approved drugs. Common Name Indication CAS Number Oral Molecular Formula Abacavir Antiviral 136470-78-5 Y C14H18N6O Abafungin Antifungal 129639-79-8 C21H22N4OS Abamectin Component B1a Anthelminithic 65195-55-3 C48H72O14 Abamectin Component B1b Anthelminithic 65195-56-4 C47H70O14 Abanoquil Adrenergic 90402-40-7 C22H25N3O4 Abaperidone Antipsychotic 183849-43-6 C25H25FN2O5 Abecarnil Anxiolytic 111841-85-1 Y C24H24N2O4 Abiraterone Antineoplastic 154229-19-3 Y C24H31NO Abitesartan Antihypertensive 137882-98-5 C26H31N5O3 Ablukast Bronchodilator 96566-25-5 C28H34O8 Abunidazole Antifungal 91017-58-2 C15H19N3O4 Acadesine Cardiotonic 2627-69-2 Y C9H14N4O5 Acamprosate Alcohol Deterrant 77337-76-9 Y C5H11NO4S Acaprazine Nootropic 55485-20-6 Y C15H21Cl2N3O Acarbose Antidiabetic 56180-94-0 Y C25H43NO18 Acebrochol Steroid 514-50-1 C29H48Br2O2 Acebutolol Antihypertensive 37517-30-9 Y C18H28N2O4 Acecainide Antiarrhythmic 32795-44-1 Y C15H23N3O2 Acecarbromal Sedative 77-66-7 Y C9H15BrN2O3 Aceclidine Cholinergic 827-61-2 C9H15NO2 Aceclofenac Antiinflammatory 89796-99-6 Y C16H13Cl2NO4 Acedapsone Antibiotic 77-46-3 C16H16N2O4S Acediasulfone Sodium Antibiotic 80-03-5 C14H14N2O4S Acedoben Nootropic 556-08-1 C9H9NO3 Acefluranol Steroid