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Progress in Medicinal Chemistry 16 This Page Intentionally Left Blank Progress in Medicinal Chemistry 16 Edited by G.P. ELLIS, D.SC., PH.D.,F.R.I.C. Department of Chemistry, University of Wales Institute of Science and Technology, King Edward VII Avenue, Card& CFl 3NU and G.B. WEST, B.PHARM., D.SC., PH.D., F.I.BIOL. Department of Paramedical Sciences, North East London Polytechnic, Romford Road, London El5 4LZ 1979 NORTH-HOLLAND PUBLISHING COMPANY AMSTERDAM.NEW YORK.OXFORD 0Elsevier/North-Holland Biomedical Press - 1979 AN rights reserved. No part of this publication may be reproduced, stored in a retrieval system. or transmitted in any form or by any means, electronic. mechanical, photocopying, recording or otherwise, without the prior permission of the copyright owner. ISBN for the series: 0 7204 7400 0 ISBN for this volume: 0 7204 0667 6 PUBLISHERS : Elsevier North-Holland Biomedical Press 335 Jan van Galenstraat, P.O. Box 21 1 Amsterdam, The Netherlands SOLE DISTRIBUTORS FOR THE U.S.A. AND CANADA: Elsevier/North-Holland Inc. 52 Vanderbilt Avenue New York, N.Y. 10017, U.S.A. LIBRARY OF CONGRESS CATALOGING IN PUBLICATION DATA Main entry under title: Progress in medicinal chemistry. London, Butterworths, 1961-1973 (Vols. 1-9). Amsterdam, North-Holland Publishing Co., 1974- (Vols. 10- ). Editors: 1961- G.P. Ellis and G.B. West. Includes bibliography. 1. Pharmacology-Collected works. 2. Chemistry, Medical and Pharmaceutical. I. Ellis, Gwynn Pennant, ed. 11. West, Geoffrey Buckle, 1961- ed. 111. Title: Medicinal chemistry. RS402.P78 615'.19 62-27 12 Photosetting by Thornson Press (India) Limited, New Delhi Printed in The Netherlands Preface We have pleasure in presenting five reviews in this volume. Recent trends towards international conformity in patent law are now beginning to show material benefits. The significance of these changes for medicinal chemists is outlined in Chapter 1. Steroids containing hetero atoms have been extensively studied in recent years and their synthesis and biological activity are described in Chapter 2, which is a longer review than is usual in this Series. The fight against neoplastic diseases continues to be waged on many fronts and one of these - with drugs which exhibit non-bonded interactions with nucleic acids - is surveyed in Chapter 3. The role of membranes in chemotherapy is well-established and Chapter 4 covers the inhibition by drugs of adenosine triphosphatase from microbial membranes. Finally, Chapter 5 assesses the progress made recently in our understanding of neuromuscular blockade at the cholinergic receptor. Much effort is required to prepare reviews of this type and we are indebted to our authors for their diligence and punctuality. Owners of copyright material have freely given their permission for it to be reproduced in this volume and we are grateful to them. As usual, the staff of our publishers have given us their full co-operation and it is a pleasure to acknowledge their contribution. November 1978 G.P. Ellis G.B. West This Page Intentionally Left Blank Contents Preface V 1. Recent Changes in Patent Law 1 F. Murphy, B.Sc., M.R.I.C., C.P.A., E.P.A. Fisons Ltd., Ipswich, Suffolk IPI IQH, England 2. Heterosteroids and Drug Research 35 H. Singh, M.Pharm., Ph.D., V.K. Kapoor, M.Pharm., Ph.D. and D. Paul, M.Pharm., Ph.D. Department of Pharmaceutical Sciences, Panjab University, Chandigarh 160014, India 3. The Molecular Basis for the Action of Some DNA-Binding Drugs 151 S. Neidle, B.Sc., Ph.D. Department of Biophysics, University of London King’s college, 26-29 Drury Lane, London WC2B 5RL, England 4. Inhibitors of Enzymes of Microbial Membranes; Agents Affecting MgZC-Activated Adenosine Triphosphatase 223 S.M. Hammond, B.Sc., Ph.D. Department of Biological Sciences, Purdue University, W.Lufayette, Indiana 47907, U.S.A. 5. Molecular Interactions at the Cholinergic Receptor in Neuro- muscular Blockade 257 J.B. Stenlake, D.Sc., Ph.D., C.Chem., F.P.S., F.R.I.C., F.R.S.E. Department of Pharmaceutical Chemistry, University of Strathclyde, Glasgow GI IXW, Scotland Index 287 vii This Page Intentionally Left Blank Contents of earlier volumes VOLUME 8 1 ORGANOPHOSPHORUS PESTICIDES : PHARMACOLOGY-Ian L. Natoff 2 THE MODE OF ACTION OF NOVOBIOCIN-A. Morris and A.D. Russell 3 SOME PYRIMIDINES OF BIOLOGICAL AND MEDICINAL INTEREST-Part 111-C. C. Cheng and Barbara Roth 4 ANTIVIRAL AGENTS-D.L. Swallow 5 ANTIFERTILITY AGENTS-V. Petrow 6 RECENT ADVANCES IN THE CHEMOTHERAPY OF MALARIA-R.M. Pinder 7 THE PROSTAGLANDINS-M.P.L. Caton VOLUME 9 1 NATURALLY-OCCURRING ANTITUMOUR AGENTS-K. Jewers, A.H. Machanda and Mrs. H.M. Rose 2 CHROMONE-2-AND-3-CARBOXYLICACIDS AND THEIR DERIVATIVES-G.P. Ellis and G. Barker 3 4-OXOPYRANOAZOLES AND 4-OXOPYRANOAZINES-Misbahul Ain Khan 4 ISOTOPE TECHNIQUES IN THE STUDY OF DRUG METABOLISM-Y. Kobayashi and D.V. Maudsley 5 THE PHARMACOTHERAPY OF PARKINSONISM-R.M. Pinder 6 ADRENOCHROME AND RELATED COMPOUNDS-R.A. Heacock and W.S. Powell VOLUME 10 1 MEDLARS COMPUTER INFORMATION RETRIEVAL-A.J. Hartley 2 THE USE OF ENZYMOLOGY IN PHARMACOLOGICAL AND TOXICOLOGICAL INVESTIGATIONS-W.G. Smith 3 THE METABOLISM AND BIOLOGICAL ACTIONS OF COUMARINS-G. Feuer 4 CARCINOGENICITY AND STRUCTURE IN POLYCYCLIC HYDRO- CARBONS-D.W. Jones and R.S. Matthews 5 LINEAR FREE ENERGY RELATIONSHIPS AND BIOLOGICAL ACTION-K.C. James 6 RECENT ADVANCES IN THE SYNTHESIS OF NITRILES-G.P. Ellis and I.L. Thomas '- VOLUME 11 1 STEREOCHEMICAL ASPECTS OF PARASYMPATHOMIMETICS AND THEIR ANTAGONISTS : RECENT DEVELOPMENTS-A.F. Casy 2 QUANTUM CHEMISTRY IN DRUG RESEARCH-W.G. Richards and M.E. Black 3 PSYCHOTOMIMETICS OF THE CONVOLVULACEAE-R.A. Heacock 4 ANTIHYPERLIPIDAEMIC AGENTS-E.C. Witte 5 THE MEDICINAL CHEMISTRY OF LITHIUM-E. Bailey, P.A. Bond, B.A. Brooks, M. Dimitrakoudi, F.D. Jenner, A. Judd, C.R. Lee, E.A. Lenton, S. McNeil, R.J. Pollitt, G.A. Sampson and E.A. Thompson ix VOLUME 12 I GAS-LIQUID CHROMATOGRAPHY-MASS SPECTROMETRY IN BIOCHEMIS- TRY, PHARMACOLOGY AND TOXICOLOGY-A.M. Lawson and G.H. Draffan 2 RECENT ADVANCES IN COLUMN CHROMATOGRAPHY-K.W. Williams and R.C. Smith 3 NMR SPECTROSCOPY IN BIOLOGICAL SCIENCES-P.J. Sadler 4 ELECTRON SPIN RESONANCE IN MEDICINAL CHEMISTRY-D.L. Williams-Smith and S.J. Wyard 5 POLAROGRAPHY IN BIOCHEMISTRY, PHARMACOLOGY AND TOXI- COLOGY-M. Brezina and J. Volke 6 METHODS RELATED TO CYCLIC AMP AND ADENYLATE CYCLASE-B.G. Benfey 7 RESISTANCE OF PSEUDOMONAS AERUCINOSA TO ANTIMICROBIAL DRUGS-R.B. Sykes and A. Morris 8 FUNCTIONAL MODIFICATIONS AND NUCLEAR ANALOGUES OF 8-LACTAM ANTIBIOTICS-Part I-J.Cs. Jaszberenyi and T.E. Gunda VOLUME 13 1 CLINICAL ENZYMOLOGY-David M. Goldberg 2 THE RELEASE OF PHARMACOLOGICALLY ACTIVE SUBSTANCES IN PARASITIC INFECTIONS-P.F.L. Boreham and I.G. Wright 3 THE MEDICINAL CHEMISTRY OF I,2,3-TRIAZINES-Malcolm F.G. Stevens 4 THE BIOLOGICAL USES AND IMPORTANCE OF GLUTARALDEHYDE-A.D. Russell and D. Hopwood 5 THE CHEMISTRY AND BIOCHEMISTRY OF C-NUCLEOSIDES-G. Doyle Daves, Jr. and C.C. Cheng VOLUME 14 1 ASPECTS OF THE PHARMACOLOGY OF PASSIVE ION TRANSFER ACROSS CELL MEMBRANES-A.W. Cuthbert 2 THE BIO-MEDICAL AND RELATED ROLES OF ION-SELECTIVE MEMBRANE ELECTRODES-G.J. Moody and J.D.R. Thomas 3 BIOLOGICAL ACTIVITY OF POLYENE ANTIBIOTICS-S.M. Hammond 4 FUNCTIONAL MODIFICATIONS AND NUCLEAR ANALOGUES OF 8-LACTAM ANTIBIOTICS-PART 11-E.T. Gunda and J.Cs. Jaszberenyi 5 THE ROLE OF BIOGENIC AGENTS IN THE ACTIONS OF CENTRALLY-ACTING ANALGESICS-R.D.E. Sewell and P.S.J. Spencer 6 FLAVONOIDS : SOME PHYSIOLOGICAL AND NUTRITIONAL CONSIDER- ATIONS-R.E. Hughes and H.K. Wilson VOLUME 15 1 THE USE OF STABLE ISOTOPES IN MEDICINAL CHEMISTRY-D. Halliday 2 MEMBRANE-ACTIVE ANTIMICROBIAL AGENTS-P.A. Lambert 3 ADRIAMYCIN AND RELATED ANTHRACYCLINE ANTIBIOTICS-J.R. Brown 4 THE HYPOPHYSIOTROPHIC HORMONES-J.C. Buckingham 5 COPPER COMPLEXES-A UNIQUE CLASS OF ANTI-ARTHRITIC DRUGS-R.J.R. Sorenson 6 NON-TRICYCLIC ANTIDEPRESSANTS-J. van Dijk, J. Hartog and F.C. Hillen 7 THE CHEMISTRY .AND BIOLOGICAL ACTIVITY OF a-(N)-HETEROCYCLIC CARBOXALDEHYDE THIOSEMICARBAZONES-K.C. Agarwal and A.C. Sartorelli 8 PROSTAGLANDINS AND THROMBOXANES-M.P.L. Caton and K. Crowshaw X Progress in Medicinal Chemistry - Vol. 16, edited by G.P. Ellis and G.B. West 0Elsevier/North-Holland Biomedical Press - 1979 1 Recent Changes in Patent Law F. MURPHY, B.Sc., M.R.I.C.,C.P.A., E.P.A. Fisons Ltd., Ipswich, Suflolk IPl lQH, England INTRODUCTION 1 THE PURPOSE OF THE PATENT SYSTEM 3 EXAMINATION OF PATENT APPLICATIONS 4 TERRITORIAL JURISDICTION 5 INTERNATIONAL CO-OPERATION ON PATENT LAW 5 UNITED KINGDOM PATENTS ACT 1977 7 Patentable inventions 7 Novelty and inventiveness 10 Procedure for filing 12 Examination 15 Revocation 16 Fees 17 Other important changes 18 PATENTS IN OTHER COUNTRIES 20 Patentable inventions - Italy 23 Procedures for securing patents overseas 25 European patent convention 27 Patent cooperation treaty 32 CONCLUSION 33 REFERENCES 33 INTRODUCTION A number of major developments in the comparatively calm world of patents occurred in 1978. These included a new Patents Act in the United Kingdom, 2 RECENT CHANGES IN PATENT LAW the commencement of operation of the European Patent Office and the institution of operations under the Patent Cooperation Treaty. Additionally, in February 1978 an important decision of the Constitutional Court in Italy nullified Article 14 of the Italian Patents Act, which had prohibited the grant of patents for pharmaceuticals. These various developments have or will have a significant effect on the procedure for obtaining patents and the importance of patents both generally and particularly as regards pharmaceuticals.