Heterocyclic Anticancer Compounds: Recent Advances and the Paradigm Shift Towards the Use of Nanomedicine’S Tool Box
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68 3 1 5"! Patent Request: Standard Patent/Patent of Addition
Λ _ ___ _ KWU/lXHJIMI AUSTRALIA Patents Act 1990 68 3 1 5"! PATENT REQUEST: STANDARD PATENT/PATENT OF ADDITION We, being the persons identified below as the Applicant, request the grant of a patent to the person identified below as the Nominated Person, for an invention described in the accompanying standard complete specification. ,· Full application details follow. [71] Applicant: ADIR ET COMPAGNIE Address: 1 RUE cXrLE HEBERT, F-92415 COURBEVOIE CEDEX, FRANCE [70] Nominated Person: ADIR ET COMPAGNIE Address: 1 RUE CARLE HEBERT, F-92415 COURBEVOIE CEDEX, FRANCE [54] Invent»·* Title: NOVEL N-PYRIDYL CARBOXAMIDES AND DERIVATIVES, PROCESSES FOR THEIR PREPARATION AND THE PHARMACEUTICAL COMPOSITIONS WHICH CONTAIN THEM Name(s) of actual inventor(s): JEAN-MICHEL ROBERT, ODILE RIDEAU, SYLVIE ROBERT-PIESSARD, JACQUELINE COURANT, GUILLAUME LE BAUT, DANIEL-HENRI CAIGNARD, PIERRE RENARD and GERARD ADAM Address for service in Australia: c/o WATERMARK PATENT & TRADEMARK ATTORNEYS, of 290 Burwood Road, Hawthorn, Victoria 3122, Australia Attorney Code: WM :,.··. BASIC CONVENTION APPLICATION(S) DETAILS .... [31] Application Number [33] Country Country [32] Date of Application : Code 9406412 FRANCE FR 27 MAY 1994 Basic Applicants): ADIR ET COMPAGNIE • · · · • · · *· Di awing number recommended to accompany the abstract ............................... By our Patent Attorneys, WATERMARK PATENT & TRADEMARK ATTORNEYS ...CM&/.VV2...... ....... DATED this 25th day of May 1995,. Carolyn J, Harris Registered Patent Attorney i P/00/008b 12/11/91 Section 29 (η Regulation 3.1 (2) AUSTRALIA Patents Act 1990 NOTICE OF ENTITLEMENT We, ADIR ET COMPAGNIE of, 1 Rue Carle Hebert, F-92415 Courbevoie Cedex, France, being the applicant in respect of Application No. -
Rhodium-Catalyzed Synthesis of Organosulfur Compounds Involving S-S Bond Cleavage of Disulfides and Sulfur
molecules Review Rhodium-Catalyzed Synthesis of Organosulfur Compounds Involving S-S Bond Cleavage of Disulfides and Sulfur Mieko Arisawa * and Masahiko Yamaguchi Department of Organic Chemistry, Graduate School of Pharmaceutical Sciences, Tohoku University, Aoba, Sendai 980-8578, Japan; [email protected] * Correspondence: [email protected]; Tel.: +81-22-795-6814 Academic Editor: Bartolo Gabriele Received: 17 July 2020; Accepted: 5 August 2020; Published: 7 August 2020 Abstract: Organosulfur compounds are widely used for the manufacture of drugs and materials, and their synthesis in general conventionally employs nucleophilic substitution reactions of thiolate anions formed from thiols and bases. To synthesize advanced functional organosulfur compounds, development of novel synthetic methods is an important task. We have been studying the synthesis of organosulfur compounds by transition-metal catalysis using disulfides and sulfur, which are easier to handle and less odiferous than thiols. In this article, we describe our development that rhodium complexes efficiently catalyze the cleavage of S-S bonds and transfer organothio groups to organic compounds, which provide diverse organosulfur compounds. The synthesis does not require use of bases or organometallic reagents; furthermore, it is reversible, involving chemical equilibria and interconversion reactions. Keywords: rhodium; catalysis; synthesis; organosulfur compounds; S-S bond cleavage; chemical equilibrium; reversible reaction 1. Introduction 1.1. Structure and Reactivity of Organic Disulfides Organosulfur compounds containing C-S bonds are widely used for the manufacture of drugs and materials. Compared with organic compounds containing oxygen, which is another group 16(6A) element, different properties appear owing to the large size and polarizability of sulfur atoms. -
B.Sc. III YEAR ORGANIC CHEMISTRY-III
BSCCH- 302 B.Sc. III YEAR ORGANIC CHEMISTRY-III SCHOOL OF SCIENCES DEPARTMENT OF CHEMISTRY UTTARAKHAND OPEN UNIVERSITY ORGANIC CHEMISTRY-III BSCCH-302 BSCCH-302 ORGANIC CHEMISTRY III SCHOOL OF SCIENCES DEPARTMENT OF CHEMISTRY UTTARAKHAND OPEN UNIVERSITY Phone No. 05946-261122, 261123 Toll free No. 18001804025 Fax No. 05946-264232, E. mail [email protected] htpp://uou.ac.in UTTARAKHAND OPEN UNIVERSITY Page 1 ORGANIC CHEMISTRY-III BSCCH-302 Expert Committee Prof. B.S.Saraswat Prof. A.K. Pant Department of Chemistry Department of Chemistry Indira Gandhi National Open University G.B.Pant Agriculture, University Maidan Garhi, New Delhi Pantnagar Prof. A. B. Melkani Prof. Diwan S Rawat Department of Chemistry Department of Chemistry DSB Campus, Delhi University Kumaun University, Nainital Delhi Dr. Hemant Kandpal Dr. Charu Pant Assistant Professor Academic Consultant School of Health Science Department of Chemistry Uttarakhand Open University, Haldwani Uttarakhand Open University, Board of Studies Prof. A.B. Melkani Prof. G.C. Shah Department of Chemistry Department of Chemistry DSB Campus, Kumaun University SSJ Campus, Kumaun University Nainital Nainital Prof. R.D.Kaushik Prof. P.D.Pant Department of Chemistry Director I/C, School of Sciences Gurukul Kangri Vishwavidyalaya Uttarakhand Open University Haridwar Haldwani Dr. Shalini Singh Dr. Charu Pant Assistant Professor Academic Consultant Department of Chemistry Department of Chemistry School of Sciences School of Science Uttarakhand Open University, Haldwani Uttarakhand Open University, Programme Coordinator Dr. Shalini Singh Assistant Professor Department of Chemistry Uttarakhand Open University Haldwani UTTARAKHAND OPEN UNIVERSITY Page 2 ORGANIC CHEMISTRY-III BSCCH-302 Unit Written By Unit No. Dr. Charu Pant 01, 02 & 03 Department of Chemistry Uttarakhand Open University Haldwani Dr. -
Heterocyclic Chemistry Updated
1 | Page Heterocyclic Chemistry By Dr Vipul Kataria Definition: A heterocyclic compound or ring structure is a cyclic compound that has atoms of at least two different elements (N, O, S, P) as members of its ring. Introduction: Heterocyclic compounds may be defined as cyclic compounds having as ring members atoms of at least two different elements. It means the cyclic compound has one another atom different than carbon. Heterocyclic compounds have much importance in organic chemistry because of abundant presence of heterocyclic compounds in present pharmaceutical drugs. Like other organic compounds, there are several defined rules for naming heterocyclic compounds. IUPAC rules for nomenclature of heterocyclic systems (SPU 2012, 2 Marks) The system for nomenclature for heterocyclic systems was given by Hantzsch and Widman. The Hantzsch-Widman nomenclature is based on the type (Z) of the heteroatom; the ring size (n) and nature of the ring, whether it is saturated or unsaturated. This system of nomenclature applies to monocyclic 3-to-10-membered ring heterocycles. Type of the heteroatom: The type of heteroatom is indicated by a prefix as shown below for common hetreroatoms. Dr Vipul Kataria, Chemistry Department, V. P. & R. P. T. P. Science College, VV Nagar 2 | Pag e When two or more of the same heteroatoms are present, the prrefix di, tri, tetra… are used. e.g. dioxa, triaza, dithia. If the heteroatoms are different their atomic number in that grroup is considered. Thus order of numbering will be O, S, N, P, Si. Ring size: The ring size is indicated by a suffix according to Table I below. -
UV-Curable Coating Composition
Europaisches Patentamt European Patent Office (fi) Publication number: 0 001 466 A1 Office europeen des brevets EUROPEAN PATENT APPLICATION 2y Application number: 78200215.8 © int. ci.*: C 09 D 3/49, C 08 F 299/00, C 08 F 2/50 §) Date of filing: 28.09.78 © Priority: 11.10.77 NL 7711121 Applicant: Akzo N.V., Ijssellaan 82, NL-6800 LS Arnhem (NL) (7g) Inventor: Noomen, Arie, Schoonoord 22, NL-2215 Ed @ Date of publication of application: 18.04.79 Voorhout (NL) Bulletin 79/8 Inventor: Wolters, Egbert, Potgieterstraat 21, NL-1053 XP Amsterdam (NL) @ Representative: Sieders, Rene et ai, P.O.Box 314, @ Designated Contracting States: BE DE FR GB NL SE NL-6800 AH Arnhem (NL) @ U.V.-curable coating composition. The invention relates to a coating composition which is curable under the influence of ultraviolet light and which comprises a U.V.-curable binder, a photoinitiator and as accelerator a tetrahydro-1,3-oxazine compound and/or an oxazolidine compound. The U.V.-curable binder is pref- erably an adduct containing at least one isocyanate group of a) an acrylic or methacrylic hydroxy ester having 5 to 20 carbon atoms and b) a polyisocyanate having 4 to 40 carbon atoms and 2 to 4 isocyanate groups. The invention relates to a coating composition which can be cured under the influence of ultraviolet light ;and is based on a U.V.-curable binder, a photoinitiator and a nitrogen-containing accelerator. In known com- positions useismade generally of an aromatic carbonyl compound as photoinitiator, and of an alkanolamine as accelerator. -
Phamarcological Effects Produced by the Modifications in Isoxazole Moeities
Archana c. et al. / Asian Journal of Phytomedicine and Clinical Research. 4(1), 2016, 29 - 32. Review Article CODEN: AJPCFF ISSN: 2321 – 0915 Asian Journal of Phytomedicine and Clinical Research Journal home page: www.ajpcrjournal.com PHAMARCOLOGICAL EFFECTS PRODUCED BY THE MODIFICATIONS IN ISOXAZOLE MOEITIES C. Archana *1 , E. Akila 2, Priya john 3 1*Department of Pharmaceutical Chemistry, Prime College of Pharmacy, Palakkad, Kerala, India. 2Department of Pharmacognosy, Prime College of Pharmacy, Palakkad, Kerala, India. 3Department of Pharmacology, Prime College of Pharmacy, Palakkad, Kerala, India. ABSTRACT Isoxazole and its derivatives are an important class of heterocyclic compound displaying a broad spectrum of biological activities which have made them privileged structures. In the present work, attempts were made to identify leading isoxazole moieties as candidate drugs against many diseases. For example, isoxazole substituted 9-anilino acridine derivatives was found to have increased antioxidant activities. The molecular docking studies show a good correlation between their biological activities screened and auto dock binding free energy. These derivatives will encourage helping to design future anti cancer agents with higher therapeutic potential. Another example is isoxazole incorporated 2-quinolones to show increased antimicrobial and anti inflammatory activities. More importantly, various isoxazole derivatives greatly increase biological properties of the structure like anti-infective action, anticancer properties, anti-protozoal and mutagenic properties. A modification in their structures has offered a high degree of diversity that has proven useful for the development of new therapeutic agents having improved potency and lesser toxicity. In the present study of concise review, is provided on the activities of isoxazole and its derivatives which involve history, chemistry, different methods of synthesis of isoxazole with biological activities and docking studies. -
Cytotoxic Chemotherapy: Still the Mainstay of Clinical Practice for All
G Model ONCH-2130; No. of Pages 14 ARTICLE IN PRESS Critical Reviews in Oncology/Hematology xxx (2016) xxx–xxx Contents lists available at ScienceDirect Critical Reviews in Oncology/Hematology journal homepage: www.elsevier.com/locate/critrevonc Cytotoxic chemotherapy: Still the mainstay of clinical practice for all subtypes metastatic breast cancer a,b b,∗ c c Chris Twelves , Maria Jove , Andrea Gombos , Ahmad Awada a Leeds Institute of Cancer and Pathology, St. James’s University Hospital, Leeds, UK b St James’s Institute of Oncology, St. James’s University Hospital, Bexley Wing, Level 4, Beckett Street, LS9 7TF Leeds, UK c Medical Oncology Clinic, Jules Bordet Institute, Université Libre de Bruxelles, Boulevard de Waterloo 121, B-1000 Brussels, Belgium Contents 1. Introduction . 00 2. Current therapeutic options for anthracycline- and taxane pretreated MBC . 00 2.1. Rechallenge with, or reformulation of, an anthracyclines or taxane . 00 2.2. Capecitabine . 00 3. Newer antimicrotubule agents . 00 3.1. Ixabepilone . 00 3.2. Eribulin . 00 4. Emerging new agents . 00 4.1. Vinflunine . 00 4.2. Etirinotecan pegol (NKTR-102). .00 4.2.1. Pharmacology. .00 4.2.2. Early clinical trials . 00 4.2.3. The BEACON trial . 00 5. Conclusions . 00 Conflict of interest . 00 Acknowledgments . 00 References . 00 Biography . 00 a r t i c l e i n f o a b s t r a c t Article history: Cytotoxic chemotherapy remains central to the treatment of all subtypes of metastatic breast cancer Received 13 October 2015 (MBC). We review evidence-based chemotherapy options for women with MBC after an anthracycline Received in revised form and a taxane including re-challenge with anthracycline or taxane, capecitabine, eribulin and ixabepilone 24 December 2015 as a single agent or combination with capecitabine (not approved in the EU); and the vinca alkaloid Accepted 20 January 2016 vinflunine as single agent or combined with either capecitabine/gemcitabine (also not approved EU or USA). -
Management of Brain and Leptomeningeal Metastases from Breast Cancer
International Journal of Molecular Sciences Review Management of Brain and Leptomeningeal Metastases from Breast Cancer Alessia Pellerino 1,* , Valeria Internò 2 , Francesca Mo 1, Federica Franchino 1, Riccardo Soffietti 1 and Roberta Rudà 1,3 1 Department of Neuro-Oncology, University and City of Health and Science Hospital, 10126 Turin, Italy; [email protected] (F.M.); [email protected] (F.F.); riccardo.soffi[email protected] (R.S.); [email protected] (R.R.) 2 Department of Biomedical Sciences and Human Oncology, University of Bari Aldo Moro, 70121 Bari, Italy; [email protected] 3 Department of Neurology, Castelfranco Veneto and Treviso Hospital, 31100 Treviso, Italy * Correspondence: [email protected]; Tel.: +39-011-6334904 Received: 11 September 2020; Accepted: 10 November 2020; Published: 12 November 2020 Abstract: The management of breast cancer (BC) has rapidly evolved in the last 20 years. The improvement of systemic therapy allows a remarkable control of extracranial disease. However, brain (BM) and leptomeningeal metastases (LM) are frequent complications of advanced BC and represent a challenging issue for clinicians. Some prognostic scales designed for metastatic BC have been employed to select fit patients for adequate therapy and enrollment in clinical trials. Different systemic drugs, such as targeted therapies with either monoclonal antibodies or small tyrosine kinase molecules, or modified chemotherapeutic agents are under investigation. Major aims are to improve the penetration of active drugs through the blood–brain barrier (BBB) or brain–tumor barrier (BTB), and establish the best sequence and timing of radiotherapy and systemic therapy to avoid neurocognitive impairment. Moreover, pharmacologic prevention is a new concept driven by the efficacy of targeted agents on macrometastases from specific molecular subgroups. -
Heterocyclic Compounds with Biological Meaning
Heterocyclic compounds with biological meaning 1 Heterocyclic compounds Cyclic, organic compounds which besides carbon atoms have one or more heteroatom (other elements than C). Heterocyclic atoms: – nitrogen, N – sulphur, S – oxygen, O – phosphorus, P – barium, Ba – zinc, Zn – silicon, Si. 2 Heterocyclic compounds From the biological point of view, the most important are heterocyclic compounds with 5- and 6-membered rings, containing: S, N, O. Most of the heterocyclic compounds have their common names. Substituent’s position in the ring is described by : – number – position of heteroatom – no. 1 – Greek letter – describes carbon atom the closest to heteroatom as a, then β and γ, respectively. 3 Heterocyclic compounds Heterocyclic compounds are: • widespread in nature • biologically active • some of them are toxic (e.g. coniine, coumarin and derivatives). Occurrence in: • natural dyes - heme, chlorophyll • alkaloids – atropine and nicotine • amino acids such as tryptophan and histidine • enzymes, nucleoproteins, antibiotics • vitamins • many synthetic pharmaceuticals. 4 Heterocyclic compounds Aromatic character of heteroatom-containing ring comes from aromatic sextet which consists of: • „not bound” electron pairs of heteroatoms • four electrons π from carbon atoms Pyrrole Furane Thiophen 5 5- membered ring heterocyclic compounds with one heteroatom 5-membered rings: • contain mostly oxygen, sulphur and nitrogen • are flat • are aromatic 6 5- membered ring heterocyclic compounds with two heteroatoms oxazole imidazole thiazole pyrazole 7 5- membered ring heterocyclic compounds With one heteroatom With two heteroatoms Condensation products with benzene 8 Pyrrole and derivatives • Pyrrole derivatives: • pyrroline • pyrrolidone • proline, • Hydroksyproline. • Condensation’s products of pyrrole with benzene: – indole, – tryptophan, – serotonin. • Condensation’s products of pyrrole with formaldehyde: – heme – hemoglobin – billirubin – porphyrins – Biliverdin. -
Tanibirumab (CUI C3490677) Add to Cart
5/17/2018 NCI Metathesaurus Contains Exact Match Begins With Name Code Property Relationship Source ALL Advanced Search NCIm Version: 201706 Version 2.8 (using LexEVS 6.5) Home | NCIt Hierarchy | Sources | Help Suggest changes to this concept Tanibirumab (CUI C3490677) Add to Cart Table of Contents Terms & Properties Synonym Details Relationships By Source Terms & Properties Concept Unique Identifier (CUI): C3490677 NCI Thesaurus Code: C102877 (see NCI Thesaurus info) Semantic Type: Immunologic Factor Semantic Type: Amino Acid, Peptide, or Protein Semantic Type: Pharmacologic Substance NCIt Definition: A fully human monoclonal antibody targeting the vascular endothelial growth factor receptor 2 (VEGFR2), with potential antiangiogenic activity. Upon administration, tanibirumab specifically binds to VEGFR2, thereby preventing the binding of its ligand VEGF. This may result in the inhibition of tumor angiogenesis and a decrease in tumor nutrient supply. VEGFR2 is a pro-angiogenic growth factor receptor tyrosine kinase expressed by endothelial cells, while VEGF is overexpressed in many tumors and is correlated to tumor progression. PDQ Definition: A fully human monoclonal antibody targeting the vascular endothelial growth factor receptor 2 (VEGFR2), with potential antiangiogenic activity. Upon administration, tanibirumab specifically binds to VEGFR2, thereby preventing the binding of its ligand VEGF. This may result in the inhibition of tumor angiogenesis and a decrease in tumor nutrient supply. VEGFR2 is a pro-angiogenic growth factor receptor -
Isoxazoles: Molecules with Potential Medicinal Properties
IJPCBS 2013, 3(2), 294-304 Jayaroopa et al. ISSN: 2249-9504 INTERNATIONAL JOURNAL OF PHARMACEUTICAL, CHEMICAL AND BIOLOGICAL SCIENCES Available online at www.ijpcbs.com Research Article ISOXAZOLES: MOLECULES WITH POTENTIAL MEDICINAL PROPERTIES K. Ajay Kumar and P. Jayaroopa* Post Graduate Department of Chemistry, Yuvaraja’s College, University of Mysore, Mysore-570 005, India. ABSTRACT Isoxazole is a five membered heterocyclic compound having various pharmacological actions. The great interest associated with isoxazoles and their derivatives is based on their versatility as synthetic building blocks, their latent functionalities as enaminones, 1,3-dicarbonyl compounds, γ-amino alcohols, and β-hydroxy nitriles have been widely exploited for the synthesis of other heterocycles and complex molecules. This review paper comprises of up to date information on isoxazole analogs. More emphasis was given to critical discussion on the synthetic strategy of isoxazole derivative, their utility as building blocks in their transformation to more biologically potent molecules. Results of isoxazole derivatives and their substitutions effect on diverse biological activities also presented. Keywords: Isoxazoles, antioxidant, antimicrobial, analgesic, anti-platelet, anti-HIV. INTRODUCTION sulfisoxazole, oxacillin, cycloserine and acivicin Nitrogen containing heterocycles with an have been in commercial use for many years. oxygen atom are considered as an important Cycloserine is the best known antibiotic drug class of compounds in medicinal chemistry that possess antitubercular, antibacterial because of their diversified biological activities and in treatment of leprosy. Acivicin is applications. The exploitation of a simple an antitumour, antileishmania drug, while molecule with different functionalities for the isoxaflutole is used as herbicidal drug. synthesis of heterocycles is a worthwhile Isoxazoles have illustrious history; their contribution in the chemistry of heterocycles. -
Dibenzothiophene/Oxide and Quinoxaline/Pyrazine Derivatives Serving As Electron-Transport Materials**
FULL PAPER DOI: 10.1002/adfm.200500823 Dibenzothiophene/Oxide and Quinoxaline/Pyrazine Derivatives Serving as Electron-Transport Materials** By Tai-Hsiang Huang, Wha-Tzong Whang,* Jiun Yi Shen, Yuh-Sheng Wen, Jiann T. Lin,* Tung-Huei Ke, Li-Yin Chen, and Chung-Chih Wu* A series of 2,8-disubstituted dibenzothiophene and 2,8-disubstituted dibenzothiophene-S,S-dioxide derivatives containing quinoxaline and pyrazine moieties are synthesized via three key steps: i) palladium-catalyzed Sonogashira coupling reaction to form dialkynes; ii) conversion of the dialkynes to diones; and iii) condensation of the diones with diamines. Single-crystal characterization of 2,8-di(6,7-dimethyl-3-phenyl-2-quinoxalinyl)-5H-5k6-dibenzo[b,d]thiophene-5,5-dione indicates a triclinic crystal structure with space group P1 and a non-coplanar structure. These new materials are amorphous, with glass-transition temperatures ranging from 132 to 194 °C. The compounds (Cpd) exhibit high electron mobilities and serve as effective elec- tron-transport materials for organic light-emitting devices. Double-layer devices are fabricated with the structure indium tin oxide (ITO)/Qn/Cpd/LiF/Al, where yellow-emitting 2,3-bis[4-(N-phenyl-9-ethyl-3-carbazolylamino)phenyl]quinoxaline (Qn) serves as the emitting layer. An external quantum efficiency of 1.41 %, a power efficiency of 4.94 lm W–1, and a current efficien- cy of 1.62 cd A–1 are achieved at a current density of 100 mA cm–2. 1. Introduction efficiency, brightness, and durability.[4] In contrast, reports of the use of small molecules as electron-transporting materials [5] Organic and polymer light-emitting diodes (OLEDs and are still rare in the literature.