RU2506256C2 - Лиганды для визуализации иннервации сердца - Google Patents

Лиганды для визуализации иннервации сердца Download PDF

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RU2506256C2
RU2506256C2 RU2009128591/04A RU2009128591A RU2506256C2 RU 2506256 C2 RU2506256 C2 RU 2506256C2 RU 2009128591/04 A RU2009128591/04 A RU 2009128591/04A RU 2009128591 A RU2009128591 A RU 2009128591A RU 2506256 C2 RU2506256 C2 RU 2506256C2
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Эджей ПЬЮРОХИТ
Томас Д. ХЭРРИС
Хайке С. РАДЕКЕ
Саймон П. РОБИНСОН
Мин Ю
Дэвид С. КЕЙСБИР
Майкл Т. ЭЖЕР
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Abstract

Изобретение относится к новым соединениям, пригодным для визуализации иннервации сердца, структурной формулы
Figure 00000079
где n=0, R и R1 независимо выбраны из группы, состоящей из H, (C1-C4)алкила, NR4(C(=NR5)NHR6, NR4C(=O)N(R5)2; R2 отсутствует; R3 представляет собой Н; R4, R5 и R6 независимо выбраны из группы, состоящей из H и (C1-C8)алкила; или любые два из R4, R5 и R6 могут образовывать циклическую структуру, состоящую из -CH2-CH2- или -CH=CH-; W и X независимо выбраны из группы, состоящей из H и Br; и A отсутствует; если соединение содержит связующую группу Q между Y и Z, Y и Z независимо выбираются из группы, состоящей из CH и NR7, и Q представляет собой CH, a R7 представляет собой (C1-C8)алкил, или если связующая группа Q отсутствует между Y и Z, Y и Z независимо выбраны из группы, состоящей из H, OR4, Cl, Br, (C6-C10)арила и CF3; где один или более из R4, R5, R6 или R7 могут быть замещены визуализирующим фрагментом; при условии, что по меньшей мере один визуализирующий фрагмент находится в любой группе Y или Z, когда Y или Z представляет собой OR4, или в R7, или в R5, или R6, когда R или R1 представляет собой NR4(C(=NR5)NHR6, и представляет собой 18F. Изобретение также относится к способу визуализации иннервации сердца и применению соединений для изготовления средства для визуализации иннервации сердца. 4 н. и 16 з.п. ф-лы, 2 ил., 2 табл., 25 пр.

Description

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Claims (20)

1. Соединение, имеющее следующую формулу:
Figure 00000067

где n=0,
R и R1 независимо выбраны из группы, состоящей из Н, (C1-C4)алкила, NR4(C(=NR5)NHR6, NR4C(=O)N(R5)2;
R2 отсутствует;
R3 представляет собой H;
R4, R5 и R6 независимо выбраны из группы, состоящей из H и (C1-C8)алкила;
при этом возможно, что любые два из R4, R5 и R6 могут образовывать циклическую структуру, состоящую из -CH2-CH2- или -CH=CH-;
W и X независимо выбраны из группы, состоящей из H и Br; и
A отсутствует;
причем, если соединение содержит связующую группу Q между Y и Z, Y и Z независимо выбираются из группы, состоящей из CH и NR7, и Q представляет собой CH, a R7 представляет собой (C1-C8)алкил, или
если связующая группа Q отсутствует между Y и Z, Y и Z независимо выбраны из группы, состоящей из H, OR4, Cl, Br, (C6-C10)арила и CF3; где
один или более из R4, R5, R6 или R7 могут быть замещены визуализирующим фрагментом;
при условии, что по меньшей мере один визуализирующий фрагмент находится в любой группе Y или Z, когда Y или Z представляет собой OR4, или в R7, или в R5 или R6 когда R или R1 представляет собой NR4(C(=NR5)NHR6, и представляет собой 18F;
или его соль.
2. Соединение по п.1, где R представляет собой NR4(C(=NR5)NHR6.
3. Соединение по п.2, где R4, R5 и R6, каждый, представляют собой H.
4. Соединение по п.1, где W и X, каждый, представляет собой H.
5. Соединение по п.1, где Z представляет собой OR4.
6. Соединение по п.5, где R4 представляет собой (C1-C8)алкил, замещенный 18F.
7. Соединение по п.1, где Z представляет собой (C6-C10)арил, замещенный l8F.
8. Соединение по п.1, где любые два из R4, R5 или R6 образуют циклическую структуру, состоящую из -CH2-CH2- или -CH=CH-.
9. Соединение по п.1, где:
X, W, R3 и R1 представляют собой Н;
R представляет собой NHC(=NH)NH2;
Z представляет собой OR4;
R4 представляет собой (C1-C8)алкил, замещенный 18F; и
Y представляет собой H, CF3, Cl или Br, или его соль.
10. Соединение по п.1, которое имеет структурную формулу, выбранную из группы, состоящей из:
Figure 00000068
Figure 00000069

Figure 00000070
Figure 00000071

или его соль.
11. Соединение по п.1, которое имеет структурную формулу, выбранную из группы, состоящей из:
Figure 00000072
Figure 00000073
и
Figure 00000074

или его соль.
12. Соединение по п.1, которое имеет структурную формулу:
Figure 00000075
,
или его соль.
13. Соединение по п.1, которое представляет собой N-[3-бpoм-4(3-[18F]фторпропокси)-бензил]-гуанидина гидрохлорид.
14. Соединение, имеющее формулу:
Figure 00000076

где n=1;
R, R1 и R2 независимо выбраны из группы, состоящей из H, (C1-C4)алкила, C(=NR4)NHR5 и NR4C(=NR5)NHR6;
R3 представляет собой H;
где R4, R5 и R6 выбраны из группы, состоящей из H и (C1-C8)алкила; при этом возможно, что любые два из R4, R5 и R6 могут образовывать циклическую структуру, состоящую из -CH=CH-;
W и X представляют собой Н;
Y выбран из группы, состоящей из H, OR4, O и Br;
Z представляет собой OR4, где R4 содержит по меньшей мере один 18F;
A представляет собой O или отсутствует, или его соль.
15. Соединение по п.14, где R обозначает NR4(C(=NR5)NHR6.
16. Соединение по п.15, где R4, R5 и R6, каждый, представляет собой H.
17. Соединение по п.14, где любые два из R4, R5 или R6 образуют циклическую структуру, состоящую из -CH=CH-.
18. Соединение по п.14, имеющее структуру, выбранную из группы, состоящей из:
Figure 00000077
и
Figure 00000078

или его соль.
19. Способ визуализации иннервации сердца, включающий стадии: введения эффективного количества соединения по пп.1-18 пациенту; выявления гамма-излучения, излучаемого указанным соединением; и формирования его изображения.
20. Применение соединения по любому из пп.1-18 для изготовления средства для визуализации иннервации сердца.
RU2009128591/04A 2006-12-26 2007-12-21 Лиганды для визуализации иннервации сердца RU2506256C2 (ru)

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Publication number Priority date Publication date Assignee Title
US7344702B2 (en) 2004-02-13 2008-03-18 Bristol-Myers Squibb Pharma Company Contrast agents for myocardial perfusion imaging
TWI549692B (zh) * 2006-12-26 2016-09-21 藍瑟斯醫學影像公司 使心臟神經分布顯像之配位體
EP2534136B1 (en) 2010-02-08 2017-09-06 Lantheus Medical Imaging, Inc. Methods for synthesizing imaging agents, and intermediates thereof
KR102136503B1 (ko) * 2010-05-11 2020-07-21 랜티우스 메디컬 이메징, 인크. 영상화제의 합성 및 사용을 위한 조성물, 방법 및 시스템
BR122014024883A2 (pt) 2010-05-14 2019-08-20 Dana-Farber Cancer Institute, Inc. Compostos no tratamento de neoplasia
MX354217B (es) 2010-05-14 2018-02-19 Dana Farber Cancer Inst Inc Composiciones y metodos para el tratamiento de leucemia.
CN103180318B (zh) 2010-05-14 2017-05-10 达那-法伯癌症研究所 雄性避孕组合物以及使用方法
AR086113A1 (es) 2011-04-30 2013-11-20 Abbott Lab Isoxazolinas como agentes terapeuticos
BR122019017259B1 (pt) * 2011-09-09 2022-05-10 Lantheus Medical Imaging, Inc Compostos úteis como agentes de imageamento, composições que os compreende, métodos, e uso de agentes de imageamento
AU2013263297B2 (en) 2012-04-10 2017-11-30 Lantheus Medical Imaging, Inc. Radiopharmaceutical synthesis methods
AU2013203000B9 (en) 2012-08-10 2017-02-02 Lantheus Medical Imaging, Inc. Compositions, methods, and systems for the synthesis and use of imaging agents
WO2014052454A1 (en) * 2012-09-25 2014-04-03 The Regents Of The University Of Michigan Imaging agents
US20150366523A1 (en) 2013-01-24 2015-12-24 Shlomo Ben-Haim Neuronal imaging and treatment
WO2014115151A1 (en) 2013-01-24 2014-07-31 Tylerton International Holdings Inc. Body structure imaging
JP2016513526A (ja) * 2013-03-11 2016-05-16 タイラートン インターナショナル ホールディングス インコーポレイテッドＴｙｌｅｒｔｏｎ Ｉｎｔｅｒｎａｔｉｏｎａｌ Ｈｏｌｄｉｎｇｓ Ｉｎｃ． 自律神経系モデリング及びその使用
WO2015013635A2 (en) 2013-07-25 2015-01-29 Dana-Farber Cancer Institute, Inc. Inhibitors of transcription factors and uses thereof
CN105744985B (zh) * 2013-09-08 2020-04-07 泰勒顿国际公司 控制减弱的心区的检测
RU2016122654A (ru) 2013-11-08 2017-12-14 Дана-Фарбер Кэнсер Инститьют, Инк. Комбинированная терапия злокачественной опухоли с использованием ингибиторов бромодоменового и экстратерминального (вет) белка
CN106102583A (zh) 2014-01-10 2016-11-09 泰勒顿国际公司 瘢痕和纤维心脏区的检测
WO2015117087A1 (en) 2014-01-31 2015-08-06 Dana-Farber Cancer Institute, Inc. Uses of diazepane derivatives
EP3099677A4 (en) 2014-01-31 2017-07-26 Dana-Farber Cancer Institute, Inc. Diaminopyrimidine benzenesulfone derivatives and uses thereof
CN106456653A (zh) 2014-02-28 2017-02-22 腾沙治疗公司 高胰岛素血症相关病症的治疗
WO2016016837A1 (en) 2014-07-30 2016-02-04 Navix International Limited Probe localization
CA2955077A1 (en) 2014-08-08 2016-02-11 Dana-Farber Cancer Institute, Inc. Dihydropteridinone derivatives and uses thereof
BR112017002369A2 (pt) 2014-08-08 2017-12-05 Dana Farber Cancer Inst Inc derivados de diazepana e usos dos mesmos
WO2016201370A1 (en) 2015-06-12 2016-12-15 Dana-Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
WO2017044792A1 (en) 2015-09-11 2017-03-16 Dana-Farber Cancer Institute, Inc. Acetamide thienotriazoldiazepines and uses thereof
BR112018004618A2 (pt) 2015-09-11 2018-09-25 Dana-Farber Cancer Institute, Inc. ciano tienotriazoldiazepinas e usos das mesmas
SG10201913450PA (en) 2015-11-25 2020-03-30 Dana Farber Cancer Inst Inc Bivalent bromodomain inhibitors and uses thereof
CN107892651A (zh) * 2017-11-29 2018-04-10 陕西慧康生物科技有限责任公司 一种合成dl‑盐酸麻黄碱的方法
WO2020081410A2 (en) * 2018-10-15 2020-04-23 Bristol-Myers Squibb Company Radioligands for imaging the lpa1 receptor
EP3682906A1 (en) * 2019-01-17 2020-07-22 Julius-Maximilians-Universität Würzburg Compound targeting norepinephrine transporter
CN109748825B (zh) * 2019-02-01 2022-02-18 原子高科股份有限公司 一种18f标记的胍甲基取代苯类似物及其应用

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2145608C1 (ru) * 1993-03-30 2000-02-20 Е.И.Дю Пон Мерк Фармацьютикал Компани Циклические пептиды, радиофармацевтический препарат, циклические пептиды, имеющие радиоактивную метку
WO2005115971A1 (ja) * 2004-05-28 2005-12-08 Hamamatsu Photonics K.K. 放射性チロシン誘導体、その製造方法、放射性チロシン誘導体からなるポジトロンイメージング用標識剤及び腫瘍の悪性度評価薬剤並びに腫瘍の検出方法
US20060127309A1 (en) * 2004-12-10 2006-06-15 The Regents Of The University Of Michigan Imaging agents

Family Cites Families (72)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6012A (en) * 1849-01-09 Lithographing co
FR1010218A (fr) 1949-02-10 1952-06-09 American Cyanamid Co Perfectionnements aux sels de guanidine
GB1215255A (en) 1968-03-13 1970-12-09 Pfizer & Co C Halophenylalkylguanidine compounds
US4094881A (en) * 1976-03-10 1978-06-13 Smithkline Corporation Process for preparing triazolethiols
US4275074A (en) 1979-03-09 1981-06-23 Graham J. Dobbie Catecholamine treatment of ocular hypertension
US4270537A (en) 1979-11-19 1981-06-02 Romaine Richard A Automatic hypodermic syringe
US4258188A (en) * 1980-02-04 1981-03-24 American Home Products Corporation 2-(1-Piperazinyl)-cycloheptimidazole derivatives
US4622217A (en) * 1984-04-27 1986-11-11 The Regents Of The University Of Michigan I-4-amino-3-iodobenzylguanidine as imaging and therapeutic agent
US4596556A (en) 1985-03-25 1986-06-24 Bioject, Inc. Hypodermic injection apparatus
CA1283827C (en) 1986-12-18 1991-05-07 Giorgio Cirelli Appliance for injection of liquid formulations
GB8704027D0 (en) 1987-02-20 1987-03-25 Owen Mumford Ltd Syringe needle combination
EP0288284A3 (en) * 1987-04-24 1990-07-25 King Faisal Specialist Hospital And Research Centre Method of producing iodine 124 and meta-iodobenzylguanidine containing iodine 124
US4790824A (en) 1987-06-19 1988-12-13 Bioject, Inc. Non-invasive hypodermic injection device
US4941880A (en) 1987-06-19 1990-07-17 Bioject, Inc. Pre-filled ampule and non-invasive hypodermic injection device assembly
US4940460A (en) 1987-06-19 1990-07-10 Bioject, Inc. Patient-fillable and non-invasive hypodermic injection device assembly
US5339163A (en) 1988-03-16 1994-08-16 Canon Kabushiki Kaisha Automatic exposure control device using plural image plane detection areas
FR2638359A1 (fr) 1988-11-03 1990-05-04 Tino Dalto Guide de seringue avec reglage de la profondeur de penetration de l'aiguille dans la peau
US5312335A (en) 1989-11-09 1994-05-17 Bioject Inc. Needleless hypodermic injection device
US5064413A (en) 1989-11-09 1991-11-12 Bioject, Inc. Needleless hypodermic injection device
US5190521A (en) 1990-08-22 1993-03-02 Tecnol Medical Products, Inc. Apparatus and method for raising a skin wheal and anesthetizing skin
US5527288A (en) 1990-12-13 1996-06-18 Elan Medical Technologies Limited Intradermal drug delivery device and method for intradermal delivery of drugs
GB9118204D0 (en) 1991-08-23 1991-10-09 Weston Terence E Needle-less injector
SE9102652D0 (sv) 1991-09-13 1991-09-13 Kabi Pharmacia Ab Injection needle arrangement
US5674863A (en) * 1991-10-18 1997-10-07 Genentech, Inc. Nonpeptidyl integrin inhibitors having specificity for the GPIIb IIIa receptor
US5328483A (en) 1992-02-27 1994-07-12 Jacoby Richard M Intradermal injection device with medication and needle guard
US5383851A (en) 1992-07-24 1995-01-24 Bioject Inc. Needleless hypodermic injection device
US5569189A (en) 1992-09-28 1996-10-29 Equidyne Systems, Inc. hypodermic jet injector
US5334144A (en) 1992-10-30 1994-08-02 Becton, Dickinson And Company Single use disposable needleless injector
TW279864B (ru) * 1993-02-19 1996-07-01 Janssen Pharmaceutica Nv
EP0639573A1 (de) * 1993-08-03 1995-02-22 Hoechst Aktiengesellschaft Benzokondensierte 5-Ringheterocyclen, Verfahren zu ihrer Herstellung, ihre Verwendung als Medikament, ihre Verwendung als Diagnostikum, sowie sie enthaltendes Medikament
WO1995024176A1 (en) 1994-03-07 1995-09-14 Bioject, Inc. Ampule filling device
US5466220A (en) 1994-03-08 1995-11-14 Bioject, Inc. Drug vial mixing and transfer device
US5599302A (en) 1995-01-09 1997-02-04 Medi-Ject Corporation Medical injection system and method, gas spring thereof and launching device using gas spring
US5730723A (en) 1995-10-10 1998-03-24 Visionary Medical Products Corporation, Inc. Gas pressured needle-less injection device and method
US5874573A (en) 1995-06-26 1999-02-23 Concat, Inc. Compounds with chelation affinity and selectivity for first transition series elements: use in medical therapy
US5893397A (en) 1996-01-12 1999-04-13 Bioject Inc. Medication vial/syringe liquid-transfer apparatus
GB9607549D0 (en) 1996-04-11 1996-06-12 Weston Medical Ltd Spring-powered dispensing device
TW499412B (en) 1996-11-26 2002-08-21 Dimensional Pharm Inc Aminoguanidines and alkoxyguanidines as protease inhibitors
ATE342262T1 (de) 1996-11-27 2006-11-15 Bristol Myers Squibb Pharma Co Neue integrin rezeptor antagonisten
US5993412A (en) 1997-05-19 1999-11-30 Bioject, Inc. Injection apparatus
CA2345710C (en) 1997-10-02 2008-12-30 The University Of Western Ontario Preparation of radiolabelled haloaromatics via polymer-bound intermediates
IT1298087B1 (it) 1998-01-08 1999-12-20 Fiderm S R L Dispositivo per il controllo della profondita' di penetrazione di un ago, in particolare applicabile ad una siringa per iniezioni
AU3406599A (en) 1998-04-09 1999-11-01 Institut Fur Diagnostikforschung Gmbh An Der Freien Universitat Berlin Novel benzyl guanidine derivatives for therapy and (in-vivo) and (in-vitro) diagnosis
AU5671699A (en) 1998-08-14 2000-03-06 Smithkline Beecham Corporation Grp receptor ligands
CN1356913A (zh) 1998-12-18 2002-07-03 杜邦药品公司 玻连蛋白受体拮抗剂药物
US6656448B1 (en) 2000-02-15 2003-12-02 Bristol-Myers Squibb Pharma Company Matrix metalloproteinase inhibitors
GB0019357D0 (en) 2000-08-07 2000-09-27 Melacure Therapeutics Ab Novel phenyl guanidines
DE10114561A1 (de) 2001-03-24 2002-09-26 Wella Ag Verwendung von Mitteln enthaltend Kreatin, Kreatin und/oder deren Derivaten zur Verstärkung und Strukturverbesserung von keratinischen Fasern
US7344702B2 (en) 2004-02-13 2008-03-18 Bristol-Myers Squibb Pharma Company Contrast agents for myocardial perfusion imaging
WO2004037166A2 (en) 2002-09-17 2004-05-06 Isis Pharmaceuticals, Inc. Therapeutic guanidines
JP2007527389A (ja) * 2003-06-30 2007-09-27 メルク　エンド　カムパニー　インコーポレーテッド 放射性カンナビノイド−１受容体修飾因子
AU2004294989B2 (en) * 2003-12-01 2009-03-19 Ignasi Carrio Novel differential imaging method
WO2005095345A2 (en) 2004-03-23 2005-10-13 Achillion Pharmaceuticals, Inc. Heteroaryl guanidines as inhibitors of viral replication
ATE493152T1 (de) 2004-09-23 2011-01-15 Guerbet Sa Liposomale kontrastmittel für die cest-bildgebung
US20060083681A1 (en) * 2004-10-18 2006-04-20 Ajay Purohit Compounds for myocardial perfusion imaging
GB0512770D0 (en) 2005-06-23 2005-07-27 Hammersmith Imanet Ltd Imaging compounds
AU2007332641A1 (en) 2006-12-13 2008-06-19 F. Hoffmann-La Roche Ag Novel 2 -imidazoles as ligands for trace amine associated receptors (TAAR)
GB0625523D0 (en) 2006-12-21 2007-01-31 Ge Healthcare Ltd In vivo imaging agents
TWI549692B (zh) 2006-12-26 2016-09-21 藍瑟斯醫學影像公司 使心臟神經分布顯像之配位體
WO2008082305A1 (en) 2006-12-28 2008-07-10 Raufoss Technology As Control arm
US7887784B2 (en) 2007-03-21 2011-02-15 University Of Montana 1-[(2′-substituted)-piperazin-1′ -yl]-isoquinolines as norepinephrine transporter inhibitor therapeutics and positron emission tomography imaging agents
BRPI0818671A2 (pt) 2007-10-18 2015-09-15 Boehringer Ingelheim Int preparação de diidrotieno[3,2-d]pirimidinas e intermediários empregados nela
WO2010015340A1 (en) 2008-08-06 2010-02-11 Bayer Schering Pharma Aktiengesellschaft Daa-pyridine as peripheral benzodiazepine receptor ligand for diagnostic imaging and pharmaceutical treatment
GB0906274D0 (en) 2009-04-09 2009-05-20 Ge Healthcare Ltd Imaging the central nervous system
CA2758883C (en) 2009-04-15 2020-03-10 Lantheus Medical Imaging, Inc. Stabilization of radiopharmaceutical compositions using ascorbic acid
CN101555232B (zh) 2009-05-21 2011-01-05 北京师范大学 氟-18标记哒嗪酮类化合物及制备方法和应用
CA2803520C (en) 2009-07-08 2019-10-22 Lantheus Medical Imaging, Inc. N-alkoxyamide conjugates as imaging agents
EP2534136B1 (en) 2010-02-08 2017-09-06 Lantheus Medical Imaging, Inc. Methods for synthesizing imaging agents, and intermediates thereof
KR102136503B1 (ko) 2010-05-11 2020-07-21 랜티우스 메디컬 이메징, 인크. 영상화제의 합성 및 사용을 위한 조성물, 방법 및 시스템
BR122019017259B1 (pt) 2011-09-09 2022-05-10 Lantheus Medical Imaging, Inc Compostos úteis como agentes de imageamento, composições que os compreende, métodos, e uso de agentes de imageamento
EP2671575A1 (en) 2012-06-04 2013-12-11 Universität Regensburg Ras inhibitors
JP2017131851A (ja) 2016-01-29 2017-08-03 日本特殊陶業株式会社 マイクロ波加熱用触媒材料、マイクロ波加熱用触媒体、及び、その製造方法

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2145608C1 (ru) * 1993-03-30 2000-02-20 Е.И.Дю Пон Мерк Фармацьютикал Компани Циклические пептиды, радиофармацевтический препарат, циклические пептиды, имеющие радиоактивную метку
WO2005115971A1 (ja) * 2004-05-28 2005-12-08 Hamamatsu Photonics K.K. 放射性チロシン誘導体、その製造方法、放射性チロシン誘導体からなるポジトロンイメージング用標識剤及び腫瘍の悪性度評価薬剤並びに腫瘍の検出方法
US20060127309A1 (en) * 2004-12-10 2006-06-15 The Regents Of The University Of Michigan Imaging agents

Non-Patent Citations (6)

* Cited by examiner, † Cited by third party
Title
G. VAIDYANATHAN ЕТ AL., "No-carrier-added iodine-131-FIBG: evaluation of an MIBG analog", The Journal of Nuclear Medicine, 1997, vol.38(2), pp.330-334. *
G. VAIDYANATHAN ЕТ AL., "No-carrier-added iodine-131-FIBG: evaluation of an MIBG analog", The Journal of Nuclear Medicine, 1997, vol.38(2), pp.330-334. M. HORBERG ЕТ AL., "Bioisosteric modification of PETT-HIV1 RT-inhibitors: Synthesis and biological evaluation", Bioorganic&Medicinal Chemistry Letters, 2000, vol.10, pp.265-268. S. DAHMEN ET AL., "A novel solid-phase synthesis of highly diverse guanidines: reactions of primary amines attached to the T2 linker", Organic Letters, 2000, vol.2(23), pp.3563-3565. R.N. HANSON, "Radioiodinated l-carboxamidino-4-phenylpiperazine: A potential adrenal and myocardial imaging radiopharmaceutical", Int. Applic. Radiat. Isotopes, 1982, vol.33, pp.629-632. OZAWA HIKARU, "Pharmacological properties of geterocyclic amidine derivatives. II. Pharmacological studies of phenylguanylpiperazine derivatives", Chem. Pharm. Bull, 1968, vol.16(12), pp.2482-2487. *
M. HORBERG ЕТ AL., "Bioisosteric modification of PETT-HIV1 RT-inhibitors: Synthesis and biological evaluation", Bioorganic&Medicinal Chemistry Letters, 2000, vol.10, pp.265-268. *
OZAWA HIKARU, "Pharmacological properties of geterocyclic amidine derivatives. II. Pharmacological studies of phenylguanylpiperazine derivatives", Chem. Pharm. Bull, 1968, vol.16(12), pp.2482-2487. *
R.N. HANSON, "Radioiodinated l-carboxamidino-4-phenylpiperazine: A potential adrenal and myocardial imaging radiopharmaceutical", Int. Applic. Radiat. Isotopes, 1982, vol.33, pp.629-632. *
S. DAHMEN ET AL., "A novel solid-phase synthesis of highly diverse guanidines: reactions of primary amines attached to the T2 linker", Organic Letters, 2000, vol.2(23), pp.3563-3565. *

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