BRPI0717169C1 - análogos de grelina substituìda no n-terminal - Google Patents

análogos de grelina substituìda no n-terminal

Info

Publication number
BRPI0717169C1
BRPI0717169C1 BRC10717169-2A BRPI0717169A BRPI0717169C1 BR PI0717169 C1 BRPI0717169 C1 BR PI0717169C1 BR PI0717169 A BRPI0717169 A BR PI0717169A BR PI0717169 C1 BRPI0717169 C1 BR PI0717169C1
Authority
BR
Brazil
Prior art keywords
analogs
apc
terminal
active
terminal substituted
Prior art date
Application number
BRC10717169-2A
Other languages
English (en)
Inventor
Zheng Xin Dong
Original Assignee
Ipsen Pharma Sas
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Ipsen Pharma Sas filed Critical Ipsen Pharma Sas
Publication of BRPI0717169A2 publication Critical patent/BRPI0717169A2/pt
Publication of BRPI0717169C1 publication Critical patent/BRPI0717169C1/pt

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/575—Hormones
    • C07K14/60—Growth hormone-releasing factor [GH-RF], i.e. somatoliberin
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2/00—Peptides of undefined number of amino acids; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/22—Hormones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/06—Anti-spasmodics, e.g. drugs for colics, esophagic dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/10—Laxatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/12—Antidiarrhoeals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/08—Bronchodilators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/02—Nutrients, e.g. vitamins, minerals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/02—Drugs for disorders of the endocrine system of the hypothalamic hormones, e.g. TRH, GnRH, CRH, GRH, somatostatin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/06—Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/10—Drugs for disorders of the endocrine system of the posterior pituitary hormones, e.g. oxytocin, ADH
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/10—Drugs for disorders of the endocrine system of the posterior pituitary hormones, e.g. oxytocin, ADH
    • A61P5/12—Drugs for disorders of the endocrine system of the posterior pituitary hormones, e.g. oxytocin, ADH for decreasing, blocking or antagonising the activity of the posterior pituitary hormones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/575—Hormones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Zoology (AREA)
  • Molecular Biology (AREA)
  • Pulmonology (AREA)
  • Toxicology (AREA)
  • Neurology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Neurosurgery (AREA)
  • Nutrition Science (AREA)
  • Biomedical Technology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Reproductive Health (AREA)
  • Child & Adolescent Psychology (AREA)
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Abstract

ANáLOGOS DE GRELINA SUBSTITUìDA NO N-TERMINAL. O presente certificado de adição refere-se a análogos de peptidil com atividade de grelina tendo maior estabilidade, os quais são ativos no receptor de GHS de acordo com a fórmula descrita abaixo: (R2)-A1-A2-A3-A4-A5-A6-A7-A8-A9-A10-A11-A12-A13-A14-A15-A1 6-A17-A18-A19-A20-A21-A22-A23-A24-A25-A26-A27-A28-R1 em que as definições de A1 a A28, R1 e R2 são fornecidas no relatório descritivo, com a exceção de que o aminoácido N-terminal precisa ser selecionado a partir do grupo que consiste em Inp, 1-Apc e 4-Apc, os sais farmaceuticamente aceitáveis desse e as composições farmacêuticas que compreendem uma quantidade eficaz do dito composto junto com usos terapêuticos e não terapêuticos desse.
BRC10717169-2A 2006-09-27 2007-09-24 análogos de grelina substituìda no n-terminal BRPI0717169C1 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US84742306P 2006-09-27 2006-09-27
US60/847,423 2006-09-27
PCT/US2007/020595 WO2008039415A2 (en) 2006-09-27 2007-09-24 Analogs of ghrelin substituted at the n-terminal

Publications (2)

Publication Number Publication Date
BRPI0717169A2 BRPI0717169A2 (pt) 2012-10-23
BRPI0717169C1 true BRPI0717169C1 (pt) 2012-12-04

Family

ID=39230783

Family Applications (1)

Application Number Title Priority Date Filing Date
BRC10717169-2A BRPI0717169C1 (pt) 2006-09-27 2007-09-24 análogos de grelina substituìda no n-terminal

Country Status (16)

Country Link
US (1) US8299022B2 (pt)
EP (1) EP2083842B1 (pt)
JP (1) JP5134627B2 (pt)
KR (1) KR101197541B1 (pt)
CN (1) CN101541341B (pt)
AR (1) AR061780A1 (pt)
AU (1) AU2007300526B2 (pt)
BR (1) BRPI0717169C1 (pt)
CA (1) CA2664558C (pt)
ES (1) ES2436419T3 (pt)
IL (1) IL197796A (pt)
MX (1) MX2009003246A (pt)
NZ (1) NZ576470A (pt)
RU (1) RU2459831C2 (pt)
TW (1) TWI370135B (pt)
WO (1) WO2008039415A2 (pt)

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CN105111302A (zh) * 2005-09-28 2015-12-02 益普生制药股份有限公司 生长素释放肽类似物
WO2007041278A2 (en) * 2005-09-29 2007-04-12 Societe De Conseils De Recherches Et D'applications Scientifiques S.A.S. Composition and methods for stimulating gastrointestinal motility
CA2682174C (en) 2007-03-28 2021-04-06 President And Fellows Of Harvard College Stitched polypeptides
US9724381B2 (en) * 2009-05-12 2017-08-08 The Administrators Of The Tulane Educational Fund Methods of inhibiting the ghrelin/growth hormone secretatogue receptor pathway and uses thereof
US9526648B2 (en) 2010-06-13 2016-12-27 Synerz Medical, Inc. Intragastric device for treating obesity
US10420665B2 (en) 2010-06-13 2019-09-24 W. L. Gore & Associates, Inc. Intragastric device for treating obesity
US10010439B2 (en) 2010-06-13 2018-07-03 Synerz Medical, Inc. Intragastric device for treating obesity
US8628554B2 (en) 2010-06-13 2014-01-14 Virender K. Sharma Intragastric device for treating obesity
WO2012021876A2 (en) 2010-08-13 2012-02-16 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
CN108929375A (zh) 2011-10-18 2018-12-04 爱勒让治疗公司 拟肽大环化合物
EP2809339A2 (en) * 2012-02-03 2014-12-10 Zealand Pharma A/S Ghrelin analogues
WO2013119800A1 (en) 2012-02-07 2013-08-15 Massachusetts Institute Of Technology Use of antagonists of ghrelin or ghrelin receptor to prevent or treat stress-sensitive psychiatric illness
WO2013123267A1 (en) 2012-02-15 2013-08-22 Aileron Therapeutics, Inc. Triazole-crosslinked and thioether-crosslinked peptidomimetic macrocycles
ES2817877T3 (es) 2012-02-15 2021-04-08 Aileron Therapeutics Inc Macrociclos peptidomiméticos
WO2014052780A2 (en) 2012-09-27 2014-04-03 Aratana Therapeutics, Inc. Compositions and methods of use of an inappetance-controlling compound
JP6526563B2 (ja) 2012-11-01 2019-06-05 エイルロン セラピューティクス，インコーポレイテッド 二置換アミノ酸ならびにその調製および使用の方法
US9724396B2 (en) 2013-03-15 2017-08-08 Massachusetts Institute Of Technology Use of antagonists of growth hormone or growth hormone receptor to prevent or treat stress-sensitive psychiatric illness
JP6295247B2 (ja) * 2013-03-25 2018-03-14 ゼリア新薬工業株式会社 食後期の胃運動亢進剤
WO2015134567A1 (en) * 2014-03-04 2015-09-11 Rhythm Pharmaceuticals, Inc. Process for the liquid phase synthesis of h-inp-(d)bal-(d)trp-phe-apc-nh2, and pharmaceutically acceptable salts thereof
SG10201902594QA (en) 2014-09-24 2019-04-29 Aileron Therapeutics Inc Peptidomimetic macrocycles and uses thereof
KR20180108916A (ko) 2015-01-28 2018-10-04 아라타나 세라퓨틱스, 인크. 체중-증량 화합물의 장기 사용을 위한 조성물 및 방법
WO2016138099A1 (en) 2015-02-24 2016-09-01 Massachusetts Institute Of Technology Use of ghrelin or functional ghrelin receptor agonists to prevent and treat stress-sensitive psychiatric illness
CA2979847A1 (en) 2015-03-20 2016-09-29 Aileron Therapeutics, Inc. Peptidomimetic macrocycles and uses thereof
US10779980B2 (en) 2016-04-27 2020-09-22 Synerz Medical, Inc. Intragastric device for treating obesity
WO2023161226A1 (en) * 2022-02-22 2023-08-31 Pephexia Therapeutics Aps Ghrelin agonists with improved potency
WO2024003381A1 (en) * 2022-07-01 2024-01-04 Pephexia Therapeutics Aps Hybrid polypeptides acting as dual ghsr and npy5r agonists

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6124263A (en) 1998-11-16 2000-09-26 Asta Medica Ag Treatment of tumors by administration of growth hormone releasing compounds and their antagonists
CN100506844C (zh) * 1999-07-23 2009-07-01 寒川贤治 新的肽
JP2004514651A (ja) * 2000-05-30 2004-05-20 メルク　エンド　カムパニー　インコーポレーテッド グレリン類似体
AU2003235401B2 (en) * 2002-05-21 2008-09-25 Daiichi Sankyo Company, Limited Medicinal compositions containing ghrelin
KR101065471B1 (ko) * 2002-07-23 2011-09-16 입센 파마 에스.에이.에스 그렐린 유사체
TWI331922B (en) * 2002-08-09 2010-10-21 Ipsen Pharma Sas Growth hormone releasing peptides
ES2300686T3 (es) * 2003-10-16 2008-06-16 F. Hoffmann-La Roche Ag Peptidos sw grelina marcados fluorescentemente.
CN105111302A (zh) 2005-09-28 2015-12-02 益普生制药股份有限公司 生长素释放肽类似物
US20100227806A1 (en) * 2006-03-10 2010-09-09 Tulipano Giovanni Use Of A Ghrelin Agonist To Improve Catabolic Effects Of Glucocorticoid Treatment

Also Published As

Publication number Publication date
TW200821328A (en) 2008-05-16
AU2007300526A1 (en) 2008-04-03
CN101541341A (zh) 2009-09-23
RU2009115711A (ru) 2010-11-10
EP2083842A4 (en) 2011-03-16
BRPI0717169A2 (pt) 2012-10-23
WO2008039415A2 (en) 2008-04-03
TWI370135B (en) 2012-08-11
CA2664558C (en) 2016-11-01
EP2083842A2 (en) 2009-08-05
MX2009003246A (es) 2009-07-29
US8299022B2 (en) 2012-10-30
RU2459831C2 (ru) 2012-08-27
US20090275511A1 (en) 2009-11-05
CA2664558A1 (en) 2008-04-03
IL197796A0 (en) 2011-08-01
JP2010504966A (ja) 2010-02-18
JP5134627B2 (ja) 2013-01-30
KR20090075838A (ko) 2009-07-09
IL197796A (en) 2015-09-24
NZ576470A (en) 2012-09-28
EP2083842B1 (en) 2013-08-28
WO2008039415A3 (en) 2008-11-13
AU2007300526B2 (en) 2011-07-21
ES2436419T3 (es) 2014-01-02
KR101197541B1 (ko) 2013-01-02
CN101541341B (zh) 2013-06-05
AR061780A1 (es) 2008-09-24

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