IL216176A - Derivatives (3'-fluoro-4'-hydroxymethyl-5 '- (methylsulfonyl) biphenyl-4-yl) -2-phenylalkyl- (h1-imidazole-4-yl) propane-2-ol and pharmaceuticals containing them - Google Patents

Derivatives (3'-fluoro-4'-hydroxymethyl-5 '- (methylsulfonyl) biphenyl-4-yl) -2-phenylalkyl- (h1-imidazole-4-yl) propane-2-ol and pharmaceuticals containing them

Info

Publication number
IL216176A
IL216176A IL216176A IL21617611A IL216176A IL 216176 A IL216176 A IL 216176A IL 216176 A IL216176 A IL 216176A IL 21617611 A IL21617611 A IL 21617611A IL 216176 A IL216176 A IL 216176A
Authority
IL
Israel
Prior art keywords
phenylalkyl
propan
methylsulfonyl
imidazol
biphenyl
Prior art date
Application number
IL216176A
Other languages
English (en)
Hebrew (he)
Other versions
IL216176A0 (en
Original Assignee
Exelixis Patent Co Llc
Bristol Myers Squibb Co
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=43223342&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=IL216176(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Exelixis Patent Co Llc, Bristol Myers Squibb Co filed Critical Exelixis Patent Co Llc
Publication of IL216176A0 publication Critical patent/IL216176A0/en
Publication of IL216176A publication Critical patent/IL216176A/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/16—Emollients or protectives, e.g. against radiation
    • 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
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P3/04—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
    • A61P3/06—Antihyperlipidemics
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • 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
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • 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
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • 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
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/14—The ring being saturated

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Dermatology (AREA)
  • Emergency Medicine (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Vascular Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Ophthalmology & Optometry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Toxicology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
IL216176A 2009-05-28 2011-11-07 Derivatives (3'-fluoro-4'-hydroxymethyl-5 '- (methylsulfonyl) biphenyl-4-yl) -2-phenylalkyl- (h1-imidazole-4-yl) propane-2-ol and pharmaceuticals containing them IL216176A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US18173609P 2009-05-28 2009-05-28
PCT/US2010/036211 WO2010138598A2 (en) 2009-05-28 2010-05-26 Lxr modulators

Publications (2)

Publication Number Publication Date
IL216176A0 IL216176A0 (en) 2012-01-31
IL216176A true IL216176A (en) 2015-10-29

Family

ID=43223342

Family Applications (1)

Application Number Title Priority Date Filing Date
IL216176A IL216176A (en) 2009-05-28 2011-11-07 Derivatives (3'-fluoro-4'-hydroxymethyl-5 '- (methylsulfonyl) biphenyl-4-yl) -2-phenylalkyl- (h1-imidazole-4-yl) propane-2-ol and pharmaceuticals containing them

Country Status (31)

Country Link
US (4) US8618154B2 (enExample)
EP (1) EP2435410B1 (enExample)
JP (1) JP5625050B2 (enExample)
KR (1) KR101676704B1 (enExample)
CN (1) CN102648184B (enExample)
AR (1) AR078049A1 (enExample)
AU (1) AU2010254082B2 (enExample)
BR (1) BRPI1013259B8 (enExample)
CA (1) CA2761934C (enExample)
CL (1) CL2011002972A1 (enExample)
CO (1) CO6470826A2 (enExample)
CY (1) CY1119407T1 (enExample)
DK (1) DK2435410T3 (enExample)
EA (1) EA019960B1 (enExample)
ES (1) ES2620451T3 (enExample)
HR (1) HRP20170194T1 (enExample)
IL (1) IL216176A (enExample)
LT (1) LT2435410T (enExample)
MX (1) MX2011012559A (enExample)
MY (1) MY153958A (enExample)
NZ (1) NZ596330A (enExample)
PE (1) PE20120797A1 (enExample)
PL (1) PL2435410T3 (enExample)
PT (1) PT2435410T (enExample)
SG (1) SG176247A1 (enExample)
SI (1) SI2435410T1 (enExample)
SM (1) SMT201700253T1 (enExample)
TN (1) TN2011000585A1 (enExample)
TW (1) TWI488844B (enExample)
WO (1) WO2010138598A2 (enExample)
ZA (1) ZA201108181B (enExample)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK2435410T3 (da) * 2009-05-28 2017-04-10 Exelixis Patent Co Llc LXR-modulatorer
AR088728A1 (es) 2011-03-25 2014-07-02 Bristol Myers Squibb Co Moduladores de lxr como prodroga de imidazol
HUE040231T2 (hu) 2012-03-02 2019-02-28 Ralexar Therapeutics Inc Máj X receptor (LXR) modulátorok bõrbetegségek, rendellenességek és állapotok kezelésére
EP3626309B1 (en) 2012-08-13 2023-03-08 The Rockefeller University Lxrbeta agonist for the treatment of cancer
ES2694001T3 (es) 2013-03-15 2018-12-17 Bristol-Myers Squibb Company Moduladores de LXR
WO2014144037A1 (en) * 2013-03-15 2014-09-18 Bristol-Myers Squibb Company Lxr modulators
US9981913B2 (en) 2013-09-04 2018-05-29 Ralexar Therapeutics, Inc. Liver X receptor (LXR) modulators
CN110003108A (zh) 2013-09-04 2019-07-12 瑞雷克萨治疗公司 肝脏x受体（lxr）调节剂
WO2015106164A1 (en) 2014-01-10 2015-07-16 Rgenix, Inc. Lxr agonists and uses thereof
KR101815734B1 (ko) 2015-05-29 2018-01-05 가톨릭대학교 산학협력단 ｍｉＲ－７, ｍｉＲ－１８ａ 또는 ｍｉＲ－１８ｂ를 유효성분으로 포함하는 대사성 질환의 예방 또는 치료용 약학적 조성물
CA3010883A1 (en) 2016-01-11 2017-07-20 The Rockefeller University Methods for the treatment of myeloid derived suppressor cells related disorders
AU2018373028A1 (en) 2017-11-21 2020-04-30 Inspirna, Inc. Polymorphs and uses thereof
EP3999055A1 (en) 2019-07-15 2022-05-25 Novartis AG Methods for treating meibomian gland dysfunction with liver x receptor agonists
CN110305141B (zh) * 2019-07-18 2022-01-11 深圳市三启药物开发有限公司 一种螺(3,3’-异丙基吡咯烷氧化吲哚)类肝x受体调节剂及其制备方法和应用
WO2021119397A1 (en) 2019-12-13 2021-06-17 Rgenix, Inc. Metal salts and uses thereof
CN115656401B (zh) * 2022-11-09 2025-03-28 武汉海特生物创新医药研究有限公司 一种咪唑-4-甲酸乙酯纯度的hplc检测方法

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US4444784A (en) 1980-08-05 1984-04-24 Merck & Co., Inc. Antihypercholesterolemic compounds
DK149080C (da) 1980-06-06 1986-07-28 Sankyo Co Fremgangsmaade til fremstilling af derivater af ml-236b-carboxylsyre
WO1984002131A1 (fr) 1982-11-22 1984-06-07 Sandoz Ag Produits analogues de mevalolactone et leurs derives, leurs procedes de production, compositions pharmaceutiques les contenant ainsi que leur utilisation en tant que produits pharmaceutiques
US5354772A (en) 1982-11-22 1994-10-11 Sandoz Pharm. Corp. Indole analogs of mevalonolactone and derivatives thereof
FI94339C (fi) 1989-07-21 1995-08-25 Warner Lambert Co Menetelmä farmaseuttisesti käyttökelpoisen /R-(R*,R*)/-2-(4-fluorifenyyli)- , -dihydroksi-5-(1-metyylietyyli)-3-fenyyli-4-/(fenyyliamino)karbonyyli/-1H-pyrroli-1-heptaanihapon ja sen farmaseuttisesti hyväksyttävien suolojen valmistamiseksi
US5177080A (en) 1990-12-14 1993-01-05 Bayer Aktiengesellschaft Substituted pyridyl-dihydroxy-heptenoic acid and its salts
WO1993006215A1 (en) 1991-09-17 1993-04-01 The Salk Institute For Biological Studies Receptor of the thyroid/steroid hormone receptor superfamily
PL334840A1 (en) 1997-01-24 2000-03-27 Univ California Application of fxr, pparalpha and lxralpha activators in order to restore the barrier function, to stimulate epithelium differentation and to inhibit proliferation
AU5994199A (en) 1998-09-23 2000-04-10 Alexander Mata De Urquiza Analysis of ligand activated nuclear receptors (in vivo)
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ATE330632T1 (de) 1999-03-26 2006-07-15 Hope City Selektion von fxr-rezeptormodulatoren
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JP5095216B2 (ja) * 2003-11-14 2012-12-12 ローラス セラピューティクス インコーポレーテッド アリールイミダゾールおよびその抗癌剤としての使用
AU2005211809B2 (en) * 2004-02-11 2009-02-12 Irm Llc Compounds and compositions as LXR modulators
CN101248048B (zh) * 2005-06-27 2013-08-28 埃克塞利希斯专利有限责任公司 吡唑基lxr调节剂
MX2008000141A (es) * 2005-06-27 2008-04-07 Exelixis Inc Moduladores de lxr basados en imidazol.
EP2121621B1 (en) 2006-12-08 2014-05-07 Exelixis Patent Company LLC Lxr and fxr modulators
DK2435410T3 (da) * 2009-05-28 2017-04-10 Exelixis Patent Co Llc LXR-modulatorer

Also Published As

Publication number Publication date
ES2620451T3 (es) 2017-06-28
TWI488844B (zh) 2015-06-21
LT2435410T (lt) 2017-04-10
WO2010138598A3 (en) 2011-07-28
DK2435410T3 (da) 2017-04-10
CO6470826A2 (es) 2012-06-29
AU2010254082B2 (en) 2015-01-29
JP2012528180A (ja) 2012-11-12
PE20120797A1 (es) 2012-07-08
EA019960B1 (ru) 2014-07-30
AU2010254082A1 (en) 2011-12-08
CA2761934C (en) 2018-01-09
CL2011002972A1 (es) 2012-08-17
PL2435410T3 (pl) 2017-07-31
WO2010138598A2 (en) 2010-12-02
CY1119407T1 (el) 2018-03-07
JP5625050B2 (ja) 2014-11-12
ZA201108181B (en) 2013-01-30
PT2435410T (pt) 2017-05-03
US20140163081A1 (en) 2014-06-12
MX2011012559A (es) 2012-06-08
KR20120047868A (ko) 2012-05-14
CA2761934A1 (en) 2010-12-02
US20120071534A1 (en) 2012-03-22
SG176247A1 (en) 2012-01-30
TW201109308A (en) 2011-03-16
NZ596330A (en) 2013-07-26
BRPI1013259B8 (pt) 2021-05-25
EA201171488A1 (ru) 2012-07-30
US20160280661A1 (en) 2016-09-29
BRPI1013259B1 (pt) 2021-04-13
SI2435410T1 (sl) 2017-06-30
EP2435410B1 (en) 2017-01-18
US8618154B2 (en) 2013-12-31
HRP20170194T1 (hr) 2017-05-19
EP2435410A2 (en) 2012-04-04
IL216176A0 (en) 2012-01-31
MY153958A (en) 2015-04-30
CN102648184A (zh) 2012-08-22
US20150299136A1 (en) 2015-10-22
TN2011000585A1 (en) 2013-05-24
KR101676704B1 (ko) 2016-11-16
CN102648184B (zh) 2015-09-30
AR078049A1 (es) 2011-10-12
SMT201700253T1 (it) 2017-07-18
BRPI1013259A2 (pt) 2016-04-05

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