EA201170130A1 - Бензоксазины, бензотиазины и родственные соединения, обладающие ингибирующей nos активностью - Google Patents
Бензоксазины, бензотиазины и родственные соединения, обладающие ингибирующей nos активностьюInfo
- Publication number
- EA201170130A1 EA201170130A1 EA201170130A EA201170130A EA201170130A1 EA 201170130 A1 EA201170130 A1 EA 201170130A1 EA 201170130 A EA201170130 A EA 201170130A EA 201170130 A EA201170130 A EA 201170130A EA 201170130 A1 EA201170130 A1 EA 201170130A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- nhc
- optionally substituted
- alkyl
- alkoxy
- benzothiazines
- Prior art date
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
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- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/538—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
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- 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
- A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/5415—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
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- 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
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- 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
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- 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
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
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- 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
- A61P25/04—Centrally acting analgesics, e.g. opioids
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- 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
- A61P25/06—Antimigraine agents
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- 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
- A61P25/08—Antiepileptics; Anticonvulsants
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- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
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- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
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- 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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- 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
- A61P25/22—Anxiolytics
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- 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
- A61P25/24—Antidepressants
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- 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
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- 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
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
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- 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]
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- 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
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- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Heart & Thoracic Surgery (AREA)
- Rheumatology (AREA)
- Addiction (AREA)
- Cardiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Описаны бензоксазины и бензотиазины формулы (I), в которой Q представляет собой О-(CHR)или S-(CHR); Rи каждый Rпредставляют собой Н, необязательно замещенный [Cалкил, Салкарил, Салкгетероциклил, Cгетероциклил, Сциклоалкил, Салкциклоалкил] или -(CRR)NRR, где R, R, R, Rпредставляют собой независимо водород, необязательно замещенный [Cалкил, Cалкарил, Салкгетероциклил, Сгетероциклил, Сциклоалкил и т.д.] или где Rи Rобъединяются с образованием =O, или где Rи Rобъединяются с образованием необязательно замещенного Сгетероциклила и n равно целому числу 1-6; каждый из Rи Rпредставляет собой Н, галоген, необязательно замещенный [C-алкил, Сарил, Cалкарил, Сгетероциклил, Cалкокси, Cтиоалкокси, (СН)NHC(NH)R, (СН)NHC(S)NHR, C-алкгетероциклил] или гидрокси, где r2 равно целому числу от 0 до 2, Rпредставляет собой необязательно замещенный [Cалкил, Сарил, Салкарил, Сгетероциклил, Салкгетероциклил, Cтиоалкокси, Стиоалкарил, арилоил, Стиоалкгетероциклил или амино]; каждый из Rи Rпредставляет собой Н, галоген, (CH)NHC(NH)Rили (CH)NHC(S)NHR; Yи Yвместе обозначают =O, или Yи Yпредставляют собой независимо Н, необязательно замещенный [Cалкил, Сарил, Cалкарил, Сгетероциклил, Cалкокси, Cтиоалкокси, Салкгетероциклил] или гидрокси; где только один из R, R, Rи Rпредставляет собой (CH)NHC(NH)Rили (CH)NHC(S)NHR; или их фармацевтически приемлемые соли или пролекарства. Указанные бензоксазины и бензотиазины формулы (I) ингибируют (оксид азота)-синтазу (NOS), особенно селективно ингибируют нейронную (оксид азота)-синтазу (nNOS), предпочтительно относительно других изоформ NOS. Ингибиторы NOS формулы (I), отдельно или в комбинации с другими фармацевтически активными агентами, можно применять для лечения или предупреждения различных патологических состояний.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US13388708P | 2008-07-03 | 2008-07-03 | |
PCT/CA2009/000923 WO2010000073A1 (en) | 2008-07-03 | 2009-07-03 | Benzoxazines, benzothiazines, and related compounds having nos inhibitory activity |
Publications (2)
Publication Number | Publication Date |
---|---|
EA201170130A1 true EA201170130A1 (ru) | 2011-08-30 |
EA021798B1 EA021798B1 (ru) | 2015-09-30 |
Family
ID=41465440
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA201170130A EA021798B1 (ru) | 2008-07-03 | 2009-07-03 | Бензоксазины, бензотиазины и родственные соединения, обладающие ингибирующей nos активностью |
Country Status (20)
Country | Link |
---|---|
US (3) | US8106043B2 (ru) |
EP (1) | EP2310386A4 (ru) |
JP (1) | JP5572157B2 (ru) |
KR (1) | KR20110036607A (ru) |
CN (1) | CN102143961B (ru) |
AR (1) | AR072471A1 (ru) |
AU (1) | AU2009266386B2 (ru) |
BR (1) | BRPI0913915A2 (ru) |
CA (1) | CA2729246C (ru) |
CL (1) | CL2010001633A1 (ru) |
EA (1) | EA021798B1 (ru) |
IL (1) | IL210195A (ru) |
MX (1) | MX2011000124A (ru) |
MY (1) | MY158796A (ru) |
NZ (1) | NZ590727A (ru) |
SG (1) | SG192470A1 (ru) |
TW (1) | TWI458726B (ru) |
UA (1) | UA105182C2 (ru) |
WO (1) | WO2010000073A1 (ru) |
ZA (1) | ZA201100436B (ru) |
Families Citing this family (119)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2011009020A2 (en) | 2009-07-16 | 2011-01-20 | Mallinckrodt Inc. | Compounds and compositions for use in phototherapy and in treatment of ocular neovascular disease and cancers |
CN101830894B (zh) * | 2010-06-01 | 2013-05-29 | 上海交通大学 | 一类苯并[d]噁唑化合物及其制备方法 |
WO2013076590A1 (en) * | 2011-11-23 | 2013-05-30 | Oxygen Healthcare Research Pvt. Ltd | Benzothiazine compounds as h3 receptor ligands |
CN102491919B (zh) * | 2011-12-15 | 2014-03-19 | 南京友杰医药科技有限公司 | 去甲维拉帕米的合成方法 |
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EP1117662A1 (en) | 1998-09-30 | 2001-07-25 | Merck Sharp & Dohme Limited | Benzimidazolinyl piperidines as cgrp ligands |
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DE19952147A1 (de) | 1999-10-29 | 2001-05-03 | Boehringer Ingelheim Pharma | Neue Cyclopropane, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung |
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KR20130136010A (ko) * | 2005-04-13 | 2013-12-11 | 네우렉슨 인코포레이티드 | Nos 저해 활성을 갖는 치환된 인돌 화합물 |
US7919510B2 (en) * | 2005-05-18 | 2011-04-05 | Neuraxon, Inc | Substituted benzimidazole compounds with dual NOS inhibitory activity and mu opioid agonist activity |
PE20070519A1 (es) * | 2005-08-25 | 2007-07-13 | Schering Corp | Derivados de fenilmorfolina y feniltiomorfolina como agonistas de adrenoreceptores alfa 2c |
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JP5350219B2 (ja) * | 2006-04-13 | 2013-11-27 | ニューラクソン,インコーポレーテッド | Nos阻害活性を有する1,5および3,6−置換インドール化合物 |
US20090131503A1 (en) | 2007-11-16 | 2009-05-21 | Annedi Subhash C | 3,5 - substituted indole compounds having nos and norepinephrine reuptake inhibitory activity |
-
2009
- 2009-03-07 UA UAA201101136A patent/UA105182C2/ru unknown
- 2009-07-03 EP EP09771883A patent/EP2310386A4/en not_active Withdrawn
- 2009-07-03 AU AU2009266386A patent/AU2009266386B2/en not_active Ceased
- 2009-07-03 JP JP2011515041A patent/JP5572157B2/ja not_active Expired - Fee Related
- 2009-07-03 CA CA2729246A patent/CA2729246C/en not_active Expired - Fee Related
- 2009-07-03 SG SG2013051644A patent/SG192470A1/en unknown
- 2009-07-03 CN CN200980134295.9A patent/CN102143961B/zh not_active Expired - Fee Related
- 2009-07-03 WO PCT/CA2009/000923 patent/WO2010000073A1/en active Application Filing
- 2009-07-03 NZ NZ590727A patent/NZ590727A/xx not_active IP Right Cessation
- 2009-07-03 MY MYPI2010006341A patent/MY158796A/en unknown
- 2009-07-03 MX MX2011000124A patent/MX2011000124A/es active IP Right Grant
- 2009-07-03 TW TW098122515A patent/TWI458726B/zh not_active IP Right Cessation
- 2009-07-03 AR ARP090102506A patent/AR072471A1/es unknown
- 2009-07-03 KR KR1020117002783A patent/KR20110036607A/ko not_active Application Discontinuation
- 2009-07-03 EA EA201170130A patent/EA021798B1/ru not_active IP Right Cessation
- 2009-07-03 BR BRPI0913915A patent/BRPI0913915A2/pt not_active IP Right Cessation
- 2009-07-06 US US12/498,185 patent/US8106043B2/en not_active Expired - Fee Related
-
2010
- 2010-12-23 IL IL210195A patent/IL210195A/en not_active IP Right Cessation
- 2010-12-30 CL CL2010001633A patent/CL2010001633A1/es unknown
-
2011
- 2011-01-17 ZA ZA2011/00436A patent/ZA201100436B/en unknown
-
2012
- 2012-01-27 US US13/360,029 patent/US8618286B2/en not_active Expired - Fee Related
-
2013
- 2013-12-11 US US14/103,446 patent/US20140163016A1/en not_active Abandoned
Also Published As
Publication number | Publication date |
---|---|
TW201002701A (en) | 2010-01-16 |
KR20110036607A (ko) | 2011-04-07 |
EP2310386A4 (en) | 2012-04-11 |
JP5572157B2 (ja) | 2014-08-13 |
WO2010000073A1 (en) | 2010-01-07 |
AR072471A1 (es) | 2010-09-01 |
BRPI0913915A2 (pt) | 2015-10-13 |
AU2009266386B2 (en) | 2015-02-19 |
TWI458726B (zh) | 2014-11-01 |
CA2729246C (en) | 2018-08-21 |
JP2011526251A (ja) | 2011-10-06 |
US8618286B2 (en) | 2013-12-31 |
CL2010001633A1 (es) | 2011-05-20 |
SG192470A1 (en) | 2013-08-30 |
IL210195A (en) | 2015-08-31 |
NZ590727A (en) | 2012-12-21 |
US20140163016A1 (en) | 2014-06-12 |
ZA201100436B (en) | 2012-10-31 |
US20120122855A1 (en) | 2012-05-17 |
CN102143961B (zh) | 2014-11-05 |
CN102143961A (zh) | 2011-08-03 |
US8106043B2 (en) | 2012-01-31 |
CA2729246A1 (en) | 2010-01-07 |
AU2009266386A1 (en) | 2010-01-07 |
MY158796A (en) | 2016-11-15 |
EA021798B1 (ru) | 2015-09-30 |
UA105182C2 (ru) | 2014-04-25 |
EP2310386A1 (en) | 2011-04-20 |
MX2011000124A (es) | 2011-02-24 |
US20100009975A1 (en) | 2010-01-14 |
IL210195A0 (en) | 2011-03-31 |
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