EA200800175A1 - НОВЫЕ ГЕТЕРОЦИКЛИЧЕСКИЕ ИНГИБИТОРЫ NF-κB - Google Patents
НОВЫЕ ГЕТЕРОЦИКЛИЧЕСКИЕ ИНГИБИТОРЫ NF-κBInfo
- Publication number
- EA200800175A1 EA200800175A1 EA200800175A EA200800175A EA200800175A1 EA 200800175 A1 EA200800175 A1 EA 200800175A1 EA 200800175 A EA200800175 A EA 200800175A EA 200800175 A EA200800175 A EA 200800175A EA 200800175 A1 EA200800175 A1 EA 200800175A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- nrr
- aryl
- heterocycloalkyl
- haloalkyl
- hydroxyalkyl
- Prior art date
Links
- 102000003945 NF-kappa B Human genes 0.000 title 1
- 108010057466 NF-kappa B Proteins 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 125000003118 aryl group Chemical group 0.000 abstract 5
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 3
- 125000001188 haloalkyl group Chemical group 0.000 abstract 3
- 229910052736 halogen Inorganic materials 0.000 abstract 3
- 150000002367 halogens Chemical class 0.000 abstract 3
- 125000001072 heteroaryl group Chemical group 0.000 abstract 3
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 3
- 125000002768 hydroxyalkyl group Chemical group 0.000 abstract 3
- 125000003282 alkyl amino group Chemical group 0.000 abstract 2
- 125000005191 hydroxyalkylamino group Chemical group 0.000 abstract 2
- 239000002253 acid Substances 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 150000003973 alkyl amines Chemical class 0.000 abstract 1
- 150000001412 amines Chemical class 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000004438 haloalkoxy group Chemical group 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4535—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
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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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P17/14—Drugs for dermatological disorders for baldness or alopecia
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- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- 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
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
- C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
- C07D263/30—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D263/34—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D263/48—Nitrogen atoms not forming part of a nitro radical
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- C—CHEMISTRY; METALLURGY
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
- C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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- 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
- C07D413/06—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 carbon chain containing only aliphatic carbon atoms
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- 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
- C07D417/06—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 carbon chain containing only aliphatic carbon atoms
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- 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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- 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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- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Public Health (AREA)
- Life Sciences & Earth Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Dermatology (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Immunology (AREA)
- Neurosurgery (AREA)
- Psychology (AREA)
- Pain & Pain Management (AREA)
- Epidemiology (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Urology & Nephrology (AREA)
- Pulmonology (AREA)
- Psychiatry (AREA)
- Heart & Thoracic Surgery (AREA)
- Transplantation (AREA)
- Vascular Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Toxicology (AREA)
- Cardiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Thiazole And Isothizaole Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Настоящее изобретение относится к соединениям общей формулы (III), или их фармацевтически приемлемым солям с кислотой или основанием, или или их фармацевтически приемлемым пролекарствам или стереоизомерам. Формула (III), где Rпредставляет собой Н, -С(O)NRR, галоген, алкил, галогеноалкил, арил, гетероарил, ОН, SH, NROR, NH, амин, алкиламин, алкокси, циклоалкил, гетероциклоалкил, гидроксиалкил или галогеноалкилокси; Rпредставляет собой Н, галоген, алкил, -C(NR)NRR, -(СН)арил, -(CH)NRR, -C(O)NRR, -N=CRR, -NRC(O)R, циклоалкил, гетероциклоалкил, галогеноалкил, гидроксиалкил, гидроксиалкиламино, алкиламино, гетероарил или арил; Rпредставляет собой галоген, алкил,-C(NR)NRR, -(СН)арил, -(CH)NRR, -C(O)NRR, -N=CRR, -NRC(O)R, циклоалкил, гетероциклоалкил, галогеноалкил, гидроксиалкил, гидроксиалкиламино, алкиламино, гетероарил или арил.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PCT/EP2005/008261 WO2006032322A1 (en) | 2004-09-20 | 2005-07-29 | NOVEL HETEROCYCLIC NF-κB INHIBITORS |
| PCT/EP2006/002396 WO2007016979A2 (en) | 2005-07-29 | 2006-03-15 | NOVEL HETEROCYCLIC NF-κB INHIBITORS |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA200800175A1 true EA200800175A1 (ru) | 2008-08-29 |
| EA016300B1 EA016300B1 (ru) | 2012-04-30 |
Family
ID=36570358
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA200800175A EA016300B1 (ru) | 2005-07-29 | 2006-03-15 | НОВЫЕ ГЕТЕРОЦИКЛИЧЕСКИЕ ИНГИБИТОРЫ NF-κB |
Country Status (13)
| Country | Link |
|---|---|
| JP (1) | JP2009502816A (ru) |
| KR (1) | KR20080031038A (ru) |
| CN (1) | CN101233119A (ru) |
| AU (1) | AU2006278998A1 (ru) |
| BR (1) | BRPI0614188A2 (ru) |
| CA (1) | CA2617225A1 (ru) |
| EA (1) | EA016300B1 (ru) |
| IL (1) | IL189112A0 (ru) |
| NO (1) | NO20081056L (ru) |
| NZ (2) | NZ565470A (ru) |
| SG (1) | SG172738A1 (ru) |
| UA (1) | UA97348C2 (ru) |
| WO (1) | WO2007016979A2 (ru) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BRPI0516958A (pt) * | 2004-09-20 | 2008-03-25 | 4Sc Ag | inibidores da nf-capab heterocìclicos |
| JP2009529555A (ja) * | 2006-03-15 | 2009-08-20 | 4エスツェー アクチェンゲゼルシャフト | 新規複素環式NF−κB阻害薬 |
| WO2009037357A1 (en) * | 2007-09-19 | 2009-03-26 | 4Sc Ag | Benzimidazole nf- kappab inhibitors |
| CN102076344B (zh) | 2008-05-28 | 2013-11-13 | 瓦利杜斯生物医药有限公司 | 用于治疗疾病的NF-κB的非激素甾体调节剂 |
| US9447049B2 (en) | 2010-03-01 | 2016-09-20 | University Of Tennessee Research Foundation | Compounds for treatment of cancer |
| US9029408B2 (en) | 2008-06-16 | 2015-05-12 | Gtx, Inc. | Compounds for treatment of cancer |
| US8822513B2 (en) | 2010-03-01 | 2014-09-02 | Gtx, Inc. | Compounds for treatment of cancer |
| ES2927660T3 (es) | 2008-06-16 | 2022-11-10 | Univ Tennessee Res Found | Compuestos para el tratamiento del cáncer |
| JP5879273B2 (ja) | 2010-03-01 | 2016-03-08 | ジーティーエックス・インコーポレイテッド | 癌を処置するための化合物 |
| US10464967B2 (en) | 2011-11-29 | 2019-11-05 | Reveragen Biopharma, Inc. | Non-hormonal steroid modulators of NF-κβ for treatment of disease |
| WO2014202638A1 (en) * | 2013-06-18 | 2014-12-24 | 4Sc Discovery Gmbh | 2,3-dihydrobenzofuran-5-yl compounds as dyrk kinase inhibitors |
| CA2937967C (en) * | 2014-01-29 | 2022-07-26 | Neuropore Therapies, Inc. | Heteroaryl amides as inhibitors of protein aggregation |
| WO2017004205A1 (en) | 2015-06-29 | 2017-01-05 | Reveragen Biopharma, Inc. | NON-HORMONAL STEROID MODULATORS OF NF-κB FOR TREATMENT OF DISEASE |
| US11382922B2 (en) | 2019-03-07 | 2022-07-12 | Reveragen Biopharma, Inc. | Aqueous oral pharmaceutical suspension compositions |
| CN116113406B (zh) * | 2020-07-10 | 2025-08-29 | 密歇根大学董事会 | Gas41抑制剂及其使用方法 |
| WO2024145662A1 (en) * | 2022-12-30 | 2024-07-04 | Altay Therapeutics, Inc. | 2-substituted thiazole and benzothiazole compositions and methods as dux4 inhibitors |
Family Cites Families (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW263508B (ru) * | 1991-02-12 | 1995-11-21 | Pfizer | |
| KR100424933B1 (ko) * | 1995-05-18 | 2004-07-27 | 제리아 신야쿠 고교 가부시키 가이샤 | 아미노티아졸유도체,이를함유하는의약및이화합물의중간체 |
| JPH0987282A (ja) * | 1995-09-21 | 1997-03-31 | Kyowa Hakko Kogyo Co Ltd | チアゾール誘導体 |
| WO1997012613A1 (en) * | 1995-10-05 | 1997-04-10 | Warner-Lambert Company | Method for treating and preventing inflammation and atherosclerosis |
| DE19817459A1 (de) * | 1998-04-20 | 1999-10-21 | Basf Ag | Neue heterozyklische substituierte Amide, Herstellung und Anwendung |
| US6506747B1 (en) * | 1998-06-05 | 2003-01-14 | Boehringer Ingelheim Pharmaceuticals, Inc. | Substituted 1-(4-aminophenyl)pyrazoles and their use as anti-inflammatory agents |
| DE19858593A1 (de) * | 1998-12-18 | 2000-06-21 | Merck Patent Gmbh | Sulfonyloxazolamine als therapeutische Wirkstoffe |
| CA2389685C (fr) * | 1999-11-05 | 2011-07-12 | Societe De Conseils De Recherches Et D'applications Scientifiques (S.C.R) | Nouveaux composes heterocycliques et leur application a titre de medicaments |
| WO2002064558A2 (en) * | 2001-02-14 | 2002-08-22 | Sankyo Company, Limited | Oxazole derivatives, their preparation and their use as cytokine inhibitors |
| CA2461363A1 (en) * | 2001-09-26 | 2003-04-03 | Bayer Pharmaceuticals Corporation | Substituted 3-pyridyl indoles and indazoles as c17,20 lyase inhibitors |
| GB0130868D0 (en) * | 2001-12-24 | 2002-02-06 | Univ Strathclyde | New compounds |
| JP2005525309A (ja) * | 2002-01-10 | 2005-08-25 | ベーリンガー インゲルハイム ファルマ ゲゼルシャフト ミット ベシュレンクテル ハフツング ウント コンパニー コマンディトゲゼルシャフト | 医薬品としての使用のためのMTPインヒビター又はapoB分泌インヒビターとフィブレートの組み合わせ |
| RU2326881C9 (ru) * | 2002-09-30 | 2009-04-10 | Байер Фармасьютикалс Корпорейшн | Конденсированные производные азолпиримидина, обладающие свойствами ингибитора фосфатидилинозитол-3-киназы (pi3k) |
| GB0230162D0 (en) * | 2002-12-24 | 2003-02-05 | Metris Therapeutics Ltd | Compounds useful in inhibiting angiogenesis |
| FR2856685B1 (fr) * | 2003-06-25 | 2005-09-23 | Merck Sante Sas | Derives de thiazolylpiperidine, leurs procedes de preparation et les compositions pharmaceutiques qui les contiennent |
| US20050090529A1 (en) * | 2003-07-31 | 2005-04-28 | Pfizer Inc | 3,5 Disubstituted indazole compounds with nitrogen-bearing 5-membered heterocycles, pharmaceutical compositions, and methods for mediating or inhibiting cell proliferation |
| WO2005030206A1 (en) * | 2003-09-24 | 2005-04-07 | Imclone Systems Incorporated | Aryl-1,3-azole derivatives and methods for inhibiting heparnase activity |
| US20050209284A1 (en) * | 2004-02-12 | 2005-09-22 | Boehringer Ingelheim Pharmaceuticals, Inc. | Tec kinase inhibitors |
| WO2005090319A1 (en) * | 2004-03-19 | 2005-09-29 | Arrow Therapeutics Limited | Process for preparing benzodiazepines |
| BRPI0516958A (pt) * | 2004-09-20 | 2008-03-25 | 4Sc Ag | inibidores da nf-capab heterocìclicos |
-
2006
- 2006-03-15 CA CA002617225A patent/CA2617225A1/en not_active Abandoned
- 2006-03-15 EA EA200800175A patent/EA016300B1/ru not_active IP Right Cessation
- 2006-03-15 JP JP2008523136A patent/JP2009502816A/ja active Pending
- 2006-03-15 SG SG2011047610A patent/SG172738A1/en unknown
- 2006-03-15 NZ NZ565470A patent/NZ565470A/en not_active IP Right Cessation
- 2006-03-15 UA UAA200802635A patent/UA97348C2/ru unknown
- 2006-03-15 BR BRPI0614188-9A patent/BRPI0614188A2/pt not_active IP Right Cessation
- 2006-03-15 KR KR1020087002431A patent/KR20080031038A/ko not_active Ceased
- 2006-03-15 NZ NZ588971A patent/NZ588971A/en not_active IP Right Cessation
- 2006-03-15 WO PCT/EP2006/002396 patent/WO2007016979A2/en not_active Ceased
- 2006-03-15 AU AU2006278998A patent/AU2006278998A1/en not_active Abandoned
- 2006-03-15 CN CNA2006800272993A patent/CN101233119A/zh active Pending
-
2008
- 2008-01-29 IL IL189112A patent/IL189112A0/en unknown
- 2008-02-28 NO NO20081056A patent/NO20081056L/no not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| NZ588971A (en) | 2012-06-29 |
| IL189112A0 (en) | 2008-08-07 |
| AU2006278998A1 (en) | 2007-02-15 |
| UA97348C2 (en) | 2012-02-10 |
| BRPI0614188A2 (pt) | 2011-03-15 |
| CA2617225A1 (en) | 2007-02-15 |
| CN101233119A (zh) | 2008-07-30 |
| SG172738A1 (en) | 2011-07-28 |
| EA016300B1 (ru) | 2012-04-30 |
| NZ565470A (en) | 2010-11-26 |
| WO2007016979A2 (en) | 2007-02-15 |
| KR20080031038A (ko) | 2008-04-07 |
| WO2007016979A3 (en) | 2007-08-02 |
| JP2009502816A (ja) | 2009-01-29 |
| NO20081056L (no) | 2008-02-28 |
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| MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
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