EA201300908A1 - ПРОИЗВОДНЫЕ 6-ЦИКЛОБУТИЛ-1,5-ДИГИДРОПИРАЗОЛО[3,4d]ПИРИМИДИН-4-ОНА И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ИНГИБИТОРОВ PDE9A - Google Patents
ПРОИЗВОДНЫЕ 6-ЦИКЛОБУТИЛ-1,5-ДИГИДРОПИРАЗОЛО[3,4d]ПИРИМИДИН-4-ОНА И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ИНГИБИТОРОВ PDE9AInfo
- Publication number
- EA201300908A1 EA201300908A1 EA201300908A EA201300908A EA201300908A1 EA 201300908 A1 EA201300908 A1 EA 201300908A1 EA 201300908 A EA201300908 A EA 201300908A EA 201300908 A EA201300908 A EA 201300908A EA 201300908 A1 EA201300908 A1 EA 201300908A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- drugs
- application
- dihydropyrazolo
- pyrimidin
- cyclobutyl
- Prior art date
Links
- 229940122229 Phosphodiesterase 9A inhibitor Drugs 0.000 title 1
- 239000003814 drug Substances 0.000 abstract 4
- 229940079593 drug Drugs 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 3
- 201000010099 disease Diseases 0.000 abstract 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 3
- 230000001575 pathological effect Effects 0.000 abstract 2
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 abstract 1
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 abstract 1
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 abstract 1
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 208000028698 Cognitive impairment Diseases 0.000 abstract 1
- 101100407341 Drosophila melanogaster Pde9 gene Proteins 0.000 abstract 1
- 208000010877 cognitive disease Diseases 0.000 abstract 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 abstract 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 abstract 1
- 230000008447 perception Effects 0.000 abstract 1
- DOTPSQVYOBAWPQ-UHFFFAOYSA-N pyrazolo[4,3-d]pyrimidin-3-one Chemical class N1=CN=C2C(=O)N=NC2=C1 DOTPSQVYOBAWPQ-UHFFFAOYSA-N 0.000 abstract 1
- 125000004076 pyridyl group Chemical group 0.000 abstract 1
- 125000000714 pyrimidinyl group Chemical group 0.000 abstract 1
- 201000000980 schizophrenia Diseases 0.000 abstract 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 abstract 1
- 125000001412 tetrahydropyranyl group Chemical group 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- 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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- 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
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
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- A—HUMAN NECESSITIES
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- A61P25/08—Antiepileptics; Anticonvulsants
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- 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
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- A61P25/16—Anti-Parkinson drugs
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- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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- A61P25/20—Hypnotics; Sedatives
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- A—HUMAN NECESSITIES
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- A61P25/00—Drugs for disorders of the nervous system
- A61P25/22—Anxiolytics
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- A—HUMAN NECESSITIES
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- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- 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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- A61P3/00—Drugs for disorders of the metabolism
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- A61P3/06—Antihyperlipidemics
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
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- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
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- 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
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- A—HUMAN NECESSITIES
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Diabetes (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Reproductive Health (AREA)
- Physical Education & Sports Medicine (AREA)
- Psychology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Hospice & Palliative Care (AREA)
- Child & Adolescent Psychology (AREA)
- Cardiology (AREA)
- Emergency Medicine (AREA)
- Anesthesiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Gynecology & Obstetrics (AREA)
- Pregnancy & Childbirth (AREA)
- Pulmonology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
В заявке описаны новые пиразолопиримидиноны формулы (I)в которой Rобозначает пиридильную или пиримидинильную группу и D обозначает необязательно замещенный циклопентил, циклогексил, тетрагидрофуранил, тетрагидропиранил или 2-, 3- или 4-пиридил. Эти новые соединения предназначены для применения в качестве активного компонента лекарственных средств или для приготовления лекарственных средств соответственно, предпочтительно лекарственных средств, предназначенных для лечения патологических состояний, связанных с недостаточностью восприятия, сосредоточенности, способности к обучению или памяти. Такие патологические состояния могут быть связаны, например, с болезнью Альцгеймера, шизофренией и другими заболеваниями. Эти новые соединения также применимы, например, для приготовления лекарственных средств и/или для применения для лечения этих заболеваний, в частности нарушения познавательной способности, связанного с таким заболеванием. Описанные в заявке соединения обладают способностью ингибировать PDE9.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP11154397 | 2011-02-14 | ||
PCT/EP2011/063705 WO2012020022A1 (en) | 2010-08-12 | 2011-08-09 | 6-cycloalkyl-1, 5-dihydro-pyrazolo [3, 4-d] pyrimidin-4-one derivatives and their use as pde9a inhibitors |
PCT/EP2012/052378 WO2012110440A1 (en) | 2011-02-14 | 2012-02-13 | 6 - cyclobutyl - 1, 5 - dihydro - pyrazolo [3, 4-d] pyrimidin- 4 - one derivatives their use as pde9a inhibitors |
Publications (2)
Publication Number | Publication Date |
---|---|
EA201300908A1 true EA201300908A1 (ru) | 2014-01-30 |
EA023574B1 EA023574B1 (ru) | 2016-06-30 |
Family
ID=46671960
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA201300908A EA023574B1 (ru) | 2011-02-14 | 2012-02-13 | ПРОИЗВОДНЫЕ 6-ЦИКЛОБУТИЛ-1,5-ДИГИДРОПИРАЗОЛО[3,4-d]ПИРИМИДИН-4-ОНА И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ИНГИБИТОРОВ PDE9A |
Country Status (22)
Country | Link |
---|---|
US (1) | US20130040971A1 (ru) |
EP (1) | EP2675807B1 (ru) |
JP (1) | JP2014505091A (ru) |
KR (1) | KR20140010036A (ru) |
CN (1) | CN103459397A (ru) |
AP (1) | AP2013007045A0 (ru) |
AR (1) | AR085219A1 (ru) |
AU (1) | AU2012217208A1 (ru) |
BR (1) | BR112013020605A2 (ru) |
CA (1) | CA2827261A1 (ru) |
CL (1) | CL2013002341A1 (ru) |
CO (1) | CO6791616A2 (ru) |
EA (1) | EA023574B1 (ru) |
EC (1) | ECSP13012852A (ru) |
IL (1) | IL227526A0 (ru) |
MA (1) | MA34889B1 (ru) |
MX (1) | MX2013009343A (ru) |
PE (1) | PE20140970A1 (ru) |
SG (1) | SG192756A1 (ru) |
TN (1) | TN2013000324A1 (ru) |
TW (1) | TW201245199A (ru) |
WO (1) | WO2012110440A1 (ru) |
Families Citing this family (21)
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DE10238722A1 (de) | 2002-08-23 | 2004-03-11 | Bayer Ag | Selektive Phosphodiesterase 9A-Inhibitoren als Arzneimittel zur Verbesserung kognitiver Prozesse |
EP2597087B1 (en) | 2005-10-25 | 2016-03-30 | Shionogi&Co., Ltd. | Dihydrooxazine and tetrahydropyrimidine derivatives as BACE 1 inhibitors |
CA2683887A1 (en) | 2007-04-24 | 2008-11-06 | Shionogi & Co., Ltd. | Aminodihydrothiazine derivatives substituted with a cyclic group having inhibitory activity against production of amyloid beta protein |
US8653067B2 (en) | 2007-04-24 | 2014-02-18 | Shionogi & Co., Ltd. | Pharmaceutical composition for treating Alzheimer's disease |
UA105362C2 (en) | 2008-04-02 | 2014-05-12 | Бьорингер Ингельхайм Интернациональ Гмбх | 1-heterocyclyl-1, 5-dihydro-pyrazolo [3, 4-d] pyrimidin-4-one derivatives and their use as pde9a modulators |
AU2009258496B8 (en) | 2008-06-13 | 2014-06-26 | Shionogi & Co., Ltd. | Sulfur-containing heterocyclic derivative having beta-secretase-inhibiting activity |
WO2010047372A1 (ja) | 2008-10-22 | 2010-04-29 | 塩野義製薬株式会社 | Bace1阻害活性を有する2-アミノピリミジン-4-オンおよび2-アミノピリジン誘導体 |
EP2414363B1 (en) * | 2009-03-31 | 2014-01-08 | Boehringer Ingelheim International GmbH | 1-heterocyclyl-1,5-dihydro-pyrazolo[3,4-d]pyrimidin-4-one derivatives and their use as pde9a modulators |
BR112012013854A2 (pt) | 2009-12-11 | 2019-09-24 | Shionogi & Co | derivados de oxazina. |
JP5766198B2 (ja) | 2010-10-29 | 2015-08-19 | 塩野義製薬株式会社 | 縮合アミノジヒドロピリミジン誘導体 |
EP2634186A4 (en) | 2010-10-29 | 2014-03-26 | Shionogi & Co | naphthyridine |
WO2012147763A1 (ja) | 2011-04-26 | 2012-11-01 | 塩野義製薬株式会社 | オキサジン誘導体およびそれを含有するbace1阻害剤 |
JP2016501827A (ja) | 2012-10-24 | 2016-01-21 | 塩野義製薬株式会社 | Bace1阻害作用を有するジヒドロオキサジンまたはオキサゼピン誘導体 |
CN105669680B (zh) * | 2016-03-24 | 2018-02-23 | 南京药捷安康生物科技有限公司 | 吡咯并[2,1‑f][1,2,4]三嗪‑4(1H)‑酮衍生物类PDE9A抑制剂 |
US11147803B2 (en) | 2017-06-01 | 2021-10-19 | Eisai R&D Management Co., Ltd. | Dementia therapeutic agent combining pyrazoloquinoline derivative and memantine |
AU2018278422B2 (en) | 2017-06-01 | 2022-03-17 | Eisai R&D Management Co., Ltd. | Lewy body disease therapeutic agent containing pyrazoloquinoline derivative |
BR112019023557A2 (pt) | 2017-06-01 | 2020-06-02 | Eisai R&D Management Co., Ltd. | Composição farmacêutica compreendendo inibidor de pde9 |
US11833146B2 (en) | 2017-06-01 | 2023-12-05 | Eisai R&D Management Co., Ltd. | Dementia therapeutic agent combining pyrazoloquinoline derivative and donepezil |
MA53841A (fr) * | 2017-06-08 | 2021-09-22 | Merck Sharp & Dohme | Inhibiteurs pde9 de pyrazolopyrimidine |
US20220017525A1 (en) * | 2018-12-12 | 2022-01-20 | Merck Sharp & Dohme Corp. | Cyclobutyl pyrazolopyrimidine pde9 inhibitors |
CN110339197A (zh) * | 2019-06-24 | 2019-10-18 | 中山大学 | 一种防治血管性痴呆的磷酸二酯酶9a抑制剂的用途 |
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JP2006525966A (ja) * | 2003-05-09 | 2006-11-16 | バイエル・ヘルスケア・アクチェンゲゼルシャフト | 6−シクリルメチル−および6−アルキルメチル置換ピラゾロピリミジン類 |
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2012
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- 2012-02-13 KR KR1020137021400A patent/KR20140010036A/ko not_active Application Discontinuation
- 2012-02-13 AR ARP120100472A patent/AR085219A1/es unknown
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- 2012-02-13 BR BR112013020605A patent/BR112013020605A2/pt not_active IP Right Cessation
- 2012-02-13 EP EP20120705246 patent/EP2675807B1/en active Active
- 2012-02-13 CN CN2012800177072A patent/CN103459397A/zh active Pending
- 2012-02-13 MX MX2013009343A patent/MX2013009343A/es active IP Right Grant
- 2012-02-13 WO PCT/EP2012/052378 patent/WO2012110440A1/en active Application Filing
- 2012-02-13 CA CA2827261A patent/CA2827261A1/en not_active Abandoned
- 2012-02-13 TW TW101104596A patent/TW201245199A/zh unknown
- 2012-02-13 PE PE2013001871A patent/PE20140970A1/es not_active Application Discontinuation
- 2012-02-13 SG SG2013061494A patent/SG192756A1/en unknown
- 2012-02-13 AU AU2012217208A patent/AU2012217208A1/en not_active Abandoned
- 2012-02-13 MA MA36160A patent/MA34889B1/fr unknown
- 2012-02-13 JP JP2013552980A patent/JP2014505091A/ja active Pending
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2013
- 2013-07-18 IL IL227526A patent/IL227526A0/en unknown
- 2013-07-29 TN TNP2013000324A patent/TN2013000324A1/fr unknown
- 2013-08-12 CL CL2013002341A patent/CL2013002341A1/es unknown
- 2013-08-26 EC ECSP13012852 patent/ECSP13012852A/es unknown
- 2013-09-12 CO CO13216891A patent/CO6791616A2/es not_active Application Discontinuation
Also Published As
Publication number | Publication date |
---|---|
EA023574B1 (ru) | 2016-06-30 |
CO6791616A2 (es) | 2013-11-14 |
IL227526A0 (en) | 2013-09-30 |
SG192756A1 (en) | 2013-09-30 |
EP2675807B1 (en) | 2015-04-22 |
AU2012217208A1 (en) | 2013-08-01 |
JP2014505091A (ja) | 2014-02-27 |
ECSP13012852A (es) | 2014-09-30 |
PE20140970A1 (es) | 2014-08-03 |
WO2012110440A1 (en) | 2012-08-23 |
BR112013020605A2 (pt) | 2016-10-18 |
WO2012110440A9 (en) | 2013-03-14 |
MA34889B1 (fr) | 2014-02-01 |
CA2827261A1 (en) | 2012-08-23 |
AP2013007045A0 (en) | 2013-08-31 |
CN103459397A (zh) | 2013-12-18 |
MX2013009343A (es) | 2013-10-01 |
CL2013002341A1 (es) | 2014-04-04 |
AR085219A1 (es) | 2013-09-18 |
TN2013000324A1 (en) | 2015-01-20 |
US20130040971A1 (en) | 2013-02-14 |
EP2675807A1 (en) | 2013-12-25 |
KR20140010036A (ko) | 2014-01-23 |
TW201245199A (en) | 2012-11-16 |
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