PE20140146A1 - Derivados de pirrolopiridina y pirrolopirimidina sustituidos con ciclobutilo como inhibidores de jak - Google Patents
Derivados de pirrolopiridina y pirrolopirimidina sustituidos con ciclobutilo como inhibidores de jakInfo
- Publication number
- PE20140146A1 PE20140146A1 PE2013001220A PE2013001220A PE20140146A1 PE 20140146 A1 PE20140146 A1 PE 20140146A1 PE 2013001220 A PE2013001220 A PE 2013001220A PE 2013001220 A PE2013001220 A PE 2013001220A PE 20140146 A1 PE20140146 A1 PE 20140146A1
- Authority
- PE
- Peru
- Prior art keywords
- cyclobutyl
- alkyl
- pyrrolopyrimidine
- substituted
- cyanomethyl
- Prior art date
Links
- -1 CYCLOBUTYL Chemical group 0.000 title abstract 5
- 150000004944 pyrrolopyrimidines Chemical group 0.000 title abstract 2
- 229940122245 Janus kinase inhibitor Drugs 0.000 title 1
- 150000005255 pyrrolopyridines Chemical group 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- 102000015617 Janus Kinases Human genes 0.000 abstract 2
- 108010024121 Janus Kinases Proteins 0.000 abstract 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-M hydroxide Chemical class [OH-] XLYOFNOQVPJJNP-UHFFFAOYSA-M 0.000 abstract 2
- WCYWZMWISLQXQU-UHFFFAOYSA-N methyl Chemical class [CH3] WCYWZMWISLQXQU-UHFFFAOYSA-N 0.000 abstract 2
- XWIYUCRMWCHYJR-UHFFFAOYSA-N 1h-pyrrolo[3,2-b]pyridine Chemical group C1=CC=C2NC=CC2=N1 XWIYUCRMWCHYJR-UHFFFAOYSA-N 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 201000006417 multiple sclerosis Diseases 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 206010039073 rheumatoid arthritis Diseases 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 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
- A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
- A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
- A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
- A01N43/90—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having two or more relevant hetero rings, condensed among themselves or with a common carbocyclic ring system
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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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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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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- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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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
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- A61P17/06—Antipsoriatics
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- A—HUMAN NECESSITIES
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- A61P17/08—Antiseborrheics
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- A—HUMAN NECESSITIES
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- A61P19/00—Drugs for skeletal disorders
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- A—HUMAN NECESSITIES
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- A61P19/00—Drugs for skeletal disorders
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
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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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- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
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- 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
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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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- A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
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- A—HUMAN NECESSITIES
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- A61P27/04—Artificial tears; Irrigation solutions
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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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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A—HUMAN NECESSITIES
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- 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
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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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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- 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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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—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
- 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
- C07D491/10—Spiro-condensed systems
- C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Physical Education & Sports Medicine (AREA)
- Immunology (AREA)
- Rheumatology (AREA)
- Diabetes (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Dermatology (AREA)
- Hematology (AREA)
- Endocrinology (AREA)
- Oncology (AREA)
- Pain & Pain Management (AREA)
- Epidemiology (AREA)
- Urology & Nephrology (AREA)
- Biomedical Technology (AREA)
- Obesity (AREA)
- Neurology (AREA)
- Dentistry (AREA)
- Environmental Sciences (AREA)
- Ophthalmology & Optometry (AREA)
- Pest Control & Pesticides (AREA)
- Wood Science & Technology (AREA)
- Zoology (AREA)
- Plant Pathology (AREA)
- Agronomy & Crop Science (AREA)
- Heart & Thoracic Surgery (AREA)
- Neurosurgery (AREA)
Abstract
SE REFIERE A COMPUESTOS DERIVADOS DE PIRROLOPIRIDINA Y PIRROLOPIRIMIDINA SUSTITUIDOS CON CICLOBUTILO DE FORMULA (I) DONDE X Y W SON CADA UNO CH O N; Y ES H, CN, ALQUILO(C1-C3), ENTRE OTROS; L ES O, S, C(=O), C(=O)O, ENTRE OTROS; Z ES CR4 O N; R1, R2, R3 Y R4 SON CADA UNO H, HIDROXI, HALO, ALQUILO(C1-C3), ENTRE OTROS; R5 ES HIDROXI, ALCOXI(C1-C4), F, ALQUILO(C1-C4), ENTRE OTROS; A ES H, ALQUILO(C1-C6), CICLOALQUILO(C3-C10), ARILO(C6-C10), ENTRE OTROS; m ES DE 0 A 2; n ES DE 0 A 4. SON COMPUESTOS PREFERIDOS: 3-[(4-{3-(CIANOMETIL)-3-[4-(7H-PIRROLO[2,3-d]PIRIMIDIN-4-IL)-1H-PIRAZOL-1-IL]CICLOBUTIL}PIPERAZIN-1-IL)METIL]-5-FLUOROBENZONITRILO; 3-[(4-{3-(CIANOMETIL)-3-[4-(7H-PIRROLO[2,3-d]PIRIMIDIN-4-IL)-1H-PIRAZOL-1-IL]CICLOBUTIL}PIPERAZIN-1-IL)METIL]-6-(DIMETILAMINO)-2-FLUOROBENZONITRILO; 4-{3-(CIANOMETIL)-3-[4-(7H-PIRROLO[2,3-d]PIRIMIDIN-4-IL)-1H-PIRAZOL-1-IL]CICLOBUTIL}-N-[4-FLUORO-2-(TRIFLUOROMETIL)FENIL]PIPERAZIN-1-CARBOXAMIDA; ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE JANUS QUINASAS (JAK) SIENDO UTILES EN EL TRATAMIENTO DE ESCLEROSIS MULTIPLE, ARTRITIS REUMATOIDE, CANCER, MIELOFIBROSIS
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US41570510P | 2010-11-19 | 2010-11-19 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20140146A1 true PE20140146A1 (es) | 2014-02-06 |
Family
ID=45094278
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2013001220A PE20140146A1 (es) | 2010-11-19 | 2011-11-18 | Derivados de pirrolopiridina y pirrolopirimidina sustituidos con ciclobutilo como inhibidores de jak |
Country Status (23)
| Country | Link |
|---|---|
| US (3) | US8933085B2 (es) |
| EP (1) | EP2640723A1 (es) |
| JP (1) | JP5917545B2 (es) |
| KR (1) | KR20140019300A (es) |
| CN (1) | CN103415515B (es) |
| AR (1) | AR083933A1 (es) |
| AU (1) | AU2011329734B2 (es) |
| BR (1) | BR112013012502A2 (es) |
| CA (1) | CA2818542A1 (es) |
| CL (1) | CL2013001412A1 (es) |
| CO (1) | CO6761386A2 (es) |
| CR (1) | CR20130280A (es) |
| EA (1) | EA026201B1 (es) |
| EC (1) | ECSP13012703A (es) |
| IL (1) | IL226407A (es) |
| MX (1) | MX344478B (es) |
| NZ (1) | NZ611151A (es) |
| PE (1) | PE20140146A1 (es) |
| PH (1) | PH12013501001A1 (es) |
| SG (1) | SG190839A1 (es) |
| TW (1) | TW201249845A (es) |
| UA (1) | UA113156C2 (es) |
| WO (1) | WO2012068450A1 (es) |
Families Citing this family (116)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3838903B1 (en) | 2005-12-13 | 2023-11-22 | Incyte Holdings Corporation | Pyrrolo[2,3-d]pyrimidine derivative as janus kinase inhibitor |
| CN101932582B (zh) | 2007-06-13 | 2013-09-25 | 因塞特公司 | 詹纳斯激酶抑制剂(R)-3-(4-(7H-吡咯并[2,3-d]嘧啶-4-基)-1H-吡唑-1-基)-3-环戊基丙腈的盐 |
| CL2008001709A1 (es) | 2007-06-13 | 2008-11-03 | Incyte Corp | Compuestos derivados de pirrolo [2,3-b]pirimidina, moduladores de quinasas jak; composicion farmaceutica; y uso en el tratamiento de enfermedades tales como cancer, psoriasis, artritis reumatoide, entre otras. |
| JOP20190230A1 (ar) | 2009-01-15 | 2017-06-16 | Incyte Corp | طرق لاصلاح مثبطات انزيم jak و المركبات الوسيطة المتعلقة به |
| US8716303B2 (en) * | 2009-05-22 | 2014-05-06 | Incyte Corporation | N-(hetero)aryl-pyrrolidine derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines and pyrrol-3-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors |
| RS59632B1 (sr) | 2009-05-22 | 2020-01-31 | Incyte Holdings Corp | 3-[4-(7h-pirolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il]oktan- ili heptan-nitril kao jak inhibitori |
| CN104945420A (zh) | 2009-06-29 | 2015-09-30 | 因塞特公司 | 作为pi3k抑制剂的嘧啶酮类 |
| TW201113285A (en) | 2009-09-01 | 2011-04-16 | Incyte Corp | Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors |
| ME02386B (me) | 2010-03-10 | 2016-09-20 | Incyte Holdings Corp | Derivati piperidin-4-il azetidina kao inhibitori jak1 |
| NZ603686A (en) | 2010-05-21 | 2014-11-28 | Incyte Corp | Topical formulation for a jak inhibitor |
| TW201249845A (en) | 2010-11-19 | 2012-12-16 | Incyte Corp | Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors |
| JP5917544B2 (ja) * | 2010-11-19 | 2016-05-18 | インサイト・ホールディングス・コーポレイションIncyte Holdings Corporation | Jak阻害剤としての複素環置換ピロロピリジンおよびピロロピリミジン |
| CA2822070C (en) | 2010-12-20 | 2019-09-17 | Incyte Corporation | N-(1-(substituted-phenyl)ethyl)-9h-purin-6-amines as pi3k inhibitors |
| MX357939B (es) | 2011-02-18 | 2018-07-31 | Novartis Pharma Ag | Terapia de combinacion de inhibidor de objetivo de rapamicina en mamifero/janus cinasa (mtor/jak). |
| KR20140040819A (ko) | 2011-06-20 | 2014-04-03 | 인사이트 코포레이션 | Jak 저해제로서의 아제티디닐 페닐, 피리딜 또는 피라지닐 카르복스아미드 유도체 |
| CA2844507A1 (en) | 2011-08-10 | 2013-02-14 | Novartis Pharma Ag | Jak pi3k/mtor combination therapy |
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| US20150087632A1 (en) | 2015-03-26 |
| CN103415515B (zh) | 2015-08-26 |
| PH12013501001A1 (en) | 2019-09-02 |
| US8933085B2 (en) | 2015-01-13 |
| IL226407A0 (en) | 2013-07-31 |
| US10640506B2 (en) | 2020-05-05 |
| US20190135813A1 (en) | 2019-05-09 |
| BR112013012502A2 (pt) | 2019-03-06 |
| WO2012068450A1 (en) | 2012-05-24 |
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| CR20130280A (es) | 2013-08-09 |
| NZ611151A (en) | 2015-06-26 |
| AU2011329734A1 (en) | 2013-05-02 |
| AR083933A1 (es) | 2013-04-10 |
| MX344478B (es) | 2016-12-16 |
| KR20140019300A (ko) | 2014-02-14 |
| UA113156C2 (xx) | 2016-12-26 |
| JP5917545B2 (ja) | 2016-05-18 |
| EP2640723A1 (en) | 2013-09-25 |
| ECSP13012703A (es) | 2013-08-30 |
| US20120149681A1 (en) | 2012-06-14 |
| JP2014500260A (ja) | 2014-01-09 |
| CA2818542A1 (en) | 2012-05-24 |
| CN103415515A (zh) | 2013-11-27 |
| EA201390736A1 (ru) | 2013-11-29 |
| SG190839A1 (en) | 2013-07-31 |
| TW201249845A (en) | 2012-12-16 |
| EA026201B1 (ru) | 2017-03-31 |
| CO6761386A2 (es) | 2013-09-30 |
| MX2013005603A (es) | 2013-06-13 |
| AU2011329734B2 (en) | 2015-05-28 |
| IL226407A (en) | 2017-04-30 |
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