DOP2014000135A - Compuestos novedosos de benzopirano, composiciones y usos de los mismos - Google Patents
Compuestos novedosos de benzopirano, composiciones y usos de los mismosInfo
- Publication number
- DOP2014000135A DOP2014000135A DO2014000135A DO2014000135A DOP2014000135A DO P2014000135 A DOP2014000135 A DO P2014000135A DO 2014000135 A DO2014000135 A DO 2014000135A DO 2014000135 A DO2014000135 A DO 2014000135A DO P2014000135 A DOP2014000135 A DO P2014000135A
- Authority
- DO
- Dominican Republic
- Prior art keywords
- compounds
- methyl
- benzopiran
- compositions
- new
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 2
- 239000000203 mixture Substances 0.000 title 1
- KDVXAPCZVZMPMU-XBBWARJSSA-N (2s)-3-(4-hydroxyphenyl)-4-methyl-2-[4-[2-[(3r)-3-methylpyrrolidin-1-yl]ethoxy]phenyl]-2h-chromen-7-ol Chemical compound C1[C@H](C)CCN1CCOC1=CC=C([C@H]2C(=C(C)C3=CC=C(O)C=C3O2)C=2C=CC(O)=CC=2)C=C1 KDVXAPCZVZMPMU-XBBWARJSSA-N 0.000 abstract 3
- 230000001833 anti-estrogenic effect Effects 0.000 abstract 3
- 229940046836 anti-estrogen Drugs 0.000 abstract 2
- 239000000328 estrogen antagonist Substances 0.000 abstract 2
- KDVXAPCZVZMPMU-COBFLCELSA-N 3-(4-hydroxyphenyl)-4-methyl-2-[4-[2-[(3r)-3-methylpyrrolidin-1-yl]ethoxy]phenyl]-2h-chromen-7-ol Chemical compound C1[C@H](C)CCN1CCOC1=CC=C(C2C(=C(C)C3=CC=C(O)C=C3O2)C=2C=CC(O)=CC=2)C=C1 KDVXAPCZVZMPMU-COBFLCELSA-N 0.000 abstract 1
- 241000124008 Mammalia Species 0.000 abstract 1
- 239000000556 agonist Substances 0.000 abstract 1
- 239000005557 antagonist Substances 0.000 abstract 1
- 150000001562 benzopyrans Chemical class 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 102000015694 estrogen receptors Human genes 0.000 abstract 1
- 108010038795 estrogen receptors Proteins 0.000 abstract 1
- 230000001076 estrogenic effect Effects 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/4025—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
-
- 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
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
-
- 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
- A61K31/66—Phosphorus compounds
- A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- 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
-
- 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
- A61P15/02—Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina
-
- 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
- A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
-
- 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
-
- 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
- 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
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/06—Phosphorus compounds without P—C bonds
- C07F9/08—Esters of oxyacids of phosphorus
- C07F9/09—Esters of phosphoric acids
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
- C07F9/65586—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system at least one of the hetero rings does not contain nitrogen as ring hetero atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Endocrinology (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Physical Education & Sports Medicine (AREA)
- Reproductive Health (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pulmonology (AREA)
- Gynecology & Obstetrics (AREA)
- Diabetes (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Se proveen compuestos de benzopirano con fuerte actividad anti-estrogénica y en esencia ninguna actividad estrogénica, que son OP-1038, que es 3-(4-hidroxifenil)-4-metil-2-(4-{2-[(3R)-3-metil-pirrolidin-1-il]etoxi}fenil)-2H-cromen-7-ol, y OP-1074, que es (2S)-3-(4-hidroxifenil)-4-metil-2-(4-{2-[(3R)-3-metilpirrolidin-1-il]etoxi}fenil)-2H-cromen-7-ol. OP-1074 es un anti-estrógeno puro cuando es probado en el modo agonista y un anti-estrógeno completo cuando se prueba en el modo antagonista. Estos compuestos son útiles para la fabricación de medicamentos útiles para el tratamiento o prevención de una variedad de condiciones que son modulados a través del receptor de estrógeno en mamíferos incluyendo humanos.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201161576890P | 2011-12-16 | 2011-12-16 |
Publications (1)
Publication Number | Publication Date |
---|---|
DOP2014000135A true DOP2014000135A (es) | 2014-08-31 |
Family
ID=48613277
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
DO2014000135A DOP2014000135A (es) | 2011-12-16 | 2014-06-16 | Compuestos novedosos de benzopirano, composiciones y usos de los mismos |
Country Status (27)
Country | Link |
---|---|
US (2) | US9018244B2 (es) |
EP (1) | EP2791128A4 (es) |
JP (1) | JP2015505856A (es) |
KR (1) | KR20140103335A (es) |
CN (1) | CN104169266A (es) |
AP (1) | AP2014007657A0 (es) |
AU (1) | AU2012353660A1 (es) |
BR (1) | BR112014014767A2 (es) |
CA (1) | CA2857061A1 (es) |
CL (1) | CL2014001533A1 (es) |
CR (1) | CR20140259A (es) |
CU (1) | CU20140066A7 (es) |
DO (1) | DOP2014000135A (es) |
EA (1) | EA201490897A1 (es) |
EC (1) | ECSP14009619A (es) |
HK (1) | HK1199246A1 (es) |
IL (1) | IL233118A0 (es) |
MA (1) | MA35722B1 (es) |
MD (1) | MD20140054A2 (es) |
MX (1) | MX2014007198A (es) |
NI (1) | NI201400057A (es) |
PE (1) | PE20150099A1 (es) |
PH (1) | PH12014501237A1 (es) |
SG (1) | SG11201402564QA (es) |
TN (1) | TN2014000243A1 (es) |
WO (1) | WO2013090921A1 (es) |
ZA (1) | ZA201404733B (es) |
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BR112014014124A2 (pt) | 2011-12-14 | 2017-08-22 | Seragon Pharmaceutical Inc | Moduladores do receptor de estrogênio fluorados e usos dos mesmos |
WO2014203129A1 (en) | 2013-06-19 | 2014-12-24 | Olema Pharmaceuticals, Inc. | Combinations of benzopyran compounds, compositions and uses thereof |
WO2014203132A1 (en) | 2013-06-19 | 2014-12-24 | Olema Pharmaceuticals, Inc. | Substituted benzopyran compounds, compositions and uses thereof |
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MA39740A (fr) * | 2014-03-13 | 2017-01-18 | Hoffmann La Roche | Méthodes et compositions pour moduler des mutants du récepteur des oestrogènes |
KR20160124909A (ko) * | 2014-03-13 | 2016-10-28 | 에프. 호프만-라 로슈 아게 | 에스트로겐 수용체 조절제를 함유하는 치료 조합물 |
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US10118910B2 (en) | 2015-12-09 | 2018-11-06 | The Board Of Trustees Of The University Of Illinois | Benzothiophene-based selective estrogen receptor downregulators |
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EP3697436A1 (en) | 2017-10-18 | 2020-08-26 | Novartis AG | Compositions and methods for selective protein degradation |
EP3752250B1 (en) | 2018-02-16 | 2022-08-03 | Constellation Pharmaceuticals, Inc. | P300/cbp hat inhibitors |
CA3091342A1 (en) | 2018-02-16 | 2019-08-22 | Constellation Pharmaceuticals, Inc. | Susbstituted aryl and heteroaryl acetamide derivatives and pharmaceutical compositions thereof useful as p300/cbp hat_inhibitors |
CN117771239A (zh) | 2018-04-10 | 2024-03-29 | 杜克大学 | 乳腺癌的拉索昔芬治疗 |
EP3897631A4 (en) | 2018-12-20 | 2022-11-23 | C4 Therapeutics, Inc. | TARGETED PROTEIN DEGRADATION |
CA3131383A1 (en) | 2019-02-27 | 2020-09-03 | Constellation Pharmaceuticals, Inc. | P300/cbp hat inhibitors and methods for their use |
WO2020219742A1 (en) | 2019-04-24 | 2020-10-29 | Novartis Ag | Compositions and methods for selective protein degradation |
KR20220046586A (ko) | 2019-07-22 | 2022-04-14 | 썬 파마 어드밴스트 리서치 컴패니 리미티드 | 선택적 에스트로겐 수용체 분해제 |
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CN113045546A (zh) * | 2021-03-25 | 2021-06-29 | 浙江天宇药业股份有限公司 | 一种吡咯替尼杂质、其制备方法及用途 |
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US20090082467A1 (en) | 2007-09-21 | 2009-03-26 | Harry Fisch | Treatment of migraine headaches using antiestrogens |
US20100317635A1 (en) | 2009-06-16 | 2010-12-16 | Endorecherche, Inc. | Treatment of hot flushes, vasomotor symptoms, and night sweats with sex steroid precursors in combination with selective estrogen receptor modulators |
EP3124481B1 (en) | 2010-02-16 | 2018-03-28 | Aragon Pharmaceuticals, Inc. | Androgen receptor modulators and uses thereof |
PL2580210T3 (pl) * | 2010-06-10 | 2017-09-29 | Seragon Pharmaceuticals, Inc. | Modulatory receptora estrogenowego i ich zastosowania |
KR20150039882A (ko) | 2010-06-16 | 2015-04-13 | 앙도르쉐르슈 인코포레이티드 | 에스트로겐-관련 질병의 치료 또는 예방 방법 |
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GB2483736B (en) | 2010-09-16 | 2012-08-29 | Aragon Pharmaceuticals Inc | Estrogen receptor modulators and uses thereof |
BR112014014124A2 (pt) | 2011-12-14 | 2017-08-22 | Seragon Pharmaceutical Inc | Moduladores do receptor de estrogênio fluorados e usos dos mesmos |
US9481663B2 (en) | 2012-06-07 | 2016-11-01 | Aragon Pharmaceuticals, Inc. | Crystalline forms of an androgen receptor modulator |
SG11201500184TA (en) | 2012-07-27 | 2015-04-29 | Aragon Pharmaceuticals Inc | Methods and compositions for determining resistance to androgen receptor therapy |
SG10201912719TA (en) | 2012-09-26 | 2020-02-27 | Aragon Pharmaceuticals Inc | Anti-androgens for the treatment of non-metastatic castrate-resistant prostate cancer |
JOP20200097A1 (ar) | 2013-01-15 | 2017-06-16 | Aragon Pharmaceuticals Inc | معدل مستقبل أندروجين واستخداماته |
-
2012
- 2012-12-17 CN CN201280062009.4A patent/CN104169266A/zh active Pending
- 2012-12-17 PE PE2014000963A patent/PE20150099A1/es not_active Application Discontinuation
- 2012-12-17 US US13/717,326 patent/US9018244B2/en not_active Expired - Fee Related
- 2012-12-17 KR KR1020147019676A patent/KR20140103335A/ko not_active Application Discontinuation
- 2012-12-17 AU AU2012353660A patent/AU2012353660A1/en not_active Abandoned
- 2012-12-17 JP JP2014547552A patent/JP2015505856A/ja active Pending
- 2012-12-17 MX MX2014007198A patent/MX2014007198A/es unknown
- 2012-12-17 AP AP2014007657A patent/AP2014007657A0/xx unknown
- 2012-12-17 SG SG11201402564QA patent/SG11201402564QA/en unknown
- 2012-12-17 WO PCT/US2012/070168 patent/WO2013090921A1/en active Application Filing
- 2012-12-17 CA CA2857061A patent/CA2857061A1/en not_active Abandoned
- 2012-12-17 EP EP20120858374 patent/EP2791128A4/en not_active Withdrawn
- 2012-12-17 BR BR112014014767A patent/BR112014014767A2/pt not_active IP Right Cessation
- 2012-12-17 EA EA201490897A patent/EA201490897A1/ru unknown
- 2012-12-17 MD MDA20140054A patent/MD20140054A2/ro not_active Application Discontinuation
-
2014
- 2014-05-28 CR CR20140259A patent/CR20140259A/es unknown
- 2014-06-02 MA MA37096A patent/MA35722B1/fr unknown
- 2014-06-02 PH PH12014501237A patent/PH12014501237A1/en unknown
- 2014-06-03 TN TNP2014000243A patent/TN2014000243A1/fr unknown
- 2014-06-11 CU CU2014000066A patent/CU20140066A7/es unknown
- 2014-06-11 CL CL2014001533A patent/CL2014001533A1/es unknown
- 2014-06-12 IL IL233118A patent/IL233118A0/en unknown
- 2014-06-13 NI NI201400057A patent/NI201400057A/es unknown
- 2014-06-16 DO DO2014000135A patent/DOP2014000135A/es unknown
- 2014-06-26 ZA ZA2014/04733A patent/ZA201404733B/en unknown
- 2014-07-16 EC ECIEPI20149619A patent/ECSP14009619A/es unknown
- 2014-12-19 HK HK14112731.3A patent/HK1199246A1/xx unknown
-
2015
- 2015-03-17 US US14/660,248 patent/US20150197506A1/en not_active Abandoned
Also Published As
Publication number | Publication date |
---|---|
TN2014000243A1 (fr) | 2015-09-30 |
JP2015505856A (ja) | 2015-02-26 |
NI201400057A (es) | 2014-10-01 |
US20150197506A1 (en) | 2015-07-16 |
MX2014007198A (es) | 2014-10-13 |
IL233118A0 (en) | 2014-08-03 |
KR20140103335A (ko) | 2014-08-26 |
BR112014014767A2 (pt) | 2017-06-13 |
WO2013090921A1 (en) | 2013-06-20 |
MD20140054A2 (ro) | 2014-10-31 |
PE20150099A1 (es) | 2015-01-30 |
CN104169266A (zh) | 2014-11-26 |
AU2012353660A1 (en) | 2014-06-12 |
EP2791128A1 (en) | 2014-10-22 |
ECSP14009619A (es) | 2015-09-30 |
ZA201404733B (en) | 2016-04-28 |
EA201490897A1 (ru) | 2015-03-31 |
EP2791128A4 (en) | 2015-04-22 |
CU20140066A7 (es) | 2014-10-02 |
AP2014007657A0 (en) | 2014-05-31 |
US20130178445A1 (en) | 2013-07-11 |
HK1199246A1 (en) | 2015-06-26 |
CA2857061A1 (en) | 2013-06-20 |
CL2014001533A1 (es) | 2014-10-17 |
US9018244B2 (en) | 2015-04-28 |
PH12014501237A1 (en) | 2014-09-08 |
SG11201402564QA (en) | 2014-09-26 |
CR20140259A (es) | 2014-08-21 |
MA35722B1 (fr) | 2014-12-01 |
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