EA201491671A1 - Гетероциклильные соединения - Google Patents
Гетероциклильные соединенияInfo
- Publication number
- EA201491671A1 EA201491671A1 EA201491671A EA201491671A EA201491671A1 EA 201491671 A1 EA201491671 A1 EA 201491671A1 EA 201491671 A EA201491671 A EA 201491671A EA 201491671 A EA201491671 A EA 201491671A EA 201491671 A1 EA201491671 A1 EA 201491671A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- present
- heterocyclic compounds
- compounds
- heteroaryl compounds
- tautomers
- Prior art date
Links
Classifications
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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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- 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
- 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
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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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
- A61K31/541—Non-condensed thiazines containing further heterocyclic rings
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61N—ELECTROTHERAPY; MAGNETOTHERAPY; RADIATION THERAPY; ULTRASOUND THERAPY
- A61N5/00—Radiation therapy
- A61N5/10—X-ray therapy; Gamma-ray therapy; Particle-irradiation therapy
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- 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
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
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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
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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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
- A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
-
- 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
-
- 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
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
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- 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
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- 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
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- 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
- 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
Abstract
Настоящее изобретение относится к гетероарильным соединениям, таким как ингибиторы MEK. Настоящее изобретение включает гетероарильные соединения с формулой (I), их таутомеры и фармацевтически приемлемые соли, комбинации с подходящим лекарственным препаратом и их фармацевтические композиции. Настоящее изобретение также включает способ получения указанных соединений и предусматривает их применение в терапии.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
IN288KO2012 | 2012-03-14 | ||
PCT/IB2013/051915 WO2013136254A1 (en) | 2012-03-14 | 2013-03-11 | Heterocyclyl compounds |
Publications (2)
Publication Number | Publication Date |
---|---|
EA201491671A1 true EA201491671A1 (ru) | 2014-12-30 |
EA029768B1 EA029768B1 (ru) | 2018-05-31 |
Family
ID=47997632
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA201491672A EA028232B1 (ru) | 2012-03-14 | 2013-03-11 | Гетероциклильные соединения как ингибиторы mek |
EA201491671A EA029768B1 (ru) | 2012-03-14 | 2013-03-11 | Гетероциклильные соединения |
Family Applications Before (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA201491672A EA028232B1 (ru) | 2012-03-14 | 2013-03-11 | Гетероциклильные соединения как ингибиторы mek |
Country Status (36)
Country | Link |
---|---|
US (5) | US9428499B2 (ru) |
EP (2) | EP2834237B1 (ru) |
JP (3) | JP6431770B2 (ru) |
KR (4) | KR20140138910A (ru) |
CN (4) | CN104271577A (ru) |
AP (2) | AP3859A (ru) |
AU (4) | AU2013234014B2 (ru) |
BR (1) | BR112014022713B1 (ru) |
CA (2) | CA2865167C (ru) |
CL (2) | CL2014002412A1 (ru) |
CO (2) | CO7170131A2 (ru) |
CR (2) | CR20140464A (ru) |
CU (2) | CU24272B1 (ru) |
DK (2) | DK2834236T3 (ru) |
DO (2) | DOP2014000204A (ru) |
EA (2) | EA028232B1 (ru) |
ES (2) | ES2741896T3 (ru) |
GE (2) | GEP201706671B (ru) |
GT (2) | GT201400196A (ru) |
HK (2) | HK1202538A1 (ru) |
IL (2) | IL234559A (ru) |
IN (2) | IN2014MN01755A (ru) |
MA (2) | MA37400B1 (ru) |
MX (3) | MX355526B (ru) |
MY (2) | MY174188A (ru) |
NI (2) | NI201400108A (ru) |
NZ (2) | NZ629432A (ru) |
PE (2) | PE20141973A1 (ru) |
PH (2) | PH12014502041B1 (ru) |
PL (1) | PL2834237T3 (ru) |
SG (2) | SG11201405006PA (ru) |
TN (2) | TN2014000356A1 (ru) |
TR (1) | TR201811976T4 (ru) |
UA (2) | UA114907C2 (ru) |
WO (2) | WO2013136254A1 (ru) |
ZA (1) | ZA201406186B (ru) |
Families Citing this family (43)
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WO2012088266A2 (en) | 2010-12-22 | 2012-06-28 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3 |
KR20140138910A (ko) | 2012-03-14 | 2014-12-04 | 루핀 리미티드 | 헤테로사이클릴 화합물 |
PT3176170T (pt) | 2012-06-13 | 2019-02-05 | Incyte Holdings Corp | Compostos tricíclicos substituídos como inibidores de fgfr |
US9388185B2 (en) | 2012-08-10 | 2016-07-12 | Incyte Holdings Corporation | Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors |
US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
PE20152033A1 (es) | 2013-04-19 | 2016-01-21 | Incyte Holdings Corp | Heterociclos bicicliclos como inhibidores de fgfr |
CN104936945B (zh) * | 2013-10-25 | 2017-11-03 | 上海恒瑞医药有限公司 | 吡啶酮类衍生物、其制备方法及其在医药上的应用 |
WO2016009306A1 (en) * | 2014-07-15 | 2016-01-21 | Lupin Limited | Heterocyclyl compounds as mek inhibitors |
WO2016035008A1 (en) * | 2014-09-04 | 2016-03-10 | Lupin Limited | Pyridopyrimidine derivatives as mek inhibitors |
US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
EP3617205B1 (en) | 2015-02-20 | 2021-08-04 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
US9580423B2 (en) | 2015-02-20 | 2017-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
LT3728254T (lt) | 2017-12-21 | 2023-05-10 | Boehringer Ingelheim International Gmbh | Naujieji benzilaminu pakeistieji piridopirimidinonai ir jų dariniai kaip sos1 inhibitoriai |
CN112867716A (zh) | 2018-05-04 | 2021-05-28 | 因赛特公司 | Fgfr抑制剂的固体形式和其制备方法 |
CA3099116A1 (en) | 2018-05-04 | 2019-11-07 | Incyte Corporation | Salts of an fgfr inhibitor |
WO2020185532A1 (en) | 2019-03-08 | 2020-09-17 | Incyte Corporation | Methods of treating cancer with an fgfr inhibitor |
AU2020242287A1 (en) | 2019-03-21 | 2021-09-02 | INSERM (Institut National de la Santé et de la Recherche Médicale) | A Dbait molecule in combination with kinase inhibitor for the treatment of cancer |
CN114375202A (zh) | 2019-06-19 | 2022-04-19 | 勃林格殷格翰国际有限公司 | 抗癌组合疗法 |
WO2021007269A1 (en) | 2019-07-09 | 2021-01-14 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
WO2021018866A1 (en) * | 2019-07-30 | 2021-02-04 | Edvince Ab | Mek inhibitor for treatment of stroke |
EP3797899A1 (de) | 2019-09-27 | 2021-03-31 | Primetals Technologies Austria GmbH | Vorrichtung und verfahren zum erkennen von einer bewegung eines körpers in einer industrieanlage |
JOP20220083A1 (ar) | 2019-10-14 | 2023-01-30 | Incyte Corp | حلقات غير متجانسة ثنائية الحلقة كمثبطات لـ fgfr |
US11566028B2 (en) | 2019-10-16 | 2023-01-31 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
US20220401436A1 (en) | 2019-11-08 | 2022-12-22 | INSERM (Institute National de la Santé et de la Recherche Médicale) | Methods for the treatment of cancers that have acquired resistance to kinase inhibitors |
CA3163875A1 (en) | 2019-12-04 | 2021-06-10 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
CA3162010A1 (en) | 2019-12-04 | 2021-06-10 | Incyte Corporation | Derivatives of an fgfr inhibitor |
WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
CN116034106A (zh) | 2020-06-02 | 2023-04-28 | 勃林格殷格翰国际有限公司 | 用于治疗癌症的环状2-氨基-3-氰基噻吩及衍生物 |
TWI825637B (zh) | 2021-03-31 | 2023-12-11 | 美商輝瑞股份有限公司 | 啶-1,6(2h,7h)-二酮 |
CN117479942A (zh) | 2021-04-09 | 2024-01-30 | 勃林格殷格翰国际有限公司 | 抗癌疗法 |
AU2022258968A1 (en) * | 2021-04-16 | 2023-10-19 | Ikena Oncology, Inc. | Mek inhibitors and uses thereof |
US11939331B2 (en) | 2021-06-09 | 2024-03-26 | Incyte Corporation | Tricyclic heterocycles as FGFR inhibitors |
WO2023099620A1 (en) | 2021-12-01 | 2023-06-08 | Boehringer Ingelheim International Gmbh | Kras degrading compounds comprising annulated 2-amino-3-cyano thiophenes |
WO2023099592A1 (en) | 2021-12-01 | 2023-06-08 | Boehringer Ingelheim International Gmbh | Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer |
WO2023099608A1 (en) | 2021-12-01 | 2023-06-08 | Boehringer Ingelheim International Gmbh | Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer |
TW202340208A (zh) | 2021-12-01 | 2023-10-16 | 德商百靈佳殷格翰國際股份有限公司 | 用於治療癌症之環狀2-胺基-3-氰基噻吩及衍生物 |
TW202337431A (zh) | 2021-12-01 | 2023-10-01 | 德商百靈佳殷格翰國際股份有限公司 | 用於治療癌症之環狀2-胺基-3-氰基噻吩及衍生物 |
CN114573582B (zh) * | 2022-03-30 | 2023-06-16 | 沈阳药科大学 | 1,2,3,4-四氢吡啶并[2,3-d]嘧啶类化合物及其制备方法和应用 |
CN114605408B (zh) * | 2022-03-30 | 2023-06-16 | 沈阳药科大学 | 5-羟基-1,3-二取代苯基吡啶并[2,3-d]嘧啶类化合物及其制法和应用 |
CN114573581B (zh) * | 2022-03-30 | 2023-09-01 | 沈阳药科大学 | 5-取代氨基-1,3-二取代苯基吡啶并[2,3-d]嘧啶类化合物及其制备与应用 |
CN114456166B (zh) * | 2022-03-30 | 2023-06-16 | 沈阳药科大学 | 5-取代氨基-3-甲基吡啶并[2,3-d]嘧啶类化合物及其制备与应用 |
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EA201101533A1 (ru) | 2009-04-21 | 2012-05-30 | Новартис Аг | Гетероциклические соединения в качестве ингибиторов mek |
KR20140138910A (ko) | 2012-03-14 | 2014-12-04 | 루핀 리미티드 | 헤테로사이클릴 화합물 |
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2013
- 2013-03-11 KR KR1020147028556A patent/KR20140138910A/ko active Application Filing
- 2013-03-11 TR TR2018/11976T patent/TR201811976T4/tr unknown
- 2013-03-11 ES ES13711973T patent/ES2741896T3/es active Active
- 2013-03-11 JP JP2014561564A patent/JP6431770B2/ja active Active
- 2013-03-11 DK DK13711973.1T patent/DK2834236T3/da active
- 2013-03-11 KR KR1020147028557A patent/KR20140138911A/ko not_active IP Right Cessation
- 2013-03-11 EA EA201491672A patent/EA028232B1/ru unknown
- 2013-03-11 GE GEAP201313595A patent/GEP201706671B/en unknown
- 2013-03-11 IN IN1755MUN2014 patent/IN2014MN01755A/en unknown
- 2013-03-11 MY MYPI2014002639A patent/MY174188A/en unknown
- 2013-03-11 MA MA37400A patent/MA37400B1/fr unknown
- 2013-03-11 UA UAA201411014A patent/UA114907C2/uk unknown
- 2013-03-11 MY MYPI2014002638A patent/MY175950A/en unknown
- 2013-03-11 AP AP2014008009A patent/AP3859A/en active
- 2013-03-11 KR KR1020197017334A patent/KR102240101B1/ko active IP Right Grant
- 2013-03-11 AP AP2014008008A patent/AP3834A/en active
- 2013-03-11 EP EP13712929.2A patent/EP2834237B1/en active Active
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