EA201490200A1 - 4-(8-метокси-1-((1-метоксипропан-2-ил)-2-(тетрагидро-2-н-пиран-4-ил)-1н-имидазо[4,5-c]хинолин-7-ил)-3,5-диметилизоксазол и его применение в качестве ингибитора бромодомена - Google Patents

4-(8-метокси-1-((1-метоксипропан-2-ил)-2-(тетрагидро-2-н-пиран-4-ил)-1н-имидазо[4,5-c]хинолин-7-ил)-3,5-диметилизоксазол и его применение в качестве ингибитора бромодомена

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Publication number
EA201490200A1
EA201490200A1 EA201490200A EA201490200A EA201490200A1 EA 201490200 A1 EA201490200 A1 EA 201490200A1 EA 201490200 A EA201490200 A EA 201490200A EA 201490200 A EA201490200 A EA 201490200A EA 201490200 A1 EA201490200 A1 EA 201490200A1
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Prior art keywords
bromodomain
metoxipropan
hinolin
isoazole
piran
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EA201490200A
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English (en)
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EA023374B1 (ru
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Эммануэль Юбер Демон
Кэтрин Луис Джонс
Роберт Дж. Ватсон
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ГЛАКСОСМИТКЛАЙН ЭлЭлСи
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Publication of EA201490200A1 publication Critical patent/EA201490200A1/ru
Publication of EA023374B1 publication Critical patent/EA023374B1/ru

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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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • 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
    • 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
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Transplantation (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Новые хинолиновые соединения формулы (I), фармацевтические композиции, содержащие такие соединения, и их применение в терапии в качестве ингибиторов бромодомена.
EA201490200A 2011-08-17 2012-08-15 4-(8-метокси-1-((1-метоксипропан-2-ил)-2-(тетрагидро-2н-пиран-4-ил)-1н-имидазо[4,5-c]хинолин-7-ил)-3,5-диметилизоксазол и его применение в качестве ингибитора бромодомена EA023374B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB1114103.3A GB201114103D0 (en) 2011-08-17 2011-08-17 Novel compounds
PCT/EP2012/065918 WO2013024104A1 (en) 2011-08-17 2012-08-15 4-(8-methoxy-1-((1-methoxypropan-2-yl)-2-(tetrahydro-2h-pyran-4-yl)-1 h-imidazo[4,5-c]quinolin-7-yl)-3,5-dimethylisoxazole and its use as bromodomain inhibitor

Publications (2)

Publication Number Publication Date
EA201490200A1 true EA201490200A1 (ru) 2014-07-30
EA023374B1 EA023374B1 (ru) 2016-05-31

Family

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Family Applications (1)

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EA201490200A EA023374B1 (ru) 2011-08-17 2012-08-15 4-(8-метокси-1-((1-метоксипропан-2-ил)-2-(тетрагидро-2н-пиран-4-ил)-1н-имидазо[4,5-c]хинолин-7-ил)-3,5-диметилизоксазол и его применение в качестве ингибитора бромодомена

Country Status (37)

Country Link
US (4) US9067936B2 (ru)
EP (2) EP3150601A1 (ru)
JP (1) JP6059723B2 (ru)
KR (1) KR20140064878A (ru)
CN (1) CN103889984B (ru)
AR (1) AR087545A1 (ru)
AU (1) AU2012296914B2 (ru)
BR (1) BR112014003681A8 (ru)
CA (1) CA2843537A1 (ru)
CL (1) CL2014000365A1 (ru)
CO (1) CO6862151A2 (ru)
CR (1) CR20140076A (ru)
CY (1) CY1118370T1 (ru)
DK (1) DK2744809T3 (ru)
DO (1) DOP2014000031A (ru)
EA (1) EA023374B1 (ru)
ES (1) ES2609857T3 (ru)
GB (1) GB201114103D0 (ru)
HR (1) HRP20161674T1 (ru)
HU (1) HUE030106T2 (ru)
IL (1) IL230489A (ru)
IN (1) IN2014CN00568A (ru)
JO (1) JO3187B1 (ru)
LT (1) LT2744809T (ru)
ME (1) ME02589B (ru)
MX (1) MX350597B (ru)
MY (1) MY170729A (ru)
PE (1) PE20141406A1 (ru)
PL (1) PL2744809T3 (ru)
PT (1) PT2744809T (ru)
RS (1) RS55560B1 (ru)
SI (1) SI2744809T1 (ru)
SM (1) SMT201700005B (ru)
TW (1) TWI558704B (ru)
UA (1) UA110838C2 (ru)
UY (1) UY34264A (ru)
WO (1) WO2013024104A1 (ru)

Families Citing this family (56)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9249161B2 (en) 2010-12-02 2016-02-02 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
AR084070A1 (es) 2010-12-02 2013-04-17 Constellation Pharmaceuticals Inc Inhibidores del bromodominio y usos de los mismos
EP2705039B1 (en) 2011-05-04 2017-07-26 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
EP2721031B1 (en) 2011-06-17 2016-01-20 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
GB201114103D0 (en) * 2011-08-17 2011-09-28 Glaxosmithkline Llc Novel compounds
WO2013184878A1 (en) 2012-06-06 2013-12-12 Constellation Pharmaceuticals, Inc. Benzo [b] isoxazoloazepine bromodomain inhibitors and uses thereof
TWI602820B (zh) 2012-06-06 2017-10-21 星宿藥物公司 溴域抑制劑及其用途
US9765039B2 (en) 2012-11-21 2017-09-19 Zenith Epigenetics Ltd. Biaryl derivatives as bromodomain inhibitors
US9073878B2 (en) 2012-11-21 2015-07-07 Zenith Epigenetics Corp. Cyclic amines as bromodomain inhibitors
US9271978B2 (en) 2012-12-21 2016-03-01 Zenith Epigenetics Corp. Heterocyclic compounds as bromodomain inhibitors
CN105164127A (zh) * 2013-03-11 2015-12-16 艾伯维公司 溴结构域抑制剂
WO2014164596A1 (en) 2013-03-11 2014-10-09 The Regents Of The University Of Michigan Bet bromodomain inhibitors and therapeutic methods using the same
MX2015012158A (es) 2013-03-11 2015-12-01 Abbvie Inc Inhibidores de bomodominio tetraciclicos fusionados.
EP3581576B1 (en) 2013-03-15 2022-01-26 Incyte Holdings Corporation Tricyclic heterocycles as bet protein inhibitors for use in the treatment of a proliferative disease in combination with a janus kinase inhibitor
TWI530499B (zh) * 2013-03-28 2016-04-21 吉李德科學股份有限公司 作為溴結構域（ｂｒｏｍｏｄｏｍａｉｎ）抑制劑之苯並咪唑酮衍生物類
EP3010503B1 (en) 2013-06-21 2020-03-11 Zenith Epigenetics Ltd. Novel bicyclic bromodomain inhibitors
CA2915561C (en) 2013-06-21 2020-09-22 Zenith Epigenetics Corp. Novel substituted bicyclic compounds as bromodomain inhibitors
JP2016523964A (ja) 2013-07-08 2016-08-12 インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ Ｂｅｔタンパク質阻害剤としての三環式複素環
US9855271B2 (en) 2013-07-31 2018-01-02 Zenith Epigenetics Ltd. Quinazolinones as bromodomain inhibitors
WO2015049629A1 (en) * 2013-10-01 2015-04-09 Piramal Enterprises Limited Imidazoquinoline compounds as bromodomain inhibitors
WO2015081189A1 (en) 2013-11-26 2015-06-04 Incyte Corporation Bicyclic heterocycles as bet protein inhibitors
WO2015081203A1 (en) 2013-11-26 2015-06-04 Incyte Corporation Bicyclic heterocycles as bet protein inhibitors
US9309246B2 (en) 2013-12-19 2016-04-12 Incyte Corporation Tricyclic heterocycles as BET protein inhibitors
EP3110818B1 (en) 2014-02-28 2019-10-23 The Regents of The University of Michigan 9h-pyrimido[4,5-b]indoles and related analogs as bet bromodomain inhibitors
AR100160A1 (es) 2014-04-23 2016-09-14 Incyte Corp 1H-PIRROLO[2,3-c]PIRIDIN-7(6H)-ONAS Y PIRAZOLO[3,4-c]PIRIDIN-7(6H)-ONAS COMO INHIBIDORES DE PROTEÍNAS BET
JP6682522B2 (ja) 2014-06-20 2020-04-15 コンステレーション・ファーマシューティカルズ・インコーポレイテッドＣｏｎｓｔｅｌｌａｔｉｏｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ，Ｉｎｃ． ２−（（４ｓ）−６−（４−クロロフェニル）−１−メチル−４ｈ−ベンゾ［ｃ］イソオキサゾロ［４，５−ｅ］アゼピン−４−イル）アセトアミドの結晶形態
EP3194406B8 (en) 2014-09-15 2021-03-31 Incyte Corporation Tricyclic heterocycles for use as bet protein inhibitors
WO2016087942A1 (en) 2014-12-01 2016-06-09 Zenith Epigenetics Corp. Substituted pyridines as bromodomain inhibitors
CA2966298A1 (en) 2014-12-01 2016-06-09 Zenith Epigenetics Ltd. Substituted pyridinones as bromodomain inhibitors
EP3230277B1 (en) 2014-12-11 2019-09-18 Zenith Epigenetics Ltd. Substituted heterocycles as bromodomain inhibitors
CN107406438B (zh) 2014-12-17 2021-05-14 恒翼生物医药科技(上海)有限公司 溴结构域的抑制剂
CA2974153A1 (en) * 2015-02-03 2016-08-11 Trillium Therapeutics Inc. Fluorinated imidazo[4,5-c]quinoline derivatives as inhibitors of bromodomain containing proteins
US10307407B2 (en) 2015-02-27 2019-06-04 The Regents Of The University Of Michigan 9H-pyrimido [4,5-B] indoles as BET bromodomain inhibitors
GB201504694D0 (en) 2015-03-19 2015-05-06 Glaxosmithkline Ip Dev Ltd Covalent conjugates
GB201504689D0 (en) * 2015-03-19 2015-05-06 Glaxosmithkline Ip Dev Ltd Chemical compounds
WO2016186453A1 (en) * 2015-05-20 2016-11-24 Kainos Medicine, Inc. Quinoline derivatives as bromodomain inhibitors
WO2016196065A1 (en) 2015-05-29 2016-12-08 Genentech, Inc. Methods and compositions for assessing responsiveness of cancers to bet inhibitors
WO2016199943A1 (en) * 2015-06-11 2016-12-15 Takeda Pharmaceutical Company Limited Heterocyclic compounds
US10501438B2 (en) 2015-08-11 2019-12-10 Neomed Institute Aryl-substituted dihydroquinolinones, their preparation and their use as pharmaceuticals
US10836742B2 (en) 2015-08-11 2020-11-17 Neomed Institute N-substituted bicyclic lactams, their preparation and their use as pharmaceuticals
KR20180039669A (ko) 2015-08-12 2018-04-18 네오메드 인스티튜트 치환된 벤즈이미다졸, 그의 제조법 및 제약으로서의 그의 용도
WO2017066876A1 (en) 2015-10-21 2017-04-27 Neomed Institute Substituted imidazopyridines, their preparation and their use as pharmaceuticals
TW201722966A (zh) 2015-10-29 2017-07-01 英塞特公司 Bet蛋白質抑制劑之非晶固體形式
US10519151B2 (en) 2016-01-28 2019-12-31 Neomed Institute Substituted [1,2,4]triazolo[4,3-A]pyridines, their preparation and their use as pharmaceuticals
JP6967522B2 (ja) 2016-02-15 2021-11-17 ザ リージェンツ オブ ザ ユニヴァシティ オブ ミシガン Ｂｅｔブロモドメイン阻害剤としての融合１，４−オキサゼピンおよび関連類似体
JP7001614B2 (ja) 2016-04-06 2022-02-03 ザ リージェンツ オブ ザ ユニヴァシティ オブ ミシガン リガンド依存性の標的タンパク質分解のための単官能性中間体
RU2021102253A (ru) 2016-04-06 2021-03-03 Дзе Риджентс Оф Дзе Юниверсити Оф Мичиган Деструкторы белка mdm2
SG11201808729WA (en) 2016-04-12 2018-11-29 Univ Michigan Regents Bet protein degraders
PT3472157T (pt) 2016-06-20 2023-05-30 Incyte Corp Formas sólidas cristalinas de um inibidor bet
AU2017326175B2 (en) 2016-09-13 2022-01-27 The Regents Of The University Of Michigan Fused 1,4-diazepines as BET protein degraders
JP6961684B2 (ja) 2016-09-13 2021-11-05 ザ リージェンツ オブ ザ ユニヴァシティ オブ ミシガン Ｂｅｔタンパク質分解物質としての縮合１，４−オキサゼピン
US11046709B2 (en) 2017-02-03 2021-06-29 The Regents Of The University Of Michigan Fused 1,4-diazepines as BET bromodomain inhibitors
US11267822B2 (en) 2017-09-13 2022-03-08 The Regents Of The University Of Michigan BET bromodomain protein degraders with cleavable linkers
CN108033957A (zh) * 2018-01-09 2018-05-15 中国药科大学 一种喹啉类BET bromodomain抑制剂及其制备方法和用途
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
WO2022132049A1 (en) * 2020-12-17 2022-06-23 National University Of Singapore Treating cancers using bet inhibitors

Family Cites Families (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9004781D0 (en) 1990-03-02 1990-04-25 Glaxo Group Ltd Device
GB0211649D0 (en) 2002-05-21 2002-07-03 Novartis Ag Organic compounds
CA2510375A1 (en) 2002-12-20 2004-07-15 3M Innovative Properties Company Aryl / hetaryl substituted imidazoquinolines
DK1699512T3 (da) 2003-11-03 2012-09-17 Glaxo Group Ltd Fluiddispenseringsindretning
ATE400573T1 (de) 2003-11-21 2008-07-15 Novartis Pharma Gmbh 1h-imidazochinolinderivate als proteinkinaseinhibitoren
AU2006216997A1 (en) 2005-02-11 2006-08-31 Coley Pharmaceutical Group, Inc. Substituted imidazoquinolines and imidazonaphthyridines
BRPI0616338A2 (pt) 2005-09-23 2011-06-14 Coley Pharm Group Inc mÉtodo para 1h-imidazo[4,5-c] piridinas e anÁlogos da mesma
EP1968587A1 (en) 2005-12-16 2008-09-17 Coley Pharmaceutical, Inc. Substituted imidazoquinolines, imidazonaphthyridines, and imidazopyridines, compositions, and methods
JP2008156311A (ja) 2006-12-26 2008-07-10 Institute Of Physical & Chemical Research Ｂｒｄ２ブロモドメイン結合剤
KR101600634B1 (ko) * 2007-12-28 2016-03-07 미쓰비시 타나베 파마 코퍼레이션 항암제
GB0919432D0 (en) * 2009-11-05 2009-12-23 Glaxosmithkline Llc Use
HUE026967T2 (en) * 2009-11-05 2016-07-28 Glaxosmithkline Llc Benzodiazepine Bromodomain inhibitor
GB0919434D0 (en) * 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919423D0 (en) * 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB201106799D0 (en) 2011-04-21 2011-06-01 Glaxosmithkline Llc Novel compounds
GB201114103D0 (en) * 2011-08-17 2011-09-28 Glaxosmithkline Llc Novel compounds

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TW201323424A (zh) 2013-06-16
CR20140076A (es) 2014-03-19
CN103889984A (zh) 2014-06-25
PL2744809T3 (pl) 2017-08-31
CN103889984B (zh) 2016-01-13
CY1118370T1 (el) 2017-06-28
JO3187B1 (ar) 2018-03-08
WO2013024104A1 (en) 2013-02-21
US20140171462A1 (en) 2014-06-19
UY34264A (es) 2013-04-05
LT2744809T (lt) 2016-12-27
MX350597B (es) 2017-09-11
ES2609857T3 (es) 2017-04-24
BR112014003681A8 (pt) 2018-01-23
IL230489A (en) 2016-07-31
EP2744809A1 (en) 2014-06-25
PT2744809T (pt) 2017-01-06
AR087545A1 (es) 2014-04-03
BR112014003681A2 (pt) 2017-03-01
CA2843537A1 (en) 2013-02-21
HUE030106T2 (en) 2017-04-28
GB201114103D0 (en) 2011-09-28
US9610284B2 (en) 2017-04-04
JP2014521735A (ja) 2014-08-28
US9067936B2 (en) 2015-06-30
JP6059723B2 (ja) 2017-01-11
PE20141406A1 (es) 2014-10-25
TWI558704B (zh) 2016-11-21
EA023374B1 (ru) 2016-05-31
SMT201700005B (it) 2017-03-08
US20150315184A1 (en) 2015-11-05
CL2014000365A1 (es) 2014-07-11
HRP20161674T1 (hr) 2017-01-27
US9861627B2 (en) 2018-01-09
ME02589B (me) 2017-06-20
AU2012296914B2 (en) 2016-03-03
US20170157113A1 (en) 2017-06-08
NZ620263A (en) 2016-04-29
IL230489A0 (en) 2014-03-31
DK2744809T3 (en) 2017-01-23
IN2014CN00568A (ru) 2015-04-03
EP2744809B1 (en) 2016-10-12
CO6862151A2 (es) 2014-02-10
SI2744809T1 (sl) 2017-01-31
MX2014001834A (es) 2014-02-27
KR20140064878A (ko) 2014-05-28
US20160317529A1 (en) 2016-11-03
RS55560B1 (sr) 2017-05-31
DOP2014000031A (es) 2014-06-01
UA110838C2 (uk) 2016-02-25
MY170729A (en) 2019-08-27
EP3150601A1 (en) 2017-04-05
AU2012296914A1 (en) 2014-02-13
US9416130B2 (en) 2016-08-16

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