CY1118143T1 - Ετεροκυκλικες ενωσεις χρησιμες ως αναστολεις της pdk1 - Google Patents

Ετεροκυκλικες ενωσεις χρησιμες ως αναστολεις της pdk1

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Publication number
CY1118143T1
CY1118143T1 CY20161100796T CY161100796T CY1118143T1 CY 1118143 T1 CY1118143 T1 CY 1118143T1 CY 20161100796 T CY20161100796 T CY 20161100796T CY 161100796 T CY161100796 T CY 161100796T CY 1118143 T1 CY1118143 T1 CY 1118143T1
Authority
CY
Cyprus
Prior art keywords
heterocyclic compounds
compounds useful
pdk1 inhibitors
pdk1
inhibitors
Prior art date
Application number
CY20161100796T
Other languages
Greek (el)
English (en)
Inventor
Joseph Arndt
Timothy Chan
Kevin Guckian
Gnanasambandam Kumaravel
Wen-Cherng Lee
Edward Yin-Shiang Lin
Daniel Scott
Lihong Sun
Jermaine Thomas
Vloten Kurt Van
Deping Wang
Lei Zhang
Daniel Erlanson
Original Assignee
Millennium Pharmaceuticals, Inc.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Millennium Pharmaceuticals, Inc. filed Critical Millennium Pharmaceuticals, Inc.
Publication of CY1118143T1 publication Critical patent/CY1118143T1/el

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    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
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    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
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    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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    • 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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    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
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    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
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    • 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
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    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
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    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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Families Citing this family (61)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3354650B1 (en) 2008-12-19 2022-02-16 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
RS55101B1 (sr) 2009-10-06 2016-12-30 Millennium Pharmaceuticals Heterociklična jedinjenja koja su korisna kao pdk1 inhibitori
EP2569286B1 (en) * 2010-05-12 2014-08-20 Vertex Pharmaceuticals Inc. Compounds useful as inhibitors of atr kinase
EP2569287B1 (en) 2010-05-12 2014-07-09 Vertex Pharmaceuticals Inc. Compounds useful as inhibitors of atr kinase
RU2012153675A (ru) 2010-05-12 2014-06-20 Вертекс Фармасьютикалз Инкорпорейтед Соединения, пригодные в качестве ингибиторов atr киназы
PT2595965T (pt) 2010-07-20 2016-08-22 Vestaron Corp Triazinas e pirimidinas inseticidas
EP2616468A4 (en) * 2010-09-16 2014-02-26 Hutchison Medipharma Ltd MELTED HETEROARLYE AND APPLICATIONS THEREOF
WO2012135631A1 (en) 2011-03-30 2012-10-04 Arrien Pharmaeuticals Llc Substituted 5-(pyrazin-2-yl)-1h-pyrazolo [3, 4-b] pyridine and pyrazolo [3, 4-b] pyridine derivatives as protein kinase inhibitors
US10457659B2 (en) 2011-04-29 2019-10-29 The Board Of Trustees Of The Leland Stanford Junior University Compositions and methods for increasing proliferation of adult salivary stem cells
SG10201606774UA (en) 2011-09-30 2016-10-28 Vertex Pharma Processes for making compounds useful as inhibitors of atr kinase
MX373340B (es) 2011-09-30 2020-05-13 Vertex Pharma Tratamiento del cancer de pancreas y del cancer de pulmon de celulas no pequeñas con inhibidores de atr.
CN103159741B (zh) * 2011-12-19 2016-08-24 天津市国际生物医药联合研究院 一类酪氨酸激酶抑制剂的制备和用途
HK1205028A1 (en) 2012-04-05 2015-12-11 沃泰克斯药物股份有限公司 Compounds useful as inhibitors of atr kinase and combination therapies thereof
CN102627632B (zh) * 2012-04-16 2014-06-18 中国科学院广州生物医药与健康研究院 一种胺基喹唑啉衍生物及其制备方法和用途
SG11201406552UA (en) 2012-04-25 2014-11-27 Takeda Pharmaceutical Nitrogenated heterocyclic compound
BR112014027561A2 (pt) * 2012-05-08 2017-06-27 Anvyl Llc moduladores alostéricos dos receptor acetilcolina alfa 7 nicotínicos, seus derivados e respectivas utilizações
US9527841B2 (en) 2012-07-13 2016-12-27 Takeda Pharmaceutical Company Limited Substituted pyrido[2,3-b]pyrazines as phosphodiesterase 2A inhibitors
WO2014052669A1 (en) 2012-09-26 2014-04-03 The Regents Of The University Of California Modulation of ire1
US8999632B2 (en) 2012-10-04 2015-04-07 Vertex Pharmaceuticals Incorporated Method for measuring ATR inhibition mediated increases in DNA damage
JP6280912B2 (ja) 2013-03-14 2018-02-14 武田薬品工業株式会社 複素環化合物
CN105358531B (zh) * 2013-03-14 2017-11-14 利兰-斯坦福大学初级学院的董事会 线粒体醛脱氢酶‑2调节剂和其使用方法
ES2651491T3 (es) * 2013-05-31 2018-01-26 Nissan Chemical Industries, Ltd. Compuesto de amida heterocíclico
JP6427491B2 (ja) 2013-07-03 2018-11-21 武田薬品工業株式会社 複素環化合物
EP3018123B1 (en) 2013-07-03 2023-05-10 Takeda Pharmaceutical Company Limited Amide compound
WO2015012328A1 (ja) 2013-07-24 2015-01-29 武田薬品工業株式会社 複素環化合物
EP3057586B1 (en) 2013-10-18 2019-12-04 Celgene Quanticel Research, Inc. Bromodomain inhibitors
US20160264570A1 (en) * 2013-11-15 2016-09-15 The United States Of America, As Represented By The Secretary, Department Of Health And Human Serv Method of blocking transmission of malarial parasite
RU2693484C1 (ru) 2013-11-22 2019-07-03 СиЭль БАЙОСАЕНСИЗ ЭлЭлСи Антагонисты гастрина для лечения и профилактики остеопороза
CN104130256B (zh) * 2014-08-01 2016-08-24 上海毕得医药科技有限公司 一种吡啶并[3,4-d]嘧啶-4（3H）-酮衍生物的制备方法
ES2807785T3 (es) * 2014-10-22 2021-02-24 Bristol Myers Squibb Co Compuestos de heteroarilamina bicíclicos como inhibidores de pi3k
WO2016075224A1 (en) 2014-11-14 2016-05-19 Nerviano Medical Sciences S.R.L. 6-amino-7-bicyclo-7-deaza-purine derivatives as protein kinase inhibitors
AR104259A1 (es) 2015-04-15 2017-07-05 Celgene Quanticel Res Inc Inhibidores de bromodominio
EP3325100A4 (en) 2015-07-17 2019-02-20 Memorial Sloan-Kettering Cancer Center COMBINATION THERAPY WITH PDK1 AND PI3K INHIBITORS
CN105130980B (zh) * 2015-09-09 2018-05-22 沈阳药科大学 N-3-苯并咪唑噻唑胺类衍生物及其制备方法与应用
CN108137586B (zh) * 2015-09-14 2021-04-13 辉瑞大药厂 作为LRRK2抑制剂的新颖咪唑并[4,5-c]喹啉和咪唑并[4,5-c][1,5]萘啶衍生物
KR102678021B1 (ko) 2015-09-30 2024-06-26 버텍스 파마슈티칼스 인코포레이티드 Dna 손상제와 병용되는, atr 저해제를 포함하는 암 치료용 약제학적 조성물
KR101753654B1 (ko) 2015-10-21 2017-07-05 한국화학연구원 3-(4-(피페라진-1-일)벤즈아미도)-1h-피라졸로피리딘 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 포함하는 melk 관련 질환의 예방 또는 치료용 약학적 조성물
KR101753652B1 (ko) * 2015-10-21 2017-07-05 한국화학연구원 N-아릴-1h-피라졸로피리딘-3-아민 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 포함하는 melk 관련 질환의 예방 또는 치료용 약학적 조성물
EP3364971B1 (en) * 2015-10-23 2020-06-17 Sunesis Pharmaceuticals, Inc. Heterocyclic pdk1 inhibitors for use to treat cancer
US9630968B1 (en) 2015-12-23 2017-04-25 Arqule, Inc. Tetrahydropyranyl amino-pyrrolopyrimidinone and methods of use thereof
CR20180516A (es) 2016-03-28 2019-03-05 Incyte Corp Compuestos de iprrolotriazina como inhibidores de tam
EP3445750A4 (en) 2016-04-18 2019-11-27 Celgene Quanticel Research, Inc. THERAPEUTIC COMPOUNDS
US10150754B2 (en) 2016-04-19 2018-12-11 Celgene Quanticel Research, Inc. Histone demethylase inhibitors
KR20190035925A (ko) 2016-08-24 2019-04-03 아르퀼 인코포레이티드 아미노-피롤로피리미디논 화합물 및 이의 사용 방법
ES2981507T3 (es) 2016-12-22 2024-10-09 Global Blood Therapeutics Inc Inhibidores de histonas metiltransferasa
KR20190120360A (ko) * 2017-03-10 2019-10-23 오츠카 가가쿠 가부시키가이샤 반응 생성물 및 고무 조성물
ES2949402T3 (es) * 2017-06-09 2023-09-28 Global Blood Therapeutics Inc Compuestos de azaindol como inhibidores de la histona metiltransferasa
WO2019094779A1 (en) * 2017-11-09 2019-05-16 Sunesis Pharmaceuticals, Inc. Pharmaceutical formulations, processes for preparation, and methods of use
EA202091777A1 (ru) 2018-01-26 2020-10-14 Бристол-Маерс Сквибб Компани Аминопирролотриазины в качестве ингибиторов киназы
CN109087534A (zh) * 2018-10-09 2018-12-25 王业宝 一种基于车辆行驶轨迹的交通冲突检测方法
US11780857B2 (en) * 2019-04-17 2023-10-10 EWHA University—Industry Collaboration Foundation Probe compounds for amino alcohols, and simultaneous fluorescence and circular dichroism analysis method
CN110066221B (zh) * 2019-05-16 2022-03-08 海门瑞一医药科技有限公司 一种环丙基甲胺的制备方法
WO2021064141A1 (en) * 2019-10-02 2021-04-08 Tolremo Therapeutics Ag Inhibitors of dual specificity tyrosine phosphorylation regulated kinase 1b
EP4067354A4 (en) * 2019-11-25 2023-11-08 Daewoong Pharmaceutical Co., Ltd. NOVEL TRIAZOLOPYRIDINE DERIVATIVE AND PHARMACEUTICAL COMPOSITION COMPRISING SAME
JP2024502083A (ja) * 2020-12-31 2024-01-17 清華大学 ピリジン－２－アミン誘導体、その医薬組成物、及び使用
AR127972A1 (es) * 2021-12-17 2024-03-13 Pi Industries Ltd Novedosos compuestos de piridina carboxamida bicíclica sustituida fusionada para combatir hongos fitopatogénicos
WO2024040241A1 (en) 2022-08-19 2024-02-22 Viracta Therapeutics, Inc. Pharmaceutical formulations, processes for preparation, and methods of use
WO2024040242A1 (en) 2022-08-19 2024-02-22 Viracta Therapeutics, Inc. Combinations of pdk1 inhibitors and kinase inhibitors
WO2024220937A2 (en) * 2023-04-21 2024-10-24 Kymera Therapeutics, Inc. Tyk2 degraders and uses thereof
CN117603068A (zh) * 2023-08-01 2024-02-27 常州寅盛药业有限公司 一种氨甲环酸的制备方法
WO2025076290A1 (en) * 2023-10-05 2025-04-10 Purdue Research Foundation 5-6-5/6-bisaryl compounds as flt3 inhibitors

Family Cites Families (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3175980A (en) * 1958-05-23 1965-03-30 Geigy Ag J R Compositions of matter of improved appearance in daylight, containing a 3.5-diaminopyrazine-2.6-dicarboxylic acid derivative
PL114780B1 (en) * 1978-03-10 1981-02-28 Inst Przemyslu Farmaceutic Process for preparing novel alkylamides of 2-anilinonicotinic acids
US4911920A (en) 1986-07-30 1990-03-27 Alcon Laboratories, Inc. Sustained release, comfort formulation for glaucoma therapy
FR2588189B1 (fr) 1985-10-03 1988-12-02 Merck Sharp & Dohme Composition pharmaceutique de type a transition de phase liquide-gel
DK0495421T3 (da) 1991-01-15 1996-12-09 Alcon Lab Inc Anvendelse af carragenaner i topiske ophthalmiske sammensætninger
US5212162A (en) 1991-03-27 1993-05-18 Alcon Laboratories, Inc. Use of combinations gelling polysaccharides and finely divided drug carrier substrates in topical ophthalmic compositions
US6309853B1 (en) 1994-08-17 2001-10-30 The Rockfeller University Modulators of body weight, corresponding nucleic acids and proteins, and diagnostic and therapeutic uses thereof
ATE240316T1 (de) * 1998-12-23 2003-05-15 Lilly Co Eli Heteroaromatische amide als inhibitoren von faktor xa
JP2004522689A (ja) * 1998-12-23 2004-07-29 イーライ・リリー・アンド・カンパニー 抗血栓アミド類
GB0001930D0 (en) * 2000-01-27 2000-03-22 Novartis Ag Organic compounds
US6878714B2 (en) * 2001-01-12 2005-04-12 Amgen Inc. Substituted alkylamine derivatives and methods of use
AU2003234464B2 (en) 2002-05-03 2009-06-04 Exelixis, Inc. Protein kinase modulators and methods of use
CL2004000234A1 (es) 2003-02-12 2005-04-15 Biogen Idec Inc Compuestos derivados 3-(piridin-2-il)-4-heteroaril-pirazol sustituidos, antagonistas de aik5 y/o aik4; composicion farmaceutica y uso del compuesto en el tratamiento de desordenes fibroticos como esclerodermia, lupus nefritico, cicatrizacion de herid
US7538135B2 (en) * 2003-07-08 2009-05-26 Novartis Ag Benzenesulfonylamino compounds and pharmaceutical compositions containing these compounds
US7320992B2 (en) 2003-08-25 2008-01-22 Amgen Inc. Substituted 2,3-dihydro-1h-isoindol-1-one derivatives and methods of use
WO2005039564A1 (en) * 2003-10-02 2005-05-06 Vertex Pharmaceuticals Incorporated Phthalimide compounds useful as protein kinase inhibitors
RU2006117635A (ru) * 2003-10-24 2007-12-10 Шеринг Акциенгезельшафт (De) Производные индолинона и их применение для лечения патологических состояний, таких как злокачественное новообразование
AR049418A1 (es) * 2004-02-27 2006-08-02 Bayer Pharmaceuticals Corp Derivados de heteroarilaminopirazol y composiciones farmaceuticas para el tratamiento de la diabetes.
SE0401345D0 (sv) * 2004-05-25 2004-05-25 Astrazeneca Ab Therapeutic compounds: Pyridine as scaffold
EP1655297A1 (en) * 2004-11-03 2006-05-10 Schering Aktiengesellschaft Nicotinamide pyridinureas as vascular endothelial growth factor (VEGF) receptor kinase inhibitors
CA2610509A1 (en) 2005-06-03 2006-12-14 Bayer Healthcare Ag 1-methyl-1h-pyrazole-4-carboxamides useful as cancer chemotherapeutic agents
TW200726765A (en) 2005-06-17 2007-07-16 Bristol Myers Squibb Co Triazolopyridine cannabinoid receptor 1 antagonists
US7547782B2 (en) * 2005-09-30 2009-06-16 Bristol-Myers Squibb Company Met kinase inhibitors
EP1945222B1 (en) 2005-11-02 2012-12-26 Bayer Pharma Aktiengesellschaft Pyrrolo[2,1-f] [1,2,4]-triazin-4-ylamines as igf-1r kinase inhibitors for the treatment of cancer and other hyperproliferative diseases
WO2007084667A2 (en) 2006-01-19 2007-07-26 Osi Pharmaceutical, Inc. Fused heterobicyclic kinase inhibitors
JP5523829B2 (ja) * 2006-06-29 2014-06-18 アステックス、セラピューティックス、リミテッド 複合薬剤
CN101541783B (zh) * 2006-06-30 2014-10-01 苏尼西斯制药有限公司 吡啶酮基pdk1抑制剂
WO2008016643A2 (en) * 2006-08-01 2008-02-07 Cytokinetics, Incorporated Certain chemical entities, compositions, and methods
AU2007338795B2 (en) 2006-12-20 2012-07-19 Amgen Inc. Substituted heterocycles and methods of use
EP2139882B1 (en) * 2007-03-23 2013-12-25 Amgen Inc. 3- substituted quinoline or quinoxaline derivatives and their use as phosphatidylinositol 3-kinase (pi3k) inhibitors
JP5478488B2 (ja) * 2007-06-20 2014-04-23 メルク・シャープ・アンド・ドーム・コーポレーション Ｊａｎｕｓキナーゼの阻害剤
US7868001B2 (en) 2007-11-02 2011-01-11 Hutchison Medipharma Enterprises Limited Cytokine inhibitors
AU2010259009A1 (en) * 2009-06-08 2012-01-12 Nantbioscience, Inc. Triazine derivatives and their therapeutical applications
RS55101B1 (sr) 2009-10-06 2016-12-30 Millennium Pharmaceuticals Heterociklična jedinjenja koja su korisna kao pdk1 inhibitori

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