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PE20091957A1 - Compuestos triazina como inhibidores mtor y quinasa pi3 - Google Patents

Compuestos triazina como inhibidores mtor y quinasa pi3

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Publication number
PE20091957A1
PE20091957A1 PE2009000725A PE2009000725A PE20091957A1 PE 20091957 A1 PE20091957 A1 PE 20091957A1 PE 2009000725 A PE2009000725 A PE 2009000725A PE 2009000725 A PE2009000725 A PE 2009000725A PE 20091957 A1 PE20091957 A1 PE 20091957A1
Authority
PE
Peru
Prior art keywords
mtor
cor3
triazin
oxa
oct
Prior art date
Application number
PE2009000725A
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English (en)
Inventor
Aranapakam Mudumbai Venkatesan
Zecheng Chen
Christoph Martin Dehnhardt
Santos Osvaldo Dos
Santos Efren Guillermo Delos
Arie Zask
Jeroen Cunera Verheijen
Joshua Aaron Kaplan
David James Richard
Semiramis Ayral-Kaloustian
Tarek Suhayl Mansour
Ariamala Jay Gopalsamy
Kevin Joseph Curran
Mengxiao Shi
Original Assignee
Wyeth Corp
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=40911929&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20091957(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Wyeth Corp filed Critical Wyeth Corp
Publication of PE20091957A1 publication Critical patent/PE20091957A1/es

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    • C07D401/02—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
    • 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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    • 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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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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    • C07D251/12—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D251/14—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom
    • C07D251/16—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom to only one ring carbon atom
    • C07D251/18—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom to only one ring carbon atom with nitrogen atoms directly attached to the two other ring carbon atoms, e.g. guanamines
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    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
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    • 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
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    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
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    • 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
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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
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  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Immunology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Vascular Medicine (AREA)
  • Dermatology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)

Abstract

SE REFIERE A DERIVADOS DE [1,3,5] TRIAZINA 2,4,6-SUSTITUIDOS DE FORMULA (I) DONDE R1 ES (a) O (b), EN DONDE R6, R7, R8 Y R9 SON CADA UNO H, ALQUILO(C1-C6) OPCIONALMENTE SUSTITUIDO CON ALQUENILO(C2-C6), ALCADIENILO(C4-C6), ALQUINILO(C2-C6), ENTRE OTROS; ---- ES UN SEGUNDO ENLACE OPCIONAL; R2 ES ARILO(C6-C14) OPCIONALMENTE SUSTITUIDO CON -NH-COR3, HETEROARILO(C6-C9) OPCIONALMENTE SUSTITUIDO CON -NH-COR3, -CH=CH-ARILO(C6-C10)-NH-COR3, ENTRE OTROS, DONDE R3 ES OR5, NR5R5 O NHR5; R5 ES ALQUILO(C1-C6), ALQUENILO(C3-C6), ALQUINILO(C3-C6), ENTRE OTROS; R4 ES ALQUENILO(C3-C6), ALQUINILO(C3-C6), CICLOALQUILO(C3-C8), ENTRE OTROS. SON COMPUESTOS PREFERIDOS: 1-{4-[4-MORFOLIN-4-IL-6-(8-OXA-3-AZABICICLO[3.2.1]OCT-3-IL)-1,3,5-TRIAZIN-2-IL]FENIL}-3-FENILUREA, 1-(4-FLUOROFENIL)-3-{4-[4-MORFOLIN-4-IL-6-(8-OXA-3-AZABICICLO[3.2.1]OCT-3-IL)-1,3,5-TRIAZIN-2-IL]FENIL}UREA, 1-(4-METILFENIL)-3-{4-[4-MORFOLIN-4-IL-6-(8-OXA-3-AZABICICLO[3.2.1]OCT-3-IL)-1,3,5-TRIAZIN-2-IL]FENIL}UREA, ENTRE OTROS. SE REFIERE TAMBIEN A UN PROCEDIMIENTO DE PREPARACION Y A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LA QUINASA FOSFATIDILINOSITOL-3 (PI3) Y mTOR SIENDO UTILES EN EL TRATAMIENTO DE CANCER, RESTENOSIS, ARTRITIS, SORIASIS
PE2009000725A 2008-05-23 2009-05-25 Compuestos triazina como inhibidores mtor y quinasa pi3 PE20091957A1 (es)

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US5566108P 2008-05-23 2008-05-23

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PE20091957A1 true PE20091957A1 (es) 2009-12-30

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Families Citing this family (54)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10022381B2 (en) * 2008-05-23 2018-07-17 Pfizer Inc. Triazine compounds as PI3 kinase and mTOR inhibitors
GEP20125502B (en) 2008-05-23 2012-04-25 Novartis Ag Derivatives of quinolines and quinoxalines as protein tyrosine kinase inhibitors
EP2300483A1 (en) * 2008-05-23 2011-03-30 Wyeth LLC Triazine compounds as p13 kinase and mtor inhibitors
GB2465405A (en) * 2008-11-10 2010-05-19 Univ Basel Triazine, pyrimidine and pyridine analogues and their use in therapy
WO2010096619A1 (en) * 2009-02-23 2010-08-26 Wyeth Llc Process, purification and crystallization of 1-(4-{[4-(dimethylamino)piperidin-1-yl]carbonyl}phenyl)-3-[4-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)phenyl]urea
JP5766177B2 (ja) 2009-03-27 2015-08-19 ベトディーシー，インコーポレイテッド ピリミジニル及び１，３，５−トリアジニルベンゾイミダゾールスルホンアミド及びガンの療法におけるその使用
UY32582A (es) 2009-04-28 2010-11-30 Amgen Inc Inhibidores de fosfoinositida 3 cinasa y/u objetivo mamífero
EP2532659A1 (en) 2009-07-07 2012-12-12 Pathway Therapeutics, Inc. Pyrimidinyl and 1,3,5-triazinyl benzimidazoles and their use in cancer therapy
BR112012003661A2 (pt) * 2009-08-19 2017-04-25 Ambit Biosciences Corp "compostos de biarila e métodos de uso dos mesmos."
US8697691B2 (en) * 2009-12-21 2014-04-15 Vanderbilt University Alkyl 3-((2-amidoethyl)amino)-8-azabicyclo[3.2.1]octane-8-carboxylate analogs as selective M1 agonists and methods of making and using same
JP2013521002A (ja) 2010-03-05 2013-06-10 プレジデント アンド フェロウズ オブ ハーバード カレッジ 誘導樹状細胞組成物及びその使用
GB201004200D0 (en) 2010-03-15 2010-04-28 Univ Basel Spirocyclic compounds and their use as therapeutic agents and diagnostic probes
US9481670B2 (en) * 2011-01-25 2016-11-01 Sphaera Pharma Pte. Ltd. Triazine compounds
WO2012103524A2 (en) * 2011-01-27 2012-08-02 The Trustees Of Princeton University Inhibitors of mtor kinasa as anti- viral agents
JP5766820B2 (ja) * 2011-02-09 2015-08-19 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ Ｐｉ３キナーゼ阻害剤としての複素環化合物
WO2012135160A1 (en) 2011-03-28 2012-10-04 Pathway Therapeutics Inc. (alpha- substituted aralkylamino and heteroarylalkylamino) pyrimidinyl and 1,3,5 -triazinyl benzimidazoles, pharmaceutical compositions containing them, and these compounds for use in treating proliferative diseases
CN102250065B (zh) * 2011-05-20 2015-05-13 浙江海正药业股份有限公司 取代的三嗪苯脲衍生物及其用途
CN102887867B (zh) * 2011-07-21 2015-04-15 中国科学院上海药物研究所 一类三嗪类化合物、该化合物的制备方法及其用途
CA2849189A1 (en) * 2011-09-21 2013-03-28 Cellzome Limited Morpholino substituted urea or carbamate derivatives as mtor inhibitors
RU2609208C2 (ru) 2011-10-07 2017-01-31 Селлзоум Лимитед МОРФОЛИНО-ЗАМЕЩЕННЫЕ ПРОИЗВОДНЫЕ БИЦИКЛИЧЕСКИХ ПИРИМИДИНМОЧЕВИНЫ ИЛИ КАРБАМАТА В КАЧЕСТВЕ ИНГИБИТОРОВ mTOR
CN102659765B (zh) * 2011-12-31 2014-09-10 沈阳药科大学 嘧啶及三嗪类化合物的制备方法和应用
KR20160027218A (ko) 2012-05-23 2016-03-09 에프. 호프만-라 로슈 아게 내배엽 및 간세포를 수득하고 사용하는 조성물 및 방법
WO2014005182A1 (en) * 2012-07-04 2014-01-09 Monash University Phosphoinositide 3-kinase (pi3k) inhibitors
CN104582707B (zh) * 2012-07-23 2017-09-26 斯法尔制药私人有限公司 三嗪化合物
GB201309807D0 (en) 2013-05-31 2013-07-17 Pharma Mar Sau Antibody drug conjugates
US9763992B2 (en) 2014-02-13 2017-09-19 Father Flanagan's Boys' Home Treatment of noise induced hearing loss
HUE043964T2 (hu) 2014-03-14 2019-09-30 Pfizer Terápiás szert tartalmazó terápiás nanorészecskék és eljárás ezek elõállítására és alkalmazására
WO2016049774A1 (en) * 2014-10-03 2016-04-07 The Royal Institution For The Advancement Of Learning/Mcgill University Urea and bis-urea based compounds and analogues thereof useful in the treatment of androgen receptor mediated diseases or disorders
EP3549583A1 (en) 2014-10-10 2019-10-09 Pfizer Inc Synergistic auristatin combinations
JP6695875B2 (ja) 2014-11-20 2020-05-20 カウンシル・オブ・サイエンティフィック・アンド・インダストリアル・リサーチ 抗がん剤としての新規な１，３，５−トリアジン系ｐｉ３ｋ阻害剤及びその製造方法
SG11201703826TA (en) 2014-12-17 2017-07-28 Pfizer Formulations of a pi3k/mtor-inhibitor for intravenous administration
CN104725361B (zh) * 2015-04-09 2017-05-31 江苏富比亚化学品有限公司 一种受阻胺类光稳定剂3346的制备方法
DK3456712T3 (da) 2016-05-12 2022-05-30 Nanjing Shiqi Pharmaceutical Co Ltd Hidtil ukendte 2,4,6-trisubstitueret S-triazinforbindelse, fremgangsmåde til fremstilling deraf og anvendelse deraf
RS61655B1 (sr) 2016-05-18 2021-04-29 Torqur Ag Lečenje neuroloških poremećaja
JOP20190254A1 (ar) 2017-04-27 2019-10-27 Pharma Mar Sa مركبات مضادة للأورام
IT201700047189A1 (it) * 2017-05-02 2018-11-02 Fondazione St Italiano Tecnologia Composti e composizioni per il trattamento di cancro, disordini della retina e cardiomiopatie
WO2018217787A1 (en) 2017-05-23 2018-11-29 Mei Pharma, Inc. Combination therapy
KR20200041358A (ko) 2017-08-14 2020-04-21 메이 파마, 아이엔씨. 병용 요법
HUE056743T2 (hu) 2017-08-25 2022-03-28 Pfizer 1-(4-{[4-(dimetilamino)piperidin-1-il]karbonil}fenil)-3-[4-(4,6-dimorfolin-4-il-1,3,5-triazin-2-il)fenil]ureát tartalmazó vizes gyógyszerkészítmény
CN108191837A (zh) * 2018-01-10 2018-06-22 贵州医科大学 PI3Kα/mTOR双激酶抑制剂及其药物组合物和应用
WO2019157516A1 (en) 2018-02-12 2019-08-15 resTORbio, Inc. Combination therapies
KR102022323B1 (ko) * 2018-03-30 2019-09-18 정하윤 트리아진 화합물 및 이의 용도
LT3810089T (lt) * 2018-06-07 2023-11-10 Pfizer Inc. Vandeninė vaisto forma, apimanti 1-(4-{[4-(dimetilamino)piperidin-1- il] karbonil}fenil)-3-[4-(4,6-dimorfolin-4-il-1,3,5-triazin-2-il)fenil]karbamidą
US10980784B2 (en) 2018-06-15 2021-04-20 Navitor Pharmaceuticals, Inc. Rapamycin analogs and uses thereof
JPWO2020130125A1 (ja) 2018-12-21 2021-11-04 第一三共株式会社 抗体−薬物コンジュゲートとキナーゼ阻害剤の組み合わせ
CN109942562B (zh) * 2019-02-27 2022-02-08 江西科技师范大学 含芳基结构的五元杂环联三嗪类化合物及其制备方法和应用
WO2021113665A1 (en) 2019-12-05 2021-06-10 Navitor Pharmaceuticals, Inc. Rapamycin analogs and uses thereof
CN115697345A (zh) * 2020-04-07 2023-02-03 梅制药公司 1,3,5-三嗪基苯并咪唑的制备
KR20220138575A (ko) 2021-04-06 2022-10-13 부산대학교병원 전좌 신장암 치료 또는 예방용 약물 스크리닝 방법
CN113200969B (zh) * 2021-05-19 2022-11-25 中国药科大学 一种PI3Kα选择性抑制剂及其制备方法和应用
TW202320795A (zh) 2021-07-26 2023-06-01 美商凱爾科迪股份有限公司 使用1-(4-{[4-(二甲胺基)哌啶-1-基]羰基}苯基)-3-[4-(4,6-二嗎啉-4-基-1,3,5-三-2-基)苯基]脲治療癌症之方法
CN115109049B (zh) * 2022-08-12 2023-08-15 江西科技师范大学 含芳基脲结构的三嗪类化合物及其应用
CN115557908B (zh) * 2022-09-28 2024-10-15 九江学院 一种含硫连接键的三嗪类衍生物及其合成方法、用途
CN116102545B (zh) * 2023-02-01 2025-03-25 贵州医科大学 一种二芳基脲类PI3K/mTOR/HDAC多靶点抑制剂及其药物组合物和应用

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP4276376B2 (ja) * 1997-07-24 2009-06-10 全薬工業株式会社 複素環式化合物及びそれを有効成分とする抗腫瘍剤
ATE239012T1 (de) * 1997-12-12 2003-05-15 Abbott Lab Triazin angiogenese-inhibitoren
WO2002088112A1 (fr) 2001-04-27 2002-11-07 Zenyaku Kogyo Kabushiki Kaisha Compose heterocyclique et agent antitumoral contenant ce dernier en tant qu'ingredient actif
GB0512324D0 (en) * 2005-06-16 2005-07-27 Novartis Ag Organic compounds
GB0423653D0 (en) * 2004-10-25 2004-11-24 Piramed Ltd Pharmaceutical compounds
CA2599320A1 (en) 2005-02-25 2006-08-31 Kudos Pharmaceuticals Limited Hydrazinomethyl, hydr zonomethyl and 5-membered heterocylic compounds which act as mtor inhibitors and their use as anti cancer agents
JP5534811B2 (ja) 2006-08-24 2014-07-02 アストラゼネカ アクチボラグ 増殖性疾患の治療に有用なモルホリノピリミジン誘導体
EP2300483A1 (en) * 2008-05-23 2011-03-30 Wyeth LLC Triazine compounds as p13 kinase and mtor inhibitors

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