PT2797888T - Ompostos tricíclicos fundidos como inibidores da quinase - Google Patents

Ompostos tricíclicos fundidos como inibidores da quinase Download PDF

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Publication number
PT2797888T
PT2797888T PT118790963T PT11879096T PT2797888T PT 2797888 T PT2797888 T PT 2797888T PT 118790963 T PT118790963 T PT 118790963T PT 11879096 T PT11879096 T PT 11879096T PT 2797888 T PT2797888 T PT 2797888T
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PT
Portugal
Prior art keywords
heteroaryl
heterocyclyl
aryl
alkyl
cycloalkyl
Prior art date
Application number
PT118790963T
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English (en)
Portuguese (pt)
Inventor
Zhou Changyou
Zhang Guoliang
Wang Shaohui
Original Assignee
Beigene Ltd
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Publication date
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Publication of PT2797888T publication Critical patent/PT2797888T/pt

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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
    • A61K31/535—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
    • A61K31/5365—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 ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • C07D405/14—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 three or more hetero 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
    • A61K31/435—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
    • 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
    • A61K31/4375—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 six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • 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
    • A61K31/44—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
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further 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
    • A61K31/495—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
    • A61K31/52—Purines, e.g. adenine
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/28—Oxygen atom
    • C07D473/30—Oxygen atom attached in position 6, e.g. hypoxanthine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • C07D519/02—Ergot alkaloids of the cyclic peptide type

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (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)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
PT118790963T 2011-12-31 2011-12-31 Ompostos tricíclicos fundidos como inibidores da quinase PT2797888T (pt)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/CN2011/085146 WO2013097224A1 (en) 2011-12-31 2011-12-31 Fused tricyclic compounds as raf kinase inhibitors

Publications (1)

Publication Number Publication Date
PT2797888T true PT2797888T (pt) 2016-09-09

Family

ID=48696279

Family Applications (1)

Application Number Title Priority Date Filing Date
PT118790963T PT2797888T (pt) 2011-12-31 2011-12-31 Ompostos tricíclicos fundidos como inibidores da quinase

Country Status (28)

Country Link
US (3) US9273046B2 (enExample)
EP (2) EP3124472B1 (enExample)
JP (1) JP5868521B2 (enExample)
KR (1) KR101713391B1 (enExample)
CN (1) CN103596926B (enExample)
AU (1) AU2011384857B2 (enExample)
BR (1) BR112014013108B1 (enExample)
CA (1) CA2856347C (enExample)
CY (1) CY1118226T1 (enExample)
DK (1) DK2797888T3 (enExample)
EA (1) EA025597B1 (enExample)
ES (1) ES2588775T3 (enExample)
HR (1) HRP20160641T1 (enExample)
HU (1) HUE029656T2 (enExample)
IL (1) IL233364A (enExample)
IN (1) IN2014DN06166A (enExample)
LT (1) LT2797888T (enExample)
ME (1) ME02529B (enExample)
MX (1) MX352617B (enExample)
NZ (1) NZ624068A (enExample)
PL (1) PL2797888T3 (enExample)
PT (1) PT2797888T (enExample)
RS (1) RS55196B1 (enExample)
SG (1) SG11201401725SA (enExample)
SI (1) SI2797888T1 (enExample)
SM (1) SMT201600302B (enExample)
WO (1) WO2013097224A1 (enExample)
ZA (1) ZA201405555B (enExample)

Families Citing this family (26)

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DK2797888T3 (en) 2011-12-31 2016-09-19 Beigene Ltd Fused tricyclic compounds as RAF kinase inhibitors
WO2014206344A1 (en) 2013-06-28 2014-12-31 Beigene, Ltd. Fused tricyclic amide compounds as multiple kinase inhibitors
WO2014206343A1 (en) 2013-06-28 2014-12-31 Beigene, Ltd. Fused tricyclic urea compounds as raf kinase and/or raf kinase dimer inhibitors
WO2015089809A1 (en) * 2013-12-19 2015-06-25 Merck Sharp & Dohme Corp. Antidiabetic substituted heteroaryl compounds
WO2015176267A1 (en) * 2014-05-22 2015-11-26 Merck Sharp & Dohme Corp. Antidiabetic tricyclic compounds
GB201416186D0 (en) * 2014-09-12 2014-10-29 Redx Pharma Ltd Compounds
AU2016248376B2 (en) * 2015-04-15 2020-10-08 Beone Medicines I Gmbh Maleate salts of a B-RAF kinase inhibitor, crystalline forms, methods of preparation, and uses therefore
JP6175519B2 (ja) * 2016-01-04 2017-08-09 ベイジーン リミテッド Rafキナーゼ阻害剤としての縮合三環式化合物
WO2018007885A1 (en) * 2016-07-05 2018-01-11 Beigene, Ltd. COMBINATION OF A PD-l ANTAGONIST AND A RAF INHIBITOR FOR TREATING CANCER
IL266842B (en) 2016-12-01 2022-09-01 Arvinas Operations Inc History of tetrahydronaphthalene and tetrahydroisoquinoline as estrogen receptor antagonists
IL325835A (en) * 2016-12-23 2026-03-01 Univ Yale Compounds and methods for the targeted degradation of rapidly accelerated fibrosarcoma polypeptides
US11173211B2 (en) 2016-12-23 2021-11-16 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides
IL319363A (en) 2017-01-31 2025-05-01 Arvinas Operations Inc Cervalon ligands and bifunctional compounds containing them
US12208099B2 (en) 2018-09-10 2025-01-28 Mirati Therapeutics, Inc. Combination therapies
TWI849043B (zh) 2019-01-25 2024-07-21 英屬開曼群島商百濟神州有限公司 B-raf激酶二聚體抑制劑之穩定固體分散體、製備方法及其用途
CN111184693B (zh) * 2019-05-29 2023-07-21 百济神州(苏州)生物科技有限公司 一种raf激酶抑制剂制剂及其制备方法
WO2021041348A1 (en) 2019-08-26 2021-03-04 Arvinas Operations, Inc. Methods of treating breast cancer with tetrahydronaphthalene derivatives as estrogen receptor degraders
WO2021127443A1 (en) 2019-12-19 2021-06-24 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor
US11858930B2 (en) 2020-07-28 2024-01-02 Jazz Pharmaceuticals Ireland Limited Fused bicyclic RAF inhibitors and methods for use thereof
WO2022047145A1 (en) 2020-08-28 2022-03-03 Arvinas Operations, Inc. Rapidly accelerating fibrosarcoma protein degrading compounds and associated methods of use
AU2021342287A1 (en) 2020-09-14 2023-04-13 Arvinas Operations, Inc. Crystalline forms of a compound for the targeted degradation of estrogen receptor
AU2021412688B2 (en) * 2020-12-29 2025-06-12 Txinno Bioscience Inc. Novel naphthyridinone derivative having inhibitory activity against ectonucleotide pyrophosphatase-phosphodiesterase and use thereof
WO2023049060A1 (en) * 2021-09-21 2023-03-30 Merck Sharp & Dohme Llc Allosteric modulators of nicotinic acetylcholine receptors
WO2023209611A1 (en) 2022-04-26 2023-11-02 Beigene Switzerland Gmbh Methods of treating cancer with a b-raf inhibitor, in particular lifirafenib
WO2023212071A1 (en) * 2022-04-26 2023-11-02 Beigene Switzerland Gmbh Combination and the use thereof
EP4584258A1 (en) 2022-09-07 2025-07-16 Arvinas Operations, Inc. Rapidly accelerated fibrosarcoma (raf) degrading compounds and associated methods of use

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AU2003245700A1 (en) 2002-02-12 2003-09-04 Glaxo Group Limited Pyrazolopyridine derivatives
JP5138938B2 (ja) 2003-12-19 2013-02-06 プレキシコン インコーポレーテッド Ret調節剤の開発のための化合物および方法
US7767687B2 (en) * 2004-12-13 2010-08-03 Biogen Idec Ma Inc. Pyrido pyrimidinones, dihydro pyrimido pyrimidinones and pteridinones useful as RAF kinase inhibitors
EP1833829A2 (en) 2004-12-23 2007-09-19 F. Hoffmann-Roche AG Benzamide substituted imidazo- and pyrrolo-pyridines as protein kinase inhibitors
TW200639163A (en) 2005-02-04 2006-11-16 Genentech Inc RAF inhibitor compounds and methods
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BRPI0716477A2 (pt) 2006-09-06 2014-03-18 Hoffmann La Roche Derivados heteroarila como inibidores de quinase protéica
JP2010502706A (ja) * 2006-09-07 2010-01-28 ミレニアム・ファーマシューティカルズ・インコーポレイテッド キナーゼ阻害活性を有するフェネチルアミド誘導体
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PE20121126A1 (es) 2006-12-21 2012-08-24 Plexxikon Inc Compuestos pirrolo [2,3-b] piridinas como moduladores de quinasa
CA2686379A1 (en) * 2007-05-04 2008-11-13 Irm Llc Phenylaminopyrimidine derivatives and compositions thereof as c-kit and pdgfr kinase inhibitors
JP2010533729A (ja) 2007-07-17 2010-10-28 プレキシコン,インコーポレーテッド キナーゼ調節のための化合物と方法、及びそのための適応
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DK2797888T3 (en) 2011-12-31 2016-09-19 Beigene Ltd Fused tricyclic compounds as RAF kinase inhibitors
AU2016248376B2 (en) 2015-04-15 2020-10-08 Beone Medicines I Gmbh Maleate salts of a B-RAF kinase inhibitor, crystalline forms, methods of preparation, and uses therefore

Also Published As

Publication number Publication date
BR112014013108B1 (pt) 2020-11-24
CN103596926B (zh) 2015-11-25
AU2011384857A1 (en) 2014-05-29
EP3124472B1 (en) 2018-07-25
US10576087B2 (en) 2020-03-03
SI2797888T1 (sl) 2017-01-31
HK1192232A1 (zh) 2014-08-15
BR112014013108A2 (pt) 2017-06-13
EP3124472A1 (en) 2017-02-01
HUE029656T2 (en) 2017-03-28
ME02529B (me) 2017-02-20
US9895376B2 (en) 2018-02-20
AU2011384857B2 (en) 2016-03-03
KR20140108541A (ko) 2014-09-11
DK2797888T3 (en) 2016-09-19
PL2797888T3 (pl) 2016-12-30
JP5868521B2 (ja) 2016-02-24
CA2856347A1 (en) 2013-07-04
US20190000857A1 (en) 2019-01-03
MX352617B (es) 2017-12-01
EA201491305A1 (ru) 2015-04-30
US20150045355A1 (en) 2015-02-12
IL233364A (en) 2017-06-29
US20160206621A1 (en) 2016-07-21
CN103596926A (zh) 2014-02-19
SMT201600302B (it) 2016-11-10
HK1221222A1 (zh) 2017-05-26
RS55196B1 (sr) 2017-01-31
SG11201401725SA (en) 2014-09-26
LT2797888T (lt) 2016-10-10
HRP20160641T1 (hr) 2016-09-23
EA025597B1 (ru) 2017-01-30
ZA201405555B (en) 2015-10-28
NZ624068A (en) 2016-09-30
US9273046B2 (en) 2016-03-01
IN2014DN06166A (enExample) 2015-08-21
IL233364A0 (en) 2014-08-31
ES2588775T3 (es) 2016-11-04
EP2797888A4 (en) 2015-09-02
WO2013097224A1 (en) 2013-07-04
EP2797888A1 (en) 2014-11-05
EP2797888B1 (en) 2016-06-08
KR101713391B1 (ko) 2017-03-07
CY1118226T1 (el) 2017-06-28
JP2015506353A (ja) 2015-03-02
CA2856347C (en) 2017-05-30
MX2014007829A (es) 2014-08-01

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