JP2016512239A - Ａｔｒキナーゼの阻害剤として有用な化合物 - Google Patents

Ａｔｒキナーゼの阻害剤として有用な化合物 Download PDF

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JP2016512239A
JP2016512239A JP2016500120A JP2016500120A JP2016512239A JP 2016512239 A JP2016512239 A JP 2016512239A JP 2016500120 A JP2016500120 A JP 2016500120A JP 2016500120 A JP2016500120 A JP 2016500120A JP 2016512239 A JP2016512239 A JP 2016512239A
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compound
cancer
alkyl
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JP2016512239A5 (enExample
Inventor
ガイ ブレンチリー，
ガイ ブレンチリー，
ジーン−ダミアン シャリエ，
ジーン−ダミアン シャリエ，
クリス デイビス，
クリス デイビス，
スティーブン ドュラント，
スティーブン ドュラント，
ゴルカ エチェバリア イ ハリディ，
ゴルカ エチェバリア イ ハリディ，
ダミアン フレイス，
ダミアン フレイス，
フアン−ミゲル ヒメネス，
フアン−ミゲル ヒメネス，
ケイ，　デイビッド
デイビッド ケイ，
ネグテル，　ロナルド
ロナルド ネグテル，
フランソワーズ ピラード，
フランソワーズ ピラード，
ジョアン ピンダー，
ジョアン ピンダー，
デイビッド ショー，
デイビッド ショー，
ピエール−アンリ シュトルク，
ピエール−アンリ シュトルク，
ジョン スタッドリー，
ジョン スタッドリー，
ヘザー ツイン，
ヘザー ツイン，
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Vertex Pharmaceuticals Inc
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Vertex Pharmaceuticals Inc
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Publication of JP2016512239A publication Critical patent/JP2016512239A/ja
Publication of JP2016512239A5 publication Critical patent/JP2016512239A5/ja
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    • 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
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/357—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
    • A61K31/36—Compounds containing methylenedioxyphenyl groups, e.g. sesamin
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4188—1,3-Diazoles condensed with other heterocyclic ring systems, e.g. biotin, sorbinil
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—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
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A—HUMAN NECESSITIES
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    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
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    • 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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    • A61N—ELECTROTHERAPY; MAGNETOTHERAPY; RADIATION THERAPY; ULTRASOUND THERAPY
    • A61N5/00—Radiation therapy
    • A61N5/10—X-ray therapy; Gamma-ray therapy; Particle-irradiation therapy
    • A61N5/1001—X-ray therapy; Gamma-ray therapy; Particle-irradiation therapy using radiation sources introduced into or applied onto the body; brachytherapy
    • A61N5/1028—X-ray therapy; Gamma-ray therapy; Particle-irradiation therapy using radiation sources introduced into or applied onto the body; brachytherapy using radiation sources applied onto the body
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
    • C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
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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
    • C07D471/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
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    • C07D491/00—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
    • 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
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
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    • C12N9/10—Transferases (2.)
    • C12N9/12—Transferases (2.) transferring phosphorus containing groups, e.g. kinases (2.7)
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    • A61N2005/1085—X-ray therapy; Gamma-ray therapy; Particle-irradiation therapy characterised by the type of particles applied to the patient
    • A61N2005/1087—Ions; Protons
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    • C12Y207/00—Transferases transferring phosphorus-containing groups (2.7)
    • C12Y207/11—Protein-serine/threonine kinases (2.7.11)
    • C12Y207/11001—Non-specific serine/threonine protein kinase (2.7.11.1), i.e. casein kinase or checkpoint kinase

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  • Microbiology (AREA)
  • General Engineering & Computer Science (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic 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)
JP2016500120A 2013-03-15 2013-12-06 Ａｔｒキナーゼの阻害剤として有用な化合物 Pending JP2016512239A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361787478P 2013-03-15 2013-03-15
US61/787,478 2013-03-15
PCT/US2013/073471 WO2014143241A1 (en) 2013-03-15 2013-12-06 Compounds useful as inhibitors of atr kinase

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JP2016512239A true JP2016512239A (ja) 2016-04-25
JP2016512239A5 JP2016512239A5 (enExample) 2017-01-26

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US (2) US8957078B2 (enExample)
EP (1) EP2970289A1 (enExample)
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JP2021523104A (ja) * 2018-04-30 2021-09-02 ライボン・セラピューティクス・インコーポレイテッドＲｉｂｏｎ Ｔｈｅｒａｐｅｕｔｉｃｓ， Ｉｎｃ． Ｐａｒｐ７阻害剤としてのピリダジノン
US11691969B2 (en) 2019-10-30 2023-07-04 Ribon Therapeutics, Inc. Pyridazinones as PARP7 inhibtors
US12371421B2 (en) 2019-04-29 2025-07-29 Ribon Therapeutics, Inc. Solid forms of a PARP7 inhibitor
US12617782B2 (en) 2023-05-12 2026-05-05 Ribon Therapeutics, Inc. Pyridazinones as PARP7 inhibitors

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US9309250B2 (en) 2011-06-22 2016-04-12 Vertex Pharmaceuticals Incorporated Substituted pyrrolo[2,3-b]pyrazines as ATR kinase inhibitors
SI2941432T1 (en) 2012-12-07 2018-07-31 Vertex Pharmaceuticals Incorporated 2-AMINO-6-FLUORO-N- (5-FLUORO-4- (4- (4- (OXETHAN-3-YL) PIPERAZIN-1-CARBONYL) PIPERIDIN-1-YLIPRIDIN-3-YL) 1,5 ALFA) PYRIMIDINE-3-CARBOXAMIDE AS ATR KINAZE INHIBITOR
WO2014143240A1 (en) 2013-03-15 2014-09-18 Vertex Pharmaceuticals Incorporated Fused pyrazolopyrimidine derivatives useful as inhibitors of atr kinase
PL2991683T3 (pl) 2013-05-02 2020-03-31 Glykos Finland Oy Koniugaty glikoproteiny lub glikanu z toksycznym ładunkiem
PT3077397T (pt) 2013-12-06 2020-01-22 Vertex Pharma Composto de 2-amino-6-fluoro-n-[5-fluoro-piridin-3-il]pirazolo[1,5-a]pirimidin-3-carboxamida útil como inibidor da atr quinase, a sua preparação, diferentes formas sólidas e derivados radiomarcados do mesmo
SG11201608303QA (en) 2014-04-04 2016-11-29 Del Mar Pharmaceuticals Use of dianhydrogalactitol and analogs or derivatives thereof to treat non-small-cell carcinoma of the lung and ovarian cancer
MX373102B (es) 2014-06-05 2020-04-17 Vertex Pharma Derivados radiomarcados de un compuesto de 2-amino-6-fluoro-n-[5-fluoro-piridin-3-il]-pirazolo[1,5-a]pirimidin-3-carboxamida útil como inhibidor de ataxia telangiectasia mutada y rad3 relacionado (atr) cinasa, preparación de tal compuesto y diferentes formas sólidas del mismo.
SG11201610500WA (en) 2014-06-17 2017-01-27 Vertex Pharma Method for treating cancer using a combination of chk1 and atr inhibitors
EP3160513B1 (en) 2014-06-30 2020-02-12 Glykos Finland Oy Saccharide derivative of a toxic payload and antibody conjugates thereof
AU2016331955B2 (en) 2015-09-30 2022-07-21 Vertex Pharmaceuticals Incorporated Method for treating cancer using a combination of DNA damaging agents and ATR inhibitors
MX2018008507A (es) 2016-01-11 2019-07-04 Merrimack Pharmaceuticals Inc Inhibición de proteína relacionada con ataxia telangiectasia y rad3 (atr).
CN109311889B (zh) 2016-04-15 2021-11-16 缆图药品公司 激活素受体样激酶抑制剂
US11021514B2 (en) 2016-06-01 2021-06-01 Athira Pharma, Inc. Compounds
JOP20190197A1 (ar) 2017-02-24 2019-08-22 Bayer Pharma AG مثبط كيناز ايه تي آر للاستخدام في طريقة لعلاج مرض فرط التكاثر
TW201840319A (zh) 2017-02-24 2018-11-16 德商拜耳廠股份有限公司 Atr激酶抑制劑與鐳-223鹽之組合
WO2018153972A1 (en) 2017-02-24 2018-08-30 Bayer Pharma Aktiengesellschaft Combination of atr kinase inhibitors and antiandrogens
WO2018206547A1 (en) 2017-05-12 2018-11-15 Bayer Pharma Aktiengesellschaft Combination of bub1 and atr inhibitors
US11485733B2 (en) 2017-06-30 2022-11-01 Bayer Animal Health Gmbh Azaquinoline derivatives
US11690911B2 (en) 2017-08-04 2023-07-04 Bayer Aktiengesellschaft Combination of ATR kinase inhibitors and PD-1/PD-L1 inhibitors
EP3461480A1 (en) 2017-09-27 2019-04-03 Onxeo Combination of a dna damage response cell cycle checkpoint inhibitors and belinostat for treating cancer
EP3697786B1 (en) 2017-10-18 2022-08-31 Blueprint Medicines Corporation Substituted pyrrolopyridines as inhibitors of activin receptor-like kinase
EP3720973A1 (en) 2017-12-08 2020-10-14 Bayer Aktiengesellschaft Predictive markers for atr kinase inhibitors
CN108059631A (zh) * 2018-01-08 2018-05-22 上海方予健康医药科技有限公司 一种pim激酶抑制剂及其中间体的制备方法
KR20210066837A (ko) 2018-09-26 2021-06-07 메르크 파텐트 게엠베하 암 치료를 위한 pd-1 안타고니스트, atr 억제제 및 백금화제의 조합
WO2020078905A1 (en) 2018-10-15 2020-04-23 Merck Patent Gmbh Combination therapy utilizing dna alkylating agents and atr inhibitors
WO2020078788A1 (en) 2018-10-16 2020-04-23 Bayer Aktiengesellschaft Combination of atr kinase inhibitors with 2,3-dihydroimidazo[1,2-c]quinazoline compounds
US11345681B1 (en) 2020-06-05 2022-05-31 Kinnate Biopharma Inc. Inhibitors of fibroblast growth factor receptor kinases

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WO2003091256A1 (en) * 2002-04-23 2003-11-06 Shionogi & Co., Ltd. PYRAZOLO[1,5-a]PYRIMIDINE DERIVATIVE AND NAD(P)H OXIDASE INHIBITOR CONTAINING THE SAME
JP2009511478A (ja) * 2005-10-06 2009-03-19 シェーリング コーポレイション プロテインキナーゼインヒビターとしてのピラゾロピリミジン
JP2012507569A (ja) * 2008-10-31 2012-03-29 ジェネンテック， インコーポレイテッド ピラゾロピリミジンｊａｋ阻害剤化合物と方法
JP2012532112A (ja) * 2009-07-02 2012-12-13 ジェネンテック， インコーポレイテッド ピラゾロピリミジンｊａｋ阻害剤化合物及び方法
WO2012178124A1 (en) * 2011-06-22 2012-12-27 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase

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