JP6186440B2 - キナーゼ阻害剤としてのジヒドロピロリジノピリミジン - Google Patents

キナーゼ阻害剤としてのジヒドロピロリジノピリミジン Download PDF

Info

Publication number
JP6186440B2
JP6186440B2 JP2015533126A JP2015533126A JP6186440B2 JP 6186440 B2 JP6186440 B2 JP 6186440B2 JP 2015533126 A JP2015533126 A JP 2015533126A JP 2015533126 A JP2015533126 A JP 2015533126A JP 6186440 B2 JP6186440 B2 JP 6186440B2
Authority
JP
Japan
Prior art keywords
alkyl
cancer
cycloalkyl
membered
mmol
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
JP2015533126A
Other languages
English (en)
Japanese (ja)
Other versions
JP2015529248A5 (enExample
JP2015529248A (ja
Inventor
ディロン,ミッチェル,パトリック
リンドヴァール,ミカ
プーン,ダニエル
ラマーシー,サビスリ
ラウニヤー,ビベック
シェーファー,シンシア
スブラマニアン,シャラドハ
タナー,フー
Original Assignee
ノバルティス アーゲー
ノバルティス アーゲー
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 ノバルティス アーゲー, ノバルティス アーゲー filed Critical ノバルティス アーゲー
Publication of JP2015529248A publication Critical patent/JP2015529248A/ja
Publication of JP2015529248A5 publication Critical patent/JP2015529248A5/ja
Application granted granted Critical
Publication of JP6186440B2 publication Critical patent/JP6186440B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/527Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim spiro-condensed
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/34Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members 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
    • C07D207/36Oxygen or sulfur atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/10Spiro-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
JP2015533126A 2012-09-19 2013-09-17 キナーゼ阻害剤としてのジヒドロピロリジノピリミジン Active JP6186440B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261702981P 2012-09-19 2012-09-19
US61/702,981 2012-09-19
PCT/US2013/060032 WO2014047020A1 (en) 2012-09-19 2013-09-17 Dihydropyrrolidino-pyrimidines as kinase inhibitors

Publications (3)

Publication Number Publication Date
JP2015529248A JP2015529248A (ja) 2015-10-05
JP2015529248A5 JP2015529248A5 (enExample) 2017-08-17
JP6186440B2 true JP6186440B2 (ja) 2017-08-23

Family

ID=49274870

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2015533126A Active JP6186440B2 (ja) 2012-09-19 2013-09-17 キナーゼ阻害剤としてのジヒドロピロリジノピリミジン

Country Status (13)

Country Link
US (1) US9546173B2 (enExample)
EP (1) EP2897961B1 (enExample)
JP (1) JP6186440B2 (enExample)
KR (1) KR20150056550A (enExample)
CN (1) CN104640865B (enExample)
AU (1) AU2013318283A1 (enExample)
BR (1) BR112015005982A2 (enExample)
CA (1) CA2882410A1 (enExample)
EA (1) EA201590600A1 (enExample)
ES (1) ES2612885T3 (enExample)
IN (1) IN2015DN01328A (enExample)
MX (1) MX2015003535A (enExample)
WO (1) WO2014047020A1 (enExample)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR112015005982A2 (pt) * 2012-09-19 2017-07-04 Novartis Ag di-hidropirrolidino-pirimidinas como inibidores de quinase
CN112334192A (zh) * 2018-07-12 2021-02-05 Ucb生物制药有限责任公司 作为il-17调节剂的螺环茚满类似物
WO2020243457A1 (en) * 2019-05-29 2020-12-03 Viogen Biosciences, Llc Compounds and therapeutic uses thereof
EP4007632A1 (en) * 2019-08-01 2022-06-08 Praetego, Inc. Inhibitors of advanced glycation end products
UA128299C2 (uk) 2019-12-10 2024-05-29 Ф. Хоффманн-Ля Рош Аг Нові похідні метилхіназолінону
WO2021116050A1 (en) * 2019-12-10 2021-06-17 F. Hoffmann-La Roche Ag New braf inhibitors as paradox breakers
JP7296017B2 (ja) * 2020-04-30 2023-06-21 メッドシャイン ディスカバリー インコーポレイテッド ベンゾスルタムを含む化合物

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004078163A2 (en) 2003-02-28 2004-09-16 Transform Pharmaceuticals, Inc. Pharmaceutical co-crystal compositions of drugs such as carbamazepine, celecoxib, olanzapine, itraconazole, topiramate, modafinil, 5-fluorouracil, hydrochlorothiazide, acetaminophen, aspirin, flurbiprofen, phenytoin and ibuprofen
ATE451369T1 (de) * 2002-07-15 2009-12-15 Merck & Co Inc Piperidinopyrimidindipeptidylpeptidaseinhibitor n zur behandlung von diabetes
WO2005068468A2 (en) * 2003-12-02 2005-07-28 Vertex Pharmaceuticals, Inc. Heterocyclic protein kinase inhibitors and uses thereof
PE20060426A1 (es) 2004-06-02 2006-06-28 Schering Corp DERIVADOS DE ACIDO TARTARICO COMO INHIBIDORES DE MMPs, ADAMs, TACE Y TNF-alfa
SI1838718T1 (sl) 2005-01-10 2011-08-31 Pfizer Pirolopirazoli, zmogljivi inhibitorji kinaze
RU2442778C9 (ru) 2005-12-13 2012-08-10 Шеринг Корпорейшн Новые соединения, действующие как ингибиторы erk
TW200911262A (en) 2007-06-05 2009-03-16 Schering Corp Novel compounds that are ERK inhibitors
WO2012030685A2 (en) 2010-09-01 2012-03-08 Schering Corporation Indazole derivatives useful as erk inhibitors
US9242981B2 (en) * 2010-09-16 2016-01-26 Merck Sharp & Dohme Corp. Fused pyrazole derivatives as novel ERK inhibitors
RU2013126036A (ru) 2010-11-17 2014-12-27 Ф. Хоффманн-Ля Рош Аг Способ лечения опухолей
KR101961500B1 (ko) 2011-02-28 2019-03-22 어레이 바이오파마 인크. 세린/트레오닌 키나제 억제제
EP2820017B1 (en) 2012-03-02 2016-12-21 Genentech, Inc. Pyridinyl and pyrimidinyl sulfoxide and sulfone derivatives
BR112015005982A2 (pt) * 2012-09-19 2017-07-04 Novartis Ag di-hidropirrolidino-pirimidinas como inibidores de quinase

Also Published As

Publication number Publication date
ES2612885T3 (es) 2017-05-19
CA2882410A1 (en) 2014-03-27
AU2013318283A1 (en) 2015-03-05
WO2014047020A1 (en) 2014-03-27
CN104640865A (zh) 2015-05-20
JP2015529248A (ja) 2015-10-05
IN2015DN01328A (enExample) 2015-07-03
CN104640865B (zh) 2018-05-11
BR112015005982A2 (pt) 2017-07-04
EP2897961B1 (en) 2016-10-26
US9546173B2 (en) 2017-01-17
KR20150056550A (ko) 2015-05-26
US20150274733A1 (en) 2015-10-01
MX2015003535A (es) 2015-07-14
EA201590600A1 (ru) 2015-07-30
EP2897961A1 (en) 2015-07-29

Similar Documents

Publication Publication Date Title
CN104379575B (zh) 用于调节egfr活性的化合物和组合物
JP6186440B2 (ja) キナーゼ阻害剤としてのジヒドロピロリジノピリミジン
CA2828478A1 (en) Serine/threonine kinase inhibitors
CN116685585A (zh) 一种高活性的hpk1激酶抑制剂
TW202523326A (zh) 雜環及其用途
EP3840747B1 (en) Novel aryloxypiperidine pyrazole compounds as indoleamine 2,3-dioxygenase inhibitors
AU2016349148C1 (en) 1,4-dicarbonyl-piperidyl derivatives
TW202220998A (zh) 雜芳基雜環化合物及其用途
CN116848115B (zh) Wnt通路抑制剂化合物
JP2025527934A (ja) ピラゾリルスルホンアミド化合物、及び療法におけるそれらの使用
WO2024044344A1 (en) Pyridinylsulfonamide compounds and their use in therapy
TWI768781B (zh) 轉化生長因子-β受體抑制劑
TW202304906A (zh) 高活性hpk1激酶抑制劑
WO2025072437A1 (en) Heteroaryl compounds and their use in treating medical conditions
CA2989684C (en) Hpk1 inhibitors and methods of using same
HK40094658A (zh) 杂芳基杂环化合物及其用途
HK40094658B (zh) 杂芳基杂环化合物及其用途
WO2024059559A1 (en) Isothiazolylcarboxamide compounds and their use in therapy
WO2025117672A1 (en) Indazolyl-piperidine sulfonamides and related compounds and their use in therapy
EP4536642A1 (en) Heterocyclic compounds as pi3ka inhibitors
HK40091563B (zh) 嘧啶酮类化合物及其用途
HK40091563A (zh) 嘧啶酮类化合物及其用途
JP2023538097A (ja) ピリミジノン化合物およびその使用

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20160708

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20160708

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20170418

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20170420

A524 Written submission of copy of amendment under article 19 pct

Free format text: JAPANESE INTERMEDIATE CODE: A524

Effective date: 20170705

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20170718

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20170731

R150 Certificate of patent or registration of utility model

Ref document number: 6186440

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250