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 (OSRAM
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

    • 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
    • A61K31/395—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
    • A61K31/495—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
    • A61K31/527—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim spiro-condensed
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic 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
    • C07D207/30—Heterocyclic 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
    • C07D207/34—Heterocyclic 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
    • C07D207/36—Oxygen or sulfur atoms
    • 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
    • C07D487/10—Spiro-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (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 (OSRAM) 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 (OSRAM)
EP (1) EP2897961B1 (OSRAM)
JP (1) JP6186440B2 (OSRAM)
KR (1) KR20150056550A (OSRAM)
CN (1) CN104640865B (OSRAM)
AU (1) AU2013318283A1 (OSRAM)
BR (1) BR112015005982A2 (OSRAM)
CA (1) CA2882410A1 (OSRAM)
EA (1) EA201590600A1 (OSRAM)
ES (1) ES2612885T3 (OSRAM)
IN (1) IN2015DN01328A (OSRAM)
MX (1) MX2015003535A (OSRAM)
WO (1) WO2014047020A1 (OSRAM)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2897961B1 (en) * 2012-09-19 2016-10-26 Novartis AG Dihydropyrrolidino-pyrimidines as kinase inhibitors
JP7349491B2 (ja) 2018-07-12 2023-09-22 ユーシービー バイオファルマ エスアールエル Ｉｌ－１７モジュレーターとしてのスピロ環状インダン類似体
WO2020243457A1 (en) * 2019-05-29 2020-12-03 Viogen Biosciences, Llc Compounds and therapeutic uses thereof
CN114502546A (zh) * 2019-08-01 2022-05-13 普拉特戈公司 晚期糖基化终产物的抑制剂
WO2021116055A1 (en) 2019-12-10 2021-06-17 F. Hoffmann-La Roche Ag New methylquinazolinone derivatives
MX2022006711A (es) * 2019-12-10 2022-07-12 Hoffmann La Roche Nuevos inhibidores de braf como rompedores de la paradoja.
WO2021218912A1 (zh) 2020-04-30 2021-11-04 南京明德新药研发有限公司 含苯基并内磺酰胺的化合物

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7208498B2 (en) * 2002-07-15 2007-04-24 Merck & Co., Inc. Piperidino pyrimidine dipeptidyl peptidase inhibitors for the treatment of diabetes
JP2007524596A (ja) 2003-02-28 2007-08-30 トランスフォーム・ファーマシューティカルズ・インコーポレイテッド 共結晶医薬組成物
US7244735B2 (en) * 2003-12-02 2007-07-17 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
AP2007004061A0 (en) 2005-01-10 2007-08-31 Galloway & Company Pyrrolopyrazoles, potent kinase inhibitors
CA2633023C (en) 2005-12-13 2015-11-24 Schering Corporation Polycyclic indazole derivatives that are erk inhibitors
KR20100025553A (ko) 2007-06-05 2010-03-09 쉐링 코포레이션 암 치료용 ｅｒｋ 억제제로서의 폴리사이클릭 인다졸 유도체 및 이의 용도
US8946216B2 (en) 2010-09-01 2015-02-03 Merck Sharp & Dohme Corp. Indazole derivatives useful as ERK inhibitors
EP2615916B1 (en) * 2010-09-16 2017-01-04 Merck Sharp & Dohme Corp. Fused pyrazole derivatives as novel erk inhibitors
KR20130121122A (ko) 2010-11-17 2013-11-05 에프. 호프만-라 로슈 아게 종양의 치료 방법
CA2828478C (en) * 2011-02-28 2019-12-31 Array Biopharma Inc. Serine/threonine kinase inhibitors
AU2013225531A1 (en) 2012-03-02 2014-09-25 Forma Tm, Llc. Pyridinyl and pyrimidinyl sulfoxide and sulfone derivatives
EP2897961B1 (en) * 2012-09-19 2016-10-26 Novartis AG Dihydropyrrolidino-pyrimidines as kinase inhibitors

Also Published As

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

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
KR20210044822A (ko) 피롤로피리미딘 itk 억제제
CA2828478A1 (en) Serine/threonine kinase inhibitors
CN116685585A (zh) 一种高活性的hpk1激酶抑制剂
WO2021060453A1 (ja) 架橋型光学活性２級アミン誘導体
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
TW202523326A (zh) 雜環及其用途
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
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
WO2024059524A1 (en) Pyrazolylcarboxamide compounds and their use in therapy
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