JP2013534233A - 選択的ｊａｋ阻害剤としてのヘテロシクリルピラゾロピリミジン類似体 - Google Patents

選択的ｊａｋ阻害剤としてのヘテロシクリルピラゾロピリミジン類似体 Download PDF

Info

Publication number
JP2013534233A
JP2013534233A JP2013524421A JP2013524421A JP2013534233A JP 2013534233 A JP2013534233 A JP 2013534233A JP 2013524421 A JP2013524421 A JP 2013524421A JP 2013524421 A JP2013524421 A JP 2013524421A JP 2013534233 A JP2013534233 A JP 2013534233A
Authority
JP
Japan
Prior art keywords
methyl
pyrazol
pyrazolo
pyrimidin
amino
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.)
Pending
Application number
JP2013524421A
Other languages
English (en)
Japanese (ja)
Other versions
JP2013534233A5 (enExample
Inventor
キャスリン ベル
ネリー ピトン
クラウディオ ダゴースティン
シリル ブウサール
アンドリュー ラトクリフ
ナイジェル ラムスデン
Original Assignee
セルゾーム リミティッド
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
Priority claimed from PCT/EP2010/065700 external-priority patent/WO2011048082A1/en
Application filed by セルゾーム リミティッド filed Critical セルゾーム リミティッド
Publication of JP2013534233A publication Critical patent/JP2013534233A/ja
Publication of JP2013534233A5 publication Critical patent/JP2013534233A5/ja
Pending legal-status Critical Current

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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic 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
    • 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
    • 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
    • C07D498/08—Bridged 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Pulmonology (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
JP2013524421A 2010-08-20 2011-08-12 選択的ｊａｋ阻害剤としてのヘテロシクリルピラゾロピリミジン類似体 Pending JP2013534233A (ja)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US37535810P 2010-08-20 2010-08-20
US61/375,358 2010-08-20
EPPCT/EP2010/065700 2010-10-19
PCT/EP2010/065700 WO2011048082A1 (en) 2009-10-20 2010-10-19 Heterocyclyl pyrazolopyrimidine analogues as jak inhibitors
US201161476398P 2011-04-18 2011-04-18
US61/476,398 2011-04-18
PCT/EP2011/063905 WO2012022681A2 (en) 2010-08-20 2011-08-12 Heterocyclyl pyrazolopyrimidine analogues as selective jak inhibitors

Publications (2)

Publication Number Publication Date
JP2013534233A true JP2013534233A (ja) 2013-09-02
JP2013534233A5 JP2013534233A5 (enExample) 2014-10-30

Family

ID=44630379

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2013524421A Pending JP2013534233A (ja) 2010-08-20 2011-08-12 選択的ｊａｋ阻害剤としてのヘテロシクリルピラゾロピリミジン類似体

Country Status (3)

Country Link
US (1) US9040545B2 (enExample)
JP (1) JP2013534233A (enExample)
WO (1) WO2012022681A2 (enExample)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2017503843A (ja) * 2014-01-24 2017-02-02 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ Ｎ−［（３−アミノオキセタン−３−イル）メチル］−２−（１，１−ジオキソ−３，５−ジヒドロ−１，４−ベンゾチアゼピン−４−イル）−６−メチル−キナゾリン−４−アミンの製造のための方法
JP2019525962A (ja) * 2016-07-29 2019-09-12 ラプト・セラピューティクス・インコーポレイテッド ケモカイン受容体調節剤及びそれの使用

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013041605A1 (en) 2011-09-20 2013-03-28 Cellzome Limited Pyrazolo[4,3-c]pyridine derivatives as kinase inhibitors
AU2012357038B2 (en) 2011-12-23 2016-05-12 Cellzome Limited Pyrimidine-2,4-diamine derivatives as kinase inhibitors
US10117430B2 (en) 2012-12-14 2018-11-06 Basf Se Malononitrile compounds for controlling animal pests
ES2765405T3 (es) 2014-04-17 2020-06-09 Boehringer Ingelheim Animal Health Usa Inc Utilización de compuestos de malononitrilo para proteger animales de parásitos
NO2721710T3 (enExample) 2014-08-21 2018-03-31
CN110885331B (zh) * 2018-09-11 2021-07-09 中国药科大学 一种6-氨基-1H-吡唑并[3，4-d]嘧啶类JAK激酶抑制剂的制备与应用
WO2020092015A1 (en) 2018-11-02 2020-05-07 University Of Rochester Therapeutic mitigation of epithelial infection
JP7696834B2 (ja) * 2019-05-27 2025-06-23 ディザル（ジァンスー）ファーマシューティカル・カンパニー・リミテッド Ｄｎａ依存性タンパク質キナーゼ阻害剤
WO2023178001A1 (en) * 2022-03-17 2023-09-21 Pfizer Inc. Methods, dosage regimens, and compositions for treating hidradenitis
WO2025235331A1 (en) * 2024-05-07 2025-11-13 Nikang Therapeutics, Inc. Bifunctional compounds containing pyrazolopyrimidine derivatives for degrading certain cyclin-dependent kinase via ubiquitin proteasome pathway

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008094602A2 (en) * 2007-01-30 2008-08-07 Biogen Idec Ma Inc. 1-h-pyrazolo (3,4b) pyrimidine derivatives and their use as modulators of mitotic kinases
WO2009098236A1 (en) * 2008-02-06 2009-08-13 Novartis Ag Pyrrolo [2, 3-d] pyridines and use thereof as tyrosine kinase inhibitors
JP2013508332A (ja) * 2009-10-20 2013-03-07 セルゾーム リミティッド Ｊａｋ阻害剤としてのヘテロシクリルピラゾロピリミジン類似体

Family Cites Families (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE69837529T2 (de) 1997-02-12 2007-07-26 Electrophoretics Ltd., Cobham Proteinmarker für lungenkrebs und deren verwendung
GB9714249D0 (en) 1997-07-08 1997-09-10 Angiogene Pharm Ltd Vascular damaging agents
BRPI0017548B8 (pt) 1999-02-10 2023-05-02 Astrazeneca Ab Composto
EE05330B1 (et) 1999-11-05 2010-08-16 Astrazeneca Ab Kinasoliini derivaadid kui VEGF-i inhibiitorid
CZ303875B6 (cs) 1999-12-10 2013-06-05 Pfizer Products Inc. Pyrrolo[2,3-d]pyrimidinová sloucenina a farmaceutická kompozice s jejím obsahem
US6573293B2 (en) 2000-02-15 2003-06-03 Sugen, Inc. Pyrrole substituted 2-indolinone protein kinase inhibitors
AU2006205851A1 (en) * 2005-01-14 2006-07-20 Janssen Pharmaceutica N.V. 5-membered annelated heterocyclic pyrimidines as kinase inhibitors
CA2611365C (en) 2005-06-14 2014-02-11 Cellzome Ag Process for the identification of novel enzyme interacting compounds
GB0605691D0 (en) 2006-03-21 2006-05-03 Novartis Ag Organic Compounds
DK1862802T3 (da) 2006-06-01 2009-04-14 Cellzome Ag Fremgangsmåde til identifikation af med ZAP-70 vekselvirkende molekyler og til rensning af ZAP-70
EP2046759A1 (en) 2006-07-21 2009-04-15 Novartis AG 2, 4 -di (arylaminio) -pyrimidine-5-carboxamide compounds as jak kinases inhibitors
BRPI0622030A2 (pt) 2006-11-16 2014-04-22 Pharmacopeia Llc Derivados de purina 7-substituída, para imunossupressão
WO2008118822A1 (en) 2007-03-23 2008-10-02 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
US7834024B2 (en) 2007-03-26 2010-11-16 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the JAK pathway
JP2010532756A (ja) 2007-07-06 2010-10-14 オーエスアイ・ファーマスーティカルズ・インコーポレーテッド ｍＴＯＲＣ１及びｍＴＯＲＣ２の両方の阻害剤を含む組み合わせ抗癌療法
CL2009001884A1 (es) 2008-10-02 2010-05-14 Incyte Holdings Corp Uso de 3-ciclopentil-3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il)propanonitrilo, inhibidor de janus quinasa, y uso de una composición que lo comprende para el tratamiento del ojo seco.
WO2010118986A1 (en) 2009-04-14 2010-10-21 Cellzome Limited Fluoro substituted pyrimidine compounds as jak3 inhibitors
US8637529B2 (en) 2010-06-11 2014-01-28 AbbYie Inc. Pyrazolo[3,4-d]pyrimidine compounds

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008094602A2 (en) * 2007-01-30 2008-08-07 Biogen Idec Ma Inc. 1-h-pyrazolo (3,4b) pyrimidine derivatives and their use as modulators of mitotic kinases
WO2009098236A1 (en) * 2008-02-06 2009-08-13 Novartis Ag Pyrrolo [2, 3-d] pyridines and use thereof as tyrosine kinase inhibitors
JP2013508332A (ja) * 2009-10-20 2013-03-07 セルゾーム リミティッド Ｊａｋ阻害剤としてのヘテロシクリルピラゾロピリミジン類似体

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2017503843A (ja) * 2014-01-24 2017-02-02 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ Ｎ−［（３−アミノオキセタン−３−イル）メチル］−２−（１，１−ジオキソ−３，５−ジヒドロ−１，４−ベンゾチアゼピン−４−イル）−６−メチル−キナゾリン−４−アミンの製造のための方法
US10253022B2 (en) 2014-01-24 2019-04-09 Hoffmann-La Roche Inc. Process for the preparation of N-[(3-aminooxetan-3-yl) methyl]-2-(1,1-dioxo-3,5-dihydro-1,4-benzothiazepin-4-yl)-6-methyl-quinazolin-4-amine
JP2019525962A (ja) * 2016-07-29 2019-09-12 ラプト・セラピューティクス・インコーポレイテッド ケモカイン受容体調節剤及びそれの使用

Also Published As

Publication number Publication date
WO2012022681A2 (en) 2012-02-23
US9040545B2 (en) 2015-05-26
WO2012022681A3 (en) 2013-01-31
US20130190292A1 (en) 2013-07-25

Similar Documents

Publication Publication Date Title
JP5744887B2 (ja) Ｊａｋ阻害剤としてのヘテロシクリルピラゾロピリミジン類似体
JP2013534233A (ja) 選択的ｊａｋ阻害剤としてのヘテロシクリルピラゾロピリミジン類似体
JP2013525392A (ja) Ｊａｋ阻害剤としてのピラゾール化合物
CN103781780B (zh) 作为jak抑制剂的杂环基嘧啶类似物
JP6197031B2 (ja) Ｔｙｋ２阻害剤としてのヘテロシクリルピリミジン類似体
US20140323504A1 (en) Pyrazolo[4,3-c]Pyridine Derivatives As Kinase Inhibitors
US20130143915A1 (en) Triazolopyridines as tyk2 inhibitors
WO2013017480A1 (en) Pyrazolo[4,3-c]pyridine derivatives as jak inhibitors
US20150005281A1 (en) Pyrimidine-2,4-diamine derivatives as kinase inhibitors
EP2406258B1 (en) PYRIMIDINE DERIVATIVES AS mTOR INHIBITORS
WO2012143320A1 (en) (7h-pyrrolo[2,3-d]pyrimidin-2-yl)amine compounds as jak3 inhibitors
WO2013017479A1 (en) Pyrazolo[4,3-c]pyridine derivatives as jak inhibitors
RU2564419C1 (ru) Гетероциклические аналоги пиримидина в качестве ингибиторов jak
EP2606050A2 (en) Heterocyclyl pyrazolopyrimidine analogues as selective jak inhibitors
AU2011246596A1 (en) Pyrazole compounds as JAK inhibitors

Legal Events

Date Code Title Description
RD03 Notification of appointment of power of attorney

Free format text: JAPANESE INTERMEDIATE CODE: A7423

Effective date: 20130606

RD04 Notification of resignation of power of attorney

Free format text: JAPANESE INTERMEDIATE CODE: A7424

Effective date: 20130606

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20140812

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20140908

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20150521

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20150526

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20150825

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20160129