JP5985473B2 - ＩＲＡＫ４モジュレーターとしてのピラゾロ［１，５ａ］ピリミジン及びチエノ［３，２ｂ］ピリミジン誘導体 - Google Patents

ＩＲＡＫ４モジュレーターとしてのピラゾロ［１，５ａ］ピリミジン及びチエノ［３，２ｂ］ピリミジン誘導体 Download PDF

Info

Publication number
JP5985473B2
JP5985473B2 JP2013519044A JP2013519044A JP5985473B2 JP 5985473 B2 JP5985473 B2 JP 5985473B2 JP 2013519044 A JP2013519044 A JP 2013519044A JP 2013519044 A JP2013519044 A JP 2013519044A JP 5985473 B2 JP5985473 B2 JP 5985473B2
Authority
JP
Japan
Prior art keywords
hydroxy
phenyl
chloro
amino
pyrimidine
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.)
Expired - Fee Related
Application number
JP2013519044A
Other languages
English (en)
Japanese (ja)
Other versions
JP2013531018A (ja
JP2013531018A5 (enExample
Inventor
アローラ，ニディ
チェン，シャオチーン
ヘルマン，ヨハネス・コーネリウス
クーグルシュタッター，アンドレアス
ラバディー，シャラダ・シェンヴィ
リン，クララ・ジウ・ジェン
ルーカス，マシュー・シー
ムーア，エイミー・ジェラルディン
パップ，エヴァ
タラマス，フランシスコ・ザヴィエル
ヴァンナー，ユッタ
ジャイ，ヤンシェン
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
F Hoffmann La Roche AG
Original Assignee
F Hoffmann La Roche AG
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 F Hoffmann La Roche AG filed Critical F Hoffmann La Roche AG
Publication of JP2013531018A publication Critical patent/JP2013531018A/ja
Publication of JP2013531018A5 publication Critical patent/JP2013531018A5/ja
Application granted granted Critical
Publication of JP5985473B2 publication Critical patent/JP5985473B2/ja
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • A61K31/4365—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 having sulfur as a ring hetero atom, e.g. ticlopidine
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/12—Antidiarrhoeals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/08—Bronchodilators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • 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
    • 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
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (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)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • Dermatology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Virology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
JP2013519044A 2010-07-13 2011-07-08 ＩＲＡＫ４モジュレーターとしてのピラゾロ［１，５ａ］ピリミジン及びチエノ［３，２ｂ］ピリミジン誘導体 Expired - Fee Related JP5985473B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US36385510P 2010-07-13 2010-07-13
US61/363,855 2010-07-13
US201161485145P 2011-05-12 2011-05-12
US61/485,145 2011-05-12
PCT/EP2011/061598 WO2012007375A1 (en) 2010-07-13 2011-07-08 Pyrazolo [1, 5a] pyrimidine and thieno [3, 2b] pyrimidine derivatives as irak4 modulators

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2016151041A Division JP6396376B2 (ja) 2010-07-13 2016-08-01 ＩＲＡＫ４モジュレーターとしてのピラゾロ［１，５ａ］ピリミジン及びチエノ［３，２ｂ］ピリミジン誘導体

Publications (3)

Publication Number Publication Date
JP2013531018A JP2013531018A (ja) 2013-08-01
JP2013531018A5 JP2013531018A5 (enExample) 2016-02-04
JP5985473B2 true JP5985473B2 (ja) 2016-09-06

Family

ID=45467432

Family Applications (3)

Application Number Title Priority Date Filing Date
JP2013519044A Expired - Fee Related JP5985473B2 (ja) 2010-07-13 2011-07-08 ＩＲＡＫ４モジュレーターとしてのピラゾロ［１，５ａ］ピリミジン及びチエノ［３，２ｂ］ピリミジン誘導体
JP2016151041A Expired - Fee Related JP6396376B2 (ja) 2010-07-13 2016-08-01 ＩＲＡＫ４モジュレーターとしてのピラゾロ［１，５ａ］ピリミジン及びチエノ［３，２ｂ］ピリミジン誘導体
JP2018159947A Pending JP2018199703A (ja) 2010-07-13 2018-08-29 ＩＲＡＫ４モジュレーターとしてのピラゾロ［１，５ａ］ピリミジン及びチエノ［３，２ｂ］ピリミジン誘導体

Family Applications After (2)

Application Number Title Priority Date Filing Date
JP2016151041A Expired - Fee Related JP6396376B2 (ja) 2010-07-13 2016-08-01 ＩＲＡＫ４モジュレーターとしてのピラゾロ［１，５ａ］ピリミジン及びチエノ［３，２ｂ］ピリミジン誘導体
JP2018159947A Pending JP2018199703A (ja) 2010-07-13 2018-08-29 ＩＲＡＫ４モジュレーターとしてのピラゾロ［１，５ａ］ピリミジン及びチエノ［３，２ｂ］ピリミジン誘導体

Country Status (11)

Country Link
US (4) US20120015962A1 (enExample)
EP (2) EP3252054A1 (enExample)
JP (3) JP5985473B2 (enExample)
KR (2) KR101995013B1 (enExample)
CN (3) CN110003219A (enExample)
AR (1) AR082154A1 (enExample)
BR (1) BR112013000868A2 (enExample)
CA (1) CA2802641C (enExample)
MX (2) MX340490B (enExample)
RU (1) RU2604062C2 (enExample)
WO (1) WO2012007375A1 (enExample)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2016222707A (ja) * 2010-07-13 2016-12-28 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft ＩＲＡＫ４モジュレーターとしてのピラゾロ［１，５ａ］ピリミジン及びチエノ［３，２ｂ］ピリミジン誘導体

Families Citing this family (112)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR101483215B1 (ko) * 2010-01-29 2015-01-16 한미약품 주식회사 단백질 키나아제 저해활성을 갖는 비시클릭 헤테로아릴 유도체
EP3239154A1 (en) * 2011-01-10 2017-11-01 Nimbus Iris, Inc. Irak inhibitors and uses thereof
EP2688872A4 (en) * 2011-03-22 2014-08-27 Merck Sharp & Dohme AMIDOPYRAZOLHEMMER OF INTERLEUKIN RECEPTOR-MEDIATED KINASES
WO2012178125A1 (en) 2011-06-22 2012-12-27 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
SG11201402765TA (en) * 2011-12-30 2014-06-27 Hanmi Pharm Ind Co Ltd THIENO[3,2-d]PYRIMIDINE DERIVATIVES HAVING INHIBITORY ACTIVITY FOR PROTEIN KINASES
TW201728592A (zh) * 2012-01-10 2017-08-16 林伯士艾瑞斯公司 Ｉｒａｋ抑制劑及其用途
JP6109193B2 (ja) * 2012-01-10 2017-04-05 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト チエノピリミジン化合物
WO2014003483A1 (en) * 2012-06-29 2014-01-03 Hanmi Pharm. Co., Ltd. Fused pyrimidine derivatives having inhibitory activity on fms kinases
BR112015000399A2 (pt) * 2012-07-10 2017-06-27 Ares Trading Sa derivados de pirazolil pirimidina
HK1210732A1 (en) 2012-07-11 2016-05-06 Nimbus Iris, Inc. Irak inhibitors and uses thereof
EP2872144A4 (en) 2012-07-11 2015-12-02 Nimbus Iris Inc IRAQ INHIBITOR AND USES THEREOF
WO2014011911A2 (en) * 2012-07-11 2014-01-16 Nimbus Iris, Inc. Irak inhibitors and uses thereof
LT3418281T (lt) 2012-12-07 2021-01-11 Vertex Pharmaceuticals Inc. Pirazolo[1,5-a]pirimidinai, naudotini kaip atr kinazės inhibitoriai, skirti vėžinių ligų gydymui
WO2014110114A1 (en) 2013-01-10 2014-07-17 Nimbus Iris, Inc. Irak inhibitors and uses thereof
EP2943485B1 (en) 2013-01-14 2017-09-20 Incyte Holdings Corporation Bicyclic aromatic carboxamide compounds useful as pim kinase inhibitors
TWI662030B (zh) 2013-01-15 2019-06-11 英塞特控股公司 適用作ｐｉｍ激酶抑制劑之噻唑甲醯胺及吡啶甲醯胺化合物
US8778365B1 (en) 2013-01-31 2014-07-15 Merz Pharmaceuticals, Llc Topical compositions and methods for making and using same
WO2014143240A1 (en) 2013-03-15 2014-09-18 Vertex Pharmaceuticals Incorporated Fused pyrazolopyrimidine derivatives useful as inhibitors of atr kinase
EP2970288A1 (en) * 2013-03-15 2016-01-20 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
EP2970289A1 (en) 2013-03-15 2016-01-20 Vertex Pharmaceuticals Inc. Compounds useful as inhibitors of atr kinase
GB201311891D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compound
GB201311888D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compounds
US20160166576A1 (en) 2013-07-11 2016-06-16 Merck Sharp & Dohme Corp. Substituted amidopyrazole inhibitors of interleukin receptor-associated kinases (irak-4)
US9556197B2 (en) * 2013-08-23 2017-01-31 Incyte Corporation Furo- and thieno-pyridine carboxamide compounds useful as pim kinase inhibitors
EP3049086A4 (en) 2013-09-27 2017-02-22 Nimbus Iris, Inc. Irak inhibitors and uses thereof
HUE046727T2 (hu) 2013-12-06 2020-03-30 Vertex Pharma Az ATR-kináz inhibitoraként használható vegyület, 2-amino-6-fluoro-N-[5-fluoro-piridin-3-IL]-pirazolo-[1,5-A]-pirimidin-3-karboxamid, ennek elõállítása, különbözõ szilárd formái és ezek radioaktív nyomjelzett származékai
USRE50030E1 (en) 2013-12-13 2024-07-02 Dana-Farber Cancer Institute, Inc. Methods to treat lymphoplasmacytic lymphoma
EP3079682A4 (en) 2013-12-13 2017-08-30 Dana-Farber Cancer Institute, Inc. Methods to treat lymphoplasmacytic lymphoma
TWI667233B (zh) 2013-12-19 2019-08-01 德商拜耳製藥公司 新穎吲唑羧醯胺，其製備方法、含彼等之醫藥製劑及其製造醫藥之用途
HK1231480A1 (zh) * 2014-01-10 2017-12-22 Aurigene Discovery Technologies Limited 作为irak4抑制剂的吲唑化合物
IL311677B2 (en) 2014-01-13 2025-06-01 Aurigene Oncology Ltd Bicyclic heterocyclyl derivatives as irak4 inhibitors
US20180228907A1 (en) 2014-04-14 2018-08-16 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
HRP20210935T1 (hr) * 2014-05-23 2021-08-06 F. Hoffmann - La Roche Ag Spojevi 5-kloro-2-difluorometoksifenil pirazolopirimidina koji predstavljaju inhibitore jak
ES2777608T3 (es) 2014-06-05 2020-08-05 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 útiles como inhibidores de ATR cinasa, la preparación de dicho compuesto y diferentes formas sólidas del mismo
US11179394B2 (en) 2014-06-17 2021-11-23 Vertex Pharmaceuticals Incorporated Method for treating cancer using a combination of Chk1 and ATR inhibitors
WO2016010897A1 (en) 2014-07-14 2016-01-21 Incyte Corporation Bicyclic heteroaromatic carboxamide compounds useful as pim kinase inhibitors
US9580418B2 (en) 2014-07-14 2017-02-28 Incyte Corporation Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors
CA2965178C (en) 2014-10-22 2023-09-26 Dana-Farber Cancer Institute, Inc. Thiazolyl-containing compounds for treating proliferative diseases
WO2016073889A1 (en) 2014-11-06 2016-05-12 Lysosomal Therapeutics Inc. Substituted imidazo[1,5-a]pyrimidines and their use in the treatment of medical disorders
EP3215511B1 (en) * 2014-11-06 2024-04-17 Bial-R&D Investments, S.A. Substituted pyrazolo(1,5-a)pyrimidines and their use in the treatment of medical disorders
US20180185368A1 (en) 2014-11-06 2018-07-05 Lysosomal Therapeutics Inc. Substituted pyrrolo[1,2-a]pyrimidines and their use in the treatment of medical disorders
LT3221306T (lt) * 2014-11-20 2020-03-10 Merck Patent Gmbh Heteroarilo junginiai, kaip irak inhibitoriai ir jų panaudojimas
US10329294B2 (en) 2015-03-12 2019-06-25 Merck Sharp & Dohme Corp. Pyrazolopyrimidine inhibitors of IRAK4 activity
US10155765B2 (en) 2015-03-12 2018-12-18 Merck Sharp & Dohme Corp. Carboxamide inhibitors of IRAK4 activity
US10329295B2 (en) 2015-03-12 2019-06-25 Merck Sharp & Dohme Corp. Pyrrolotriazine inhibitors of IRAK4 activity
US10040798B2 (en) 2015-03-12 2018-08-07 Merck Sharp & Dohme Corp. Pyrrolopyridazine inhibitors of IRAK4 activity
US10040802B2 (en) 2015-03-12 2018-08-07 Merck Sharp & Dohme Corp. Thienopyrazine inhibitors of IRAK4 activity
WO2016196244A1 (en) 2015-05-29 2016-12-08 Incyte Corporation Pyridineamine compounds useful as pim kinase inhibitors
WO2017004134A1 (en) * 2015-06-29 2017-01-05 Nimbus Iris, Inc. Irak inhibitors and uses thereof
CA2992406A1 (en) * 2015-07-15 2017-01-19 Aurigene Discovery Technologies Limited Indazole and azaindazole compounds as irak-4 inhibitors
AR105967A1 (es) 2015-09-09 2017-11-29 Incyte Corp Sales de un inhibidor de pim quinasa
KR102768838B1 (ko) 2015-09-17 2025-02-14 시티 오브 호프 Pcna 억제제
CN105237414B (zh) * 2015-09-30 2017-03-22 浙江永宁药业股份有限公司 ivacaftor中间体及其制备方法和用途
US11464774B2 (en) 2015-09-30 2022-10-11 Vertex Pharmaceuticals Incorporated Method for treating cancer using a combination of DNA damaging agents and ATR inhibitors
WO2017059251A1 (en) 2015-10-02 2017-04-06 Incyte Corporation Heterocyclic compounds useful as pim kinase inhibitors
EP3394066A2 (en) 2015-12-22 2018-10-31 H. Hoffnabb-La Roche Ag PYRAZOLO[1,5a]PYRIMIDINE DERIVATIVES AS IRAK4 MODULATORS
KR20180133461A (ko) 2016-04-06 2018-12-14 리소소말 테라퓨틱스 인크. 피라졸로[1,5-a]피리미디닐 카르복스아미드 화합물 및 의학적 장애의 치료에서의 그의 용도
WO2017176961A1 (en) 2016-04-06 2017-10-12 Lysosomal Therapeutics Inc. Imidazo [1,5-a]pyrimidinyl carboxamide compounds and their use in the treatment of medical disorders
MX388912B (es) 2016-04-06 2025-03-20 Lysosomal Therapeutics Inc Compuestos de pirrol[1,2-a]pirimidinil carboxamida y su uso en el tratamiento de trastornos médicos
EP3452045A1 (en) * 2016-05-04 2019-03-13 Lysosomal Therapeutics Inc. Methods of treatment and combination therapies using gcase activator heterobicyclic and related compounds
WO2017192931A1 (en) 2016-05-05 2017-11-09 Lysosomal Therapeutics Inc. SUBSTITUTED IMDAZO[1,2-α]PYRIDINES, SUBSTITUTED IMIDAZO[1,2-α]PYRAZINES, RELATED COMPOUNDS, AND THEIR USE IN THE TREATMENT OF MEDICAL DISORDERS
WO2017192930A1 (en) 2016-05-05 2017-11-09 Lysosomal Therapeutics Inc. SUBSTITUTED IMIDAZO[1,2-b]PYRIDAZINES, SUBSTITUTED IMIDAZO[1,5-b]PYRIDAZINES, RELATED COMPOUNDS, AND THEIR USE IN THE TREATMENT OF MEDICAL DISORDERS
CN106222183B (zh) * 2016-07-25 2019-11-08 南通大学 靶向人irak1基因的小干扰rna及其应用
WO2018083085A1 (en) 2016-11-02 2018-05-11 F. Hoffmann-La Roche Ag PYRAZOLO[1,5a]PYRIMIDINE DERIVATIVES AS IRAK4 MODULATORS
WO2018142393A1 (en) 2017-02-01 2018-08-09 Yissum Research Development Company Of The Hebrew N1 -(4-(5-(cyclopropylmethyl)-1 -methyl-1 h-pyrazol-4-yl)pyridin-2-yl)cyclohexane-1,4-diamine derivatives and related compounds as ck1 and/or iraki inhibitors for treating cancer
TW202340194A (zh) 2017-02-16 2023-10-16 美商基利科學股份有限公司 吡咯并[1,2-b]嗒𠯤衍生物
CN120267671A (zh) 2017-03-31 2025-07-08 奥锐金肿瘤有限公司 用于治疗血液病的化合物和组合物
CN106946890A (zh) * 2017-04-26 2017-07-14 中国药科大学 吡啶类irak4抑制剂、其制备方法及应用
JP7256757B2 (ja) 2017-05-22 2023-04-12 エフ． ホフマン－ラ ロシュ アーゲー 処置用化合物及び組成物、並びにその使用方法
CN110785418A (zh) * 2017-06-21 2020-02-11 豪夫迈·罗氏有限公司 作为irak4调节剂的异二氢吲哚酮衍生物
JP2020524692A (ja) * 2017-06-21 2020-08-20 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ Ｉｒａｋ４調節因子としてのベンゾフラン
WO2018234345A1 (en) * 2017-06-21 2018-12-27 F. Hoffmann-La Roche Ag PYRAZOLO [1,5A] PYRIMIDINE DERIVATIVES AS MODULATORS OF IRAK4
WO2019001460A1 (zh) * 2017-06-27 2019-01-03 南京明德新药研发股份有限公司 作为 irak4 抑制剂的稠环化合物
JP7114394B2 (ja) * 2017-08-18 2022-08-08 住友化学株式会社 化合物、レジスト組成物及びレジストパターンの製造方法
MX2020003190A (es) 2017-09-22 2020-11-11 Kymera Therapeutics Inc Degradadores de proteinas y usos de los mismos.
WO2019060693A1 (en) 2017-09-22 2019-03-28 Kymera Therapeutics, Inc. CRBN LIGANDS AND USES THEREOF
EP4410377A3 (en) 2017-10-31 2024-11-13 Curis, Inc. Compounds and compositions for treating hematological disorders
US11065231B2 (en) 2017-11-17 2021-07-20 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of interleukin-1 receptor- associated kinase 4 polypeptides
BR112020010905A2 (pt) * 2017-11-30 2020-11-17 Hanmi Pharm. Co., Ltd. compostos, composição farmacêutica e uso de um composto ou da composiçao farmacêutica
TW201924683A (zh) 2017-12-08 2019-07-01 美商英塞特公司 用於治療骨髓增生性贅瘤的低劑量組合療法
WO2019111218A1 (en) 2017-12-08 2019-06-13 Cadila Healthcare Limited Novel heterocyclic compounds as irak4 inhibitors
IL315310A (en) 2017-12-26 2024-10-01 Kymera Therapeutics Inc Irak degraders and uses thereof
US11512080B2 (en) 2018-01-12 2022-11-29 Kymera Therapeutics, Inc. CRBN ligands and uses thereof
EP3737666A4 (en) 2018-01-12 2022-01-05 Kymera Therapeutics, Inc. PROTEIN DEGRADATION AGENTS AND ASSOCIATED USES
EP3774797B1 (en) * 2018-04-05 2025-11-19 Merck Patent GmbH Heteroaryl compounds as type ii irak inhibitors and uses hereof
US12454520B2 (en) 2018-07-06 2025-10-28 Kymera Therapeutics, Inc. Protein degraders and uses thereof
US11292792B2 (en) 2018-07-06 2022-04-05 Kymera Therapeutics, Inc. Tricyclic CRBN ligands and uses thereof
TWI721483B (zh) 2018-07-13 2021-03-11 美商基利科學股份有限公司 吡咯并[1,2-b]嗒𠯤衍生物
CN110862375B (zh) 2018-08-27 2022-10-25 深圳铂立健医药有限公司 吡唑化合物及其药物组合物和应用
KR20250174699A (ko) 2018-10-30 2025-12-12 크로노스 바이오, 인코포레이티드 Cdk9 활성을 조절하기 위한 화합물, 조성물 및 방법
AU2019389174A1 (en) 2018-11-30 2021-07-01 Kymera Therapeutics, Inc. Irak degraders and uses thereof
KR20220027196A (ko) * 2019-06-27 2022-03-07 바이오젠 엠에이 인코포레이티드 이미다조[1,2-a]피리디닐 유도체 및 질병의 치료에서 이것들의 용도
PH12022500002A1 (en) 2019-06-28 2023-04-03 Kymera Therapeutics Inc Irak degraders and uses thereof
US12558427B2 (en) 2019-07-17 2026-02-24 Kymera Therapeutics, Inc. IRAK degraders and uses thereof
KR102782229B1 (ko) 2019-10-02 2025-03-20 (주)카이노스메드 N-(1h-이미다졸-2-일)벤즈아미드 화합물 및 활성 성분으로 이를 포함하는 약학 조성물
WO2021119159A1 (en) 2019-12-10 2021-06-17 Kymera Therapeutics, Inc. Irak degraders and uses thereof
CA3161878A1 (en) 2019-12-17 2021-06-24 Matthew M. Weiss Irak degraders and uses thereof
EP4076524A4 (en) 2019-12-17 2023-11-29 Kymera Therapeutics, Inc. IRAQ DEGRADERS AND USES THEREOF
BR112022020020A2 (pt) 2020-04-04 2022-11-22 Pfizer Métodos de tratamento da doença do coronavírus 2019
TW202210483A (zh) 2020-06-03 2022-03-16 美商凱麥拉醫療公司 Irak降解劑之結晶型
EP4161521A4 (en) 2020-06-03 2024-07-10 Kymera Therapeutics, Inc. DEUTERED IRAQ DEGRADERS AND USES THEREOF
CA3194164A1 (en) * 2020-09-30 2022-04-07 Koichiro Arai Pyrimidine- and nitrogen-containing bicyclic compound
EP4247790B1 (en) 2020-11-23 2024-10-09 Regor Pharmaceuticals, Inc. Sting antagonists and uses thereof
US11866405B2 (en) 2020-12-10 2024-01-09 Astrazeneca Ab Substituted indazoles as IRAK4 inhibitors
AR124547A1 (es) 2020-12-30 2023-04-05 Kymera Therapeutics Inc Degradadores de irak y sus usos
WO2022174268A1 (en) 2021-02-15 2022-08-18 Kymera Therapeutics, Inc. Irak4 degraders and uses thereof
MX2023009178A (es) 2021-02-15 2023-08-21 Kymera Therapeutics Inc Degradadores de la cinasa 4 asociada al receptor de interleucina 1 (irak4) y usos de los mismos.
CA3214747A1 (en) 2021-04-08 2022-10-13 Reinhard Von Roemeling Combination therapies for the treatment of cancer
CA3217792A1 (en) 2021-05-07 2022-11-10 Kymera Therapeutics, Inc Cdk2 degraders and uses thereof
KR102869914B1 (ko) * 2021-10-28 2025-10-13 재단법인 대구경북첨단의료산업진흥재단 신규한 티에노[2,3-d]피리미딘 유도체, 이의 제조방법 및 이를 유효성분으로 포함하는 암 또는 자가면역질환의 예방 또는 치료용 약학적 조성물
JP2024540080A (ja) 2021-10-29 2024-10-31 カイメラ セラピューティクス， インコーポレイテッド Ｉｒａｋ４分解剤およびその合成
EP4472967A4 (en) 2022-01-31 2026-04-15 Kymera Therapeutics Inc Iraqi Degradation Agents and Their Uses

Family Cites Families (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6436628B1 (en) * 1998-06-19 2002-08-20 The Rockefeller University Methods of identifying an agent which modulates period and doubletime protein interaction
EP1434579B1 (en) 2001-10-09 2011-06-08 Amgen Inc. Imidazole derivatives as antiinflammatory agents
AR038118A1 (es) 2002-01-14 2004-12-29 Upjohn Co Compuestos derivados de la bencinamida del acido 7-oxo-4,7-dihidrotien[2,3-b[piridin-6-carboxilico 3-sustituido que son utiles como antivirales
WO2005004810A2 (en) * 2003-07-02 2005-01-20 Merck & Co., Inc. Arylsulfonamide derivatives
TWI372050B (en) 2003-07-03 2012-09-11 Astex Therapeutics Ltd (morpholin-4-ylmethyl-1h-benzimidazol-2-yl)-1h-pyrazoles
GB0329214D0 (en) * 2003-12-17 2004-01-21 Glaxo Group Ltd Novel compounds
WO2005080394A1 (en) 2004-02-24 2005-09-01 Bioaxone Therapeutique Inc. 4-substituted piperidine derivatives
JPWO2005095317A1 (ja) 2004-03-31 2008-02-21 株式会社クラレ ハロゲン化不飽和カルボニル化合物の製造方法
JP2008013527A (ja) 2006-07-10 2008-01-24 Sankyo Co Ltd チエノ［３，２−ｄ］ピリミジン−２，４−ジアミン誘導体
US20080176870A1 (en) * 2006-11-20 2008-07-24 Bert Nolte Heterobicyclic metalloprotease inhibitors
AU2008309517B2 (en) * 2007-10-12 2013-03-14 Astrazeneca Ab Inhibitors of protein kinases
ES2710701T3 (es) * 2008-09-24 2019-04-26 Basf Se Compuestos de pirazol para el control de plagas de invertebrados
BRPI0914404A2 (pt) * 2008-10-31 2019-03-06 Genentech Inc "compostos, composição farmacêutica e método para tratar ou atenuar a gravidade de uma doença ou condição responsiva à inibição da atividade jak quinase em um paciente"
IT1392824B1 (it) * 2009-02-13 2012-03-23 Sacmi Apparato per formare oggetti
CN101537007A (zh) * 2009-03-18 2009-09-23 中国医学科学院血液病医院（血液学研究所） N-(噻吩-2)吡唑并[1,5-a]嘧啶-3-甲酰胺类化合物在制备抗恶性肿瘤药物方面的应用
UA110324C2 (en) * 2009-07-02 2015-12-25 Genentech Inc Jak inhibitory compounds based on pyrazolo pyrimidine
EP2470538A1 (en) * 2009-08-28 2012-07-04 Array Biopharma, Inc. Raf inhibitor compounds and methods of use thereof
KR101483215B1 (ko) 2010-01-29 2015-01-16 한미약품 주식회사 단백질 키나아제 저해활성을 갖는 비시클릭 헤테로아릴 유도체
EP2528925B1 (en) * 2010-01-29 2017-07-05 Hanmi Science Co., Ltd. THIENO[3,2-d]PYRIMIDINE DERIVATIVES HAVING INHIBITORY ACTIVITY ON PROTEIN KINASES
JP5985473B2 (ja) * 2010-07-13 2016-09-06 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ ＩＲＡＫ４モジュレーターとしてのピラゾロ［１，５ａ］ピリミジン及びチエノ［３，２ｂ］ピリミジン誘導体

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2016222707A (ja) * 2010-07-13 2016-12-28 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft ＩＲＡＫ４モジュレーターとしてのピラゾロ［１，５ａ］ピリミジン及びチエノ［３，２ｂ］ピリミジン誘導体
JP2018199703A (ja) * 2010-07-13 2018-12-20 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ ＩＲＡＫ４モジュレーターとしてのピラゾロ［１，５ａ］ピリミジン及びチエノ［３，２ｂ］ピリミジン誘導体

Also Published As

Publication number Publication date
JP2013531018A (ja) 2013-08-01
US20180298026A1 (en) 2018-10-18
CA2802641A1 (en) 2012-01-19
MX358682B (es) 2018-08-31
CN105367577A (zh) 2016-03-02
HK1183029A1 (zh) 2013-12-13
AR082154A1 (es) 2012-11-14
CN105367577B (zh) 2019-04-23
KR101995013B1 (ko) 2019-07-02
US20120015962A1 (en) 2012-01-19
CN102985426A (zh) 2013-03-20
US9255110B2 (en) 2016-02-09
US20160207936A1 (en) 2016-07-21
RU2604062C2 (ru) 2016-12-10
EP2593457A1 (en) 2013-05-22
CN110003219A (zh) 2019-07-12
CA2802641C (en) 2019-03-12
US10023589B2 (en) 2018-07-17
EP3252054A1 (en) 2017-12-06
WO2012007375A1 (en) 2012-01-19
MX340490B (es) 2016-07-11
KR20190077610A (ko) 2019-07-03
BR112013000868A2 (pt) 2016-05-17
JP6396376B2 (ja) 2018-09-26
JP2018199703A (ja) 2018-12-20
EP2593457B1 (en) 2017-08-23
JP2016222707A (ja) 2016-12-28
CN102985426B (zh) 2015-10-07
RU2013103539A (ru) 2014-08-20
KR20130132396A (ko) 2013-12-04
MX2013000390A (es) 2013-03-08
US20140303149A1 (en) 2014-10-09

Similar Documents

Publication Publication Date Title
JP6396376B2 (ja) ＩＲＡＫ４モジュレーターとしてのピラゾロ［１，５ａ］ピリミジン及びチエノ［３，２ｂ］ピリミジン誘導体
AU2007328981B2 (en) Substituted pyrimidines and their use as JNK modulators
US6949560B2 (en) Imidazo-substituted compounds as p38 kinase inhibitors
WO2023186069A1 (zh) 一类白介素-1受体相关激酶4的双功能嵌合体杂环化合物及其制备方法、药用组合物和用途
AU2006283940A1 (en) P38 MAP kinase inhibitors and methods for using the same
ES2389907T9 (es) Compuesto de amida heterocíclica y uso del mismo como un inhibidor de MMP-13
IL297879A (en) Amidopyrimidone derivatives
TW201035095A (en) Pyrazolo[1,5-a]pyridine derivatives
TW202448888A (zh) 三環雜環衍生物及其組合物和應用
US20080207684A1 (en) Kinase inhibitors and methods for using the same
CA2810659A1 (en) Quinoxaline compound
EP2576537B1 (en) 2-amino-pyrimidine derivatives useful as inhibitors of jnk
CA2799817A1 (en) Inhibitors of jnk
CN119365454A (zh) 通过半胱氨酸775的共价egfr抑制剂的发现
HK1183029B (en) Pyrazolo [1, 5a] pyrimidine and thieno [3, 2b] pyrimidine derivatives as irak4 modulators
TR201908937T4 (tr) P38 MAP kinazı inhibe eden indanil üre bileşikleri.
CA3008653C (en) Bruton's tyrosine kinase inhibitors
TW201217379A (en) Pyrazolo[1,5a]pyrimidine derivatives as IRAK4 modulators
HK1226734A1 (en) Inhibitors of bruton’s tyrosine kinase

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20130111

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20140707

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: 20150522

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20150813

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20151120

A524 Written submission of copy of amendment under article 19 pct

Free format text: JAPANESE INTERMEDIATE CODE: A524

Effective date: 20151120

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20151222

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20160317

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20160518

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20160614

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: 20160705

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20160803

R150 Certificate of patent or registration of utility model

Ref document number: 5985473

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

LAPS Cancellation because of no payment of annual fees