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)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Dermatology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Urology & Nephrology (AREA)
  • Virology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (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) EP2593457B1 (enExample)
JP (3) JP5985473B2 (enExample)
KR (2) KR101995013B1 (enExample)
CN (3) CN102985426B (enExample)
AR (1) AR082154A1 (enExample)
BR (1) BR112013000868A2 (enExample)
CA (1) CA2802641C (enExample)
MX (2) MX358682B (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 (110)

* 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
EP2663312B1 (en) 2011-01-10 2017-10-11 Nimbus Iris, Inc. Irak inhibitors and uses thereof
US9169260B2 (en) 2011-03-22 2015-10-27 Merck Sharp & Dohme Corp. Amidopyrazole inhibitors of interleukin receptor-associated kinases
JP2014517079A (ja) 2011-06-22 2014-07-17 バーテックス ファーマシューティカルズ インコーポレイテッド Ａｔｒキナーゼ阻害剤として有用な化合物
USRE47451E1 (en) * 2011-12-30 2019-06-25 Hanmi Pharm. Co. Ltd. Thieno[3,2-D]pyrimidine derivatives having inhibitory activity for protein kinases
CN104582705A (zh) * 2012-01-10 2015-04-29 林伯士艾瑞斯公司 白介素-1受体相关激酶(irak)抑制剂和其用途
CN104159904B (zh) * 2012-01-10 2016-12-14 霍夫曼-拉罗奇有限公司 噻吩并嘧啶化合物
WO2014003483A1 (en) * 2012-06-29 2014-01-03 Hanmi Pharm. Co., Ltd. Fused pyrimidine derivatives having inhibitory activity on fms kinases
SG11201500005SA (en) * 2012-07-10 2015-01-29 Ares Trading Sa Pyrimidine pyrazolyl derivatives
WO2014011911A2 (en) * 2012-07-11 2014-01-16 Nimbus Iris, Inc. Irak inhibitors and uses thereof
CN104902959A (zh) 2012-07-11 2015-09-09 林伯士艾瑞斯公司 Irak抑制剂和其用途
HK1210696A1 (en) * 2012-07-11 2016-05-06 Nimbus Iris, Inc. Irak inhibitors and uses thereof
SMT202000713T1 (it) 2012-12-07 2021-03-15 Vertex Pharma Pirazolo [1,5-a] pirimidine utili come inibitori dell'atr chinasi per il trattamento di malattie del cancro
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
ME03780B (me) 2013-01-15 2021-04-20 Incyte Holdings Corp Jedinjenja tiazolkarboksamida i piridinkarboksamida korisna kao inhibitori pim kinaze
US8778365B1 (en) 2013-01-31 2014-07-15 Merz Pharmaceuticals, Llc Topical compositions and methods for making and using same
JP2016512815A (ja) 2013-03-15 2016-05-09 バーテックス ファーマシューティカルズ インコーポレイテッドＶｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ Ａｔｒキナーゼの阻害剤として有用な縮合ピラゾロピリミジン誘導体
EP2970288A1 (en) * 2013-03-15 2016-01-20 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
WO2014143241A1 (en) 2013-03-15 2014-09-18 Vertex Pharmaceuticals Incorporated 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
WO2015006181A1 (en) 2013-07-11 2015-01-15 Merck Sharp & Dohme Corp. Substituted amidopyrazole inhibitors of interleukin receptor-associated kinases (irak-4)
TW201605866A (zh) 2013-08-23 2016-02-16 英塞特公司 可用作ｐｉｍ激酶抑制劑之呋喃并－及噻吩并－吡啶甲醯胺化合物
WO2015048281A1 (en) 2013-09-27 2015-04-02 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
JP6879740B2 (ja) 2013-12-13 2021-06-02 ダナ−ファーバー キャンサー インスティテュート， インコーポレイテッド リンパ形質細胞性リンパ腫を処置する方法
JP6878004B2 (ja) 2013-12-13 2021-05-26 ダナ−ファーバー キャンサー インスティテュート， インコーポレイテッド リンパ形質細胞性リンパ腫を処置する方法
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
BR112016015983A2 (pt) * 2014-01-10 2017-08-08 Aurigene Discovery Tech Ltd Compostos de indazol como inibidores de irak4, seus usos, e composição farmacêutica
SMT202400142T1 (it) 2014-01-13 2024-05-14 Aurigene Oncology Ltd Enantiomeri (r) e (s) di n-(5-(3-idrossipirrolidin-1-il)-2-morfolinoossazolo[4,5-b]piridin-6-il)-2-(2-metilpiridin-4-il)ossazolo-carbossammide in qualità di inibitori di irak4 per il trattamento di un cancro
US20180228907A1 (en) 2014-04-14 2018-08-16 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
EA032488B1 (ru) 2014-05-23 2019-06-28 Ф. Хоффманн-Ля Рош Аг Соединения 5-хлор-дифторметоксифенилпиразолопиримидина, представляющие собой ингибиторы янус-киназы
CN107074863B (zh) 2014-06-05 2019-12-03 沃泰克斯药物股份有限公司 Atr激酶抑制剂的制备方法及其不同的固体形式
PL3157566T3 (pl) 2014-06-17 2019-10-31 Vertex Pharma Metoda leczenia nowotworu przy użyciu kombinacji inhibitorów chk1 i atr
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
US10112957B2 (en) 2014-10-22 2018-10-30 Dana-Farber Cancer Institute, Inc. Thiazolyl-containing compounds for treating proliferative diseases
AU2015342883B2 (en) 2014-11-06 2020-07-02 Bial - R&D Investments, S.A. Substituted pyrrolo(1,2-a)pyrimidines and their use in the treatment of medical disorders
CN107001379B (zh) * 2014-11-06 2022-11-01 Bial研发投资股份有限公司 取代的吡唑并[1,5-a]嘧啶以及它们在治疗医学障碍中的用途
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
ES2772133T3 (es) * 2014-11-20 2020-07-07 Merck Patent Gmbh Compuestos heteroarilo como inhibidores de IRAK y sus usos
US10040798B2 (en) 2015-03-12 2018-08-07 Merck Sharp & Dohme Corp. Pyrrolopyridazine inhibitors of IRAK4 activity
US10155765B2 (en) 2015-03-12 2018-12-18 Merck Sharp & Dohme Corp. Carboxamide inhibitors of IRAK4 activity
WO2016144846A1 (en) * 2015-03-12 2016-09-15 Merck Sharp & Dohme Corp. Pyrazolopyrimidine inhibitors of irak4 activity
EP3268003B1 (en) * 2015-03-12 2020-07-29 Merck Sharp & Dohme Corp. Thienopyrazine inhibitors of irak4 activity
WO2016144848A1 (en) * 2015-03-12 2016-09-15 Merck Sharp & Dohme Corp. Pyrrolotriazine 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
AU2016293441A1 (en) * 2015-07-15 2018-02-01 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
US10550070B2 (en) 2015-09-17 2020-02-04 City Of Hope PCNA inhibitors
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
KR102678021B1 (ko) 2015-09-30 2024-06-26 버텍스 파마슈티칼스 인코포레이티드 Dna 손상제와 병용되는, atr 저해제를 포함하는 암 치료용 약제학적 조성물
WO2017059251A1 (en) 2015-10-02 2017-04-06 Incyte Corporation Heterocyclic compounds useful as pim kinase inhibitors
CN108473498B (zh) * 2015-12-22 2021-11-02 豪夫迈·罗氏有限公司 作为IRAK4调节剂的吡唑并[1,5a]嘧啶衍生物
WO2017176960A1 (en) 2016-04-06 2017-10-12 Lysosomal Therapeutics Inc. Pyrazolo[1,5-a]pyrimidinyl carboxamide compounds and their use in the treatment of medical disorders
US10787454B2 (en) 2016-04-06 2020-09-29 BIAL—BioTech Investments, Inc. Imidazo[1,5-a]pyrimidinyl carboxamide compounds and their use in the treatment of medical disorders
WO2017176962A1 (en) 2016-04-06 2017-10-12 Lysosomal Therapeutics, Inc. Pyrrolo[1,2-a]pyrimidinyl carboxamide compounds and their use in the treatment of medical disorders
WO2017192841A1 (en) * 2016-05-04 2017-11-09 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
MX389579B (es) 2016-05-05 2025-03-20 Bial R&D Invest S A IMIDAZO[1,2-b]PIRIDAZINAS SUSTITUIDAS, IMIDAZO[1,5-b]PIRIDAZINAS SUSTITUIDAS, COMPUESTOS RELACIONADOS Y SU USO EN EL TRATAMIENTO DE TRASTORNOS MÉDICOS
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
NZ755447A (en) * 2017-02-01 2023-05-26 Yissum Res Dev Co Of Hebrew Univ Jerusalem Ltd 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
TWI733982B (zh) 2017-02-16 2021-07-21 美商基利科學股份有限公司 吡咯并[1,2-b]嗒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
WO2018215389A1 (en) 2017-05-22 2018-11-29 F. Hoffmann-La Roche Ag Therapeutic compounds and compositions, and methods of use thereof
EP3642204A1 (en) * 2017-06-21 2020-04-29 H. Hoffnabb-La Roche Ag PYRAZOLO[1,5a]PYRIMIDINE DERIVATIVES AS IRAK4 MODULATORS
CN110770229A (zh) * 2017-06-21 2020-02-07 豪夫迈·罗氏有限公司 作为irak4调节剂的苯并呋喃化合物
JP2020524663A (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調節因子としてのイソインドリノン誘導体
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
JP7366031B2 (ja) 2017-09-22 2023-10-20 カイメラ セラピューティクス， インコーポレイテッド タンパク質分解剤およびそれらの使用
WO2019060693A1 (en) 2017-09-22 2019-03-28 Kymera Therapeutics, Inc. CRBN LIGANDS AND USES THEREOF
MX2020003666A (es) 2017-10-31 2020-08-03 Curis Inc Compuestos y composiciones para el tratamiento de trastornos hematologicos.
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
US11492357B2 (en) * 2017-11-30 2022-11-08 Hanmi Pharm. Co., Ltd. Thieno[3,2-d]pyrimidine derivative compound having inhibitory activity for protein kinase
WO2019111218A1 (en) 2017-12-08 2019-06-13 Cadila Healthcare Limited Novel heterocyclic compounds as irak4 inhibitors
US10596161B2 (en) 2017-12-08 2020-03-24 Incyte Corporation Low dose combination therapy for treatment of myeloproliferative neoplasms
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
MX2020009234A (es) 2018-04-05 2020-10-12 Merck Patent Gmbh Compuestos de heteroarilo como inhibidores de cinasas asociadas con receptores de interleucina-1 (irak) tipo ii y usos de los mismos.
EP3817822A4 (en) 2018-07-06 2022-07-27 Kymera Therapeutics, Inc. PROTEIN DEGRADANTS AND USES THEREOF
WO2020010177A1 (en) 2018-07-06 2020-01-09 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
IL282254B2 (en) 2018-10-30 2025-08-01 Kronos Bio Inc Compounds, compositions, and methods for modulating cdk9 activity
JP7623943B2 (ja) 2018-11-30 2025-01-29 カイメラ セラピューティクス， インコーポレイテッド Ｉｒａｋ分解剤およびそれらの使用
AR119234A1 (es) * 2019-06-27 2021-12-01 Biogen Ma Inc Derivados de imidazo[1,2-a]piridinilo y su uso en el tratamiento de enfermedades
BR112021026517A2 (pt) 2019-06-28 2022-05-10 Kymera Therapeutics Inc Degradadores de irak e usos dos mesmos
WO2021011868A1 (en) 2019-07-17 2021-01-21 Kymera Therapeutics, Inc. Irak degraders and uses thereof
AU2020360000B2 (en) 2019-10-02 2023-04-20 Kainos Medicine, Inc. N-(1H-imidazol-2-yl)benzamide compound and pharmaceutical composition comprising the same as active ingredient
EP4072591A4 (en) 2019-12-10 2024-06-05 Kymera Therapeutics, Inc. IRAQ DEGRADER AND USES THEREOF
WO2021127283A2 (en) 2019-12-17 2021-06-24 Kymera Therapeutics, Inc. Irak degraders and uses thereof
JP2023509366A (ja) 2019-12-17 2023-03-08 カイメラ セラピューティクス， インコーポレイテッド Ｉｒａｋ分解剤およびそれらの使用
CA3177852A1 (en) 2020-04-04 2021-10-07 Pfizer Inc. Methods of treating coronavirus disease 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
ES3036969T3 (en) 2020-09-30 2025-09-25 Asahi Kasei Pharma Corp Nitrogen-containing bicyclic compounds which contain pyrimidine as interleukin 1 receptor-associated kinase 4 (irak-4) inhibitors to be used in the treatment of inflammatory or autoimmune diseases
US11866405B2 (en) 2020-12-10 2024-01-09 Astrazeneca Ab Substituted indazoles as IRAK4 inhibitors
WO2022147465A1 (en) 2020-12-30 2022-07-07 Kymera Therapeutics, Inc. Irak degraders and uses thereof
TW202245788A (zh) 2021-02-15 2022-12-01 美商凱麥拉醫療公司 Irak4降解劑及其用途
CN116867494A (zh) 2021-02-15 2023-10-10 凯麦拉医疗公司 Irak4降解剂和其用途
US12178821B2 (en) 2021-04-08 2024-12-31 Curis, Inc. Combination therapies for the treatment of cancer
AU2022271290A1 (en) 2021-05-07 2023-11-23 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
EP4422635A4 (en) 2021-10-29 2025-11-26 Kymera Therapeutics Inc IRAQ4 DEGRADATION AGENTS AND THEIR SYNTHESIS
IL314437A (en) 2022-01-31 2024-09-01 Kymera Therapeutics Inc IRAK joints 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
ES2367422T3 (es) 2001-10-09 2011-11-03 Amgen Inc. Derivados de imidazol como agentes antiinflamatorios.
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
WO2005095317A1 (ja) 2004-03-31 2005-10-13 Kuraray Co., Ltd. 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
CA2670083A1 (en) * 2006-11-20 2008-05-29 Alantos Pharmaceuticals Holding, Inc. Heterobicyclic metalloprotease inhibitors
WO2009047359A1 (en) * 2007-10-12 2009-04-16 Ingenium Pharmaceuticals Gmbh Inhibitors of protein kinases
WO2010034738A2 (en) * 2008-09-24 2010-04-01 Basf Se Pyrazole compounds for controlling invertebrate pests
CN102271515B (zh) * 2008-10-31 2014-07-02 健泰科生物技术公司 吡唑并嘧啶jak抑制剂化合物和方法
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
KR101347303B1 (ko) 2010-01-29 2014-01-06 한미사이언스 주식회사 단백질 키나아제 저해활성을 갖는 티에노[3,2-ｄ]피리미딘 유도체
KR101483215B1 (ko) 2010-01-29 2015-01-16 한미약품 주식회사 단백질 키나아제 저해활성을 갖는 비시클릭 헤테로아릴 유도체
CN102985426B (zh) * 2010-07-13 2015-10-07 弗·哈夫曼-拉罗切有限公司 作为irak4调节剂的吡唑并[1,5a]嘧啶和噻吩并[3,2b]嘧啶衍生物

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

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
US20080207684A1 (en) Kinase inhibitors and methods for using the same
TW202448888A (zh) 三環雜環衍生物及其組合物和應用
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