JP2011518836A - 大環状化合物およびそれらのキナーゼ阻害剤としての使用 - Google Patents

大環状化合物およびそれらのキナーゼ阻害剤としての使用 Download PDF

Info

Publication number
JP2011518836A
JP2011518836A JP2011506453A JP2011506453A JP2011518836A JP 2011518836 A JP2011518836 A JP 2011518836A JP 2011506453 A JP2011506453 A JP 2011506453A JP 2011506453 A JP2011506453 A JP 2011506453A JP 2011518836 A JP2011518836 A JP 2011518836A
Authority
JP
Japan
Prior art keywords
chloro
docosa
nonaen
tetraazatetracyclo
pentaazatetracyclo
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
JP2011506453A
Other languages
English (en)
Japanese (ja)
Other versions
JP2011518836A5 (enExample
Inventor
アンドリュー・ポール・コムス
リチャード・ビー・スパークス
エディ・ダブリュー・ユー
フェン・ハオ
マイケル・ジェイソン・バウアー
チュ・ウェンユ
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.)
Incyte Corp
Original Assignee
Incyte Corp
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 Incyte Corp filed Critical Incyte Corp
Publication of JP2011518836A publication Critical patent/JP2011518836A/ja
Publication of JP2011518836A5 publication Critical patent/JP2011518836A5/ja
Pending legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48Two nitrogen atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/02Nasal agents, e.g. decongestants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/08Bronchodilators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/04Antipruritics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/14Drugs for dermatological disorders for baldness or alopecia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/20Antivirals for DNA viruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/14Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D407/00Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/02Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
    • C07D407/12Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic 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
    • C07D498/04Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Virology (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Oncology (AREA)
  • Diabetes (AREA)
  • Dermatology (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • Hematology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Cardiology (AREA)
  • Endocrinology (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Obesity (AREA)
  • Biotechnology (AREA)
  • Biomedical Technology (AREA)
  • Emergency Medicine (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • Ophthalmology & Optometry (AREA)
  • Hospice & Palliative Care (AREA)
JP2011506453A 2008-04-24 2009-04-23 大環状化合物およびそれらのキナーゼ阻害剤としての使用 Pending JP2011518836A (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US4754708P 2008-04-24 2008-04-24
US61/047,547 2008-04-24
US12258208P 2008-12-15 2008-12-15
US61/122,582 2008-12-15
PCT/US2009/041555 WO2009132202A2 (en) 2008-04-24 2009-04-23 Macrocyclic compounds and their use as kinase inhibitors

Publications (2)

Publication Number Publication Date
JP2011518836A true JP2011518836A (ja) 2011-06-30
JP2011518836A5 JP2011518836A5 (enExample) 2012-06-14

Family

ID=41100487

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2011506453A Pending JP2011518836A (ja) 2008-04-24 2009-04-23 大環状化合物およびそれらのキナーゼ阻害剤としての使用

Country Status (5)

Country Link
US (1) US8871753B2 (enExample)
EP (1) EP2274288A2 (enExample)
JP (1) JP2011518836A (enExample)
CA (1) CA2722326A1 (enExample)
WO (1) WO2009132202A2 (enExample)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2016505069A (ja) * 2013-01-25 2016-02-18 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company C型肝炎の治療用のアンモニウム誘導体
JP2016041709A (ja) * 2012-03-06 2016-03-31 ファイザー・インク 増殖性疾患の治療のための大環状誘導体
JP2016540824A (ja) * 2013-12-20 2016-12-28 インスティテュート オブ ファーマコロジー アンド トキシコロジー アカデミー オブ ミリタリー メディカル サイエンシズ ピー.エル.エー.チャイナ 新規ピペリジンカルボキサミド化合物、その調製方法及び使用
JP2023513793A (ja) * 2020-02-14 2023-04-03 ソーク インスティテュート フォー バイオロジカル スタディーズ 大環状ulk1/2阻害剤

Families Citing this family (77)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8338439B2 (en) 2008-06-27 2012-12-25 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
US11351168B1 (en) 2008-06-27 2022-06-07 Celgene Car Llc 2,4-disubstituted pyrimidines useful as kinase inhibitors
TWI458721B (zh) 2008-06-27 2014-11-01 Celgene Avilomics Res Inc 雜芳基化合物及其用途
AU2013202496B2 (en) * 2008-06-27 2016-08-04 Celgene Car Llc Heteroaryl compounds and uses thereof
JP5749645B2 (ja) 2008-09-08 2015-07-15 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングMerck Patent Gesellschaft mit beschraenkter Haftung タンパク質キナーゼ阻害剤としての大環状ピリミジン
WO2010085597A1 (en) * 2009-01-23 2010-07-29 Incyte Corporation Macrocyclic compounds and their use as kinase inhibitors
KR101705158B1 (ko) 2009-05-05 2017-02-09 다나-파버 캔서 인스티튜트 인크. Egfr 억제제 및 질환 치료방법
TW201100441A (en) 2009-06-01 2011-01-01 Osi Pharm Inc Amino pyrimidine anticancer compounds
US8445490B2 (en) 2009-10-14 2013-05-21 Bristol-Myers Squibb Company Compounds for the treatment of hepatitis C
EP2488526B1 (en) * 2009-10-14 2013-07-24 Bristol-Myers Squibb Company Compounds for the treatment of hepatitis c
HU0900798D0 (en) * 2009-12-21 2010-03-01 Vichem Chemie Kutato Kft 4-phenylamino-pyrimidine derivatives having protein kinase inhibitor activity
EP2566872B1 (en) 2010-05-04 2014-12-24 Bristol-Myers Squibb Company Compounds for the treatment of hepatitis c
TWI513694B (zh) * 2010-05-11 2015-12-21 Amgen Inc 抑制間變性淋巴瘤激酶的嘧啶化合物
WO2012019132A2 (en) 2010-08-06 2012-02-09 Cell Signaling Technology, Inc. Anaplastic lymphoma kinase in kidney cancer
RU2013109393A (ru) 2010-08-10 2014-09-20 Сэлджин Авиаломикс Ресеарч, Инк. Безилатная соль ингибитора втк
US8765944B2 (en) 2010-08-19 2014-07-01 Bristol-Myers Squibb Company Compounds for the treatment of hepatitis C
CA2815858C (en) 2010-11-01 2018-10-16 Celgene Avilomics Research, Inc. Heterocyclic compounds and uses thereof
EP2635285B1 (en) 2010-11-01 2017-05-03 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
CN103370076A (zh) * 2010-11-02 2013-10-23 纽约市哥伦比亚大学托管会 治疗毛发脱落疾病的方法
US9198911B2 (en) 2010-11-02 2015-12-01 The Trustees Of Columbia University In The City Of New York Methods for treating hair loss disorders
EP2637502B1 (en) 2010-11-10 2018-01-10 Celgene CAR LLC Mutant-selective egfr inhibitors and uses thereof
PL2646448T3 (pl) 2010-11-29 2017-12-29 OSI Pharmaceuticals, LLC Makrocykliczne inhibitory kinazy
WO2012125603A1 (en) 2011-03-16 2012-09-20 Cephalon, Inc. Macrocyclic compounds as alk, fak and jak2 inhibitors
US8933066B2 (en) * 2011-04-14 2015-01-13 Bristol-Myers Squibb Company Compounds for the treatment of hepatitis C
WO2012141704A1 (en) * 2011-04-14 2012-10-18 Bristol-Myers Squibb Company Compounds for the treatment of hepatitis c
EP2744507A4 (en) * 2011-08-19 2015-01-28 Merck Sharp & Dohme CRYSTAL FORMS OF AN HCV PROTEASE HEMMER
US8629150B2 (en) 2011-09-28 2014-01-14 Bristol-Myers Squibb Company Compounds for the treatment of hepatitis C
US8697706B2 (en) 2011-10-14 2014-04-15 Bristol-Myers Squibb Company Compounds for the treatment of hepatitis C
CA2853498A1 (en) 2011-10-28 2013-05-02 Celgene Avilomics Research, Inc. Methods of treating a bruton's tyrosine kinase disease or disorder
US9089574B2 (en) 2011-11-30 2015-07-28 Emory University Antiviral JAK inhibitors useful in treating or preventing retroviral and other viral infections
US8916702B2 (en) 2012-02-06 2014-12-23 Bristol-Myers Squibb Company Compounds for the treatment of hepatitis C
RU2711077C9 (ru) 2012-03-15 2020-08-11 Селджен Кар Ллс Соли ингибитора киназы рецептора эпидермального фактора роста
BR112014022789B1 (pt) 2012-03-15 2022-04-19 Celgene Car Llc Formas sólidas de um inibidor de quinase de receptor do fator de crescimento epidérmico, composição farmacêutica e usos do mesmo
CN104334191A (zh) * 2012-03-29 2015-02-04 纽约市哥伦比亚大学托管会 治疗毛发脱落疾病的方法
US9422311B2 (en) 2012-10-18 2016-08-23 Bristol-Myers Squibb Company Compounds for the treatment of hepatitis C
WO2014072419A1 (en) 2012-11-08 2014-05-15 Universiteit Antwerpen Novel anti-hiv compounds
US8987265B2 (en) 2012-11-09 2015-03-24 Bristol-Myers Squibb Company Substituted 1,3,5-triazine derivatives of fused bicyclic oxalamide compounds for treatment of Hepatitis C
US8987264B2 (en) 2012-11-09 2015-03-24 Bristol-Myers Squibb Company 1,3,5-triazine derivatives of spiro bicyclic oxalamide-compounds for treatment of hepatitis C
WO2014100748A1 (en) 2012-12-21 2014-06-26 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
WO2014116772A2 (en) 2013-01-25 2014-07-31 Bristol-Myers Squibb Company Squaric derivatives for the treatment of hepatitis c
JP2016505070A (ja) 2013-01-25 2016-02-18 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company C型肝炎の治療用のグアニジン誘導体
US9624245B2 (en) 2013-02-07 2017-04-18 Bristol-Myers Squibb Company Macrocyclic compounds as HCV entry inhibitors
WO2014123892A1 (en) 2013-02-07 2014-08-14 Bristol-Myers Squibb Company Macrocyclic molecules as hcv entry inhibitors
EP2953457B1 (en) 2013-02-08 2020-04-08 Celgene CAR LLC Erk inhibitors and uses thereof
HK1211235A1 (en) 2013-02-22 2016-05-20 霍夫曼-拉罗奇有限公司 Methods of treating cancer and preventing drug resistance
JP2016515105A (ja) 2013-03-07 2016-05-26 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company C型肝炎の処置のためのピリミジン化合物
ES2673867T3 (es) 2013-03-07 2018-06-26 Bristol-Myers Squibb Company Compuestos macrocíclicos para el tratamiento de la hepatitis C
SG11201507486SA (en) 2013-03-13 2015-10-29 Forma Therapeutics Inc Novel compounds and compositions for inhibition of fasn
US9492471B2 (en) 2013-08-27 2016-11-15 Celgene Avilomics Research, Inc. Methods of treating a disease or disorder associated with Bruton'S Tyrosine Kinase
US9415049B2 (en) 2013-12-20 2016-08-16 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
EP3179858B1 (en) 2014-08-13 2019-05-15 Celgene Car Llc Forms and compositions of an erk inhibitor
JP6902466B2 (ja) 2014-11-07 2021-07-14 ザ リージェンツ オブ ザ ユニバーシティ オブ ミシガン ミオカルディン関連転写因子および血清応答因子(mrtf/srf)媒介性遺伝子転写の阻害剤ならびにその使用方法
CA2999931A1 (en) 2015-09-29 2017-04-06 Bayer Pharma Aktiengesellschaft Novel macrocyclic sulfondiimine compounds
CN108368129B (zh) 2015-10-08 2021-08-17 拜耳医药股份有限公司 改性大环化合物
WO2017060322A2 (en) 2015-10-10 2017-04-13 Bayer Pharma Aktiengesellschaft Ptefb-inhibitor-adc
GB2560713A (en) * 2017-03-20 2018-09-26 Eternygen Gmbh Inhibitor of citrate transporter
EP3601253B1 (en) 2017-03-28 2021-09-15 Bayer Aktiengesellschaft Novel ptefb inhibiting macrocyclic compounds
EP3601236A1 (en) 2017-03-28 2020-02-05 Bayer Aktiengesellschaft Novel ptefb inhibiting macrocyclic compounds
TWI767148B (zh) 2018-10-10 2022-06-11 美商弗瑪治療公司 抑制脂肪酸合成酶(fasn)
CN113382633A (zh) 2018-10-29 2021-09-10 福马治疗股份有限公司 (4-(2-氟-4-(1-甲基-1H-苯并[d]咪唑-5-基)苯甲酰基)哌嗪-1-基)(1-羟基环丙基)甲酮的固体形式
SG11202107080VA (en) 2019-01-11 2021-07-29 Naegis Pharmaceuticals Inc Leukotriene synthesis inhibitors
KR20210142154A (ko) 2019-03-21 2021-11-24 옹쎄오 암 치료를 위한 키나제 억제제와 조합된 dbait 분자
CN114761013A (zh) 2019-09-27 2022-07-15 迪斯克医药公司 治疗骨髓纤维化和相关病症的方法
CN114761006A (zh) 2019-11-08 2022-07-15 Inserm(法国国家健康医学研究院) 对激酶抑制剂产生耐药性的癌症的治疗方法
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
WO2021168074A1 (en) * 2020-02-18 2021-08-26 Theseus Pharmaceuticals, Inc. Macrocyclic compounds and uses thereof
KR20230012539A (ko) 2020-05-13 2023-01-26 디스크 메디슨, 인크. 골수섬유증을 치료하기 위한 항-헤모주벨린 (hjv) 항체
CN113698408B (zh) * 2020-05-22 2025-07-25 武汉朗来科技发展有限公司 Jnk抑制剂、其药物组合物和用途
CN113735856A (zh) * 2020-05-29 2021-12-03 百极弘烨(南通)医药科技有限公司 大环jak抑制剂及其应用
CN113549113A (zh) * 2020-06-17 2021-10-26 广州百霆医药科技有限公司 一种含膦大环化合物及其制备方法与应用
CN114805371B (zh) * 2021-01-19 2024-05-24 江苏开元药业有限公司 含2-氨基嘧啶大环类化合物及其制备方法和用途
WO2023046030A1 (zh) * 2021-09-23 2023-03-30 河南晟翔医药科技有限公司 一种egfr小分子抑制剂、含其的药物组合物及其用途
JP2024546154A (ja) * 2021-12-15 2024-12-17 ワン イン ファーマシューティカル カンパニー リミテッド 大環状ピリミジン誘導体、その製造方法、及び、それを活性成分として含む神経変性疾患の予防又は治療のための医薬組成物
CN114394974B (zh) * 2022-03-25 2022-12-06 中国药科大学 多取代三芳基大环化合物与应用
TW202417421A (zh) * 2022-08-08 2024-05-01 美商雅捷可斯治療公司 作為jak2抑制劑之雜環醯胺及脲化合物
WO2024094171A1 (zh) * 2022-11-04 2024-05-10 江苏恒瑞医药股份有限公司 取代的氨基嘧啶类化合物、其制备方法及其在医药上的应用
CN116496234B (zh) * 2023-02-09 2024-09-13 江苏润安制药有限公司 一种盐酸乌拉地尔关键中间体的制备方法

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2006501271A (ja) * 2002-08-21 2006-01-12 シエーリング アクチエンゲゼルシャフト 大環状ピリミジン類、それらの生成及び医薬剤
WO2006061415A1 (en) * 2004-12-08 2006-06-15 Janssen Pharmaceutica N.V. 2,4 (4,6) pyrimidine derivatives

Family Cites Families (41)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5521184A (en) 1992-04-03 1996-05-28 Ciba-Geigy Corporation Pyrimidine derivatives and processes for the preparation thereof
JP2002517396A (ja) 1998-06-04 2002-06-18 アボット・ラボラトリーズ 細胞接着阻害抗炎症性化合物
PA8474101A1 (es) 1998-06-19 2000-09-29 Pfizer Prod Inc Compuestos de pirrolo [2,3-d] pirimidina
ATE459616T1 (de) 1998-08-11 2010-03-15 Novartis Ag Isochinoline derivate mit angiogenesis-hemmender wirkung
US6133031A (en) 1999-08-19 2000-10-17 Isis Pharmaceuticals Inc. Antisense inhibition of focal adhesion kinase expression
GB9905075D0 (en) 1999-03-06 1999-04-28 Zeneca Ltd Chemical compounds
UA72290C2 (uk) 1999-12-10 2005-02-15 Пфайзер Продактс Інк. СПОЛУКИ ПІРОЛО[2.3-d]ПІРИМІДИНУ, ФАРМАЦЕВТИЧНА КОМПОЗИЦІЯ (ВАРІАНТИ), СПОСІБ ІНГІБУВАННЯ ПРОТЕЇНКІНАЗ АБО JANUS КІНАЗИ 3 (ВАРІАНТИ)
CN1615873A (zh) 1999-12-24 2005-05-18 阿文蒂斯药物有限公司 氮杂吲哚类化合物
GB0004890D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
GB0011527D0 (en) 2000-05-12 2000-06-28 Unilever Plc Bleach catalyst and composition and method for bleaching a substrate
JP4188078B2 (ja) 2000-06-28 2008-11-26 スミスクライン ビーチャム ピー エル シー 湿式粉砕法
AU2002337142B2 (en) 2001-09-19 2007-10-11 Aventis Pharma S.A. Indolizines as kinase protein inhibitors
EP1441737B1 (en) 2001-10-30 2006-08-09 Novartis AG Staurosporine derivatives as inhibitors of flt3 receptor tyrosine kinase activity
PE20040522A1 (es) 2002-05-29 2004-09-28 Novartis Ag Derivados de diarilurea dependientes de la cinasa de proteina
GB0215676D0 (en) 2002-07-05 2002-08-14 Novartis Ag Organic compounds
US6919484B2 (en) 2002-07-25 2005-07-19 University Of Florida Method for incorporation of pentafluorosulfanyl (SF5) substituents into aliphatic and aromatic compounds
TWI335913B (en) 2002-11-15 2011-01-11 Vertex Pharma Diaminotriazoles useful as inhibitors of protein kinases
UA80767C2 (en) 2002-12-20 2007-10-25 Pfizer Prod Inc Pyrimidine derivatives for the treatment of abnormal cell growth
WO2004072063A1 (en) 2003-02-07 2004-08-26 Vertex Pharmaceuticals Incorporated Heteroaryl substituted pyrolls useful as inhibitors of protein kinases
WO2004078682A2 (en) 2003-03-05 2004-09-16 Irm Llc Cyclic compounds and compositions as protein kinase inhibitors
DK1454992T3 (da) 2003-03-07 2006-10-02 Ist Naz Stud Cura Dei Tumori Anaplastisk lymfomakinaseassay, reagenser og sammensætninger deraf
GB0305929D0 (en) 2003-03-14 2003-04-23 Novartis Ag Organic compounds
SE0301373D0 (sv) 2003-05-09 2003-05-09 Astrazeneca Ab Novel compounds
SE0301372D0 (sv) 2003-05-09 2003-05-09 Astrazeneca Ab Novel compounds
GB0316109D0 (en) 2003-07-09 2003-08-13 Dystar Textilfarben Gmbh & Co Water-soluble macrocyclic azacalixarenes
GB0316915D0 (en) 2003-07-18 2003-08-20 Glaxo Group Ltd Compounds
DE10333183A1 (de) 2003-07-22 2005-02-17 Daimlerchrysler Ag Verfahren zum Betrieb eines Antriebsstranges für ein Kraftfahrzeug
CN1867334A (zh) 2003-07-22 2006-11-22 詹森药业有限公司 作为c-fms激酶抑制剂的喹啉酮衍生物
AR045944A1 (es) 2003-09-24 2005-11-16 Novartis Ag Derivados de isoquinolina 1.4-disustituidas
JP2005220116A (ja) 2004-02-09 2005-08-18 Japan Science & Technology Agency 1,3,5−トリアジン環を環構成要素として含むシクロファン型化合物、その製造方法、中間体及びその利用
RS55546B1 (sr) 2004-05-13 2017-05-31 Icos Corp Hinazolinoni kao inhibitori humane fosfatidilonozitol 3-delta kinaze
WO2006056399A2 (en) 2004-11-24 2006-06-01 Novartis Ag Combinations of jak inhibitors and at least one of bcr-abl, flt-3, fak or raf kinase inhibitors
US20060194823A1 (en) 2004-12-22 2006-08-31 Georg Kettschau Sulfonamido-macrocycles as Tie2 inhibitors and the salts thereof, a pharmaceutical composition comprising these compounds, the method of preparing and the use thereof
EP1674470A1 (en) 2004-12-22 2006-06-28 Schering Aktiengesellschaft Sulfonamido-macrocycles as Tie2 inhibitors
EP1710246A1 (en) 2005-04-08 2006-10-11 Schering Aktiengesellschaft Sulfoximine-pyrimidine Macrocycles and the salts thereof, a process for making them, and their pharmaceutical use against cancer
ES2330789T3 (es) 2005-06-30 2009-12-15 Janssen Pharmaceutica Nv Anilino-piridinotriazinas ciclicas como inhibidores de gsk-3.
TWI525096B (zh) 2005-11-16 2016-03-11 Cti生技製藥有限公司 氧連接之嘧啶衍生物
DK3184526T3 (en) 2005-12-13 2019-01-14 Incyte Holdings Corp PYRROLO [2,3-D] PYRIMIDINE DERIVATIVES AS A JANUS-KINASE INHIBITOR
EP1803723A1 (de) 2006-01-03 2007-07-04 Bayer Schering Pharma Aktiengesellschaft (2,4,9-triaza-1(2,4)-pyrimidina-3(1,3)-benzenacyclononaphan-3^4-yl)-sulfoximid derivate als selektive inhibitoren der aurora kinase zur behandlung von krebs
EP1873159A1 (en) 2006-06-21 2008-01-02 Bayer Schering Pharma Aktiengesellschaft Substituted sulphonamido-macrocycles as Tie2 inhibitors and salts thereof, pharmaceutical compositions comprising same, methods of preparing same and uses of same
EP1870416A1 (en) 2006-06-21 2007-12-26 Bayer Schering Pharma Aktiengesellschaft Sulphonamido-macrocycles as tie2 inhibitors

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2006501271A (ja) * 2002-08-21 2006-01-12 シエーリング アクチエンゲゼルシャフト 大環状ピリミジン類、それらの生成及び医薬剤
WO2006061415A1 (en) * 2004-12-08 2006-06-15 Janssen Pharmaceutica N.V. 2,4 (4,6) pyrimidine derivatives

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2016041709A (ja) * 2012-03-06 2016-03-31 ファイザー・インク 増殖性疾患の治療のための大環状誘導体
JP2016505069A (ja) * 2013-01-25 2016-02-18 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company C型肝炎の治療用のアンモニウム誘導体
JP2016540824A (ja) * 2013-12-20 2016-12-28 インスティテュート オブ ファーマコロジー アンド トキシコロジー アカデミー オブ ミリタリー メディカル サイエンシズ ピー.エル.エー.チャイナ 新規ピペリジンカルボキサミド化合物、その調製方法及び使用
JP2023513793A (ja) * 2020-02-14 2023-04-03 ソーク インスティテュート フォー バイオロジカル スタディーズ 大環状ulk1/2阻害剤

Also Published As

Publication number Publication date
WO2009132202A3 (en) 2010-11-25
EP2274288A2 (en) 2011-01-19
US20090286778A1 (en) 2009-11-19
WO2009132202A2 (en) 2009-10-29
CA2722326A1 (en) 2009-10-29
US8871753B2 (en) 2014-10-28

Similar Documents

Publication Publication Date Title
US8871753B2 (en) Macrocyclic compounds and their use as kinase inhibitors
JP6173327B2 (ja) イミダゾピリダジン化合物
JP5063700B2 (ja) アニリノピペラジン誘導体およびアニリノピペラジン誘導体を使用する方法
JP5335426B2 (ja) ジアリールアミン含有化合物および組成物、ならびにc−kit受容体のモジュレーターとしてのそれらの使用
KR101663277B1 (ko) TNIK, IKKε 및 TBK1 억제제로서의 피라졸계 유도체 및 이를 포함하는 약학적 조성물
RU2610840C2 (ru) Тиазолопиримидины
CN105209468B (zh) 取代的7‑氮杂二环化合物以及它们作为食欲素受体调节剂的用途
CN112638373A (zh) 细胞周期蛋白依赖性激酶抑制剂
AU2014248763B2 (en) Substituted piperidine compounds and their use as orexin receptor modulators
MX2011005800A (es) Derivados de n{[(1r,4s,6r)-3-(2-piridinilcarbonil)-3-azabiciclo[4. 1.0]hept-4-il]metil}-2-heteroarilamina y sus usos.
JP2007514690A (ja) ヒスタミンh3アンタゴニストとしてのベンズアゼピン誘導体
JP2008531723A (ja) フタラジン、アザ及びジアザフタラジン化合物並びに使用方法
KR20100134693A (ko) 2-아미노퀴나졸린 유도체
WO2015152367A1 (ja) オキソ複素環誘導体
JP2017122103A (ja) うつ病、糖尿病及びパーキンソン病のような幾つかの障害の処置において使用するためのtaar調節薬としてのピラゾールカルボキサミド誘導体
CN111225912A (zh) 作为btk抑制剂的5-氨基吡唑甲酰胺化合物及其制备方法
DK2832728T3 (en) TRIAZINONE CONNECTION AND TYPE OF T-CALCIUM CHANNEL INHIBITORS
CN103443107B (zh) 噻唑并嘧啶化合物
HK1192227B (en) Thiazolopyrimidine compounds
HK1196359A (en) Imidazopyridazine compounds
HK1196359B (en) Imidazopyridazine compounds

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20120423

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20120423

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20131031

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20140219

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20140226

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20140319

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20140327

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20140418

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20140425

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20140519

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20140909