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

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic 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
    • C07D239/28—Heterocyclic 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
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen atoms
    • 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
    • A61P1/04—Drugs 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
    • 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
    • A61P11/02—Nasal agents, e.g. decongestants
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • 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
    • A61P17/04—Antipruritics
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • 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
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • 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
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • 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
    • A61P31/20—Antivirals for DNA viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D407/00—Heterocyclic 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
    • C07D407/02—Heterocyclic 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
    • C07D407/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic 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
    • C07D413/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (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)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Endocrinology (AREA)
  • Rheumatology (AREA)
  • Neurology (AREA)
  • Cardiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Biomedical Technology (AREA)
  • Emergency Medicine (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • Ophthalmology & Optometry (AREA)
  • Obesity (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 (78)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2013202496B2 (en) * 2008-06-27 2016-08-04 Celgene Car Llc Heteroaryl compounds and uses thereof
US11351168B1 (en) 2008-06-27 2022-06-07 Celgene Car Llc 2,4-disubstituted pyrimidines useful as kinase inhibitors
US8338439B2 (en) 2008-06-27 2012-12-25 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
AU2009262068C1 (en) 2008-06-27 2015-07-02 Celgene Car Llc Heteroaryl compounds and uses thereof
ES2668834T3 (es) * 2008-09-08 2018-05-22 Merck Serono Sa Pirimidinas macrociclicas como inhibidores de proteína quinasas
US8765727B2 (en) 2009-01-23 2014-07-01 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
JP2013508285A (ja) 2009-10-14 2013-03-07 ブリストル−マイヤーズ スクイブ カンパニー C型肝炎の処置のための組成物
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
US20120101108A1 (en) 2010-08-06 2012-04-26 Cell Signaling Technology, Inc. Anaplastic Lymphoma Kinase In Kidney Cancer
PH12013500246A1 (en) 2010-08-10 2019-10-11 Celgene Avilomics Res Inc Besylate salt of a btk inhibitor
US8765944B2 (en) 2010-08-19 2014-07-01 Bristol-Myers Squibb Company Compounds for the treatment of hepatitis C
BR112013010564B1 (pt) 2010-11-01 2021-09-21 Celgene Car Llc Compostos heterocíclicos e composições compreendendo os mesmos
JP5956999B2 (ja) 2010-11-01 2016-07-27 セルジーン アヴィロミクス リサーチ, インコーポレイテッド ヘテロアリール化合物およびその使用
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
PT2635299T (pt) * 2010-11-02 2019-10-14 Univ Columbia Métodos de tratamento de distúrbios de perda de cabelo
EP2637502B1 (en) 2010-11-10 2018-01-10 Celgene CAR LLC Mutant-selective egfr inhibitors and uses thereof
WO2012074951A1 (en) * 2010-11-29 2012-06-07 OSI Pharmaceuticals, LLC Macrocyclic kinase inhibitors
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
EP2697230B1 (en) * 2011-04-14 2016-03-30 Bristol-Myers Squibb Company Compounds for the treatment of hepatitis c
MX2014001945A (es) 2011-08-19 2014-03-27 Merck Sharp & Dohme Procedimiento e intermedios para la preparacion de macrolactamas.
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
JP2014532658A (ja) 2011-10-28 2014-12-08 セルジーン アヴィロミクス リサーチ, インコーポレイテッド ブルトン型チロシンキナーゼ疾患または障害を治療する方法
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
ES2880109T3 (es) 2012-03-15 2021-11-23 Celgene Car Llc Formas sólidas de un inhibidor de la cinasa del receptor del factor de crecimiento epidérmico
JP6317320B2 (ja) 2012-03-15 2018-04-25 セルジーン シーエーアール エルエルシー 上皮成長因子受容体キナーゼ阻害剤の塩
DK2830662T3 (da) * 2012-03-29 2019-01-02 Univ Columbia Fremgangsmåder til behandlng af hårtabsforstyrrelser
EP2917222A1 (en) 2012-10-18 2015-09-16 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
US9126950B2 (en) 2012-12-21 2015-09-08 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
EP2948434B1 (en) 2013-01-25 2017-03-01 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
EP2953953B1 (en) 2013-02-07 2017-11-15 Bristol-Myers Squibb Company Macrocyclic molecules as hcv entry inhibitors
EP2953954B1 (en) 2013-02-07 2017-11-15 Bristol-Myers Squibb Company Macrocyclic compounds as hcv entry inhibitors
CN105188371A (zh) 2013-02-08 2015-12-23 西建阿维拉米斯研究公司 Erk抑制剂及其用途
WO2014128235A1 (en) 2013-02-22 2014-08-28 F. Hoffmann-La Roche Ag Methods of treating cancer and preventing drug resistance
CN105164115A (zh) 2013-03-07 2015-12-16 百时美施贵宝公司 用于治疗丙型肝炎的嘧啶化合物
EP2964655B1 (en) 2013-03-07 2018-04-25 Bristol-Myers Squibb Company Macrocyclic compounds for the treatment of hepatitis c
MX364895B (es) 2013-03-13 2019-05-10 Forma Therapeutics Inc Nuevos compuestos y composiciones para la inhibicion de 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
WO2016025561A1 (en) 2014-08-13 2016-02-18 Celgene Avilomics Research, Inc. Forms and compositions of an erk inhibitor
EP3215150B1 (en) 2014-11-07 2022-07-20 The Regents of The University of Michigan Inhibitors of myocardin-related transcription factor and serum response factor (mrtf/srf)-mediated gene transcription and methods for use of the same
JP6847099B2 (ja) 2015-09-29 2021-03-24 バイエル ファーマ アクチエンゲゼルシャフト 新規な大環状スルホンジイミン化合物
ES2819869T3 (es) 2015-10-08 2021-04-19 Bayer Pharma AG Nuevos compuestos macrocíclicos modificados
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
CA3057891A1 (en) 2017-03-28 2018-10-04 Bayer Aktiengesellschaft Novel ptefb inhibiting macrocyclic compounds
EP3601253B1 (en) 2017-03-28 2021-09-15 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
CA3126021A1 (en) 2019-01-11 2020-07-16 Naegis Pharmaceuticals Inc. Leukotriene synthesis inhibitors
CA3129665A1 (en) 2019-03-21 2020-09-24 Onxeo A dbait molecule in combination with kinase inhibitor for the treatment of cancer
CA3156007A1 (en) 2019-09-27 2021-04-01 Disc Medicine, Inc. METHODS OF TREATING MYELOFIBROSE AND ASSOCIATED CONDITIONS
KR20220098759A (ko) 2019-11-08 2022-07-12 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) 키나제 억제제에 대해 내성을 획득한 암의 치료 방법
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
JP2023513854A (ja) * 2020-02-18 2023-04-03 テーセウス ファーマシューティカルズ, インコーポレイテッド 大環状化合物およびその使用
ES3075793T3 (en) 2020-05-13 2026-08-07 Disc Medicine Inc Anti-hemojuvelin (hjv) antibodies for treating myelofibrosis
AU2021273014A1 (en) 2020-05-13 2022-11-17 AbbVie Deutschland GmbH & Co. KG Anti-hemojuvelin (HJV) antibodies for treating anemia of chronic disease
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
JP2025528119A (ja) * 2022-08-08 2025-08-26 エイジャックス セラピューティクス, インコーポレイテッド Jak2阻害剤としての複素環式アミド及び尿素化合物
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
AU4231299A (en) 1998-06-04 1999-12-20 Abbott Laboratories Cell adhesion-inhibiting antinflammatory compounds
PA8474101A1 (es) 1998-06-19 2000-09-29 Pfizer Prod Inc Compuestos de pirrolo [2,3-d] pirimidina
ES2342240T3 (es) 1998-08-11 2010-07-02 Novartis Ag Derivados de isoquinolina con actividad que inhibe la angiogenia.
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
OA12118A (en) 1999-12-10 2006-05-04 Pfizer Prod Inc PyrroloÄ2,3-dÜpyrimidine compounds.
HUP0203895A3 (en) 1999-12-24 2004-09-28 Aventis Pharma Ltd West Mallin Substituted azaindoles and pharmaceutical compositions containing them and their use
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
EP1294358B1 (en) 2000-06-28 2004-08-18 Smithkline Beecham Plc Wet milling process
CN100391958C (zh) 2001-09-19 2008-06-04 安万特医药股份有限公司 化合物
PT1441737E (pt) 2001-10-30 2006-12-29 Dana Farber Cancer Inst Inc Derivados de estrutura como inibidores da actividade do receptor de tirosina cinase flt3
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
AR042052A1 (es) 2002-11-15 2005-06-08 Vertex Pharma Diaminotriazoles utiles como inhibidores de proteinquinasas
UA80767C2 (en) 2002-12-20 2007-10-25 Pfizer Prod Inc Pyrimidine derivatives for the treatment of abnormal cell growth
CA2515132C (en) 2003-02-07 2012-01-03 Vertex Pharmaceuticals Incorporated Heteroaryl substituted pyrroles useful as inhibitors of protein kinases
US7151096B2 (en) 2003-03-05 2006-12-19 Irm Llc Cyclic compounds and compositions as protein kinase inhibitors
EP1454992B1 (en) 2003-03-07 2006-05-31 Istituto Nazionale Per Lo Studio E La Cura Dei Tumori Anaplastic lymphoma kinase assay, reagents and compositions thereof
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
CA2533626A1 (en) 2003-07-22 2005-02-03 Janssen Pharmaceutica, N.V. Quinolinone derivatives as inhibitors of c-fms kinase
PE20050952A1 (es) 2003-09-24 2005-12-19 Novartis Ag Derivados de isoquinolina como inhibidores de b-raf
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
LT2612862T (lt) 2004-05-13 2017-01-25 Icos Corporation Chinazolinonai kaip žmogaus fosfatidilinozitol-3-kinazės delta inhibitoriai
RU2007123675A (ru) 2004-11-24 2008-12-27 Новартис АГ (CH) Комбинации ингибиторов jak
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
UA92608C2 (en) 2005-06-30 2010-11-25 Янссен Фармацевтика Н.В. Cyclic anilino - pyridinotriazines as gsk-3 inhibitors
CN101360751B (zh) 2005-11-16 2011-09-14 S*Bio私人有限公司 氧连接的嘧啶衍生物
HUE028588T2 (hu) 2005-12-13 2016-12-28 Incyte Holdings Corp Heteroaril-szubsztituált pirrolo[2,3-b]piridinek és pirrolo[2,3-b]pirimidinek mint Janus-kináz inhibitorok
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
EP2274288A2 (en) 2011-01-19
CA2722326A1 (en) 2009-10-29
US20090286778A1 (en) 2009-11-19
US8871753B2 (en) 2014-10-28
WO2009132202A2 (en) 2009-10-29
WO2009132202A3 (en) 2010-11-25

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
CN103443107B (zh) 噻唑并嘧啶化合物
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
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
CN114728170A (zh) 对核受体具有活性的化合物
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
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