JP2011525915A - キナーゼ阻害薬としてのアルキニルアルコール類 - Google Patents

キナーゼ阻害薬としてのアルキニルアルコール類 Download PDF

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JP2011525915A
JP2011525915A JP2011516311A JP2011516311A JP2011525915A JP 2011525915 A JP2011525915 A JP 2011525915A JP 2011516311 A JP2011516311 A JP 2011516311A JP 2011516311 A JP2011516311 A JP 2011516311A JP 2011525915 A JP2011525915 A JP 2011525915A
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alkylene
mmol
bromo
alkyl
balance
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JP2011525915A5 (enExample
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チエン，クオチン
クツシング，テイモシー・デイー
フイツシヤー，ベンジヤミン
ホー，シヤオ
リー，カーシユエ
リー，ジーホン
マギー，ローレンス・アール
パツタロポン，バテイー
フオルダー，ポール
セガニツシユ，ジエニフアー・エル
シン，ヨンスク
ワン，ジユウラン
リウ，ウエン
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アムジエン・インコーポレーテツド
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Publication of JP2011525915A publication Critical patent/JP2011525915A/ja
Publication of JP2011525915A5 publication Critical patent/JP2011525915A5/ja
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    • 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
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
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    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
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    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • C07D213/82—Amides; Imides in position 3
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    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D233/88—Nitrogen atoms, e.g. allantoin
    • C—CHEMISTRY; METALLURGY
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
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    • 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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
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    • 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
    • C07D407/08—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 carbon chain containing alicyclic rings
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    • 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
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
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    • 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
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    • 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
    • C07D417/02—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 two hetero rings
    • C07D417/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07—ORGANIC CHEMISTRY
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    • 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
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    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
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    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
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    • C07D495/10—Spiro-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Oncology (AREA)
  • Psychiatry (AREA)
  • Transplantation (AREA)
  • Hematology (AREA)
  • Otolaryngology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pyridine Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
JP2011516311A 2008-06-26 2009-06-26 キナーゼ阻害薬としてのアルキニルアルコール類 Withdrawn JP2011525915A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US13324908P 2008-06-26 2008-06-26
US61/133,249 2008-06-26
PCT/US2009/003803 WO2009158011A1 (en) 2008-06-26 2009-06-26 Alkynyl alcohols as kinase inhibitors

Publications (2)

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JP2011525915A true JP2011525915A (ja) 2011-09-29
JP2011525915A5 JP2011525915A5 (enExample) 2012-06-07

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JP2011516311A Withdrawn JP2011525915A (ja) 2008-06-26 2009-06-26 キナーゼ阻害薬としてのアルキニルアルコール類

Country Status (7)

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US (1) US20110086834A1 (enExample)
EP (1) EP2315751A1 (enExample)
JP (1) JP2011525915A (enExample)
AU (1) AU2009263037B2 (enExample)
CA (1) CA2728767A1 (enExample)
MX (1) MX2010013920A (enExample)
WO (1) WO2009158011A1 (enExample)

Cited By (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2016517859A (ja) * 2013-04-24 2016-06-20 ヤンセン ファーマシューティカ エヌ．ベー． 癌を治療するための、ｎｉｋ阻害剤としての３−（２−アミノピリミジン−４−イル）−５−（３−ヒドロキシプロピニル）−１ｈ−ピロロ［２，３−ｃ］ピリジン誘導体
JP2016531127A (ja) * 2013-08-22 2016-10-06 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ アルキニルアルコール及び使用方法
JP2016531868A (ja) * 2013-09-26 2016-10-13 ヤンセン ファーマシューティカ エヌ．ベー． 新規な、ＮＩＫ阻害剤としての１−（４−ピリミジニル）−１Ｈ−ピロロ［３，２−ｃ］ピリジン誘導体
JP2016531858A (ja) * 2013-09-26 2016-10-13 ヤンセン ファーマシューティカ エヌ．ベー． 新規な、ＮＩＫ阻害剤としての３−（１Ｈ−ピラゾール−４−イル）−１Ｈ−ピロロ［２，３−ｃ］ピリジン誘導体
JP2016533385A (ja) * 2013-08-22 2016-10-27 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ アルキニルアルコール及び使用方法
KR20170068489A (ko) * 2014-10-23 2017-06-19 얀센 파마슈티카 엔.브이. Ｎｉｋ 억제제로서의 신규 피라졸로피리미딘 유도체
JP2017531681A (ja) * 2014-10-23 2017-10-26 ヤンセン ファーマシューティカ エヌ．ベー． Ｎｉｋ阻害剤としての新規化合物
JP2017531675A (ja) * 2014-10-23 2017-10-26 ヤンセン ファーマシューティカ エヌ．ベー． Ｎｉｋ阻害剤としての新規のチエノピリミジン誘導体
JP2017531677A (ja) * 2014-10-23 2017-10-26 ヤンセン ファーマシューティカ エヌ．ベー． 新規な、ｎｉｋ阻害剤としてのピラゾール誘導体
JP2018514587A (ja) * 2015-04-29 2018-06-07 カントン チョンション ファーマシューティカル カンパニー，リミティド キナーゼ阻害剤としての縮合環式または三環式アリールピリミジン化合物
JP2019502714A (ja) * 2016-01-22 2019-01-31 ジャンセン ファーマシューティカ エヌブイ Ｎｉｋ阻害剤としての新たな６員のヘテロ芳香族置換シアノインドリン誘導体
JP2019504067A (ja) * 2016-01-22 2019-02-14 ジャンセン ファーマシューティカ エヌブイ Ｎｉｋ阻害剤としての新たな置換されたシアノインドリン誘導体
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JP2019528293A (ja) * 2016-08-24 2019-10-10 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ ２−アザビシクロ［３．１．０］ヘキサン−３−オン誘導体及び使用方法
JP2022534302A (ja) * 2019-05-31 2022-07-28 ヤンセン ファーマシューティカ エヌ．ベー． ＮＦ－κＢ誘導キナーゼの低分子阻害剤
JP2023530271A (ja) * 2020-06-12 2023-07-14 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 Ａｐｏｌ１の阻害剤及びこれを使用する方法

Families Citing this family (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2787785C (en) 2010-01-28 2018-03-06 President And Fellows Of Harvard College Compositions and methods for enhancing proteasome activity
EP2796456A1 (en) * 2010-12-09 2014-10-29 Amgen Inc. Bicyclic compounds as Pim inhibitors
CN103476768B (zh) 2011-03-16 2015-07-08 弗·哈夫曼-拉罗切有限公司 6,5-杂环炔丙醇化合物及其用途
EP2688886A1 (en) 2011-03-22 2014-01-29 Amgen Inc. Azole compounds as pim inhibitors
WO2012135697A2 (en) * 2011-03-30 2012-10-04 H. Lee Moffitt Cancer Center & Research Institute Inc. Novel rho kinase inhibitors and methods of use
WO2012154967A1 (en) 2011-05-12 2012-11-15 Proteostasis Therapeutics, Inc. Proteostasis regulators
EP2551670A1 (en) 2011-07-27 2013-01-30 Merck Patent GmbH NIK inhibitors cell-based assay
WO2013057944A1 (ja) 2011-10-19 2013-04-25 興和株式会社 新規なスピロインドリン化合物、及びそれを含有する医薬
BR112014019209A2 (pt) 2012-02-17 2017-07-04 Hoffmann La Roche compostos tricíclicos e métodos de uso para os mesmos
US9849135B2 (en) 2013-01-25 2017-12-26 President And Fellows Of Harvard College USP14 inhibitors for treating or preventing viral infections
WO2015073528A1 (en) 2013-11-12 2015-05-21 Proteostasis Therapeutics, Inc. Proteasome activity enhancing compounds
HUE052099T2 (hu) 2014-04-04 2021-04-28 Iomet Pharma Ltd Indol származékok felhasználásra az orvostudományban
KR101551313B1 (ko) 2014-07-28 2015-09-09 충남대학교산학협력단 신규한 인덴 유도체, 이의 제조방법 및 이를 유효성분으로 함유하는 망막 질환의 예방 또는 치료용 약학적 조성물
EP3262035A1 (en) * 2015-02-25 2018-01-03 F. Hoffmann-La Roche AG Alkynyl alcohols and methods of use
CN105769871A (zh) * 2016-03-03 2016-07-20 东北师范大学 Nik蛋白激酶抑制剂作为制备治疗肝病的药物的应用
EA037358B1 (ru) * 2016-03-10 2021-03-17 Янссен Фармасьютика Нв Новые замещённые производные цианиндолина в качестве nik-ингибиторов
CA3027416A1 (en) 2016-06-30 2018-01-04 Janssen Pharmaceutica Nv Heteroaromatic derivatives as nik inhibitors
ES2837157T3 (es) 2016-06-30 2021-06-29 Janssen Pharmaceutica Nv Derivados de cianoindolina como inhibidores de NIK
US10858319B2 (en) 2016-10-03 2020-12-08 Iomet Pharma Ltd. Indole derivatives for use in medicine
CA3063288A1 (en) 2017-05-12 2018-11-15 Mavalon Therapeutics Limited Substituted heterocyclic compounds as allosteric modulators of group ii metabotropic glutamate receptors
CN109810110B (zh) * 2017-11-22 2023-01-24 中国科学院上海药物研究所 一种具有2-氨基嘧啶结构的化合物，其制备方法和用途
WO2019183145A1 (en) 2018-03-20 2019-09-26 Plexxikon Inc. Compounds and methods for ido and tdo modulation, and indications therefor
EP3782702A1 (en) * 2019-08-21 2021-02-24 AC BioScience SA Compounds and use thereof for the treatment of infectious diseases and cancer
CN113831325A (zh) * 2020-06-23 2021-12-24 沈阳药科大学 新型吲哚类衍生物及其制备方法和应用
CN111960983A (zh) * 2020-08-31 2020-11-20 南通大学 一种n-甲基-3-(1-甲基吡咯烷-3-基)丙-1-胺及其合成方法
CN112194609B (zh) * 2020-10-22 2022-11-04 西北农林科技大学 3,3-二取代氧化吲哚类化合物及其制备方法与用途
CN112174938A (zh) * 2020-10-27 2021-01-05 浙江工业大学 4-吲哚-2-氨基嘧啶类化合物及其应用
CN115215861B (zh) * 2021-04-16 2024-03-15 上海翊石医药科技有限公司 一种芳杂环取代的炔烃类化合物及其制备方法和用途

Family Cites Families (35)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK429884A (da) * 1983-10-07 1985-04-08 Hoffmann La Roche Heterocycliske forbindelser
GB8714537D0 (en) * 1987-06-22 1987-07-29 Ici Plc Pyrazine derivatives
GB2208860B (en) * 1987-08-20 1991-10-09 Ici Plc Pyrimidine derivatives
GB9016783D0 (en) * 1989-09-01 1990-09-12 Ici Plc Agrochemical compositions
CA2167673C (en) * 1993-07-21 2004-09-21 Akihiro Tanaka Condensed benzazepine derivative and pharmaceutical composition thereof
EP0746554A1 (en) * 1994-02-23 1996-12-11 Pfizer Inc. 4-heterocyclyl-substituted quinazoline derivatives, processes for their preparation and their use as anti-cancer agents
US6063930A (en) * 1996-04-03 2000-05-16 Merck & Co., Inc. Substituted imidazole compounds useful as farnesyl-protein transferase inhibitors
ZA986729B (en) * 1997-07-29 1999-02-02 Warner Lambert Co Irreversible inhibitors of tyrosine kinases
GB9716446D0 (en) * 1997-08-05 1997-10-08 Agrevo Uk Ltd Fungicides
US6576656B1 (en) * 1998-08-20 2003-06-10 Sumitomo Pharmaceuticals Co., Ltd. Oxindole derivative
UA71945C2 (en) * 1999-01-27 2005-01-17 Pfizer Prod Inc Substituted bicyclic derivatives being used as anticancer agents
JP2002053561A (ja) * 1999-12-08 2002-02-19 Sumitomo Chem Co Ltd ジフルオロメチルトリアゾロン化合物、その用途およびその製造中間体
US6313310B1 (en) * 1999-12-15 2001-11-06 Hoffmann-La Roche Inc. 4-and 5-alkynyloxindoles and 4-and 5-alkenyloxindoles
US20020019527A1 (en) * 2000-04-27 2002-02-14 Wei-Bo Wang Substituted phenyl farnesyltransferase inhibitors
US20020115640A1 (en) * 2000-11-30 2002-08-22 Claiborne Akiyo K. Farnesyltransferase inhibitors
US7211595B2 (en) * 2000-11-30 2007-05-01 Abbott Laboratories Farnesyltransferase inhibitors
US6504034B2 (en) * 2001-01-23 2003-01-07 Hoffmann-La Roche Inc. Naphthostyrils
GB0123589D0 (en) * 2001-10-01 2001-11-21 Syngenta Participations Ag Organic compounds
JP4559087B2 (ja) * 2002-04-26 2010-10-06 イーライ リリー アンド カンパニー タキキニン受容体アンタゴニストとしてのトリアゾール誘導体
PT1501808E (pt) * 2002-04-26 2008-09-26 Lilly Co Eli Antagonistas de receptores taquiquininas
US20030216441A1 (en) * 2002-05-10 2003-11-20 Gwaltney Stephen L. Farnesyltransferase inhibitors
DE10229762A1 (de) * 2002-07-03 2004-01-22 Aventis Pharma Deutschland Gmbh Pyrazoloisoquinolinenderivaten zur Inhibierung von NFkappaB-induzierende Kinase
US20050035498A1 (en) * 2003-08-13 2005-02-17 Stevens Randal Alan Methods of making a negative hearing aid mold
US20070167426A1 (en) * 2004-06-02 2007-07-19 Schering Corporation Compounds for the treatment of inflammatory disorders and microbial diseases
PE20060426A1 (es) * 2004-06-02 2006-06-28 Schering Corp DERIVADOS DE ACIDO TARTARICO COMO INHIBIDORES DE MMPs, ADAMs, TACE Y TNF-alfa
US7396852B2 (en) * 2005-11-16 2008-07-08 Xerox Corporation Compound having indolocarbazole moiety and divalent linkage
US7829727B2 (en) * 2005-11-16 2010-11-09 Xerox Corporation Device containing compound having indolocarbazole moiety and divalent linkage
CA2570780C (en) * 2004-06-17 2013-12-03 Infinity Pharmaceuticals, Inc. Compounds and methods for inhibiting the interaction of bcl proteins with binding partners
JP2008519850A (ja) * 2004-11-10 2008-06-12 シンタ ファーマシューティカルズ コーポレーション Ｉｌ−１２調節化合物
US20060174937A1 (en) * 2005-02-09 2006-08-10 Zhang-Lin Zhou High performance organic materials for solar cells
AR056786A1 (es) * 2005-11-10 2007-10-24 Smithkline Beecham Corp Compuesto de 1h- imidazo ( 4,5-c) piridin-2-ilo, composicion farmaceutica que lo comprende, procedimiento para preparar dicha composicion, su uso para preparar unmedicamento, uso de una combinacion que omprende al compuesto y al menos un agente antineoplasico para preparar un medicamento y dicha com
WO2007058852A2 (en) * 2005-11-10 2007-05-24 Smithkline Beecham Corporation Inhibitors of akt activity
US20080269131A1 (en) * 2005-11-10 2008-10-30 Smithkline Beecham Corporation Inhibitors of Akt Activity
JP2010518014A (ja) * 2007-01-31 2010-05-27 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 キナーゼ阻害剤として有用な２−アミノピリジン誘導体
US8343966B2 (en) * 2008-01-11 2013-01-01 Novartis Ag Organic compounds

Cited By (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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JP2016533385A (ja) * 2013-08-22 2016-10-27 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ アルキニルアルコール及び使用方法
US9981963B2 (en) 2013-09-26 2018-05-29 Janssen Pharmaceutica Nv 3-(1H-pyrazol-4-yl)-1H-pyrrolo[2,3-c]pyridine derivatives as NIK inhibitors
JP2016531868A (ja) * 2013-09-26 2016-10-13 ヤンセン ファーマシューティカ エヌ．ベー． 新規な、ＮＩＫ阻害剤としての１−（４−ピリミジニル）−１Ｈ−ピロロ［３，２−ｃ］ピリジン誘導体
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US9981962B2 (en) 2014-10-23 2018-05-29 Janssen Pharmaceutica Nv Pyrazole derivatives as NIK inhibitors
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