CN102625803A - 药学上有用的杂环-取代的内酰胺 - Google Patents

药学上有用的杂环-取代的内酰胺 Download PDF

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Publication number
CN102625803A
CN102625803A CN2010800499575A CN201080049957A CN102625803A CN 102625803 A CN102625803 A CN 102625803A CN 2010800499575 A CN2010800499575 A CN 2010800499575A CN 201080049957 A CN201080049957 A CN 201080049957A CN 102625803 A CN102625803 A CN 102625803A
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pyrazolo
alkyl
compound
cancer
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CN2010800499575A
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English (en)
Chinese (zh)
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M·哈达齐
D·雷克曼
N·拉法勒
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Cylene Pharmaceuticals Inc
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Cylene Pharmaceuticals Inc
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Publication of CN102625803A publication Critical patent/CN102625803A/zh
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • 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
    • A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • 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
    • C07D403/06—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 carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Vascular Medicine (AREA)
  • Rheumatology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CN2010800499575A 2009-09-11 2010-09-10 药学上有用的杂环-取代的内酰胺 Pending CN102625803A (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US24180609P 2009-09-11 2009-09-11
US61/241,806 2009-09-11
US37114710P 2010-08-05 2010-08-05
US61/371,147 2010-08-05
PCT/US2010/048441 WO2011031979A1 (en) 2009-09-11 2010-09-10 Pharmaceutically useful heterocycle-substituted lactams

Publications (1)

Publication Number Publication Date
CN102625803A true CN102625803A (zh) 2012-08-01

Family

ID=43732815

Family Applications (1)

Application Number Title Priority Date Filing Date
CN2010800499575A Pending CN102625803A (zh) 2009-09-11 2010-09-10 药学上有用的杂环-取代的内酰胺

Country Status (13)

Country Link
US (1) US20110071115A1 (enExample)
EP (1) EP2475652A1 (enExample)
JP (1) JP2013504594A (enExample)
KR (1) KR20120104521A (enExample)
CN (1) CN102625803A (enExample)
AU (1) AU2010292116A1 (enExample)
BR (1) BR112012005550A2 (enExample)
CA (1) CA2773854A1 (enExample)
IL (1) IL218521A0 (enExample)
IN (1) IN2012DN03112A (enExample)
MX (1) MX2012002994A (enExample)
SG (1) SG179083A1 (enExample)
WO (1) WO2011031979A1 (enExample)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014154026A1 (zh) * 2013-03-28 2014-10-02 山东轩竹医药科技有限公司 PI3K和/或mTOR抑制剂的前药
CN115160341A (zh) * 2022-07-18 2022-10-11 中国医学科学院医学实验动物研究所 苯并噁嗪类化合物及其药物用途

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US8329897B2 (en) 2007-07-26 2012-12-11 Vitae Pharmaceuticals, Inc. Synthesis of inhibitors of 11β-hydroxysteroid dehydrogenase type 1
AR069207A1 (es) 2007-11-07 2010-01-06 Vitae Pharmaceuticals Inc Ureas ciclicas como inhibidores de la 11 beta - hidroxi-esteroide deshidrogenasa 1
CA2708303A1 (en) 2007-12-11 2009-06-18 Vitae Pharmaceuticals, Inc. Cyclic urea inhibitors of 11.beta.-hydroxysteroid dehydrogenase 1
TW200934490A (en) 2008-01-07 2009-08-16 Vitae Pharmaceuticals Inc Lactam inhibitors of 11 &abgr;-hydroxysteroid dehydrogenase 1
JP5490020B2 (ja) 2008-01-24 2014-05-14 ヴァイティー ファーマシューティカルズ，インコーポレイテッド １１β−ヒドロキシステロイドデヒドロゲナーゼ１の環状カルバゼート及びセミカルバジドインヒビター
US8598160B2 (en) 2008-02-15 2013-12-03 Vitae Pharmaceuticals, Inc. Cycloalkyl lactame derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
PL2300461T3 (pl) 2008-05-01 2013-09-30 Vitae Pharmaceuticals Inc Cykliczne inhibitory dehydrogenazy 11beta-hydroksysteroidów 1
CA2723034A1 (en) 2008-05-01 2009-11-05 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
JP5379160B2 (ja) 2008-07-25 2013-12-25 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング １１β−ヒドロキシステロイドデヒドロゲナーゼ１の環状インヒビター
WO2010010150A1 (en) 2008-07-25 2010-01-28 Boehringer Ingelheim International Gmbh Synthesis of inhibitors of 11beta-hydroxysteroid dehydrogenase type 1
TW201016691A (en) 2008-07-25 2010-05-01 Boehringer Ingelheim Int Inhibitors of 11beta-hydroxysteroid dehydrogenase 1
EP2393807B1 (en) 2009-02-04 2013-08-14 Boehringer Ingelheim International GmbH Cyclic inhibitors of 11 -hydroxysteroid dehydrogenase 1
MA33216B1 (fr) 2009-04-30 2012-04-02 Boehringer Ingelheim Int Inhibiteurs cycliques de la 11béta-hydroxysteroïde déshydrogénase 1
JP5656986B2 (ja) 2009-06-11 2015-01-21 ヴァイティー ファーマシューティカルズ，インコーポレイテッド １，３−オキサジナン−２−オン構造に基づく１１β−ヒドロキシステロイドデヒドロゲナーゼ１の環状阻害剤
US8552212B2 (en) 2009-11-05 2013-10-08 Boehringer Ingelheim International Gmbh Chiral phosphorus ligands
US8648192B2 (en) 2010-05-26 2014-02-11 Boehringer Ingelheim International Gmbh 2-oxo-1,2-dihydropyridin-4-ylboronic acid derivatives
EP2582698B1 (en) 2010-06-16 2016-09-14 Vitae Pharmaceuticals, Inc. Substituted 5-,6- and 7-membered heterocycles, medicaments containing such compounds, and their use
JP5813106B2 (ja) 2010-06-25 2015-11-17 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 代謝障害の処置のための１１−β−ＨＳＤ１のインヒビターとしてのアザスピロヘキサノン
WO2012059416A1 (en) 2010-11-02 2012-05-10 Boehringer Ingelheim International Gmbh Pharmaceutical combinations for the treatment of metabolic disorders
WO2012112568A1 (en) * 2011-02-14 2012-08-23 The Broad Institute, Inc. Small molecule inhibitors for treating parasitic infections
WO2012170827A2 (en) * 2011-06-08 2012-12-13 Cylene Pharmaceuticals, Inc. Pyrazolopyrimidines and related heterocycles as ck2 inhibitors
WO2013051672A1 (ja) * 2011-10-04 2013-04-11 株式会社ヤクルト本社 チアゾリジン誘導体又はその塩を有効成分とする医薬品
JP6280546B2 (ja) 2012-06-26 2018-02-14 デル マー ファーマシューティカルズ ジアンヒドロガラクチトール、ジアセチルジアンヒドロガラクチトール、ジブロモズルシトール、又はこれらの類似体若しくは誘導体を用いた、遺伝子多型又はａｈｉ１の調節不全若しくは変異を有する患者におけるチロシンキナーゼインヒビター抵抗性悪性腫瘍を処置するための方法
TW201414737A (zh) * 2012-07-13 2014-04-16 必治妥美雅史谷比公司 作爲激酶抑制劑之咪唑并三□甲腈
JP6437452B2 (ja) 2013-01-14 2018-12-12 インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ Ｐｉｍキナーゼ阻害剤として有用な二環式芳香族カルボキサミド化合物
ME03780B (me) 2013-01-15 2021-04-20 Incyte Holdings Corp Jedinjenja tiazolkarboksamida i piridinkarboksamida korisna kao inhibitori pim kinaze
EP2983674A4 (en) 2013-04-08 2017-05-10 Dennis M. Brown Therapeutic benefit of suboptimally administered chemical compounds
EA201690458A1 (ru) 2013-08-23 2016-07-29 Инсайт Корпорейшн Фуро- и тиенопиридинкарбоксамиды, используемые в качестве ингибиторов pim-киназы
US9580418B2 (en) 2014-07-14 2017-02-28 Incyte Corporation Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors
US9822124B2 (en) 2014-07-14 2017-11-21 Incyte Corporation Bicyclic heteroaromatic carboxamide compounds useful as Pim kinase inhibitors
WO2016196244A1 (en) 2015-05-29 2016-12-08 Incyte Corporation Pyridineamine compounds useful as pim kinase inhibitors
AR105967A1 (es) 2015-09-09 2017-11-29 Incyte Corp Sales de un inhibidor de pim quinasa
WO2017059251A1 (en) 2015-10-02 2017-04-06 Incyte Corporation Heterocyclic compounds useful as pim kinase inhibitors
US11046698B2 (en) 2017-07-28 2021-06-29 Nimbus Lakshmi, Inc. TYK2 inhibitors and uses thereof
WO2019113487A1 (en) 2017-12-08 2019-06-13 Incyte Corporation Low dose combination therapy for treatment of myeloproliferative neoplasms
US11071727B2 (en) 2018-01-26 2021-07-27 Northwestern University Therapeutic targeting of proteolytic cleavage of the mixed lineage leukemia gene product (MLL1) by taspase1 using kinase inhibitors
EP3866804A4 (en) * 2018-10-19 2022-08-03 Senhwa Biosciences, Inc. Combinations for immune-modulation in cancer treatment
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CN115209952B (zh) 2020-01-13 2025-05-30 维基分析有限公司 经取代的吡唑并嘧啶及其用途
MX2022013619A (es) 2020-05-01 2022-11-16 Gilead Sciences Inc Compuestos de 2,4-dioxopirimidina que inhiben cd73.
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JP7787991B2 (ja) * 2021-10-29 2025-12-17 ギリアード サイエンシーズ， インコーポレイテッド Ｃｄ７３化合物

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CN1880317A (zh) * 2002-09-04 2006-12-20 先灵公司 作为细胞周期蛋白依赖性激酶抑制剂的吡唑并嘧啶
US20080045496A1 (en) * 2006-08-09 2008-02-21 Bristol-Myers Squibb Company Pyrrolotriazine kinase inhibitors
US20080275043A1 (en) * 2004-10-29 2008-11-06 Thomas Daniel Aicher Cycloalkyl Lactam Derivatives as Inhibitors of 11-Beta-Hydroxysteroid Dehydrogenase 1
CN101495481A (zh) * 2006-05-22 2009-07-29 先灵公司 作为CDK抑制剂的吡唑并[1,5-α]嘧啶

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US20080275043A1 (en) * 2004-10-29 2008-11-06 Thomas Daniel Aicher Cycloalkyl Lactam Derivatives as Inhibitors of 11-Beta-Hydroxysteroid Dehydrogenase 1
CN101495481A (zh) * 2006-05-22 2009-07-29 先灵公司 作为CDK抑制剂的吡唑并[1,5-α]嘧啶
US20080045496A1 (en) * 2006-08-09 2008-02-21 Bristol-Myers Squibb Company Pyrrolotriazine kinase inhibitors

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014154026A1 (zh) * 2013-03-28 2014-10-02 山东轩竹医药科技有限公司 PI3K和/或mTOR抑制剂的前药
CN105121442A (zh) * 2013-03-28 2015-12-02 山东轩竹医药科技有限公司 PI3K和/或mTOR抑制剂的前药
CN105121442B (zh) * 2013-03-28 2017-05-17 山东轩竹医药科技有限公司 PI3K和/或mTOR抑制剂的前药
CN115160341A (zh) * 2022-07-18 2022-10-11 中国医学科学院医学实验动物研究所 苯并噁嗪类化合物及其药物用途

Also Published As

Publication number Publication date
IL218521A0 (en) 2012-07-31
WO2011031979A1 (en) 2011-03-17
SG179083A1 (en) 2012-04-27
KR20120104521A (ko) 2012-09-21
US20110071115A1 (en) 2011-03-24
IN2012DN03112A (enExample) 2015-09-18
CA2773854A1 (en) 2011-03-17
AU2010292116A1 (en) 2012-05-03
JP2013504594A (ja) 2013-02-07
EP2475652A1 (en) 2012-07-18
BR112012005550A2 (pt) 2015-09-08
MX2012002994A (es) 2012-07-17

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Application publication date: 20120801