WO2003016275A1 - Agent antiviral - Google Patents

Agent antiviral Download PDF

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Publication number
WO2003016275A1
WO2003016275A1 PCT/JP2002/008108 JP0208108W WO03016275A1 WO 2003016275 A1 WO2003016275 A1 WO 2003016275A1 JP 0208108 W JP0208108 W JP 0208108W WO 03016275 A1 WO03016275 A1 WO 03016275A1
Authority
WO
WIPO (PCT)
Prior art keywords
ring
formula
antiviral agent
compound
integrase
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.)
Ceased
Application number
PCT/JP2002/008108
Other languages
English (en)
French (fr)
Japanese (ja)
Inventor
Ryuichi Kiyama
Yasuhiko Kanda
Yukio Tada
Toshio Fujishita
Takashi Kawasuji
Shozo Takechi
Masahiro Fuji
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.)
Shionogi and Co Ltd
Original Assignee
Shionogi and Co Ltd
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=27347328&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=WO2003016275(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority to ES02749384T priority Critical patent/ES2383262T3/es
Application filed by Shionogi and Co Ltd filed Critical Shionogi and Co Ltd
Priority to US10/485,394 priority patent/US20040229909A1/en
Priority to MXPA04000646A priority patent/MXPA04000646A/es
Priority to JP2003521202A priority patent/JP4338192B2/ja
Priority to CA2452769A priority patent/CA2452769C/en
Priority to BR0211750-9A priority patent/BR0211750A/pt
Priority to AT02749384T priority patent/ATE550320T1/de
Priority to KR1020047002062A priority patent/KR100977701B1/ko
Priority to EP02749384A priority patent/EP1422218B1/en
Publication of WO2003016275A1 publication Critical patent/WO2003016275A1/ja
Anticipated expiration legal-status Critical
Priority to US14/603,979 priority patent/US9572813B2/en
Priority to US15/356,343 priority patent/US20170066754A1/en
Ceased legal-status Critical Current

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    • 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
    • C07D417/02—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
    • C07D417/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/351—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom not condensed with another ring
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4025—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
    • A—HUMAN NECESSITIES
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
    • A—HUMAN NECESSITIES
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    • A61K31/33—Heterocyclic compounds
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4196—1,2,4-Triazoles
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    • A61K31/42—Oxazoles
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    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A—HUMAN NECESSITIES
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    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4433—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
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    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • A—HUMAN NECESSITIES
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    • A61K31/47—Quinolines; Isoquinolines
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    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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ES02749384T ES2383262T3 (es) 2001-08-10 2002-08-08 Agente antiviral
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Cited By (65)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004072063A1 (en) * 2003-02-07 2004-08-26 Vertex Pharmaceuticals Incorporated Heteroaryl substituted pyrolls useful as inhibitors of protein kinases
JP2004250693A (ja) * 2003-01-29 2004-09-09 Sanyo Chem Ind Ltd ウレタン樹脂及びその粉体の製造方法
WO2005061490A1 (ja) 2003-12-22 2005-07-07 Shionogi & Co., Ltd. Hivインテグラーゼ阻害活性を有するヒドロキシピリミジノン誘導体
WO2005087766A1 (en) 2004-03-09 2005-09-22 Istituto Di Ricerche Di Biologia Molecolare P Angeletti Spa Hiv integrase inhibitors
WO2006030807A1 (ja) * 2004-09-15 2006-03-23 Shionogi & Co., Ltd. Ｈｉｖインテグラーゼ阻害活性を有するカルバモイルピリドン誘導体
US7037908B2 (en) 2003-04-24 2006-05-02 Bristol-Myers Squibb Company HIV integrase inhibitors
US7109186B2 (en) 2002-07-09 2006-09-19 Bristol-Myers Squibb Company HIV integrase inhibitors
JP2006342115A (ja) * 2005-06-10 2006-12-21 Shionogi & Co Ltd Ｈｉｖインテグラーゼ阻害活性を有する多環性化合物
US7211572B2 (en) 2003-08-13 2007-05-01 Japan Tobacco Inc. Nitrogen-containing fused ring compound and use thereof as HIV integrase inhibitor
US7414045B2 (en) 2002-12-27 2008-08-19 Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. Substituted pyrimido[1,2-a]azepines useful as HIV integrase inhibitors
US7585868B2 (en) 2006-04-04 2009-09-08 The Regents Of The University Of California Substituted pyrazolo[3,4-D]pyrimidines as kinase antagonists
US8129385B2 (en) 2005-04-28 2012-03-06 Shionogi & Co., Ltd. Substituted 5-hydroxy-3,4,6,9,9a, 10-hexanhydro-2h-1-oxa04a,8a-diaza-anthracene-6,10-dioness
US8476282B2 (en) 2008-11-03 2013-07-02 Intellikine Llc Benzoxazole kinase inhibitors and methods of use
US8569323B2 (en) 2009-07-15 2013-10-29 Intellikine, Llc Substituted isoquinolin-1(2H)-one compounds, compositions, and methods thereof
US8604032B2 (en) 2010-05-21 2013-12-10 Infinity Pharmaceuticals, Inc. Chemical compounds, compositions and methods for kinase modulation
US8637542B2 (en) 2008-03-14 2014-01-28 Intellikine, Inc. Kinase inhibitors and methods of use
US8697709B2 (en) 2008-10-16 2014-04-15 The Regents Of The University Of California Fused ring heteroaryl kinase inhibitors
US8703777B2 (en) 2008-01-04 2014-04-22 Intellikine Llc Certain chemical entities, compositions and methods
US8703778B2 (en) 2008-09-26 2014-04-22 Intellikine Llc Heterocyclic kinase inhibitors
US8785454B2 (en) 2009-05-07 2014-07-22 Intellikine Llc Heterocyclic compounds and uses thereof
US8785470B2 (en) 2011-08-29 2014-07-22 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
US8809349B2 (en) 2011-01-10 2014-08-19 Infinity Pharmaceuticals, Inc. Processes for preparing isoquinolinones and solid forms of isoquinolinones
US8828998B2 (en) 2012-06-25 2014-09-09 Infinity Pharmaceuticals, Inc. Treatment of lupus, fibrotic conditions, and inflammatory myopathies and other disorders using PI3 kinase inhibitors
US8835449B2 (en) 2011-11-11 2014-09-16 Pfizer Inc. 2-thiopyrimidinones
US8901133B2 (en) 2010-11-10 2014-12-02 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
US8940742B2 (en) 2012-04-10 2015-01-27 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
US8969363B2 (en) 2011-07-19 2015-03-03 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
US8980899B2 (en) 2009-10-16 2015-03-17 The Regents Of The University Of California Methods of inhibiting Ire1
US8993580B2 (en) 2008-03-14 2015-03-31 Intellikine Llc Benzothiazole kinase inhibitors and methods of use
US9056877B2 (en) 2011-07-19 2015-06-16 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
US9096611B2 (en) 2008-07-08 2015-08-04 Intellikine Llc Kinase inhibitors and methods of use
US9200009B2 (en) 2011-10-12 2015-12-01 Shionogi & Co., Ltd. Polycyclic pyridone derivative having integrase inhibitory activity
US9216995B2 (en) 2010-04-12 2015-12-22 Shionogi & Co., Ltd. Pyridone derivative having integrase inhibitory activity
WO2016021539A1 (ja) * 2014-08-06 2016-02-11 エーザイ・アール・アンド・ディー・マネジメント株式会社 ピリミジン－１－オール化合物の製造方法及びその中間体
US9295673B2 (en) 2011-02-23 2016-03-29 Intellikine Llc Combination of mTOR inhibitors and P13-kinase inhibitors, and uses thereof
US9321772B2 (en) 2011-09-02 2016-04-26 The Regents Of The University Of California Substituted pyrazolo[3,4-D]pyrimidines and uses thereof
US9359349B2 (en) 2007-10-04 2016-06-07 Intellikine Llc Substituted quinazolines as kinase inhibitors
US9359365B2 (en) 2013-10-04 2016-06-07 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
US9481667B2 (en) 2013-03-15 2016-11-01 Infinity Pharmaceuticals, Inc. Salts and solid forms of isoquinolinones and composition comprising and methods of using the same
US9512125B2 (en) 2004-11-19 2016-12-06 The Regents Of The University Of California Substituted pyrazolo[3.4-D] pyrimidines as anti-inflammatory agents
US9572813B2 (en) 2001-08-10 2017-02-21 Shionogi & Co., Ltd. Antiviral agent
US9629843B2 (en) 2008-07-08 2017-04-25 The Regents Of The University Of California MTOR modulators and uses thereof
CN106810458A (zh) * 2016-12-31 2017-06-09 武汉工程大学 一种拆分dl‑2‑氨基丙醇制备l‑2‑氨基丙醇的方法
US9708348B2 (en) 2014-10-03 2017-07-18 Infinity Pharmaceuticals, Inc. Trisubstituted bicyclic heterocyclic compounds with kinase activities and uses thereof
US9751888B2 (en) 2013-10-04 2017-09-05 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
US9771332B2 (en) 2015-05-05 2017-09-26 Pfizer Inc. 2-thiopyrimidinones
US9775844B2 (en) 2014-03-19 2017-10-03 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
CN108658784A (zh) * 2018-04-26 2018-10-16 联化科技股份有限公司 (r)-1-(4-甲基苯基)乙胺的合成方法
US10131668B2 (en) 2012-09-26 2018-11-20 The Regents Of The University Of California Substituted imidazo[1,5-a]pYRAZINES for modulation of IRE1
US10160761B2 (en) 2015-09-14 2018-12-25 Infinity Pharmaceuticals, Inc. Solid forms of isoquinolinones, and process of making, composition comprising, and methods of using the same
WO2019054427A1 (ja) 2017-09-14 2019-03-21 第一三共株式会社 環状構造を有する化合物
JP2019512485A (ja) * 2016-03-08 2019-05-16 ノバルティス アーゲー オルトミクソウイルス感染の処置に有用な三環式化合物
WO2020083662A1 (en) 2018-10-23 2020-04-30 Basf Se Tricyclic pesticidal compounds
US10759806B2 (en) 2016-03-17 2020-09-01 Infinity Pharmaceuticals, Inc. Isotopologues of isoquinolinone and quinazolinone compounds and uses thereof as PI3K kinase inhibitors
EP3757105A2 (en) 2014-08-22 2020-12-30 Shionogi & Co., Ltd Polycyclic pyridone derivative having integrase inhibitory activity
US10919914B2 (en) 2016-06-08 2021-02-16 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
US11098051B2 (en) 2016-08-29 2021-08-24 Novartis Ag Fused tricyclic pyridazinone compounds useful to treat orthomyxovirus infections
US11110096B2 (en) 2014-04-16 2021-09-07 Infinity Pharmaceuticals, Inc. Combination therapies
US11147818B2 (en) 2016-06-24 2021-10-19 Infinity Pharmaceuticals, Inc. Combination therapies
WO2021209265A1 (en) 2020-04-14 2021-10-21 Basf Se Tricyclic pesticidal compounds
US11629149B2 (en) 2018-02-28 2023-04-18 Novartis Ag 10-(di(phenyl)methyl)-4-hydroxy-8,9,9A,10-tetrahydro-7H-pyrrolo[1′,2′:4,5]pyrazino[1,2-b]pyridazine-3,5-dione derivatives and related compounds as inhibitors of the orthomyxovirus replication for treating influenza
JP2023527281A (ja) * 2020-05-18 2023-06-28 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 神経炎症の処置のためのｃｋ２阻害剤として使用するための、例えばフラボンなどのクロメン－４－オン誘導体
WO2023243678A1 (ja) 2022-06-15 2023-12-21 日産化学株式会社 ピラゾール化合物、その製造中間体、及び有害生物防除剤
WO2024204842A1 (ja) 2023-03-31 2024-10-03 日産化学株式会社 ピラゾール化合物及び有害生物防除剤
US12213983B2 (en) 2012-11-01 2025-02-04 Infinity Pharmaceuticals, Inc. Treatment of cancers using PI3 kinase isoform modulators

Families Citing this family (75)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK1441734T3 (da) 2001-10-26 2007-06-11 Angeletti P Ist Richerche Bio Dihydroxypyrimidin-carboxamid-inhibitorer a HIV-integrase
CA2463976C (en) * 2001-10-26 2007-02-13 Benedetta Crescenzi N-substituted hydroxypyrimidinone carboxamide inhibitors of hiv integrase
WO2004062613A2 (en) 2003-01-13 2004-07-29 Bristol-Myers Squibb Company Hiv integrase inhibitors
US20050014753A1 (en) * 2003-04-04 2005-01-20 Irm Llc Novel compounds and compositions as protein kinase inhibitors
CN101014571A (zh) * 2004-01-30 2007-08-08 默克公司 用作hiv整合酶抑制剂的n－苄基－3,4－二羟基吡啶－2－羧酰胺类和n－苄基－2,3－二羟基吡啶－4－羧酰胺类化合物
CN101014574A (zh) * 2004-03-09 2007-08-08 默克公司 Hiv整合酶抑制剂
EP1725102A4 (en) 2004-03-09 2009-04-29 Merck & Co Inc HIV integrase
NZ549449A (en) 2004-03-09 2009-05-31 Merck & Co Inc HIV Integrase inhibitors
CN1964975B (zh) * 2004-05-07 2011-11-30 默沙东公司 Hiv整合酶抑制剂
US7115601B2 (en) * 2004-05-18 2006-10-03 Bristol-Myers Squibb Company HIV integrase inhibitors
CA2568389A1 (en) 2004-06-09 2005-12-22 Merck & Co., Inc. Hiv integrase inhibitors
EP1852434B1 (en) * 2005-02-21 2011-07-13 Shionogi Co., Ltd. Bicyclic carbamoylpyridone derivative having hiv integrase inhibiting activity
CN101146811B (zh) 2005-03-31 2012-01-11 P.安杰莱蒂分子生物学研究所 Hiv整合酶抑制剂
WO2006121831A2 (en) 2005-05-10 2006-11-16 Merck & Co., Inc. Hiv integrase inhibitors
EP1937678B1 (en) * 2005-10-04 2011-07-27 Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. Hiv integrase inhibitors
JP5131689B2 (ja) 2005-10-27 2013-01-30 塩野義製薬株式会社 Ｈｉｖインテグラーゼ阻害活性を有する多環性カルバモイルピリドン誘導体
EP1951726A2 (en) * 2005-11-14 2008-08-06 H.Lundbeck A/S Method for the preparation of escitalopram
US20100056516A1 (en) * 2006-07-17 2010-03-04 Williams Peter D 1-hydroxy naphthyridine compounds as anti-hiv agents
WO2008127275A2 (en) * 2006-09-22 2008-10-23 Ptc Therapeutics, Inc. Pyrrolinone compounds as inhibitors of bacterial peptidyl trna hydrolase and uses thereof
US20100216834A1 (en) * 2006-10-18 2010-08-26 Isaacs Richard C A Hiv integrase inhibitors
EP2095819A1 (en) * 2008-02-28 2009-09-02 Maastricht University N-benzyl imidazole derivatives and their use as aldosterone synthase inhibitors
DE102008028905A1 (de) 2008-06-18 2009-12-24 Merck Patent Gmbh 3-(3-Pyrimidin-2-yl-benzyl)-[1,2,4]triazolo[4,3-b]pyridazinderivate
PL2247601T3 (pl) 2008-07-02 2013-09-30 Avexa Ltd Tiazopirymidynony i ich zastosowanie
BRPI0913934A2 (pt) * 2008-07-02 2015-10-20 Avexa Ltd compostos tendo propriedades antivirais
JP5592360B2 (ja) * 2008-07-02 2014-09-17 アベキサ・リミテッド イミダゾピリミジノンおよびその使用
EP2334188A4 (en) * 2008-08-15 2012-08-08 Burnham Inst Medical Research COMPOSITION AND METHOD FOR THE DESIGN AND DEVELOPMENT OF METAL OXYCLES
MX2011003637A (es) * 2008-10-06 2011-04-27 Merck Sharp & Dohme Inhibidores de la integrasa del virus de inmunodeficiencia humana.
TW201116522A (en) * 2009-07-10 2011-05-16 Vivalis 1-(6 members azo-heterocyclic)-pyrrolin-2-one compounds as inhibitors of Hepatitis C NS5B polymerase, the pharmaceutical composition thereof and their therapeutic use
CN101967209B (zh) * 2010-10-20 2012-11-07 南京大学 一种n-乙酰基乙二胺螯合树脂及其制备方法
GB201020076D0 (en) * 2010-11-26 2011-01-12 Liverpool School Tropical Medicine Antimalarial compounds
US8952180B2 (en) 2011-09-27 2015-02-10 Bristol-Myers Squibb Company Pyrrolinone carboxamide compounds useful as endothelial lipase inhibitors
EP2760830B1 (en) 2011-09-27 2016-08-03 Bristol-Myers Squibb Company Pyrrolinone carboxamide compounds useful as endothelial lipase inhibitors
US9249096B2 (en) 2011-09-27 2016-02-02 Bristol-Myers Squibb Company Pyrrolinone carboxamide compounds useful as endothelial lipase inhibitors
JP6183053B2 (ja) * 2012-08-22 2017-08-23 宇部興産株式会社 テトラヒドロピラニルピリミジン化合物の製造方法
US9714243B2 (en) 2012-12-17 2017-07-25 Merck Sharp & Dohme Corp. 4-pyridinonetriazine derivatives as HIV integrase inhibitors
DK3067358T3 (da) 2012-12-21 2019-11-04 Gilead Sciences Inc Polycykliske carbamoylpyridon-forbindelser og deres farmaceutiske anvendelse
CN103172581A (zh) * 2013-04-07 2013-06-26 杨国成 一种5-氨基-3-巯基-1,2,4-三氮唑晶体及其制备方法
EP2986291B1 (en) 2013-04-16 2020-05-27 Merck Sharp & Dohme Corp. 4-pyridone derivative compounds and uses thereof as hiv integrase inhibitors
GB201308217D0 (en) 2013-05-08 2013-06-12 Ucl Business Plc Compounds and their use in therapy
CN104148018B (zh) * 2013-05-14 2018-04-20 上海亨臻实业有限公司 抗体亲和纯化材料及其用途
LT2997033T (lt) 2013-05-17 2018-02-12 Merck Sharp & Dohme Corp. Kondensuoti tricikliniai heterocikliniai junginiai, kaip živ integrazės inhibitoriai
US9951079B2 (en) 2013-06-13 2018-04-24 Merck Sharp & Dohme Corp. Fused tricyclic heterocyclic compounds as HIV integrase inhibitors
PL3019503T3 (pl) 2013-07-12 2018-01-31 Gilead Sciences Inc Policykliczne związki karbamoilopirydonowe i ich zastosowanie do leczenia infekcji hiv
NO2865735T3 (enExample) 2013-07-12 2018-07-21
EP3049081B1 (en) 2013-09-27 2019-11-27 Merck Sharp & Dohme Corp. Substituted quinolizine derivatives useful as hiv integrase inhibitors
US20170166543A1 (en) * 2014-02-03 2017-06-15 American Life Science Pharmaceuticals, Inc. Compositions and methods for synthesizing (2s,3s)-trans-epoxysuccinyl-l-leucyl-amido-3-methylbutane ethyl ester
TWI744723B (zh) 2014-06-20 2021-11-01 美商基利科學股份有限公司 多環型胺甲醯基吡啶酮化合物之合成
NO2717902T3 (enExample) 2014-06-20 2018-06-23
TW201613936A (en) 2014-06-20 2016-04-16 Gilead Sciences Inc Crystalline forms of(2R,5S,13aR)-8-hydroxy-7,9-dioxo-n-(2,4,6-trifluorobenzyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxamide
TWI695003B (zh) 2014-12-23 2020-06-01 美商基利科學股份有限公司 多環胺甲醯基吡啶酮化合物及其醫藥用途
EP3277691B1 (en) 2015-04-02 2019-01-30 Gilead Sciences, Inc. Polycyclic-carbamoylpyridone compounds and their pharmaceutical use
WO2016187788A1 (en) 2015-05-25 2016-12-01 Merck Sharp & Dohme Corp. Fused tricyclic heterocyclic compounds useful for treating hiv infection
CN105237406A (zh) * 2015-10-14 2016-01-13 湖南华腾制药有限公司 (r)-(-)-1-甲基-3-苯丙胺的合成方法
EP3374350B1 (en) 2015-11-09 2022-01-05 Forge Therapeutics, Inc. Hydroxypyridinone and hydroxypyrimidinone based compounds for treating bacterial infections
US10611747B2 (en) 2015-11-09 2020-04-07 Forge Therapeutics, Inc. Pyrone based compounds for treating bacterial infections
WO2017087257A1 (en) 2015-11-17 2017-05-26 Merck Sharp & Dohme Corp. Amido-substituted pyridotriazine derivatives useful as hiv integrase inhibitors
EP3389380B1 (en) 2015-12-15 2021-07-21 Merck Sharp & Dohme Corp. Spirocyclic quinolizine derivatives useful as hiv integrase inhibitors
WO2017113288A1 (en) 2015-12-31 2017-07-06 Merck Sharp & Dohme Corp. Fused tricyclic heterocyclic compounds as hiv integrase inhibitors
US10981899B2 (en) 2016-04-28 2021-04-20 Cornell University Inhibitors of soluble adenylyl cyclase
CN107773562B (zh) * 2016-08-25 2020-04-07 清华大学 化合物在抗登革和寨卡病毒感染中的应用
JOP20190130A1 (ar) 2016-12-02 2019-06-02 Merck Sharp & Dohme مركبات حلقية غير متجانسة رباعية الحلقات مفيدة كمثبطات إنزيم مدمج لفيروس نقص المناعة البشرية (hiv)
CN110062627A (zh) 2016-12-02 2019-07-26 默沙东公司 可用作hiv整合酶抑制剂的三环杂环化合物
EP3573984A4 (en) 2017-01-26 2020-07-29 Merck Sharp & Dohme Corp. USEFUL SUBSTITUTE QUINOLIZINE DERIVATIVES AS HIV INTEGRASE INHIBITORS
EP3596199A1 (en) * 2017-03-13 2020-01-22 DSM IP Assets B.V. Zinc binuclear cluster transcriptional regulator-deficient strain
WO2018166855A1 (en) 2017-03-16 2018-09-20 Basf Se Heterobicyclic substituted dihydroisoxazoles
US11021471B2 (en) * 2017-05-10 2021-06-01 Forge Therapeutics, Inc. Antibacterial compounds
AU2019345150A1 (en) 2018-09-20 2021-05-13 Blacksmith Medicines, Inc. Antibacterial compounds
WO2020132820A1 (zh) * 2018-12-24 2020-07-02 广东莱佛士制药技术有限公司 一种3-(苄氧基)-4-氧代-4h-吡喃-2-羧酸的合成方法
RU2717101C1 (ru) 2019-06-03 2020-03-18 Андрей Александрович Иващенко Анелированные 9-гидрокси-1,8-диоксо-1,3,4,8-тетрагидро-2Н-пиридо[1,2-a]пиразин-7-карбоксамиды - ингибиторы интегразы ВИЧ, способы их получения и применения
US20200398978A1 (en) 2019-06-20 2020-12-24 Bell Helicopter Textron Inc. Low-drag rotor blade extension
CN110563943A (zh) * 2019-09-09 2019-12-13 中国科学院长春应用化学研究所 一种生物基聚合物及其制备方法
WO2021195260A1 (en) 2020-03-25 2021-09-30 Forge Therapeutics, Inc. Lpxc inhibitor and methods of making
WO2022061224A1 (en) 2020-09-21 2022-03-24 Landos Biopharma, Inc. Nlrx1 ligands
MX2024003859A (es) 2021-09-28 2024-05-21 Blacksmith Medicines Inc Inhibidores de lpxc y usos de estos.
WO2025085347A1 (en) * 2023-10-19 2025-04-24 Merck Sharp & Dohme Llc Il4i1 inhibitors and uses thereof

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1992002523A1 (fr) 1990-08-02 1992-02-20 Sankei Pharmaceutical Company Limited Nouveau compose de cephalosporine
JPH06100445A (ja) * 1992-07-06 1994-04-12 Banyu Pharmaceut Co Ltd 抗腫瘍剤
WO2000039086A1 (en) * 1998-12-25 2000-07-06 Shionogi & Co., Ltd. Aromatic heterocycle compounds having hiv integrase inhibiting activities

Family Cites Families (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3244725A (en) 1964-09-21 1966-04-05 Taub William 4, 5-diacyl-3-hydroxy-3-pyrrolin-2-ones
US4298743A (en) * 1979-09-11 1981-11-03 Merck & Co., Inc. 4-(Substituted phenyl thiazolyl)-3-hydroxy-3-pyrroline-2,5-diones
DE3820176A1 (de) 1987-12-18 1989-06-29 Bayer Ag Verfahren zur herstellung von phosphorsaeurederivaten und zwischenprodukten
DK0553130T3 (da) 1990-10-15 1996-02-05 Pfizer Pyrrolidindionderivater
JPH06100405A (ja) * 1992-08-07 1994-04-12 Yoshitomi Pharmaceut Ind Ltd 水中防汚剤
WO1998011876A1 (de) 1996-09-18 1998-03-26 Marigen S.A. Bioflavonol-glykosid-perester und ihre aufarbeitung zu pharmakologisch wirksamen konzentraten und ultramikroemulsionen
IL137974A0 (en) 1998-03-26 2001-10-31 Shionogi & Co Indole derivatives having antiviral activity
WO1999062513A1 (en) 1998-06-03 1999-12-09 Merck & Co., Inc. Hiv integrase inhibitors
EP1086091A4 (en) 1998-06-03 2001-10-10 Merck & Co Inc INTEGRASE HIV INHIBITORS
EP1082121A4 (en) 1998-06-03 2003-02-05 Merck & Co Inc HIV integrase
EP1124822A4 (en) 1998-10-30 2002-04-03 Merck & Co Inc THROMBIN INHIBITORS
GB2345058A (en) 1998-12-01 2000-06-28 Cerebrus Pharm Ltd Hydroxypyridone compounds useful in the treatment of oxidative damage to the central nervous system
AU5880600A (en) 1999-06-25 2001-01-31 Merck & Co., Inc. 1-(aromatic- or heteroaromatic-substituted)-3-(heteroaromatic substituted)-1,3-propanediones and uses thereof
US7576198B1 (en) 1999-09-02 2009-08-18 Shionogi & Co., Ltd. Integrase inhibitors containing aromatic heterocycle derivatives
JP2001270884A (ja) 2000-03-23 2001-10-02 Mitsubishi-Tokyo Pharmaceuticals Inc ピリミドン誘導体
AU2001262732A1 (en) 2000-06-14 2001-12-24 Shionogi And Co., Ltd. Inhibitor for enzyme having two divalent metal ions as active centers
US20050010048A1 (en) 2000-10-12 2005-01-13 Linghang Zhuang Aza-and polyaza-naphthalenly ketones useful as hiv integrase inhibitors
ATE364385T1 (de) 2000-10-12 2007-07-15 Merck & Co Inc Aza- und polyaza-naphthalenylcarbonsäureamide als hiv-integrase-hemmer
WO2002030931A2 (en) 2000-10-12 2002-04-18 Merck & Co., Inc. Aza- and polyaza-naphthalenyl carboxamides useful as hiv integrase inhibitors
WO2002070491A1 (en) 2001-03-01 2002-09-12 Shionogi & Co., Ltd. Nitrogenous heteroaromatic ring derivative having hiv integrase inhibitory activity
WO2002070486A1 (en) 2001-03-01 2002-09-12 Shionogi & Co., Ltd. Nitrogen-containing heteroaryl compounds having hiv integrase inhibitory activity
EP2181985B1 (en) * 2001-08-10 2011-10-26 Shionogi & Co., Ltd. Antiviral Agent
NZ532018A (en) * 2001-10-03 2004-12-24 Ucb S Pyrrolidinone derivatives
DK1441734T3 (da) 2001-10-26 2007-06-11 Angeletti P Ist Richerche Bio Dihydroxypyrimidin-carboxamid-inhibitorer a HIV-integrase
CA2463976C (en) * 2001-10-26 2007-02-13 Benedetta Crescenzi N-substituted hydroxypyrimidinone carboxamide inhibitors of hiv integrase
WO2004004657A2 (en) 2002-07-09 2004-01-15 Bristol-Myers Squibb Company Hiv integrase inhibitors
TW200526635A (en) * 2003-12-22 2005-08-16 Shionogi & Co Hydroxypyrimidinone derivative having HIV integrase inhibitory activity
CN101014571A (zh) 2004-01-30 2007-08-08 默克公司 用作hiv整合酶抑制剂的n－苄基－3,4－二羟基吡啶－2－羧酰胺类和n－苄基－2,3－二羟基吡啶－4－羧酰胺类化合物
WO2012151567A1 (en) 2011-05-05 2012-11-08 St. Jude Children's Research Hospital Pyrimidinone compounds and methods for preventing and treating influenza

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1992002523A1 (fr) 1990-08-02 1992-02-20 Sankei Pharmaceutical Company Limited Nouveau compose de cephalosporine
JPH06100445A (ja) * 1992-07-06 1994-04-12 Banyu Pharmaceut Co Ltd 抗腫瘍剤
WO2000039086A1 (en) * 1998-12-25 2000-07-06 Shionogi & Co., Ltd. Aromatic heterocycle compounds having hiv integrase inhibiting activities

Non-Patent Citations (11)

* Cited by examiner, † Cited by third party
Title
ANDREICHIKOV YU. S. ET AL.: "Five-membered-ring 2,3-dioxoheterocycles. XIV. Synthesis of 1,4-disubstituted 5-aryltetrahydropyrrole-2,3-diones by reaction of diethoxalylacetone with azomethines", ZH. ORG. KHIM., vol. 25, no. 12, 1989, pages 2494 - 2500, XP002957388 *
BETAIL G. ET AL.: "Induction of antinuclear antibodies. Study of new molecules with a hydrazine structure or their analogs in mice", ANN. PHARM. FR., vol. 36, no. 7-8, 1978, pages 317 - 322, XP002957391 *
ELBEN ULRICH, VOEGTLE FRITZ: "Cryptomycins - crown ether analogs of the actinomycins", J. CHEM. RES. (S), no. 9, 1978, pages 316 - 317, XP002957390 *
J. ORG. CHEM., vol. 33, 1968, pages 2051
ORG. PREP. PROCED. INT., vol. 29, 1997, pages 330 - 335
PHAM HUU CHANH ET AL.: "Pharmacological aspects of pyrazoline derivatives from 2-hydroxybutenolides", ARZNEIM.-FORSCH., vol. 26, no. 11, 1976, pages 2050 - 2052, XP002957387 *
See also references of EP1422218A4
SILHANKOVA ALEXANDRA ET AL.: "Studies in the pyridine series. part LVIII. Condensation reactions of 2,4- and 2,6-dimethylpyridines and their 1-oxides", COLLECT. CZECH. CHEM. COMMUN., vol. 54, no. 6, 1989, pages 1687 - 1704, XP002957386 *
SKLYAROVA I.V. ET AL.: "Synthesis of actinomycin analogs. XVII. Actinomycin amides containing a benzimidazole fragment", ZH. ORG. KHIM., vol. 25, no. 1, 1989, pages 186 - 189, XP002957389 *
TETRAHEDRON, vol. 53, no. 15, 1997, pages 5617
TETRAHEDRON, vol. 54, 1998, pages 12745 - 12774

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9572813B2 (en) 2001-08-10 2017-02-21 Shionogi & Co., Ltd. Antiviral agent
US7109186B2 (en) 2002-07-09 2006-09-19 Bristol-Myers Squibb Company HIV integrase inhibitors
US7968553B2 (en) 2002-12-27 2011-06-28 Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. Tetrahydro-4H-pyrido[1,2-a] pyrimidines useful as HIV integrase inhibitors
US7414045B2 (en) 2002-12-27 2008-08-19 Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. Substituted pyrimido[1,2-a]azepines useful as HIV integrase inhibitors
JP2004250693A (ja) * 2003-01-29 2004-09-09 Sanyo Chem Ind Ltd ウレタン樹脂及びその粉体の製造方法
US7407962B2 (en) 2003-02-07 2008-08-05 Vertex Pharmaceuticals Incorporated Heteroaryl compounds useful as inhibitors or protein kinases
WO2004072063A1 (en) * 2003-02-07 2004-08-26 Vertex Pharmaceuticals Incorporated Heteroaryl substituted pyrolls useful as inhibitors of protein kinases
JP2006518381A (ja) * 2003-02-07 2006-08-10 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 プロテインキナーゼのインヒビターとして有用なヘテロアリール置換ピロール
US7037908B2 (en) 2003-04-24 2006-05-02 Bristol-Myers Squibb Company HIV integrase inhibitors
EP2042502A1 (en) 2003-08-13 2009-04-01 Japan Tobacco Inc. Nitrogen-containing fused ring compound and use thereof as HIV integrase inhibitor
US7211572B2 (en) 2003-08-13 2007-05-01 Japan Tobacco Inc. Nitrogen-containing fused ring compound and use thereof as HIV integrase inhibitor
JP4798608B2 (ja) * 2003-12-22 2011-10-19 塩野義製薬株式会社 Ｈｉｖインテグラーゼ阻害活性を有するヒドロキシピリミジノン誘導体
WO2005061490A1 (ja) 2003-12-22 2005-07-07 Shionogi & Co., Ltd. Hivインテグラーゼ阻害活性を有するヒドロキシピリミジノン誘導体
US7745453B2 (en) 2003-12-22 2010-06-29 Shionogi & Co., Ltd. Hydroxypyrimidinone derivatives having inhibitory activity against HIV integrase
WO2005087766A1 (en) 2004-03-09 2005-09-22 Istituto Di Ricerche Di Biologia Molecolare P Angeletti Spa Hiv integrase inhibitors
JP4953297B2 (ja) * 2004-09-15 2012-06-13 塩野義製薬株式会社 Ｈｉｖインテグラーゼ阻害活性を有するカルバモイルピリドン誘導体
US7550463B2 (en) 2004-09-15 2009-06-23 Shionogi & Co., Ltd. Carbamoylpyridone derivatives having inhibitory activity against HIV integrase
WO2006030807A1 (ja) * 2004-09-15 2006-03-23 Shionogi & Co., Ltd. Ｈｉｖインテグラーゼ阻害活性を有するカルバモイルピリドン誘導体
JPWO2006030807A1 (ja) * 2004-09-15 2008-05-15 塩野義製薬株式会社 Ｈｉｖインテグラーゼ阻害活性を有するカルバモイルピリドン誘導体
US9512125B2 (en) 2004-11-19 2016-12-06 The Regents Of The University Of California Substituted pyrazolo[3.4-D] pyrimidines as anti-inflammatory agents
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US11267823B2 (en) 2005-04-28 2022-03-08 Shionogi & Co., Ltd. Substituted 1,2,3,3a,4,5,7,9,13,13a-decahydropyrido[1′,2′:4,5]pyrazino[1,2-a]pyrrolo[1,2-c]pyrimidines having HIV integrase inhibitory activity
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US8410103B2 (en) 2005-04-28 2013-04-02 Shionogi & Co., Ltd. (3S,11aR)-N-[2,4-difluorophenyl)methyl]-6-hydroxy-3-methyl-5,7-dioxo-2,3,5,7,11,11a-hexahydro[1,3]oxazolo[3,2-a]pyrido[1,2-d]pyrazine-8-carboxamide useful as anti-HIV agent
US8129385B2 (en) 2005-04-28 2012-03-06 Shionogi & Co., Ltd. Substituted 5-hydroxy-3,4,6,9,9a, 10-hexanhydro-2h-1-oxa04a,8a-diaza-anthracene-6,10-dioness
US10927129B2 (en) 2005-04-28 2021-02-23 Shinogi & Co., Ltd. N-[(2,4-difluorophenyl)methyl]-6-hydroxy-3-methyl-5,7-dioxo-2,3,5,7,11,11a-hexahydro[1,3] oxazolo[3,2-a]pyrido[1,2-d]pyrazine-8-carboxamide having HIV integrase inhibitory activity
US9273065B2 (en) 2005-04-28 2016-03-01 Shionogi & Co., Ltd. Substituted pyrido[1',2':4,5]pyrazino[1,2-a]pyrimidines as HIV integrase inhibitors
EP2465580A1 (en) 2005-04-28 2012-06-20 Glaxosmithkline LLC Polycyclic carbamoylpyridone derivatives having hiv integrase inhibitory activity
US9051337B2 (en) 2005-04-28 2015-06-09 Shionogi & Co., Ltd. Substituted 10-hydroxy-9,11-dioxo-2,3,4a,5,9,11,13,13a-octahydro-1h-pyrido[1,2-a]pyrrolo[1′,2′:3,4]imidazo[1,2-d]pyrazine-8-carboxamides
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US8778943B2 (en) 2005-04-28 2014-07-15 Shionogi & Co., Ltd. Substituted 10-hydroxy-9,11-dioxo-2,3,4a,5,9,11,13,13a-octahydro-1h-pyrido[1,2-α]pyrrolo[1′,2′:3,4]imidazo[1,2-d]pyrazine-8-carboxamides
EP3372281A1 (en) 2005-04-28 2018-09-12 VIIV Healthcare Company Polycyclic carbamoylpyridone derivative having hiv integrase inhibitory activity
JP2006342115A (ja) * 2005-06-10 2006-12-21 Shionogi & Co Ltd Ｈｉｖインテグラーゼ阻害活性を有する多環性化合物
US8642604B2 (en) 2006-04-04 2014-02-04 The Regents Of The University Of California Substituted pyrazolo[3,2-d]pyrimidines as anti-cancer agents
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US9359349B2 (en) 2007-10-04 2016-06-07 Intellikine Llc Substituted quinazolines as kinase inhibitors
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US8476431B2 (en) 2008-11-03 2013-07-02 Itellikine LLC Benzoxazole kinase inhibitors and methods of use
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US9315505B2 (en) 2009-05-07 2016-04-19 Intellikine Llc Heterocyclic compounds and uses thereof
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US9206182B2 (en) 2009-07-15 2015-12-08 Intellikine Llc Substituted isoquinolin-1(2H)-one compounds, compositions, and methods thereof
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US9738644B2 (en) 2010-05-21 2017-08-22 Infinity Pharmaceuticals, Inc. Chemical compounds, compositions and methods for kinase modulation
US8604032B2 (en) 2010-05-21 2013-12-10 Infinity Pharmaceuticals, Inc. Chemical compounds, compositions and methods for kinase modulation
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US9290497B2 (en) 2011-01-10 2016-03-22 Infinity Pharmaceuticals, Inc. Processes for preparing isoquinolinones and solid forms of isoquinolinones
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US10550122B2 (en) 2011-01-10 2020-02-04 Infinity Pharmaceuticals, Inc. Solid forms of (S)-3-(1-(9H-purin-6-ylamino)ethyl)-8-chloro-2-phenylisoquinolin-1(2H)-one and methods of use thereof
US9840505B2 (en) 2011-01-10 2017-12-12 Infinity Pharmaceuticals, Inc. Solid forms of (S)-3-(1-(9H-purin-6-ylamino)ethyl)-8-chloro-2-phenylisoquinolin-1 (2H)-one and methods of use thereof
US8809349B2 (en) 2011-01-10 2014-08-19 Infinity Pharmaceuticals, Inc. Processes for preparing isoquinolinones and solid forms of isoquinolinones
USRE46621E1 (en) 2011-01-10 2017-12-05 Infinity Pharmaceuticals, Inc. Processes for preparing isoquinolinones and solid forms of isoquinolinones
US9295673B2 (en) 2011-02-23 2016-03-29 Intellikine Llc Combination of mTOR inhibitors and P13-kinase inhibitors, and uses thereof
US9605003B2 (en) 2011-07-19 2017-03-28 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
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US9718815B2 (en) 2011-07-19 2017-08-01 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
US9546180B2 (en) 2011-08-29 2017-01-17 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
US9115141B2 (en) 2011-08-29 2015-08-25 Infinity Pharmaceuticals, Inc. Substituted isoquinolinones and methods of treatment thereof
US8785470B2 (en) 2011-08-29 2014-07-22 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
US9895373B2 (en) 2011-09-02 2018-02-20 The Regents Of The University Of California Substituted pyrazolo[3,4-D]pyrimidines and uses thereof
US9321772B2 (en) 2011-09-02 2016-04-26 The Regents Of The University Of California Substituted pyrazolo[3,4-D]pyrimidines and uses thereof
US9200009B2 (en) 2011-10-12 2015-12-01 Shionogi & Co., Ltd. Polycyclic pyridone derivative having integrase inhibitory activity
US9399626B2 (en) 2011-11-11 2016-07-26 Pfizer Inc. 2-thiopyrimidinones
US8835449B2 (en) 2011-11-11 2014-09-16 Pfizer Inc. 2-thiopyrimidinones
US9873673B2 (en) 2011-11-11 2018-01-23 Pfizer Inc. 2-thiopyrimidinones
US8841314B2 (en) 2011-11-11 2014-09-23 Pfizer Inc. 2-Thiopyrimidinones
US8940742B2 (en) 2012-04-10 2015-01-27 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
US9255108B2 (en) 2012-04-10 2016-02-09 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
US8828998B2 (en) 2012-06-25 2014-09-09 Infinity Pharmaceuticals, Inc. Treatment of lupus, fibrotic conditions, and inflammatory myopathies and other disorders using PI3 kinase inhibitors
US9527847B2 (en) 2012-06-25 2016-12-27 Infinity Pharmaceuticals, Inc. Treatment of lupus, fibrotic conditions, and inflammatory myopathies and other disorders using PI3 kinase inhibitors
US10822340B2 (en) 2012-09-26 2020-11-03 The Regents Of The University Of California Substituted imidazolopyrazine compounds and methods of using same
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US12213983B2 (en) 2012-11-01 2025-02-04 Infinity Pharmaceuticals, Inc. Treatment of cancers using PI3 kinase isoform modulators
US9481667B2 (en) 2013-03-15 2016-11-01 Infinity Pharmaceuticals, Inc. Salts and solid forms of isoquinolinones and composition comprising and methods of using the same
US9751888B2 (en) 2013-10-04 2017-09-05 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
US9359365B2 (en) 2013-10-04 2016-06-07 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
US12152032B2 (en) 2013-10-04 2024-11-26 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
US9828377B2 (en) 2013-10-04 2017-11-28 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
US10329299B2 (en) 2013-10-04 2019-06-25 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
US11541059B2 (en) 2014-03-19 2023-01-03 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
US10675286B2 (en) 2014-03-19 2020-06-09 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
US9775844B2 (en) 2014-03-19 2017-10-03 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
US11110096B2 (en) 2014-04-16 2021-09-07 Infinity Pharmaceuticals, Inc. Combination therapies
US11944631B2 (en) 2014-04-16 2024-04-02 Infinity Pharmaceuticals, Inc. Combination therapies
JPWO2016021539A1 (ja) * 2014-08-06 2017-04-27 エーザイ・アール・アンド・ディー・マネジメント株式会社 ピリミジン−１−オール化合物の製造方法及びその中間体
US10065930B2 (en) 2014-08-06 2018-09-04 Eisai R&D Management Co., Ltd. Method for producing pyrimidine-1-ol compound, and intermediate thereof
WO2016021539A1 (ja) * 2014-08-06 2016-02-11 エーザイ・アール・アンド・ディー・マネジメント株式会社 ピリミジン－１－オール化合物の製造方法及びその中間体
RU2681937C2 (ru) * 2014-08-06 2019-03-14 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Способ получения пиримидин-1-олового соединения и его промежуточного соединения
EP3757105A2 (en) 2014-08-22 2020-12-30 Shionogi & Co., Ltd Polycyclic pyridone derivative having integrase inhibitory activity
US9708348B2 (en) 2014-10-03 2017-07-18 Infinity Pharmaceuticals, Inc. Trisubstituted bicyclic heterocyclic compounds with kinase activities and uses thereof
US10253047B2 (en) 2014-10-03 2019-04-09 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
US10941162B2 (en) 2014-10-03 2021-03-09 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
US9771332B2 (en) 2015-05-05 2017-09-26 Pfizer Inc. 2-thiopyrimidinones
US12384792B2 (en) 2015-09-14 2025-08-12 Twelve Therapeutics, Inc. Solid forms of isoquinolinones, and process of making, composition comprising, and methods of using the same
US11939333B2 (en) 2015-09-14 2024-03-26 Infinity Pharmaceuticals, Inc. Solid forms of isoquinolinones, and process of making, composition comprising, and methods of using the same
US10160761B2 (en) 2015-09-14 2018-12-25 Infinity Pharmaceuticals, Inc. Solid forms of isoquinolinones, and process of making, composition comprising, and methods of using the same
US11247995B2 (en) 2015-09-14 2022-02-15 Infinity Pharmaceuticals, Inc. Solid forms of isoquinolinones, and process of making, composition comprising, and methods of using the same
US11453677B2 (en) 2016-03-08 2022-09-27 Novartis Ag Tricyclic compounds useful to treat orthomyxovirus infections
JP2019512485A (ja) * 2016-03-08 2019-05-16 ノバルティス アーゲー オルトミクソウイルス感染の処置に有用な三環式化合物
US10759806B2 (en) 2016-03-17 2020-09-01 Infinity Pharmaceuticals, Inc. Isotopologues of isoquinolinone and quinazolinone compounds and uses thereof as PI3K kinase inhibitors
US10919914B2 (en) 2016-06-08 2021-02-16 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
US11147818B2 (en) 2016-06-24 2021-10-19 Infinity Pharmaceuticals, Inc. Combination therapies
US11912715B2 (en) 2016-08-29 2024-02-27 Novartis Ag Fused tricyclic pyridazinone compounds useful to treat orthomyxovirus infections
US11098051B2 (en) 2016-08-29 2021-08-24 Novartis Ag Fused tricyclic pyridazinone compounds useful to treat orthomyxovirus infections
CN106810458A (zh) * 2016-12-31 2017-06-09 武汉工程大学 一种拆分dl‑2‑氨基丙醇制备l‑2‑氨基丙醇的方法
CN106810458B (zh) * 2016-12-31 2019-05-03 武汉工程大学 一种拆分dl-2-氨基丙醇制备l-2-氨基丙醇的方法
WO2019054427A1 (ja) 2017-09-14 2019-03-21 第一三共株式会社 環状構造を有する化合物
US11629149B2 (en) 2018-02-28 2023-04-18 Novartis Ag 10-(di(phenyl)methyl)-4-hydroxy-8,9,9A,10-tetrahydro-7H-pyrrolo[1′,2′:4,5]pyrazino[1,2-b]pyridazine-3,5-dione derivatives and related compounds as inhibitors of the orthomyxovirus replication for treating influenza
US12071441B2 (en) 2018-02-28 2024-08-27 Novartis Ag 10-(di(phenyl)methyl)-4-hydroxy-8,9,9A,10-tetrahydro-7H-pyrrolo[1′,2′:4,5]pyrazino[1,2-b]pyridazine-3,5-dione derivatives and related compounds as inhibitors of the orthomyxovirus replication for treating influenza
CN108658784A (zh) * 2018-04-26 2018-10-16 联化科技股份有限公司 (r)-1-(4-甲基苯基)乙胺的合成方法
WO2020083662A1 (en) 2018-10-23 2020-04-30 Basf Se Tricyclic pesticidal compounds
WO2021209265A1 (en) 2020-04-14 2021-10-21 Basf Se Tricyclic pesticidal compounds
JP2023527281A (ja) * 2020-05-18 2023-06-28 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 神経炎症の処置のためのｃｋ２阻害剤として使用するための、例えばフラボンなどのクロメン－４－オン誘導体
WO2023243678A1 (ja) 2022-06-15 2023-12-21 日産化学株式会社 ピラゾール化合物、その製造中間体、及び有害生物防除剤
WO2024204842A1 (ja) 2023-03-31 2024-10-03 日産化学株式会社 ピラゾール化合物及び有害生物防除剤

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US9572813B2 (en) 2017-02-21
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US20170066754A1 (en) 2017-03-09
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