JP2007519735A - Ｈｉｖインテグラーゼ阻害剤として有用であるｎ−ベンジル−３，４−ジヒドロキシピリジン−２−カルボキサミド及びｎ−ベンジル−２，３−ジヒドロキシピリジン−４−カルボキサミド化合物 - Google Patents

Ｈｉｖインテグラーゼ阻害剤として有用であるｎ−ベンジル−３，４−ジヒドロキシピリジン−２−カルボキサミド及びｎ−ベンジル−２，３−ジヒドロキシピリジン−４−カルボキサミド化合物 Download PDF

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Publication number
JP2007519735A
JP2007519735A JP2006551441A JP2006551441A JP2007519735A JP 2007519735 A JP2007519735 A JP 2007519735A JP 2006551441 A JP2006551441 A JP 2006551441A JP 2006551441 A JP2006551441 A JP 2006551441A JP 2007519735 A JP2007519735 A JP 2007519735A
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alkyl
fluorobenzyl
ring
dihydroxy
aryl
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JP2007519735A5 (enExample
Inventor
ジヨーンズ，フイリツプ
ウイリアムズ，ピーター・デイー
モリセツト，マシユー・エム
クオ，ミシエル・スパークス
バツカ，ジヨゼフ・ピー
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Merck and Co Inc
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Merck and Co Inc
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Publication of JP2007519735A publication Critical patent/JP2007519735A/ja
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/63—One oxygen atom
    • C07D213/64—One oxygen atom attached in position 2 or 6
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/69—Two or more oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • 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
    • 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
    • C07D409/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D417/02—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
    • 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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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Virology (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oncology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • AIDS & HIV (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2006551441A 2004-01-30 2005-01-26 Ｈｉｖインテグラーゼ阻害剤として有用であるｎ−ベンジル−３，４−ジヒドロキシピリジン−２−カルボキサミド及びｎ−ベンジル−２，３−ジヒドロキシピリジン−４−カルボキサミド化合物 Withdrawn JP2007519735A (ja)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US54053804P 2004-01-30 2004-01-30
PCT/US2005/002472 WO2005074513A2 (en) 2004-01-30 2005-01-26 N-benzyl-3,4-dihyroxypyridine-2-carboxamide and n-benzyl-2,3-dihydroxypyridine-4-carboxamide compounds useful as hiv integrase inhibitors

Publications (2)

Publication Number Publication Date
JP2007519735A true JP2007519735A (ja) 2007-07-19
JP2007519735A5 JP2007519735A5 (enExample) 2008-03-13

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JP2006551441A Withdrawn JP2007519735A (ja) 2004-01-30 2005-01-26 Ｈｉｖインテグラーゼ阻害剤として有用であるｎ−ベンジル−３，４−ジヒドロキシピリジン−２−カルボキサミド及びｎ−ベンジル−２，３−ジヒドロキシピリジン−４−カルボキサミド化合物

Country Status (7)

Country Link
US (1) US20070155744A1 (enExample)
EP (1) EP1713773A4 (enExample)
JP (1) JP2007519735A (enExample)
CN (1) CN101014571A (enExample)
AU (1) AU2005211349A1 (enExample)
CA (1) CA2554120A1 (enExample)
WO (1) WO2005074513A2 (enExample)

Cited By (5)

* Cited by examiner, † Cited by third party
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JP2013521286A (ja) * 2010-03-04 2013-06-10 メルク・シャープ・エンド・ドーム・コーポレイション カテコールｏ−メチルトランスフェラーゼの阻害剤および精神障害の治療におけるその使用
JP2014221826A (ja) * 2009-11-06 2014-11-27 エアーピオ セラピューティクス インコーポレイテッド 大腸炎を治療するための組成物および方法
JP2016508145A (ja) * 2013-01-08 2016-03-17 ザヴィラ ファーマシューティカルズ ゲーエムベーハー ピリドン誘導体及びウイルス性疾患の治療、改善又は予防におけるそれらの使用
JP2017520597A (ja) * 2014-07-16 2017-07-27 ライフサイ ファーマシューティカルズ，インク． 治療用阻害化合物
JP2017523197A (ja) * 2014-07-30 2017-08-17 エービーエーシー セラピューティクス，エス．エル． ２−ピリドン部分を含む選択的抗菌剤としてのアリールヒドラジド

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WO2003016275A1 (fr) 2001-08-10 2003-02-27 Shionogi & Co., Ltd. Agent antiviral
AU2006306355A1 (en) * 2005-10-27 2007-05-03 Merck & Co., Inc. HIV integrase inhibitors
US8278337B2 (en) 2006-12-20 2012-10-02 Merck Sharp & Dohme Substituted pyridines that are JNK inhibitors
US8993557B2 (en) * 2011-09-30 2015-03-31 Bristol-Myers Squibb Company Pyridinedione carboxamide inhibitors of endothelial lipase
US8933235B2 (en) 2011-09-30 2015-01-13 Bristol-Myers Squibb Company Pyridinedione carboxamide inhibitors of endothelial lipase
EP2780014A4 (en) * 2011-11-18 2015-07-01 Constellation Pharmaceuticals Inc MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF
EP2780013A4 (en) 2011-11-18 2015-07-01 Constellation Pharmaceuticals Inc MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF
HRP20171665T1 (hr) 2011-12-28 2017-12-15 Global Blood Therapeutics, Inc. Supstituirani spojevi benzaldehida i metode za njihovu primjenu u povećanju oksigenacije tkiva
HK1203412A1 (en) 2011-12-28 2015-10-30 Global Blood Therapeutics, Inc. Substituted heteroaryl aldehyde compounds and methods for their use in increasing tissue oxygenation
EP2812001B1 (en) 2012-02-10 2017-06-14 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
JP6243908B2 (ja) 2012-08-23 2017-12-06 アリオス バイオファーマ インク． パラミクソウイルス感染症を治療するための化合物
WO2014043252A2 (en) * 2012-09-11 2014-03-20 Rutgers, The State University Of New Jersey Therapeutic hydroxypyridinones, hydroxypyrimidinones and hydroxypyridazinones
MX344879B (es) 2012-12-21 2017-01-11 Gilead Sciences Inc Compuestos de carbamoilpiridona policiclicos y su uso farmaceutico.
EP2970308B1 (en) 2013-03-15 2021-07-14 Global Blood Therapeutics, Inc. Compounds and uses thereof for the modulation of hemoglobin
US20140274961A1 (en) 2013-03-15 2014-09-18 Global Blood Therapeutics, Inc. Compounds and uses thereof for the modulation of hemoglobin
US9422279B2 (en) 2013-03-15 2016-08-23 Global Blood Therapeutics, Inc. Compounds and uses thereof for the modulation of hemoglobin
US10266551B2 (en) 2013-03-15 2019-04-23 Global Blood Therapeutics, Inc. Compounds and uses thereof for the modulation of hemoglobin
WO2014151142A1 (en) 2013-03-15 2014-09-25 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
PE20161035A1 (es) 2013-03-15 2016-11-13 Global Blood Therapeutics Inc Compuestos y usos de estos para la modulacion de la hemoglobina
US9458139B2 (en) 2013-03-15 2016-10-04 Global Blood Therapeutics, Inc. Compounds and uses thereof for the modulation of hemoglobin
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US9802900B2 (en) 2013-03-15 2017-10-31 Global Blood Therapeutics, Inc. Bicyclic heteroaryl compounds and uses thereof for the modulation of hemoglobin
CA2902711C (en) 2013-03-15 2021-07-06 Global Blood Therapeutics, Inc. Substituted pyridinyl-6-methoxy-2-hydroxybenzaldehyde derivatives and pharmaceutical compositions thereof useful for the modulation of hemoglobin
US10100043B2 (en) 2013-03-15 2018-10-16 Global Blood Therapeutics, Inc. Substituted aldehyde compounds and methods for their use in increasing tissue oxygenation
US9604999B2 (en) 2013-03-15 2017-03-28 Global Blood Therapeutics, Inc. Compounds and uses thereof for the modulation of hemoglobin
EP2986291B1 (en) 2013-04-16 2020-05-27 Merck Sharp & Dohme Corp. 4-pyridone derivative compounds and uses thereof as hiv integrase inhibitors
LT3019503T (lt) 2013-07-12 2017-11-27 Gilead Sciences, Inc. Policikliniai karbamoilpiridono junginiai ir jų panaudojimas živ infekcijų gydymui
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EP3033334A1 (en) 2013-08-15 2016-06-22 Constellation Pharmaceuticals, Inc. Indole derivatives as modulators of methyl modifying enzymes, compositions and uses thereof
EA201992707A1 (ru) 2013-11-18 2020-06-30 Глобал Блад Терапьютикс, Инк. Соединения и их применения для модуляции гемоглобина
AP2016009261A0 (en) 2014-02-07 2016-06-30 Global Blood Therapeutics Inc Crystalline polymorphs of the free base of 2-hydroxy-6-((2-(1-isopropyl-1h-pyrazol-5-yl)pyridin-3-yl)methoxy)benzaldehyde
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TWI738321B (zh) 2014-12-23 2021-09-01 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
MA41614A (fr) 2015-02-25 2018-01-02 Alios Biopharma Inc Composés antiviraux
MA41841A (fr) 2015-03-30 2018-02-06 Global Blood Therapeutics Inc Composés aldéhyde pour le traitement de la fibrose pulmonaire, de l'hypoxie, et de maladies auto-immunes et des tissus conjonctifs
CA2980362C (en) 2015-04-02 2020-02-25 Gilead Sciences, Inc. Polycyclic-carbamoylpyridone compounds and their pharmaceutical use
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TW202332423A (zh) 2016-10-12 2023-08-16 美商全球血液治療公司 包含2-羥基-6-((2-(1-異丙基-1h-吡唑-5-基)吡啶-3-基)甲氧基)-苯甲醛之片劑
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US11014884B2 (en) 2018-10-01 2021-05-25 Global Blood Therapeutics, Inc. Modulators of hemoglobin
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US6306891B1 (en) * 1998-06-03 2001-10-23 Merck & Co., Inc. HIV integrase inhibitors
PE20000942A1 (es) * 1998-07-31 2000-09-28 Lilly Co Eli Derivados de amida, carbamato y urea
NZ525088A (en) * 2000-10-12 2004-11-26 Merck & Co Inc Aza- and polyaza-naphthalenyl carboxamides useful as HIV integrase inhibitors
WO2003016275A1 (fr) * 2001-08-10 2003-02-27 Shionogi & Co., Ltd. Agent antiviral
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WO2005042524A1 (en) * 2003-10-30 2005-05-12 Virochem Pharma Inc. Pyridine carboxamide and methods for inhibiting hiv integrase

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JP2014221826A (ja) * 2009-11-06 2014-11-27 エアーピオ セラピューティクス インコーポレイテッド 大腸炎を治療するための組成物および方法
JP2013521286A (ja) * 2010-03-04 2013-06-10 メルク・シャープ・エンド・ドーム・コーポレイション カテコールｏ−メチルトランスフェラーゼの阻害剤および精神障害の治療におけるその使用
US9309199B2 (en) 2010-03-04 2016-04-12 Merck Sharp & Dohme Corp. Inhibitors of catechol O-methyl transferase and their use in the treatment of psychotic disorders
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JP2017520597A (ja) * 2014-07-16 2017-07-27 ライフサイ ファーマシューティカルズ，インク． 治療用阻害化合物
JP2020147575A (ja) * 2014-07-16 2020-09-17 ライフサイ ファーマシューティカルズ，インク． 治療用阻害化合物
JP2017523197A (ja) * 2014-07-30 2017-08-17 エービーエーシー セラピューティクス，エス．エル． ２−ピリドン部分を含む選択的抗菌剤としてのアリールヒドラジド

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