TWI664967B - 新穎化合物（一） - Google Patents

新穎化合物（一） Download PDF

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Publication number
TWI664967B
TWI664967B TW104104905A TW104104905A TWI664967B TW I664967 B TWI664967 B TW I664967B TW 104104905 A TW104104905 A TW 104104905A TW 104104905 A TW104104905 A TW 104104905A TW I664967 B TWI664967 B TW I664967B
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Taiwan
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compound
formula
dry powder
disease
compounds
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TW104104905A
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Chinese (zh)
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TW201620518A (zh
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艾利斯泰爾 龍修
尤安 佛迪斯
史都亞特 翁尼恩斯
約翰 金安得伍德
珍妮佛 維納伯
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英商瑞斯比維特有限公司
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/007—Pulmonary tract; Aromatherapy
    • A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
    • A61K9/0075—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy for inhalation via a dry powder inhaler [DPI], e.g. comprising micronized drug mixed with lactose carrier particles
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    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
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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
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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965—Non-condensed pyrazines
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    • A61K31/5375—1,4-Oxazines, e.g. morpholine
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    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
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    • 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
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    • 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
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    • 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
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  • Health & Medical Sciences (AREA)
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  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Diabetes (AREA)
  • Otolaryngology (AREA)
  • Emergency Medicine (AREA)
  • Rheumatology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Biochemistry (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Molecular Biology (AREA)
  • Transplantation (AREA)
  • Endocrinology (AREA)
  • Cardiology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Virology (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
TW104104905A 2014-02-14 2015-02-13 新穎化合物（一） TWI664967B (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201461940282P 2014-02-14 2014-02-14
US61/940,282 2014-02-14
US201461941064P 2014-02-18 2014-02-18
US61/941,064 2014-02-18

Publications (2)

Publication Number Publication Date
TW201620518A TW201620518A (zh) 2016-06-16
TWI664967B true TWI664967B (zh) 2019-07-11

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TW104104905A TWI664967B (zh) 2014-02-14 2015-02-13 新穎化合物（一）
TW104104906A TWI751099B (zh) 2014-02-14 2015-02-13 作為激酶抑制劑之吡唑基脲，包含其之製藥組成物及其用途

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US (8) US9447076B2 (enExample)
EP (4) EP3105223B1 (enExample)
JP (4) JP6586098B2 (enExample)
KR (1) KR102413704B1 (enExample)
CN (4) CN106164067B (enExample)
AU (3) AU2015216705B2 (enExample)
BR (1) BR112016015838B1 (enExample)
CA (1) CA2938924C (enExample)
DK (2) DK3105222T3 (enExample)
EA (1) EA034927B1 (enExample)
ES (2) ES2774249T3 (enExample)
JO (1) JO3392B1 (enExample)
MX (2) MX371353B (enExample)
PL (2) PL3357919T3 (enExample)
PT (2) PT3357919T (enExample)
SG (1) SG11201607058PA (enExample)
TR (1) TR201809072T4 (enExample)
TW (2) TWI664967B (enExample)
UY (1) UY35998A (enExample)
WO (2) WO2015121444A1 (enExample)

Families Citing this family (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009077766A1 (en) 2007-12-19 2009-06-25 Cancer Research Technology Limited Pyrido[2,3-b]pyrazine-8-substituted compounds and their use
JP5760010B2 (ja) 2010-02-01 2015-08-05 キャンサー・リサーチ・テクノロジー・リミテッド １−（５−ｔｅｒｔ−ブチル−２−フェニル−２Ｈ−ピラゾール−３−イル）−３−［２−フルオロ−４−（１−メチル−２−オキソ−２，３−ジヒドロ−１Ｈ−イミダゾ［４，５−Ｂ］ピリジン−７−イルオキシ）−フェニル］−尿素および関連化合物ならびに治療におけるそれらの使用
KR102057058B1 (ko) 2011-10-03 2019-12-18 레스피버트 리미티드 P38 map 키나제 저해제인 1-피라졸릴-3-(4-((2-아닐리노피리미딘-4-일)옥시)나프탈렌-1-일) 우레아
EP2578582A1 (en) 2011-10-03 2013-04-10 Respivert Limited 1-Pyrazolyl-3-(4-((2-anilinopyrimidin-4-yl)oxy)napththalen-1-yl)ureas as p38 MAP kinase inhibitors
GB201214750D0 (en) 2012-08-17 2012-10-03 Respivert Ltd Compounds
US20150225373A1 (en) 2012-08-29 2015-08-13 Respivert Limited Kinase inhibitors
US9783556B2 (en) 2012-08-29 2017-10-10 Respivert Limited Kinase inhibitors
US20150210722A1 (en) 2012-08-29 2015-07-30 Respivert Limited Kinase inhibitors
EP2925742B1 (en) 2012-11-16 2016-10-26 Respivert Limited Kinase inhibitors
US20160016934A1 (en) 2013-03-14 2016-01-21 Respivert Limited Kinase inhibitors
TWI641592B (zh) 2013-04-02 2018-11-21 英商瑞斯比維特有限公司 激酶抑制劑
US9771353B2 (en) 2013-04-02 2017-09-26 Topivert Pharma Limited Kinase inhibitors based upon N-alkyl pyrazoles
GB201320729D0 (en) 2013-11-25 2014-01-08 Cancer Rec Tech Ltd Therapeutic compounds and their use
GB201320732D0 (en) 2013-11-25 2014-01-08 Cancer Rec Tech Ltd Methods of chemical synthesis
JP6514703B2 (ja) 2013-12-20 2019-05-15 トピバート ファーマ リミテッド キナーゼインヒビターとして有用な尿素誘導体
CN106164067B (zh) 2014-02-14 2019-09-10 瑞斯比维特有限公司 作为抗炎化合物的芳族杂环化合物
MA40774A (fr) 2014-10-01 2017-08-08 Respivert Ltd Dérivés de diaryle-urée en tant qu'inhibiteurs de kinase p38
CN105801486A (zh) * 2016-03-31 2016-07-27 常州大学 一种1-（2,4二溴苯基）-3-吡唑醇的合成方法
MA44607A (fr) 2016-04-06 2021-05-19 Oxular Acquisitions Ltd Inhibiteurs de kinase
CN116570594A (zh) * 2016-06-23 2023-08-11 马里兰大学巴尔的摩分校 选择性p38α特异性MAPK抑制剂
US20200087390A1 (en) 2016-12-21 2020-03-19 Amgen Inc. Anti-tnf alpha antibody formulations
US10342786B2 (en) 2017-10-05 2019-07-09 Fulcrum Therapeutics, Inc. P38 kinase inhibitors reduce DUX4 and downstream gene expression for the treatment of FSHD
PT3691620T (pt) 2017-10-05 2022-10-06 Fulcrum Therapeutics Inc Os inibidores da quinase p38 reduzem a expressão de dux4 e genes a jusante para o tratamento de fshd
AU2019392904B9 (en) 2018-12-07 2022-12-22 University Of Maryland, Baltimore Non-ATP/catalytic site p38 mitogen activated protein kinase inhibitors
US10851102B2 (en) * 2019-01-23 2020-12-01 Theravance Biopharma R&D Ip, Llc Imidazole and triazole containing bicyclic compounds as JAK inhibitors
CN116406355A (zh) 2020-05-18 2023-07-07 Gen1E生命科学公司 P38α促分裂原活化蛋白激酶抑制剂
CN111889025B (zh) * 2020-09-01 2022-01-11 山东大学 一种耐酸碱耐盐超两亲分子乳化剂及其制备方法和乳液
AU2021370893B2 (en) 2020-10-29 2024-03-07 Gen1E Lifesciences Inc. Crystalline 5-(dimethylamino) -n- (4-(morpholinomethyl)phenyl) naphthalene-1-sulfonamide di-hydrochloride di-hydrate
WO2022169962A1 (en) * 2021-02-03 2022-08-11 Bp Asset V, Inc. Formulation of furin inhibitor for inhalation
WO2022204046A1 (en) 2021-03-23 2022-09-29 Gen1E Lifesciences Inc. Substituted naphthyl p38alpha mitogen-activated protein kinase inhibitors
CN116655608B (zh) * 2023-05-30 2025-08-19 成都瑞芬思德丹生物科技有限公司 一种具有抗炎活性的吡咯烷酮类化合物及其制备方法和应用

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000043384A1 (en) * 1999-01-19 2000-07-27 Boehringer Ingelheim Pharmaceuticals, Inc. Aromatic heterocyclic compounds as antiinflammatory agents
WO2013050757A1 (en) * 2011-10-03 2013-04-11 Respivert Limited 1-pyrazolyl-3- (4- ( (2 -anilinopyrimidin- 4 - yl) oxy) napththalen- 1 - yl) ureas as p38 map kinase inhibitors

Family Cites Families (51)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20080300281A1 (en) 1997-12-22 2008-12-04 Jacques Dumas Inhibition of p38 Kinase Activity Using Aryl and Heteroaryl Substituted Heterocyclic Ureas
EP1056725B1 (en) 1997-12-22 2006-06-07 Bayer Pharmaceuticals Corp. Inhibition of raf kinase using aryl and heteroaryl substituted heterocyclic ureas
AU762077B2 (en) 1997-12-22 2003-06-19 Bayer Healthcare Llc Inhibition of p38 kinase activity using aryl and heteroaryl substituted heterocyclic ureas
US7329670B1 (en) 1997-12-22 2008-02-12 Bayer Pharmaceuticals Corporation Inhibition of RAF kinase using aryl and heteroaryl substituted heterocyclic ureas
EP1200411B1 (en) 1999-07-09 2005-12-14 Boehringer Ingelheim Pharmaceuticals Inc. Process for synthesis of heteroaryl-substituted urea compounds
US6492393B1 (en) 1999-11-16 2002-12-10 Boehringer Ingelheim Pharmaceuticals, Inc. Compounds useful as anti-inflammatory agents
US6525046B1 (en) 2000-01-18 2003-02-25 Boehringer Ingelheim Pharmaceuticals, Inc. Aromatic heterocyclic compounds as antiinflammatory agents
US6492529B1 (en) 2000-01-18 2002-12-10 Boehringer Ingelheim Pharmaceuticals, Inc. Bis pyrazole-1H-pyrazole intermediates and their synthesis
WO2001064643A2 (en) 2000-02-29 2001-09-07 Cor Therapeutics, Inc. BENZAMIDES AND RELATED INHIBITORS OF FACTOR Xa
JP2004530690A (ja) 2001-05-16 2004-10-07 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド 抗炎症性薬剤として有用なジアリールウレア誘導体
JP2004536845A (ja) 2001-07-11 2004-12-09 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド サイトカイン媒介疾患の治療方法
SI1478358T1 (sl) 2002-02-11 2013-09-30 Bayer Healthcare Llc Sorafenib tozilat za zdravljenje bolezni, značilnih po abnormalni angiogenezi
WO2003068229A1 (en) 2002-02-11 2003-08-21 Bayer Pharmaceuticals Corporation Pyridine, quinoline, and isoquinoline n-oxides as kinase inhibitors
US7041669B2 (en) 2002-02-25 2006-05-09 Boehringer Ingelheim Pharmaceuticals, Inc. 1,4-benzofused urea compounds useful in treating cytokine mediated diseases
AU2003243921B2 (en) 2002-06-27 2009-05-07 Novo Nordisk A/S Aryl carbonyl derivatives as therapeutic agents
US20060004010A1 (en) 2002-07-10 2006-01-05 Hiromu Habashita Ccr4 antagonist and medical use thereof
US7557129B2 (en) 2003-02-28 2009-07-07 Bayer Healthcare Llc Cyanopyridine derivatives useful in the treatment of cancer and other disorders
WO2004078746A2 (en) 2003-02-28 2004-09-16 Bayer Pharmaceuticals Corporation 2-oxo-1,3,5-perhydrotriazapine derivatives useful in the treatment of hyper-proliferative, angiogenesis, and inflammatrory disorders
CN101010315A (zh) 2004-04-30 2007-08-01 拜耳制药公司 用于治疗癌症的取代的吡唑基脲衍生物
GB0500435D0 (en) 2005-01-10 2005-02-16 Novartis Ag Organic compounds
ES2352796T3 (es) 2005-06-27 2011-02-23 Bristol-Myers Squibb Company Antagonistas cíclicos unidos a c del receptor p2y1 útiles en el tratamiento de afecciones trombóticas.
CA2673483C (en) 2006-10-20 2014-04-08 Icos Corporation Compositions of chk1 inhibitors
PL2947072T3 (pl) 2008-03-17 2017-05-31 Ambit Biosciences Corporation 1-(3-(6,7-dimetoksychinazolin-4-yloksy)fenylo)-3-(5-(1,1,1-trifluoro-2-metylopropan-2-ylo)izoksazol-3-ilo)mocznik jako modulator kinazy RAF w leczeniu chorób nowotworowych
BRPI0920707A2 (pt) 2008-10-02 2015-12-29 Respivert Ltd compostos
GB0818033D0 (en) 2008-10-02 2008-11-05 Respivert Ltd Novel compound
WO2010067131A1 (en) 2008-12-11 2010-06-17 Respivert Limited P38 map kinase inhibitors
GB0905955D0 (en) * 2009-04-06 2009-05-20 Respivert Ltd Novel compounds
GB0921731D0 (en) 2009-12-11 2010-01-27 Respivert Ltd Theraputic uses
GB0921730D0 (en) 2009-12-11 2010-01-27 Respivert Ltd Method of treatment
EP2738161B1 (en) 2010-03-15 2018-04-11 Ube Industries, Ltd. Method for producing amide compound
GB201005589D0 (en) 2010-04-01 2010-05-19 Respivert Ltd Novel compounds
WO2011124923A2 (en) * 2010-04-08 2011-10-13 Respivert Limited Novel compounds
EP2556068B1 (en) 2010-04-08 2019-01-23 Respivert Limited P38 map kinase inhibitors
GB201010196D0 (en) 2010-06-17 2010-07-21 Respivert Ltd Methods
US8933228B2 (en) 2010-06-17 2015-01-13 Respivert, Ltd. Respiratory formulations and compounds for use therein
GB201010193D0 (en) 2010-06-17 2010-07-21 Respivert Ltd Medicinal use
EP2578582A1 (en) 2011-10-03 2013-04-10 Respivert Limited 1-Pyrazolyl-3-(4-((2-anilinopyrimidin-4-yl)oxy)napththalen-1-yl)ureas as p38 MAP kinase inhibitors
BR112014013760A2 (pt) 2011-12-09 2017-06-13 Chiesi Farm Spa composto, composição farmacêutica e uso de um composto
GB201214750D0 (en) 2012-08-17 2012-10-03 Respivert Ltd Compounds
US9783556B2 (en) 2012-08-29 2017-10-10 Respivert Limited Kinase inhibitors
US20150225373A1 (en) 2012-08-29 2015-08-13 Respivert Limited Kinase inhibitors
GB201215357D0 (en) 2012-08-29 2012-10-10 Respivert Ltd Compounds
US20150210722A1 (en) 2012-08-29 2015-07-30 Respivert Limited Kinase inhibitors
EP2925742B1 (en) 2012-11-16 2016-10-26 Respivert Limited Kinase inhibitors
US20160016934A1 (en) 2013-03-14 2016-01-21 Respivert Limited Kinase inhibitors
TWI641592B (zh) 2013-04-02 2018-11-21 英商瑞斯比維特有限公司 激酶抑制劑
US9771353B2 (en) 2013-04-02 2017-09-26 Topivert Pharma Limited Kinase inhibitors based upon N-alkyl pyrazoles
JP6514703B2 (ja) 2013-12-20 2019-05-15 トピバート ファーマ リミテッド キナーゼインヒビターとして有用な尿素誘導体
CN106164067B (zh) * 2014-02-14 2019-09-10 瑞斯比维特有限公司 作为抗炎化合物的芳族杂环化合物
EP3201189A1 (en) 2014-10-01 2017-08-09 Respivert Limited N-phenyl-3-quinazolin-6-yl-benzamide derivatives as p38 kinase inhibitors
MA40774A (fr) 2014-10-01 2017-08-08 Respivert Ltd Dérivés de diaryle-urée en tant qu'inhibiteurs de kinase p38

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000043384A1 (en) * 1999-01-19 2000-07-27 Boehringer Ingelheim Pharmaceuticals, Inc. Aromatic heterocyclic compounds as antiinflammatory agents
WO2013050757A1 (en) * 2011-10-03 2013-04-11 Respivert Limited 1-pyrazolyl-3- (4- ( (2 -anilinopyrimidin- 4 - yl) oxy) napththalen- 1 - yl) ureas as p38 map kinase inhibitors

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