JP5903499B2 - ジヒドロ−ベンゾ−オキサジンおよびジヒドロ−ピリド−オキサジン誘導体 - Google Patents

ジヒドロ−ベンゾ−オキサジンおよびジヒドロ−ピリド−オキサジン誘導体 Download PDF

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JP5903499B2
JP5903499B2 JP2014548315A JP2014548315A JP5903499B2 JP 5903499 B2 JP5903499 B2 JP 5903499B2 JP 2014548315 A JP2014548315 A JP 2014548315A JP 2014548315 A JP2014548315 A JP 2014548315A JP 5903499 B2 JP5903499 B2 JP 5903499B2
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dihydro
yloxy
benzo
oxazin
pyridin
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JP2015506344A (ja
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ジョルジオ・カラヴァッティ
シルヴィー・シャモワン
パスカル・フュレ
クレメンス・ヘゲナウアー
コンスタンツェ・フルト
クリストフ・カリス
カレン・カマーテンス
イアン・ルイス
ヘンリク・メビッツ
アレクサンダー・バクスター・スミス
ニコラ・ソルダーマン
ロマン・ウルフ
フレデリック・ゼクリ
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ノバルティス アーゲー
ノバルティス アーゲー
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    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
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    • 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
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/538—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
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    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • 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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    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
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  • Biomedical Technology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
JP2014548315A 2011-12-22 2012-12-20 ジヒドロ−ベンゾ−オキサジンおよびジヒドロ−ピリド−オキサジン誘導体 Active JP5903499B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161579231P 2011-12-22 2011-12-22
US61/579,231 2011-12-22
PCT/IB2012/057554 WO2013093849A1 (en) 2011-12-22 2012-12-20 Dihydro-benzo-oxazine and dihydro-pyrido-oxazine derivatives

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JP2015506344A JP2015506344A (ja) 2015-03-02
JP5903499B2 true JP5903499B2 (ja) 2016-04-13

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US (2) US9539260B2 (forum.php)
EP (1) EP2794600B1 (forum.php)
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KR (1) KR101656592B1 (forum.php)
CN (1) CN104011045B (forum.php)
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Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT2794627T (pt) 2011-12-22 2018-12-19 Janssen Biopharma Inc Nucleósidos substituídos, nucleótidos e análogos dos mesmos
HUE036953T2 (hu) 2011-12-22 2018-08-28 Novartis Ag 2,3-dihidro-benzo[1,4]oxazin-származékok és rokon vegyületek, mint foszfoinozitid-3-kináz (PI3K) inhibitorok például reumatoid arthritis kezelésére
AR089284A1 (es) 2011-12-22 2014-08-13 Galapagos Nv Dihidropirimidinoisoquinolinonas y composiciones farmaceuticas de las mismas para el tratamiento de trastornos inflamatorios
US9441007B2 (en) 2012-03-21 2016-09-13 Alios Biopharma, Inc. Substituted nucleosides, nucleotides and analogs thereof
USRE48171E1 (en) 2012-03-21 2020-08-25 Janssen Biopharma, Inc. Substituted nucleosides, nucleotides and analogs thereof
TW201422625A (zh) * 2012-11-26 2014-06-16 Novartis Ag 二氫－吡啶并－□衍生物之固體形式
SI2928896T1 (sl) * 2012-11-26 2017-10-30 Novartis Ag Trdna oblika derivata dihidro-pirido-oksazina
CN105541698B (zh) * 2015-12-23 2018-07-10 滨海康杰化学有限公司 一种5-溴-2-三氟甲基吡啶的制备方法
GB2550437B (en) * 2016-05-20 2021-06-23 Bugworks Res Inc Heterocyclic compounds useful as anti-bacterial agents and method for production
MX2020006614A (es) * 2017-12-22 2020-11-06 Ravenna Pharmaceuticals Inc Derivados de cromenopiridina como inhibidores de fosfatidilinositol fosfato cinasa,.
AU2019322538B2 (en) 2018-08-13 2021-09-30 F. Hoffmann-La Roche Ag New heterocyclic compounds as monoacylglycerol lipase inhibitors
KR20210100612A (ko) 2018-12-06 2021-08-17 다이이찌 산쿄 가부시키가이샤 시클로알칸-1,3-디아민 유도체
TW202112784A (zh) 2019-06-17 2021-04-01 美商佩特拉製藥公司 作為磷脂酸肌醇磷酸激酶抑制劑之𠳭唏并嘧啶衍生物
CR20220104A (es) 2019-09-12 2022-04-20 Hoffmann La Roche Compuestos de 4,4a,5,7,8,8a-hexapirido[4,3-b][1,4]oxazin-3-ona como inhibidores de magl
CN114728988B (zh) * 2019-11-20 2024-12-10 豪夫迈·罗氏有限公司 用于治疗自身免疫性疾病的螺(异苯并呋喃氮杂环丁烷)化合物
US11407712B2 (en) * 2020-03-19 2022-08-09 Arcus Biosciences, Inc. Tetralin and tetrahydroquinoline compounds as inhibitors of HIF-2α
ES2982017T3 (es) 2020-07-15 2024-10-14 Chiesi Farm Spa Derivados de pirido-oxazina como inhibidores de ALK5
JP2025509154A (ja) 2022-03-08 2025-04-11 エクアシールド メディカル リミテッド ロボット医薬品調製システムにおける流体移送ステーション
CN116535436B (zh) * 2023-05-06 2024-04-30 遵义医科大学 一种氟离子荧光探针及其合成方法和应用
WO2025099111A1 (en) * 2023-11-10 2025-05-15 Wella Germany Gmbh New telescoping syntheses of 6-hydroxy-benzomorpholine (3,4-dihydro-2h-1,4-benzoxazin-6-ol)

Family Cites Families (79)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1524747A (en) 1976-05-11 1978-09-13 Ici Ltd Polypeptide
LU88769I2 (fr) 1982-07-23 1996-11-05 Zeneca Ltd Bicalutamide et ses sels et esters pharmaceutiquement acceptables (Casodex (R))
GB8327256D0 (en) 1983-10-12 1983-11-16 Ici Plc Steroid derivatives
US5093330A (en) 1987-06-15 1992-03-03 Ciba-Geigy Corporation Staurosporine derivatives substituted at methylamino nitrogen
US5010099A (en) 1989-08-11 1991-04-23 Harbor Branch Oceanographic Institution, Inc. Discodermolide compounds, compositions containing same and method of preparation and use
TW224941B (forum.php) 1989-11-08 1994-06-11 Yamanouchi Pharma Co Ltd
NZ243082A (en) 1991-06-28 1995-02-24 Ici Plc 4-anilino-quinazoline derivatives; pharmaceutical compositions, preparatory processes, and use thereof
GB9300059D0 (en) 1992-01-20 1993-03-03 Zeneca Ltd Quinazoline derivatives
TW225528B (forum.php) 1992-04-03 1994-06-21 Ciba Geigy Ag
GB9309716D0 (en) 1993-05-12 1993-06-23 Zeneca Ltd Heterocyclic derivatives
GB9314893D0 (en) 1993-07-19 1993-09-01 Zeneca Ltd Quinazoline derivatives
WO1996030347A1 (en) 1995-03-30 1996-10-03 Pfizer Inc. Quinazoline derivatives
GB9508538D0 (en) 1995-04-27 1995-06-14 Zeneca Ltd Quinazoline derivatives
US5747498A (en) 1996-05-28 1998-05-05 Pfizer Inc. Alkynyl and azido-substituted 4-anilinoquinazolines
US5843901A (en) 1995-06-07 1998-12-01 Advanced Research & Technology Institute LHRH antagonist peptides
SI9620103A (sl) 1995-07-06 1998-10-31 Novartis Ag Pirolopirimidini in postopki za njihovo pripravo
US5760041A (en) 1996-02-05 1998-06-02 American Cyanamid Company 4-aminoquinazoline EGFR Inhibitors
GB9603095D0 (en) 1996-02-14 1996-04-10 Zeneca Ltd Quinazoline derivatives
JP3370340B2 (ja) 1996-04-12 2003-01-27 ワーナー―ランバート・コンパニー チロシンキナーゼの不可逆的阻害剤
AU2912997A (en) 1996-06-24 1998-01-14 Pfizer Inc. Phenylamino-substituted tricyclic derivatives for treatment of hyperproliferative diseases
JP2001500851A (ja) 1996-08-30 2001-01-23 ノバルティス アクチエンゲゼルシャフト エポシロンの製造法および製造過程中に得られる中間生産物
EP0938597B1 (en) 1996-09-06 2003-08-20 Obducat Aktiebolag Method for anisotropic etching of structures in conducting materials
WO1998010767A2 (en) 1996-09-13 1998-03-19 Sugen, Inc. Use of quinazoline derivatives for the manufacture of a medicament in the treatment of hyperproliferative skin disorders
EP0837063A1 (en) 1996-10-17 1998-04-22 Pfizer Inc. 4-Aminoquinazoline derivatives
ES2312695T3 (es) 1996-11-18 2009-03-01 Gesellschaft Fur Biotechnologische Forschung Mbh (Gbf) Epotilones e y f.
US6441186B1 (en) 1996-12-13 2002-08-27 The Scripps Research Institute Epothilone analogs
CO4940418A1 (es) 1997-07-18 2000-07-24 Novartis Ag Modificacion de cristal de un derivado de n-fenil-2- pirimidinamina, procesos para su fabricacion y su uso
GB9721069D0 (en) 1997-10-03 1997-12-03 Pharmacia & Upjohn Spa Polymeric derivatives of camptothecin
US6194181B1 (en) 1998-02-19 2001-02-27 Novartis Ag Fermentative preparation process for and crystal forms of cytostatics
MXPA00008365A (es) 1998-02-25 2002-11-07 Sloan Kettering Inst Cancer Sintesis de epotilonas, intermediarios y analogos de las mismas.
BR9912938B1 (pt) 1998-08-11 2011-06-28 derivados de isoquinolina, composição que os compreende, processo para preparação e uso dos mesmos.
JP4662635B2 (ja) 1998-11-20 2011-03-30 コーサン バイオサイエンシーズ， インコーポレイテッド エポチロンおよびエポチロン誘導体を生成するための組換え方法および材料
WO2000039103A1 (en) 1998-12-23 2000-07-06 Aventis Pharma Limited Dihydro-benzo(1,4)oxazines and tetrahydroquinoxalines
NZ517575A (en) 1999-09-30 2004-04-30 Neurogen Corp Certain alkylene diamine-substituted heterocycles
EP1255743A1 (en) 2000-02-01 2002-11-13 Millenium Pharmaceuticals, Inc. 3,4-DIHYDRO-2H-BENZO[1,4]OXAZINE INHIBITORS OF FACTOR Xa
PE20020354A1 (es) 2000-09-01 2002-06-12 Novartis Ag Compuestos de hidroxamato como inhibidores de histona-desacetilasa (hda)
CN1253449C (zh) 2000-11-07 2006-04-26 诺瓦提斯公司 作为蛋白激酶c抑制剂的吲哚基马来酰亚胺衍生物
WO2002072049A1 (fr) 2001-02-27 2002-09-19 Yamanouchi Pharmaceutical Co., Ltd. Compositions medicamenteuses servant a stimuler la croissance capillaire
TWI238824B (en) 2001-05-14 2005-09-01 Novartis Ag 4-amino-5-phenyl-7-cyclobutyl-pyrrolo[2,3-d]pyrimidine derivatives
GB0119249D0 (en) 2001-08-07 2001-10-03 Novartis Ag Organic compounds
TWI324064B (en) 2002-04-03 2010-05-01 Novartis Ag Indolylmaleimide derivatives
BR0316386A (pt) 2002-12-06 2005-09-27 Warner Lambert Co Benzoxazin-3-onas e seus derivados como inibidores de p13k
CN1747729A (zh) 2002-12-09 2006-03-15 得克萨斯系统大学董事会 Janus酪氨酸激酶3(JAK3)的选择性抑制方法
EP1581529A1 (en) * 2002-12-20 2005-10-05 Warner-Lambert Company Benzoxazines and derivatives thereof as inhibitors of pi3ks
EP1631260A2 (en) 2003-02-28 2006-03-08 Transform Pharmaceuticals, Inc. Pharmaceutical co-crystal compositions of drugs such as carbamazepine, celecoxib, olanzapine, itraconazole, topiramate, modafinil, 5-fluorouracil, hydrochlorothazide, acetaminophen, aspirin, flurbiprofen, phenytoin and ibuprofen
ATE430139T1 (de) 2003-04-03 2009-05-15 Merck Patent Gmbh Pyrrolidin-1,2-dicarbonsäure-1-(phenylamid)-2-( - (3-oxo-morpholin-4-yl)-phenylamid) derivate und verwandte verbindungen als inhibitoren des koagulationsfaktors xa zur behandlung von thromboembolischen erkrankungen
AU2004283313A1 (en) 2003-10-24 2005-05-06 Exelixis, Inc. TAO kinase modulators and methods of use
GB2432834A (en) 2004-01-12 2007-06-06 Cytopia Res Pty Ltd Selective Kinase Inhibitors
EP2314585B1 (en) 2004-07-15 2012-09-12 Japan Tobacco, Inc. Condensed benzamide compounds as inhibitors of vanilloid receptor subtype 1 (VR1) activity
DE102004045796A1 (de) 2004-09-22 2006-03-23 Merck Patent Gmbh Arzneimittel enthaltend Carbonylverbindungen sowie deren Verwendung
DE102004047254A1 (de) 2004-09-29 2006-04-13 Merck Patent Gmbh Carbonylverbindungen
BRPI0517416A (pt) 2004-10-12 2008-10-07 Serono Lab inibidores de pi3 quinase gama para o tratamento de anemia
US20080269204A1 (en) 2004-11-01 2008-10-30 Tatyana Dyakonov Compounds and Methods of Use Thereof
US20060161001A1 (en) 2004-12-20 2006-07-20 Amgen Inc. Substituted heterocyclic compounds and methods of use
GB0510390D0 (en) 2005-05-20 2005-06-29 Novartis Ag Organic compounds
UA96736C2 (ru) * 2005-09-07 2011-12-12 Мерк Сероно Са Ингибиторы pi3k для лечения эндометриоза
TWI385161B (zh) 2006-02-02 2013-02-11 Mitsubishi Tanabe Pharma Corp 含氮雜雙環化合物
EP2035436B1 (en) 2006-06-26 2011-05-25 UCB Pharma S.A. Fused thiazole derivatives as kinase inhibitors
GB0620059D0 (en) * 2006-10-10 2006-11-22 Ucb Sa Therapeutic agents
NZ576278A (en) 2006-10-19 2011-12-22 Signal Pharm Llc Heteroaryl compounds, compositions thereof, and their use as protein kinase inhibitors
US8173647B2 (en) 2007-02-06 2012-05-08 Gordana Atallah PI 3-kinase inhibitors and methods of their use
US20080221095A1 (en) 2007-03-07 2008-09-11 Christian Gege Metalloprotease inhibitors containing a heterocyclic moiety
US9603848B2 (en) 2007-06-08 2017-03-28 Senomyx, Inc. Modulation of chemosensory receptors and ligands associated therewith
US20110263569A1 (en) 2007-08-22 2011-10-27 President And Fellows Of Harvard College Ryanodine channel binders and uses thereof
WO2009071895A1 (en) 2007-12-04 2009-06-11 Ucb Pharma S.A. Fused thiazole and thiophene derivatives as kinase inhibitors
US20110130384A1 (en) 2008-06-25 2011-06-02 Takeda Pharmaceutical Company Limited Amide compound
EP2341052A4 (en) 2008-09-05 2011-10-12 Shionogi & Co RING-CONDENSED MORPHOLINE DERIVATIVITY WITH PI3K-INHIBITING EFFECT
US20100152160A1 (en) 2008-12-12 2010-06-17 Khamrai Uttam Novel benzodioxane and benzoxazine derivatives useful as cc chemokine receptor ligands
EP2415767B1 (en) 2009-03-27 2014-09-03 Takeda Pharmaceutical Company Limited Poly (ADP-ribose) Polymerase (PARP) Inhibitors
WO2010117425A1 (en) 2009-03-31 2010-10-14 Biogen Idec Ma Inc. Certain substituted pyrimidines, pharmaceutical compositions thereof, and methods for their use
US8765940B2 (en) * 2009-06-25 2014-07-01 Amgen Inc. Heterocyclic compounds and their uses
EP2569302A1 (en) 2010-05-13 2013-03-20 Amgen, Inc Heteroaryloxyheterocyclyl compounds as pde10 inhibitors
UA112517C2 (uk) 2010-07-06 2016-09-26 Новартіс Аг Тетрагідропіридопіримідинові похідні
KR20120018236A (ko) 2010-07-23 2012-03-02 현대약품 주식회사 치환된 피리미디닐 유도체 및 이의 제조방법
WO2012068096A2 (en) 2010-11-15 2012-05-24 Exelixis, Inc. Benzoxazepines as inhibitors of pi3k/mtor and methods of their use and manufacture
EP2640367A2 (en) 2010-11-15 2013-09-25 Exelixis, Inc. Benzoxazepines as inhibitors of pi3k/mtor and methods of their use and manufacture
CN102731525A (zh) * 2011-04-08 2012-10-17 上海艾力斯医药科技有限公司 苯并吗啉衍生物
HUE036953T2 (hu) 2011-12-22 2018-08-28 Novartis Ag 2,3-dihidro-benzo[1,4]oxazin-származékok és rokon vegyületek, mint foszfoinozitid-3-kináz (PI3K) inhibitorok például reumatoid arthritis kezelésére
TW201422625A (zh) 2012-11-26 2014-06-16 Novartis Ag 二氫－吡啶并－□衍生物之固體形式

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