JP5475778B2 - 腫瘍の治療のための二環式トリアゾール誘導体 - Google Patents

腫瘍の治療のための二環式トリアゾール誘導体 Download PDF

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Publication number
JP5475778B2
JP5475778B2 JP2011522392A JP2011522392A JP5475778B2 JP 5475778 B2 JP5475778 B2 JP 5475778B2 JP 2011522392 A JP2011522392 A JP 2011522392A JP 2011522392 A JP2011522392 A JP 2011522392A JP 5475778 B2 JP5475778 B2 JP 5475778B2
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het
hal
atoms
mmol
proportions
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JP2011522392A
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Japanese (ja)
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JP2011530545A (ja
JP2011530545A5 (enExample
Inventor
スティーバー,フランク
シャット,オリバー
ドルシュ,ディーター
ブラウカット,アンドレ
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Merck Patent GmbH
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Merck Patent GmbH
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2011522392A 2008-08-14 2009-07-16 腫瘍の治療のための二環式トリアゾール誘導体 Expired - Fee Related JP5475778B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DE102008037790A DE102008037790A1 (de) 2008-08-14 2008-08-14 Bicyclische Triazolderivate
DE102008037790.2 2008-08-14
PCT/EP2009/005172 WO2010017870A1 (de) 2008-08-14 2009-07-16 Bicyclische triazolderivate zur behandlung von tumoren

Publications (3)

Publication Number Publication Date
JP2011530545A JP2011530545A (ja) 2011-12-22
JP2011530545A5 JP2011530545A5 (enExample) 2012-08-30
JP5475778B2 true JP5475778B2 (ja) 2014-04-16

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
JP2011522392A Expired - Fee Related JP5475778B2 (ja) 2008-08-14 2009-07-16 腫瘍の治療のための二環式トリアゾール誘導体

Country Status (16)

Country Link
US (1) US8435986B2 (enExample)
EP (1) EP2310013B1 (enExample)
JP (1) JP5475778B2 (enExample)
KR (1) KR20110051243A (enExample)
CN (1) CN102123710B (enExample)
AR (1) AR073055A1 (enExample)
AU (1) AU2009281491B2 (enExample)
BR (1) BRPI0914555A2 (enExample)
CA (1) CA2733941C (enExample)
DE (1) DE102008037790A1 (enExample)
EA (1) EA201100334A1 (enExample)
ES (1) ES2648233T3 (enExample)
IL (1) IL211193A0 (enExample)
MX (1) MX2011001511A (enExample)
WO (1) WO2010017870A1 (enExample)
ZA (1) ZA201101899B (enExample)

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8598184B2 (en) * 2008-03-03 2013-12-03 Tiger Pharmatech Protein kinase inhibitors
PT3511330T (pt) * 2009-12-31 2020-12-24 Hutchison Medipharma Ltd Intermediário sintético útil na preparação de inibidores de triazolopiridina c-met
JP5960688B2 (ja) 2010-05-17 2016-08-02 インコゼン セラピューティクス プライベート リミテッド プロテインキナーゼ調節物質としての新規3,5−二置換−3h−[1,2,3]トリアゾロ[4,5−b]ピリジン化合物
EA201300389A1 (ru) * 2010-09-23 2013-09-30 Бёрингер Ингельхайм Интернациональ Гмбх Оксадиазольные ингибиторы продуцирования лейкотриена
AU2013402175B2 (en) * 2013-09-30 2017-09-07 Handok Inc. Novel triazolopyrazine derivative and use thereof
EP3722277A3 (en) * 2013-10-04 2021-01-20 Novartis AG 3'end caps for rna-interferring agents for use in rna
WO2015050871A2 (en) 2013-10-04 2015-04-09 Novartis Ag Organic compounds to treat hepatitis b virus
GB201321740D0 (en) * 2013-12-09 2014-01-22 Ucb Pharma Sa Therapeutic agents
KR102379517B1 (ko) * 2013-12-30 2022-03-25 제넨테크, 인크. 세린/트레오닌 키나아제 억제제
US9815850B2 (en) 2016-02-05 2017-11-14 Denali Therapeutics Inc. Compounds, compositions and methods
LT3552017T (lt) 2016-12-09 2022-05-10 Denali Therapeutics Inc. Junginiai, naudotini kaip ripk1 inhibitoriai
KR20180092096A (ko) 2017-02-08 2018-08-17 에이비온 주식회사 트리아졸로 피라진 유도체의 신규한 다형체 및 이의 제조 방법
CN108570053A (zh) * 2017-03-13 2018-09-25 中国科学院上海药物研究所 五元并六元杂环化合物、制备方法、中间体、组合和应用
BR102018007822A2 (pt) 2017-04-20 2018-11-06 Gilead Sciences, Inc. composto, métodos para inibir pd-1, pd-l1 e/ou interação de pd-1/pd-l1 e para tratamento de câncer, composição farmacêutica, e, kit para tratamento de ou prevenção de câncer ou uma doença ou condição
WO2019160882A1 (en) 2018-02-13 2019-08-22 Gilead Sciences, Inc. Pd-1/pd-l1 inhibitors
KR102591947B1 (ko) 2018-04-19 2023-10-25 길리애드 사이언시즈, 인코포레이티드 Pd-1/pd-l1 억제제
PE20210642A1 (es) 2018-07-13 2021-03-23 Gilead Sciences Inc Inhibidores de pd-1/pd-l1
US11236085B2 (en) 2018-10-24 2022-02-01 Gilead Sciences, Inc. PD-1/PD-L1 inhibitors
EP4463229A1 (en) 2022-01-12 2024-11-20 Denali Therapeutics Inc. Crystalline forms of (s)-5-benzyl-n-(5-methyl-4-oxo-2, 3,4,5- tetrahydropyrido [3,2-b] [l,4]oxazepin-3-yl)-4h-l,2,4-triazole-3-carboxamide

Family Cites Families (46)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9624482D0 (en) 1995-12-18 1997-01-15 Zeneca Phaema S A Chemical compounds
DE19604388A1 (de) 1996-02-07 1997-08-14 Merck Patent Gmbh Arylalkyl-diazinone
CA2242425C (en) 1996-02-13 2006-07-18 Zeneca Limited Quinazoline derivatives as vegf inhibitors
NZ331191A (en) 1996-03-05 2000-03-27 Zeneca Ltd 4-anilinoquinazoline derivatives and pharmaceutical compositions thereof
GB9718972D0 (en) 1996-09-25 1997-11-12 Zeneca Ltd Chemical compounds
JPH10259176A (ja) 1997-03-17 1998-09-29 Japan Tobacco Inc 血管新生阻害作用を有する新規アミド誘導体及びその用途
GB9714249D0 (en) 1997-07-08 1997-09-10 Angiogene Pharm Ltd Vascular damaging agents
TWI241295B (en) 1998-03-02 2005-10-11 Kowa Co Pyridazine derivative and medicine containing the same as effect component
GB9900334D0 (en) 1999-01-07 1999-02-24 Angiogene Pharm Ltd Tricylic vascular damaging agents
GB9900752D0 (en) 1999-01-15 1999-03-03 Angiogene Pharm Ltd Benzimidazole vascular damaging agents
AUPQ462299A0 (en) 1999-12-13 2000-01-13 Fujisawa Pharmaceutical Co., Ltd. Pyrazolopyridine compound and pharmaceutical use thereof
US6242461B1 (en) 2000-01-25 2001-06-05 Pfizer Inc. Use of aryl substituted azabenzimidazoles in the treatment of HIV and AIDS related diseases
BR0111230A (pt) 2000-05-31 2003-06-10 Astrazeneca Ab Composto, e, uso e processo para a preparação do mesmo
EE200300015A (et) 2000-07-07 2004-10-15 Angiogene Pharmaceuticals Limited Kolhinooli derivaadid kui angiogeneesi inhibiitorid
KR20030014425A (ko) 2000-07-07 2003-02-17 앤지오젠 파마슈티칼스 리미티드 혈관 손상제인 콜치놀 유도체
MXPA04003668A (es) 2001-10-31 2004-07-22 Merck Patent Gmbh Inhibidores de fosfodiesteresa de tipo 4 y usos de los mismos.
DE10228103A1 (de) 2002-06-24 2004-01-15 Bayer Cropscience Ag Fungizide Wirkstoffkombinationen
BR0317430A (pt) 2002-12-20 2005-10-25 Pharmacia Corp Compostos inibidores de quinase-2 de proteìna ativada por quinase de proteìna ativada por mitógeno
US7563748B2 (en) 2003-06-23 2009-07-21 Cognis Ip Management Gmbh Alcohol alkoxylate carriers for pesticide active ingredients
JP2007516180A (ja) * 2003-07-02 2007-06-21 スゲン,インコーポレイティド c−Met阻害薬としてのアリールメチルトリアゾロおよびイミダゾピラジン類
US7959919B2 (en) * 2003-11-19 2011-06-14 Novelmed Therapeutics, Inc. Method of inhibiting factor B-mediated complement activation
EP1769092A4 (en) 2004-06-29 2008-08-06 Europ Nickel Plc IMPROVED LIXIVIATION OF BASE METALS
US20070015771A1 (en) * 2004-07-29 2007-01-18 Threshold Pharmaceuticals, Inc. Lonidamine analogs
US20070043057A1 (en) * 2005-02-09 2007-02-22 Threshold Pharmaceuticals, Inc. Lonidamine analogs
TW200612918A (en) * 2004-07-29 2006-05-01 Threshold Pharmaceuticals Inc Lonidamine analogs
ATE498358T1 (de) 2005-06-29 2011-03-15 Compumedics Ltd Sensoranordnung mit leitfähiger brücke
US7728017B2 (en) 2005-11-30 2010-06-01 Vertex Pharmaceuticals Incorporated Inhibitors of c-Met and uses thereof
DE102005057924A1 (de) 2005-12-05 2007-06-06 Merck Patent Gmbh Pyridazinonderivate
RS55630B1 (sr) 2005-12-21 2017-06-30 Janssen Pharmaceutica Nv Triazolopiridazini kao modulatori tirozin kinaze
NL2000613C2 (nl) 2006-05-11 2007-11-20 Pfizer Prod Inc Triazoolpyrazinederivaten.
CA2651979A1 (en) 2006-05-30 2007-12-06 Pfizer Products Inc. Triazolopyridazine derivatives
TW200801513A (en) 2006-06-29 2008-01-01 Fermiscan Australia Pty Ltd Improved process
PE20121506A1 (es) 2006-07-14 2012-11-26 Amgen Inc Compuestos triazolopiridinas como inhibidores de c-met
WO2008033455A2 (en) * 2006-09-13 2008-03-20 The Institutes For Pharmaceutical Discovery, Llc Biphenyl and heteroaryl phenyl derivatives as protein tyrosine phosphatases inhibitors
EA016527B1 (ru) 2006-10-23 2012-05-30 ЭсДжиЭкс ФАРМАСЬЮТИКАЛЗ, ИНК. Триазолопиридазиновые модуляторы протеинкиназ
DE102007026341A1 (de) 2007-06-06 2008-12-11 Merck Patent Gmbh Benzoxazolonderivate
DE102007032507A1 (de) 2007-07-12 2009-04-02 Merck Patent Gmbh Pyridazinonderivate
JP5423679B2 (ja) 2007-10-31 2014-02-19 日産化学工業株式会社 ピリダジノン化合物及びp2x7受容体阻害剤
DE102007061963A1 (de) 2007-12-21 2009-06-25 Merck Patent Gmbh Pyridazinonderivate
CN101538245B (zh) 2008-03-18 2011-02-16 中国科学院上海药物研究所 一类哒嗪酮类化合物及其制备方法和制备药物的用途
DE102008019907A1 (de) 2008-04-21 2009-10-22 Merck Patent Gmbh Pyridazinonderivate
EP2328586A2 (en) 2008-05-20 2011-06-08 Cephalon, Inc. Substituted pyridazinone derivatives as histamine-3 (h3) receptor ligands
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
CA2729993A1 (en) 2008-07-25 2010-01-28 Boehringer Ingelheim International Gmbh Synthesis of inhibitors of 11beta-hydroxysteroid dehydrogenase type 1
BRPI1013159A2 (pt) 2009-03-30 2015-09-15 Sumitomo Chemical Co Uso de composto de piridazinona para controle de peste artrópode
AR082590A1 (es) 2010-08-12 2012-12-19 Hoffmann La Roche Inhibidores de la tirosina-quinasa de bruton

Also Published As

Publication number Publication date
MX2011001511A (es) 2011-03-15
CA2733941C (en) 2016-10-04
AU2009281491A1 (en) 2010-02-18
JP2011530545A (ja) 2011-12-22
IL211193A0 (en) 2011-04-28
CN102123710A (zh) 2011-07-13
BRPI0914555A2 (pt) 2015-12-15
DE102008037790A1 (de) 2010-02-18
AR073055A1 (es) 2010-10-13
US8435986B2 (en) 2013-05-07
ZA201101899B (en) 2011-11-30
HK1159989A1 (en) 2012-08-10
EP2310013A1 (de) 2011-04-20
US20110135600A1 (en) 2011-06-09
ES2648233T3 (es) 2017-12-29
AU2009281491B2 (en) 2014-02-20
KR20110051243A (ko) 2011-05-17
CN102123710B (zh) 2012-11-07
EA201100334A1 (ru) 2011-08-30
CA2733941A1 (en) 2010-02-18
EP2310013B1 (de) 2017-08-23
WO2010017870A1 (de) 2010-02-18

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