CN101379060B - 作为Aurora激酶抑制剂的苯并唑系衍生物、组合物和使用方法 - Google Patents

作为Aurora激酶抑制剂的苯并唑系衍生物、组合物和使用方法 Download PDF

Info

Publication number
CN101379060B
CN101379060B CN2007800047858A CN200780004785A CN101379060B CN 101379060 B CN101379060 B CN 101379060B CN 2007800047858 A CN2007800047858 A CN 2007800047858A CN 200780004785 A CN200780004785 A CN 200780004785A CN 101379060 B CN101379060 B CN 101379060B
Authority
CN
China
Prior art keywords
indazol
carboxylic acid
benzimidazole
mmol
amide
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.)
Expired - Fee Related
Application number
CN2007800047858A
Other languages
English (en)
Chinese (zh)
Other versions
CN101379060A (zh
Inventor
A·M·M·米加里
B·S·格雷拉
G·苏布拉马尼安
M·N·阿里米里
R·高伯拉斯瓦米
R·C·安德鲁斯
S·戴维斯
郭晓川
J·朱
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.)
vTv Therapeutics LLC
Original Assignee
Trans Tech Pharma Inc
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
Application filed by Trans Tech Pharma Inc filed Critical Trans Tech Pharma Inc
Publication of CN101379060A publication Critical patent/CN101379060A/zh
Application granted granted Critical
Publication of CN101379060B publication Critical patent/CN101379060B/zh
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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 three or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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 chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CN2007800047858A 2006-02-10 2007-02-09 作为Aurora激酶抑制剂的苯并唑系衍生物、组合物和使用方法 Expired - Fee Related CN101379060B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US77249706P 2006-02-10 2006-02-10
US60/772,497 2006-02-10
US79118706P 2006-04-11 2006-04-11
US60/791,187 2006-04-11
PCT/US2007/003579 WO2007095124A2 (en) 2006-02-10 2007-02-09 Benzazole derivatives, compositions, and methods of use as aurora kinase inhibitors

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CN2012101215887A Division CN102633783A (zh) 2006-02-10 2007-02-09 作为Aurora激酶抑制剂的苯并唑系衍生物、组合物和使用方法

Publications (2)

Publication Number Publication Date
CN101379060A CN101379060A (zh) 2009-03-04
CN101379060B true CN101379060B (zh) 2012-05-23

Family

ID=38157823

Family Applications (2)

Application Number Title Priority Date Filing Date
CN2012101215887A Pending CN102633783A (zh) 2006-02-10 2007-02-09 作为Aurora激酶抑制剂的苯并唑系衍生物、组合物和使用方法
CN2007800047858A Expired - Fee Related CN101379060B (zh) 2006-02-10 2007-02-09 作为Aurora激酶抑制剂的苯并唑系衍生物、组合物和使用方法

Family Applications Before (1)

Application Number Title Priority Date Filing Date
CN2012101215887A Pending CN102633783A (zh) 2006-02-10 2007-02-09 作为Aurora激酶抑制剂的苯并唑系衍生物、组合物和使用方法

Country Status (9)

Country Link
US (2) US7820821B2 (OSRAM)
EP (2) EP1987028A2 (OSRAM)
JP (1) JP5188988B2 (OSRAM)
CN (2) CN102633783A (OSRAM)
AU (1) AU2007215247B2 (OSRAM)
BR (1) BRPI0708034A2 (OSRAM)
CA (1) CA2641744C (OSRAM)
IL (1) IL192580A0 (OSRAM)
WO (1) WO2007095124A2 (OSRAM)

Families Citing this family (66)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2006223070B2 (en) * 2005-03-14 2012-02-09 High Point Pharmaceuticals, Llc Benzazole derivatives, compositions, and methods of use as B-secretase inhibitors
DK1976828T3 (en) 2005-12-29 2017-03-06 Celtaxsys Inc DIAMINE DERIVATIVES AS INhibitors of Leukotriene A4 HYDROLASE
WO2009064835A1 (en) * 2007-11-16 2009-05-22 Incyte Corporation 4-pyrazolyl-n-arylpyrimidin-2-amines and 4-pyrazolyl-n-heteroarylpyrimidin-2-amines as janus kinase inhibitors
WO2009084008A1 (en) * 2007-12-28 2009-07-09 Cadila Healthcare Limited Process for preparing mycophenolate mofetil
EP2303841A1 (en) 2008-07-14 2011-04-06 Gilead Sciences, Inc. Oxindolyl inhibitor compounds
UY32138A (es) * 2008-09-25 2010-04-30 Boehringer Ingelheim Int Amidas sustituidas del ácido 2-(2,6-dicloro-fenilamino)-6-fluoro-1-metil-1h-bencimidazol-5-carboxílico y sus sales farmacéuticamente aceptables
AU2009296820B2 (en) 2008-09-26 2014-03-20 Merck Sharp & Dohme Llc Novel cyclic benzimidazole derivatives useful anti-diabetic agents
US8410284B2 (en) 2008-10-22 2013-04-02 Merck Sharp & Dohme Corp Cyclic benzimidazole derivatives useful as anti-diabetic agents
US8563746B2 (en) 2008-10-29 2013-10-22 Merck Sharp & Dohme Corp Cyclic benzimidazole derivatives useful as anti-diabetic agents
US8329914B2 (en) 2008-10-31 2012-12-11 Merck Sharp & Dohme Corp Cyclic benzimidazole derivatives useful as anti-diabetic agents
JP5738196B2 (ja) * 2008-12-22 2015-06-17 ミレニアム ファーマシューティカルズ, インコーポレイテッドMillennium Pharmaceuticals, Inc. オーロラキナーゼ阻害剤および抗cd20抗体の併用
UY32470A (es) 2009-03-05 2010-10-29 Boehringer Ingelheim Int Derivados de 2-{2-cloro-5-[(sustituido) metil]fenilamino} -1-metil]fenilamino}-1-metilbencimidazol-5-carboxamidas-n-(sustituidas) y sus sales fisiológicamente aceptables, composiciones conteniéndolos y aplicaciones
US8283357B2 (en) 2009-06-08 2012-10-09 Gilead Sciences, Inc. Cycloalkylcarbamate benzamide aniline HDAC inhibitor compounds
KR20120031170A (ko) 2009-06-08 2012-03-30 길리애드 사이언시즈, 인코포레이티드 알카노일아미노 벤즈아미드 아닐린 hdac 저해제 화합물
US9125901B2 (en) 2009-06-23 2015-09-08 The Translational Genomics Research Institute 4-(benzimidazol-2-ylamino)benzamide derivatives and salts or solvates thereof
JP2013506686A (ja) 2009-09-30 2013-02-28 プレジデント アンド フェロウズ オブ ハーバード カレッジ オートファジー阻害遺伝子産物の変調によりオートファジーを変調する方法
US8759535B2 (en) 2010-02-18 2014-06-24 High Point Pharmaceuticals, Llc Substituted fused imidazole derivatives, pharmaceutical compositions, and methods of use thereof
DK2536285T3 (en) 2010-02-18 2018-07-16 Vtv Therapeutics Llc Substituted fused imidazole derivatives, pharmaceutical compositions and methods for their use
JP2013520502A (ja) 2010-02-25 2013-06-06 メルク・シャープ・エンド・ドーム・コーポレイション 有用な抗糖尿病薬である新規な環状ベンズイミダゾール誘導体
US8586604B2 (en) 2010-08-20 2013-11-19 Boehringer Ingelheim International Gmbh Inhibitors of the microsomal prostaglandin E2 synthase-1
US8759537B2 (en) * 2010-08-20 2014-06-24 Boehringer Ingelheim International Gmbh 3H-imidazo [4, 5-C] pyridine-6-carboxamides as anti-inflammatory agents
US8466186B2 (en) 2010-12-10 2013-06-18 Boehringer Ingelheim International Gmbh Compounds
US8674113B2 (en) 2010-12-10 2014-03-18 Boehringer Ingelheim International Gmbh Compounds
US8486968B2 (en) 2010-12-10 2013-07-16 Boehringer Ingelheim International Gmbh Compounds
US9290489B2 (en) 2012-07-06 2016-03-22 Duke University Activation of TRPV4 ion channel by physical stimuli and critical role for TRPV4 in organ-specific inflammation and itch
CA2894536C (en) 2012-12-18 2020-07-28 Vertex Pharmaceuticals Incorporated Mannose derivatives for treating bacterial infections
JP6527851B2 (ja) 2013-03-12 2019-06-05 セルタクシス,インコーポレイテッド ロイコトリエンa4加水分解酵素を阻害する方法
AU2014248717B2 (en) 2013-03-12 2018-03-29 Vertex Pharmaceuticals Incorporated Mannose derivatives for treating bacterial infections
MX2015011676A (es) 2013-03-14 2016-04-25 Celtaxsys Inc Inhibidores de leucotrieno a4 hidrolasa.
EP2970309A4 (en) 2013-03-14 2016-11-09 Celtaxsys Inc INHIBITORS OF LEUCOTRIENE A4 HYDROLASE
MX2015011677A (es) 2013-03-14 2016-07-08 Celtaxsys Inc Inhibidores de leucotrieno a4 hidrolasa.
WO2014193696A2 (en) 2013-05-28 2014-12-04 Transtech Pharma, Llc Benzimidazole carboxylic acid derivatives, compositions, and methods of use as aurora kinase inhibitors
TWI667233B (zh) 2013-12-19 2019-08-01 德商拜耳製藥公司 新穎吲唑羧醯胺,其製備方法、含彼等之醫藥製劑及其製造醫藥之用途
JP2017505337A (ja) 2014-01-10 2017-02-16 アウリジーン ディスカバリー テクノロジーズ リミテッド Irak4阻害剤としてのインダゾール化合物
PL3805233T3 (pl) 2014-01-13 2024-06-10 Aurigene Oncology Limited ENANCJOMERY (R) I (S) (S)-N-(5-(3-hydroksypirolidyn-1-ylo)-2-morfolinooksazolo[4,5-b]pirydyn-6-ylo)-2-(2-metylopirydyn-4-ylo)oksazolo-4-karboksyamidu jako inhibitory IRAK4 do leczenia nowotworu złośliwego
CN106456609A (zh) * 2014-06-20 2017-02-22 奥瑞基尼探索技术有限公司 作为irak4抑制剂的取代的吲唑化合物
WO2016028325A1 (en) 2014-08-22 2016-02-25 Duke University Trpa1 and trpv4 inhibitors and methods of using the same for organ-specific inflammation and itch
WO2016089648A1 (en) 2014-12-01 2016-06-09 Vtv Therapeutics Llc Bach 1 inhibitors in combination with nrf2 activators and pharmaceutical compositions thereof
US11229628B2 (en) 2015-01-09 2022-01-25 Duke University TRPA1 and TRPV4 inhibitors and methods of using the same for organ-specific inflammation and itch
AU2016267059B2 (en) * 2015-05-22 2020-08-13 Translational Drug Development Llc Benzamide and active compound compositions and methods of use
ES2824450T3 (es) 2015-06-22 2021-05-12 Actelion Pharmaceuticals Ltd Compuestos de benzoxazol y de benzotiazol 2,5-disustituidos como inhibidores de la NADPH oxidasa 4
EP3439656A4 (en) 2016-04-07 2020-03-11 Duke University DOUBLE SMALL MOLECULE INHIBITORS OF TRPV4 AND TRPA1 FOR DISINFECTION AND ANESTHESIA
CN120267671A (zh) 2017-03-31 2025-07-08 奥锐金肿瘤有限公司 用于治疗血液病的化合物和组合物
JP7241747B2 (ja) 2017-10-31 2023-03-17 キュリス,インコーポレイテッド 血液学的障害を治療するための化合物および組成物
MX2020009391A (es) * 2018-03-29 2021-01-08 Elex Biotech Inc Compuestos para el tratamiento de arritmias cardiacas e insuficiencia cardiaca.
AU2019278935B2 (en) 2018-05-31 2025-02-13 Celltaxis, Llc Method of reducing pulmonary exacerbations in respiratory disease patients
US12415816B2 (en) 2018-11-07 2025-09-16 Dana-Farber Cancer Institute, Inc. Benzothiazole derivatives and 7-aza-benzothiazole derivatives as janus kinase 2 inhibitors and uses thereof
CN109675040B (zh) * 2018-12-31 2021-07-30 清华大学 治疗乳腺癌的组合物及其应用
IL287183B2 (en) 2019-04-12 2025-01-01 Mitobridge Inc Inductors 1 HMOX
US11427558B1 (en) 2019-07-11 2022-08-30 ESCAPE Bio, Inc. Indazoles and azaindazoles as LRRK2 inhibitors
BR112022010561A2 (pt) 2019-12-02 2022-11-16 Storm Therapeutics Ltd Compostos poli-heterocíclicos como inibidores de mettl3
CN110903246A (zh) * 2019-12-19 2020-03-24 赵洁 一种用于治疗甲状腺癌的化合物及其组合物和医药用途
EP4146639A1 (en) 2020-05-06 2023-03-15 Ajax Therapeutics, Inc. 6-heteroaryloxy benzimidazoles and azabenzimidazoles as jak2 inhibitors
CN112552287B (zh) * 2020-12-16 2021-11-30 北京华氏精恒医药科技有限公司 一种吲哚类衍生物药物制剂及其制备方法
TW202241889A (zh) 2020-12-23 2022-11-01 美商雅捷可斯治療公司 作為jak2抑制劑之6-雜芳基氧基苯并咪唑及氮雜苯并咪唑
CN117120054A (zh) 2021-04-08 2023-11-24 柯里斯公司 治疗癌症的组合疗法
CN115594671B (zh) * 2021-07-08 2024-03-15 沈阳药科大学 苯并噻唑类衍生物及其制备方法和用途
WO2023086320A1 (en) 2021-11-09 2023-05-19 Ajax Therapeutics, Inc. Forms and compositions of inhibitors of jak2
JP7782035B2 (ja) 2021-11-09 2025-12-08 エイジャックス セラピューティクス, インコーポレイテッド Jak2阻害剤としての6-ヘテロアリールオキシベンゾイミダゾール及びアザベンゾイミダゾール
US12084453B2 (en) 2021-12-10 2024-09-10 Incyte Corporation Bicyclic amines as CDK12 inhibitors
WO2024229406A1 (en) 2023-05-04 2024-11-07 Revolution Medicines, Inc. Combination therapy for a ras related disease or disorder
WO2025034702A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Rmc-6291 for use in the treatment of ras protein-related disease or disorder
TW202530228A (zh) 2023-10-12 2025-08-01 美商銳新醫藥公司 Ras抑制劑
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
WO2025240847A1 (en) 2024-05-17 2025-11-20 Revolution Medicines, Inc. Ras inhibitors
WO2025255438A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder

Family Cites Families (54)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5481271A (en) 1977-12-09 1979-06-28 Ouchi Shinkou Kagaku Kougiyou Benzimidazole derivatives and manufacture
EP0178413A1 (en) * 1984-08-17 1986-04-23 Beecham Group Plc Benzimidazoles
NZ221729A (en) 1986-09-15 1989-07-27 Janssen Pharmaceutica Nv Imidazolyl methyl-substituted benzimidazole derivatives and pharmaceutical compositions
SE8604566D0 (sv) * 1986-10-27 1986-10-27 Haessle Ab Novel compunds
FR2643903A1 (fr) 1989-03-03 1990-09-07 Union Pharma Scient Appl Nouveaux derives de benzimidazole, leurs procedes de preparation, intermediaires de synthese, compositions pharmaceutiques les contenant, utiles notamment pour le traitement des maladies cardiovasculaires, et des ulceres duodenaux
US6288100B1 (en) 1995-06-06 2001-09-11 American Home Products Corporation Benzimidazole derivatives
GB9514265D0 (en) * 1995-07-13 1995-09-13 Wellcome Found Hetrocyclic compounds
WO1997011075A1 (en) 1995-09-22 1997-03-27 Takeda Chemical Industries, Ltd. Triazole compounds, their production and use
WO1997029079A1 (en) * 1996-02-06 1997-08-14 Japan Tobacco Inc. Novel compounds and pharmaceutical use thereof
WO1997048697A1 (en) * 1996-06-19 1997-12-24 Rhone-Poulenc Rorer Limited Substituted azabicylic compounds and their use as inhibitors of the production of tnf and cyclic amp phosphodiesterase
HRP970371A2 (en) 1996-07-13 1998-08-31 Kathryn Jane Smith Heterocyclic compounds
US6114532A (en) * 1998-02-03 2000-09-05 Boehringer Ingelheim Pharma Kg Bicyclic heterocycles, the preparation thereof, and their use as pharmaceuticals
FR2778662B1 (fr) * 1998-05-12 2000-06-16 Adir Nouveaux composes cycliques substitues, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
JP2000143635A (ja) 1998-06-10 2000-05-26 Takeda Chem Ind Ltd 血管新生阻害剤
JP4622020B2 (ja) * 1999-02-26 2011-02-02 住友電気工業株式会社 絶縁被膜を有する酸化物超電導線材およびその製造方法
CN1348370A (zh) 1999-04-15 2002-05-08 布里斯托尔-迈尔斯斯奎布公司 环状蛋白酪氨酸激酶抑制剂
US6326385B1 (en) * 1999-08-04 2001-12-04 Icagen, Inc. Methods for treating or preventing pain
JP2003508509A (ja) * 1999-09-04 2003-03-04 アストラゼネカ アクチボラグ ピルビン酸デヒドロゲナーゼの阻害剤としてのアミド
US6316474B1 (en) * 1999-10-29 2001-11-13 Merck & Co., Inc. 2-benzyl and 2-heteroaryl benzimidazole NMDA/NR2B antagonists
WO2001094318A2 (en) * 2000-06-05 2001-12-13 Ortho-Mcneil Pharmaceutical, Inc. Method for synthesis of substituted azole libraries
AU2002223492A1 (en) 2000-11-14 2002-05-27 Neurosearch A/S Use of malaria parasite anion channel blockers for treating malaria
WO2002053160A1 (en) * 2000-12-29 2002-07-11 Alteon, Inc. Method for treating glaucoma ivb
WO2002053101A2 (en) * 2000-12-29 2002-07-11 Alteon, Inc. Method for treating fibrotic diseases or other indications
MXPA03007765A (es) 2001-03-01 2003-12-08 Shionogi & Co Compuestos heteroarilo que contienen nitrogeno, que tienen actividad inhibitoria contra virus de inmunodeficiencia humana integrasa.
US20030109714A1 (en) * 2001-03-22 2003-06-12 Neil Wishart Transition metal mediated process
AU2002317377A1 (en) 2001-07-20 2003-03-03 Cancer Research Technology Limited Biphenyl apurinic/apyrimidinic site endonuclease inhibitors to treat cancer
FR2833948B1 (fr) * 2001-12-21 2004-02-06 Sod Conseils Rech Applic Nouveaux derives de benzimidazole et leur utilisation en tant que medicament
US20030171411A1 (en) * 2001-12-21 2003-09-11 Kodra Janos Tibor Amide derivatives as therapeutic agents
JPWO2003068753A1 (ja) * 2002-02-14 2005-06-02 小野薬品工業株式会社 N−カルバモイル窒素含有縮合環化合物およびその化合物を有効成分として含有する薬剤
MXPA04008680A (es) * 2002-02-19 2004-12-06 Pharmacia Italia Spa Derivados de pirazol triciclicos, procedimientos para su preparacion y su uso como agentes anti-tumorales.
DE10207037A1 (de) * 2002-02-20 2003-08-28 Bayer Cropscience Gmbh 2-Amino-4-bicyclyamino-6H-1,3.5-triazine, Verfahren zu deren Herstellung und deren Verwendung als Herbizide und Pflanzenwachstumsregulatoren
DK1499311T3 (da) 2002-03-29 2010-03-08 Novartis Vaccines & Diagnostic Substituerede benzaboler og anvendelse deraf som RAF-kinaseinhibitorer
US8299108B2 (en) 2002-03-29 2012-10-30 Novartis Ag Substituted benzazoles and methods of their use as inhibitors of raf kinase
WO2003082265A2 (en) * 2002-04-02 2003-10-09 Fujisawa Pharmaceutical Co Pharmaceutical composition for treating or preventing virus infectious diseases
DE10214832A1 (de) * 2002-04-04 2003-10-16 Merck Patent Gmbh Phenylderivate 4
US7135493B2 (en) 2003-01-13 2006-11-14 Astellas Pharma Inc. HDAC inhibitor
DE10306250A1 (de) * 2003-02-14 2004-09-09 Aventis Pharma Deutschland Gmbh Substituierte N-Arylheterozyklen, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
ES2337254T3 (es) * 2003-02-14 2010-04-22 Glaxo Group Limited Derivados de carboxamida.
AR043633A1 (es) * 2003-03-20 2005-08-03 Schering Corp Ligandos de receptores de canabinoides
US7531553B2 (en) * 2003-03-21 2009-05-12 Amgen Inc. Heterocyclic compounds and methods of use
EP2258365B1 (en) * 2003-03-28 2013-05-29 Novartis Vaccines and Diagnostics, Inc. Use of organic compounds for immunopotentiation
GB0311201D0 (en) * 2003-05-15 2003-06-18 Merck Sharp & Dohme Therapeutic agents
WO2004112719A2 (en) * 2003-06-19 2004-12-29 Smithkline Beecham Corporation Chemical compounds
EP1654251A4 (en) 2003-08-14 2009-03-11 Smithkline Beecham Corp CHEMICAL COMPOUNDS
WO2005035526A1 (en) 2003-10-09 2005-04-21 Argenta Discovery Ltd. Bicyclic compounds and their therapeutic use
EP1682126B1 (en) * 2003-10-16 2009-07-01 Novartis Vaccines and Diagnostics, Inc. Substituted benzazoles and use thereof as inhibitors of raf kinase
DE10349587A1 (de) * 2003-10-24 2005-05-25 Merck Patent Gmbh Benzimidazolylderivate
US7470712B2 (en) * 2004-01-21 2008-12-30 Bristol-Myers Squibb Company Amino-benzazoles as P2Y1 receptor inhibitors
WO2005090379A1 (en) 2004-03-17 2005-09-29 The Central Science Laboratory, 'csl' Compounds and sensor for detecion of polycyclic aromatic hydrocarbons
US20060019967A1 (en) * 2004-07-21 2006-01-26 Su-Ying Wu SARS CoV main protease inhibitors
US20060068998A1 (en) * 2004-09-27 2006-03-30 Fuji Photo Film Co. Ltd. Lubricant composition and triazine ring-containing compound
EP1853606B1 (en) 2005-02-10 2008-11-19 Smithkline Beecham Corporation Pyridopyrazolopyrimidine compounds and their uses as anti-cancer and anti-diabete drugs
AU2006223070B2 (en) 2005-03-14 2012-02-09 High Point Pharmaceuticals, Llc Benzazole derivatives, compositions, and methods of use as B-secretase inhibitors
ES2432361T3 (es) * 2005-12-02 2013-12-03 Bayer Healthcare, Llc Derivados de pirrolotriazina útiles para el tratamiento de cáncer por inhibición de cinasa Aurora

Also Published As

Publication number Publication date
CA2641744C (en) 2012-09-25
CN101379060A (zh) 2009-03-04
HK1125631A1 (en) 2009-08-14
JP2009526072A (ja) 2009-07-16
WO2007095124A3 (en) 2007-11-01
US20100152170A1 (en) 2010-06-17
JP5188988B2 (ja) 2013-04-24
AU2007215247A1 (en) 2007-08-23
EP2295432A1 (en) 2011-03-16
CN102633783A (zh) 2012-08-15
WO2007095124A2 (en) 2007-08-23
EP1987028A2 (en) 2008-11-05
US8377983B2 (en) 2013-02-19
CA2641744A1 (en) 2007-08-23
US7820821B2 (en) 2010-10-26
IL192580A0 (en) 2009-02-11
US20070219235A1 (en) 2007-09-20
BRPI0708034A2 (pt) 2011-05-17
AU2007215247B2 (en) 2012-12-13

Similar Documents

Publication Publication Date Title
CN101379060B (zh) 作为Aurora激酶抑制剂的苯并唑系衍生物、组合物和使用方法
KR102747104B1 (ko) 단백질 키나아제 저해 활성을 갖는 신규한 피리도[3,4-d]피리미딘-8-온 유도체 및 이를 포함하는 암의 예방, 개선 또는 치료용 약학 조성물
TWI527800B (zh) 作為聚(二磷酸腺苷酸-核醣)聚合酶(parp)之抑制劑之1-(芳基甲基)喹唑啉-2,4(1h,3h)-二酮及其應用
CN118055930A (zh) 噻二唑衍生物及其组合物和应用
WO2011093672A2 (en) Bicyclic heteroaryl derivatives having inhibitory activity for protein kinase
WO2005095386A1 (en) Substituted thiophene derivatives as anti-cancer agents
JP2013515736A (ja) キナーゼ調節のための化合物及び方法ならびにそれらの適応症
CN104024257A (zh) Pi3k的新的喹喔啉抑制剂
JP2013082757A (ja) プロテインキナーゼ阻害薬として有用なベンズイミダゾール
CN104926788B (zh) 取代哌啶类衍生物、含其的药物组合物及其在抗肿瘤中的应用
JP2018528193A (ja) インドール誘導体、その調製方法および医薬におけるその使用
JP2020023554A (ja) ピリミジン化合物及びその医薬用途
JP2019519534A (ja) 五員複素環[3,4−d]ピリダジノン系化合物、その製造方法、医薬組成物及び応用
WO2017085483A1 (en) Pyrropyrimidine compounds as mnks inhibitors
WO2017008708A1 (zh) 吲唑类化合物的制备方法和用途
KR102329720B1 (ko) 단백질 키나아제 저해 활성을 갖는 신규한 피리미도[4,5-d]피리미딘-2-온 유도체
HK1125631B (en) Benzazole derivatives, compositions, and methods of use as aurora kinase inhibitors
HK1170723A (en) Benzazole derivatives, compositions, and methods of use as aurora kinase inhibitors
KR102329723B1 (ko) 단백질 키나아제 저해 활성을 갖는 신규한 피리미도[4,5-d]피리미딘-2-온 유도체
MX2008009811A (en) Benzazole derivatives, compositions, and methods of use as aurora kinase inhibitors
JP2025535036A (ja) Parg阻害化合物
KR20210048701A (ko) 단백질 키나아제 저해 활성을 갖는 신규한 피리디닐트리아진 유도체 및 이를 포함하는 암의 예방, 개선 또는 치료용 약학 조성물
HK1122558A (en) Benzimidazoles useful as inhibitors of protein kinases
MX2008001172A (en) Benzimidazoles useful as inhibitors of protein kinases

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 1125631

Country of ref document: HK

C14 Grant of patent or utility model
GR01 Patent grant
REG Reference to a national code

Ref country code: HK

Ref legal event code: GR

Ref document number: 1125631

Country of ref document: HK

ASS Succession or assignment of patent right

Owner name: TRANSFORMATION TECHNOLOGY PHARMA, LLC

Free format text: FORMER OWNER: TRANSTECH PHARMA INC.

Effective date: 20140328

C41 Transfer of patent application or patent right or utility model
TR01 Transfer of patent right

Effective date of registration: 20140328

Address after: North Carolina

Patentee after: TRANSTECH PHARMA INC.

Address before: North Carolina

Patentee before: Transtech Pharma, Inc.

CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20120523

Termination date: 20160209

CF01 Termination of patent right due to non-payment of annual fee