CN113831345A - 二氢吡嗪并吡嗪化合物的药物组合物、其固体形式和它们的用途 - Google Patents

二氢吡嗪并吡嗪化合物的药物组合物、其固体形式和它们的用途 Download PDF

Info

Publication number
CN113831345A
CN113831345A CN202111157002.8A CN202111157002A CN113831345A CN 113831345 A CN113831345 A CN 113831345A CN 202111157002 A CN202111157002 A CN 202111157002A CN 113831345 A CN113831345 A CN 113831345A
Authority
CN
China
Prior art keywords
compound
weight
pyrazin
methoxycyclohexyl
trans
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.)
Pending
Application number
CN202111157002.8A
Other languages
English (en)
Chinese (zh)
Inventor
玛丽·乔治·彼彻姆斯
安东尼奥·克里斯蒂安·费雷蒂
胡安·安东尼奥·甘博亚
凯文·克洛普弗
威廉·爱德华·柯内可
马修·迈克尔·克雷莱茵
阿尼尔·门诺
阿曼达·尼科尔·米克洛斯
约翰·菲茨杰拉德·特拉弗斯
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.)
Signal Pharmaceuticals LLC
Original Assignee
Signal Pharmaceuticals LLC
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 Signal Pharmaceuticals LLC filed Critical Signal Pharmaceuticals LLC
Publication of CN113831345A publication Critical patent/CN113831345A/zh
Pending legal-status Critical Current

Links

Images

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • A61K9/2018Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/28Dragees; Coated pills or tablets, e.g. with film or compression coating
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/28Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806Coating materials
    • A61K9/2833Organic macromolecular compounds
    • A61K9/286Polysaccharides, e.g. gums; Cyclodextrin
    • A61K9/2866Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members 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
    • C07D241/20Nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05Isotopically modified compounds, e.g. labelled
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07Optical isomers
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Hematology (AREA)
  • Immunology (AREA)
  • Obesity (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Rheumatology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicinal Preparation (AREA)
CN202111157002.8A 2013-05-29 2014-05-28 二氢吡嗪并吡嗪化合物的药物组合物、其固体形式和它们的用途 Pending CN113831345A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361828506P 2013-05-29 2013-05-29
US61/828,506 2013-05-29
CN201480042684.XA CN105407892B (zh) 2013-05-29 2014-05-28 一种化合物的药物组合物、其固体形式及它们的使用方法

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
CN201480042684.XA Division CN105407892B (zh) 2013-05-29 2014-05-28 一种化合物的药物组合物、其固体形式及它们的使用方法

Publications (1)

Publication Number Publication Date
CN113831345A true CN113831345A (zh) 2021-12-24

Family

ID=50983209

Family Applications (4)

Application Number Title Priority Date Filing Date
CN201480042684.XA Active CN105407892B (zh) 2013-05-29 2014-05-28 一种化合物的药物组合物、其固体形式及它们的使用方法
CN202111157002.8A Pending CN113831345A (zh) 2013-05-29 2014-05-28 二氢吡嗪并吡嗪化合物的药物组合物、其固体形式和它们的用途
CN201811517073.2A Active CN109503591B (zh) 2013-05-29 2014-05-28 二氢吡嗪并吡嗪化合物的药物组合物、其固体形式和它们的用途
CN201710769972.0A Active CN107474051B (zh) 2013-05-29 2014-05-28 二氢吡嗪并吡嗪化合物的药物组合物、其固体形式和它们的用途

Family Applications Before (1)

Application Number Title Priority Date Filing Date
CN201480042684.XA Active CN105407892B (zh) 2013-05-29 2014-05-28 一种化合物的药物组合物、其固体形式及它们的使用方法

Family Applications After (2)

Application Number Title Priority Date Filing Date
CN201811517073.2A Active CN109503591B (zh) 2013-05-29 2014-05-28 二氢吡嗪并吡嗪化合物的药物组合物、其固体形式和它们的用途
CN201710769972.0A Active CN107474051B (zh) 2013-05-29 2014-05-28 二氢吡嗪并吡嗪化合物的药物组合物、其固体形式和它们的用途

Country Status (9)

Country Link
US (4) US9604939B2 (enExample)
EP (1) EP3003313A1 (enExample)
JP (1) JP6401250B2 (enExample)
CN (4) CN105407892B (enExample)
CA (2) CA2912627C (enExample)
HK (1) HK1223286A1 (enExample)
MX (1) MX2015015880A (enExample)
NZ (1) NZ629486A (enExample)
WO (1) WO2014193912A1 (enExample)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110062624B (zh) * 2016-10-14 2023-07-28 中国医学科学院药物研究所 二氢小檗碱型化合物在制备治疗stat3信号通路相关肿瘤疾病药品中的用途
IL271491B2 (en) 2017-06-22 2023-09-01 Celgene Corp Treatment of carcinoma of the liver characterized by hepatitis b virus infection
BR112021021405A2 (pt) 2019-04-26 2022-02-15 Bobby Gallagher Capacidade de manutenção de estação e desconexão de emergência melhoradas para uma embarcação conectada a um poço submarino em águas rasas

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102245611A (zh) * 2008-10-27 2011-11-16 西格诺药品有限公司 用于与 mTOR/PI3K/AKT/途径相关的肿瘤适应症和疾病的 mTOR激酶抑制剂
CN102686225A (zh) * 2009-10-26 2012-09-19 西格诺药品有限公司 杂芳基化合物的合成和纯化方法
WO2013082344A1 (en) * 2011-12-02 2013-06-06 Signal Pharmaceuticals, Llc Pharmaceutical compositions of 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino [2,3-b]pyrazin-2(1h)-one, a solid form thereof and methods of their use

Family Cites Families (130)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3507866A (en) 1967-08-08 1970-04-21 Merck & Co Inc 1h - imidazo(4,5-b)pyrazin - 2 - one and processes for their preparation
US3567725A (en) 1968-11-20 1971-03-02 Merck & Co Inc Process for preparation of 1h-imidazo-(4,5-b)pyrazin-2-ones
US4294836A (en) 1980-03-24 1981-10-13 Sterling Drug Inc. 1,3-Dihydro-6-(pyridinyl)-2H-imidazo[4,5-b]pyridin-2-ones and -imidazo[4,5-b]-pyridine-2-thiones and their cardiotonic use
US4294837A (en) 1980-03-28 1981-10-13 Sterling Drug Inc. 1,3-Dihydro-6-(pyridinyl)-2H-imidazo[4,5-b]pyridin-2-ones and -imidazo[4,5-b]pyridine-2-thiones and their cardiotonic use
US4317909A (en) 1980-03-24 1982-03-02 Sterling Drug Inc. Preparation of 1,3-dihydro-5-(pyridinyl)-2H-imidazo[4,5-b]pyridin-2-ones
US4309537A (en) 1980-03-28 1982-01-05 Sterling Drug Inc. Production of imidazo[4,5-b]pyridin-2-ones or thiones
GB8709448D0 (en) 1987-04-21 1987-05-28 Pfizer Ltd Heterobicyclic quinoline derivatives
JPS63275582A (ja) 1987-05-02 1988-11-14 Naade Kenkyusho:Kk 2−アミノイミダゾ〔4,5−b〕ピリジン誘導体の製造方法
DD262026A1 (de) 1987-07-10 1988-11-16 Akad Wissenschaften Ddr Verfahren zur herstellung von 4-substituierten 6-(pyrid-4-yl)-2,4-dihydro-1h-imidazo[4,5-b]pyrid-2-onen
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
US4963561A (en) 1990-02-28 1990-10-16 Sterling Drug Inc. Imidazopyridines, their preparation and use
TW274550B (enExample) 1992-09-26 1996-04-21 Hoechst Ag
DE19601627A1 (de) 1996-01-18 1997-07-24 Bayer Ag Heteroatomhaltige Cyclopentanopyridyl-Oxazolidinone
US6031105A (en) 1996-04-09 2000-02-29 Pfizer Inc Substituted pyridines
SK285357B6 (sk) 1997-09-26 2006-11-03 Zentaris Gmbh Zlúčeniny na báze azabenzimidazolu modulujúce funkciu serínovej/treonínovej proteínkinázy
CA2311414A1 (en) 1997-11-27 1999-06-10 Chugai Research Institute For Molecular Medicine, Inc. Diagnostic method, diagnostic reagent and therapeutic preparation for diseases caused by variation in lkb1 gene
ZA9810490B (en) 1997-12-03 1999-05-20 Dainippon Pharmaceutical Co 2-Aryl-8-oxodihydropurine derivative process for the preparation thereof pharmaceutical composition containing the same and intermediate therefor
JP2003146987A (ja) 1999-05-31 2003-05-21 Dainippon Pharmaceut Co Ltd 2−アリールプリン−9−アセトアミド誘導体
AU4951300A (en) 1999-05-31 2000-12-18 Chugai Research Institute For Molecular Medicine, Inc. Lkb1 gene knockout animals
JP3814125B2 (ja) 1999-06-02 2006-08-23 大日本住友製薬株式会社 2−アリール−8−オキソジヒドロプリン誘導体からなる医薬
CA2415697A1 (en) 2000-07-13 2002-01-24 James C. Forbes Combination of a cox-2 inhibitor and a vasomodulator for treating pain and headache pain
JP2002100363A (ja) 2000-09-25 2002-04-05 Mitsubishi Chemicals Corp リチウム二次電池用正極材料、リチウム二次電池用正極及びリチウム二次電池
JP2002167387A (ja) 2000-11-29 2002-06-11 Dainippon Pharmaceut Co Ltd 2−(7,8−ジヒドロ−8−オキソ−9h−プリン−9−イル)酢酸誘導体
ATE310004T1 (de) 2000-12-12 2005-12-15 Neurogen Corp Spiro(isobenzofuran-1,4'-piperidin)-3-one und 3h- spiroisobenzofuran-1,4'-piperidine
WO2002076954A1 (en) 2001-03-23 2002-10-03 Smithkline Beecham Corporation Compounds useful as kinase inhibitors for the treatment of hyperproliferative diseases
CA2458699C (en) 2001-09-04 2010-10-19 Boehringer Ingelheim Pharma Gmbh & Co. Kg Novel dihydropteridinones, method for producing the same and the use thereof as medicaments
US6825184B2 (en) 2001-10-18 2004-11-30 Boehringer Ingelheim Pharmaceuticals, Inc. 1,4-Disubstituted benzo-fused urea compounds
TWI314928B (en) 2002-02-28 2009-09-21 Novartis A 5-phenylthiazole derivatives and use as pi3 kinase inhibitors
US7247621B2 (en) 2002-04-30 2007-07-24 Valeant Research & Development Antiviral phosphonate compounds and methods therefor
CA2484921A1 (en) 2002-05-06 2003-11-13 Genelabs Technologies, Inc. Nucleoside derivatives for treating hepatitis c virus infection
AU2003299531A1 (en) 2002-08-05 2004-06-07 University Of Massachusetts Compounds for modulating rna interference
EP1556053A4 (en) 2002-10-31 2006-04-19 Amgen Inc ANTI-INFLAMMATORY AGENTS
JP4673218B2 (ja) 2002-11-21 2011-04-20 ノバルティス バクシンズ アンド ダイアグノスティックス,インコーポレーテッド ホスホチジルイノシトール(pi)3−キナーゼインヒビターとしての2,4,6−三置換ピリミジン、および癌の処置におけるその使用
MXPA05007503A (es) 2003-01-17 2005-09-21 Warner Lambert Co Heterociclicos 2-aminopiridina sustituidos como inhibidores de proliferacion celular.
DK1599478T3 (da) 2003-02-26 2007-09-17 Boehringer Ingelheim Pharma Dihydropteridinoner, fremgangsmåde til fremstilling af disse og anvendelse af disse som lægemiddel
GB0305152D0 (en) 2003-03-06 2003-04-09 Novartis Ag Organic compounds
GB2400101A (en) 2003-03-28 2004-10-06 Biofocus Discovery Ltd Compounds capable of binding to the active site of protein kinases
TW200519106A (en) 2003-05-02 2005-06-16 Novartis Ag Organic compounds
EP2345659A1 (en) 2003-05-30 2011-07-20 Pharmasset, Inc. Modified fluorinated nucleoside analogues
CA2529196A1 (en) 2003-06-26 2005-02-17 Merck & Co., Inc. Benzodiazepine cgrp receptor antagonists
US20070036793A1 (en) 2003-07-17 2007-02-15 Hardie David G Methods for use of an lkb1/strad7mo25 complex
GB0320197D0 (en) 2003-08-28 2003-10-01 Novartis Ag Organic compounds
US20080194019A1 (en) 2003-09-09 2008-08-14 Beth Israel Deaconess Medical Center, Inc. Tumor Suppressor Lkb1 Kinase Directly Activates Amp-Activated Kinase
EP1750715A1 (en) 2004-06-04 2007-02-14 Icos Corporation Methods for treating mast cell disorders
DE102004029784A1 (de) 2004-06-21 2006-01-05 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue 2-Benzylaminodihydropteridinone, Verfahren zur deren Herstellung und deren Verwendung als Arzneimittel
WO2006001266A1 (ja) 2004-06-23 2006-01-05 Banyu Pharmaceutical Co., Ltd. 2-アリールプリン誘導体の製造方法
US20060058311A1 (en) 2004-08-14 2006-03-16 Boehringer Ingelheim International Gmbh Combinations for the treatment of diseases involving cell proliferation
GB0420719D0 (en) 2004-09-17 2004-10-20 Addex Pharmaceuticals Sa Novel allosteric modulators
EP1796467A4 (en) 2004-09-24 2009-07-01 Janssen Pharmaceutica Nv INHIBITORS IMIDAZO {4,5-B} PYRAZINONE PROTEIN KINASES
GB0423653D0 (en) 2004-10-25 2004-11-24 Piramed Ltd Pharmaceutical compounds
KR20070085286A (ko) 2004-10-29 2007-08-27 티보텍 파마슈티칼즈 리미티드 Hiv를 저해하는 바이사이클릭 피리미딘 유도체
WO2006050076A1 (en) 2004-10-29 2006-05-11 Janssen Pharmaceutica, N.V. Pyrimidinyl substituted fused-pyrrolyl compounds useful in treating kinase disorders
SE0403006D0 (sv) 2004-12-09 2004-12-09 Biovitrum Ab New compounds
JP5111113B2 (ja) 2004-12-13 2012-12-26 サネシス ファーマシューティカルズ, インコーポレイテッド Rafキナーゼ阻害剤として有用なピリドピリミジノン、ジヒドロピリミドピリミジノンおよびプテリジノン
PL1853588T3 (pl) 2005-02-16 2008-11-28 Astrazeneca Ab Związki chemiczne
WO2006091737A1 (en) 2005-02-24 2006-08-31 Kemia, Inc. Modulators of gsk-3 activity
JP2008531538A (ja) 2005-02-25 2008-08-14 クドス ファーマシューティカルズ リミテッド 2,4−ジアミノ−ピリドピリミジン誘導体とmTOR阻害剤としてのその使用
KR20070108916A (ko) 2005-02-25 2007-11-13 쿠도스 파마슈티칼스 리미티드 Mtor 억제제로서 작용하는 하이드라지노메틸,하이드라조노메틸 및 5-원 복소환 화합물 및 이의항암제로서의 용도
JP2008534689A (ja) 2005-04-05 2008-08-28 ファーマコペイア, インコーポレイテッド 免疫抑制のためのプリン及びイミダゾピリジン誘導体
JP5461012B2 (ja) 2005-10-07 2014-04-02 エクセリクシス, インク. PI3Kαのピリドピリミジノン型阻害剤
CN101282948A (zh) 2005-10-07 2008-10-08 埃克塞里艾克西斯公司 N-(3-氨基-喹喔啉-2-基)-磺酰胺衍生物及其作为磷脂酰肌醇3-激酶抑制剂的用途
EP1931670B1 (en) 2005-10-07 2012-09-12 Exelixis, Inc. Pyridopyrimidinone inhibitors of pi3k
EP1946120A2 (en) 2005-10-18 2008-07-23 George Mason Intellectual Properties, Inc. Mtor pathway theranostic
AU2006316605B2 (en) 2005-11-17 2012-04-26 Osi Pharmaceuticals, Inc. Fused bicyclic mTOR inhibitors
EP2275103B1 (en) 2005-11-21 2014-04-23 Novartis AG mTOR inhibitors in the treatment of endocrine tumors
EP1954699B1 (en) 2005-11-22 2012-09-19 Kudos Pharmaceuticals Ltd PYRIDO-, PYRAZO- AND PYRIMIDOPYRIMIDINE DERIVATIVES AS mTOR INHIBITORS
GB0525083D0 (en) 2005-12-09 2006-01-18 Astrazeneca Ab Pyrimidine derivatives
GB0525080D0 (en) 2005-12-09 2006-01-18 Astrazeneca Ab Pyrimidine derivatives
KR20080083188A (ko) 2006-01-11 2008-09-16 아스트라제네카 아베 모르폴리노 피리미딘 유도체 및 요법에서의 그 유도체의용도
US20090281075A1 (en) 2006-02-17 2009-11-12 Pharmacopeia, Inc. Isomeric purinones and 1h-imidazopyridinones as pkc-theta inhibitors
EP3719018B1 (en) 2006-04-25 2025-08-27 Astex Therapeutics Ltd Purine and deazapurine derivatives as pharmaceutical compounds
BRPI0710874A2 (pt) 2006-04-26 2012-02-14 Hoffmann La Roche compostos de tienopirimidina, processos de produção dos referidos compostos, composições farmacêuticas contendo os mesmos, kit, produto, e usos dos compostos
US20090076009A1 (en) 2006-05-03 2009-03-19 Arnould Jean-Claude Retired Thiazole derivatives and their use as anti-tumour agents
JP2009535388A (ja) 2006-05-03 2009-10-01 アストラゼネカ アクチボラグ ピラゾール誘導体、及びそのpi3k阻害薬としての使用
EP2029593A1 (en) 2006-05-22 2009-03-04 AstraZeneca AB Indole derivatives
EA017925B1 (ru) 2006-08-02 2013-04-30 Цитокинетикс, Инкорпорэйтед ПРОИЗВОДНЫЕ 1Н-ИМИДАЗО[4,5-b]ПИРАЗИНА
LT2057156T (lt) 2006-08-23 2017-05-25 Kudos Pharmaceuticals Limited 2-metilmorfolino pirido-, pirazo- ir pirimidopirimidino dariniai kaip mtor slopikliai
WO2008030744A2 (en) 2006-09-05 2008-03-13 Board Of Regents, The University Of Texas System Inhibitors of c-met and uses thereof
JP5600004B2 (ja) 2006-09-05 2014-10-01 エモリー ユニバーシティー 感染の予防または治療のためのチロシンキナーゼ阻害剤
WO2008032077A1 (en) 2006-09-14 2008-03-20 Astrazeneca Ab Pyrimidine derivatives
WO2008032091A1 (en) 2006-09-14 2008-03-20 Astrazeneca Ab 4-benzimidaz0lyl-6-m0rph0lin0-2-piperidin-4-ylpyrimidine derivatives as pi3k and mtor inhibitors for the treatment of proliferative disorders
WO2008032027A1 (en) 2006-09-14 2008-03-20 Astrazeneca Ab Pyrimidine derivatives
CN101595103A (zh) 2006-09-14 2009-12-02 阿斯利康(瑞典)有限公司 嘧啶衍生物
WO2008032060A1 (en) 2006-09-14 2008-03-20 Astrazeneca Ab 4-benzimidaz0lyl-6-m0rph0lin0-2-piperazinylpyrimidine derivatives as p13k and mtor inhibitors for the treatment of proliferative disorders
WO2008032036A1 (en) 2006-09-14 2008-03-20 Astrazeneca Ab 6-benzimidaz0lyl-2-m0rph0lin0-4- (azetidine, pyrrolidine, piperidine or azepine) pyrimidine derivatives as pi3k and mtor inhibitors for the treatment of proliferative disorders
WO2008032033A1 (en) 2006-09-14 2008-03-20 Astrazeneca Ab 4-benzimidazolyl-2-morpholino-6-piperazinylpyrimidine derivatives as pi3k and mtor inhibitors for the treatment of proliferative disorders
WO2008032072A1 (en) 2006-09-14 2008-03-20 Astrazeneca Ab 2-benzimidaz0lyl-6-m0rph0lin0-4-piperidin-4-ylpyrimidine derivatives as pi3k and mtor inhibitors for the treatment of proliferative disorders
US20100022534A1 (en) 2006-09-14 2010-01-28 Astrazeneca 2-benzimidazolyl-6-morpholino-4- (azetidine, pyrrolidine, piperidine or azepine) pyrimidine derivatives as pi3k and mtor inhibitors for the treatment of proliferative disorders
WO2008032089A1 (en) 2006-09-14 2008-03-20 Astrazeneca Ab 4-benzimidaz0lyl-2-m0rph0lin0-6-piperidin-4-ylpyrimidine derivatives as pi3k and mtor inhibitors for the treatment of proliferative disorders
CL2007002866A1 (es) 2006-10-04 2008-07-04 Pharmacopeia Inc Compuestos derivados de 6-sustituidos-2-(bencimidazolil) purina y purinona; composicion farmaceutica que comprende a dicho compuesto; y uso del compuesto en el tratamiento de enfermedades autoinmunes, enfermedad inflamatoria, enfermedad mediada por m
US7902187B2 (en) 2006-10-04 2011-03-08 Wyeth Llc 6-substituted 2-(benzimidazolyl)purine and purinone derivatives for immunosuppression
CN101679432B (zh) 2006-10-19 2015-04-22 西格诺药品有限公司 杂芳基化合物、其组合物及其作为蛋白激酶抑制剂的用途
KR101504669B1 (ko) 2006-10-19 2015-03-20 시그날 파마소티칼 엘엘씨 헤테로아릴 화합물, 이들의 조성물 그리고 단백질 키나아제 억제제로서의 이들의 용도
CA2669415A1 (en) * 2006-11-14 2008-05-22 Ariad Pharmaceuticals, Inc. Solid dosage form comprising ap23573
MX2009005360A (es) 2006-11-20 2009-06-05 Novartis Ag Sales y formas de cristal del 2-metil-2-[4-(3-metil-2-oxo-8-quinol in-3-il-2,3-dihidro-imidazo-[4,5-c]-quinolin-1-il)-fenil]-propion itrilo.
US20080234262A1 (en) 2007-03-21 2008-09-25 Wyeth Pyrazolopyrimidine analogs and their use as mtor kinase and pi3 kinase inhibitors
UA99284C2 (ru) 2007-05-11 2012-08-10 Елі Ліллі Енд Компані ИНГИБИТОРЫ р70 S6-КИНАЗЫ
KR20100042643A (ko) 2007-07-09 2010-04-26 아스트라제네카 아베 증식성 질환을 치료하기 위한 삼중치환된 피리미딘 유도체
CN101809002B (zh) 2007-07-09 2013-03-27 阿斯利康(瑞典)有限公司 用于与mtor激酶和/或pi3k相关的疾病中的吗啉代嘧啶衍生物
AU2008273889B2 (en) 2007-07-09 2012-03-08 Astrazeneca Ab Trisubstituted pyrimidine derivatives for the treatment of proliferative diseases
MX2010004260A (es) 2007-10-16 2010-04-30 Wyeth Llc Compuestos de tienopirimidina y pirazolopirimidina y su uso como inhibidores de mtor cinasa y pi3 cinasa.
US8642660B2 (en) 2007-12-21 2014-02-04 The University Of Rochester Method for altering the lifespan of eukaryotic organisms
AP2010005346A0 (en) 2008-01-15 2010-08-31 Wyeth Llc 3H-[1,2,3]triazolo[4,5-D]pyrimidine compounds, their use as mTOR kinase and P13 kinase inhibitors, and their synthesis.
WO2009102986A1 (en) 2008-02-15 2009-08-20 Catholic Healthcare West (D/B/A St. Joseph's Hospital And Medical Center) Treatment of adenocarcinoma expressing lkb1 with mtor inhibitor in combination with cox1 inhibitor
US20110224223A1 (en) 2008-07-08 2011-09-15 The Regents Of The University Of California, A California Corporation MTOR Modulators and Uses Thereof
AU2009324894B2 (en) 2008-11-25 2015-04-09 University Of Rochester MLK inhibitors and methods of use
KR101921934B1 (ko) 2009-02-13 2018-11-26 베링거 인겔하임 인터내셔날 게엠베하 글루코피라노실 디페닐메탄 유도체를 포함하는 약제학적 조성물, 이들의 약제학적 용량형, 이들의 제조방법 및 환자에서의 개선된 당 조절을 위한 이들의 용도
JP5763077B2 (ja) 2009-09-14 2015-08-12 ギリアード サイエンシーズ, インコーポレイテッド トール様受容体のモジュレーター
KR20120120252A (ko) 2009-12-23 2012-11-01 엘란 파마슈티칼스, 인크. 폴로-유사 키나제의 억제제로서의 프테리디논
ES2670659T3 (es) 2010-02-03 2018-05-31 Signal Pharmaceuticals, Llc Identificación de mutación en LKB1 como un biomarcador predictivo para la sensibilidad a inhibidores de la quinasa TOR
US20110318336A1 (en) 2010-03-29 2011-12-29 George Mason Intellectual Properties, Inc. Identification and Treatment of Aggressive Lung Cancer Tumors
US20120028972A1 (en) 2010-07-30 2012-02-02 Lilly Wong Biomarker assays for detecting or measuring inhibition of tor kinase activity
AR086647A1 (es) * 2011-06-03 2014-01-15 Hoffmann La Roche Metodos para tratar el mesotelioma con un compuesto inhibidor de la pi3k
WO2013019927A1 (en) 2011-08-03 2013-02-07 Signal Pharmaceuticals, Llc Identification of gene expression profile as a predictive biomarker for lkb1 status
SG10201505102WA (en) * 2011-10-19 2015-07-30 Signal Pharm Llc Treatment Of Cancer With TOR Kinase Inhibitors
KR102064626B1 (ko) 2012-02-24 2020-01-09 시그날 파마소티칼 엘엘씨 Tor 키나제 억제자 복합 치료법을 사용한 비소세포 폐암의 치료 방법
CN104519885A (zh) 2012-03-15 2015-04-15 西格诺药品有限公司 用tor激酶抑制剂治疗癌症
AU2013203156C1 (en) 2012-03-15 2016-02-18 Signal Pharmaceuticals, Llc Treatment of cancer with TOR kinase inhibitors
KR102057359B1 (ko) 2012-03-15 2019-12-18 시그날 파마소티칼 엘엘씨 Tor 키나아제 억제제를 사용하는 암 치료법
EA028062B1 (ru) 2012-03-15 2017-10-31 СИГНАЛ ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи Лечение рака ингибиторами tor киназы
AU2013203714B2 (en) 2012-10-18 2015-12-03 Signal Pharmaceuticals, Llc Inhibition of phosphorylation of PRAS40, GSK3-beta or P70S6K1 as a marker for TOR kinase inhibitory activity
WO2014172436A1 (en) 2013-04-17 2014-10-23 Signal Pharmaceuticals, Llc Combination therapy comprising a tor kinase inhibitor and a 5-substituted quinazolinone compound for treating cancer
KR102223060B1 (ko) 2013-04-17 2021-03-05 시그날 파마소티칼 엘엘씨 암 치료를 위한 TOR 키나제 억제제 및 IMiD 화합물을 포함하는 조합요법
NZ631082A (en) 2013-04-17 2017-06-30 Signal Pharm Llc Methods for treating cancer using tor kinase inhibitor combination therapy
US9358232B2 (en) 2013-04-17 2016-06-07 Signal Pharmaceuticals, Llc Methods for treating cancer using TOR kinase inhibitor combination therapy
KR102221029B1 (ko) 2013-04-17 2021-02-26 시그날 파마소티칼 엘엘씨 디하이드로피라지노-피라진을 사용한 암의 치료
US20140314673A1 (en) 2013-04-17 2014-10-23 Signal Pharmaceuticals, Llc Treatment of cancer with dihydropyrazino-pyrazines
EA037683B1 (ru) 2013-04-17 2021-04-29 СИГНАЛ ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи Фармацевтические составы, способы, твердые формы и способы применения, относящиеся к 1-этил-7-(2-метил-6-(1h-1,2,4-триазол-3-ил)пиридин-3-ил)-3,4-дигидропиразино[2,3-b] пиразин-2(1h)-ону
UA115805C2 (uk) * 2013-04-17 2017-12-26 Сігнал Фармасьютікалз, Елелсі Комбінована терапія, яка включає сполуку дигідропіразинопіразину й антагоніст рецептора андрогену, для лікування раку простати
PH12021552945B1 (en) 2013-04-17 2024-02-28 Signal Pharm Llc Treatment of cancer with dihydropyrazino-pyrazines

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102245611A (zh) * 2008-10-27 2011-11-16 西格诺药品有限公司 用于与 mTOR/PI3K/AKT/途径相关的肿瘤适应症和疾病的 mTOR激酶抑制剂
CN102686225A (zh) * 2009-10-26 2012-09-19 西格诺药品有限公司 杂芳基化合物的合成和纯化方法
WO2013082344A1 (en) * 2011-12-02 2013-06-06 Signal Pharmaceuticals, Llc Pharmaceutical compositions of 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino [2,3-b]pyrazin-2(1h)-one, a solid form thereof and methods of their use
CN104093398A (zh) * 2011-12-02 2014-10-08 西格诺药品有限公司 7-(6-(2-羟基丙烷-2-基)吡啶-3-基)-1-((反式)-4-甲氧基环己基)-3,4-二氢吡嗪并[2,3-b]吡嗪-2(1h)-酮、其固体形式的药物组合物及其使用方法

Also Published As

Publication number Publication date
CN109503591B (zh) 2022-03-01
CN107474051B (zh) 2020-10-30
HK1248225A1 (zh) 2018-10-12
CN109503591A (zh) 2019-03-22
NZ629486A (en) 2017-11-24
JP6401250B2 (ja) 2018-10-10
US9604939B2 (en) 2017-03-28
US9795603B2 (en) 2017-10-24
CN105407892B (zh) 2019-05-07
US20180200252A1 (en) 2018-07-19
US20180071287A1 (en) 2018-03-15
US10052323B2 (en) 2018-08-21
CA2912627C (en) 2022-03-15
CN107474051A (zh) 2017-12-15
EP3003313A1 (en) 2016-04-13
US9974786B2 (en) 2018-05-22
MX2015015880A (es) 2016-05-31
US20140356430A1 (en) 2014-12-04
CA2912627A1 (en) 2014-12-04
WO2014193912A1 (en) 2014-12-04
CA3143529A1 (en) 2014-12-04
HK1223286A1 (zh) 2017-07-28
CN105407892A (zh) 2016-03-16
JP2016523225A (ja) 2016-08-08
US20170182042A1 (en) 2017-06-29

Similar Documents

Publication Publication Date Title
JP6076370B2 (ja) 7−(6−(2−ヒドロキシプロパン−2−イル)ピリジン−3−イル)−1−((トランス)−4−メトキシシクロヘキシル)−3,4−ジヒドロピラジノ[2,3−b]ピラジン−2(1H)−オンの薬剤組成物、その固体形態、およびその使用方法
US10052323B2 (en) Pharmaceutical compositions of 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-(trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino [2,3-b]pyrazin-2(1H)-one, a solid form thereof and methods of their use
HK1263197A1 (en) Pharmaceutical compositions of a dihydropyrazino-pyrazine compound, a solid form thereof and uses of the same
AU2015201807B2 (en) Pharmaceutical compositions of 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methocyclohexyl)-3,4-dihydropyrazino[2,3-b] pyrazin-2(1H)-one, a solid form thereof and methods of their use
HK1263197B (zh) 二氢吡嗪并吡嗪化合物的药物组合物、其固体形式和它们的用途
HK1248225B (zh) 二氢吡嗪并吡嗪化合物的药物组合物、其固体形式和它们的用途
HK1202052B (en) Pharmaceutical compositions of 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino [2,3-b]pyrazin-2(1h)-one, a solid form thereof and methods of their use
NZ625511B2 (en) Pharmaceutical compositions of 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino [2,3-b]pyrazin-2(1h)-one, a solid form thereof and methods of their use
NZ711123B2 (en) Pharmaceutical compositions of 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino [2,3-b]pyrazin-2(1h)-one, a solid form thereof and methods of their use

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
WD01 Invention patent application deemed withdrawn after publication
WD01 Invention patent application deemed withdrawn after publication

Application publication date: 20211224