CA2773661A1 - Ether derivatives of bicyclic heteroaryls - Google Patents

Ether derivatives of bicyclic heteroaryls Download PDF

Info

Publication number
CA2773661A1
CA2773661A1 CA2773661A CA2773661A CA2773661A1 CA 2773661 A1 CA2773661 A1 CA 2773661A1 CA 2773661 A CA2773661 A CA 2773661A CA 2773661 A CA2773661 A CA 2773661A CA 2773661 A1 CA2773661 A1 CA 2773661A1
Authority
CA
Canada
Prior art keywords
7alkyl
mmol
amino
pyrrolo
pyrimidin
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.)
Abandoned
Application number
CA2773661A
Other languages
English (en)
French (fr)
Inventor
Bei Chen
Robin Alec Fairhurst
Andreas Floersheimer
Pascal Furet
Vito Guagnano
Songchun Jiang
Wenshuo Lu
Thomas H. Marsilje
Clive Mccarthy
Pierre-Yves Michellys
Frederic Stauffer
Stefan Stutz
Andrea Vaupel
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.)
IRM LLC
Novartis AG
Original Assignee
IRM LLC
Novartis AG
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 IRM LLC, Novartis AG filed Critical IRM LLC
Publication of CA2773661A1 publication Critical patent/CA2773661A1/en
Abandoned legal-status Critical Current

Links

Classifications

    • 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
    • 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
    • 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61K9/2009Inorganic compounds
    • 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
    • A61K9/2059Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841Filling excipients; Inactive ingredients
    • A61K9/4858Organic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biophysics (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Inorganic Chemistry (AREA)
  • Pulmonology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CA2773661A 2009-09-10 2010-09-10 Ether derivatives of bicyclic heteroaryls Abandoned CA2773661A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US24118209P 2009-09-10 2009-09-10
US61/241,182 2009-09-10
PCT/EP2010/063334 WO2011029915A1 (en) 2009-09-10 2010-09-10 Ether derivatives of bicyclic heteroaryls

Publications (1)

Publication Number Publication Date
CA2773661A1 true CA2773661A1 (en) 2011-03-17

Family

ID=43511862

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2773661A Abandoned CA2773661A1 (en) 2009-09-10 2010-09-10 Ether derivatives of bicyclic heteroaryls

Country Status (12)

Country Link
US (1) US20120165310A1 (instruction)
EP (1) EP2475668A1 (instruction)
JP (1) JP2013504543A (instruction)
KR (1) KR20120093867A (instruction)
CN (1) CN102596963A (instruction)
AU (1) AU2010294209A1 (instruction)
BR (1) BR112012005400A2 (instruction)
CA (1) CA2773661A1 (instruction)
EA (1) EA201200471A1 (instruction)
IN (1) IN2012DN02139A (instruction)
MX (1) MX2012002997A (instruction)
WO (1) WO2011029915A1 (instruction)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011146313A1 (en) 2010-05-19 2011-11-24 The University Of North Carolina At Chapel Hill Pyrazolopyrimidine compounds for the treatment of cancer
BR112014007788A2 (pt) * 2011-10-03 2017-04-18 Univ North Carolina Chapel Hill compostos de pirrolopirimidina para tratamento do câncer
EP2809673B1 (en) * 2012-01-31 2016-11-02 Nanjing Allgen Pharma Co. Ltd. Spirocyclic molecules as bruton's tyrosine kinase inhibitors
TW201348231A (zh) * 2012-02-29 2013-12-01 Amgen Inc 雜雙環化合物
IN2014DN09610A (instruction) 2012-05-22 2015-07-31 Univ North Carolina
US9562047B2 (en) 2012-10-17 2017-02-07 The University Of North Carolina At Chapel Hill Pyrazolopyrimidine compounds for the treatment of cancer
JP6359020B6 (ja) 2012-11-06 2018-08-15 シャンハイ フォチョン ファーマシューティカル カンパニー リミテッド Alkキナーゼ阻害剤
WO2014085225A1 (en) 2012-11-27 2014-06-05 The University Of North Carolina At Chapel Hill Pyrimidine compounds for the treatment of cancer
US20150291609A1 (en) 2014-04-11 2015-10-15 The University Of North Carolina At Chapel Hill Mertk-specific pyrimidine compounds
US10112924B2 (en) 2015-12-02 2018-10-30 Astraea Therapeutics, Inc. Piperdinyl nociceptin receptor compounds
EP4455145A3 (en) * 2015-12-02 2025-03-12 Astraea Therapeutics, LLC Piperidinyl nociceptin receptor compounds
US10709708B2 (en) 2016-03-17 2020-07-14 The University Of North Carolina At Chapel Hill Method of treating cancer with a combination of MER tyrosine kinase inhibitor and an epidermal growth factor receptor (EGFR) inhibitor
CN106008527B (zh) 2016-06-29 2018-05-15 四川大学华西医院 吡唑并[3,4-d]嘧啶衍生物
CN107098909B (zh) * 2017-05-19 2019-02-22 四川大学华西医院 烷氧端基寡peg修饰的氨基嘧啶衍生物及抗肿瘤应用
JP2023512082A (ja) * 2020-01-30 2023-03-23 ザ・リージエンツ・オブ・ザ・ユニバーシテイー・オブ・カリフオルニア Strad結合剤およびその使用
US12084453B2 (en) 2021-12-10 2024-09-10 Incyte Corporation Bicyclic amines as CDK12 inhibitors

Family Cites Families (46)

* 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
US5010099A (en) 1989-08-11 1991-04-23 Harbor Branch Oceanographic Institution, Inc. Discodermolide compounds, compositions containing same and method of preparation and use
NZ243082A (en) 1991-06-28 1995-02-24 Ici Plc 4-anilino-quinazoline derivatives; pharmaceutical compositions, preparatory processes, and use thereof
AU661533B2 (en) 1992-01-20 1995-07-27 Astrazeneca Ab Quinazoline derivatives
TW225528B (instruction) 1992-04-03 1994-06-21 Ciba Geigy Ag
DK1167384T3 (da) 1992-10-28 2007-04-10 Genentech Inc Vaskular endotheliel cellevækstfaktor antagonister
MX9702307A (es) 1994-09-29 1998-04-30 Novartis Ag Pirrolo (2,3-d)pirimidinas y su uso.
GB9508538D0 (en) 1995-04-27 1995-06-14 Zeneca Ltd Quinazoline derivatives
US5843901A (en) 1995-06-07 1998-12-01 Advanced Research & Technology Institute LHRH antagonist peptides
US5880141A (en) 1995-06-07 1999-03-09 Sugen, Inc. Benzylidene-Z-indoline compounds for the treatment of disease
IL122855A (en) 1995-07-06 2004-08-31 Novartis Ag History of N-Phenyl (Alkyl) - 7H-Pyrolo [-3,2d] Pyrimidine - 4 Amine, their preparation and pharmaceutical preparations containing them
GB9517060D0 (en) 1995-08-17 1995-10-25 Ciba Geigy Ag Acylated oligopeptide derivatives
GB9516842D0 (en) 1995-08-17 1995-10-18 Ciba Geigy Ag Various acylated oligopeptides
CH690773A5 (de) 1996-02-01 2001-01-15 Novartis Ag Pyrrolo(2,3-d)pyrimide und ihre Verwendung.
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
AU1794697A (en) 1996-03-06 1997-09-22 Novartis Ag 7-alkyl-pyrrolo{2,3-d}pyrimidines
WO1997038983A1 (en) 1996-04-12 1997-10-23 Warner-Lambert Company Irreversible inhibitors of tyrosine kinases
CA2258548C (en) 1996-06-24 2005-07-26 Pfizer Inc. Phenylamino-substituted tricyclic derivatives for treatment of hyperproliferative diseases
AU3176297A (en) 1996-06-25 1998-01-14 Novartis Ag Substituted 7-amino-pyrrolo{3,2-d}pyrimidines and the use thereof
DE19638745C2 (de) 1996-09-11 2001-05-10 Schering Ag Monoklonale Antikörper gegen die extrazelluläre Domäne des menschlichen VEGF - Rezeptorproteins (KDR)
EP0954315A2 (en) 1996-09-13 1999-11-10 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
CO4950519A1 (es) 1997-02-13 2000-09-01 Novartis Ag Ftalazinas, preparaciones farmaceuticas que las comprenden y proceso para su preparacion
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
PT1107964E (pt) 1998-08-11 2010-06-11 Novartis Ag Derivados de isoquinolina com actividade inibidora da angiogénese
UA71587C2 (uk) 1998-11-10 2004-12-15 Шерінг Акцієнгезелльшафт Аміди антранілової кислоти та їхнє застосування як лікарських засобів
GB9824579D0 (en) 1998-11-10 1999-01-06 Novartis Ag Organic compounds
EP1140173B2 (en) 1998-12-22 2013-04-03 Genentech, Inc. Vascular endothelial cell growth factor antagonists and uses thereof
PT1165085E (pt) 1999-03-30 2006-10-31 Novartis Ag Derivados de ftalazina para tratar doencas inflamatorias
GB0001930D0 (en) 2000-01-27 2000-03-22 Novartis Ag Organic compounds
DE60110749T2 (de) 2000-02-09 2006-02-02 Novartis Ag Pyridinderivative als angiogenese- und/oder vegf-rezeptor-tyrosinkinase-inhibitoren
WO2001072751A1 (en) * 2000-03-29 2001-10-04 Knoll Gesellschaft Mit Beschraenkter Haftung Pyrrolopyrimidines as tyrosine kinase inhibitors
JP4175115B2 (ja) 2001-05-11 2008-11-05 和光純薬工業株式会社 フッ素置換トリフェニルスルホニウム塩
AR035885A1 (es) * 2001-05-14 2004-07-21 Novartis Ag Derivados de 4-amino-5-fenil-7-ciclobutilpirrolo (2,3-d)pirimidina, un proceso para su preparacion, una composicion farmaceutica y el uso de dichos derivados para la preparacion de una composicion farmaceutica
WO2004078163A2 (en) 2003-02-28 2004-09-16 Transform Pharmaceuticals, Inc. Pharmaceutical co-crystal compositions of drugs such as carbamazepine, celecoxib, olanzapine, itraconazole, topiramate, modafinil, 5-fluorouracil, hydrochlorothiazide, acetaminophen, aspirin, flurbiprofen, phenytoin and ibuprofen
US7320992B2 (en) * 2003-08-25 2008-01-22 Amgen Inc. Substituted 2,3-dihydro-1h-isoindol-1-one derivatives and methods of use
RU2405784C2 (ru) * 2003-10-15 2010-12-10 Оси Фармасьютикалз, Инк. Имидазопиразины в качестве ингибиторов тирозинкиназ
PT1740591E (pt) 2004-04-02 2009-09-24 Osi Pharm Inc Inibidores da proteína quinase heterobicíclicos em substituição de anel bicíclico 6,6
JP2008521790A (ja) 2004-11-29 2008-06-26 ファルマシア・アンド・アップジョン・カンパニー・エルエルシー 抗菌剤としてのチアゼピンオキサゾリジノン
TW200730529A (en) 2005-12-07 2007-08-16 Osi Pharm Inc Process to prepare substituted imidazopyrazine compounds
WO2009080694A1 (en) 2007-12-20 2009-07-02 Novartis Ag Thiazole derivatives used as pi 3 kinase inhibitors
JP2011506563A (ja) 2007-12-20 2011-03-03 ノバルティス アーゲー ビスチアゾール誘導体、その製造方法および医薬品としてのその使用

Also Published As

Publication number Publication date
BR112012005400A2 (pt) 2016-04-05
CN102596963A (zh) 2012-07-18
KR20120093867A (ko) 2012-08-23
JP2013504543A (ja) 2013-02-07
IN2012DN02139A (instruction) 2015-08-07
EA201200471A1 (ru) 2012-10-30
MX2012002997A (es) 2012-08-01
US20120165310A1 (en) 2012-06-28
WO2011029915A1 (en) 2011-03-17
EP2475668A1 (en) 2012-07-18
AU2010294209A1 (en) 2012-03-29

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Legal Events

Date Code Title Description
FZDE Discontinued

Effective date: 20140910