CA2436487A1 - Methods of inhibiting kinases - Google Patents

Methods of inhibiting kinases Download PDF

Info

Publication number
CA2436487A1
CA2436487A1 CA002436487A CA2436487A CA2436487A1 CA 2436487 A1 CA2436487 A1 CA 2436487A1 CA 002436487 A CA002436487 A CA 002436487A CA 2436487 A CA2436487 A CA 2436487A CA 2436487 A1 CA2436487 A1 CA 2436487A1
Authority
CA
Canada
Prior art keywords
heterocyclyl
alkyl
halo
amino
heterocycle
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
CA002436487A
Other languages
English (en)
French (fr)
Inventor
Christopher John Burns
Andrew Frederick Wilks
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.)
Cytopia Pty Ltd
Original Assignee
Individual
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
Priority claimed from AUPR2792A external-priority patent/AUPR279201A0/en
Priority claimed from AUPR2793A external-priority patent/AUPR279301A0/en
Application filed by Individual filed Critical Individual
Publication of CA2436487A1 publication Critical patent/CA2436487A1/en
Abandoned legal-status Critical Current

Links

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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/443Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4436Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/02Nasal agents, e.g. decongestants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • 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
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/14Decongestants or antiallergics
    • 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
    • A61P3/08Drugs 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
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/12Antidiuretics, e.g. drugs for diabetes insipidus

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Virology (AREA)
  • Neurosurgery (AREA)
  • Rheumatology (AREA)
  • Immunology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Communicable Diseases (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Molecular Biology (AREA)
  • Obesity (AREA)
  • Hospice & Palliative Care (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • AIDS & HIV (AREA)
  • Ophthalmology & Optometry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Dermatology (AREA)
CA002436487A 2001-01-30 2002-01-30 Methods of inhibiting kinases Abandoned CA2436487A1 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
AUPR2792 2001-01-30
AUPR2793 2001-01-30
AUPR2792A AUPR279201A0 (en) 2001-01-30 2001-01-30 Jak inhibitors
AUPR2793A AUPR279301A0 (en) 2001-01-30 2001-01-30 Method of inhibiting jak
PCT/AU2002/000089 WO2002060492A1 (en) 2001-01-30 2002-01-30 Methods of inhibiting kinases

Publications (1)

Publication Number Publication Date
CA2436487A1 true CA2436487A1 (en) 2002-08-08

Family

ID=25646570

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002436487A Abandoned CA2436487A1 (en) 2001-01-30 2002-01-30 Methods of inhibiting kinases

Country Status (5)

Country Link
US (2) US20040102455A1 (https=)
EP (1) EP1363702A4 (https=)
JP (1) JP2004528295A (https=)
CA (1) CA2436487A1 (https=)
WO (1) WO2002060492A1 (https=)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006059245A3 (en) * 2004-11-16 2006-10-05 Neurochem Int Ltd Compounds for the treatment of cns and amyloid associated diseases

Families Citing this family (138)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2002330713A1 (en) * 2001-09-24 2003-04-07 University Of Aarhus Methods for diagnosis and treatment of diseases associated with altered expression of neurogranin
TWI329105B (en) * 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
KR20050008691A (ko) * 2002-04-19 2005-01-21 셀룰러 지노믹스 아이엔씨 이미다조[1,2-a]피라진-8-일 아민, 그의 제조방법 및사용방법
WO2003099811A1 (en) 2002-05-23 2003-12-04 Cytopia Pty Ltd Kinase inhibitors
CA2486183C (en) 2002-05-23 2012-01-10 Cytopia Pty Ltd. Protein kinase inhibitors
AU2003249369A1 (en) 2002-06-21 2004-01-06 Cellular Genomics, Inc. Certain amino-substituted monocycles as kinase modulators
GB0215775D0 (en) * 2002-07-06 2002-08-14 Astex Technology Ltd Pharmaceutical compounds
HRP20050089B1 (hr) 2002-07-29 2015-06-19 Rigel Pharmaceuticals Upotreba 2,4 pirimidindiaminskog spoja za proizvodnju lijeka za lijeäśenje ili sprjeäśavanje autoimunosne bolesti
US7205308B2 (en) 2002-09-04 2007-04-17 Schering Corporation Trisubstituted 7-aminopyrazolopyrimidines as cyclin dependent kinase inhibitors
DE60313872T2 (de) 2002-09-04 2008-01-17 Schering Corp. Pyrazoloä1,5-aüpyrimidine als hemmstoffe cyclin-abhängiger kinasen
AU2003270489A1 (en) 2002-09-09 2004-03-29 Cellular Genomics, Inc. 6-ARYL-IMIDAZO(1,2-a)PYRAZIN-8-YLAMINES, METHOD OF MAKING, AND METHOD OF USE THEREOF
NZ538685A (en) 2002-09-23 2008-02-29 Schering Corp Imidazopyrazines as cyclin dependent kinase inhibitors
NZ538686A (en) * 2002-09-23 2008-01-31 Schering Corp Novel imidazopyrazines as cyclin dependent kinase inhibitors
WO2004035571A1 (en) * 2002-10-15 2004-04-29 Rigel Pharmaceuticals, Inc. Substituted indoles and their use as hcv inhibitors
AU2002953255A0 (en) * 2002-12-11 2003-01-02 Cytopia Research Pty Ltd Protein kinase inhibitors
WO2004072080A1 (en) * 2003-02-10 2004-08-26 Cellular Genomics, Inc. Certain 8-heteroaryl-6-phenyl-imidazo[1,2-a]pyrazines as modulators of hsp90 complex activity
AR043002A1 (es) * 2003-02-18 2005-07-13 Altana Pharma Ag Imidazopirazinas 6-substituidos
US7157460B2 (en) 2003-02-20 2007-01-02 Sugen Inc. Use of 8-amino-aryl-substituted imidazopyrazines as kinase inhibitors
US7186832B2 (en) 2003-02-20 2007-03-06 Sugen Inc. Use of 8-amino-aryl-substituted imidazopyrazines as kinase inhibitors
WO2004083235A2 (en) * 2003-03-19 2004-09-30 Exelixis Inc. Tie-2 modulators and methods of use
US7459454B2 (en) 2003-03-21 2008-12-02 Smithkline Beecham Corporation Aminopyrazine derivatives and compositions
JP4895806B2 (ja) * 2003-04-09 2012-03-14 エクセリクシス, インク. Tie−2モジュレータと使用方法
US7405295B2 (en) * 2003-06-04 2008-07-29 Cgi Pharmaceuticals, Inc. Certain imidazo[1,2-a]pyrazin-8-ylamines and method of inhibition of Bruton's tyrosine kinase by such compounds
WO2005005429A1 (en) * 2003-06-30 2005-01-20 Cellular Genomics, Inc. Certain heterocyclic substituted imidazo[1,2-a]pyrazin-8-ylamines and methods of inhibition of bruton’s tyrosine kinase by such compounds
WO2005012294A1 (en) * 2003-07-30 2005-02-10 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds for use in the treatment or prevention of autoimmune diseases
US7259164B2 (en) 2003-08-11 2007-08-21 Cgi Pharmaceuticals, Inc. Certain substituted imidazo[1,2-a]pyrazines, as modulators of kinase activity
EP1670794A2 (en) 2003-09-30 2006-06-21 Amgen Inc. Vanilloid receptor ligands and their use in treatments
UA83509C2 (en) * 2003-10-15 2008-07-25 Оси Фармасьютикалз, Инк. Imidazopyrazines as tyrosine kinase inhibitors
WO2005047290A2 (en) * 2003-11-11 2005-05-26 Cellular Genomics Inc. Imidazo[1,2-a] pyrazin-8-ylamines as kinase inhibitors
NZ545694A (en) * 2003-12-03 2010-04-30 Ym Bioscience Australia Pty Lt Azole-based kinase inhibitors
CA2545422C (en) * 2003-12-03 2015-06-02 Cytopia Research Pty Ltd Tubulin inhibitors
US20080194574A1 (en) * 2003-12-16 2008-08-14 Axxima Pharmaceuticals Ag Pyrazine Derivatives As Effective Compounds Against Infectious Diseases
WO2005085252A1 (en) * 2004-03-04 2005-09-15 Biofocus Discovery Limited Imidazo ‘1,2-a’ pyrazine compounds which interact with protein kinases
EP2168968B1 (en) 2004-04-02 2017-08-23 OSI Pharmaceuticals, LLC 6,6-bicyclic ring substituted heterobicyclic protein kinase inhibitors
CA2561831A1 (en) 2004-04-13 2005-12-22 Icagen, Inc. Polycyclic pyrazines as potassium ion channel modulators
AU2005309019A1 (en) * 2004-11-24 2006-06-01 Novartis Ag Combinations of JAK inhibitors and at least one of Bcr-Abl, Flt-3, FAK or RAF kinase inhibitors
AR054416A1 (es) 2004-12-22 2007-06-27 Incyte Corp Pirrolo [2,3-b]piridin-4-il-aminas y pirrolo [2,3-b]pirimidin-4-il-aminas como inhibidores de las quinasas janus. composiciones farmaceuticas.
GB0428082D0 (en) * 2004-12-22 2005-01-26 Welcome Trust The Ltd Therapeutic compounds
WO2007024294A2 (en) 2005-05-03 2007-03-01 Cgi Pharmaceuticals, Inc. Certain substituted ureas, as modulators of kinase activity
BRPI0610876B8 (pt) 2005-06-08 2021-05-25 Rigel Pharmaceuticals Inc composto, formulação farmacêutica, e métodos de inibir uma atividade de uma jak cinase, e de inibir uma cascata de transdução de sinal em que jak3 cinase desempenha um papel
US20070203161A1 (en) 2006-02-24 2007-08-30 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
JP2009507032A (ja) 2005-09-02 2009-02-19 アボット・ラボラトリーズ 新規なイミダゾ系複素環
CA2621261C (en) 2005-09-22 2014-05-20 Incyte Corporation Azepine inhibitors of janus kinases
US20070117804A1 (en) * 2005-11-10 2007-05-24 Schering Corporation Imidazopyrazines as protein kinase inhibitors
SG10202003901UA (en) 2005-12-13 2020-05-28 Incyte Holdings Corp Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as janus kinase inhibitors
US8575164B2 (en) * 2005-12-19 2013-11-05 OSI Pharmaceuticals, LLC Combination cancer therapy
ES2622493T3 (es) 2006-02-24 2017-07-06 Rigel Pharmaceuticals, Inc. Composiciones y métodos para la inhibición de la ruta de JAK
MX2008012658A (es) 2006-03-31 2008-12-16 Schering Corp Inhibidores de cinasa.
US7893058B2 (en) * 2006-05-15 2011-02-22 Janssen Pharmaceutica Nv Imidazolopyrazine compounds useful for the treatment of degenerative and inflammatory diseases
PT2029602E (pt) * 2006-05-31 2010-07-08 Galapagos Nv Compostos de triazolopirazina uteis para o tratamento de doenãas degenerativas e inflamatërias
US20090175852A1 (en) 2006-06-06 2009-07-09 Schering Corporation Imidazopyrazines as protein kinase inhibitors
CA2660560A1 (en) 2006-08-16 2008-02-21 Boehringer Ingelheim International Gmbh Pyrazine compounds, their use and methods of preparation
CA2673038C (en) 2006-12-22 2015-12-15 Incyte Corporation Substituted tricyclic heteroaryl compounds as janus kinase inhibitors
KR101566840B1 (ko) 2007-03-12 2015-11-06 와이엠 바이오사이언시즈 오스트레일리아 피티와이 엘티디 페닐 아미노 피리미딘 화합물 및 이의 용도
US8148369B2 (en) 2007-05-10 2012-04-03 Janssen Pharmaceutica Nv Fused pyrazine compounds useful for the treatment of degenerative and inflammatory diseases
MX2009013213A (es) * 2007-06-08 2010-03-30 Abbott Lab Indazoles 5-sustituidos 5-heteroarilo como inhibidores de cinasa.
CL2008001709A1 (es) 2007-06-13 2008-11-03 Incyte Corp Compuestos derivados de pirrolo [2,3-b]pirimidina, moduladores de quinasas jak; composicion farmaceutica; y uso en el tratamiento de enfermedades tales como cancer, psoriasis, artritis reumatoide, entre otras.
KR20150036210A (ko) 2007-06-13 2015-04-07 인사이트 코포레이션 야누스 키나제 억제제(R)―3―(4―(7H―피롤로[2,3-d]피리미딘―4―일)―1H―피라졸―1―일)―3―사이클로펜틸프로판니트릴의 염
DE102007032349A1 (de) * 2007-07-11 2009-01-15 Bayer Healthcare Ag Imidazo-, Pyrazolopyrazine und Imidazotriazine und ihre Verwendung
GB0716292D0 (en) * 2007-08-21 2007-09-26 Biofocus Dpi Ltd Imidazopyrazine compounds
US20110046144A1 (en) * 2008-01-18 2011-02-24 Mulvihill Mark J Imidazopyrazinol derivatives for the treatment of cancers
MX2010007973A (es) 2008-02-01 2010-11-09 Akinion Pharmaceuticals Ab Derivados de pirazina y su uso como inhibidores de proteina cinasa.
WO2009102468A1 (en) 2008-02-13 2009-08-20 Cgi Pharmaceuticals, Inc. 6-aryl-imidaz0[l, 2-a] pyrazine derivatives, method of making, and method of use thereof
HUE030912T2 (en) 2008-02-15 2017-06-28 Rigel Pharmaceuticals Inc Pyrimidine-2-amine compounds and their use as inhibitors of yak kinases
HUE029767T2 (en) 2008-03-11 2017-04-28 Incyte Holdings Corp JAK inhibitor azetidine and cyclobutane derivatives
US8063058B2 (en) 2008-04-16 2011-11-22 Portola Pharmaceuticals, Inc. Inhibitors of syk and JAK protein kinases
US8138339B2 (en) 2008-04-16 2012-03-20 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
AU2009238590A1 (en) * 2008-04-22 2009-10-29 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
US20090275529A1 (en) * 2008-05-05 2009-11-05 Reiss Allison B Method for improving cardiovascular risk profile of cox inhibitors
ES2396613T3 (es) * 2008-05-19 2013-02-22 OSI Pharmaceuticals, LLC Imidazopirazinas e imidazotriazinas sustituidas
US8450321B2 (en) 2008-12-08 2013-05-28 Gilead Connecticut, Inc. 6-(1H-indazol-6-yl)-N-[4-(morpholin-4-yl)phenyl]imidazo-[1,2-A]pyrazin-8-amine, or a pharmaceutically acceptable salt thereof, as a SYK inhibitor
PL2716157T3 (pl) * 2008-12-08 2017-06-30 Gilead Connecticut, Inc. Imidazopirazynowe inhibitory Syk
PE20120121A1 (es) * 2008-12-08 2012-02-20 Gilead Connecticut Inc Derivados de imidazopirazina como inhibidores de syk
GB0822981D0 (en) * 2008-12-17 2009-01-21 Summit Corp Plc Compounds for treatment of duchenne muscular dystrophy
BRPI1014572B8 (pt) * 2009-04-16 2022-07-19 Fundacion Centro Nac De Investigaciones Oncologicas Carlos Iii Imidazopirazinas para uso como inibidores de cinase
US8513415B2 (en) 2009-04-20 2013-08-20 OSI Pharmaceuticals, LLC Preparation of C-pyrazine-methylamines
EP2427192A1 (en) * 2009-05-07 2012-03-14 OSI Pharmaceuticals, LLC Use of osi-906 for treating adrenocortical carcinoma
AR076794A1 (es) 2009-05-22 2011-07-06 Incyte Corp Derivados de n-(hetero)aril-pirrolidina de pirazol-4-il-pirrolo [2,3-d]pirimidinas y pirrol-3-il-pirrolo [2,3-d ]pirimidinas como inhibidores de la quinasa janus y composiciones farmaceuticas que los contienen
SI2432472T1 (sl) 2009-05-22 2019-11-29 Incyte Holdings Corp 3-(4-(7H-pirolo(2,3-d)pirimidin-4-il)-1H-pirazol-1-il)oktan- ali heptan-nitril kot inhibitorji JAK
TW201113285A (en) 2009-09-01 2011-04-16 Incyte Corp Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
EA021478B1 (ru) 2009-10-09 2015-06-30 Инсайт Корпорейшн ГИДРОКСИЛЬНЫЕ, КЕТО И ГЛЮКУРОНИДНЫЕ ПРОИЗВОДНЫЕ 3-(4-(7Н-ПИРРОЛО[2,3-d]ПИРИМИДИН-4-ИЛ)-1Н-ПИРАЗОЛ-1-ИЛ)-3-ЦИКЛОПЕНТИЛПРОПАННИТРИЛА
CN102711749A (zh) * 2009-11-05 2012-10-03 莱西肯医药有限公司 用于癌症治疗的色氨酸羟化酶抑制剂
PH12012501361A1 (en) * 2009-12-31 2012-10-22 Centro Nac De Investigaciones Oncologicas Cnio Tricyclic compounds for use as kinase inhibitors
NZ600136A (en) * 2009-12-31 2013-09-27 Novartis Ag Pyrazine derivatives and their use in the treatment of neurological disorders
US9073927B2 (en) 2010-01-22 2015-07-07 Fundacion Centro Nacional De Investigaciones Oncologicas Carlos Iii Inhibitors of PI3 kinase
EP3354652B1 (en) 2010-03-10 2020-05-06 Incyte Holdings Corporation Piperidin-4-yl azetidine derivatives as jak1 inhibitors
AU2011226689B2 (en) 2010-03-11 2016-09-01 Kronos Bio, Inc. Imidazopyridines Syk inhibitors
WO2011141713A1 (en) * 2010-05-13 2011-11-17 Centro Nacional De Investigaciones Oncologicas (Cnio) New bicyclic compounds as pi3-k and mtor inhibitors
PE20130216A1 (es) 2010-05-21 2013-02-27 Incyte Corp Formulacion topica para un inhibidor de jak
EP2441755A1 (en) * 2010-09-30 2012-04-18 Almirall, S.A. Pyridine- and isoquinoline-derivatives as Syk and JAK kinase inhibitors
EP2444084A1 (en) * 2010-10-21 2012-04-25 Centro Nacional de Investigaciones Oncológicas (CNIO) Use of PI3K inibitors for the treatment of obesity
WO2012052745A1 (en) 2010-10-21 2012-04-26 Centro Nacional De Investigaciones Oncológicas (Cnio) Combinations of pi3k inhibitors with a second anti -tumor agent
EP2975027A1 (en) 2010-11-01 2016-01-20 Portola Pharmaceuticals, Inc. Nicotinamides as jak kinase modulators
PE20140146A1 (es) 2010-11-19 2014-02-06 Incyte Corp Derivados de pirrolopiridina y pirrolopirimidina sustituidos con ciclobutilo como inhibidores de jak
US9034884B2 (en) 2010-11-19 2015-05-19 Incyte Corporation Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as JAK inhibitors
ES2547916T3 (es) 2011-02-18 2015-10-09 Novartis Pharma Ag Terapia de combinación de inhibidores de mTOR/JAK
JO3363B1 (ar) 2011-04-13 2019-03-13 Epizyme Inc مركبات بنزين مستبدلة بأريل أو أريل غير متجانس
US9145391B2 (en) 2011-05-10 2015-09-29 Merck Sharp & Dohme Corp. Bipyridylaminopyridines as Syk inhibitors
CN103797010B (zh) 2011-06-20 2016-02-24 因塞特控股公司 作为jak抑制剂的氮杂环丁烷基苯基、吡啶基或吡嗪基甲酰胺衍生物
CA2840883C (en) * 2011-07-07 2019-07-16 Merck Patent Gmbh Substituted azaheterocycles
EP2741747A1 (en) 2011-08-10 2014-06-18 Novartis Pharma AG JAK P13K/mTOR COMBINATION THERAPY
TW201313721A (zh) 2011-08-18 2013-04-01 Incyte Corp 作為jak抑制劑之環己基氮雜環丁烷衍生物
UA111854C2 (uk) 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки для отримання інгібіторів jak
MX363551B (es) 2011-11-23 2019-03-27 Portola Pharmaceuticals Inc Star Compuestos derivados de pirazina como inhibidores de cinasa.
TW201406761A (zh) 2012-05-18 2014-02-16 Incyte Corp 做爲jak抑制劑之哌啶基環丁基取代之吡咯并吡啶及吡咯并嘧啶衍生物
WO2014013014A1 (en) 2012-07-18 2014-01-23 Fundació Privada Centre De Regulació Genòmica (Crg) Jak inhibitors for activation of epidermal stem cell populations
WO2014058921A2 (en) 2012-10-08 2014-04-17 Portola Pharmaceuticals, Inc. Substituted pyrimidinyl kinase inhibitors
PE20150887A1 (es) 2012-10-15 2015-06-04 Epizyme Inc Compuestos de benceno sustituidos
WO2014074421A1 (en) * 2012-11-07 2014-05-15 Merck Sharp & Dohme Corp. Prodrug bipyridylaminopyridines as syk inhibitors
PH12020551186B1 (en) 2012-11-15 2024-03-20 Incyte Holdings Corp Sustained-release dosage forms of ruxolitinib
WO2014106606A1 (en) * 2013-01-05 2014-07-10 F. Hoffmann-La Roche Ag Nove phenyl/pyridine series substitued by hydroxyethylamino for the treatment of cancer
ES2675720T3 (es) 2013-01-10 2018-07-12 Pulmokine, Inc. Inhibidores de quinasa no selectivos
RS62867B1 (sr) 2013-03-06 2022-02-28 Incyte Holdings Corp Postupci i intermedijeri za dobijanje inhibitora jak
KR101810798B1 (ko) 2013-07-30 2017-12-19 질레드 코네티컷 인코포레이티드 Syk 억제제의 다형체
PE20160605A1 (es) 2013-07-30 2016-07-20 Gilead Connecticut Inc Formulaciones de inhibidores de la syk
SMT202000315T1 (it) 2013-08-07 2020-07-08 Incyte Corp Forme di dosaggio a rilascio prolungato per un inibitore di jak1
US9925184B2 (en) 2013-10-11 2018-03-27 Pulmokine, Inc. Spray-dry formulations
KR20160090903A (ko) 2013-12-04 2016-08-01 길리애드 사이언시즈, 인코포레이티드 암을 치료하는 방법
US9290505B2 (en) 2013-12-23 2016-03-22 Gilead Sciences, Inc. Substituted imidazo[1,2-a]pyrazines as Syk inhibitors
TWI735853B (zh) 2013-12-23 2021-08-11 美商克洛諾斯生技有限公司 脾酪胺酸激酶抑制劑
WO2015157955A1 (en) * 2014-04-17 2015-10-22 Abbvie Inc. Heterocyclic btk inhibit ors
EP3137454A1 (en) 2014-04-28 2017-03-08 Pfizer Inc. Heteroaromatic compounds and their use as dopamine d1 ligands
US9498467B2 (en) 2014-05-30 2016-11-22 Incyte Corporation Treatment of chronic neutrophilic leukemia (CNL) and atypical chronic myeloid leukemia (aCML) by inhibitors of JAK1
TWI729644B (zh) 2014-06-12 2021-06-01 美商西爾拉癌症醫學公司 N-(氰基甲基)-4-(2-(4-𠰌啉基苯基胺基)嘧啶-4-基)苯甲醯胺
SG11201610551TA (en) 2014-07-14 2017-01-27 Gilead Sciences Inc Combinations for treating cancers
WO2018041989A1 (en) 2016-09-02 2018-03-08 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for diagnosing and treating refractory celiac disease type 2
CA3041679A1 (en) 2016-10-27 2018-05-03 Lawrence S. ZISMAN Combination therapy for treating pulmonary hypertension
EP3672974A1 (en) 2017-08-25 2020-07-01 Gilead Sciences, Inc. Polymorphs of syk inhibitors
WO2019113487A1 (en) 2017-12-08 2019-06-13 Incyte Corporation Low dose combination therapy for treatment of myeloproliferative neoplasms
SG11202007164UA (en) 2018-01-30 2020-08-28 Incyte Corp Processes for preparing (1 -(3-fluoro-2-(trifluoromethyl)isonicotinyl)piperidine-4-one)
SMT202400306T1 (it) 2018-03-30 2024-09-16 Incyte Corp Trattamento dell'idrosadenite suppurativa utilizzando inibitori di jak.
US11339168B2 (en) 2019-02-22 2022-05-24 Kronos Bio, Inc. Crystalline forms of 6-(6-aminopyrazin-2-yl)-N-(4-(4-(oxetan-3-yl)piperazin-1-yl)phenyl)imidazo[1,2-a]pyrazin-8-amine as Syk inhibitors
EP3947737A2 (en) 2019-04-02 2022-02-09 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods of predicting and preventing cancer in patients having premalignant lesions
EP3955920A1 (en) 2019-04-16 2022-02-23 Institut National de la Santé et de la Recherche Médicale (INSERM) Use of jak inhibitors for the treatment of painful conditions involving nav1.7 channels
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
WO2021249417A1 (zh) * 2020-06-09 2021-12-16 赛诺哈勃药业(成都)有限公司 杂环化合物及其衍生物
WO2023222565A1 (en) 2022-05-16 2023-11-23 Institut National de la Santé et de la Recherche Médicale Methods for assessing the exhaustion of hematopoietic stems cells induced by chronic inflammation
CN119630668A (zh) * 2022-07-25 2025-03-14 细胞基因公司 取代的咪唑并吡嗪化合物作为irak3结合剂

Family Cites Families (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1345449A (en) * 1971-05-14 1974-01-30 Science Union & Cie Pyridylpiperazines and process for their preparation
US4876256A (en) * 1988-04-29 1989-10-24 Merck & Co., Inc. Alkylpiperazinylpyridines as hypoglycemic agents
US5494908A (en) * 1992-11-23 1996-02-27 Hoechst-Roussel Pharmaceutical Incorporated Substituted 3-(aminoalkylamino)-1,2-benzisoxazoles and related compounds
US5654307A (en) * 1994-01-25 1997-08-05 Warner-Lambert Company Bicyclic compounds capable of inhibiting tyrosine kinases of the epidermal growth factor receptor family
US6231833B1 (en) * 1999-08-05 2001-05-15 Pfizer Inc 2,7-substituted octahydro-1H-pyrido[1,2-A]pyrazine derivatives as ligands for serotonin receptors
JPH09132529A (ja) * 1995-11-09 1997-05-20 Ono Pharmaceut Co Ltd 一酸化窒素合成酵素阻害剤
US5958919A (en) * 1996-09-20 1999-09-28 Washington University Treatment of presymptomatic alzheimer's disease to prevent neuronal degeneration
CA2322311C (en) * 1998-03-04 2009-10-13 Bristol-Myers Squibb Company Heterocyclo-substituted imidazopyrazine protein tyrosine kinase inhibitors
SK286640B6 (sk) * 1998-06-19 2009-03-05 Pfizer Products Inc. Pyrol [2,3-d] pyrimidínová zlúčenina, jej použitie na výrobu liečiva, farmaceutická kompozícia s jej obsahom, použitie jej kombinácie s ďalšími činidlami a súpravy s jej obsahom na výrobu liečiva
EP0982030A3 (en) * 1998-08-17 2000-05-10 Pfizer Products Inc. 2,7-substituted octahydro-pyrrolo 1,2-a]pyrazine derivatives as 5ht 1a ligands
DE69914357T2 (de) * 1998-11-04 2004-11-11 Smithkline Beecham Corp. Pyridin-4-yl oder pyrimidin-4-yl substituierte pyrazine
CN1660840A (zh) * 1999-03-30 2005-08-31 诺瓦提斯公司 治疗炎性疾病的酞嗪衍生物
AU779908B2 (en) * 1999-09-10 2005-02-17 Merck & Co., Inc. Tyrosine kinase inhibitors
JP2003516974A (ja) * 1999-12-17 2003-05-20 カイロン コーポレイション グリコーゲンシンターゼキナーゼ3のピラジンベースインヒビター
US6335342B1 (en) * 2000-06-19 2002-01-01 Pharmacia & Upjohn S.P.A. Azaindole derivatives, process for their preparation, and their use as antitumor agents
EP1317266A2 (en) * 2000-08-08 2003-06-11 Ortho-McNeil Pharmaceutical, Inc. Neuroprotective 2-pyridinamine compositions and related methods
DE60118025T2 (de) * 2000-10-24 2006-11-23 Merck & Co., Inc. Dibenzoxazepin-alpha-v-integrin-rezeptorantagonist
CA2450769A1 (en) * 2001-06-15 2002-12-27 Vertex Pharmaceuticals Incorporated 5-(2-aminopyrimidin-4-yl) benzisoxazoles as protein kinase inhibitors

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006059245A3 (en) * 2004-11-16 2006-10-05 Neurochem Int Ltd Compounds for the treatment of cns and amyloid associated diseases

Also Published As

Publication number Publication date
US20060069084A1 (en) 2006-03-30
US20040102455A1 (en) 2004-05-27
EP1363702A1 (en) 2003-11-26
JP2004528295A (ja) 2004-09-16
EP1363702A4 (en) 2007-08-22
WO2002060492A1 (en) 2002-08-08

Similar Documents

Publication Publication Date Title
CA2436487A1 (en) Methods of inhibiting kinases
US7598272B2 (en) Kinase inhibitors
RU2632900C2 (ru) Гетероциклические амины и их применение
CA2545427C (en) Selective kinase inhibitors
KR102510588B1 (ko) 카텝신 c의 스피로사이클릭 억제제
EP1689739B1 (en) Azole-based kinase inhibitors
WO2021258010A1 (en) Oxime compounds useful as t cell activators
CN102015717A (zh) 趋化因子受体调节剂
JP2023520759A (ja) がん治療のための置換オキソイソインドリン化合物
JP2010527999A (ja) PKC−θ阻害剤としてのプリノン類および1H−イミダゾピリジノン類
CN107438598A (zh) 喹唑啉和喹啉化合物及其用途
JP2018512062A (ja) Tnf阻害剤として有用なヘテロ環式化合物
US20190241574A1 (en) Phenyl phthalazine derivative, method for the preparation thereof, and pharmaceutical composition comprising the same
WO2007063935A1 (ja) 芳香族化合物
AU2002226197B2 (en) Methods of inhibiting kinases
AU2002226197A1 (en) Methods of inhibiting kinases
ZA200409346B (en) Kinase inhibitors.
JP2016525071A (ja) ヤーヌスキナーゼのインヒビターとしてのn−シアノメチルアミド
CN121127464A (zh) Lrrk2的抑制剂
AU2004294355A1 (en) Azole-based kinase inhibitors
HK40019824B (en) Therapeutic compounds and compositions, and methods of use thereof

Legal Events

Date Code Title Description
EEER Examination request
FZDE Discontinued