HRP20000209A2 - Bicyclic kinase inhibitors - Google Patents

Bicyclic kinase inhibitors Download PDF

Info

Publication number
HRP20000209A2
HRP20000209A2 HR20000209A HRP20000209A HRP20000209A2 HR P20000209 A2 HRP20000209 A2 HR P20000209A2 HR 20000209 A HR20000209 A HR 20000209A HR P20000209 A HRP20000209 A HR P20000209A HR P20000209 A2 HRP20000209 A2 HR P20000209A2
Authority
HR
Croatia
Prior art keywords
alkyl
hydrogen
amino
heteroalkyl
formula
Prior art date
Application number
HR20000209A
Other languages
English (en)
Croatian (hr)
Inventor
Soan Cheng
David
Teresa
Eric Brian Sjogren
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of HRP20000209A2 publication Critical patent/HRP20000209A2/hr

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/70—Sulfur atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A61P31/06—Antibacterial agents for tuberculosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/04—Immunostimulants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/02—Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/26—Radicals substituted by halogen atoms or nitro radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/72—Nitrogen atoms
    • C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/72—Nitrogen atoms
    • C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D237/10—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-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
    • C07D237/20—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic 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
    • C07D241/14—Heterocyclic 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
    • C07D241/18—Oxygen or sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Biomedical Technology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pulmonology (AREA)
  • Hospice & Palliative Care (AREA)
  • Transplantation (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Urology & Nephrology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Psychology (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
HR20000209A 1997-10-20 1998-10-13 Bicyclic kinase inhibitors HRP20000209A2 (en)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US6254897P 1997-10-20 1997-10-20
US7551598P 1998-02-20 1998-02-20
US9691698P 1998-08-18 1998-08-18
PCT/EP1998/006472 WO1999020624A1 (en) 1997-10-20 1998-10-13 Bicyclic kinase inhibitors

Publications (1)

Publication Number Publication Date
HRP20000209A2 true HRP20000209A2 (en) 2001-04-30

Family

ID=27370326

Family Applications (1)

Application Number Title Priority Date Filing Date
HR20000209A HRP20000209A2 (en) 1997-10-20 1998-10-13 Bicyclic kinase inhibitors

Country Status (26)

Country Link
US (4) US6316464B1 (de)
EP (1) EP1025102B1 (de)
JP (1) JP3579350B2 (de)
KR (1) KR100378937B1 (de)
CN (1) CN1279682A (de)
AT (1) ATE267200T1 (de)
AU (1) AU745579B2 (de)
BR (1) BR9812944A (de)
CA (1) CA2306870A1 (de)
CO (1) CO4980857A1 (de)
DE (1) DE69824029T2 (de)
ES (1) ES2221213T3 (de)
HR (1) HRP20000209A2 (de)
HU (1) HUP0100348A3 (de)
ID (1) ID27124A (de)
IL (1) IL135302A0 (de)
MA (1) MA26555A1 (de)
NO (1) NO316734B1 (de)
NZ (1) NZ503685A (de)
PE (1) PE120999A1 (de)
PL (1) PL340412A1 (de)
RU (1) RU2219178C2 (de)
TR (1) TR200001079T2 (de)
TW (1) TWI224596B (de)
WO (1) WO1999020624A1 (de)
YU (1) YU22000A (de)

Families Citing this family (91)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE69728688T2 (de) * 1996-11-19 2004-08-19 Amgen Inc., Thousand Oaks Aryl und heteroaryl substituierte kondensierte pyrrole als entzündunghemmende mittel
AU4994899A (en) * 1998-07-13 2000-02-01 University Of South Florida Modulation of the phospholipase a2 pathway as a therapeutic
CA2346665A1 (en) 1998-10-07 2000-04-13 Smithkline Beecham Corporation Novel treatment for stroke management
CA2348740A1 (en) * 1998-12-23 2000-07-06 Ruth R. Wexler Thrombin or factor xa inhibitors
KR100523120B1 (ko) * 1999-10-21 2005-10-20 에프. 호프만-라 로슈 아게 Ｐ38 단백질 키나제 저해제로서 헤테로알킬아미노-치환된이환 질소 헤테로환
PL357494A1 (en) * 1999-10-21 2004-07-26 F.Hoffmann-La Roche Ag Alkylamino substituted bicyclic nitrogen heterocycles as inhibitors of p38 protein kinase
AU7922900A (en) * 1999-10-27 2001-05-08 Novartis Ag Thiazole and imidazo (4,5-b) pyridine compounds and their pharmaceutical use
GB9930698D0 (en) * 1999-12-24 2000-02-16 Rhone Poulenc Rorer Ltd Chemical compounds
EP1990343B1 (de) * 1999-12-24 2012-04-04 Aventis Pharma Limited Azaindole
GB0112348D0 (en) * 2001-05-19 2001-07-11 Smithkline Beecham Plc Compounds
GB0115109D0 (en) * 2001-06-21 2001-08-15 Aventis Pharma Ltd Chemical compounds
US20030216396A1 (en) 2002-02-11 2003-11-20 Bayer Corporation Pyridine, quinoline, and isoquinoline N-oxides as kinase inhibitors
US20090306182A1 (en) * 2002-02-20 2009-12-10 Sirna Therapeutics, Inc. RNA INTERFERENCE MEDIATED INHIBITION OF MAP KINASE GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA)
RU2301233C2 (ru) * 2002-03-07 2007-06-20 Ф.Хоффманн-Ля Рош Аг Бициклические пиридины и пиримидины в качестве ингибиторов киназы р38
KR20040111445A (ko) * 2002-03-28 2004-12-31 에자이 가부시키가이샤 신경퇴행성 질환 치료용 ｃ─Ｊｕｎ Ｎ─말단 키나아제억제제로서의 ７─아자인돌
KR20050004214A (ko) * 2002-05-31 2005-01-12 에자이 가부시키가이샤 피라졸 화합물 및 이것을 포함하여 이루어지는 의약 조성물
SG135051A1 (en) * 2002-06-20 2007-09-28 Aventis Pharma Ltd Azaindoles
CA2492112A1 (en) * 2002-08-06 2004-02-19 F. Hoffmann-La Roche Ag 6-alkoxy-pyrido-pyrimidines as p-38 map kinase inhibitors
EP1388541A1 (de) * 2002-08-09 2004-02-11 Centre National De La Recherche Scientifique (Cnrs) Pyrrolopyrazine als Kinasehemmer
WO2004053107A2 (en) * 2002-12-06 2004-06-24 Scios Inc. Methods for treating diabetes
US20040225077A1 (en) 2002-12-30 2004-11-11 Angiotech International Ag Drug delivery from rapid gelling polymer composition
US7135575B2 (en) 2003-03-03 2006-11-14 Array Biopharma, Inc. P38 inhibitors and methods of use thereof
MXPA05009459A (es) * 2003-03-03 2006-05-17 Array Biopharma Inc Inhibidores de p38 y sus metodos de uso.
GB0305142D0 (en) 2003-03-06 2003-04-09 Eisai London Res Lab Ltd Synthesis
EP1599475A2 (de) 2003-03-06 2005-11-30 Eisai Co., Ltd. Jnk-hemmer
US7687506B2 (en) * 2003-04-11 2010-03-30 The Regents Of The University Of California Selective serine/threonine kinase inhibitors
CN1809351A (zh) * 2003-04-24 2006-07-26 麦克公司 Akt活性抑制剂
US7902192B2 (en) 2003-05-15 2011-03-08 Arqule, Inc. Inhibitors of P38 and methods of using the same
WO2004101565A2 (en) * 2003-05-16 2004-11-25 Eisai Co., Ltd. Jnk inhibitors
EP1631145A4 (de) * 2003-06-06 2009-12-23 Univ Pennsylvania P38-kinasehemmer-zusammensetzung sowie verfahren zu deren verwendung
SE0301906D0 (sv) * 2003-06-26 2003-06-26 Astrazeneca Ab New compounds
US7202363B2 (en) * 2003-07-24 2007-04-10 Abbott Laboratories Thienopyridine and furopyridine kinase inhibitors
US20050026944A1 (en) * 2003-07-24 2005-02-03 Patrick Betschmann Thienopyridine and furopyridine kinase inhibitors
ES2365617T3 (es) 2003-11-25 2011-10-07 Virginia Tech Intellectual Properties, Inc. Composición para su consumo en animales y método para reducir la actividad de map quinasa.
KR100703068B1 (ko) * 2003-12-30 2007-04-05 에스케이케미칼주식회사 피리딘 유도체와 이의 제조방법, 및 이를 포함하는약제조성물
US7504403B2 (en) * 2004-01-22 2009-03-17 Amgen Inc. Substituted heterocyclic compounds and methods of use
GB0405055D0 (en) * 2004-03-05 2004-04-07 Eisai London Res Lab Ltd JNK inhibitors
WO2005091891A2 (en) * 2004-03-11 2005-10-06 Kythera Biopharmaceuticals, Inc. Compositions and methods for preventing and treating skin and hair conditions
US20050203111A1 (en) * 2004-03-12 2005-09-15 Vvii Newco 2003, Inc. Compositions and methods for preventing and treating skin and hair conditions
WO2006010082A1 (en) 2004-07-08 2006-01-26 Arqule, Inc. 1,4-disubstituted naphtalenes as inhibitors of p38 map kinase
US20080113016A1 (en) * 2004-07-26 2008-05-15 Gary Steven Firestein Method for Prevention or Treatment of Inflammatory Disease
US7465726B2 (en) * 2004-08-02 2008-12-16 Osi Pharmaceuticals, Inc. Substituted pyrrolo[2.3-B]pyridines
EP2258704A1 (de) 2004-10-19 2010-12-08 ArQule, Inc. Synthese aus Imidazooxazol- und Imidazothiazol-hemmern der P38-map-kinase
US20090131430A1 (en) * 2004-11-23 2009-05-21 Palle Venkata P Pyrido'2,3-dipyrimidines as anti-inflammatory agents
EP1846403A1 (de) * 2005-02-02 2007-10-24 Ranbaxy Laboratories Limited Azabicycloderivate als entzündungshemmende mittel
KR101142363B1 (ko) * 2005-06-27 2012-05-21 주식회사유한양행 피롤로피리딘 유도체를 포함하는 항암제 조성물
GB0516156D0 (en) * 2005-08-05 2005-09-14 Eisai London Res Lab Ltd JNK inhibitors
WO2007031098A1 (en) 2005-09-12 2007-03-22 Xigen S.A. Cell-permeable peptide inhibitors of the jnk signal transduction pathway
AU2007210073B2 (en) * 2006-01-31 2011-10-06 Array Biopharma Inc. Kinase inhibitors and methods of use thereof
CA2641254A1 (en) * 2006-02-14 2007-08-23 Vertex Pharmaceuticals Incorporated Pyrrolo(3,2-c) pyridines useful as inhibitors of protein kinases
CL2007002617A1 (es) 2006-09-11 2008-05-16 Sanofi Aventis Compuestos derivados de pirrolo[2,3-b]pirazin-6-ilo; composicion farmaceutica que comprende a dichos compuestos; y su uso para tratar inflamacion de las articulaciones, artritis reumatoide, tumores, linfoma de las celulas del manto.
US7687893B2 (en) 2006-12-27 2010-03-30 Amkor Technology, Inc. Semiconductor package having leadframe with exposed anchor pads
CA2681420A1 (en) * 2007-03-20 2008-09-25 Cadila Pharmaceuticals Limited P38 inhibitors
GB0708141D0 (en) * 2007-04-26 2007-06-06 Syngenta Participations Ag Improvements in or relating to organic compounds
WO2009143864A1 (en) 2008-05-30 2009-12-03 Xigen S.A. Use of cell-permeable peptide inhibitors of the jnk signal transduction pathway for the treatment of chronic or non-chronic inflammatory digestive diseases
WO2009143865A1 (en) 2008-05-30 2009-12-03 Xigen S.A. Use of cell-permeable peptide inhibitors of the jnk signal transduction pathway for the treatment of various diseases
US8119637B2 (en) * 2008-06-10 2012-02-21 Plexxikon Inc. Substituted pyrrolo[2,3-b]pyrazines and methods for kinase modulation, and indications therefor
WO2010046215A2 (en) * 2008-10-21 2010-04-29 Syngenta Participations Ag Diaza-indole derivatives and their use as fungicides
DE102008052943A1 (de) * 2008-10-23 2010-04-29 Merck Patent Gmbh Azaindolderivate
KR101639642B1 (ko) 2008-12-05 2016-07-14 애브비 바하마스 리미티드 암 치료에 사용하기 위한 키나제 억제제로서의 티에노［3,2-ｃ］피리딘 유도체
JP6093110B2 (ja) 2008-12-17 2017-03-08 ザ スクリプス リサーチ インスティテュート 幹細胞の作製と維持
WO2010072228A1 (en) 2008-12-22 2010-07-01 Xigen S.A. Novel transporter constructs and transporter cargo conjugate molecules
US20170117214A1 (en) 2009-01-05 2017-04-27 Amkor Technology, Inc. Semiconductor device with through-mold via
EP2245936A1 (de) 2009-04-27 2010-11-03 Bayer CropScience AG Verwendung von 4-Azaindolderivaten zur Verringerung von Mykotoxinkontamination
EP2338890A1 (de) 2009-12-22 2011-06-29 Bayer CropScience AG 4,7-Diazaindolderivate und ihre Verwendung als Fungizide
JP2013525304A (ja) * 2010-04-16 2013-06-20 アッヴィ・インコーポレイテッド ピロロピラジノン系キナーゼ阻害薬
WO2011160653A1 (en) 2010-06-21 2011-12-29 Xigen S.A. Novel jnk inhibitor molecules
US9150618B2 (en) 2010-10-14 2015-10-06 Xigen Inflammation Ltd. Use of cell-permeable peptide inhibitors of the JNK signal transduction pathway for the treatment of chronic or non-chronic inflammatory eye diseases
WO2013012909A1 (en) 2011-07-20 2013-01-24 Abbott Laboratories Kinase inhibitor with improved aqueous solubility
BR112014005104A2 (pt) * 2011-09-02 2017-07-04 Salk Inst For Biological Studi inibidores camkii, ip3r, calcineurin, p38 e mk2/3 para tratar atar distúrbios metabólicos de obesidade
WO2013091670A1 (en) 2011-12-21 2013-06-27 Xigen S.A. Novel jnk inhibitor molecules for treatment of various diseases
WO2013162027A1 (ja) 2012-04-27 2013-10-31 学校法人 慶應義塾 神経分化促進剤
GB201304526D0 (en) 2013-03-13 2013-04-24 Proximagen Ltd New compounds
HRP20181392T1 (hr) 2013-03-15 2018-10-19 Plexxikon Inc. Heterociklični spojevi i njihova uporaba
US20140303121A1 (en) 2013-03-15 2014-10-09 Plexxikon Inc. Heterocyclic compounds and uses thereof
WO2014206563A2 (en) * 2013-06-26 2014-12-31 Xigen Inflammation Ltd. New use of cell-permeable peptide inhibitors of the jnk signal transduction pathway for the treatment of various diseases
WO2014206427A1 (en) 2013-06-26 2014-12-31 Xigen Inflammation Ltd. New use of cell-permeable peptide inhibitors of the jnk signal transduction pathway for the treatment of various diseases
WO2015197097A1 (en) 2014-06-26 2015-12-30 Xigen Inflammation Ltd. New use for jnk inhibitor molecules for treatment of various diseases
EP3033087A4 (de) 2013-08-16 2017-03-15 The J. David Gladstone Institutes Zusammensetzungen und verfahre zur identifizierung von latent infizierten zellen
WO2015173788A1 (en) 2014-05-16 2015-11-19 Westfaelische Wilhelms-Universitaet Muenster Novel anti-infective strategy against influenza virus and s. aureus coinfections
AR103232A1 (es) 2014-12-22 2017-04-26 Bristol Myers Squibb Co ANTAGONISTAS DE TGFbR
EP3368052B1 (de) 2015-10-27 2021-12-08 Children's Hospital Medical Center Verwendung von mapk-inhibitoren zur verringerung des verlusts hämatopoetischer stammzellen während der ex-vivo-kultivierung und genetischen manipulation
US10342786B2 (en) 2017-10-05 2019-07-09 Fulcrum Therapeutics, Inc. P38 kinase inhibitors reduce DUX4 and downstream gene expression for the treatment of FSHD
WO2019071144A1 (en) 2017-10-05 2019-04-11 Fulcrum Therapeutics, Inc. USE OF P38 INHIBITORS TO REDUCE DUX4 EXPRESSION
US10717735B2 (en) 2017-10-13 2020-07-21 Plexxikon Inc. Solid forms of a compound for modulating kinases
JP7289301B2 (ja) 2017-12-18 2023-06-09 ブリストル－マイヤーズ スクイブ カンパニー ４－アザインドール化合物
CA3128946A1 (en) 2019-02-07 2020-08-13 Bayer Aktiengesellschaft 3-amino-2-[2-(acylamino)pyridin-4-yl]-1,5,6,7-tetrahydro-4h-pyrrolo[3,2-c]pyridin-4-one as csnk1 inhibitors
EP4188928B1 (de) 2020-07-29 2024-07-24 Bayer Aktiengesellschaft Substituierte 1h-pyrrolo[3,2-b pyridin-verbindungen und anwendungsverfahren dafür
US20230322767A1 (en) 2020-07-29 2023-10-12 Bayer Aktiengesellschaft Aryl substituted pyrrolo-pyridinones and therapeutic uses thereof
WO2023280911A1 (en) 2021-07-06 2023-01-12 Westfälische Wilhelms-Universität Münster P38-inhibitors for the treatment of coronavirus infections and/or covid-19 cytokine storm
EP4469457A4 (de) * 2022-01-27 2026-01-21 Broad Inst Inc Substituierte heterocyclische csnk1-inhibitoren

Family Cites Families (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SU371228A1 (ru) 1971-04-02 1973-02-22 Всесоюзный научно исследовательский химико фармацевтический институт Серго Орджоникидзе Способ получения пирроло-
RO62428A (fr) 1971-05-04 1978-01-15 Thomae Gmbh Dr K Procede pour la preparation des thyeno-(3,2-d)-pyrimidines
JPS56104870A (en) 1980-01-25 1981-08-20 Dai Ichi Seiyaku Co Ltd 2-halogeno-3,4-dihydro-condensed pyrimidine and its preparation
US4767766A (en) * 1987-01-30 1988-08-30 Merck & Co., Inc. Derivatives of 3-hydroxyazabenzo(B)thiophene useful as 5-lipoxygenase inhibitors
EP0300688A1 (de) 1987-07-21 1989-01-25 FISONS plc Pyrrol-Derivate, Verfahren zu ihrer Herstellung und pharmazeutische Zusammenstellungen, die sie enthalten
US5236925A (en) 1991-10-24 1993-08-17 American Home Products Corporation Fused pyrimidines as angiotensin II antagonists
FR2687402B1 (fr) 1992-02-14 1995-06-30 Lipha Nouveaux azaindoles, procedes de preparation et medicaments les contenant.
US5502187A (en) 1992-04-03 1996-03-26 The Upjohn Company Pharmaceutically active bicyclic-heterocyclic amines
DE4304650A1 (de) 1993-02-16 1994-08-18 Thomae Gmbh Dr K Kondensierte 5-gliedrige Heterocyclen, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende Arzneimittel
US6756388B1 (en) 1993-10-12 2004-06-29 Pfizer Inc. Benzothiophenes and related compounds as estrogen agonists
CA2134192A1 (en) 1993-11-12 1995-05-13 Michael L. Denney 5, 6-bicyclic glycoprotein iib/iiia antagonists
US5468757A (en) 1994-01-31 1995-11-21 Eli Lilly And Company 6-azaindole thromboxane synthase inhibitors
EP0766684A4 (de) 1994-06-09 1997-07-16 Smithkline Beecham Corp Endothelin-rezeptor antagonisten
WO1995033748A1 (en) 1994-06-09 1995-12-14 Smithkline Beecham Corporation Endothelin receptor antagonists
US5521213A (en) 1994-08-29 1996-05-28 Merck Frosst Canada, Inc. Diaryl bicyclic heterocycles as inhibitors of cyclooxygenase-2
US5589482A (en) 1994-12-14 1996-12-31 Pfizer Inc. Benzo-thiophene estrogen agonists to treat prostatic hyperplasia
GB2298199A (en) 1995-02-21 1996-08-28 Merck Sharp & Dohme Synthesis of azaindoles
FR2732969B1 (fr) 1995-04-14 1997-05-16 Adir Nouveaux composes pyridiniques, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
AU699148B2 (en) * 1995-08-10 1998-11-26 Merck & Co., Inc. 2,5-substituted aryl pyrroles, compositions containing such compounds and methods of use
AU3176297A (en) 1996-06-25 1998-01-14 Novartis Ag Substituted 7-amino-pyrrolo{3,2-d}pyrimidines and the use thereof
DE69728688T2 (de) * 1996-11-19 2004-08-19 Amgen Inc., Thousand Oaks Aryl und heteroaryl substituierte kondensierte pyrrole als entzündunghemmende mittel
WO1998047899A1 (en) 1997-04-24 1998-10-29 Ortho-Mcneil Corporation, Inc. Substituted pyrrolopyridines useful in the treatment of inflammatory diseases

Also Published As

Publication number Publication date
NO20001940L (no) 2000-04-13
ES2221213T3 (es) 2004-12-16
US20020013354A1 (en) 2002-01-31
NO20001940D0 (no) 2000-04-13
US6316464B1 (en) 2001-11-13
AU9749998A (en) 1999-05-10
US6630485B2 (en) 2003-10-07
US6479507B2 (en) 2002-11-12
NO316734B1 (no) 2004-04-19
CA2306870A1 (en) 1999-04-29
EP1025102B1 (de) 2004-05-19
JP3579350B2 (ja) 2004-10-20
HUP0100348A3 (en) 2002-12-28
PE120999A1 (es) 1999-12-01
DE69824029D1 (de) 2004-06-24
AU745579B2 (en) 2002-03-21
IL135302A0 (en) 2001-05-20
NZ503685A (en) 2002-05-31
ID27124A (id) 2001-03-01
PL340412A1 (en) 2001-01-29
RU2219178C2 (ru) 2003-12-20
KR100378937B1 (ko) 2003-05-09
US20010044538A1 (en) 2001-11-22
YU22000A (sh) 2003-01-31
WO1999020624A1 (en) 1999-04-29
TWI224596B (en) 2004-12-01
CO4980857A1 (es) 2000-11-27
US20030139462A1 (en) 2003-07-24
EP1025102A1 (de) 2000-08-09
HUP0100348A2 (hu) 2001-08-28
MA26555A1 (fr) 2004-12-20
DE69824029T2 (de) 2005-05-12
KR20010031285A (ko) 2001-04-16
JP2001520227A (ja) 2001-10-30
BR9812944A (pt) 2000-08-08
CN1279682A (zh) 2001-01-10
TR200001079T2 (tr) 2000-07-21
ATE267200T1 (de) 2004-06-15

Similar Documents

Publication Publication Date Title
AU745579B2 (en) Bicyclic kinase inhibitors
JP4801724B2 (ja) ｍＧｌｕＲ２アンタゴニストとしてのアセチレニル−ピラゾロ−ピリミジン誘導体
US8138173B2 (en) Pyrazolo[3,4-C]quinolines, pyrazolo[3,4-C]naphthyridines, analogs thereof, and methods
US7566708B2 (en) Substituted pyrazolo{3,4-D}pyrimidines as p38 map kinase inhibitors
US7528138B2 (en) Pyrazolo[1,5-a]pyrimidines useful as inhibitors of protein kinases
EP2325184A1 (de) Als Hemmer von Proteinkinasen verwendbare Azaindole
AU2008224785B2 (en) Azabicycloalkane derivatives, preparation thereof and use thereof in therapy
MXPA00003810A (en) Bicyclic kinase inhibitors
CZ20001308A3 (cs) Bicyklické inhibitory kinasy
TW200303316A (en) Substituted indolizine-like compounds and methods of use
MXPA06009465A (en) Fused derivatives of pyrazole

Legal Events

Date Code Title Description
A1OB Publication of a patent application
ARAI Request for the grant of a patent on the basis of the submitted results of a substantive examination of a patent application
OBST Application withdrawn