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PE20060583A1 - Tiazolil-dihidro-indazoles como inhibidores de pi3-quinasas - Google Patents

Tiazolil-dihidro-indazoles como inhibidores de pi3-quinasas

Info

Publication number
PE20060583A1
PE20060583A1 PE2005001178A PE2005001178A PE20060583A1 PE 20060583 A1 PE20060583 A1 PE 20060583A1 PE 2005001178 A PE2005001178 A PE 2005001178A PE 2005001178 A PE2005001178 A PE 2005001178A PE 20060583 A1 PE20060583 A1 PE 20060583A1
Authority
PE
Peru
Prior art keywords
kinases
inhibitors
tiazolil
dihidro
indazoles
Prior art date
Application number
PE2005001178A
Other languages
English (en)
Inventor
Bodo Betzemeier
Trixi Brandl
Ralph Bruckner
Michael Gmachl
Frank Hilberg
Matthias Hoffmann
Dirk Kessler
Bernd Krist
Steffen Steurer
Martin Steegmaier
Oliver Simon
Norbert Schweifer
Andreas Schoop
Stefan Scheuerer
Charlotte Reither
Darryl Mcconnell
Udo Maier
Andreas Zophel
Ulrike Weyer-Czernilofsky
Irene Waizenegger
Christian Klein
Maria Impagnatiello
Christoph Hoenke
Matthias Grauert
Thomas Gerstberger
Steffen Breitfelder
Original Assignee
Boehringer Ingelheim Int
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 DE102004048877A external-priority patent/DE102004048877A1/de
Priority claimed from DE102005005813A external-priority patent/DE102005005813A1/de
Application filed by Boehringer Ingelheim Int filed Critical Boehringer Ingelheim Int
Publication of PE20060583A1 publication Critical patent/PE20060583A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04Ortho-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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425Thiazoles
    • A61K31/428Thiazoles condensed with carbocyclic rings
    • 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
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • 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
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • 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
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10Antimycotics
    • 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
    • A61P33/00Antiparasitic agents
    • 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
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62Benzothiazoles
    • C07D277/68Benzothiazoles 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 in position 2
    • C07D277/82Nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/84Naphthothiazoles
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Immunology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Virology (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Neurosurgery (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Transplantation (AREA)
  • Molecular Biology (AREA)
  • Hospice & Palliative Care (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Psychiatry (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • AIDS & HIV (AREA)
  • Urology & Nephrology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

SE REFIERE A UN COMPUESTO DE FORMULA (I) DONDE R1 ES NHRc, NHC(O)RC, NHC(O)ORC, ENTRE OTROS; DONDE RC ES H O UN RADICAL SUSTITUIDO CON ALQUILO(C1-C6), CICLOALQUILO(C3-C8), ARILO(C6-C10), ENTRE OTROS; R2 ES UN RADICAL SUSTITUIDO TAL COMO ALQUILO(C1-C6), CICLOALQUILO(C3-C8), HETEROCICLOALQUILO(C3-C8), ENTRE OTROS; R3 ES UN RADICAL SUSTITUIDO SELECCIONADO ENTRE ARILO C(6-C10), HETEROARILO DE 5 A 10 MIEMBROS, ENTRE OTROS. ES COMPUESTO PREFERIDO: N-[1-(2-CLORO-4-MORFOLINCARBONIL-FENIL-4,5-DIHIDRO-1H-PIRAZOLO[3´,4´:3,4]BENZ[1,2-d]TIAZOL-7-IL]-ACETAMIDA. DICHOS COMPUESTOS SON INHIBIDORES DE LA FOSFATIDILINOSITOL-3-QUINASA (PI3-QUINASAS) SIENDO UTILES PARA EL TRATAMIENTO DE ENFERMEDADES QUE SE CARACTERIZAN POR UNA PROLIFERACION CELULAR EXCESIVA O ANORMAL
PE2005001178A 2004-10-07 2005-10-05 Tiazolil-dihidro-indazoles como inhibidores de pi3-quinasas PE20060583A1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DE102004048877A DE102004048877A1 (de) 2004-10-07 2004-10-07 PI3-Kinasen
DE102005005813A DE102005005813A1 (de) 2005-02-09 2005-02-09 PI3-Kinasen
EP05107230 2005-08-05

Publications (1)

Publication Number Publication Date
PE20060583A1 true PE20060583A1 (es) 2006-08-17

Family

ID=35448324

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2005001178A PE20060583A1 (es) 2004-10-07 2005-10-05 Tiazolil-dihidro-indazoles como inhibidores de pi3-quinasas

Country Status (23)

Country Link
EP (1) EP1799690B1 (es)
JP (1) JP5090914B2 (es)
KR (1) KR20070113188A (es)
CN (1) CN101035795B (es)
AR (1) AR051743A1 (es)
AT (1) ATE392425T1 (es)
AU (1) AU2005293609B2 (es)
BR (1) BRPI0518169A (es)
CA (1) CA2579288A1 (es)
CY (1) CY1108183T1 (es)
DE (1) DE502005003777D1 (es)
DK (1) DK1799690T3 (es)
ES (1) ES2304022T3 (es)
IL (1) IL182397A (es)
MX (1) MX2007003802A (es)
NZ (1) NZ554695A (es)
PE (1) PE20060583A1 (es)
PL (1) PL1799690T3 (es)
PT (1) PT1799690E (es)
SI (1) SI1799690T1 (es)
TW (1) TW200630374A (es)
UY (1) UY29149A1 (es)
WO (1) WO2006040281A1 (es)

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BRPI0709612A2 (pt) 2006-03-15 2011-07-19 Wyeth Corp composto de fórmula i; método para o tratamento de um distúrbio no sistema nervoso central relacionado ou afetado pelo receptor histamina-3 em um paciente que necessita deste tratamento; método para a inibição do receptor h3; composição farmacêutica; e processo para a preparação de um composto de fórmula i
US7517995B2 (en) 2006-04-06 2009-04-14 Boehringer Ingelheim International Gmbh Thiazolyl-dihydro-cyclopentapyrazole
CA2646536A1 (en) * 2006-04-06 2007-10-11 Boehringer Ingelheim International Gmbh Thiazolyl dihydro-indazoles
AU2007233729A1 (en) * 2006-04-06 2007-10-11 Boehringer Ingelheim International Gmbh Thiazolyldihydroindazole derivatives as protein kinase inhibitors
US20070259855A1 (en) * 2006-04-06 2007-11-08 Udo Maier Thiazolyl-dihydro-indazole
US20070238718A1 (en) * 2006-04-06 2007-10-11 Matthias Grauert Thiazolyl-dihydro-indazole
US7691868B2 (en) 2006-04-06 2010-04-06 Boehringer Ingelheim International Gmbh Thiazolyl-dihydro-quinazoline
US20070238746A1 (en) 2006-04-06 2007-10-11 Trixi Brandl Thiazolyl-dihydro-chinazoline
CA2649913A1 (en) 2006-05-19 2007-11-29 Wyeth N-benzoyl- and n-benzylpyrrolidin-3-ylamines as histamine-3 antagonists
WO2008001883A1 (en) * 2006-06-29 2008-01-03 Nissan Chemical Industries, Ltd. α-AMINO ACID DERIVATIVE AND PHARMACEUTICAL COMPRISING THE SAME AS ACTIVE INGREDIENT
US8779154B2 (en) 2006-09-26 2014-07-15 Qinglin Che Fused ring compounds for inflammation and immune-related uses
PE20081152A1 (es) * 2006-10-06 2008-08-10 Wyeth Corp Azaciclilaminas n-sustituidas como antagonistas de histamina-3
US7803825B2 (en) 2007-07-16 2010-09-28 Wyeth Llc Aminoalkylazole derivatives as histamine-3 antagonists
US8278313B2 (en) 2008-03-11 2012-10-02 Abbott Laboratories Macrocyclic spiro pyrimidine derivatives
UY31700A (es) 2008-03-13 2009-11-10 Boehringer Ingelheim Int Tiazolil-dihidro-indazoles
US8436005B2 (en) 2008-04-03 2013-05-07 Abbott Laboratories Macrocyclic pyrimidine derivatives
WO2010007943A1 (ja) * 2008-07-17 2010-01-21 旭化成ファーマ株式会社 含窒素複素環化合物
JP5579724B2 (ja) 2008-10-17 2014-08-27 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング ホスファチジルイノシトール−3−キナーゼ(pi−3キナーゼ)阻害剤としてのテトラ−アザ−複素環
WO2010122091A1 (en) 2009-04-22 2010-10-28 Boehringer Ingelheim International Gmbh Thia-triaza-as-indacenes as pi3-kinases inhibitors for the treatment of cancer
US8288379B2 (en) * 2009-04-22 2012-10-16 Boehringer Ingelheim International Gmbh Thia-triaza-cyclopentazulenes
JP2012531454A (ja) 2009-07-02 2012-12-10 ノバルティス アーゲー Pi3k阻害剤として有用な2−カルボキサミドシクロアミノウレア類
CA2839621A1 (en) * 2011-06-21 2012-12-27 Novartis Ag Polymorphs of (s)-pyrrolidine-1,2-dicarboxylic acid 2-amide 1-({4-methyl-5-[2-(2,2,2-trifluoro-1,1-dimethyl-ethyl)-pyridin-4-yl]-thiazol-2-yl}-amide
DK4013502T3 (da) * 2019-08-16 2025-11-10 Cyclacel Pharmaceuticals Inc Fremgangsmåde til fremstillingen af et pyrimidino-diazepinderivat
CN112876503B (zh) * 2021-03-18 2022-04-29 中国科学院兰州化学物理研究所 用于癌症硼中子俘获治疗药物的硼酸盐化合物及其制备

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US6608053B2 (en) * 2000-04-27 2003-08-19 Yamanouchi Pharmaceutical Co., Ltd. Fused heteroaryl derivatives
KR100423899B1 (ko) * 2000-05-10 2004-03-24 주식회사 엘지생명과학 세포 증식 억제제로 유용한 1,1-디옥소이소티아졸리딘을갖는 인다졸
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PE20030968A1 (es) * 2002-02-28 2004-01-12 Novartis Ag Derivados de 5-feniltiazol como inhibidores de cinasas

Also Published As

Publication number Publication date
PL1799690T3 (pl) 2008-09-30
AU2005293609B2 (en) 2011-11-24
EP1799690B1 (de) 2008-04-16
JP2008515854A (ja) 2008-05-15
TW200630374A (en) 2006-09-01
JP5090914B2 (ja) 2012-12-05
CY1108183T1 (el) 2014-02-12
UY29149A1 (es) 2006-05-31
DE502005003777D1 (de) 2008-05-29
BRPI0518169A (pt) 2008-11-04
CA2579288A1 (en) 2006-04-20
NZ554695A (en) 2010-12-24
IL182397A0 (en) 2007-07-24
DK1799690T3 (da) 2008-06-30
AR051743A1 (es) 2007-02-07
CN101035795B (zh) 2012-03-21
KR20070113188A (ko) 2007-11-28
PT1799690E (pt) 2008-06-16
CN101035795A (zh) 2007-09-12
AU2005293609A1 (en) 2006-04-20
ES2304022T3 (es) 2008-09-01
ATE392425T1 (de) 2008-05-15
MX2007003802A (es) 2007-04-23
IL182397A (en) 2011-11-30
WO2006040281A1 (de) 2006-04-20
EP1799690A1 (de) 2007-06-27
SI1799690T1 (sl) 2008-08-31

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