PE20040171A1 - Heterociclos biciclicos, medicamentos que contienen estos compuestos su empleo y procedimientos para su preparacion - Google Patents

Heterociclos biciclicos, medicamentos que contienen estos compuestos su empleo y procedimientos para su preparacion

Info

Publication number
PE20040171A1
PE20040171A1 PE2003000384A PE2003000384A PE20040171A1 PE 20040171 A1 PE20040171 A1 PE 20040171A1 PE 2003000384 A PE2003000384 A PE 2003000384A PE 2003000384 A PE2003000384 A PE 2003000384A PE 20040171 A1 PE20040171 A1 PE 20040171A1
Authority
PE
Peru
Prior art keywords
amino
bicycle
phenyl
ilo
buten
Prior art date
Application number
PE2003000384A
Other languages
English (en)
Inventor
Frank Himmelsbach
Flavio Solca
Birgit Jung
Original Assignee
Boehringer Ingelheim Pharma
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 Boehringer Ingelheim Pharma filed Critical Boehringer Ingelheim Pharma
Publication of PE20040171A1 publication Critical patent/PE20040171A1/es

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • 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
    • A61P11/06—Antiasthmatics
    • 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
    • A61P11/08—Bronchodilators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • 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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • 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
    • A61P37/08—Antiallergic agents
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • 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
    • C07D471/08—Bridged 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
    • C07D487/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/08—Bridged systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Diabetes (AREA)
  • Oncology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Dermatology (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Indole Compounds (AREA)

Abstract

SE REFIERE A HETEROCICLOS BICICLICOS DE FORMULA I DONDE Ra ES HIDROGENO, ALQUILO C1-C4; Rb ES FENILO, BENCILO O 1-FENILETILO, ENTRE OTROS; Rc ES HIDROGENO, FLUOR, CLORO, BROMO, HIDROXI, ENTRE OTROS; A ES GRUPO IMINO O ALQUIL(C1-C4)-IMINO; B ES CARBONILO O SULFONILO; C ES 1,3-ALENILENO, 1,1-VINILENO, 1,2-VINILENO, ENTRE OTROS; D ES ALQUILENO C1-C4 DE CADENA LINEAL O RAMIFICADO; E ES PIRROLIDIN-1-ILO, PIPERIDIN-1-ILO U HOMOPIPERIDIN -1-ILO, ENTRE OTROS; X ES UN GRUPO METINO SUSTITUIDO CON GRUPO CIANO, NITROGENO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS:4-[(3-CLORO-4-FLUORO-FENIL)AMINO]-6-{[4-((1S,4S)-2-OXA-5-AZA-BICICLO[2.2.1]HEPT-5-IL)-1-OXO-2-BUTEN-1-IL]AMINO}-7-CICLOPROPILMETOXI-QUINAZOLINA,4-[(3-CLORO-4-FLUORO-FENIL)AMINO]-6-{[4-((1S,4S)-2-OXA-5-AZA-BICICLO[2.2.1]HEPT-5-IL)-1-OXO-2-BUTEN-1-IL]AMINO}-7-CICLOPETILOXI-QUINAZOLINA,4-[(3-CLORO-4-FLUORO-FENIL)AMINO]-6-{[4-((1S,4S)-2-OXA-5-AZA-BICICLO[2.2.1]HEPT-5-IL)-1-OXO-2-BUTEN-1-IL]AMINO}-7-[(S)-(TETRAHIDROFURAN-3-IL)OXI]-QUINAZOLINA, ENTRE OTROS. SE REFIERE TAMBIEN A UN PROCEDIMIENTO PARA LA PREPARACION. LOS COMPUESTOS MENCIONADOS TIENEN ACCION INHIBIDORA SOBRE LA TRANSDUCCION DE SENAL MEDIADA POR TIROSINCINASAS Y SON UTILES PARA EL TRATAMIENTO DE ENFERMEDADES TUMORALES E HIPERPLASIA PROSTATICA BENIGNA (BHP)
PE2003000384A 2002-04-19 2003-04-15 Heterociclos biciclicos, medicamentos que contienen estos compuestos su empleo y procedimientos para su preparacion PE20040171A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE10217689A DE10217689A1 (de) 2002-04-19 2002-04-19 Bicyclische Heterocyclen, diese Verbindungen enthaltende Arzneimittel, ihre Verwendung und Verfahren zu ihrer Herstellung

Publications (1)

Publication Number Publication Date
PE20040171A1 true PE20040171A1 (es) 2004-06-02

Family

ID=29224623

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2003000384A PE20040171A1 (es) 2002-04-19 2003-04-15 Heterociclos biciclicos, medicamentos que contienen estos compuestos su empleo y procedimientos para su preparacion

Country Status (10)

Country Link
EP (1) EP1499619A1 (es)
JP (1) JP4527406B2 (es)
AR (1) AR039571A1 (es)
AU (1) AU2003226806A1 (es)
CA (1) CA2484395C (es)
DE (1) DE10217689A1 (es)
PE (1) PE20040171A1 (es)
TW (1) TW200408643A (es)
UY (1) UY27767A1 (es)
WO (1) WO2003089439A1 (es)

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HUP0201900A3 (en) 1999-06-21 2003-02-28 Boehringer Ingelheim Pharma Bicyclic heterocycles, pharmaceutical compositions containing them, their use and methods for the production thereof
US7019012B2 (en) 2000-12-20 2006-03-28 Boehringer Ingelheim International Pharma Gmbh & Co. Kg Quinazoline derivatives and pharmaceutical compositions containing them
US20040044014A1 (en) 2002-04-19 2004-03-04 Boehringer Ingelheim Pharma Gmbh & Co. Kg Bicyclic heterocycles, pharmaceutical compositions containing these compounds, their use and processes for the preparation thereof
CA2491191C (en) 2002-07-15 2014-02-04 Exelixis, Inc. Receptor-type kinase modulators and methods of use
US8309562B2 (en) 2003-07-03 2012-11-13 Myrexis, Inc. Compounds and therapeutical use thereof
ES2925655T3 (es) 2003-09-26 2022-10-19 Exelixis Inc Moduladores c-Met y métodos de uso
PT1746999E (pt) * 2004-05-06 2012-01-11 Warner Lambert Co 4-fenilamino-quinazolin-6-il-amidas
US8258145B2 (en) 2005-01-03 2012-09-04 Myrexis, Inc. Method of treating brain cancer
CA2592900A1 (en) 2005-01-03 2006-07-13 Myriad Genetics Inc. Nitrogen containing bicyclic compounds and therapeutical use thereof
KR100832594B1 (ko) * 2005-11-08 2008-05-27 한미약품 주식회사 다중저해제로서의 퀴나졸린 유도체 및 이의 제조방법
CA2833706C (en) 2005-11-11 2014-10-21 Boehringer Ingelheim International Gmbh Quinazoline derivatives for the treatment of cancer diseases
AU2007299080B2 (en) 2006-09-18 2013-04-18 Boehringer Ingelheim International Gmbh Method for treating cancer harboring EGFR mutations
TWI447108B (zh) 2009-01-16 2014-08-01 Exelixis Inc Ｎ－（４－｛〔６，７雙（甲氧基）喹啉－４－基〕氧基｝苯基）－ｎ’－（４－氟苯基）環丙烷－１，１－二甲醯胺之蘋果酸鹽及其結晶型
AU2010266725A1 (en) 2009-07-02 2012-02-23 Newgen Therapeutics, Inc. Phosphorus containing quinazoline compounds and methods of use
DK2451445T3 (da) 2009-07-06 2019-06-24 Boehringer Ingelheim Int Fremgangsmåde til at tørre bibw2992, dets salte og faste farmaceutiske formuleringer omfattende denne aktive ingrediens
UA108618C2 (uk) 2009-08-07 2015-05-25 Застосування c-met-модуляторів в комбінації з темозоломідом та/або променевою терапією для лікування раку
CN102020639A (zh) 2009-09-14 2011-04-20 上海恒瑞医药有限公司 6-氨基喹唑啉或3-氰基喹啉类衍生物、其制备方法及其在医药上的应用
HUE033575T2 (hu) 2011-05-26 2017-12-28 Xuanzhu Pharma Co Ltd Tirozin-kináz inhibitor kinazolin származék, elõállítási eljárása és alkalmazása
JP2014532063A (ja) * 2011-10-12 2014-12-04 テリジェン リミテッドＴｅｌｉｇｅｎｅ Ｌｔｄ キナーゼ阻害剤としてのキナゾリン誘導体およびその使用方法
US9242965B2 (en) 2013-12-31 2016-01-26 Boehringer Ingelheim International Gmbh Process for the manufacture of (E)-4-N,N-dialkylamino crotonic acid in HX salt form and use thereof for synthesis of EGFR tyrosine kinase inhibitors
AU2019346550A1 (en) 2018-09-25 2021-04-22 Black Diamond Therapeutics, Inc. Quinazoline derivatives as tyrosine kinase inhibitor, compositions, methods of making them and their use

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2249446C (en) * 1996-04-12 2008-06-17 Warner-Lambert Company Irreversible inhibitors of tyrosine kinases
TW436485B (en) * 1997-08-01 2001-05-28 American Cyanamid Co Substituted quinazoline derivatives
AU6159499A (en) * 1998-09-29 2000-04-17 Wyeth Holdings Corporation Substituted 3-cyanoquinolines as protein tyrosine kinases inhibitors
DE19908567A1 (de) * 1999-02-27 2000-08-31 Boehringer Ingelheim Pharma Bicyclische Heterocyclen, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
AU3281600A (en) * 1999-02-27 2000-09-21 Boehringer Ingelheim Pharma Gmbh & Co. Kg 4-amino-quinazoline and quinoline derivatives having an inhibitory effect on signal transsduction mediated by tyrosine kinases
HUP0201900A3 (en) * 1999-06-21 2003-02-28 Boehringer Ingelheim Pharma Bicyclic heterocycles, pharmaceutical compositions containing them, their use and methods for the production thereof
ES2280375T3 (es) * 2000-04-08 2007-09-16 BOEHRINGER INGELHEIM PHARMA GMBH &amp; CO.KG Heterociclos biciclicos, medicamentos que contienen estos compuestos, su uso y procedimiento para su preparacion.
DE10017539A1 (de) * 2000-04-08 2001-10-11 Boehringer Ingelheim Pharma Bicyclische Heterocyclen, diese Verbingungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
DE10042061A1 (de) * 2000-08-26 2002-03-07 Boehringer Ingelheim Pharma Bicyclische Heterocyclen,diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
DE10042062A1 (de) * 2000-08-26 2002-03-07 Boehringer Ingelheim Pharma Bicyclische Heterocyclen, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Hertellung

Also Published As

Publication number Publication date
UY27767A1 (es) 2003-11-28
AR039571A1 (es) 2005-02-23
EP1499619A1 (de) 2005-01-26
DE10217689A1 (de) 2003-11-13
CA2484395A1 (en) 2003-10-30
JP2005526837A (ja) 2005-09-08
CA2484395C (en) 2011-11-22
JP4527406B2 (ja) 2010-08-18
AU2003226806A1 (en) 2003-11-03
WO2003089439A1 (de) 2003-10-30
TW200408643A (en) 2004-06-01

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