PE20040780A1 - Compuestos heterociclicos como antagonista de cgrp y procedimiento para su preparacion - Google Patents

Compuestos heterociclicos como antagonista de cgrp y procedimiento para su preparacion

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Publication number
PE20040780A1
PE20040780A1 PE2003001078A PE2003001078A PE20040780A1 PE 20040780 A1 PE20040780 A1 PE 20040780A1 PE 2003001078 A PE2003001078 A PE 2003001078A PE 2003001078 A PE2003001078 A PE 2003001078A PE 20040780 A1 PE20040780 A1 PE 20040780A1
Authority
PE
Peru
Prior art keywords
alkyl
piperidin
oxo
substituted
compounds
Prior art date
Application number
PE2003001078A
Other languages
English (en)
Inventor
Klaus Rudolf
Stephan Georg Muller
Dirk Stenkamp
Philipp Lustenberger
Alexander Dreyer
Eckhart Bauer
Marcus Schindler
Kirsten Arndt
Henri Doods
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 PE20040780A1 publication Critical patent/PE20040780A1/es

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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-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
    • A61K31/435Heterocyclic 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
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • A61K31/54Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541Non-condensed thiazines 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/554Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
    • 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
    • A61P1/02Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/12Antidiarrhoeals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61P17/00Drugs for dermatological disorders
    • A61P17/16Emollients or protectives, e.g. against radiation
    • 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
    • A61P25/06Antimigraine agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36Opioid-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/16Otologicals
    • 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
    • A61P31/04Antibacterial 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
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • 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
    • C07D417/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Epidemiology (AREA)
  • Pulmonology (AREA)
  • Neurology (AREA)
  • Addiction (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Biomedical Technology (AREA)
  • Dermatology (AREA)
  • Neurosurgery (AREA)
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  • Psychiatry (AREA)
  • Communicable Diseases (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Oncology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)

Abstract

SE REFIERE A COMPUESTOS HETEROCICLICOS DE FORMULA I DONDE A ES O o S, FENILSULFONILAMINO O CIANIMINO; X ES O o S, IMINO EVENTUALMENTE SUSTITUIDO CON ALQUILO C1-C6, ENTRE OTROS; Y y Z SON ALQUILO C1-C6 LINEAL O RAMIFICADO, SUSTITUIDO O NO CON F, PUDIENDO FORMAR DICHOS GRUPOS ALQUILO, JUNTO AL CARBONO AL QUE ESTAN UNIDOS, UN ANILLO DE 4-8 MIEMBROS; R1 ES UN HETEROCICLO AZA, DIAZA, ENTRE OTROS; R2 ES H, FENILMETILO, ALQUILO C2-C7, QUE EN POSICION w PUEDE ESTAR SUSTITUIDO POR CICLOHEXILO, FENILO, ENTRE OTROS; R3 ES H, ALQUILO C1-C3 SUSTITUIDO O NO CON FENILO O PIRIDINILO; R2 Y R3 JUNTO CON EL N AL QUE ESTAN UNIDOS FORMAN UN RADICAL DE FORMULA II, EN DONDE Y1 ES C o CUANDO R5 REPRESENTA UN PAR DE ELECTRONES LIBRES, TAMBIEN PUEDE SER N; q Y r, CUANDO Y1 ES C, ES 0, 1 o 2, o CUANDO Y1 ES N, ES 1 o 2; R4 ES H, AMINO, ALQUILAMINO, ENTRE OTROS; R5 ES H, ALQUILO C1-C4; R6 Y R7 SON H, ALQUILO C1-C3, DIALQUILO C1-C3-AMINO, O CUANDO Y1 NO ES N PUEDE SER F; R8 Y R9 SON H o ALQUILO C1-C3. SON COMPUESTOS PREFERIDOS: {(R)-1-(3,4-DIETIL-BENCIL)-2-[4-(1-METIL-PIPERIDIN-4-IL)-PIPERAZIN-1-IL]-2-OXO-ETIL}-AMIDA DE ACIDO 4-(2-OXO-1,2,4,5-TETRAHIDRO-1,3-BENZODIAZEPIN-3-IL)-PIPERIDIN-1-CARBOXILICO; {(R)-1-(3,4-DIETIL-BENCIL)-2-[4-(4-METIL-PIPERAZIN-1-IL)-PIPERIDIN-1-IL]-2-OXO-ETIL}-AMIDA DE ACIDO 4-(2-OXO-1,2,4,5-TETRAHIDRO-1,3-BENZODIAZEPIN-3-IL)-PIPERIDIN-1-CARBOXILICO; TAMBIEN SE REFIERE A UN PROCEDIMIENTO PARA LA PREPARACION UNA COMPOSICION FARMACEUTICA. ESTOS COMPUESTOS SON ANTAGONISTAS DE GCRP
PE2003001078A 2002-10-25 2003-10-23 Compuestos heterociclicos como antagonista de cgrp y procedimiento para su preparacion PE20040780A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE10250082A DE10250082A1 (de) 2002-10-25 2002-10-25 Ausgewählte CGRP-Antagonisten, Verfahren zu deren Herstellung sowie deren Verwendung als Arzneimittel

Publications (1)

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PE20040780A1 true PE20040780A1 (es) 2005-01-14

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US (3) US20040132716A1 (es)
EP (1) EP1558601A1 (es)
JP (1) JP4435687B2 (es)
KR (1) KR20050083821A (es)
CN (1) CN1708492A (es)
AR (1) AR043056A1 (es)
AU (1) AU2003276157A1 (es)
BR (1) BR0315642A (es)
CA (1) CA2503462A1 (es)
CO (1) CO5570703A2 (es)
DE (1) DE10250082A1 (es)
EA (1) EA009984B1 (es)
EC (1) ECSP055746A (es)
HR (1) HRP20050365A2 (es)
ME (1) MEP51408A (es)
MX (1) MXPA05004188A (es)
NO (1) NO20052493L (es)
PE (1) PE20040780A1 (es)
PL (1) PL376373A1 (es)
RS (1) RS20050329A (es)
TW (1) TW200427681A (es)
UA (1) UA82206C2 (es)
UY (1) UY28040A1 (es)
WO (1) WO2004037811A1 (es)
ZA (1) ZA200502247B (es)

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DE102004019492A1 (de) 2004-04-22 2005-11-10 Boehringer Ingelheim Pharma Gmbh & Co. Kg Ausgewählte CGRP-Antagonisten, Verfahren zu deren Herstellung sowie deren Verwendung als Arzneimittel
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EP1770091A1 (de) 2005-09-29 2007-04-04 Boehringer Ingelheim Pharma GmbH & Co. KG CGRP-Antagonisten, Verfahren zu deren Herstellung sowie deren Verwendung als Arzneimittel
US7491717B2 (en) 2005-03-23 2009-02-17 Boehringer Ingelheim International Gmbh Selected CGRP-antagonists, process for preparing them and their use as pharmaceutical compositions
US7439237B2 (en) 2005-04-15 2008-10-21 Boehringer Ingelheim International Gmbh Selected CGRP-antagonists, process for preparing them and their use as pharmaceutical compositions
DE102005038831A1 (de) 2005-08-17 2007-02-22 Boehringer Ingelheim Pharma Gmbh & Co. Kg Ausgewählte CGRP-Antagonisten, Verfahren zu deren Herstellung sowie deren Verwendung als Arzneimittel
EP1770087A1 (de) 2005-09-29 2007-04-04 Boehringer Ingelheim Pharma GmbH & Co. KG Ausgewählte CGRP-Antagonisten, Verfahren zu deren Herstellung sowie deren Verwendung als Arzneimittel
EP1770086A1 (de) 2005-09-29 2007-04-04 Boehringer Ingelheim Pharma GmbH & Co. KG Ausgewählte CGRP-Antagonisten, Verfahren zu deren Herstellung sowie deren Verwendung als Arzneimittel
DE102005050892A1 (de) 2005-10-21 2007-04-26 Boehringer Ingelheim Pharma Gmbh & Co. Kg Ausgewählte CGRP-Antagonisten, Verfahren zu deren Herstellung sowie deren Verwendung als Arzneimittel

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MXPA05004188A (es) 2005-10-05
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US7700589B2 (en) 2010-04-20
US20100152171A1 (en) 2010-06-17
UA82206C2 (uk) 2008-03-25
HRP20050365A2 (en) 2006-05-31
BR0315642A (pt) 2005-08-30
CA2503462A1 (en) 2004-05-06
US20040132716A1 (en) 2004-07-08
PL376373A1 (en) 2005-12-27
JP4435687B2 (ja) 2010-03-24
KR20050083821A (ko) 2005-08-26
DE10250082A1 (de) 2004-05-13
EA009984B1 (ru) 2008-04-28
ECSP055746A (es) 2005-07-06
NO20052493D0 (no) 2005-05-24
ZA200502247B (en) 2005-09-19
EA200500601A1 (ru) 2006-02-24
NO20052493L (no) 2005-05-24
WO2004037811A1 (de) 2004-05-06
UY28040A1 (es) 2004-05-31
EP1558601A1 (de) 2005-08-03
AR043056A1 (es) 2005-07-13
JP2006505573A (ja) 2006-02-16
CO5570703A2 (es) 2005-10-31
CN1708492A (zh) 2005-12-14
RS20050329A (en) 2007-08-03
AU2003276157A1 (en) 2004-05-13
MEP51408A (en) 2011-02-10
US20070244099A1 (en) 2007-10-18

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