WO2005103037A3 - Selected cgrp antagonists, methods for the production thereof, and use thereof as medicaments - Google Patents

Selected cgrp antagonists, methods for the production thereof, and use thereof as medicaments Download PDF

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Publication number
WO2005103037A3
WO2005103037A3 PCT/EP2005/004104 EP2005004104W WO2005103037A3 WO 2005103037 A3 WO2005103037 A3 WO 2005103037A3 EP 2005004104 W EP2005004104 W EP 2005004104W WO 2005103037 A3 WO2005103037 A3 WO 2005103037A3
Authority
WO
WIPO (PCT)
Prior art keywords
production
methods
medicaments
cgrp antagonists
salts
Prior art date
Application number
PCT/EP2005/004104
Other languages
German (de)
French (fr)
Other versions
WO2005103037A2 (en
Inventor
Stephan Georg Mueller
Klaus Rudolf
Philipp Lustenberger
Dirk Stenkamp
Marco Santagostino
Fabio Paleari
Gerhard Schaenzle
Kirsten Arndt
Henri Doods
Original Assignee
Boehringer Ingelheim Int
Boehringer Ingelheim Pharma
Stephan Georg Mueller
Klaus Rudolf
Philipp Lustenberger
Dirk Stenkamp
Marco Santagostino
Fabio Paleari
Gerhard Schaenzle
Kirsten Arndt
Henri Doods
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 Int, Boehringer Ingelheim Pharma, Stephan Georg Mueller, Klaus Rudolf, Philipp Lustenberger, Dirk Stenkamp, Marco Santagostino, Fabio Paleari, Gerhard Schaenzle, Kirsten Arndt, Henri Doods filed Critical Boehringer Ingelheim Int
Priority to EP05735460A priority Critical patent/EP1740577A2/en
Priority to JP2007508815A priority patent/JP2007533689A/en
Priority to CA002565219A priority patent/CA2565219A1/en
Publication of WO2005103037A2 publication Critical patent/WO2005103037A2/en
Publication of WO2005103037A3 publication Critical patent/WO2005103037A3/en
Priority to CA002600909A priority patent/CA2600909A1/en
Priority to KR1020077024324A priority patent/KR20070114831A/en
Priority to MX2007011527A priority patent/MX2007011527A/en
Priority to BRPI0607577-0A priority patent/BRPI0607577A2/en
Priority to EP06723538A priority patent/EP1863799A1/en
Priority to PCT/EP2006/002515 priority patent/WO2006100009A1/en
Priority to RU2007138881/04A priority patent/RU2007138881A/en
Priority to AU2006226615A priority patent/AU2006226615A1/en
Priority to JP2008502299A priority patent/JP2008538209A/en
Priority to TW095109753A priority patent/TW200700408A/en
Priority to US11/277,177 priority patent/US7528129B2/en
Priority to IL186090A priority patent/IL186090A0/en
Priority to US12/707,890 priority patent/US20100144716A1/en

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Classifications

    • CCHEMISTRY; METALLURGY
    • 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
    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61P17/02Drugs 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
    • 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
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • 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
    • 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
    • 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
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms 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
    • 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

Abstract

The invention relates to CGRP antagonists of general formula (I), wherein A, X, Q, and R1 to R3 are defined as indicated in claim 1, the tautomers, isomers, diastereomers, enantiomers, hydrates, mixtures, and salts thereof, and the hydrates of the salts, especially the physiologically acceptable salts thereof with inorganic or organic acids, medicaments containing said compounds, the use thereof, and methods for the production thereof.
PCT/EP2005/004104 2004-04-22 2005-04-18 Selected cgrp antagonists, methods for the production thereof, and use thereof as medicaments WO2005103037A2 (en)

Priority Applications (16)

Application Number Priority Date Filing Date Title
EP05735460A EP1740577A2 (en) 2004-04-22 2005-04-18 Selected cgrp antagonists, methods for the production thereof, and use thereof as medicaments
JP2007508815A JP2007533689A (en) 2004-04-22 2005-04-18 Selected CGRP antagonists, methods for their production and their use as drugs
CA002565219A CA2565219A1 (en) 2004-04-22 2005-04-18 Selected cgrp antagonists, methods for the production thereof, and use thereof as medicaments
JP2008502299A JP2008538209A (en) 2005-03-23 2006-03-18 CGRP antagonists, methods for their production and their use as drugs
AU2006226615A AU2006226615A1 (en) 2005-03-23 2006-03-18 CGRP antagonists, method for the production thereof, and their use as medicaments
MX2007011527A MX2007011527A (en) 2005-03-23 2006-03-18 Cgrp antagonists, method for the production thereof, and their use as medicaments.
KR1020077024324A KR20070114831A (en) 2005-03-23 2006-03-18 Cgrp antagonists, method for the production thereof, and their use as medicaments
CA002600909A CA2600909A1 (en) 2005-03-23 2006-03-18 Cgrp antagonists, method for the production thereof, and their use as medicaments
BRPI0607577-0A BRPI0607577A2 (en) 2005-03-23 2006-03-18 cgrp antagonists, process for preparation as well as use as a medicine
EP06723538A EP1863799A1 (en) 2005-03-23 2006-03-18 Cgrp-antagonists, process for their preparation as well as their use as medicaments
PCT/EP2006/002515 WO2006100009A1 (en) 2005-03-23 2006-03-18 Cgrp antagonists, method for the production thereof, and their use as medicaments
RU2007138881/04A RU2007138881A (en) 2005-03-23 2006-03-18 CGRP-PEPTIDE ANTAGONISTS, METHOD FOR PRODUCING THEM, AND ALSO THEIR APPLICATION AS MEDICINES
TW095109753A TW200700408A (en) 2005-03-23 2006-03-22 New cgrp-antagonists, process for preparing them and their use as pharmaceutical compositions
US11/277,177 US7528129B2 (en) 2005-03-23 2006-03-22 CGRP-antagonists, process for preparing them and their use as pharmaceutical compositions
IL186090A IL186090A0 (en) 2005-03-23 2007-09-20 Cgrp antagonists, method for the production thereof, and their use as medicaments
US12/707,890 US20100144716A1 (en) 2005-03-23 2010-02-18 New CGRP-antagonists, process for preparing them and their use as pharmaceutical compositions

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE102004019492.0 2004-04-22
DE102004019492A DE102004019492A1 (en) 2004-04-22 2004-04-22 Selected CGRP antagonists, process for their preparation and their use as pharmaceuticals

Publications (2)

Publication Number Publication Date
WO2005103037A2 WO2005103037A2 (en) 2005-11-03
WO2005103037A3 true WO2005103037A3 (en) 2006-01-12

Family

ID=35140095

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2005/004104 WO2005103037A2 (en) 2004-04-22 2005-04-18 Selected cgrp antagonists, methods for the production thereof, and use thereof as medicaments

Country Status (9)

Country Link
EP (1) EP1740577A2 (en)
JP (1) JP2007533689A (en)
AR (1) AR049422A1 (en)
CA (1) CA2565219A1 (en)
DE (1) DE102004019492A1 (en)
PE (1) PE20060186A1 (en)
TW (1) TW200606151A (en)
UY (1) UY28859A1 (en)
WO (1) WO2005103037A2 (en)

Families Citing this family (30)

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US7842808B2 (en) 2002-06-05 2010-11-30 Bristol-Myers Squibb Company Anti-migraine spirocycles
US7220862B2 (en) 2002-06-05 2007-05-22 Bristol-Myers Squibb Company Calcitonin gene related peptide receptor antagonists
DE10250082A1 (en) 2002-10-25 2004-05-13 Boehringer Ingelheim Pharma Gmbh & Co. Kg Selected CGRP antagonists, process for their preparation and their use as pharmaceuticals
US7595312B2 (en) 2002-10-25 2009-09-29 Boehringer Ingelheim Pharma Gmbh & Co. Kg Selected CGRP antagonists, processes for preparing them and their use as pharmaceutical compositions
TW200524601A (en) 2003-12-05 2005-08-01 Bristol Myers Squibb Co Heterocyclic anti-migraine agents
DE102004015723A1 (en) 2004-03-29 2005-10-20 Boehringer Ingelheim Pharma Selected CGRP antagonists, process for their preparation and their use as pharmaceuticals
TW200533398A (en) 2004-03-29 2005-10-16 Bristol Myers Squibb Co Novel therapeutic agents for the treatment of migraine
US7384931B2 (en) 2004-11-03 2008-06-10 Bristol-Myers Squibb Company Constrained compounds as CGRP-receptor antagonists
US7384930B2 (en) 2004-11-03 2008-06-10 Bristol-Myers Squibb Company Constrained compounds as CGRP-receptor antagonists
US7449586B2 (en) 2004-12-03 2008-11-11 Bristol-Myers Squibb Company Processes for the preparation of CGRP-receptor antagonists and intermediates thereof
DE102004063753A1 (en) * 2004-12-29 2006-07-13 Boehringer Ingelheim Pharma Gmbh & Co. Kg Use of selected CGRP antagonists in combination with other migraine medicines for the treatment of migraine
DE102004063752A1 (en) * 2004-12-29 2006-07-13 Boehringer Ingelheim Pharma Gmbh & Co. Kg Use of selected CGRP antagonists to combat menopausal hot flashes
EP1770091A1 (en) * 2005-09-29 2007-04-04 Boehringer Ingelheim Pharma GmbH & Co. KG CGRP-antagonists, process for their preparation as well as their use as medicaments
DE102005038831A1 (en) * 2005-08-17 2007-02-22 Boehringer Ingelheim Pharma Gmbh & Co. Kg New N-acylalkoxycarbonyl-piperidine derivatives, useful as CGRP antagonists, for treating e.g. headaches, cardiovascular disease, skin disorders, morphine tolerance, and inflammatory diseases such as osteoarthritis and allergic rhinitis
US7834007B2 (en) 2005-08-25 2010-11-16 Bristol-Myers Squibb Company CGRP antagonists
US8168592B2 (en) 2005-10-21 2012-05-01 Amgen Inc. CGRP peptide antagonists and conjugates
DE102005050892A1 (en) 2005-10-21 2007-04-26 Boehringer Ingelheim Pharma Gmbh & Co. Kg Selected CGRP antagonists, process for their preparation and their use as pharmaceuticals
PE20080153A1 (en) * 2006-06-08 2008-04-14 Boehringer Ingelheim Int PHARMACEUTICAL COMPOSITION INCLUDING AN ANTAGONIST OF THE PEPTIDE RELATED TO THE CALCITONIN GENE (CGRP)
US9108948B2 (en) * 2006-06-23 2015-08-18 Abbvie Inc. Cyclopropyl amine derivatives
EP2099767A1 (en) 2006-11-01 2009-09-16 Brystol-Myers Squibb Company Modulators of glucocorticoid receptor, ap-1, and/or nf- b activity and use thereof
BRPI0817835A2 (en) 2007-10-18 2015-03-31 Boehringer Ingelheim Int CGRP ANTAGONISTS
EP2065381A1 (en) 2007-10-18 2009-06-03 Boehringer Ingelheim Pharma GmbH & Co. KG CGRP antagonists
EP2225223B1 (en) 2007-11-22 2017-01-11 Boehringer Ingelheim International GmbH Organic compounds
CN103108873A (en) * 2010-07-16 2013-05-15 皮拉马尔企业有限公司 Substituted imidazoquinoline derivatives as kinase inhibitors
AU2014334040A1 (en) 2013-10-07 2016-04-28 Bayer Pharma Aktiengesellschaft Cyclic thienouracil-carboxamides and use thereof
GB201519195D0 (en) 2015-10-30 2015-12-16 Heptares Therapeutics Ltd CGRP Receptor Antagonists
GB201519194D0 (en) 2015-10-30 2015-12-16 Heptares Therapeutics Ltd CGRP receptor antagonists
GB201519196D0 (en) 2015-10-30 2015-12-16 Heptares Therapeutics Ltd CGRP Receptor Antagonists
WO2017148519A1 (en) 2016-03-03 2017-09-08 Boehringer Ingelheim International Gmbh Pyridinylmethyl carbamimidoylcarbamate derivatives and their use as aoc3 inhibitors
EP3423434B1 (en) 2016-03-03 2020-01-15 Boehringer Ingelheim International GmbH 4-cyano-benzyl carbamimidoylcarbamate derivatives and their use as aoc3 inhibitors

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WO2000018764A1 (en) * 1998-09-30 2000-04-06 Merck Sharp & Dohme Limited Benzimidazolinyl piperidines as cgrp ligands
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WO2000018764A1 (en) * 1998-09-30 2000-04-06 Merck Sharp & Dohme Limited Benzimidazolinyl piperidines as cgrp ligands
WO2001010425A2 (en) * 1999-08-10 2001-02-15 Boehringer Ingelheim Pharma Kg Use of cgrp antagonists and cgrp release inhibitors for controlling menopausal hot flashes
WO2004063171A1 (en) * 2003-01-14 2004-07-29 Boehringer Ingelheim International Gmbh N- (1-benzyl-2-oxo-2- (1-piperazinyl) ethyl) -1-piperidincarboxamid-derivatives and related compounds use as cgrp-antagonists for treating a headache
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PASTERNAK A ET AL: "Potent, orally bioavailable somatostatin agonists: good absorption achieved by urea backbone cyclization", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, OXFORD, GB, vol. 9, no. 3, 8 February 1999 (1999-02-08), pages 491 - 496, XP004157253, ISSN: 0960-894X *
See also references of EP1740577A2 *

Also Published As

Publication number Publication date
WO2005103037A2 (en) 2005-11-03
TW200606151A (en) 2006-02-16
EP1740577A2 (en) 2007-01-10
DE102004019492A1 (en) 2005-11-10
JP2007533689A (en) 2007-11-22
PE20060186A1 (en) 2006-04-18
AR049422A1 (en) 2006-08-02
CA2565219A1 (en) 2005-11-03
UY28859A1 (en) 2005-11-30

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