EP1888542A1 - Composes spiro substitues, et leur utilisation pour produire des medicaments - Google Patents

Composes spiro substitues, et leur utilisation pour produire des medicaments

Info

Publication number
EP1888542A1
EP1888542A1 EP06753674A EP06753674A EP1888542A1 EP 1888542 A1 EP1888542 A1 EP 1888542A1 EP 06753674 A EP06753674 A EP 06753674A EP 06753674 A EP06753674 A EP 06753674A EP 1888542 A1 EP1888542 A1 EP 1888542A1
Authority
EP
European Patent Office
Prior art keywords
phenyl
butyl
group
tert
radical
Prior art date
Legal status (The legal status 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 status listed.)
Withdrawn
Application number
EP06753674A
Other languages
German (de)
English (en)
Inventor
Robert Frank
Ruth Jostock
Melanie Reich
Gregor Bahrenberg
Hans Schick
Helmut Sonnenschein
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Gruenenthal GmbH
Original Assignee
Gruenenthal GmbH
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 Gruenenthal GmbH filed Critical Gruenenthal GmbH
Publication of EP1888542A1 publication Critical patent/EP1888542A1/fr
Withdrawn legal-status Critical Current

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D261/00Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/20Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings condensed with carbocyclic rings or ring systems
    • 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
    • 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
    • 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
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • 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
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/06Anti-spasmodics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/02Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina
    • 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
    • A61P17/04Antipruritics
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • 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
    • A61P25/32Alcohol-abuse
    • 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
    • A61P27/02Ophthalmic agents
    • 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
    • A61P3/04Anorexiants; Antiobesity 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
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10Antioedematous agents; Diuretics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/12Antidiuretics, e.g. drugs for diabetes insipidus
    • 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
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D417/12Heterocyclic 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 chain containing hetero atoms as chain links

Definitions

  • a suitable starting point for the treatment of pain, in particular of neuropathic pain is the vanilloid receptor of subtype 1 (VR1 / TRPV1), which is often referred to as the capsaicin receptor.
  • This receptor is u.a. by vanilloids such as e.g. Capsaicin, heat and protons stimulates and plays a central role in the onset of pain.
  • vanilloids such as e.g. Capsaicin, heat and protons stimulates and plays a central role in the onset of pain.
  • it is important for a variety of other physiological and pathophysiological processes such as migraine; Depressions; neurodegenerative diseases; cognitive disorders; Anxiety; Epilepsy; To cough; diarrhea; pruritus; Disorders of the cardiovascular system; Disorders of food intake; Drug addiction; Drug abuse and especially urinary incontinence.
  • alkylene, alkenylene or alkynylene groups have optionally in each case 1 or 2 heteroatom (s) selected from the group consisting of oxygen, nitrogen, that -N (H) -. And -N (C 1 6 alkyl ) -, and sulfur as a chain link (er) on.
  • R 15 , R 16 , R 19 and R 20 are each a hydrogen radical
  • step 1 compounds of general formula II in a reaction medium, preferably in a reaction medium selected from the group consisting of methanol, tetrahydrofuran, dichloromethane and corresponding mixtures, in the presence of at least one base, preferably in the presence of at least one base selected from the group consisting of Sodium bicarbonate, lithium hydroxide, triethylamine or N-diisopropylethylamine, reacted with compounds of general formula III at temperatures between 0 C C and 100 0 C to compounds of general formula IV.
  • a reaction medium selected from the group consisting of methanol, tetrahydrofuran, dichloromethane and corresponding mixtures
  • at least one base preferably in the presence of at least one base selected from the group consisting of Sodium bicarbonate, lithium hydroxide, triethylamine or N-diisopropylethylamine
  • inorganic base preferably selected from the group consisting of potassium carbonate and cesium carbonate
  • an organic base preferably selected from the group consisting of triethylamine, 4-methylmorpholine, pyridine, N, N-dimethylaminopyridine and diisopropylethylamine, preferably at temperatures from -70 0 C to 100 0 C to give
  • substituted spiro compounds of the abovementioned general formulas I and Ia 1 according to the invention referred to below only as spiro compounds of the general formula I, and corresponding stereoisomers can be used both in the form of their free bases, their free acids and in the form of corresponding salts, in particular physiologically acceptable salts.
  • At least one substituted spiro compound according to the invention including the compounds excluded above and optionally one or more pharmaceutically acceptable excipients for the manufacture of a medicament for the treatment and / or prophylaxis of one or more diseases selected from the group consisting of pain, preferably pain selected from the group consisting of acute pain, chronic pain, neuropathic pain and visceral pain; Joint pain; Migraine; Depressions; Neuropathy; Nerve injuries; neurodegenerative diseases, preferably selected from the group consisting of multiple sclerosis, Alzheimer's disease, Parkinson's disease and Huntington's disease; cognitive dysfunctions, preferably cognitive deficits, particularly preferred memory disorders; Epilepsy; urinary incontinence; an overactive bladder (overactive bladder, OAB); Stomach ulcers; Irritable bowel syndrome; Stroke; diarrhea; pruritus; Food ingestion, preferably selected from the group consisting of bulimia, cachexia, anorexia and obesity; Drug addiction; Drug abuse; Withdrawal symptoms in drug dependence
  • the pharmaceutical composition of the invention is suitable for administration to adults and children, including infants and babies.
  • ester 8- (1,1-dimethylpropyl) -1-oxa-2-azaspiro [4.5] dec-2-ene-3-carboxylic acid ethyl ester (2.8 g, 10 mmol) was dissolved in MeOH (50 ml), washed with Lithium hydroxide (357 mg, 15 mmol) in water (8 ml) and stirred for 23 h at RT. To work up the reaction, MeOH was removed in vacuo and water (25 ml) added. After the addition of 10% aq. Citric acid sol.
  • ester 8-cyclohexyl-1-oxa-2-azaspiro [4.5] dec-2-ene-3-carboxylic acid ethyl ester (2.5g, 8.5mmol) was dissolved in MeOH (80ml) with heating, with lithium hydroxide (306mg , 13 mmol) in water (8 ml) and stirred at RT for 60 h. To work up the reaction, MeOH was removed in vacuo and water (25 ml) added. After the addition of 10% aq. Citric acid sol. (20 ml) precipitated at pH 4 the acid 8-cyclohexyl-1-oxa-2-azaspiro [4.5] dec-2-ene-3-carboxylic acid.
  • the viscous residue was dissolved in 0.5 N aq. HCl (10 ml) and EtOAc (10 ml). The phases were separated. The organic phase was washed successively with 0.5 N aq. HCl (2 * 5 ml), with 1.1 M aq. NaHCO 3 (3 ⁇ 5 ml) and water (2 * 5 ml). The organic phase was dried with NaaSO 4 . The solvent was distilled off. The beige residue was the mixture of diastereoisomers of 8-th /?

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Addiction (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Psychology (AREA)
  • Urology & Nephrology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Nutrition Science (AREA)
  • Hospice & Palliative Care (AREA)
  • Vascular Medicine (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Ophthalmology & Optometry (AREA)
  • Child & Adolescent Psychology (AREA)
  • Immunology (AREA)

Abstract

L'invention concerne des composés spiro substitués, leurs procédés de production, des médicaments les contenant, et l'utilisation de ces composés pour produire des médicaments.
EP06753674A 2005-05-19 2006-05-17 Composes spiro substitues, et leur utilisation pour produire des medicaments Withdrawn EP1888542A1 (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DE102005023779 2005-05-19
DE102005044814A DE102005044814A1 (de) 2005-05-19 2005-09-20 Substituierte Sprio-Verbindungen und deren Verwendung zur Herstellung von Arzneimitteln
PCT/EP2006/004653 WO2006136245A1 (fr) 2005-05-19 2006-05-17 Composes spiro substitues, et leur utilisation pour produire des medicaments

Publications (1)

Publication Number Publication Date
EP1888542A1 true EP1888542A1 (fr) 2008-02-20

Family

ID=36917274

Family Applications (1)

Application Number Title Priority Date Filing Date
EP06753674A Withdrawn EP1888542A1 (fr) 2005-05-19 2006-05-17 Composes spiro substitues, et leur utilisation pour produire des medicaments

Country Status (6)

Country Link
US (1) US7981883B2 (fr)
EP (1) EP1888542A1 (fr)
JP (1) JP5376942B2 (fr)
CA (1) CA2608319C (fr)
DE (1) DE102005044814A1 (fr)
WO (1) WO2006136245A1 (fr)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010027567A2 (fr) * 2008-07-23 2010-03-11 Schering Corporation Dérivés spirocycliques tricycliques et leurs procédés d’utilisation
US8232409B2 (en) 2008-10-15 2012-07-31 Janssen Pharmaceutica N.V. Heterocyclic benzimidazoles as TRPM8 modulators
US8349852B2 (en) 2009-01-13 2013-01-08 Novartis Ag Quinazolinone derivatives useful as vanilloid antagonists
US20120071481A1 (en) * 2009-02-04 2012-03-22 Ronald Palin Isoxazole-5-carboxamide derivatives
AR080056A1 (es) 2010-02-01 2012-03-07 Novartis Ag Derivados de ciclohexil-amida como antagonistas de los receptores de crf
WO2011092290A1 (fr) 2010-02-01 2011-08-04 Novartis Ag Dérivés de pyrazolo[5,1-b] utilisés en tant qu'antagonistes du récepteur de crf-1
WO2011095450A1 (fr) 2010-02-02 2011-08-11 Novartis Ag Dérivés de cyclohexylamide à titre d'antagonistes du récepteur crf
SI3700902T1 (sl) * 2017-10-27 2023-10-30 Boehringer Ingelheim International Gmbh Inhibitorji trpc6

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Publication number Priority date Publication date Assignee Title
JP2001527513A (ja) * 1996-03-15 2001-12-25 デュポン ファーマシューティカルズ カンパニー スピロ環インテグリン阻害剤
WO1998043962A1 (fr) * 1997-03-28 1998-10-08 Du Pont Pharmaceuticals Company Promedicaments heterocycliques inhibiteurs d'integrine
AU775426B2 (en) * 1999-07-21 2004-07-29 Astrazeneca Ab New compounds
DE10130020A1 (de) * 2001-06-25 2003-12-04 Gruenenthal Gmbh Substituierte 1-Oxa-2,8-diaza-spiro[4.5]dec-2-en-derivate
EP1506166B1 (fr) * 2002-05-17 2011-11-16 Janssen Pharmaceutica NV Modulateurs de l'uree derives de l'aminotetraline du recepteur vanilloide vr1
ATE493987T1 (de) * 2002-05-22 2011-01-15 Amgen Inc Aminopyrimidin-derivate zur verwendung als vanilloid-rezeptor-liganden zur behandlung von schmerzen
AU2003301903A1 (en) * 2002-11-06 2004-06-03 Bristol-Myers Squibb Company Isoxazoline derivatives as inhibitors of matrix metalloproteinases and/or tnf-alpha converting enzyme
AU2004268847A1 (en) * 2003-08-29 2005-03-10 Ranbaxy Laboratories Limited Inhibitors of phosphodiesterase type-IV
US7786141B2 (en) * 2004-08-19 2010-08-31 Vertex Pharmaceuticals Incorporated Dihydrospiroindene modulators of muscarinic receptors
US20070208001A1 (en) * 2006-03-03 2007-09-06 Jincong Zhuo Modulators of 11- beta hydroxyl steroid dehydrogenase type 1, pharmaceutical compositions thereof, and methods of using the same

Non-Patent Citations (1)

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Title
See references of WO2006136245A1 *

Also Published As

Publication number Publication date
US7981883B2 (en) 2011-07-19
CA2608319C (fr) 2014-04-15
JP5376942B2 (ja) 2013-12-25
JP2008540594A (ja) 2008-11-20
WO2006136245A1 (fr) 2006-12-28
DE102005044814A1 (de) 2006-11-23
CA2608319A1 (fr) 2006-12-28
US20090275628A1 (en) 2009-11-05

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