ES2138977T3 - Agonistas muscarinicos. - Google Patents

Agonistas muscarinicos.

Info

Publication number
ES2138977T3
ES2138977T3 ES92919345T ES92919345T ES2138977T3 ES 2138977 T3 ES2138977 T3 ES 2138977T3 ES 92919345 T ES92919345 T ES 92919345T ES 92919345 T ES92919345 T ES 92919345T ES 2138977 T3 ES2138977 T3 ES 2138977T3
Authority
ES
Spain
Prior art keywords
acetiolas
tetrahydropyrimidine
substituted
muscarinic agonists
acetielas
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.)
Expired - Lifetime
Application number
ES92919345T
Other languages
English (en)
Inventor
Philip G Dunbar
Graham J Durant
Wayne Hoss
William S Messer Jr
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.)
University of Toledo
Original Assignee
University of Toledo
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 University of Toledo filed Critical University of Toledo
Application granted granted Critical
Publication of ES2138977T3 publication Critical patent/ES2138977T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/06—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/68—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D211/72—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D211/78—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • 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
    • C07D405/02—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 two hetero rings
    • C07D405/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D411/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms
    • C07D411/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D411/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic 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
    • C07D413/04—Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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
    • C07D417/04—Heterocyclic 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

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
  • Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Hydrogenated Pyridines (AREA)

Abstract

SE PRESENTAN COMPOSICIONES DE 1,4,5,6-TETRAHIDROPIRIMIDINA SUSTITUIDA, COMPOSICIONES DE 1,2,3,6-TETRAHIDROPIRIMIDINA SUSTITUIDA, COMPOSICIONES DE 3,4,5,6-TETRAHIDROPIRIMIDINA SUSTITUIDA. ESTAS SON UTILES PARA ESTIMULAR LOS RECEPTORES MUSCARINICOS, INCLUYENDO, POR EJEMPLO EL TRATAMIENTO EN LOS SINTOMAS DE TRASTORNOS COGNITIVOS, ESPECIALMENTE MEMORIA DISMINUIDA, QUE ESTAN ASOCIADAS CON UN DECRECIMIENTO DE LA SINTESIS DE LA ACETILCOLINA Y UNA DEGENERACION DE LAS CELULAS COLINERGICAS.
ES92919345T 1991-08-27 1992-08-12 Agonistas muscarinicos. Expired - Lifetime ES2138977T3 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US07/750,504 US5175166A (en) 1991-08-27 1991-08-27 Muscarinic agonists

Publications (1)

Publication Number Publication Date
ES2138977T3 true ES2138977T3 (es) 2000-02-01

Family

ID=25018129

Family Applications (1)

Application Number Title Priority Date Filing Date
ES92919345T Expired - Lifetime ES2138977T3 (es) 1991-08-27 1992-08-12 Agonistas muscarinicos.

Country Status (8)

Country Link
US (2) US5175166A (es)
EP (1) EP0630244B1 (es)
JP (2) JP3411276B2 (es)
AT (1) ATE187070T1 (es)
CA (1) CA2113424C (es)
DE (1) DE69230378T2 (es)
ES (1) ES2138977T3 (es)
WO (1) WO1993003726A1 (es)

Families Citing this family (57)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5043345A (en) * 1989-02-22 1991-08-27 Novo Nordisk A/S Piperidine compounds and their preparation and use
EP0724570B1 (en) * 1993-10-21 1999-03-03 G.D. Searle & Co. Amidino derivatives useful as nitric oxide synthase inhibitors
DE4342560A1 (de) 1993-12-14 1995-06-22 Marbert Gmbh Ectoin und Ectoinderivate als Feuchtigkeitsspender in Kosmetikprodukten
WO1997016192A1 (en) * 1995-10-31 1997-05-09 Merck & Co., Inc. Muscarine antagonists
AU1582197A (en) * 1996-01-22 1997-08-11 Eli Lilly And Company Combinatorial process for preparing substituted indane libraries
US5618818A (en) * 1996-03-20 1997-04-08 The University Of Toledo Muscarinic agonist compounds
US5726179A (en) * 1996-04-01 1998-03-10 The University Of Toledo Muscarinic agonists
AU2730097A (en) * 1997-04-15 1998-11-11 University Of Toledo, The Muscarinic agonists
US6528529B1 (en) 1998-03-31 2003-03-04 Acadia Pharmaceuticals Inc. Compounds with activity on muscarinic receptors
US20040047828A1 (en) * 1998-08-01 2004-03-11 Merck Patent Gmbh Ectoin or ection derivatives and surfactants
US8914114B2 (en) * 2000-05-23 2014-12-16 The Feinstein Institute For Medical Research Inhibition of inflammatory cytokine production by cholinergic agonists and vagus nerve stimulation
US7048910B2 (en) 2000-09-07 2006-05-23 Merck Patent Gmbh Use of ectoine or ectoine derivatives for oral care
US20040048795A1 (en) * 2002-02-26 2004-03-11 North Shore-Long Island Jewish Research Institute Inhibition of inflammatory cytokine production by stimulation of brain muscarinic receptors
DE10214257A1 (de) * 2002-03-28 2003-10-16 Merck Patent Gmbh Verwendung von kompatiblen Soluten zur Inhibierung der Freisetzung von Ceramiden
US8729129B2 (en) 2004-03-25 2014-05-20 The Feinstein Institute For Medical Research Neural tourniquet
US10912712B2 (en) 2004-03-25 2021-02-09 The Feinstein Institutes For Medical Research Treatment of bleeding by non-invasive stimulation
KR100621192B1 (ko) 2004-10-13 2006-09-19 한국화학연구원 무스카린 수용체 작용물질로서 작용하는1,2,3,4-테트라하이드로피리미디닐-1,2,4-옥사다이아졸유도체와 이의 제조방법
CN102793972A (zh) 2004-12-27 2012-11-28 范因斯坦医学研究院 通过电刺激迷走神经治疗炎症性疾病
US11207518B2 (en) 2004-12-27 2021-12-28 The Feinstein Institutes For Medical Research Treating inflammatory disorders by stimulation of the cholinergic anti-inflammatory pathway
US20090012101A1 (en) * 2005-12-27 2009-01-08 University Of Toledo Mucarinic Agonists and Methods of Use Thereof
US8391970B2 (en) * 2007-08-27 2013-03-05 The Feinstein Institute For Medical Research Devices and methods for inhibiting granulocyte activation by neural stimulation
US9662490B2 (en) 2008-03-31 2017-05-30 The Feinstein Institute For Medical Research Methods and systems for reducing inflammation by neuromodulation and administration of an anti-inflammatory drug
US9211409B2 (en) 2008-03-31 2015-12-15 The Feinstein Institute For Medical Research Methods and systems for reducing inflammation by neuromodulation of T-cell activity
US20090275997A1 (en) * 2008-05-01 2009-11-05 Michael Allen Faltys Vagus nerve stimulation electrodes and methods of use
US20110294835A1 (en) 2008-05-15 2011-12-01 The Board Of Trustees Of The University Of Illinois Muscarinic Agonists as Cognitive Enhancers
ES2452484T3 (es) 2008-11-18 2014-04-01 Setpoint Medical Corporation Dispositivos para optimizar la colocación de electrodos para la estimulación antiinflamatoria
WO2010102218A1 (en) * 2009-03-05 2010-09-10 Mithridion, Inc. Compounds and compositions for cognition-enhancement, methods of making, and methods of treating
US9211410B2 (en) 2009-05-01 2015-12-15 Setpoint Medical Corporation Extremely low duty-cycle activation of the cholinergic anti-inflammatory pathway to treat chronic inflammation
US8996116B2 (en) 2009-10-30 2015-03-31 Setpoint Medical Corporation Modulation of the cholinergic anti-inflammatory pathway to treat pain or addiction
WO2010144578A2 (en) 2009-06-09 2010-12-16 Setpoint Medical Corporation Nerve cuff with pocket for leadless stimulator
US9833621B2 (en) 2011-09-23 2017-12-05 Setpoint Medical Corporation Modulation of sirtuins by vagus nerve stimulation
WO2014169145A1 (en) 2013-04-10 2014-10-16 Setpoint Medical Corporation Closed-loop vagus nerve stimulation
CN105126248B (zh) 2009-12-23 2018-06-12 赛博恩特医疗器械公司 用于治疗慢性炎症的神经刺激设备和系统
US8853219B2 (en) 2010-01-11 2014-10-07 Neurosolis, Inc. Compounds and compositions for cognition-enhancement, methods of making, and methods of treating
WO2012033956A1 (en) 2010-09-08 2012-03-15 Mithridion, Inc. Cognition enhancing compounds and compositions, methods of making, and methods of treating
US9549928B2 (en) 2011-04-29 2017-01-24 The University Of Toledo Muscarinic agonists as enhancers of cognitive flexibility
EP2707094B1 (en) 2011-05-09 2016-02-03 Setpoint Medical Corporation Single-pulse activation of the cholinergic anti-inflammatory pathway to treat chronic inflammation
US12172017B2 (en) 2011-05-09 2024-12-24 Setpoint Medical Corporation Vagus nerve stimulation to treat neurodegenerative disorders
CN102429909A (zh) * 2011-11-26 2012-05-02 济南环肽医药科技有限公司 一种治疗神经退行性疾病的药物
US9572983B2 (en) 2012-03-26 2017-02-21 Setpoint Medical Corporation Devices and methods for modulation of bone erosion
US11311725B2 (en) 2014-10-24 2022-04-26 Setpoint Medical Corporation Systems and methods for stimulating and/or monitoring loci in the brain to treat inflammation and to enhance vagus nerve stimulation
US20170333407A1 (en) * 2014-11-03 2017-11-23 William Beaumont Hospital Method for treating underactive bladder syndrome
US11406833B2 (en) 2015-02-03 2022-08-09 Setpoint Medical Corporation Apparatus and method for reminding, prompting, or alerting a patient with an implanted stimulator
US10596367B2 (en) 2016-01-13 2020-03-24 Setpoint Medical Corporation Systems and methods for establishing a nerve block
CN108882885A (zh) 2016-01-20 2018-11-23 赛博恩特医疗器械公司 迷走神经刺激的控制
US10314501B2 (en) 2016-01-20 2019-06-11 Setpoint Medical Corporation Implantable microstimulators and inductive charging systems
US11471681B2 (en) 2016-01-20 2022-10-18 Setpoint Medical Corporation Batteryless implantable microstimulators
US10583304B2 (en) 2016-01-25 2020-03-10 Setpoint Medical Corporation Implantable neurostimulator having power control and thermal regulation and methods of use
US11173307B2 (en) 2017-08-14 2021-11-16 Setpoint Medical Corporation Vagus nerve stimulation pre-screening test
US11660443B2 (en) 2018-04-20 2023-05-30 The Feinstein Institutes For Medical Research Methods and apparatuses for reducing bleeding via electrical trigeminal nerve stimulation
US11260229B2 (en) 2018-09-25 2022-03-01 The Feinstein Institutes For Medical Research Methods and apparatuses for reducing bleeding via coordinated trigeminal and vagal nerve stimulation
US12343535B2 (en) 2019-04-12 2025-07-01 Setpoint Medical Corporation Vagus nerve stimulation to treat neurodegenerative disorders
JP2021066707A (ja) * 2019-10-25 2021-04-30 学校法人上智学院 環状化合物の製造方法
AU2021207815B2 (en) 2020-01-13 2026-03-26 The Feinstein Institutes For Medical Research Treating bleeding and bleeding disorders via high intensity focused ultrasound stimulation of the spleen
US11938324B2 (en) 2020-05-21 2024-03-26 The Feinstein Institutes For Medical Research Systems and methods for vagus nerve stimulation
WO2022245878A1 (en) 2021-05-17 2022-11-24 Setpoint Medical Corporation Neurostimulation parameter authentication and expiration system for neurostimulation
US20250229086A1 (en) 2022-01-20 2025-07-17 Setpoint Medical Corporation Treatment of inflammatory disorders

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL83275A (en) * 1986-09-08 1994-02-27 Novo Nordisk As Substituted 1, 2, 4- oxadiazolyl piperidine compounds, their preparation and pharmaceutical compositions containing them
US4786648A (en) * 1986-12-08 1988-11-22 Warner-Lambert Company O-substituted tetrahydropyridine oxime cholinergic agents
US4710508A (en) * 1986-12-08 1987-12-01 Warner-Lambert Company O-substituted tetrahydropyridine oxime cholinergic agents
GB8714789D0 (en) * 1987-06-24 1987-07-29 Lundbeck & Co As H Heterocyclic compounds
US5043345A (en) * 1989-02-22 1991-08-27 Novo Nordisk A/S Piperidine compounds and their preparation and use

Also Published As

Publication number Publication date
US5403845A (en) 1995-04-04
JP3519062B2 (ja) 2004-04-12
EP0630244A1 (en) 1994-12-28
JPH06510287A (ja) 1994-11-17
WO1993003726A1 (en) 1993-03-04
ATE187070T1 (de) 1999-12-15
CA2113424A1 (en) 1993-03-04
DE69230378T2 (de) 2000-04-06
EP0630244B1 (en) 1999-12-01
CA2113424C (en) 2003-11-11
DE69230378D1 (de) 2000-01-05
US5175166A (en) 1992-12-29
JP3411276B2 (ja) 2003-05-26
JP2002047276A (ja) 2002-02-12
EP0630244A4 (en) 1994-04-07

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