CN1242991C - 阿朴啡酯类及其治疗用途 - Google Patents

阿朴啡酯类及其治疗用途 Download PDF

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Publication number
CN1242991C
CN1242991C CNB018142222A CN01814222A CN1242991C CN 1242991 C CN1242991 C CN 1242991C CN B018142222 A CNB018142222 A CN B018142222A CN 01814222 A CN01814222 A CN 01814222A CN 1242991 C CN1242991 C CN 1242991C
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CN
China
Prior art keywords
general formula
group
aporphine
replaced
alkyloyl
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 - Fee Related
Application number
CNB018142222A
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English (en)
Chinese (zh)
Other versions
CN1447792A (zh
Inventor
H·维克斯卓姆
D·迪杰克斯特拉
T·克里默斯
P·E·安德仁
S·马凯斯
U·朱瓦
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Axon Biochemicals BV
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Axon Biochemicals BV
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Publication of CN1447792A publication Critical patent/CN1447792A/zh
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Publication of CN1242991C publication Critical patent/CN1242991C/zh
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/485—Morphinan derivatives, e.g. morphine, codeine
    • 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
    • C07D211/06—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 no double bonds between ring members or between ring members and non-ring members
    • C07D211/08—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 no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18—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 no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/44—Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0014—Skin, i.e. galenical aspects of topical compositions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • 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
    • 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
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/10—Drugs for disorders of the endocrine system of the posterior pituitary hormones, e.g. oxytocin, ADH
    • A61P5/12—Drugs for disorders of the endocrine system of the posterior pituitary hormones, e.g. oxytocin, ADH for decreasing, blocking or antagonising the activity of the posterior pituitary hormones
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/04—Ortho- or peri-condensed ring systems
    • C07D221/18—Ring systems of four or more rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/20—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Dermatology (AREA)
  • Emergency Medicine (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Endocrinology (AREA)
  • Psychiatry (AREA)
  • Reproductive Health (AREA)
  • Pain & Pain Management (AREA)
  • Diabetes (AREA)
  • Psychology (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
CNB018142222A 2000-08-17 2001-07-20 阿朴啡酯类及其治疗用途 Expired - Fee Related CN1242991C (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
SE0002934A SE0002934D0 (sv) 2000-08-17 2000-08-17 New aporphine esters and in their use in therapy
SE00029348 2000-08-17

Publications (2)

Publication Number Publication Date
CN1447792A CN1447792A (zh) 2003-10-08
CN1242991C true CN1242991C (zh) 2006-02-22

Family

ID=20280719

Family Applications (1)

Application Number Title Priority Date Filing Date
CNB018142222A Expired - Fee Related CN1242991C (zh) 2000-08-17 2001-07-20 阿朴啡酯类及其治疗用途

Country Status (19)

Country Link
US (3) US7238705B2 (https=)
EP (1) EP1309553A1 (https=)
JP (1) JP2004506041A (https=)
KR (1) KR100865503B1 (https=)
CN (1) CN1242991C (https=)
AU (2) AU2001271228B2 (https=)
BR (1) BR0113291A (https=)
CA (1) CA2419842C (https=)
CZ (1) CZ2003454A3 (https=)
EA (1) EA006388B1 (https=)
HU (1) HUP0301685A3 (https=)
IL (2) IL154096A0 (https=)
MX (1) MXPA03001465A (https=)
NO (1) NO324409B1 (https=)
NZ (1) NZ523893A (https=)
PL (1) PL360089A1 (https=)
SE (1) SE0002934D0 (https=)
WO (1) WO2002014279A1 (https=)
ZA (1) ZA200300828B (https=)

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* Cited by examiner, † Cited by third party
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SE0002934D0 (sv) * 2000-08-17 2000-08-17 Axon Biochemicals Bv New aporphine esters and in their use in therapy
SE0102036D0 (sv) * 2001-06-08 2001-06-08 Axon Biochemicals Bv Pharmaceutical formulation for the efficient administration of apomorphine, 6aR- (-) -N- Propyl- norapomorphine and their derivatives and pro-drugs thereof
BR0318360A (pt) * 2003-06-19 2006-07-25 Lotus Pharmaceutical Co Ltd aporfina e oxoaporfina e o uso médico das mesmas
US20070065463A1 (en) 2003-06-20 2007-03-22 Ronald Aung-Din Topical therapy for the treatment of migranes, muscle sprains, muscle spasms, spasticity and related conditions
AU2005232748A1 (en) 2004-04-13 2005-10-27 The Mclean Hospital Corporation R(-)-11-hydroxyaporphine derivatives and uses thereof
GB2437488A (en) * 2006-04-25 2007-10-31 Optinose As Pharmaceutical oily formulation for nasal or buccal administration
US20110111014A1 (en) * 2007-06-26 2011-05-12 Parkinson's Institute Methods and compositions for treatment of neurological disorders
WO2009009083A1 (en) * 2007-07-12 2009-01-15 The Mclean Hospital Corporation R(-)-2-methoxy-11-hydroxyaporphine and derivatives thereof
US8129530B2 (en) 2007-08-31 2012-03-06 H. Lundbeck A/S Catecholamine derivatives and prodrugs thereof
TWI404702B (zh) * 2007-08-31 2013-08-11 Lundbeck & Co As H 兒茶酚胺衍生物和其前藥
ES2315203B1 (es) * 2007-09-11 2010-01-13 Universidade De Santiago De Compostela Uso de oxoisoaporfinas y sus derivados como inhibidores selectivos de la monoamino oxidasa a.
GB0721394D0 (en) * 2007-10-31 2007-12-12 Vectura Group Plc Compositions for trating parkinson's disease
US8592424B2 (en) 2008-06-30 2013-11-26 Afgin Pharma Llc Topical regional neuro-affective therapy
EP2419508A4 (en) * 2009-04-17 2012-11-14 Somalabs Inc METHOD OF INDUCING REWARD RESPONSE BY MODULATION OF DOPAMINERGIC SYSTEMS IN THE CENTRAL NERVOUS SYSTEM
PT2952191T (pt) 2009-06-12 2018-11-30 Sunovion Pharmaceuticals Inc Apomorfina sublingual
NZ612686A (en) 2010-12-16 2015-11-27 Cynapsus Therapeutics Inc Sublingual films
ES2673672T3 (es) * 2011-02-11 2018-06-25 The Regents Of The University Of Michigan Composiciones tripeptídicas y su uso para el tratamiento de la diabetes
JP7211706B2 (ja) 2015-04-21 2023-01-24 サノヴィオン ファーマシュティカルズ インコーポレーテッド 口腔粘膜へのアポモルフィンの投与によるパーキンソン病の治療方法
US10989704B2 (en) 2015-06-24 2021-04-27 Koninklijke Philips N.V. Sweat monitoring apparatus and monitoring method
JP7320507B2 (ja) 2017-11-24 2023-08-03 ハー・ルンドベック・アクチエゼルスカベット パーキンソン病の治療に使用するための新規なカテコールアミンプロドラッグ
HUE070062T2 (hu) * 2018-01-18 2025-05-28 Leukos Biotech S L Apomorfin-palmitinsav kokristály szilárd részecske kristályos forma
JP2021522196A (ja) * 2018-04-20 2021-08-30 ザ ジェネラル ホスピタル コーポレイション 血液脳関門を越えて送達するためのアセチル化プロドラッグ
US11130775B2 (en) 2019-05-20 2021-09-28 H. Lundbeck A/S Solid forms of (2S,3S,4S,5R,6S)-3,4,5-trihydroxy-6-(((4aR,10aR)-7-hydroxy-1-propyl-1,2,3,4,4A,5,10,10A-octahydrobenzo[g]quinolin-6-yl)oxy)tetrahydro-2H-pyran-2-carboxylic acid
US11111263B2 (en) 2019-05-20 2021-09-07 H. Lundbeck A/S Process for the manufacture of (2S,3S,4S,5R,6S)-3,4,5-trihydroxy-6-(((4aR,10aR)-7-hydroxy-1-propyl-1,2,3,4,4a,5,10,10a-octahydrobenzo[g]quinolin-6-yl)oxy)tetrahydro-2H-pyran-2-carboxylic acid
US11168056B2 (en) 2019-05-20 2021-11-09 H. Lundbeck A/S Process for the manufacturing of (6aR,10aR)-7-propyl-6,6a,7,8,9,10,10a,11-octahydro-[1,3]dioxolo[4′,5′:5,6]benzo[1,2-G]quinoline and (4aR,10aR)-1-propyl-1,2,3,4,4a,5,10,10a-octahydro-benzo[G]quinoline-6,7-diol
WO2020234274A1 (en) 2019-05-21 2020-11-26 H. Lundbeck A/S New catecholamine prodrugs for use in the treatment of parkinson's disease
JP7562562B2 (ja) 2019-05-21 2024-10-07 ハー・ルンドベック・アクチエゼルスカベット パーキンソン病の治療に使用するための新規なカテコールアミンプロドラッグ
EP3972971A1 (en) 2019-05-21 2022-03-30 H. Lundbeck A/S New catecholamine prodrugs for use in the treatment of parkinson's diseases
CN113727712B (zh) 2019-05-21 2024-11-15 H.隆德贝克有限公司 用于治疗帕金森病的儿茶酚胺氨基甲酸酯前药

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AU3140577A (en) * 1976-12-13 1979-06-14 Sterling Drug Inc N-propylnorapormorphine diesters
DE2717001C2 (de) 1977-04-18 1984-06-20 Karl O. Helm Ag, 2000 Hamburg Arzneimittel mit antithrombotischer Wirkung
DE3171561D1 (en) 1980-05-08 1985-09-05 Univ Northeastern N-substituted aporphines, a method of inducing emesis and a method of controlling psychosis utilising the same
US4353912A (en) * 1980-05-08 1982-10-12 Northeastern University N-Haloalkyl nor apomorphines and method of inactivating dopamine receptor sites and enhancing dopaminergic activity therewith
WO1990012574A1 (en) * 1989-04-25 1990-11-01 Northeastern University Dopamine agonist compounds
GB9517062D0 (en) 1995-08-18 1995-10-25 Scherer Ltd R P Pharmaceutical compositions
GB9700878D0 (en) 1997-01-17 1997-03-05 Scherer Ltd R P Dosage forms and method for ameliorating male erectile dysfunction
US6403605B1 (en) 1998-05-29 2002-06-11 Queen's University At Kingston Methods for the normalization of sexual response and amelioration of long term genital tissue degradation
IT1299566B1 (it) 1998-07-17 2000-03-16 Ifi Istituto Farmacoterapico I Cerotto transdermico e composizioni farmaceutiche comprendenti r (-)- norapropilapomorfina cloridrato e/o s (+) - norapropilapomorfina
WO2000069416A1 (en) 1999-05-13 2000-11-23 Unihart Corporation Pharmaceutical compositions comprising apocodeine and/or its derivatives
BR0109515A (pt) * 2000-04-07 2004-08-10 Tap Pharmaceutical Prod Inc Derivados da apomorfina e métodos para seu uso
SE0102036D0 (sv) * 2001-06-08 2001-06-08 Axon Biochemicals Bv Pharmaceutical formulation for the efficient administration of apomorphine, 6aR- (-) -N- Propyl- norapomorphine and their derivatives and pro-drugs thereof
SE0002934D0 (sv) 2000-08-17 2000-08-17 Axon Biochemicals Bv New aporphine esters and in their use in therapy
EP1950203A1 (en) 2007-01-24 2008-07-30 Laboratorios del Dr. Esteve S.A. Substituted pyrazoline compounds with ACAT, their preparation and use as medicaments

Also Published As

Publication number Publication date
HUP0301685A2 (hu) 2003-08-28
US20080119504A1 (en) 2008-05-22
CA2419842A1 (en) 2002-02-21
WO2002014279A1 (en) 2002-02-21
MXPA03001465A (es) 2004-12-13
EA200300266A1 (ru) 2003-08-28
PL360089A1 (en) 2004-09-06
NZ523893A (en) 2003-10-31
IL154096A (en) 2009-11-18
BR0113291A (pt) 2004-01-06
CA2419842C (en) 2011-10-18
EA006388B1 (ru) 2005-12-29
US20050143408A1 (en) 2005-06-30
CN1447792A (zh) 2003-10-08
HUP0301685A3 (en) 2010-03-29
SE0002934D0 (sv) 2000-08-17
US20040018956A1 (en) 2004-01-29
IL154096A0 (en) 2003-07-31
US7238705B2 (en) 2007-07-03
NO20030677D0 (no) 2003-02-11
AU2001271228B2 (en) 2006-02-02
ZA200300828B (en) 2004-05-17
CZ2003454A3 (cs) 2003-06-18
KR100865503B1 (ko) 2008-10-28
JP2004506041A (ja) 2004-02-26
US7332503B2 (en) 2008-02-19
KR20030036703A (ko) 2003-05-09
EP1309553A1 (en) 2003-05-14
NO324409B1 (no) 2007-10-08
NO20030677L (no) 2003-03-05
AU7122801A (en) 2002-02-25

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Granted publication date: 20060222

Termination date: 20120720