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
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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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Dermatology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Psychology (AREA)
  • Reproductive Health (AREA)
  • Psychiatry (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Diabetes (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 (enExample)
EP (1) EP1309553A1 (enExample)
JP (1) JP2004506041A (enExample)
KR (1) KR100865503B1 (enExample)
CN (1) CN1242991C (enExample)
AU (2) AU7122801A (enExample)
BR (1) BR0113291A (enExample)
CA (1) CA2419842C (enExample)
CZ (1) CZ2003454A3 (enExample)
EA (1) EA006388B1 (enExample)
HU (1) HUP0301685A3 (enExample)
IL (2) IL154096A0 (enExample)
MX (1) MXPA03001465A (enExample)
NO (1) NO324409B1 (enExample)
NZ (1) NZ523893A (enExample)
PL (1) PL360089A1 (enExample)
SE (1) SE0002934D0 (enExample)
WO (1) WO2002014279A1 (enExample)
ZA (1) ZA200300828B (enExample)

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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
WO2004110449A1 (en) * 2003-06-19 2004-12-23 Lotus Pharmaceutical Co., Ltd. Aporphine and oxoaporphine and the medical use thereof
WO2004112723A2 (en) 2003-06-20 2004-12-29 Ronald Aung-Din Tropical therapy for the treatment of migraines, muscle sprains, muscle spasm, spasticity and related conditions
US7648995B2 (en) 2004-04-13 2010-01-19 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
US8431591B2 (en) 2007-07-12 2013-04-30 The Mclean Hospital Corporation R(−)-2-methoxy-11-hydroxyaporphine and derivatives thereof
US20090124651A1 (en) 2007-08-31 2009-05-14 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
WO2010005507A1 (en) 2008-06-30 2010-01-14 Afgin Pharma, Llc Topical regional neuro-affective therapy
WO2010121159A1 (en) * 2009-04-17 2010-10-21 Somalabs, Inc. Method for the induction of a reward response by modulation of dopaminergic systems in the central nervous system
ES2699077T3 (es) 2009-06-12 2019-02-07 Sunovion Pharmaceuticals Inc Apomorfina sublingual
EA031156B1 (ru) 2010-12-16 2018-11-30 Суновион Фармасьютикалз Инк. Сублингвальные пленки
AU2012214283B2 (en) * 2011-02-11 2016-01-28 The Regents Of The University Of Michigan Tripeptide compositions and methods for treatment of diabetes
WO2016172095A1 (en) 2015-04-21 2016-10-27 Cynapsus Therapeutics, Inc. Methods of treating parkinson's disease by administration of apomorphine to an oral mucosa
WO2016207070A1 (en) 2015-06-24 2016-12-29 Koninklijke Philips N.V. Sweat monitoring apparatus and monitoring method
TWI816716B (zh) 2017-11-24 2023-10-01 丹麥商Ｈ 朗德貝克公司 用於治療帕金森病之新兒茶酚胺前驅藥
HUE070062T2 (hu) * 2018-01-18 2025-05-28 Leukos Biotech S L Apomorfin-palmitinsav kokristály szilárd részecske kristályos forma
CA3097568A1 (en) * 2018-04-20 2019-10-24 The General Hospital Corporation Acetylated prodrugs for delivery across the blood-brain barrier
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
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
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
US12319710B2 (en) 2019-05-21 2025-06-03 H. Lundbeck A/S Catecholamine prodrugs for use in the treatment of Parkinson's diseases
US12384765B2 (en) 2019-05-21 2025-08-12 H. Lundbeck A/S Catecholamine prodrugs for use in the treatment of Parkinson's Disease
EP3972959A1 (en) 2019-05-21 2022-03-30 H. Lundbeck A/S New catecholamine prodrugs for use in the treatment of parkinson's disease
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
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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
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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
EP1175206A1 (en) * 1999-05-13 2002-01-30 Unihart Corporation Pharmaceutical compositions comprising apocodeine and/or its derivatives
AU2001255818A1 (en) * 2000-04-07 2001-10-23 Tap Pharmaceutical Products Inc. Apomorphine derivatives and methods for their use
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
AU2001271228B2 (en) 2006-02-02
US7238705B2 (en) 2007-07-03
HUP0301685A2 (hu) 2003-08-28
WO2002014279A1 (en) 2002-02-21
EP1309553A1 (en) 2003-05-14
SE0002934D0 (sv) 2000-08-17
NO20030677D0 (no) 2003-02-11
BR0113291A (pt) 2004-01-06
PL360089A1 (en) 2004-09-06
KR100865503B1 (ko) 2008-10-28
IL154096A (en) 2009-11-18
EA006388B1 (ru) 2005-12-29
ZA200300828B (en) 2004-05-17
MXPA03001465A (es) 2004-12-13
JP2004506041A (ja) 2004-02-26
NO20030677L (no) 2003-03-05
US20040018956A1 (en) 2004-01-29
US20080119504A1 (en) 2008-05-22
IL154096A0 (en) 2003-07-31
US20050143408A1 (en) 2005-06-30
NZ523893A (en) 2003-10-31
CN1447792A (zh) 2003-10-08
EA200300266A1 (ru) 2003-08-28
KR20030036703A (ko) 2003-05-09
CZ2003454A3 (cs) 2003-06-18
US7332503B2 (en) 2008-02-19
CA2419842C (en) 2011-10-18
HUP0301685A3 (en) 2010-03-29
AU7122801A (en) 2002-02-25
CA2419842A1 (en) 2002-02-21
NO324409B1 (no) 2007-10-08

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