HK63992A - 1-phenyl-3-naphthalenyloxy-propanamines - Google Patents

1-phenyl-3-naphthalenyloxy-propanamines

Info

Publication number
HK63992A
HK63992A HK639/92A HK63992A HK63992A HK 63992 A HK63992 A HK 63992A HK 639/92 A HK639/92 A HK 639/92A HK 63992 A HK63992 A HK 63992A HK 63992 A HK63992 A HK 63992A
Authority
HK
Hong Kong
Prior art keywords
compound
naphthalenyloxy
formula
methyl
phenyl
Prior art date
Application number
HK639/92A
Other languages
English (en)
French (fr)
Inventor
David Wayne Robertson
Dennis Charles Thompson
David Taiwai Wong
Original Assignee
Eli Lilly And Company
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 Eli Lilly And Company filed Critical Eli Lilly And Company
Publication of HK63992A publication Critical patent/HK63992A/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C217/00—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton
    • C07C217/02—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C217/48—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being unsaturated and containing rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D317/00—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D317/08—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
    • C07D317/44—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D317/46—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C07D317/48—Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring
    • C07D317/50—Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to atoms of the carbocyclic ring
    • C07D317/58—Radicals substituted by nitrogen atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Health & Medical Sciences (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)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Diabetes (AREA)
  • Pain & Pain Management (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Anesthesiology (AREA)
  • Addiction (AREA)
  • Nutrition Science (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Compounds That Contain Two Or More Ring Oxygen Atoms (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)

Claims (9)

1. Verbindung der Formel (I) worin
jeder der Reste R1 und R2 unabhängig Wasserstoff oder eine Methylgruppe ist;
R3 Wasserstoff, Halogen, ein C1-C4-Alkyl-, C1-C3-Alkoxy- oder Trifluormethylrest ist ;
jeder Rest R4 unabhängig Wasserstoff, Halogen, ein C1-C4-Alkyl-, C1-C3-Alkoxy- oder Trifluormethylrest ist;
m 1 oder 2 ist;
wenn m 2 ist, die Reste R4 unter Bildung eines Methylendioxyrestes kombiniert sein können ;
oder ein pharmazeutisch annehmbares Säureadditionssalz davon.
2. Verbindung nach Anspruch 1, worin beide Reste R1 und R2 Methylreste sind.
3. N,N-Dimethyl-1-phenyl-3-(1-naphthalenyloxy)propanamin oder ein pharmazeutisch annehmbares Säureadditionssalz davon.
4. Verbindung nach einem der Ansprüche 1 bis 3, die das (+)-Stereoisomer ist.
5. (+)-N,N-Dimethyl-1-phenyl-3-(1-naphthalenyloxy)propanamin oder ein pharmazeutisch annehmbares Säureadditionssalz davon.
6. (+)-N,N-Dimethyl-1-phenyl-3-(1-naphthalenyloxy)propanamintartrat.
7. Pharmazeutisches Präparat, umfassend eine Verbindung der Formel (I) nach einem der Ansprüche 1 bis 6 oder ein pharmazeutisch annehmbares Säureadditionssalz davon und einen oder mehrere pharmazeutisch annehmbare Träger, Verdünnungsmittel oder Hilfsstoffe dafür.
8. Verbindung der Formel (I) oder ein pharmazeutisch annehmbares Salz davon zur Verwendung der Hemmung der Aufnahme von Serotonin bei Säugetieren.
9. Verfahren zur Herstellung einer Verbindung der Formel (I) worin
jeder der Reste R1 und R2 unabhängig Wasserstoff oder eine Methylgruppe ist;
R3 Wasserstoff, Halogen, ein C1-C4-Alkyl-, C1-C3-Alkoxy- oder Trifluormethylrest ist ;
jeder Rest R4 unabhängig Wasserstoff, Halogen, ein C1-C4-Alkyl-, C1-C3-Alkoxy- oder Trifluormethylrest ist;
m 1 oder 2 ist;
wenn m 2 ist, jeder Rest R4 unter Bildung eines Methylendioxyrestes kombiniert sein kann ;
oder eines pharmazeutisch annehmbaren Säureadditionssalzes davon, das umfaßt
A) Hydrolyse einer Verbindung der Formel unter sauren Bedingungen, um eine Verbindung zu liefern, worin R1 und R2 Wasserstoff sind ; oder
B) Methylieren einer Verbindung der Formel (I), worin R1 Wasserstoff ist, um eine Verbindung der Formel (I) herzustellen, worin R1 ein Methylrest ist; oder
C) Umsetzen einer Verbindung der Formel mit einer Verbindung der Formel worin einer der Reste J und Y eine gute Abgangsgruppe ist und der andere Rest eine Hydroxygruppe ist, in Gegenwart einer Base, die stark genug ist, um das Anion der die Hydroxygruppe enthaltenden Verbindung zu erzeugen ; oder
D) Umsetzen einer Verbindung der Formel worin X Halogen ist, mit NHR1R2; oder
E) Reduzieren einer Verbindung der Formel um eine Verbindung der Formel I zu liefem, worin R1 und R2 Wasserstoff sind ; oder
F) Demethylieren einer Verbindung der Formel I, worin R1 ein Methylrest ist, um eine Verbindung der Formel I zu liefern, worin R1 Wasserstoff ist.
HK639/92A 1987-04-09 1992-08-20 1-phenyl-3-naphthalenyloxy-propanamines HK63992A (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US3653487A 1987-04-09 1987-04-09

Publications (1)

Publication Number Publication Date
HK63992A true HK63992A (en) 1992-08-28

Family

ID=21889125

Family Applications (1)

Application Number Title Priority Date Filing Date
HK639/92A HK63992A (en) 1987-04-09 1992-08-20 1-phenyl-3-naphthalenyloxy-propanamines

Country Status (23)

Country Link
EP (1) EP0288188B1 (de)
JP (1) JPH0637443B2 (de)
KR (1) KR960007723B1 (de)
CN (1) CN1020093C (de)
AT (1) ATE68473T1 (de)
AU (1) AU602971B2 (de)
CA (1) CA1329937C (de)
CY (1) CY1658A (de)
DE (1) DE3865504D1 (de)
DK (1) DK170637B1 (de)
EG (1) EG18584A (de)
ES (1) ES2045109T3 (de)
GR (1) GR3003267T3 (de)
HK (1) HK63992A (de)
HU (1) HU204767B (de)
IL (1) IL85988A (de)
MX (1) MX11031A (de)
NZ (1) NZ224161A (de)
PH (1) PH27141A (de)
PT (1) PT87163B (de)
SG (1) SG67092G (de)
SU (1) SU1568886A3 (de)
ZA (1) ZA882418B (de)

Families Citing this family (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK258389D0 (da) * 1989-05-26 1989-05-26 Ferrosan As Aryloxyphenylpropylaminer, deres fremstilling og anvendelse
PH30083A (en) * 1991-02-25 1996-12-27 Lilly Co Eli Treatment of lower urinary tract disorders
AU3079692A (en) * 1991-12-20 1993-07-28 Karin Elisabeth Peuschel Using the immunoactivating activity of 3-naphthyloxy-2-hydroxy-propylamines, in particular for providing cell immunity, e.g. against viral infections
TW344661B (en) * 1993-11-24 1998-11-11 Lilly Co Eli Pharmaceutical composition for treatment of incontinence
JP3870419B2 (ja) * 1994-08-22 2007-01-17 三菱ウェルファーマ株式会社 ベンゼン化合物およびその医薬としての用途
US5948820A (en) 1994-08-22 1999-09-07 Yoshitomi Pharmaceutical Industries, Ltd. Benzene compound and pharmaceutical use thereof
DE19956786A1 (de) * 1999-11-25 2001-05-31 Basf Ag Verfahren zur Herstellung optisch aktiver Amine
CN100402488C (zh) * 2006-03-15 2008-07-16 上海玛耀化学技术有限公司 一种达泊西汀的合成方法
WO2008035358A2 (en) * 2006-06-05 2008-03-27 Cadila Healthcare Limited Process for preparing dapoxetine
CN101367739B (zh) * 2008-09-24 2013-02-13 台州职业技术学院 N,n-二甲基-1-苯基-3-(1-萘氧基)丙胺制备工艺
DE102009015702A1 (de) 2009-03-31 2010-10-07 Ratiopharm Gmbh Tabletten enthaltend Dapoxetin und Trockenverarbeitungsverfahren zu deren Herstellung
EP2513042A4 (de) 2009-11-13 2013-06-26 Symed Labs Ltd Dapoxetin in fester form
DE102009058321A1 (de) 2009-12-15 2011-06-16 Ratiopharm Gmbh Schmelztablette, enthaltend Dapoxetin
WO2011161690A1 (en) * 2010-06-23 2011-12-29 Symed Labs Limited Processes for the preparation of (+)-n,n-dimethyl-2-[1-(naphthalenyloxy) ethyl] benzene methanamine and intermediates thereof
CN102229538B (zh) * 2011-05-11 2013-11-13 中南大学 一种达泊西汀的合成方法
CN102850318A (zh) * 2011-07-01 2013-01-02 中国人民解放军军事医学科学院毒物药物研究所 新的选择性5-羟色胺重摄取抑制剂及其医药用途
CN103130660B (zh) * 2011-11-25 2014-09-17 厦门福满药业有限公司 一类达泊西汀的酸式盐及其晶体,以及晶体的制备方法
WO2013180675A1 (en) 2012-05-28 2013-12-05 Mahmut Bilgic Tablet formulation comprising dapoxetine
CN102746170A (zh) * 2012-07-28 2012-10-24 湖南尔文生物科技有限公司 一种达泊西汀的制备方法
US20150216798A1 (en) 2012-08-17 2015-08-06 Sanovel Ilac Sanayi Ve Ticaret Anonim Sirketi Novel orally administered pharmaceutical formulations
US20150231092A1 (en) 2012-08-17 2015-08-20 Sanovell IIac Sanayi Ve Ticaret Anonim Sirketi Novel effervescent sachet formulations of dapoxetine and a pde5 inhibitor
WO2014027979A2 (en) 2012-08-17 2014-02-20 Sanovel Ilac Sanayi Ve Ticaret Anonim Sirketi Tablet formulations comprising tadalafil and dapoxetine
TR201309037A2 (tr) 2012-08-17 2014-03-21 Sanovel Ilac Sanayi Ve Ticaret Anonim Sirketi Dapoksetin ve bir pde5 inhibitörü içeren yeni efervesan saşe formülasyonları.
US20150202168A1 (en) 2012-08-17 2015-07-23 Sanovel llac Sanayi Ve Ticaret Anonim Sirketi Oral film formulations comprising dapoxetine and tadalafil
WO2014027981A2 (en) 2012-08-17 2014-02-20 Sanovel Ilac Sanayi Ve Ticaret Anonim Sirketi Effervescent tablet formulations of dapoxetine and a pde5 inhibitor
CN102942496B (zh) * 2012-11-28 2014-06-11 扬州工业职业技术学院 (s)-n,n-二甲基-3-(萘酚-1-氧基)-1-苯基丙基-1-胺的制备方法
EP2749553A1 (de) 2012-12-31 2014-07-02 Deva Holding Anonim Sirketi Verfahren zur Herstellung von enantiomerisch reinem S-(+)-N, N-dimethyl-a-[2-(naphthalenyloxy)ethyl]benzenmethanamin
CN106748825A (zh) * 2016-11-29 2017-05-31 聊城大学 一种达泊西汀的合成、拆分纯化和成盐方法
CN108853072A (zh) * 2018-08-03 2018-11-23 安徽省金楠医疗科技有限公司 一种盐酸达泊西汀片及其制备方法

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4018895A (en) * 1974-01-10 1977-04-19 Eli Lilly And Company Aryloxyphenylpropylamines in treating depression
US4207343A (en) * 1978-06-22 1980-06-10 Eli Lilly And Company 1-Phenyl-3-(substituted phenoxy)propylamines
NZ213651A (en) * 1984-10-11 1989-07-27 Hoffmann La Roche Tetrahydronapthalene derivatives and medicaments

Also Published As

Publication number Publication date
ZA882418B (en) 1989-12-27
DK188288D0 (da) 1988-04-07
EP0288188B1 (de) 1991-10-16
AU602971B2 (en) 1990-11-01
AU1433588A (en) 1988-10-13
CN1020093C (zh) 1993-03-17
PT87163A (pt) 1988-05-01
CA1329937C (en) 1994-05-31
MX11031A (es) 1993-11-01
GR3003267T3 (en) 1993-02-17
IL85988A0 (en) 1988-09-30
KR880012526A (ko) 1988-11-28
EP0288188A1 (de) 1988-10-26
PT87163B (pt) 1992-07-31
PH27141A (en) 1993-04-02
ATE68473T1 (de) 1991-11-15
DE3865504D1 (de) 1991-11-21
DK170637B1 (da) 1995-11-20
EG18584A (en) 1994-07-30
ES2045109T3 (es) 1994-01-16
IL85988A (en) 1992-08-18
CN88102018A (zh) 1988-10-26
DK188288A (da) 1989-01-12
JPH0637443B2 (ja) 1994-05-18
SU1568886A3 (ru) 1990-05-30
HU204767B (en) 1992-02-28
SG67092G (en) 1992-09-04
JPS63258837A (ja) 1988-10-26
CY1658A (en) 1993-05-14
KR960007723B1 (ko) 1996-06-11
HUT50316A (en) 1990-01-29
NZ224161A (en) 1990-04-26

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Legal Events

Date Code Title Description
PC Patent ceased (i.e. patent has lapsed due to the failure to pay the renewal fee)