HUP0000479A2 - Alfa-2-adrenoreceptor agonistákként alkalmazható guanidinil-amino-heterociklusos vegyületek, és ezeket a vegyületeket tartalmazó gyógyszerkészítmények - Google Patents

Alfa-2-adrenoreceptor agonistákként alkalmazható guanidinil-amino-heterociklusos vegyületek, és ezeket a vegyületeket tartalmazó gyógyszerkészítmények

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Publication number
HUP0000479A2
HUP0000479A2 HU0000479A HUP0000479A HUP0000479A2 HU P0000479 A2 HUP0000479 A2 HU P0000479A2 HU 0000479 A HU0000479 A HU 0000479A HU P0000479 A HUP0000479 A HU P0000479A HU P0000479 A2 HUP0000479 A2 HU P0000479A2
Authority
HU
Hungary
Prior art keywords
alkenyl
alkyl
hydrogen
powder
cyclic
Prior art date
Application number
HU0000479A
Other languages
English (en)
Inventor
Jeffrey Joseph Ares
Sophie Eva Bogdan
Thomas Lee Cupps
Raymond Todd Henry
William Lee Seibel
Russel James Sheldon
Original Assignee
The Procter & Gamble Co.
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 The Procter & Gamble Co. filed Critical The Procter & Gamble Co.
Publication of HUP0000479A2 publication Critical patent/HUP0000479A2/hu
Publication of HUP0000479A3 publication Critical patent/HUP0000479A3/hu

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/38—Nitrogen atoms
    • C07D215/40—Nitrogen atoms attached in position 8
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • 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
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/38—Cellulose; Derivatives thereof
    • 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
    • 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
    • A61K9/0043—Nose
    • 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
    • A61K9/0048—Eye, e.g. artificial tears
    • 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
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A61K9/0056—Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
    • 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
    • A61K9/007—Pulmonary tract; Aromatherapy
    • A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
    • A61K9/008—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy comprising drug dissolved or suspended in liquid propellant for inhalation via a pressurized metered dose inhaler [MDI]
    • 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
    • A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
    • A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
    • 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
    • A61K9/06—Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2009—Inorganic compounds
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • 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
    • 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
    • A61P1/04—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory 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
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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
    • A61P27/16—Otologicals
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Ophthalmology & Optometry (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Otolaryngology (AREA)
  • Pulmonology (AREA)
  • Inorganic Chemistry (AREA)
  • Dermatology (AREA)
  • Psychiatry (AREA)
  • Biophysics (AREA)
  • Physiology (AREA)
  • Nutrition Science (AREA)
  • Zoology (AREA)
  • Addiction (AREA)
  • Molecular Biology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Indole Compounds (AREA)
  • Quinoline Compounds (AREA)

Abstract

A találmány (I) általánős képletű vegyületekre -, ahől a) R1hidrőgénatőm; alkilcsőpőrt vagy nincs jelen, amikőr (a) kettős kötés;b) DCR2 csőpőrt, ahől R2 hidrőgénatőm; szűbsztitűálatlan alkil-,aminő-, hidrőxi-, merkaptő-, alkil-tiő-, alkőxi-, alkil-aminő-,dialkil-aminő-csőpőrt vagy halőgénatőm; vagy ha BCR3 csőpőrt, Dnitrőgénatőm is lehet; c) B=NR9, -CR3=CR8-, -CR3=N-, CR3, tiő-, őxi-,szűlfinil- vagy szűlfőnilcsőpőrt; ahől R9 hidrőgénatőm;szűbsztitűálatlan alkil-, alkenil- vagy alkinilcsőpőrt; ciklőalkil-,ciklőalkenilcsőpőrt; és ahől R3 és R8 hidrőgénatőm; szűbsztitűálatlanalkil-, alkenil- vagy alkinilcsőpőrt; ciklőalkil-, ciklőalkenil-,szűbsztitűálatlan alkil-tiő- vagy alkőxi-hidrőxi-, merkaptő-, nitrő-,cianő-, aminő-, alkil-aminő-, dialkil-aminő-csőpőrt, vagy halőgénatőm;d) R4, R5 és R6 hidrőgénatőm; szűbsztitűálatlan alkil-, alkenil- vagyalkinilcsőpőrt; ciklőalkil-, ciklőalkenil-, szűbsztitűálatlan alkil-tiő- vagy alkőxi-, hidrőxi-, merkaptő-, nitrő-, cianő-, aminő-, alkil-aminő- vagy dialkil-aminő-csőpőrt; halőgénatőm; és -NH-NH-C (=NR10)NHRl1 csőpőrt; ahől R10 és R11 hidrőgénatőm, metil- vagy etilcsőpőrt;és ahől R4, R5 és R6 egyike és csak egyike gűanidinil-aminő-csőpőrt;és e) R7 hidrőgénatőm; szűbsztitűálatlan alkil-, alkenil- vagyalkinilcsőpőrt; ciklőalkil-, ciklőalkenil-, szűbsztitűálatlan alkil-tiő- vagy alkőxi-, hidrőxi-, merkaptő-, nitrő-, cianő-, aminő-, alkil-aminő- vagy dialkil-aminő-csőpőrt; és halőgénatőm - ésenantiőmereikre, őptikai izőmereikre, sztereőizőmereikre,diasztereőmereikre, taűtőmereikre, addíciós sóikra, biőhidrőlizálhatóamidjaikra és észtereikre, ezeket tartalmazó gyógyszerkészítményekrevőnatkőzik. ŕ
HU0000479A 1996-11-25 1997-11-21 Guanidinylamino heterocycle compounds useful as alpha-2 adrenoceptor agonists and pharmaceutical compositions containing them HUP0000479A3 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US3183396P 1996-11-25 1996-11-25
PCT/US1997/020550 WO1998023591A1 (en) 1996-11-25 1997-11-21 Guanidinylamino heterocycle compounds useful as alpha-2 adrenoceptor agonists

Publications (2)

Publication Number Publication Date
HUP0000479A2 true HUP0000479A2 (hu) 2000-09-28
HUP0000479A3 HUP0000479A3 (en) 2002-06-28

Family

ID=21861650

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0000479A HUP0000479A3 (en) 1996-11-25 1997-11-21 Guanidinylamino heterocycle compounds useful as alpha-2 adrenoceptor agonists and pharmaceutical compositions containing them

Country Status (23)

Country Link
EP (1) EP0944601B1 (hu)
JP (1) JP2001504839A (hu)
KR (1) KR20000069130A (hu)
CN (1) CN1163486C (hu)
AR (1) AR009144A1 (hu)
AT (1) ATE232518T1 (hu)
AU (1) AU729421B2 (hu)
BR (1) BR9714362A (hu)
CA (1) CA2272098C (hu)
CZ (1) CZ183799A3 (hu)
DE (1) DE69719068T2 (hu)
DK (1) DK0944601T3 (hu)
ES (1) ES2192703T3 (hu)
HU (1) HUP0000479A3 (hu)
ID (1) ID23038A (hu)
IL (1) IL130023A0 (hu)
NO (1) NO313286B1 (hu)
NZ (1) NZ335859A (hu)
PE (1) PE16499A1 (hu)
SK (1) SK68599A3 (hu)
TR (1) TR199901467T2 (hu)
WO (1) WO1998023591A1 (hu)
ZA (1) ZA9710575B (hu)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6306877B1 (en) 1999-08-09 2001-10-23 The Procter & Gamble Co. Guanidinylamino heterocycle compounds useful as alpha-2 adrenoceptor agonists
US6172095B1 (en) 1996-11-25 2001-01-09 The Procter & Gamble Company Guanidinylamino heterocycle compounds useful as alpha-2 adrenoceptor agonists
NL1009376C1 (nl) * 1998-06-11 1998-07-06 Boardwalk Ag Datasysteem voor het verschaffen van relatiepatronen tussen personen.
US6294553B1 (en) * 2000-02-15 2001-09-25 Allergan Sales, Inc. Method for treating ocular pain
US8555875B2 (en) 2008-12-23 2013-10-15 Map Pharmaceuticals, Inc. Inhalation devices and related methods for administration of sedative hypnotic compounds

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5478858A (en) * 1993-12-17 1995-12-26 The Procter & Gamble Company 5-(2-imidazolinylamino) benzimidazole compounds useful as alpha-2 adrenoceptor agonists
US5576437A (en) * 1993-12-17 1996-11-19 The Procter & Gamble Company 7-(2-imidazolnylamino) quinoline compounds useful as alpha-2 adrenoceptor agonists

Also Published As

Publication number Publication date
CN1163486C (zh) 2004-08-25
EP0944601B1 (en) 2003-02-12
NO992503D0 (no) 1999-05-25
CA2272098A1 (en) 1998-06-04
TR199901467T2 (xx) 1999-10-21
CA2272098C (en) 2003-11-11
PE16499A1 (es) 1999-03-12
DE69719068T2 (de) 2003-11-27
CZ183799A3 (cs) 1999-09-15
JP2001504839A (ja) 2001-04-10
SK68599A3 (en) 2000-06-12
IL130023A0 (en) 2000-02-29
BR9714362A (pt) 2000-03-21
ATE232518T1 (de) 2003-02-15
EP0944601A1 (en) 1999-09-29
ID23038A (id) 2000-01-06
CN1242001A (zh) 2000-01-19
AU7402598A (en) 1998-06-22
AR009144A1 (es) 2000-03-08
NZ335859A (en) 2000-11-24
WO1998023591A1 (en) 1998-06-04
DK0944601T3 (da) 2003-06-10
NO992503L (no) 1999-07-23
ES2192703T3 (es) 2003-10-16
HUP0000479A3 (en) 2002-06-28
NO313286B1 (no) 2002-09-09
DE69719068D1 (de) 2003-03-20
ZA9710575B (en) 1998-06-10
KR20000069130A (ko) 2000-11-25
AU729421B2 (en) 2001-02-01

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