HUP0402357A2 - Antihisztaminok alkalmazása megnövelt koponyán belüli nyomás akut csökkentésére és gyógyszerkészítmények előállítására - Google Patents

Antihisztaminok alkalmazása megnövelt koponyán belüli nyomás akut csökkentésére és gyógyszerkészítmények előállítására

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Publication number
HUP0402357A2
HUP0402357A2 HU0402357A HUP0402357A HUP0402357A2 HU P0402357 A2 HUP0402357 A2 HU P0402357A2 HU 0402357 A HU0402357 A HU 0402357A HU P0402357 A HUP0402357 A HU P0402357A HU P0402357 A2 HUP0402357 A2 HU P0402357A2
Authority
HU
Hungary
Prior art keywords
alkyl
het
amino
independently
intracranial pressure
Prior art date
Application number
HU0402357A
Other languages
English (en)
Inventor
Frank Tegtmeier
Frans Eduard Janssens
Joseph Elisabeth Leenaerts
Koenraad Arthur Rossem
Manuel Jesús Alcázar-Vaca
Pedro Martínez-Jiménez
José Manuel Bartolomé-Nebreda
Antonio Gómez-Sánchez
Francisco Javier Fernández-Gadea
Jozef Leo Henri Van Reempts
Original Assignee
Janssen Pharmaceutica N.V.
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.)
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Publication date
Application filed by Janssen Pharmaceutica N.V. filed Critical Janssen Pharmaceutica N.V.
Publication of HUP0402357A2 publication Critical patent/HUP0402357A2/hu
Publication of HUP0402357A3 publication Critical patent/HUP0402357A3/hu
Publication of HU229118B1 publication Critical patent/HU229118B1/hu

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/02Nasal agents, e.g. decongestants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/04Antipruritics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Nutrition Science (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Vascular Medicine (AREA)
  • Transplantation (AREA)
  • Epidemiology (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)

Abstract

A találmány tárgya új hisztamin receptor antagonista, és a hisztaminreceptor antagonista alkalmazása koponyán belüli nyomás (ICP)csökkentésére, különösen megnövelt koponyán belüli nyomás és/vagyszekunder iszchémia kezelésére és megelőzésére, különösen olyanesetekben, amikor az ilyen állapotokat agysérülés, közelebbről traumás(TBI) vagy nem traumás agysérülés idézi elő. Az új vegyületek (I)általános képletű vegyületek, gyógyászatilag elfogadható sav- vagybázis-addíciós sói, sztereokémiai izomer formák és N-oxid formái. Azelőnyös vegyület a 3-[2-[4-(11,12-dihidro-6-H-benzimidazo[2,1-b][3]benzazepin-6-il)-2-(fenil-metil)-1-piperidinil]-etil)-2,10-dimetil-pirimido[1,2-a)benzimidazol-4(10)-on, gyógyászatilag elfogadható sav- vagy bázisaddíciós sói,sztereokémiai izomer formái és N-oxidjai. Kiterjed a találmány akereskedelemben kapható hisztamin H1- és H2-receptor antagonisták újalkalmazására koponyán belüli nyomás (ICP) csökkentésére is. Az (I)általános képletű vegyület, gyógyászatilag elfogadható sav- vagybázisaddíciós sója, sztereokémiai izomer formája és N-oxidjai, ahol mértéke 1 vagy 2; n értéke 0, 1 vagy 2; a, b, c jelentése egymástólfüggetlenül vegyértékvonal vagy kettős kötés; X jelentése kovalenskötés vagy kétértékű 1-6 szénatomos alkán-diil-csoport, ahol egy vagytöbb -CH2- csoportot adott esetben -O-, -S-, -CO- vagy -NR7-helyettesít, Y jelentése kétértékű 1-4 szénatomos alkán-diil- vagy 2-4szénatomos alkén-diil-csoport; Z jelentése nitrogénatom, ez esetben ajelentése kettős kötés és b vegyértékvonal, vagy Z jelentése N-R7,amely esetben a jelentése vegyértékvonal és b kettős kötés és R7jelentése a fenti; R1 és R2 jelentése egymástól függetlenülhidrogénatom, hidroxil-, alkil-, alkoxi-, Ar, Ar-alkil-, di(Ar)-alkil-, Het vagy Het-alkil-csoport; -A-B-jelentése egymástólfüggetlenül az alábbi kétértékű csoportok valamelyike: -E-CR8=CR8- (a-1); -CR8=CR8-E- (a-2); -CR8=CR8-CR8=CR8- (a-3); ahol R8 jelentéseegymástól függetlenül hidrogén- vagy halogénatom, hidroxil-, - alkil-vagy alkoxicsoport; E jelentése kétértékű -O-, -S- vagy -NR7-, ahol R7jelentése a fenti; -C-D- jelentése egymástól függetlenül az alábbikétértékű csoportok valamelyike: -CR8=CR8-CR8=CR8- (b-1); -N=CR8-CR8=CR8- (b-2); -CRB=N-CR8=CR8- (b-3); -CR8=CR8-N=CR8- (b-4); -CRB=CR8-CR8=N- (b-5); ahol R8 jelentése a fenti; R3 jelentésehidrogén- vagy halogénatom, hidroxil-, alkil-, alkoxi-, Ar, Ar-alkil-,di(Ar)-alkil-, Het vagy Het-alkil-csoport; R4 jelentése hidrogénatom,alkil-, amino-, alkil-amino-, Ar-amino-, Het-amino-, alkil-karbonil-amino-, Ar-karbonil-amino-, Het-karbonil-amino-, alkil-amino-karbonil-amino-, Ar-amino-karbonil-amino-, Het-amino-karbonil-amino-, alkoxi-alkil-amino-, Ar-oxi-alkil-amino- vagy Het-oxi-alkil-amino-csoport; R5jelentése hidrogénatom vagy alkilcsoport. Ó
HU0402357A 2001-11-23 2002-11-22 The use of substituted tetracyclic imidazole derivatives as anti-histaminics HU229118B1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP01204574 2001-11-23
PCT/EP2002/013180 WO2003044023A1 (en) 2001-11-23 2002-11-22 The use of anti-histaminics for acute reduction of elevated intracranial pressure

Publications (3)

Publication Number Publication Date
HUP0402357A2 true HUP0402357A2 (hu) 2005-02-28
HUP0402357A3 HUP0402357A3 (en) 2009-10-28
HU229118B1 HU229118B1 (en) 2013-08-28

Family

ID=8181317

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0402357A HU229118B1 (en) 2001-11-23 2002-11-22 The use of substituted tetracyclic imidazole derivatives as anti-histaminics

Country Status (26)

Country Link
US (1) US7732437B2 (hu)
EP (2) EP1451196B1 (hu)
JP (2) JP4505226B2 (hu)
KR (1) KR100967601B1 (hu)
CN (2) CN100478031C (hu)
AT (2) ATE370149T1 (hu)
AU (1) AU2002356715B2 (hu)
CA (2) CA2467097C (hu)
CY (2) CY1107472T1 (hu)
DE (2) DE60231351D1 (hu)
DK (2) DK1451196T3 (hu)
ES (2) ES2290364T3 (hu)
HK (2) HK1073309A1 (hu)
HR (1) HRP20040427B1 (hu)
HU (1) HU229118B1 (hu)
IL (4) IL162109A0 (hu)
MX (1) MXPA04004867A (hu)
NO (1) NO333656B1 (hu)
NZ (2) NZ550723A (hu)
PL (1) PL209953B1 (hu)
PT (2) PT1451196E (hu)
RU (1) RU2311418C2 (hu)
SI (2) SI1451196T1 (hu)
UA (1) UA76803C2 (hu)
WO (1) WO2003044023A1 (hu)
ZA (1) ZA200403923B (hu)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK1451196T3 (da) 2001-11-23 2007-11-12 Janssen Pharmaceutica Nv Anvendelse af substituerede tetracykliske imidazolderivater som antihistaminstoffer
TWI290140B (en) * 2003-08-25 2007-11-21 Schering Corp 2-Substituted benzimidazole derivatives as selective melanin concentrating hormone receptor antagonists for thr treatment of obesity and related disorders
EP2796683A4 (en) * 2011-12-20 2015-05-20 Toyota Motor Co Ltd ERROR DETECTION DEVICE FOR AN ELECTRICALLY HEATABLE CATALYST
US9717726B2 (en) * 2013-03-14 2017-08-01 Maregade Rx, LLC Product and method for treating diarrhea
EP3558296B1 (en) 2016-12-23 2023-06-28 Maregade RX, LLC Low dose product and method for treating diarrhea
US10947253B2 (en) 2019-08-05 2021-03-16 Ankh Life Sciences Limited Fused polycyclic dimers

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5595988A (en) * 1992-12-04 1997-01-21 Janssen Pharmaceutica N.V. Triazolo(pyrrolo, thieno or furano)azepine derivatives
TW382017B (en) * 1995-12-27 2000-02-11 Janssen Pharmaceutica Nv 1-(1,2-disubstituted piperidinyl)-4-(fused imidazole)-piperidine derivatives
TW429256B (en) 1995-12-27 2001-04-11 Janssen Pharmaceutica Nv 1-(1,2-disubstituted piperidinyl)-4-(benzimidazolyl- and imidazopyridinyl)-piperidine derivatives
TW527186B (en) * 1996-03-19 2003-04-11 Janssen Pharmaceutica Nv Fused imidazole derivatives as multidrug resistance modulators
EP1011726B1 (en) * 1997-09-18 2003-02-26 Janssen Pharmaceutica N.V. Fused imidazole derivatives for improving oral bioavailability of pharmaceutical agents
EP1401838B1 (en) * 2001-06-12 2014-03-26 Janssen Pharmaceutica NV Novel substituted tetracyclic imidazole derivatives, processes for their preparation, pharmaceutical compositions comprising them and their use as a medicine
DK1451196T3 (da) 2001-11-23 2007-11-12 Janssen Pharmaceutica Nv Anvendelse af substituerede tetracykliske imidazolderivater som antihistaminstoffer

Also Published As

Publication number Publication date
SI1832287T1 (sl) 2009-06-30
DE60221891T2 (de) 2008-05-08
DE60221891D1 (de) 2007-09-27
MXPA04004867A (es) 2004-07-30
CY1107472T1 (el) 2012-12-19
IL162109A0 (en) 2005-11-20
EP1451196A1 (en) 2004-09-01
EP1832287A3 (en) 2007-12-26
IL194992A (en) 2010-12-30
IL188457A (en) 2010-11-30
SI1451196T1 (sl) 2007-12-31
NO333656B1 (no) 2013-08-05
ATE370149T1 (de) 2007-09-15
EP1832287A2 (en) 2007-09-12
IL188457A0 (en) 2008-03-20
ES2290364T3 (es) 2008-02-16
EP1451196B1 (en) 2007-08-15
DE60231351D1 (de) 2009-04-09
RU2311418C2 (ru) 2007-11-27
NZ532718A (en) 2007-01-26
IL194992A0 (en) 2009-08-03
CN100478031C (zh) 2009-04-15
JP4505226B2 (ja) 2010-07-21
PL209953B1 (pl) 2011-11-30
WO2003044023A1 (en) 2003-05-30
HK1073309A1 (en) 2005-09-30
AU2002356715A1 (en) 2003-06-10
PT1832287E (pt) 2009-05-05
HRP20040427B1 (en) 2012-09-30
HRP20040427A2 (en) 2005-06-30
HU229118B1 (en) 2013-08-28
JP2009102417A (ja) 2009-05-14
DK1451196T3 (da) 2007-11-12
KR20050044328A (ko) 2005-05-12
AU2002356715B2 (en) 2008-05-15
JP4991770B2 (ja) 2012-08-01
CA2690483A1 (en) 2003-05-30
NO20042618L (no) 2004-06-22
CA2467097C (en) 2011-02-01
NZ550723A (en) 2008-06-30
CN100379744C (zh) 2008-04-09
EP1832287B1 (en) 2009-02-25
ATE423599T1 (de) 2009-03-15
JP2005509680A (ja) 2005-04-14
ZA200403923B (en) 2005-10-26
HK1101672A1 (en) 2007-10-26
US20050070525A1 (en) 2005-03-31
ES2321987T3 (es) 2009-06-15
DK1832287T3 (da) 2009-06-08
CA2467097A1 (en) 2003-05-30
CN1895673A (zh) 2007-01-17
CA2690483C (en) 2012-07-24
KR100967601B1 (ko) 2010-07-05
CN1589273A (zh) 2005-03-02
UA76803C2 (uk) 2006-09-15
IL162109A (en) 2010-04-29
RU2004118838A (ru) 2005-04-10
CY1109108T1 (el) 2014-07-02
PL369864A1 (en) 2005-05-02
US7732437B2 (en) 2010-06-08
HUP0402357A3 (en) 2009-10-28
PT1451196E (pt) 2007-10-25

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