DK2382013T3 - Selektive histamin h4-receptorantagonister til behandling af vestibulære sygdomme - Google Patents

Selektive histamin h4-receptorantagonister til behandling af vestibulære sygdomme Download PDF

Info

Publication number
DK2382013T3
DK2382013T3 DK09798938.8T DK09798938T DK2382013T3 DK 2382013 T3 DK2382013 T3 DK 2382013T3 DK 09798938 T DK09798938 T DK 09798938T DK 2382013 T3 DK2382013 T3 DK 2382013T3
Authority
DK
Denmark
Prior art keywords
pyrimidin
methyl
amine
methylamino
pyrrolidin
Prior art date
Application number
DK09798938.8T
Other languages
English (en)
Inventor
Gilles Desmadryl
Christian Chabbert
Original Assignee
Inserm (Institut Nat De La Santé Et De La Rech Médicale)
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 Inserm (Institut Nat De La Santé Et De La Rech Médicale) filed Critical Inserm (Institut Nat De La Santé Et De La Rech Médicale)
Application granted granted Critical
Publication of DK2382013T3 publication Critical patent/DK2382013T3/da

Links

Classifications

    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K48/00—Medicinal preparations containing genetic material which is inserted into cells of the living body to treat genetic diseases; Gene therapy
    • A61K48/005—Medicinal preparations containing genetic material which is inserted into cells of the living body to treat genetic diseases; Gene therapy characterised by an aspect of the 'active' part of the composition delivered, i.e. the nucleic acid delivered
    • A61K48/0058—Nucleic acids adapted for tissue specific expression, e.g. having tissue specific promoters as part of a contruct
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • 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
    • A61P25/06—Antimigraine agents
    • 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
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • 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
    • A61K9/0046—Ear

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Immunology (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Oncology (AREA)
  • Otolaryngology (AREA)
  • Communicable Diseases (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Claims (6)

1. Selektiv Histamin H4-receptorantagonist til anvendelse til behandling og/eller forebyggelse af mindst ét symptom på vestibulære sygdomme, hvor den selektive Histamin H4-receptorantagonist: har et KiH3 :KiH4-forhold på over 10:1 og er udvalgt fra gruppen bestående af: • 1 -[(5-chlor-1 H-benzimidazol-2-yl)carbonyl] -4-methylpiperazin, • l-[(5-chlor-lH-indol-2-yl)carbonyl]-4-methylpiperazin, • 4-((3R)-3-aminopyrrolidin-l-yl)-6,7-dihydro-5H-benzo[6,7]cyclohepta[l,2-d]pyrimidin-2-ylamin, • cis-4-(Piperazin-l-yl)-5,6,7a,8,9,10,l 1,1 la-octahydrobenzofuro[2,3-h]quinazolin-2-amin, • 2-isobutyl-6-(3-(methylamino)azetidin-l -yl)pyrimidin-4-amin, • 2-isobutyl-6-((3r)-3 -(methylamino)pyrrolidin-1 -yl)pyrimidin-4-amin, • 2-cyclohexylmethyl-6-((3r)-3-(methylamino)pyrrolidin-lyl)pyrimidin-4-amin, • 2-(4-fhrorbenzyl)-6-(3-(methylamino)azetidin-l-yl)pyrimidin-4-amin, • 2-cyclopropyl-6-(3-(methylamino)azetidin-l-yl)pyrimidin-4-amin, • 2-tert-butyl-6-(3 -(methylamino)azetidin-1 -yl)pyrimidin-4-amin, • 2-isopropyl-6-(3 -(methylamino)azetidin-l-yl)pyrimidin-4-amin, • 2-(cyclopropylmethyl)-6-(3 -(methylamino)azetidin-1 -yl)pyrimidin-4-amin, • 6-(3 -(methylamino)azetidin-1 -yl)-2-(phenoxymethyl)pyrimidin-4-amin, • 2-cyclopropyl-6-((3r)-3-(methylamino)pyrrolidin-l-yl)pyrimidin-4-amin, • 2-tert-butyl-6-((3r)-3-(methylamino)pyrrolidin-l-yl)pyrimidin-4-amin, • 2-isopropyl-6-((3r)-3-(methylamino)pyrrolidin-l-yl)pyrimidin-4-amin, • 6-((3r)-3-(methylamino)pyrrolidin-l-yl)-2-(phenoxymethyl)pyrimidin-4-amin, • 6-(3 -aminoazetidin-1 -yl)-2-isobutylpyrimidin-4-amin, • 2-isobutyl-6-(3-methyl-3-(methylamino)azetidin-l-yl)-pyrimidin-4-amin, • 6-((3r)-3 -aminopyrrolidin-1 -yl)-2-isobutylpyrimidin-4-amin, • 2-cyclobutyl-6-(3 -(methylamino)azetidin-1 -yl)pyrimidin-4-amin, • 2-cyclobutyl-6-((3R)-3-(methylamino)pyrrolidin-l-yl)pyrimidin-4-amin, • 2-cyclopentyl-6-(3-(methylamino)azetidin-l -yl)pyrimidin-4-amin, • 2-Cyclopentyl-6-((3R)-3-(methylamino)pyrrolidin-l-yl)pyrimidin-4-amin, • 2-(2,2-dimethylpropyl)-6-(3-(methylamino)azetidin-l-yl)pyrimidin-4-amin, • 2-(2,2-dimethylpropyl)-6-((3R)-3-(methylamino)pyrrolidin-l-yl)pyrimidin-4-amin, • 2-(2-cyclopentylethyl)-6-((3R)-3 -(methylamino)pyrrolidin-1 -yl)pyrimidin-4-amin, • 2-cyclohexylmethyl-6-(3-(methylamino)azetidin-l-yl)pyrimidin-4-amin, • 2-cyclopropylmethyl-6-((3R)-3-(methylamino)pyrrolidin-l-yl)pyrimidin-4-amin, • 2-cyclohexyl-6-(3-(methylamino)azetidin-l-yl)pyrimidin-4-amin, • 2-cyclohexyl-6-((3R)-3 -(methylamino)pyrrolidin-1 -yl)pyrimidin-4-amin, • 2-(4-fluorbenzyl)-6-((3R)-3-(methylamino)pyrrolidin-l-yl)pyrimidin-4-amin, • N4-(cyclopropyhnethyl)-6-[(3R)-3-(methylammo)pyrrolidin-l-yl]pyrimidin-2,4-diamin, • N4-(cyclopropylmethyl)-6-[(3R)-3-(methylammo)pyrrolidin-l-yl]pyrimidin-2,4-diamintartrat, • N4-isobutyI-6-[(3R)-3-(mcthylamino)pyrrolidin-l-yl]pyrimidin-2,4-diamin, • N4-(2,2-dimethylpropyl)-6-[(3R)-3-(methylamino)pyrrolidin-l-yl]pyrimidin-2,4-diamin • N-isobutyl-6-[(3R)-3-(methylamino)pyrrolidin-l-yl]pyrimidin-4-amin, • N-(cyclopropylmethyl)-6-[(3R)-3-(methylamino)pynOlidin-l-yl]pyrimidin-4-amin, • N4-(2,2-dimethylpropyl)-6-[(4aR*,7aR*)-octahydro-6H-pyrrol[3,4-b]pyridin-6-yl] pyrimidin-2,4 -diamin, • N4-cyclopropyl-6-[(4aR*,7aR*)-octahydro-6H-pyrTol[3,4-b]pyridin-6-yl]pyrimidin-2,4-diamin • N4-cyclobutyl-6-[(4aR*,7aR*)-octahydro-6H-pyrrol[3,4-b]pyridin-6-yl]pyrimidin-2,4-diamin, • N4-(2,2-dimethylpropyl)-6-[3-(methylamino)azetidin-l-yl]pyrimidin-2,4-diamin, • 6-(3-methylamino-azetidin-l-yl)-N4-(3,3,3-trifluor-propyl)-pyrimidin-2,4-diamin, • N4-cyclopropylmethyl-6-(3-methylamino-azetidin-l-yl)-pyrimidin-2,4-diamin, • N4-(3,3-dimethyl-butyl)-6-(3-methylamino-azetidin-l-yl)-pyrimidin-2,4-diamin, • N4-(3-fluor-benzyl)-6-(3-methylamino-azetidin-l-yl)-pyrimidin-2,4-diamin, • N4-cyclopentylmethyl-6-(3-methylamino-azetidin-l-yl)-pyrimidin-2,4-diamin, • N4-isobutyl-6-[3 -(methylamino)azetidin-l -yl]pyrimidin-2,4-diamin, • 6- [3 -(methylamino)azetidin-1 -yl] -N4-propyl-pyrimidin-2,4-diamin, • N4-(2-methoxybenzyl)-6-[3-(methylamino)azetidin-l-yl]pyrimidin-2,4-diamin, • N4-(2,2-dimethylpropyl)-6-[(3R)-3-methylpiperazin-l-yl]pyrimidin-2,4-diamin, • N4-ethyl-6-(4-methylpiperazin-1 -yl)pyrimidin-2,4-diamin, • N4-(cyclopropylmethyl)-6-(4-methylpiperazin-1 -yl)pyrimidin-2,4-diamin, • 6-[3-(methylamino)azetidin-l-yl]-N4-(2-methylbutyl)pyrimidin-2,4-diamin, • N4-(2,5-difluorbenzyl)-6-[3-(methylamino)azetidin-l-yl]pyrimidin-2,4-diamin, • N4-(2,3-difluorbenzyl)-6-[3-(methylamino)azetidin-l-yl]pyrimidin-2,4-diamin, • N4-butyl-6-[3-(methylamino)azetidin-l -yl]pyrimidin-2,4-diamin, • 6-[(3R)-3-(methylamino)pyrrolidin-l-yl]-N4-(2-methylcyclopropyl)pyrimidin-2,4-diamin, • N4-isobutyl-6-(4 -methyl-1,4-diazepan-1 -yl)pyrimidin-2,4-diamin, • N4-(cyclopropylmethyl)-6-(3-pynOlidin-l-yl-azetidin-l-yl)pyrimidin-2,4-diamin, • N4-bicyclo[l. 1.1 ]pent-l -yl-6-[(3R)-3-(methylamino)pyrrolidin-l -yl]pyrimidin-2,4-diamin, • 6- [3 -methyl-3 -(methylamino)azetidin-1 -yl] -N4-propylpyrimidin-2,4-diamin, • N4-(2,2-dimethylpropyl)-6-(hexahydropyrrol[l,2-a]pyrazin-2(lH)-yl)pyrimidin-2,4-diamin, • N4-(2,2-dimethylpropyl)-6-(3-pyrrolidin-l-yl-azetidin-l-yl)pyrimidin-2,4-diamin, • N4-(2,2-dimethylpropyl)-6-[3-(isopropylamino)azetidin-l-yl]pyrimidin-2,4-diamin, • N4-(tert-butyl)-6-[(3R)-3-(methylamino)pyrrolidin-l-yl]pyrimidin-2,4-diamin, • 6-[(3R)-3-(methylamino)pyrrolidin-l-yl]-N4-(l-methylcyclopropyl)pyrimidin-2,4-diamin, • N4-(tert-butyl)-6-[(4aS*,7aS*)-octahydro-6H-pyrrol[3,4-b]pyridin-6-yl]pyrimidin-2,4-diamin, • N4-(2,2-dimethylpropyl)-6-piperazin-1 -ylpyrimidin-2,4-diamin, • N4-(2,2-dimethylpropyl)-6-[3-(methylamino)azetidin-l-yl]pyrimidin-2,4-diaminhydrochlorid, • N4-(2,2-dimethylpropyl)-6-[(3aR*,7aS*)-octahydro-5H-pyrrol[3,2-c]pyridin-5-yl] pyrimidin-2,4 -diamin, • 6-piperazin-1 -yl-N4-propylpyrimidin-2,4-diamin, • N4-(cyclopropylmethyl)-6-[4aR,7aR]-octahydro-6H-pyrrol[3,4-b]pyridin-6-yl]pyrimidin- 2.4- diamin, • N4-(2,2-dimethylpropyl)-6-[(4aS,7aS)-octahydro-6H-pyrrol[3,4-b]pyridin-6-yl]pyrimidin- 2.4- diamin, • N4-(cyclopropylmethyl)-6-[(3R)-3-(methylamino)pyrrolidin-l-yl]pyrimidin-2,4-diamin, • N4-isopropyl-6-[(4aS,7aS)-octahydro-6H-pyrrol[3,4-b]pyridin-6-yl]pyrimidin-2,4-diamin, • 4- [3 -(methylamino)azetidin-1 -yl] -6-(4-methylpiperidin-1 -yl)pyrimidin-2-amin, • N4-(cyclopentylmethyl)-6-[(3R)-3-(methylamino)pyrrolidin-l-yl]pymmdin-2,4-diamin, • N4-cyclobutyl-6-[(4aS,7aS)-octahydro-6H-pyrrol[3,4-b]pyridin-6-yl]pyrimidin-2,4-diamin, • 6-[(3R)-3-(methylamino)pyrrolidin-l-yl]-N4-propylpyrimidin-2,4-diamin og • N4-ethyl-6-(4-methyl-1,4-diazepan-1 -yl)pyrimidin-2,4-diamin.
2. Selektiv Histamin H4-receptorantagonist til anvendelse ifølge krav 1, hvor mindst et symptom på vestibulær sygdom er udvalgt fra gruppen bestående af vertigo, svimmelhed, ubalance og kvalme.
3. Selektiv Histamin H4-receptorantagonist til anvendelse ifølge krav 1 eller 2, hvor vertigo er en benign paroksysmal vertigo eller familiær episodisk vertigo.
4. Selektiv Histamin H4-receptorantagonist til anvendelse ifølge et hvilket som helst af kravene 1 til 3, hvor den vestibulære sygdom er udvalgt fra vestibulær neurit, anfald af Meniéres sygdom, endolymfatiske hydrops, perilymfatisk fistel, hovedtraume med vestibulære sygdomme, labyrintblødning, kronisk eller akut labyrintinfektion, svær labyrintisk, barotraume med vestibulære sygdomme, vestibulære syndromer efter autoimmun sygdom i det indre øre, vestibulær migræne, vestibulære syndromer efter kirurgiske behandlinger af mellemøret, endolymfatiske sæk eller cerebello-pontinvinkeltumorer, indre øre-kanalopatier, kronisk Meniéres sygdom, vestibulære schwannomer, presbyvestibulia og vestibulær ataksi.
5. Selektiv Histamin H4-receptorantagonist til anvendelse ifølge et hvilket som helst af kravene 1 til 4 til administration via trommehinden eller til systemisk administration.
6. Farmaceutisk sammensætning, der omfatter en selektiv Histamin H4 receptorantagonist ifølge et hvilket som helst af kravene 1 til 5 til anvendelse til behandling og/eller forebyggelse af mindst ét symptom på vestibulære sygdomme.
DK09798938.8T 2008-12-24 2009-12-23 Selektive histamin h4-receptorantagonister til behandling af vestibulære sygdomme DK2382013T3 (da)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP20080306013 EP2201982A1 (en) 2008-12-24 2008-12-24 Histamine H4 receptor antagonists for the treatment of vestibular disorders
PCT/EP2009/067897 WO2010072829A1 (en) 2008-12-24 2009-12-23 Selective histamine h4 receptor antagonists for the treatment of vestibular disorders.

Publications (1)

Publication Number Publication Date
DK2382013T3 true DK2382013T3 (da) 2016-11-14

Family

ID=40466853

Family Applications (1)

Application Number Title Priority Date Filing Date
DK09798938.8T DK2382013T3 (da) 2008-12-24 2009-12-23 Selektive histamin h4-receptorantagonister til behandling af vestibulære sygdomme

Country Status (19)

Country Link
US (2) US9526725B2 (da)
EP (3) EP2201982A1 (da)
JP (2) JP5814126B2 (da)
KR (1) KR101749285B1 (da)
CN (2) CN107050030A (da)
CA (1) CA2748159C (da)
CY (1) CY1118106T1 (da)
DK (1) DK2382013T3 (da)
ES (1) ES2597834T3 (da)
HR (1) HRP20161290T1 (da)
HU (1) HUE031645T2 (da)
IL (1) IL213540A (da)
LT (1) LT2382013T (da)
PL (1) PL2382013T3 (da)
PT (1) PT2382013T (da)
RU (1) RU2589846C2 (da)
SI (1) SI2382013T1 (da)
SM (1) SMT201600368B (da)
WO (1) WO2010072829A1 (da)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HUE039713T2 (hu) * 2012-06-08 2019-02-28 Sensorion H4 receptor inhibitorok tinnitus kezelésére
CN105017385B (zh) * 2015-07-02 2018-08-03 吉林大学 基于模拟人组胺受体4（hr4）表位的疫苗及其构建方法
US11180480B2 (en) 2017-10-17 2021-11-23 Sensorion Synthesis of 4-aminopyrimidine compounds

Family Cites Families (64)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB8308235D0 (en) 1983-03-25 1983-05-05 Celltech Ltd Polypeptides
US5225539A (en) 1986-03-27 1993-07-06 Medical Research Council Recombinant altered antibodies and methods of making altered antibodies
US4946778A (en) 1987-09-21 1990-08-07 Genex Corporation Single polypeptide chain binding molecules
RU2214245C2 (ru) * 1997-03-26 2003-10-20 Сепракор Инк. Химически- и термостабильные готовые формы норастемизола
US6506559B1 (en) 1997-12-23 2003-01-14 Carnegie Institute Of Washington Genetic inhibition by double-stranded RNA
AUPP249298A0 (en) 1998-03-20 1998-04-23 Ag-Gene Australia Limited Synthetic genes and genetic constructs comprising same I
US6566131B1 (en) 2000-10-04 2003-05-20 Isis Pharmaceuticals, Inc. Antisense modulation of Smad6 expression
US6410323B1 (en) 1999-08-31 2002-06-25 Isis Pharmaceuticals, Inc. Antisense modulation of human Rho family gene expression
US6107091A (en) 1998-12-03 2000-08-22 Isis Pharmaceuticals Inc. Antisense inhibition of G-alpha-16 expression
US5981732A (en) 1998-12-04 1999-11-09 Isis Pharmaceuticals Inc. Antisense modulation of G-alpha-13 expression
US6093417A (en) * 1999-01-11 2000-07-25 Advanced Medical Instruments Composition to treat ear disorders
US6046321A (en) 1999-04-09 2000-04-04 Isis Pharmaceuticals Inc. Antisense modulation of G-alpha-i1 expression
GB9927444D0 (en) 1999-11-19 2000-01-19 Cancer Res Campaign Tech Inhibiting gene expression
EP1272630A2 (en) 2000-03-16 2003-01-08 Genetica, Inc. Methods and compositions for rna interference
US6365354B1 (en) 2000-07-31 2002-04-02 Isis Pharmaceuticals, Inc. Antisense modulation of lysophospholipase I expression
US6566135B1 (en) 2000-10-04 2003-05-20 Isis Pharmaceuticals, Inc. Antisense modulation of caspase 6 expression
EP1373204B1 (en) 2001-03-09 2016-10-26 Janssen Pharmaceuticals, Inc. Heterocyclic compounds
PL375964A1 (en) 2002-09-06 2005-12-12 Janssen Pharmaceutica, N.V. Use of indolyl derivatives for the manufacture of a medicament for the treatment allergic rhinitis
EP1543011B1 (en) 2002-09-06 2006-05-03 Janssen Pharmaceutica N.V. Thienopyrrolyl and furanopyrrolyl compounds and their use as histamine h4 receptor ligands
WO2004022060A2 (en) 2002-09-06 2004-03-18 Janssen Pharmaceutica, N.V. (1h-benzoimidazol-2-yl)-(piperazinyl)-methanone derivatives and related compounds as histamine h4-receptor antagonists for the treatment of inflammatory and allergic disorders
EP1545596A4 (en) * 2002-09-06 2005-12-28 Janssen Pharmaceutica Nv USE OF HISTAMINE H4 RECEPTOR MODULATORS FOR THE TREATMENT OF ALLERGIES AND ASTHMA
US20040127395A1 (en) 2002-09-06 2004-07-01 Desai Pragnya J. Use of histamine H4 receptor modulators for the treatment of allergy and asthma
US20040105856A1 (en) 2002-12-02 2004-06-03 Robin Thurmond Use of histamine H4 receptor antagonist for the treatment of inflammatory responses
SE0302116D0 (sv) 2003-07-21 2003-07-21 Astrazeneca Ab Novel compounds
EP1505064A1 (en) 2003-08-05 2005-02-09 Bayer HealthCare AG 2-Aminopyrimidine derivatives
RU2006110561A (ru) 2003-09-30 2007-10-10 Янссен Фармацевтика Н.В. (Be) Соединения бензоимидазола
KR20060111466A (ko) 2003-09-30 2006-10-27 얀센 파마슈티카 엔.브이. 퀴녹살린 화합물
WO2005054239A1 (en) 2003-12-05 2005-06-16 Bayer Healthcare Ag 2-aminopyrimidine derivatives
WO2005089748A1 (en) 2004-03-17 2005-09-29 Pfizer Limited Combination for treating inflammatory diseases
AU2005226729B2 (en) 2004-03-25 2010-01-28 Janssen Pharmaceutica N.V. Imidazole compounds
EP1812113A1 (en) 2004-11-11 2007-08-01 Argenta Discovery Limited Pyrimidine compounds as histamine modulators
JP2008520644A (ja) 2004-11-24 2008-06-19 ファイザー・インク オクタヒドロピロロ［３，４−ｃ］ピロール誘導体
CA2622372A1 (en) 2005-09-13 2007-03-22 Palau Pharma, S.A. 2-aminopyrimidine derivatives as modulators of the histamine h4 receptor activity
EP1767537A1 (en) 2005-09-21 2007-03-28 Cellzome (UK) Ltd. Pyrimidine compounds for the treatment of inflammatory disorders
KR101271263B1 (ko) 2005-09-28 2013-06-07 아우리스 메디칼 아게 내이 장애 치료용 약학 조성물
NL2000323C2 (nl) 2005-12-20 2007-11-20 Pfizer Ltd Pyrimidine-derivaten.
EP1829879A1 (en) 2006-02-10 2007-09-05 Cellzome (UK) Ltd. Amino pyrimidine compounds for the treatment of inflammatory disorders
WO2007090854A1 (en) 2006-02-10 2007-08-16 Cellzome (Uk) Ltd. Azetidine amino pyrimidine compounds for the treatment of inflammatory disorders
WO2007090853A1 (en) 2006-02-10 2007-08-16 Cellzome (Uk) Ltd. Enantiomers of amino pyrimidine compounds for the treatment of inflammatory disorders
PL2007752T3 (pl) 2006-03-31 2011-02-28 Janssen Pharmaceutica Nv Benzoimidazol-2-ilopirymidyny i pirazyny jako modulatory receptora histaminowego H4
EP2010172B1 (en) 2006-04-07 2012-08-29 Janssen Pharmaceutica N.V. Indoles and benzoimidazoles as modulators of the histamine h4 receptor
WO2007120690A2 (en) 2006-04-10 2007-10-25 Janssen Pharmaceutica N.V. Combination histamine h1r and h4r antagonist therapy for treating pruritus
AU2007271187A1 (en) 2006-07-03 2008-01-10 Vereniging Voor Christelijk Hoger Onderwijs, Wetenschappelijk Onderzoek En Patientenzorg Fused bicyclic compounds interacting with the histamine H4 receptor
KR20090028819A (ko) 2006-07-11 2009-03-19 얀센 파마슈티카 엔.브이. 히스타민 ｈ４ 수용체의 벤조푸로- 및 벤조티에노피리미딘 조절제
US20100035863A1 (en) 2006-09-12 2010-02-11 Ucb Pharma, S.A. 2 Amino-Pyrimidine Derivatives As H4 Receptor Antagonists, Processes For Preparing Them And Their Use In Pharmaceutical Compositions
US8735411B2 (en) 2006-10-02 2014-05-27 Abbvie Inc. Macrocyclic benzofused pyrimidine derivatives
WO2008074445A1 (en) 2006-12-18 2008-06-26 Ucb Pharma, S.A. Novel tricyclic and heterotricyclic derivatives, processes for preparing them, pharmaceutical compositions thereof
CL2008000467A1 (es) 2007-02-14 2008-08-22 Janssen Pharmaceutica Nv Compuestos derivados de 2-aminopirimidina, moduladores del receptor histamina h4; su procedimiento de preparacion; composicion farmaceutica que comprende a dichos compuestos; y su uso para tratar un trastorno inflamatorio seleccionado de alegia, asma
WO2008122378A1 (en) 2007-04-04 2008-10-16 Ucb Pharma, S.A. Novel pyridine derivatives, processes for preparing them, pharmaceutical compositions thereof
CA2705719C (en) 2007-09-14 2016-10-11 Janssen Pharmaceutica N.V. Thieno-and furo-pyrimidine modulators of the histamine h4 receptor
US20100298289A1 (en) 2007-10-09 2010-11-25 Ucb Pharma, S.A. Heterobicyclic compounds as histamine h4-receptor antagonists
PE20090978A1 (es) 2007-10-30 2009-07-13 Palau Pharma Sa DERIVADOS DE FURO {3,2-d} PIRIMIDINA
WO2009068512A1 (en) 2007-11-30 2009-06-04 Palau Pharma, S. A. 2 -amino-pyrimidine derivatives as histamine h4 antagonists
FR2924344B1 (fr) 2007-12-04 2010-04-16 Pf Medicament Utilisation de la mequitazine sous la forme de racemate ou d'enantiomeres pour la preparation d'un medicament destine au traitement ou a la prevention de pathologies impliquant les recepteurs histaminiques h4.
WO2009079001A1 (en) 2007-12-18 2009-06-25 Janssen Pharmaceutica N.V. Bicyclic heteroaryl-substituted imidazoles as modulators of the histamine h4 receptor
PE20091524A1 (es) 2007-12-19 2009-09-25 Palau Pharma Sa Derivados de 2-aminopirimidina
CN101903385B (zh) * 2007-12-21 2013-11-06 帕劳制药股份有限公司 作为组胺h4受体拮抗剂的4-氨基嘧啶衍生物
WO2009107767A1 (ja) 2008-02-29 2009-09-03 大日本住友製薬株式会社 Ｈ４受容体アンタゴニスト作用を有する新規２環性ピリミジン誘導体
US8278313B2 (en) 2008-03-11 2012-10-02 Abbott Laboratories Macrocyclic spiro pyrimidine derivatives
WO2009115496A1 (en) 2008-03-17 2009-09-24 Palau Pharma, S. A. Furo [3, 2-d] pyrimidine derivatives as h4 receptor antagonists
US8436005B2 (en) 2008-04-03 2013-05-07 Abbott Laboratories Macrocyclic pyrimidine derivatives
US8278311B2 (en) 2008-04-28 2012-10-02 Abbott Laboratories Substituted pyrimidine derivatives
US8546410B2 (en) 2008-05-05 2013-10-01 Abbvie Inc. Heteroaryl-fused macrocyclic pyrimidine derivatives
TW201206936A (en) * 2010-07-19 2012-02-16 Alcon Res Ltd Methods and compositions for the treatment of allergy

Also Published As

Publication number Publication date
KR20110117661A (ko) 2011-10-27
PL2382013T3 (pl) 2017-01-31
JP2012513968A (ja) 2012-06-21
US9526725B2 (en) 2016-12-27
EP2201982A1 (en) 2010-06-30
LT2382013T (lt) 2016-10-25
JP5814126B2 (ja) 2015-11-17
HK1163571A1 (zh) 2012-09-14
EP3130376A1 (en) 2017-02-15
HRP20161290T1 (hr) 2016-11-18
KR101749285B1 (ko) 2017-06-20
EP2382013B1 (en) 2016-07-13
CA2748159C (en) 2017-06-27
ES2597834T3 (es) 2017-01-23
IL213540A (en) 2015-10-29
RU2589846C2 (ru) 2016-07-10
EP2382013A1 (en) 2011-11-02
CA2748159A1 (en) 2010-07-01
CN102325566A (zh) 2012-01-18
US20120039913A1 (en) 2012-02-16
HUE031645T2 (en) 2017-07-28
CY1118106T1 (el) 2017-06-28
CN107050030A (zh) 2017-08-18
US20170056397A1 (en) 2017-03-02
RU2012101595A (ru) 2013-07-27
SI2382013T1 (sl) 2017-02-28
IL213540A0 (en) 2011-07-31
PT2382013T (pt) 2016-10-25
US10195195B2 (en) 2019-02-05
WO2010072829A1 (en) 2010-07-01
SMT201600368B (it) 2016-11-10
JP2016041694A (ja) 2016-03-31

Similar Documents

Publication Publication Date Title
JP6185574B2 (ja) 耳鳴りを治療するためのｈ４受容体阻害剤
EP3875078A1 (en) Compounds for the treatment of covid-19
US7985745B2 (en) Method for pain treatment
JP2017512841A (ja) 肺の非小細胞癌腫及び卵巣癌を処置するためのジアンヒドロガラクチトール及びその類縁体又は誘導体の使用
JP2011500774A5 (da)
WO2008083367A4 (en) Polycyclic heteroaryl substituted triazoles useful as axl inhibitors
JP2015504057A5 (da)
US20240101576A1 (en) Heterocyclic inhibitors of egfr and/or her2, for use in the treatment of cancer
US11446274B2 (en) Use of dianhydrogalactitol or derivatives or analogs thereof for treatment of pediatric central nervous system malignancies
US10195195B2 (en) Selective histamine H4 receptor antagonists for the treatment of vestibular disorders
US20240156825A1 (en) Use of selective vegfr2 and fgfr1 inhibitors
US20250360137A1 (en) Enhancement of the efficacy of serotonergic psychedelic drugs in the treatment or prevention of certain neuropsychiatric disorders through inhibition of type-9 phosphodiesterases
HK1163571B (en) Selective histamine h4 receptor antagonists for the treatment of vestibular disorders
TW201815395A (zh) 二去水半乳糖醇或其衍生物或類似物於治療小兒中樞神經系統惡性病之用途
WO2020183011A1 (en) Htr1d inhibitors and uses thereof in the treatment of cancer
Dash A review on quinazoline heterocycles: A Pharmacophoric Scaffold
WO2025172573A1 (en) Combinations of par2 inhibitors and immune checkpoint inhibitors for the treatment of cancer