HRP20161290T1 - Selektivni antagonisti histaminskih h4 receptora za liječenje vestibularnih poremećaja - Google Patents

Selektivni antagonisti histaminskih h4 receptora za liječenje vestibularnih poremećaja Download PDF

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HRP20161290T1
HRP20161290T1 HRP20161290TT HRP20161290T HRP20161290T1 HR P20161290 T1 HRP20161290 T1 HR P20161290T1 HR P20161290T T HRP20161290T T HR P20161290TT HR P20161290 T HRP20161290 T HR P20161290T HR P20161290 T1 HRP20161290 T1 HR P20161290T1
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pyrimidin
methylamino
diamine
azetidin
amine
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Gilles Desmadryl
Christian Chabbert
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INSERM (Institut National de la Santé et de la Recherche Médicale)
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Claims (6)

1. Selektivni antagonist histaminskih H4 receptora za uporabu u liječenju i /ili prevenciji najmanje jednog od simptoma vestibularnih poremećaja, naznačen time što selektivni antagonist histaminskih H4 receptora: - ima KiH3:KiH4 odnos iznad 10:1, i - izabran je iz grupe koja se sastoji od: • -1- [(5-kloro-1H-benzimidazol-2-il)karbonil]-4-metilpiperazin, • 1-[(5-kloro-1H-indol-2-il) karbonil]-4-metilpiperazin, • 4-((3R)-3-Aminopirolidin-1-il)-6,7-dihidro-5H-benzo[6,7]ciklohepta[1,2-d]pirimidin-2-ilamin, • cis-4-(Piperazin-1-il)-5,6,7a,8,9,10,11,11a-oktahidrobenzofuro[2,3-h] kinazolin-2-amin, • 2-Izobutil-6-(3-(metilamino)-azetidin-1-il)pirimidin-4-amin, • 2-Izobutil-6-((3R)-3-(metilamino)pirolidin-1-il)pirimidin-4-amin, • 2-Cikloheksilmetil-6-((3R)-3-(metilamino)pirolidin-1-il)pirimidin-4-amin, • 2-(4-Fluorobenzil)-6-(3-(metilamino)azetidin-1-il)pirimidin-4-amin, • 2-Ciklopropil-6-(3-(metilamino)azetidin-1-il)pirimidin-4-amin, • 2-terc-Butil-6-(3-(metilamino)azetidin-1-il)pirimidin-4-amin, • 2-Izopropil-6-(3-(metilamino)azetidin-1-il)pirimidin-4-amin, • 2-(Ciklopropilmetil)-6-(3-(metilamino)azetidin-1-il)pirimidin-4-amin, • 6-(3-(Metilamino)azetidin-1-il)-2-(fenoksimetil)pirimidin-4-amin, • 2-Ciklopropil-6-((3R)-3-(metilamino)pirolidin-1-il)pirimidin-4-amin, • 2-terc-Butil-6-((3R)-3-(metilamino)pirolidin-1-il)pirimidin-4-amin, • 2-Izopropil-6-((3R)-3-(metilamino)pirolidin-1-il)pirimidin-4-amin, • 6-((3R)-3-(Metilamino)pirolidin-1-il)-2-(fenoksimetil)pirimidin-4-amin • 6-(3-Aminoazetidin-1-il)-2-izobutilpirimidin-4-amin • 2-Izobutil-6-(3-metil-3-(metilamino)azetidin-1-il)pirimidin-4-amin, • 6-((3R)-3-aminopirolidin-1-il)-2-izobutilpirimidin-4-amin, • 2-Ciklobutil-6-(3-(metilamino)azetidin-1-il)pirimidin-4-amin, • 2-Ciklobutil-6-((3R)-3-(metilamino)pirolidin-1-il)pirimidin-4-amin, • 2-Ciklopentil-6-(3-(metilamino)azetidin-1-il)pirimidin-4-amin, • 2-Ciklopentil-6-((3R)-3-(metilamino)pirolidin-1-il)pirimidin-4-amin, • 2-(2,2-Dimetilpropil)-6-(3-(metilamino)azetidin-1-il)pirimidin-4-amin, • 2-(2,2-Dimetilpropil)-6-((3R)-3-(metilamino)pirolidin-1-il)pirimidin-4-amin, • 2-(2-Ciklopentiletil)-6-((3R)-3-(metilamino)pirolidin-1-il)pirimidin-4-amin, • 2-Cikloheksilmetil-6-(3-(metilamino)azetidin-1-il)pirimidin-4-amin, • 2-Ciklopropilmetil-6-((3R)-3-(metilamino)pirolidin-1-il)pirimidin-4-amin, • 2-Cikloheksil-6-(3-(metilamino)azetidin-1-il)pirimidin-4-amin, • 2-Cikloheksil-6-((3R)-3-(metilamino)pirolidin-1-il)pirimidin-4-amin, • 2-(4-Fluorobenzil)-6-((3R)-3-(metilamino)pirolidin-1-il)pirimidin-4-amin, • N4-(Ciklopropilmetil)-6-[(3R)-3-(metilamino)pirolidin-1-il]pirimidin-2,4-diamin, • N4-(Ciklopropilmetil)-6-[(3R)-3-(metilamino)pirolidin-1-il]pirimidin-2,4-diamin tartarat, • N4-Izobutil-6-[(3R)-3-(metilamino)pirolidin-1-il]pirimidin-2,4-diamin, • N4-(2,2-Dimetilpropil)-6-[(3R)-3-(metilamino)pirolidin-1-il]pirimidin-2,4-diamin, • N-Izobutil-6-[(3R)-3-(metilamino)pirolidin-1-il]pirimidin-4-amin, • N-(Ciklopropilmetil)-6-[(3R)-3-(metilamino)pirolidin-1-il]pirimidin-4-amin, • N4-(2,2-Dimetilpropil)-6-[(4aR*,7aR*)-oktahidro-6H-pirolo[3,4-b]piridin-6-il]pirimidin-2,4-diamin, • N4-Ciklopropil-6-[(4aR*,7aR*)-oktahidro-6H-pirolo[3,4-b]piridin-6-il]pirimidin-2,4-diamin, • N4-Ciklobutil-6-[(4aR*,7aR*)-oktahidro-6H-pirolo[3,4-b]piridin-6-il]pirimidin-2,4-diamin, • N4-(2,2-Dimetilpropil)-6-[3-(metilamino)azetidin-1-il]pirimidin-2,4-diamin, • 6-(3-Metilamino-azetidin-1-il)-N4-(3,3,3-trifluoro-propil)-pirimidin-2,4-diamin, • N4-Ciklopropilmetil-6-(3-metilamino-azetidin-1-il)pirimidin-2,4-diamin, • N4-(3,3-Dimetil-butil)-6-(3-metilamino-azetidin-1-il)pirimidin-2,4-diamin, • N4-(3-Fluoro-benzil)-6-(3-metilamino-azetidin-1-il)pirimidin-2,4-diamin, • N4-Ciklopentilmetil-6-(3-metilamino-azetidin-1-il)pirimidin-2,4-diamin, • N4-Izobutil-6-[3-(metilamino)azetidin-1-il]pirimidin-2,4-diamin, • 6-[3-(Metilamino)azetidin-1-il]-N4-propil-pirimidin-2,4-diamin, • N4-(2-Metoksibenzil)-6-[3-(metilamino)azetidin-1-il]pirimidin-2,4-diamin, • N4-(2,2-Dimetilpropil)-6-[(3R)-3-metilpiperazin-1-il]pirimidin-2,4-diamin, • N4-Etil-6-(4-metilpiperazin-1-il)pirimidin-2,4-diamin, • N4-(Ciklopropilmetil)-6-(4-metilpiperazin-1-il)pirimidin-2,4-diamin, • 6-[3-(Metilamino)azetidin-1-il]-N4-(2-metilbutil)pirimidin-2,4-diamin, • N4-(2,5-Difluorobenzil)-6-[3-(metilamino)azetidin-1-il]pirimidin-2,4-diamin, • N4-(2,3-Difluorobenzil)-6-[3-(metilamino)azetidin-1-il]pirimidin-2,4-diamin, • N4-Butil-6-[3-(metilamino)azetidin-1-il]pirimidin-2,4-diamin, • 6-[(3R)-3-(Metilamino)pirolidin-1-il]-N4-(2-metilciklopropil)pirimidin-2,4-diamin, • N4-Izobutil-6-(4-metil-1,4-diazepam-1-il)pirimidin-2,4-diamin, • N4-(Ciklopropilmetil)-6-(3-pirolidin-1-il-azetidin-1-il)pirimidin-2,4-diamin, • N4-Biciklo[1.1.1]pent-1-il-6-[(3R)-3-(metilamino)pirolidin-1-il]pirimidin-2,4-diamin, • 6-[3-Metil-3-(metilamino)azetidin-1-il]-N4-propilpirimidin-2,4-diamin, • N4-(2,2-Dimetilpropil)-6-(heksahidropirolo[1,2-a]pirazin-2(1H)-1-il)pirimidin-2,4-diamin, • N4-(2,2-Dimetilpropil)-6-(3-pirolidin-1-il-azetidin-1-il)pirimidin-2,4-diamin, • N4-(2,2-Dimetilpropil)-6-[3-(izopropilamino)azetidin-1-il]pirimidin-2,4-diamin, • N4-(terc-Butil)-6-[(3R)-3-(metilamino)pirolidin-1-il]pirimidin-2,4-diamin, • 6-[(3R)-3-(Metilamino)pirolidin-1-il]-N4-(1-metilciklopropil)pirimidin-2,4-diamin, • N4-(terc-Butil)-6-[(4aS*,7aS*)-oktahidro-6H-pirolo[3,4-b]piridin-6-il]pirimidin-2,4-diamin, • N4-(2,2-Dimetilpropil)-6-piperazin-1-ilpirimidin-2,4-diamin, • N4-(2,2-Dimetilpropil)-6-[3-(metilamino)azetidin-1-il]pirimidin-2,4-diamin hidroklorid, • N4-(2,2-Dimetilpropil)-6-[(3aR*,7aS*)-oktahidro-5H-pirolo[3,2-c]piridin-5-il]pirimidin-2,4-diamin, • 6-Piperazin-1-il-N4-propilpirimidin-2,4-diamin, • N4-(Ciklopropilmetil)-6-[4aR,7aR]-oktahidro-6H-pirolo[3,4-b]piridin-6-il]pirimidin-2,4-diamin, • N4-(2,2-Dimetilpropil)-6-[(4aS,7aS)-oktahidro-6H-pirolo[3,4-b]piridin-6-il]pirimidin-2,4-diamin, • N4-(Ciklopropilmetil)-6-[(3R)-3-(metilamino)pirolidin-1-il]pirimidin-2,4-diamin, • N4-izopropil-6-[(4aS,7aS)-oktahidro-6H-pirolo[3,4-b]piridin-6-il]pirimidin-2,4-diamin, • 4-[3-(Metilamino)azetidin-1-il]-6-(4-metilpiperidin-1-il)pirimidin-2-amin, • N4-(Ciklopentilmetil)-6-[(3R)-3-(metilamino)pirolidin-1-il]pirimidin-2,4-diamin, • N4-Ciklobutil-6-[(4aS,7aS)-oktahidro-6H-pirolo[3,4-b]piridin-6-il]pirimidin-2,4-diamin, • 6-[(3R)-3-(Metilamino)pirolidin-1-il]-N4-propilpirimidin-2,4-diamin i • N4-Etil-6-(4-metil-1,4-diazepan-1-il)pirimidin-2,4-diamin.
2. Selektivni antagonist histaminskih H4 receptora za uporabu prema patentnom zahtjevu 1, pri čemu je najmanje jedan od spomenutih simptoma vestibularnih poremećaja izabran iz grupe koju čine vertigo, vrtoglavice, poremećaj ravnoteže i mučnina.
3. Selektivni antagonist histaminskih H4 receptora za uporabu prema patentnom zahtjevu 1 ili 2, gdje je vrtoglavica benigna paroksizmalna vrtoglavica ili obiteljska epizodična vrtoglavica.
4. Selektivni antagonist histaminskih H4 receptora za uporabu prema bilo kojem od patentnih zahtjeva 1 do 3, pri čemu je spomenuti vestibularni poremećaj izabran od vestibularnog neuritisa, nastupa Meniereove bolesti, endolimfatičnog hidropsa, perilimfatične fistule, povreda glave s vestibularnim poremećajima, krvarenja labirinta, kronične ili akutne labirintne infekcije, seroznog labirinta, barotraumatizma s vestibularnim poremećajima, vestibularnih sindroma nakon autoimune bolesti unutrašnjeg uha, vestibularne migrene, vestibularnih sindroma nakon kirurškog tretmana srednjeg uha, endolimfatične vrećice ili tumora pontocerebelarnog kuta, kanalopatija unutrašnjeg uha, kronične Menierove bolesti, vestibularnih švanoma, presbivestibulia i vestibularne ataksije.
5. Selektivni antagonist histaminskih H4 receptora za uporabu prema bilo kojem od patentnih zahtjeva 1 do 4, za primjenu preko bubnjića ili za sistemsku primjenu.
6. Farmaceutska kompozicija koja sadrži selektivni antagonist histaminskih H4 receptora prema bilo kojem od patentnih zahtjeva 1 do 5, za uporabu u liječenju i/ili prevenciji najmanje jednog od simptoma vestibularnih poremećaja.
HRP20161290TT 2008-12-24 2016-10-06 Selektivni antagonisti histaminskih h4 receptora za liječenje vestibularnih poremećaja HRP20161290T1 (hr)

Applications Claiming Priority (3)

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.
EP09798938.8A EP2382013B1 (en) 2008-12-24 2009-12-23 Selective histamine h4 receptor antagonists for the treatment of vestibular disorders.

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US (2) US9526725B2 (hr)
EP (3) EP2201982A1 (hr)
JP (2) JP5814126B2 (hr)
KR (1) KR101749285B1 (hr)
CN (2) CN102325566A (hr)
CA (1) CA2748159C (hr)
CY (1) CY1118106T1 (hr)
DK (1) DK2382013T3 (hr)
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PL (1) PL2382013T3 (hr)
PT (1) PT2382013T (hr)
RU (1) RU2589846C2 (hr)
SI (1) SI2382013T1 (hr)
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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
ES2946551T3 (es) 2017-10-17 2023-07-20 Palau Pharma S L U Síntesis de compuestos de 4-aminopirimidina

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
NZ527200A (en) * 1997-03-26 2004-12-24 Sepracor Inc Stable norastemizole formulations including a super disintegrant
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
JP4544820B2 (ja) 2001-03-09 2010-09-15 オーソ−マクニール・フアーマシユーチカル・インコーポレーテツド 複素環化合物
US20040127395A1 (en) 2002-09-06 2004-07-01 Desai Pragnya J. Use of histamine H4 receptor modulators for the treatment of allergy and asthma
MXPA05002577A (es) * 2002-09-06 2005-09-20 Johnson & Johnson Uso de moduladores del receptor h4 de histamina para el tratamiento de alergia y asma.
CA2497827A1 (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
CA2497829A1 (en) 2002-09-06 2004-03-18 Janssen Pharmaceutica, N.V. Method to treat allergic rhinitis
US7226938B2 (en) 2002-09-06 2007-06-05 Janssen Pharmaceutica, N.V. Heterocyclic compounds
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
MXPA06003578A (es) 2003-09-30 2006-08-31 Johnson & Johnson Compuestos de quinoxalina.
CN1886380B (zh) 2003-09-30 2010-12-22 詹森药业有限公司 苯并咪唑化合物
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
JP5162236B2 (ja) 2004-03-25 2013-03-13 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ イミダゾール化合物
EP1812113A1 (en) 2004-11-11 2007-08-01 Argenta Discovery Limited Pyrimidine compounds as histamine modulators
CA2587141A1 (en) 2004-11-24 2006-06-01 Pfizer Inc. Octahydropyrrolo[3,4-c]pyrrole derivatives
BRPI0615880A2 (pt) 2005-09-13 2011-05-31 Palau Pharma Sa compostos derivados de 2-aminopirimidina como moduladores da atividade de receptor da histamina h4, uso dos mesmos e composição farmacêutica
EP1767537A1 (en) 2005-09-21 2007-03-28 Cellzome (UK) Ltd. Pyrimidine compounds for the treatment of inflammatory disorders
US20090246255A1 (en) 2005-09-28 2009-10-01 Thomas Meyer Pharmaceutical Compositions for the Treatment of Inner Ear Disorders
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
WO2007090853A1 (en) 2006-02-10 2007-08-16 Cellzome (Uk) Ltd. Enantiomers of 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
PT2007752E (pt) 2006-03-31 2010-10-18 Janssen Pharmaceutica Nv Benzoimidazol-2-il pirimidinas e pirazinas como moduladores do receptor de histamina h4
EP2010172B1 (en) 2006-04-07 2012-08-29 Janssen Pharmaceutica N.V. Indoles and benzoimidazoles as modulators of the histamine h4 receptor
US20090069343A1 (en) * 2006-04-10 2009-03-12 Dunford Paul J Combination Histamine H1R and H4R Antagonist Therapy for Treating Pruritus
US20100016293A1 (en) 2006-07-03 2010-01-21 Rogier Adriaan Smits Quinazolines and Related Heterocyclic Compounds, and Their Therapeutic Use
AU2007272956B2 (en) 2006-07-11 2013-05-02 Janssen Pharmaceutica, N.V. Benzofuro-and benzothienopyryimidine modulators of the histamine H4 receptor
EP2066645A2 (en) 2006-09-12 2009-06-10 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
TW200904437A (en) 2007-02-14 2009-02-01 Janssen Pharmaceutica Nv 2-aminopyrimidine modulators of the histamine H4 receptor
US20100168077A1 (en) 2007-04-04 2010-07-01 Ucb Pharma, S.A. Novel Pyridine Derivatives, Processes for Preparing Them, Pharmaceutical Compositions Thereof
KR101470933B1 (ko) 2007-09-14 2014-12-09 얀센 파마슈티카 엔.브이. 히스타민 ｈ4 수용체의 티에노- 및 푸로-피리미딘 조절제
EP2209775A1 (en) 2007-10-09 2010-07-28 UCB Pharma, S.A. Heterobicyclic compounds as histamine h4-receptor antagonists
WO2009056551A1 (en) 2007-10-30 2009-05-07 Palau Pharma, S. A. Furo[3,2-d]pyrimidine derivatives
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.
US8084466B2 (en) 2007-12-18 2011-12-27 Janssen Pharmaceutica Nv Bicyclic heteroaryl-substituted imidazoles as modulators of the histamine H4 receptor
TW200940529A (en) 2007-12-19 2009-10-01 Palau Pharma Sa 2-amino-pyrimidine derivatives
WO2009080721A2 (en) * 2007-12-21 2009-07-02 Palau Pharma, S. A. 4 -aminopyrimidine derivatives as histamine h4 receptor antagonists
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
PE20091958A1 (es) 2008-03-17 2010-01-15 Palau Pharma Sa DERIVADOS DE FURO[3,2-d] PIRIMIDINA
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
WO2009137492A1 (en) 2008-05-05 2009-11-12 Abbott Laboratories Heteroaryl-fused macrocyclic pyrimidine derivatives
TW201206936A (en) * 2010-07-19 2012-02-16 Alcon Res Ltd Methods and compositions for the treatment of allergy

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