AR068513A1 - Moduladores tieno- y furo- pirimidina del receptor de histamina h4 - Google Patents

Moduladores tieno- y furo- pirimidina del receptor de histamina h4

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Publication number
AR068513A1
AR068513A1 ARP080104005A ARP080104005A AR068513A1 AR 068513 A1 AR068513 A1 AR 068513A1 AR P080104005 A ARP080104005 A AR P080104005A AR P080104005 A ARP080104005 A AR P080104005A AR 068513 A1 AR068513 A1 AR 068513A1
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AR
Argentina
Prior art keywords
compounds
formula
receptor
methyl
furo
Prior art date
Application number
ARP080104005A
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English (en)
Original Assignee
Janssen Pharmaceutica Nv
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 Nv filed Critical Janssen Pharmaceutica Nv
Publication of AR068513A1 publication Critical patent/AR068513A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P11/00—Drugs for disorders of the respiratory system
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • 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
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/04—Antipruritics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • 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
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/04—Artificial tears; Irrigation solutions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • 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]
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    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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    • A61P37/08—Antiallergic agents
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • A61P5/16—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4 for decreasing, blocking or antagonising the activity of the thyroid hormones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • 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
    • 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
    • A61P9/10—Drugs 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic 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

Abstract

Se describen compuestos de tieno- y furo-pirimidina, como moduladores del receptor de H4. Dichos compuestos pueden usarse en composiciones farmacéuticas y métodos para modular la actividad del receptor de histamina H4 y para tratar estados patologicos, trastornos y afecciones mediadas por la actividad del receptor de H4, tales como la inflamacion. Reivindicacion 1: Una entidad química seleccionada del grupo que consiste en compuestos de Formula (1), sales farmacéuticamente aceptables de compuestos de Formula (1), prodrogas farmacéuticamente aceptables de compuestos de Formula (1), y metabolitos farmacéuticamente activos de compuestos de Formula (1); en donde X es O o S; R1 es H, metilo o bromo; R2 es H o alquiloC1-4; o R1 y R2 tornados juntos forman -(CH2)4-5-, opcionalmente sustituido con uno o dos sustituyentes independientemente seleccionados de alquiloC1-4, alcoxiC1-4 , CF3 y fluoro; -N(R3)R4 es una de los siguientes restos, en donde R3 y se toman juntos o por separado, segun se define por cada uno de dichos restos de formulas (2); donde q es 0 o 1; p es 0 o 1; r es 0 o 1; Ra es H o OH; Rb y Rc son cada uno independientemente H o alquiloC1-3; Rd es H o un grupo alquiloC1-3 no sustituido o sustituido con OH o NH2; Re y Rf son cada uno metilo, o Re y Rf tomados juntos forman un puente metileno o etileno; y R5 es H o NH2; con la condicion de que, cuando R1 es H y R2 es H, metilo o ter-butilo, entonces -N(R3)R4 no es 3-aminopirrolidina, 3-aminopiperidina, piperazina ni N-metilpiperazina.
ARP080104005A 2007-09-14 2008-09-15 Moduladores tieno- y furo- pirimidina del receptor de histamina h4 AR068513A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US97258907P 2007-09-14 2007-09-14

Publications (1)

Publication Number Publication Date
AR068513A1 true AR068513A1 (es) 2009-11-18

Family

ID=40455164

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP080104005A AR068513A1 (es) 2007-09-14 2008-09-15 Moduladores tieno- y furo- pirimidina del receptor de histamina h4

Country Status (18)

Country Link
US (5) US8193178B2 (es)
EP (1) EP2200595B1 (es)
JP (1) JP5439377B2 (es)
KR (1) KR101470933B1 (es)
CN (1) CN101998958B (es)
AR (1) AR068513A1 (es)
AU (1) AU2008301897B2 (es)
BR (1) BRPI0816922A2 (es)
CA (1) CA2705719C (es)
CL (1) CL2008002747A1 (es)
HK (1) HK1143325A1 (es)
MX (1) MX2010002926A (es)
NZ (1) NZ583509A (es)
PA (1) PA8796001A1 (es)
PE (1) PE20091083A1 (es)
TW (1) TW200924781A (es)
UY (1) UY31340A1 (es)
WO (1) WO2009038673A2 (es)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR101470933B1 (ko) 2007-09-14 2014-12-09 얀센 파마슈티카 엔.브이. 히스타민 ｈ4 수용체의 티에노- 및 푸로-피리미딘 조절제
WO2010075270A1 (en) 2008-12-22 2010-07-01 Incyte Corporation 4, 6-disubstituted 2-amino-pyrimidines as histamine h4 receptor modulators
EP2201982A1 (en) 2008-12-24 2010-06-30 INSERM (Institut National de la Santé et de la Recherche Médicale) Histamine H4 receptor antagonists for the treatment of vestibular disorders
WO2010108059A1 (en) * 2009-03-20 2010-09-23 Incyte Corporation Substituted pyrimidine derivatives as antagonists of the histamine h4 receptor
BR112013007566A2 (pt) 2010-09-28 2016-08-02 Panacea Biotec Ltd novos compostos bicíclicos
JP2013542243A (ja) 2010-11-15 2013-11-21 カトリーケ ウニヴェルシテイト ルーヴェン 新規な抗ウイルス性化合物
AR090037A1 (es) * 2011-11-15 2014-10-15 Xention Ltd Derivados de tieno y/o furo-pirimidinas y piridinas inhibidores de los canales de potasio
EP2858647B1 (en) 2012-06-08 2018-05-23 Sensorion H4 receptor inhibitors for treating tinnitus
US10227357B2 (en) 2012-09-06 2019-03-12 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
WO2014079545A1 (en) 2012-11-20 2014-05-30 Ktb Tumorforschungsgesellschaft Mbh Thioether derivatives as protein kinase inhibitors
GB201410816D0 (en) * 2014-06-17 2014-07-30 Ucb Biopharma Sprl And Katholieke Universiteit Leuven Therapeutic agents

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BE759371A (fr) * 1969-11-24 1971-05-24 Bristol Myers Co Azaspirodecanediones heterocycliques et procedes pour leur preparation
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EP1437348A1 (fr) 2003-01-13 2004-07-14 L'oreal Dérivés de de la 6-méthyl-pyrimidine-2,4-diamine, procédé de synthèse, compositions les comprenant et utilisations comme agents neutralisants basiques
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Also Published As

Publication number Publication date
KR20100085913A (ko) 2010-07-29
CN101998958A (zh) 2011-03-30
JP5439377B2 (ja) 2014-03-12
CL2008002747A1 (es) 2009-01-16
US8440654B2 (en) 2013-05-14
EP2200595A4 (en) 2011-06-01
AU2008301897A1 (en) 2009-03-26
BRPI0816922A2 (pt) 2015-03-17
JP2010539169A (ja) 2010-12-16
US8937075B2 (en) 2015-01-20
US8927555B2 (en) 2015-01-06
US20120214792A1 (en) 2012-08-23
NZ583509A (en) 2012-01-12
EP2200595A2 (en) 2010-06-30
US20120208793A1 (en) 2012-08-16
WO2009038673A2 (en) 2009-03-26
WO2009038673A3 (en) 2009-08-20
CN101998958B (zh) 2014-03-12
UY31340A1 (es) 2009-03-31
CA2705719C (en) 2016-10-11
US20120238544A1 (en) 2012-09-20
EP2200595B1 (en) 2013-11-20
MX2010002926A (es) 2010-03-31
TW200924781A (en) 2009-06-16
US8193178B2 (en) 2012-06-05
US20090075970A1 (en) 2009-03-19
US8445482B2 (en) 2013-05-21
PA8796001A1 (es) 2009-04-23
HK1143325A1 (en) 2010-12-31
CA2705719A1 (en) 2009-03-26
US20120270855A1 (en) 2012-10-25
PE20091083A1 (es) 2009-07-23
AU2008301897B2 (en) 2013-08-01
KR101470933B1 (ko) 2014-12-09

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