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PE20070790A1 - Derivados de 2-aminopirimidina como moduladores de la actividad del receptor de histamina h-4 - Google Patents

Derivados de 2-aminopirimidina como moduladores de la actividad del receptor de histamina h-4

Info

Publication number
PE20070790A1
PE20070790A1 PE2006001110A PE2006001110A PE20070790A1 PE 20070790 A1 PE20070790 A1 PE 20070790A1 PE 2006001110 A PE2006001110 A PE 2006001110A PE 2006001110 A PE2006001110 A PE 2006001110A PE 20070790 A1 PE20070790 A1 PE 20070790A1
Authority
PE
Peru
Prior art keywords
alkyl
histamine
amino
modulators
receptor activity
Prior art date
Application number
PE2006001110A
Other languages
English (en)
Inventor
Gonzalez Elena Carceller
Solana Jorge Salas
Soliva Robert Soliva
Fuentes Eva Maria Medina
Via Josep Marti
Original Assignee
Palau Pharma Sa
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 Palau Pharma Sa filed Critical Palau Pharma Sa
Publication of PE20070790A1 publication Critical patent/PE20070790A1/es

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • 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
    • 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
    • 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
    • A61P17/06—Antipsoriatics
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • 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
    • A61P37/08—Antiallergic agents
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/50—Three nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Otolaryngology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

SE REFIERE A COMPUESTOS DE 2-AMINOPIRIMIDINA DE FORMULA(I), EN DONDE R1 ES SELECCIONADO DE a), b), Y c); R2 ES H O ALQUILO(C1-C4); R3 ES FENILO OPCIONALMENTE FUSIONADO A UN ANILLO DE 5 O 6 MIEMBROS PUDIENDO SER CARBOCICLICO O HETEROCICLO TAL COMO NAFTILO, OPCIONALMENTE SUSTITUIDOS POR R8; R4, R5, R6 Y R7 SON INDEPENDIENTEMENTE H O ALQUILO(C1-C4); R8 ES ALQUILO(C1-C47), HALOGENO, HALOALCOXI(C1-C4), -CN O ALQUINILO(C2-C4); m ES 1,2 O 3; n ES 0 O 1; Y p ES 1 O 2. SON PREFERIDOS: 2-AMINO-4-CLORO-6-(4-METILPIPERAZIN-1-IL)PIRIMIDINA, [(3R)-1-(2-AMINO-6-CLOROPIRIMIDIN-4-IL)PIRROLIDIN-3-IL]CARBAMATO DE TERC-BUTILO, 2-AMINO-4-(4-CLOROFENILAMINO)-6-(4-METIL-[1,4]DIAZEPAN-1-IL)PIRIMIDINA, ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCEDIMEINTO DE PREPARACION Y UNA COMPOSICION FARMACEUTICA. ESTOS COMPUESTOS PRESENTAN ACTIVIDAD MODULADORA DEL RECEPTOR DE HISTAMINA H-4, POR LO QUE SON UTILES EN EL TRATAMIENTO DE UNA ENFERMEDAD INMUNOLOGICA O INFLAMATORIA
PE2006001110A 2005-09-13 2006-09-13 Derivados de 2-aminopirimidina como moduladores de la actividad del receptor de histamina h-4 PE20070790A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP05380195 2005-09-13
EP06381027 2006-06-09

Publications (1)

Publication Number Publication Date
PE20070790A1 true PE20070790A1 (es) 2007-08-24

Family

ID=37596549

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2006001110A PE20070790A1 (es) 2005-09-13 2006-09-13 Derivados de 2-aminopirimidina como moduladores de la actividad del receptor de histamina h-4

Country Status (14)

Country Link
US (1) US20090306038A1 (es)
EP (1) EP1928862A1 (es)
JP (1) JP2009507896A (es)
KR (1) KR20080043840A (es)
AR (1) AR056511A1 (es)
AU (1) AU2006290715A1 (es)
BR (1) BRPI0615880A2 (es)
CA (1) CA2622372A1 (es)
IL (1) IL189947A0 (es)
NO (1) NO20081003L (es)
PE (1) PE20070790A1 (es)
RU (1) RU2008114378A (es)
TW (1) TW200800956A (es)
WO (1) WO2007031529A1 (es)

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NL2000323C2 (nl) * 2005-12-20 2007-11-20 Pfizer Ltd Pyrimidine-derivaten.
ES2348829T3 (es) 2006-03-31 2010-12-15 Janssen Pharmaceutica Nv Benzimidazol-2-il-pirimidinas y pirazinas moduladoras del receptor h4 de histamina.
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
JP4827986B2 (ja) 2007-06-08 2011-11-30 マンカインド コーポレ−ション ＩＲＥ−１αインヒビター
US8022209B2 (en) 2007-09-12 2011-09-20 Janssen Pharmaceutica Nv Substituted nitrogen-containing heteroaryl derivatives useful as modulators of the histamine H4 receptor
PE20091035A1 (es) * 2007-11-30 2009-07-16 Palau Pharma Sa Derivados de 2-aminopirimidina
PE20091524A1 (es) * 2007-12-19 2009-09-25 Palau Pharma Sa Derivados de 2-aminopirimidina
CA2709650C (en) * 2007-12-21 2016-06-07 Palau Pharma, S.A. 4-aminopyrimidine derivatives as histamine h4 receptor antagonists
EP2077263A1 (en) 2008-01-02 2009-07-08 Vereniging voor christelijk hoger onderwijs, wetenschappelijk onderzoek en patiëntenzorg Quinazolines and related heterocyclic compounds and their therapeutic use
JP5658661B2 (ja) * 2008-06-12 2015-01-28 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Ｊａｎｓｓｅｎ Ｐｈａｒｍａｃｅｕｔｉｃａ Ｎａａｍｌｏｚｅ Ｖｅｎｎｏｏｔｓｃｈａｐ 手術後癒着の治療のためのヒスタミンｈ４拮抗物質の使用
CN102118969B (zh) 2008-06-12 2017-03-08 詹森药业有限公司 组胺h4受体的二氨基吡啶、二氨基嘧啶和二氨基哒嗪调节剂
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
US8349852B2 (en) 2009-01-13 2013-01-08 Novartis Ag Quinazolinone derivatives useful as vanilloid antagonists
KR101740085B1 (ko) 2009-12-23 2017-05-25 메디시스 파마수티컬 코포레인션 히스타민 ｈ４ 수용체 길항제로서의 아미노알킬피리미딘 유도체
AR080056A1 (es) 2010-02-01 2012-03-07 Novartis Ag Derivados de ciclohexil-amida como antagonistas de los receptores de crf
AR080055A1 (es) 2010-02-01 2012-03-07 Novartis Ag Derivados de pirazolo-[5,1-b]-oxazol como antagonistas de los receptores de crf -1
US8835444B2 (en) 2010-02-02 2014-09-16 Novartis Ag Cyclohexyl amide derivatives as CRF receptor antagonists
JP6185574B2 (ja) 2012-06-08 2017-08-23 センソリオン 耳鳴りを治療するためのｈ４受容体阻害剤
EA201591648A1 (ru) 2013-03-06 2016-02-29 Янссен Фармацевтика Нв Бензимидазол-2-ил-пиримидиновые модуляторы рецептора гистамина h4
JP6507157B2 (ja) * 2013-10-07 2019-04-24 カドモン コーポレイション，リミティド ライアビリティ カンパニー Ｒｈｏキナーゼ阻害剤
JP6535007B2 (ja) * 2013-12-20 2019-06-26 インスティテュート オブ ファーマコロジー アンド トキシコロジー アカデミー オブ ミリタリー メディカル サイエンシズ ピー．エル．エー．チャイナ 新規ピペリジンカルボキサミド化合物、その調製方法及び使用
JO3517B1 (ar) 2014-01-17 2020-07-05 Novartis Ag ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2
US10093646B2 (en) 2014-01-17 2018-10-09 Novartis Ag 1-pyridazin-/triazin-3-yl-piper(-azine)/idine/pyrolidine derivatives and compositions thereof for inhibiting the activity of SHP2
JP6473457B2 (ja) 2014-01-17 2019-02-20 ノバルティス アーゲー Ｓｈｐ２の活性を阻害するための１−（トリアジン−３−イル／ピリダジン−３−イル）−ピペリジン／ピペラジン誘導体およびその組成物
US10975080B2 (en) 2015-06-19 2021-04-13 Novartis Ag Compounds and compositions for inhibiting the activity of SHP2
EP3310774B1 (en) 2015-06-19 2020-04-29 Novartis AG Compounds and compositions for inhibiting the activity of shp2
JP6878316B2 (ja) 2015-06-19 2021-05-26 ノバルティス アーゲー Ｓｈｐ２の活性を阻害するための化合物および組成物
RU2744988C2 (ru) 2016-06-14 2021-03-17 Новартис Аг Соединения и композиции для подавления активности shp2
AU2017388466B2 (en) 2016-12-29 2022-04-28 Minoryx Therapeutics S.L. Heteroaryl compounds and their use
EP3568204B1 (en) 2017-01-10 2023-08-30 Novartis AG Pharmaceutical combination comprising an alk inhibitor and an shp2 inhibitor
US10172856B2 (en) 2017-04-06 2019-01-08 Janssen Pharmaceutica Nv 2,4-diaminopyrimidine derivatives as histamine H4 modulators

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CA2394727A1 (en) * 1999-12-28 2001-07-05 Pharmacopeia, Inc. Pyrimidine and triazine kinase inhibitors
EP1505064A1 (en) * 2003-08-05 2005-02-09 Bayer HealthCare AG 2-Aminopyrimidine derivatives
US20070021435A1 (en) * 2005-06-10 2007-01-25 Gaul Michael D Aminopyrimidines as kinase modulators
US20060281764A1 (en) * 2005-06-10 2006-12-14 Gaul Michael D Aminopyrimidines as kinase modulators
NL2000323C2 (nl) * 2005-12-20 2007-11-20 Pfizer Ltd Pyrimidine-derivaten.

Also Published As

Publication number Publication date
JP2009507896A (ja) 2009-02-26
US20090306038A1 (en) 2009-12-10
IL189947A0 (en) 2008-08-07
NO20081003L (no) 2008-04-11
EP1928862A1 (en) 2008-06-11
AU2006290715A1 (en) 2007-03-22
AR056511A1 (es) 2007-10-10
BRPI0615880A2 (pt) 2011-05-31
WO2007031529A1 (en) 2007-03-22
TW200800956A (en) 2008-01-01
RU2008114378A (ru) 2009-10-20
KR20080043840A (ko) 2008-05-19
CA2622372A1 (en) 2007-03-22

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