RU2573828C2 - Производные аминоалкилпиримидина в качестве антагонистов h4 рецептора гистамина - Google Patents

Производные аминоалкилпиримидина в качестве антагонистов h4 рецептора гистамина Download PDF

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RU2573828C2
RU2573828C2 RU2012131223/04A RU2012131223A RU2573828C2 RU 2573828 C2 RU2573828 C2 RU 2573828C2 RU 2012131223/04 A RU2012131223/04 A RU 2012131223/04A RU 2012131223 A RU2012131223 A RU 2012131223A RU 2573828 C2 RU2573828 C2 RU 2573828C2
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alkyl
methyl
formula
cycloalkyl
group
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RU2012131223/04A
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RU2012131223A (ru
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ГОНСАЛЕС Элена КАРСЕЛЬЕР
БЕРНАДО Марина ВИРХИЛИ
СОЛИВА Роберт СОЛИВА
КОСТА Карлес ФЕРРЕР
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Медисиз Фармасьютикал Корпорейшн
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    • 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
    • C07D239/48—Two 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
    • C07D403/04—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
    • 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
    • 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
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    • A61P11/06—Antiasthmatics
    • 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
    • A61P11/16—Central respiratory analeptics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
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    • A61P27/02—Ophthalmic agents
    • A61P27/04—Artificial tears; Irrigation solutions
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    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/12—Ophthalmic agents for cataracts
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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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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P37/02—Immunomodulators
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    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • 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
    • 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

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  • Health & Medical Sciences (AREA)
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  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Dermatology (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Epidemiology (AREA)
  • Transplantation (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Cardiology (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
RU2012131223/04A 2009-12-23 2010-12-22 Производные аминоалкилпиримидина в качестве антагонистов h4 рецептора гистамина RU2573828C2 (ru)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
EP09382302 2009-12-23
EP09382302.9 2009-12-23
US30757910P 2010-02-24 2010-02-24
US61/307,579 2010-02-24
PCT/EP2010/070562 WO2011076878A1 (en) 2009-12-23 2010-12-22 Aminoalkylpyrimidine derivatives as histamine h4 receptor antagonists

Publications (2)

Publication Number Publication Date
RU2012131223A RU2012131223A (ru) 2014-02-10
RU2573828C2 true RU2573828C2 (ru) 2016-01-27

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RU2012131223/04A RU2573828C2 (ru) 2009-12-23 2010-12-22 Производные аминоалкилпиримидина в качестве антагонистов h4 рецептора гистамина

Country Status (17)

Country Link
US (1) US8901146B2 (en:Method)
EP (1) EP2516420B8 (en:Method)
JP (1) JP5781537B2 (en:Method)
KR (1) KR101740085B1 (en:Method)
CN (1) CN102803248B (en:Method)
AR (1) AR079725A1 (en:Method)
AU (1) AU2010334804B2 (en:Method)
BR (1) BR112012017126A2 (en:Method)
CA (1) CA2785353C (en:Method)
IL (1) IL220554A (en:Method)
MX (1) MX345142B (en:Method)
NZ (1) NZ601021A (en:Method)
PE (1) PE20121505A1 (en:Method)
RU (1) RU2573828C2 (en:Method)
TW (1) TWI487697B (en:Method)
UA (1) UA107818C2 (en:Method)
WO (1) WO2011076878A1 (en:Method)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US12234227B2 (en) 2018-10-19 2025-02-25 Nxera Pharma Uk Limited Pyrazole derivatives as H4 antagonist compounds
RU2837355C1 (ru) * 2020-04-22 2025-03-31 НКСЕРА ФАРМА Юкей ЛИМИТЕД Соединения-антагонисты н4

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SI2493895T1 (sl) 2009-10-29 2017-10-30 Vectura Limited Derivati heteroarila, ki vsebujejo N, kot inhibitorji JAK3 kinaze
UA121539C2 (uk) * 2011-09-02 2020-06-25 Інсайт Холдинґс Корпорейшн Гетероцикліламіни як інгібітори рі3к
ES2946551T3 (es) 2017-10-17 2023-07-20 Palau Pharma S L U Síntesis de compuestos de 4-aminopirimidina
JP2022165429A (ja) * 2019-10-02 2022-11-01 Ｍｅｉｊｉ Ｓｅｉｋａファルマ株式会社 ヒスタミンｈ４受容体調節作用を有する新規トリアジン誘導体
CN117018194B (zh) * 2023-07-26 2026-04-17 同济大学 毒蕈碱型受体5型受体拮抗剂的用途

Citations (5)

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WO2004039796A1 (de) * 2002-10-28 2004-05-13 Bayer Healthcare Ag Heteroaryloxy-substituierte phenylaminopyrimidine als rho-kinaseinhibitoren
EP1505064A1 (en) * 2003-08-05 2005-02-09 Bayer HealthCare AG 2-Aminopyrimidine derivatives
WO2006110763A1 (en) * 2005-04-08 2006-10-19 Bayer Pharmaceuticals Corporation Pyrimidine derivatives and their use for the treatment of cancer
WO2009068512A1 (en) * 2007-11-30 2009-06-04 Palau Pharma, S. A. 2 -amino-pyrimidine derivatives as histamine h4 antagonists
WO2009080721A2 (en) * 2007-12-21 2009-07-02 Palau Pharma, S. A. 4 -aminopyrimidine derivatives as histamine h4 receptor antagonists

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TR200001256T2 (tr) * 1997-11-04 2000-11-21 Pfizer Products Inc. Terapötik olarak aktif bileşimler.
JP4544999B2 (ja) * 2002-11-25 2010-09-15 持田製薬株式会社 ４−ヒドロキシピペリジン誘導体を有効成分とする呼吸器疾患治療剤
WO2005054239A1 (en) 2003-12-05 2005-06-16 Bayer Healthcare Ag 2-aminopyrimidine 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
US7528143B2 (en) * 2005-11-01 2009-05-05 Targegen, Inc. Bi-aryl meta-pyrimidine inhibitors of kinases
NL2000323C2 (nl) 2005-12-20 2007-11-20 Pfizer Ltd Pyrimidine-derivaten.
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
US7985745B2 (en) 2006-10-02 2011-07-26 Abbott Laboratories Method for pain treatment
TW200904437A (en) 2007-02-14 2009-02-01 Janssen Pharmaceutica Nv 2-aminopyrimidine modulators of the histamine H4 receptor
WO2009077608A1 (en) 2007-12-19 2009-06-25 Palau Pharma, S. A. 2 -aminopyrimidine derivatives as histamine h4 antagonists

Patent Citations (5)

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WO2004039796A1 (de) * 2002-10-28 2004-05-13 Bayer Healthcare Ag Heteroaryloxy-substituierte phenylaminopyrimidine als rho-kinaseinhibitoren
EP1505064A1 (en) * 2003-08-05 2005-02-09 Bayer HealthCare AG 2-Aminopyrimidine derivatives
WO2006110763A1 (en) * 2005-04-08 2006-10-19 Bayer Pharmaceuticals Corporation Pyrimidine derivatives and their use for the treatment of cancer
WO2009068512A1 (en) * 2007-11-30 2009-06-04 Palau Pharma, S. A. 2 -amino-pyrimidine derivatives as histamine h4 antagonists
WO2009080721A2 (en) * 2007-12-21 2009-07-02 Palau Pharma, S. A. 4 -aminopyrimidine derivatives as histamine h4 receptor antagonists

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& RU2489430 C2. *
COWART M D; ET AL Rotationally Constrained 2,4-Diamino-5,6-disubstituted Pyrimidines: A New Class of Histamine H4 Receptor Antagonists with Improved Druglikeness and in Vivo Efficacy in Pain and Inflammation Models, Journal of Medicinal Chemistry, 26.09.2008,Vol.51, Page(s):6547 " 6557. *

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US12234227B2 (en) 2018-10-19 2025-02-25 Nxera Pharma Uk Limited Pyrazole derivatives as H4 antagonist compounds
RU2837355C1 (ru) * 2020-04-22 2025-03-31 НКСЕРА ФАРМА Юкей ЛИМИТЕД Соединения-антагонисты н4

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EP2516420A1 (en) 2012-10-31
MX2012007385A (es) 2012-08-15
NZ601021A (en) 2014-09-26
MX345142B (es) 2017-01-18
RU2012131223A (ru) 2014-02-10
IL220554A (en) 2016-08-31
WO2011076878A1 (en) 2011-06-30
AU2010334804B2 (en) 2015-04-02
UA107818C2 (en) 2015-02-25
JP2013515698A (ja) 2013-05-09
CN102803248B (zh) 2015-09-16
CN102803248A (zh) 2012-11-28
PE20121505A1 (es) 2012-11-05
BR112012017126A2 (pt) 2017-10-31
CA2785353C (en) 2017-10-31
US20130018031A1 (en) 2013-01-17
KR20120124421A (ko) 2012-11-13
AU2010334804A1 (en) 2012-07-19
CA2785353A1 (en) 2011-06-30
KR101740085B1 (ko) 2017-05-25
US8901146B2 (en) 2014-12-02
AR079725A1 (es) 2012-02-15
JP5781537B2 (ja) 2015-09-24
EP2516420B1 (en) 2018-08-22
TW201141840A (en) 2011-12-01
TWI487697B (zh) 2015-06-11
EP2516420B8 (en) 2018-10-17

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