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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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
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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
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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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
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    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/16—Central respiratory analeptics
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    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • 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
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    • 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
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    • 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)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Biomedical Technology (AREA)
  • Dermatology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Transplantation (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Otolaryngology (AREA)
  • Orthopedic Medicine & Surgery (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

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

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

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
AU2010311378B2 (en) 2009-10-29 2014-04-24 Vectura Limited N-containing heteroaryl derivatives as JAK3 kinase inhibitors
SI3513793T1 (sl) * 2011-09-02 2021-07-30 Incyte Holdings Corporation Heterociklilamini kot zaviralci PI3K
EP3697776B1 (en) 2017-10-17 2023-04-19 Palau Pharma, S.L.U. Synthesis of 4-aminopyrimidine compounds
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
CN117018194A (zh) * 2023-07-26 2023-11-10 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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BR9813938A (pt) * 1997-11-04 2000-09-26 Pfizer Prod Inc Compostos terapeuticamente ativos baseados na substituição bioisóstera de indazol por catecol em inibidores de pde4
EP1568688B1 (en) * 2002-11-25 2011-08-31 Mochida Pharmaceutical Co., Ltd. Therapeutic agent for respiratory disease containing 4-hydroxypiperidine derivative as active ingredient
WO2005054239A1 (en) 2003-12-05 2005-06-16 Bayer Healthcare Ag 2-aminopyrimidine derivatives
RU2008114378A (ru) 2005-09-13 2009-10-20 Палау Фарма, С.А. (Es) Производные 2-аминопиримидина как модуляторы активности н4-рецептора гистамина
MY167260A (en) * 2005-11-01 2018-08-14 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
AR069813A1 (es) 2007-12-19 2010-02-17 Palau Pharma Sa Derivados de 2- amino-pirimidina, una composicion farmaceutica, un metodo de preparacion del compuesto y uso del mismo para preparar un medicamento

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

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