CN102803248B - 作为组胺h4受体拮抗剂的氨烷基嘧啶 - Google Patents

作为组胺h4受体拮抗剂的氨烷基嘧啶 Download PDF

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Publication number
CN102803248B
CN102803248B CN201080064585.3A CN201080064585A CN102803248B CN 102803248 B CN102803248 B CN 102803248B CN 201080064585 A CN201080064585 A CN 201080064585A CN 102803248 B CN102803248 B CN 102803248B
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alkyl
formula
cycloalkyl
methyl
compound
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CN102803248A (zh
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依伦娜·卡尔塞勒·冈萨雷斯
玛丽娜·维尔吉利·博纳多
罗伯特·萨利维·萨利维
卡勒斯·费雷尔·科斯塔
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Palau Pharmaceutical Co ltd
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Palau Pharma SA
Medicis Pharmaceutical Corp
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    • 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
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/16—Central respiratory analeptics
    • 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
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • 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
    • A61P27/04—Artificial tears; Irrigation solutions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P27/02—Ophthalmic agents
    • A61P27/12—Ophthalmic agents for cataracts
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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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    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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    • C—CHEMISTRY; METALLURGY
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    • 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
    • C07D403/02—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
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    • C07—ORGANIC CHEMISTRY
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    • 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
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    • 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
    • A—HUMAN NECESSITIES
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    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
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    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (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)
  • Biomedical Technology (AREA)
  • Dermatology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Neurology (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Epidemiology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Transplantation (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN201080064585.3A 2009-12-23 2010-12-22 作为组胺h4受体拮抗剂的氨烷基嘧啶 Active CN102803248B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
EP09382302.9 2009-12-23
EP09382302 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
CN102803248A CN102803248A (zh) 2012-11-28
CN102803248B true CN102803248B (zh) 2015-09-16

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CN201080064585.3A Active CN102803248B (zh) 2009-12-23 2010-12-22 作为组胺h4受体拮抗剂的氨烷基嘧啶

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

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP5759471B2 (ja) 2009-10-29 2015-08-05 ヴェクチュラ リミテッド Ｊａｋ３キナーゼ阻害剤としての窒素含有ヘテロアリール誘導体
MX389479B (es) * 2011-09-02 2025-03-20 Incyte Holdings Corp Heterociclilaminas como inhibidores de fosfoinositida 3-cinasas (pi3k)
ES2946551T3 (es) 2017-10-17 2023-07-20 Palau Pharma S L U Síntesis de compuestos de 4-aminopirimidina
GB201817047D0 (en) 2018-10-19 2018-12-05 Heptares Therapeutics Ltd H4 antagonist 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
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 (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004039796A1 (de) * 2002-10-28 2004-05-13 Bayer Healthcare Ag Heteroaryloxy-substituierte phenylaminopyrimidine als rho-kinaseinhibitoren
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

Family Cites Families (11)

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CN1281441A (zh) * 1997-11-04 2001-01-24 辉瑞产品公司 以在pde4抑制剂中的儿茶酚的吲唑生物等排物置换为基础的治疗活性化合物
US7494987B2 (en) * 2002-11-25 2009-02-24 Mochida Pharmaceutical Co., Ltd. Agent for treating respiratory diseases containing 4-hydroxypiperidine derivative as active ingredient
EP1505064A1 (en) * 2003-08-05 2005-02-09 Bayer HealthCare AG 2-Aminopyrimidine derivatives
WO2005054239A1 (en) 2003-12-05 2005-06-16 Bayer Healthcare Ag 2-aminopyrimidine derivatives
US20090306038A1 (en) 2005-09-13 2009-12-10 Carceller Gonzalez Elena 2-Aminopyrimidine derivatives as modulators of the histamine H4 receptor activity
WO2007053452A1 (en) * 2005-11-01 2007-05-10 Targegen, Inc. Bi-aryl meta-pyrimidine inhibitors of kinases
NL2000323C2 (nl) 2005-12-20 2007-11-20 Pfizer Ltd Pyrimidine-derivaten.
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
US7985745B2 (en) 2006-10-02 2011-07-26 Abbott Laboratories Method for pain treatment
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
PE20091524A1 (es) 2007-12-19 2009-09-25 Palau Pharma Sa Derivados de 2-aminopirimidina

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004039796A1 (de) * 2002-10-28 2004-05-13 Bayer Healthcare Ag Heteroaryloxy-substituierte phenylaminopyrimidine als rho-kinaseinhibitoren
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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EP2516420B8 (en) 2018-10-17
KR20120124421A (ko) 2012-11-13
IL220554A (en) 2016-08-31
EP2516420A1 (en) 2012-10-31
RU2012131223A (ru) 2014-02-10
MX2012007385A (es) 2012-08-15
TW201141840A (en) 2011-12-01
AU2010334804B2 (en) 2015-04-02
CA2785353A1 (en) 2011-06-30
UA107818C2 (en) 2015-02-25
AU2010334804A1 (en) 2012-07-19
BR112012017126A2 (pt) 2017-10-31
PE20121505A1 (es) 2012-11-05
KR101740085B1 (ko) 2017-05-25
US8901146B2 (en) 2014-12-02
US20130018031A1 (en) 2013-01-17
RU2573828C2 (ru) 2016-01-27
NZ601021A (en) 2014-09-26
AR079725A1 (es) 2012-02-15
JP2013515698A (ja) 2013-05-09
MX345142B (es) 2017-01-18
EP2516420B1 (en) 2018-08-22
CN102803248A (zh) 2012-11-28
JP5781537B2 (ja) 2015-09-24
WO2011076878A1 (en) 2011-06-30
TWI487697B (zh) 2015-06-11
CA2785353C (en) 2017-10-31

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