CN102884048B - 用作hcn阻滞剂的氨基杂芳基衍生物 - Google Patents

用作hcn阻滞剂的氨基杂芳基衍生物 Download PDF

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Publication number
CN102884048B
CN102884048B CN201080064520.9A CN201080064520A CN102884048B CN 102884048 B CN102884048 B CN 102884048B CN 201080064520 A CN201080064520 A CN 201080064520A CN 102884048 B CN102884048 B CN 102884048B
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CN
China
Prior art keywords
pyrimidin
ethyl
amine
formula
alkyl
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Expired - Fee Related
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CN201080064520.9A
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English (en)
Chinese (zh)
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CN102884048A (zh
Inventor
S.J.A.格罗夫
A.J.莫里森
C.贾米森
R.帕林
J.K.F.麦利恩
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Organic Agricultural Biological Sciences Holland Co ltd
Merck Sharp & Dohme BV
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Merck Sharp & Dohme BV
Organon NV
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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
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • 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
    • 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
    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32—Alcohol-abuse
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic 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
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/73—Unsubstituted amino or imino radicals
    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/12—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 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
    • C07D403/02—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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Addiction (AREA)
  • Virology (AREA)
  • Pain & Pain Management (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Psychiatry (AREA)
  • AIDS & HIV (AREA)
  • Molecular Biology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
CN201080064520.9A 2009-12-22 2010-12-20 用作hcn阻滞剂的氨基杂芳基衍生物 Expired - Fee Related CN102884048B (zh)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US28918209P 2009-12-22 2009-12-22
US61/289,182 2009-12-22
EP09180321.3 2009-12-22
EP09180321 2009-12-22
US61/289182 2009-12-22
PCT/EP2010/070213 WO2011076723A1 (en) 2009-12-22 2010-12-20 Amino-heteroaryl derivatives as hcn blockers

Publications (2)

Publication Number Publication Date
CN102884048A CN102884048A (zh) 2013-01-16
CN102884048B true CN102884048B (zh) 2014-07-23

Family

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CN201080064520.9A Expired - Fee Related CN102884048B (zh) 2009-12-22 2010-12-20 用作hcn阻滞剂的氨基杂芳基衍生物

Country Status (12)

Country Link
US (1) US8952001B2 (enExample)
EP (1) EP2516397B1 (enExample)
JP (1) JP5728024B2 (enExample)
KR (1) KR20120095481A (enExample)
CN (1) CN102884048B (enExample)
AR (1) AR079543A1 (enExample)
AU (1) AU2010335231C1 (enExample)
BR (1) BR112012015170A8 (enExample)
CA (1) CA2783209C (enExample)
MX (1) MX2012007426A (enExample)
RU (1) RU2549546C2 (enExample)
WO (1) WO2011076723A1 (enExample)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP5917503B2 (ja) * 2011-05-19 2016-05-18 株式会社東芝 モリブデン造粒粉の製造方法
US9163008B2 (en) 2011-09-02 2015-10-20 Purdue Pharma, L.P. Pyrimidines as sodium channel blockers
WO2013072758A1 (en) 2011-11-15 2013-05-23 Purdue Pharma L.P. Pyrimidine diol amides as sodium channel blockers
CN104363908B (zh) * 2012-05-30 2017-12-22 霍夫曼-拉罗奇有限公司 吡咯烷基杂环类
CN106588803A (zh) * 2016-11-16 2017-04-26 西南科技大学 一种制备5‑乙酰基异噁唑的新方法

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008067389A2 (en) * 2006-11-28 2008-06-05 Alsgen, Inc. Modulation of sod protein synthesis for the treatment of neurodegenerative diseases
US20090221597A1 (en) * 2008-02-28 2009-09-03 Sara Hadida Ruah Heteroaryl derivatives as cftr modulators

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4606757A (en) * 1982-12-23 1986-08-19 The Dow Chemical Company Diphenoxymethylpyridines having herbicidal properties
KR100197583B1 (ko) 1997-02-04 1999-06-15 이민화 환자용모니터를 구비한 초음파진단장치
US7329510B2 (en) 2000-05-24 2008-02-12 N.V. Organon Full length human HCN1Ih channel subunit and variants
US6967211B2 (en) * 2001-04-10 2005-11-22 Nippon Shinyaku Co. Ltd. Remedial agent for chronic articular rheumatism
US6980419B2 (en) 2003-03-12 2005-12-27 Zonare Medical Systems, Inc. Portable ultrasound unit and docking station
JP2008513084A (ja) 2004-09-17 2008-05-01 コーニンクレッカ フィリップス エレクトロニクス エヌ ヴィ ワイヤレス超音波システムディスプレイ
PL2848610T3 (pl) * 2006-11-15 2018-01-31 Ym Biosciences Australia Pty Inhibitory aktywności kinazy
PE20091524A1 (es) * 2007-12-19 2009-09-25 Palau Pharma Sa Derivados de 2-aminopirimidina
TW201022233A (en) 2008-11-04 2010-06-16 Organon Nv (Pyrrolidin-2-yl)phenyl derivatives

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008067389A2 (en) * 2006-11-28 2008-06-05 Alsgen, Inc. Modulation of sod protein synthesis for the treatment of neurodegenerative diseases
US20090221597A1 (en) * 2008-02-28 2009-09-03 Sara Hadida Ruah Heteroaryl derivatives as cftr modulators

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
RN 338397-88-9 REGISTRY;-;《STN REGISTRY》;20010525 *
RN 338976-09-3 REGISTRY;-;《STN REGISTRY》;20010530 *

Also Published As

Publication number Publication date
BR112012015170A8 (pt) 2017-12-26
JP5728024B2 (ja) 2015-06-03
CA2783209C (en) 2017-03-14
RU2012131279A (ru) 2014-01-27
WO2011076723A1 (en) 2011-06-30
AU2010335231B2 (en) 2014-09-11
RU2549546C2 (ru) 2015-04-27
US20120264728A1 (en) 2012-10-18
AR079543A1 (es) 2012-02-01
US8952001B2 (en) 2015-02-10
CN102884048A (zh) 2013-01-16
AU2010335231A1 (en) 2012-06-21
AU2010335231C1 (en) 2015-04-16
KR20120095481A (ko) 2012-08-28
BR112012015170A2 (pt) 2016-03-29
EP2516397B1 (en) 2016-07-13
MX2012007426A (es) 2012-07-23
EP2516397A1 (en) 2012-10-31
CA2783209A1 (en) 2011-06-30
JP2013515031A (ja) 2013-05-02

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