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

Info

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
Authority
CN
China
Prior art keywords
pyrimidin
ethyl
amine
formula
alkyl
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Fee Related
Application number
CN201080064520.9A
Other languages
English (en)
Chinese (zh)
Other versions
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
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Organic Agricultural Biological Sciences Holland Co ltd
Merck Sharp and Dohme BV
Original Assignee
MSD Oss BV
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 MSD Oss BV filed Critical MSD Oss BV
Publication of CN102884048A publication Critical patent/CN102884048A/zh
Application granted granted Critical
Publication of CN102884048B publication Critical patent/CN102884048B/zh
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Virology (AREA)
  • Pain & Pain Management (AREA)
  • Addiction (AREA)
  • Oncology (AREA)
  • Rheumatology (AREA)
  • Communicable Diseases (AREA)
  • Psychiatry (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • AIDS & HIV (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
US61/289182 2009-12-22
US61/289,182 2009-12-22
EP09180321.3 2009-12-22
EP09180321 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

ID=42045216

Family Applications (1)

Application Number Title Priority Date Filing Date
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
CN103442829B (zh) * 2011-05-19 2016-11-16 株式会社东芝 钼造粒粉的制造方法及钼造粒粉
EP3255041A1 (en) 2011-09-02 2017-12-13 Purdue Pharma L.P. Pyrimidines as sodium channel blockers
US9133131B2 (en) 2011-11-15 2015-09-15 Purdue Pharma L.P. Pyrimidine diol amides as sodium channel blockers
MX2014014308A (es) * 2012-05-30 2015-02-12 Hoffmann La Roche Pirrolidino heterociclos.
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
WO2001090142A2 (en) 2000-05-24 2001-11-29 Akzo Nobel N.V. FULL LENGTH HUMAN HCN1 Ih CHANNEL SUBUNIT AND VARIANTS
CN1237969C (zh) * 2001-04-10 2006-01-25 日本新药株式会社 慢性关节风湿病的治疗剂
US6980419B2 (en) 2003-03-12 2005-12-27 Zonare Medical Systems, Inc. Portable ultrasound unit and docking station
US20090182228A1 (en) 2004-09-17 2009-07-16 Koninklijke Philips Electronics, N.V. Wireless ultrasound system display
SI2848610T1 (en) * 2006-11-15 2018-02-28 Ym Biosciences Australia Pty Ltd Inhibitors of kinase activity
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
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
RU2012131279A (ru) 2014-01-27
CA2783209C (en) 2017-03-14
JP2013515031A (ja) 2013-05-02
KR20120095481A (ko) 2012-08-28
EP2516397A1 (en) 2012-10-31
CN102884048A (zh) 2013-01-16
US8952001B2 (en) 2015-02-10
AR079543A1 (es) 2012-02-01
AU2010335231B2 (en) 2014-09-11
MX2012007426A (es) 2012-07-23
AU2010335231C1 (en) 2015-04-16
WO2011076723A1 (en) 2011-06-30
CA2783209A1 (en) 2011-06-30
EP2516397B1 (en) 2016-07-13
JP5728024B2 (ja) 2015-06-03
BR112012015170A2 (pt) 2016-03-29
RU2549546C2 (ru) 2015-04-27
AU2010335231A1 (en) 2012-06-21
US20120264728A1 (en) 2012-10-18

Similar Documents

Publication Publication Date Title
TWI414291B (zh) 新穎的氮雜聯苯胺基苯甲酸衍生物
CN101589025B (zh) 氨基烟酸和异烟酸的衍生物作为二氢乳酸脱氢酶(dhodh)抑制剂
CN1890218B (zh) 微管蛋白抑制剂
CN102143955A (zh) 作为代谢型谷氨酸受体调节剂的3-氮杂二环[3.1.0]己烷衍生物
JP2008536950A (ja) 置換ヘテロアリールのｃｂ１拮抗薬
SK6142000A3 (en) HETEROARYL DIAZACYCLOALKANES AS CHOLINERGIC LIGANDS AT NICOTINICì (54) ACETYLCHOLINE RECEPTORS
CN114761003A (zh) 具有雄激素受体降解活性的新型脲类及其用途
CN102884048B (zh) 用作hcn阻滞剂的氨基杂芳基衍生物
WO2020135210A1 (zh) 取代芳基化合物及其制备方法和用途
WO2020021015A1 (en) New imidazopyridine derivatives for treating pain and pain related conditions
TW200944512A (en) Hydroxyquinoxaline carboxamide derivatives
JP2022544700A (ja) 筋萎縮性側索硬化症および関連障害の治療のためにｔｄｐ－４３に結合する分子
WO2000078730A1 (en) Novel dihydropyrimidine derivatives
EP0973766B1 (en) Quinoxalinediones
JP2003528098A (ja) 抗血栓症薬および抗凝血薬としてのｎ−（ヘテロ環式）ベンゼン−または−ピリジンスルホンアミド
JP6983222B2 (ja) 肺線維症の処置のための組成物
AP982A (en) Quinoxalinediones.
CN105722823A (zh) 新型细胞色素p450抑制剂及其使用方法
WO2024059216A2 (en) 6,6 southwestern core compounds as mglu5 negative allosteric modulators and methods of making and using the same
TW201130812A (en) Amino-heteroaryl derivatives
WO2024059212A2 (en) 6,6 western core compounds as mglu5 negative allosteric modulators and methods of making and using the same
HK40075584A (en) Kv3 enhancers for the treatment of cognitive disorders
EP3873901A1 (en) New alcoxyaminopyridine derivatives for treating pain and pain related conditions

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
ASS Succession or assignment of patent right

Owner name: ORGANON BIOSCIENCES NEDERLAND B. V.

Free format text: FORMER OWNER: MSD OUSI CO., LTD.

Effective date: 20130620

Owner name: MERCK SHARP + DOHME CORP.

Free format text: FORMER OWNER: ORGANON BIOSCIENCES NEDERLAND B. V.

Effective date: 20130620

C41 Transfer of patent application or patent right or utility model
TA01 Transfer of patent application right

Effective date of registration: 20130620

Address after: Haarlem

Applicant after: MERCK SHARP & DOHME B.V.

Address before: Holland

Applicant before: Organic agricultural biological sciences Holland Co.,Ltd.

Effective date of registration: 20130620

Address after: Holland

Applicant after: Organic agricultural biological sciences Holland Co.,Ltd.

Address before: Holland

Applicant before: N.V. Organon

C14 Grant of patent or utility model
GR01 Patent grant
CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20140723

Termination date: 20191220

CF01 Termination of patent right due to non-payment of annual fee