TW201321353A - 胺基甲酸酯／尿素衍生物 - Google Patents

胺基甲酸酯／尿素衍生物 Download PDF

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Publication number
TW201321353A
TW201321353A TW101137030A TW101137030A TW201321353A TW 201321353 A TW201321353 A TW 201321353A TW 101137030 A TW101137030 A TW 101137030A TW 101137030 A TW101137030 A TW 101137030A TW 201321353 A TW201321353 A TW 201321353A
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TW
Taiwan
Prior art keywords
ester
carboxylic acid
hexahydropyridin
isopropylhexahydropyrazine
alkyl
Prior art date
Application number
TW101137030A
Other languages
English (en)
Chinese (zh)
Inventor
Tielin Wang
xue-chun Zhang
Original Assignee
Novartis Ag
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 Novartis Ag filed Critical Novartis Ag
Publication of TW201321353A publication Critical patent/TW201321353A/zh

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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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines 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
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/40—Oxygen atoms
    • C07D211/44—Oxygen atoms attached in position 4
    • C07D211/46—Oxygen atoms attached in position 4 having a hydrogen atom as the second substituent in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/92—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with a hetero atom directly attached to the ring nitrogen atom
    • C07D211/94—Oxygen atom, e.g. piperidine N-oxide
    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Anesthesiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Hydrogenated Pyridines (AREA)
TW101137030A 2011-10-08 2012-10-05 胺基甲酸酯／尿素衍生物 TW201321353A (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN2011080529 2011-10-08
CN2012081326 2012-09-13

Publications (1)

Publication Number Publication Date
TW201321353A true TW201321353A (zh) 2013-06-01

Family

ID=47278913

Family Applications (1)

Application Number Title Priority Date Filing Date
TW101137030A TW201321353A (zh) 2011-10-08 2012-10-05 胺基甲酸酯／尿素衍生物

Country Status (15)

Country Link
US (1) US9216182B2 (OSRAM)
EP (1) EP2763978B1 (OSRAM)
JP (1) JP6046149B2 (OSRAM)
KR (1) KR20140072076A (OSRAM)
CN (1) CN103917534B (OSRAM)
AR (1) AR088256A1 (OSRAM)
AU (1) AU2012320038A1 (OSRAM)
BR (1) BR112014007578A2 (OSRAM)
CA (1) CA2851405A1 (OSRAM)
EA (1) EA201490754A1 (OSRAM)
ES (1) ES2624421T3 (OSRAM)
IN (1) IN2014DN01629A (OSRAM)
MX (1) MX2014004254A (OSRAM)
TW (1) TW201321353A (OSRAM)
WO (1) WO2013050987A1 (OSRAM)

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* Cited by examiner, † Cited by third party
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US9034874B2 (en) * 2012-07-20 2015-05-19 Novartis Ag Carbamate/urea derivatives
CA2934700A1 (en) 2014-01-06 2015-07-09 Rhizen Pharmaceuticals Sa Glutaminase inhibitors
EP3391886A1 (en) 2017-04-19 2018-10-24 Novartis AG The use of a h3r inverse agonist for the treatment of shift work disorder
US20190381056A1 (en) 2018-06-17 2019-12-19 Axsome Therapeutics, Inc. Compositions for delivery of reboxetine
US11020402B2 (en) 2018-10-15 2021-06-01 Axsome Therapeutics, Inc. Use of reboxetine to treat narcolepsy
US20200147093A1 (en) 2018-10-15 2020-05-14 Axsome Therapeutics, Inc. Use of esreboxetine to treat nervous system disorders such as fibromyalgia
CN109666020A (zh) * 2018-12-20 2019-04-23 苏州麦迪耐斯医药科技有限公司 一种新型化合物及其制备方法和应用
US12616702B2 (en) 2019-12-03 2026-05-05 Axsome Therapeutics, Inc. Use of reboxetine to treat narcolepsy
CN111057045A (zh) * 2019-12-18 2020-04-24 安徽红杉生物医药科技有限公司 Hcv ns3/4a蛋白酶抑制剂中间体及其合成方法、应用
EP4251148A1 (en) 2020-11-27 2023-10-04 Richter Gedeon Nyrt. Histamine h3 receptor antagonists/inverse agonists for the treatment of autism spectrum disorder
JP2025536720A (ja) * 2022-11-17 2025-11-07 ディーアールアイ バイオサイエンシーズ コーポレイション 神経状態を処置する組成物及び方法
US12565478B1 (en) 2025-01-21 2026-03-03 Axsome Therapeutics, Inc. (S)-2-((S)-(2-ethoxyphenoxy)(phenyl)methyl)-4-nitrosomorpholine

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US4513135A (en) * 1982-03-05 1985-04-23 Eli Lilly And Company Diaryl-pyrazine derivatives affecting GABA binding
FR2567518B1 (fr) * 1984-07-11 1987-11-13 Sanofi Sa Nouveaux composes a noyau heterocyclique azote, leur preparation et les medicaments qui en contiennent
US5124457A (en) 1986-05-21 1992-06-23 Abbott Laboratories Phencyclidine and phencyclidine metabolites assay, tracers, immunogens and antibodies
TW301607B (OSRAM) 1993-03-09 1997-04-01 Takeda Pharm Industry Co Ltd
JPH06316522A (ja) * 1993-03-09 1994-11-15 Takeda Chem Ind Ltd 細胞接着阻害剤
MXPA03008356A (es) 2001-03-13 2003-12-11 Schering Corp Compuestos del tipo no imidazol como antagonistas de histamina h3.
CA2514733A1 (en) 2003-02-28 2004-09-16 Transform Pharmaceuticals, Inc. Pharmaceutical co-crystal compositions of drugs such as carbamazepine, celecoxib, olanzapine, itraconazole, topiramate, modafinil, 5-fluorouracil, hydrochlorothiazide, acetaminophen, aspirin, flurbiprofen, phenytoin and ibuprofen
MXPA05011352A (es) 2003-04-23 2005-11-28 Glaxo Group Ltd Derivados de piperazina y su uso para el tratamiento de enfermedades neurologicas y psiquiatricas.
SE0401971D0 (sv) 2004-08-02 2004-08-02 Astrazeneca Ab Piperidne derivatives
AU2006275568A1 (en) * 2005-08-02 2007-02-08 Neurogen Corporation Dipiperazinyl ketones and related analogues
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US20090182140A1 (en) * 2005-12-02 2009-07-16 Mitsubishi Tanabe Pharma Corporation Alicyclic Heterocyclic Compound
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US9034874B2 (en) 2012-07-20 2015-05-19 Novartis Ag Carbamate/urea derivatives

Also Published As

Publication number Publication date
US20140235609A1 (en) 2014-08-21
US9216182B2 (en) 2015-12-22
CN103917534A (zh) 2014-07-09
AU2012320038A1 (en) 2014-04-24
KR20140072076A (ko) 2014-06-12
EP2763978B1 (en) 2017-02-01
BR112014007578A2 (pt) 2017-04-11
WO2013050987A9 (en) 2013-07-25
WO2013050987A1 (en) 2013-04-11
EP2763978A1 (en) 2014-08-13
JP6046149B2 (ja) 2016-12-14
CA2851405A1 (en) 2013-04-11
CN103917534B (zh) 2016-11-16
AR088256A1 (es) 2014-05-21
EA201490754A1 (ru) 2014-07-30
ES2624421T3 (es) 2017-07-14
MX2014004254A (es) 2014-10-17
JP2014530807A (ja) 2014-11-20
IN2014DN01629A (OSRAM) 2015-05-15

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