CN107739338A - 作为辣椒素类似物受体配体的甲酰胺及脲衍生物 - Google Patents

作为辣椒素类似物受体配体的甲酰胺及脲衍生物 Download PDF

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Publication number
CN107739338A
CN107739338A CN201710970447.5A CN201710970447A CN107739338A CN 107739338 A CN107739338 A CN 107739338A CN 201710970447 A CN201710970447 A CN 201710970447A CN 107739338 A CN107739338 A CN 107739338A
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China
Prior art keywords
phenyl
methyl
pyrazol
fluoro
mmol
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Pending
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CN201710970447.5A
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English (en)
Chinese (zh)
Inventor
R.弗兰克-福尔蒂恩
T.克里斯托弗
K.希内
J.德夫里
N.达曼
B.莱施
G.巴伦贝格
D.J.绍恩德斯
H.施托克豪森
金勇洙
金明燮
李智雨
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MEDIFRON DBT CO Ltd
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MEDIFRON DBT CO Ltd
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Publication of CN107739338A publication Critical patent/CN107739338A/zh
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • 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
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • 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
    • 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
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P23/00—Anaesthetics
    • A61P23/02—Local anaesthetics
    • 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
    • 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
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • A61P31/20—Antivirals for DNA viruses
    • A61P31/22—Antivirals for DNA viruses for herpes viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10—Antioedematous agents; Diuretics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
    • C07D407/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Virology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Pulmonology (AREA)
  • Anesthesiology (AREA)
  • Immunology (AREA)
  • Obesity (AREA)
  • Biomedical Technology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Child & Adolescent Psychology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Cardiology (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • Oncology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Dermatology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Biotechnology (AREA)
CN201710970447.5A 2011-11-09 2012-11-08 作为辣椒素类似物受体配体的甲酰胺及脲衍生物 Pending CN107739338A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP11008914.1 2011-11-09
EP11008914 2011-11-09
CN201280053470.3A CN103889961A (zh) 2011-11-09 2012-11-08 作为辣椒素类似物受体配体的携带被含氧基团取代的苯基的被取代的基于吡唑基的甲酰胺及脲衍生物

Related Parent Applications (1)

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CN201280053470.3A Division CN103889961A (zh) 2011-11-09 2012-11-08 作为辣椒素类似物受体配体的携带被含氧基团取代的苯基的被取代的基于吡唑基的甲酰胺及脲衍生物

Publications (1)

Publication Number Publication Date
CN107739338A true CN107739338A (zh) 2018-02-27

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CN201710970447.5A Pending CN107739338A (zh) 2011-11-09 2012-11-08 作为辣椒素类似物受体配体的甲酰胺及脲衍生物
CN201280053470.3A Pending CN103889961A (zh) 2011-11-09 2012-11-08 作为辣椒素类似物受体配体的携带被含氧基团取代的苯基的被取代的基于吡唑基的甲酰胺及脲衍生物

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EP (1) EP2776398B1 (enExample)
JP (1) JP6189313B2 (enExample)
KR (1) KR101985442B1 (enExample)
CN (2) CN107739338A (enExample)
AR (1) AR088702A1 (enExample)
AU (1) AU2012334065B2 (enExample)
BR (1) BR112014011262B1 (enExample)
CA (1) CA2854932A1 (enExample)
ES (1) ES2823577T3 (enExample)
HK (1) HK1201839A1 (enExample)
IN (1) IN2014KN00849A (enExample)
MX (1) MX2014005610A (enExample)
TW (1) TW201326133A (enExample)
WO (1) WO2013068461A1 (enExample)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2016096140A1 (en) * 2014-12-19 2016-06-23 Grünenthal GmbH Process for the preparation of 1-[(heteroaryl)-methyl]- or 1-[(aryl)-methyl]-3-[4-(hydroxymethyl)-phenyl]-ureas
WO2017170884A1 (ja) * 2016-03-31 2017-10-05 富山化学工業株式会社 新規なヒドロキサム酸誘導体の製造方法およびその中間体
CA3062444A1 (en) * 2017-05-19 2018-11-22 Etna-Tec, Ltd Methods for making functionalized fluorinated monomers, fluorinated monomers, and compositions for making the same
CN113135856B (zh) * 2021-04-08 2022-10-11 天津大学 一类3-三氟甲基-5-氰基吡唑化合物及其制备方法

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007045462A2 (de) * 2005-10-19 2007-04-26 Grünenthal GmbH Neue vanilloid-rezeptor liganden und ihre verwendung zur herstellung von arzneimitteln
CN101687799A (zh) * 2007-04-16 2010-03-31 格吕伦塔尔有限公司 新的香草素受体配体及其在制备药物中的用途
WO2010127856A1 (en) * 2009-05-07 2010-11-11 Grünenthal GmbH Substituted phenyllureas and phenylamides as vanilloid receptor ligands

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Publication number Priority date Publication date Assignee Title
EP1020447A4 (en) * 1997-09-11 2000-11-15 Nissan Chemical Ind Ltd PYRAZOLE-BASED COMPOUNDS AND PLANT DISEASE CONTROL AGENT
WO2005048953A2 (en) * 2003-11-13 2005-06-02 Ambit Biosciences Corporation Amide derivatives as kinase modulators
JP2005314407A (ja) * 2004-03-31 2005-11-10 Nippon Nohyaku Co Ltd 新規なハロアルキルスルホンアニリド誘導体、除草剤及びその使用方法並びにその中間体
EP2121621B1 (en) * 2006-12-08 2014-05-07 Exelixis Patent Company LLC Lxr and fxr modulators
PL2427436T3 (pl) * 2009-05-07 2013-06-28 Gruenenthal Gmbh Podstawione aromatyczne pochodne karboksamidu i mocznika jako ligandy receptora waniloidowego
BR112012021806A2 (pt) * 2010-03-01 2015-09-08 Myrexis Inc compostos e seus usos terapêusticos.

Patent Citations (3)

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Publication number Priority date Publication date Assignee Title
WO2007045462A2 (de) * 2005-10-19 2007-04-26 Grünenthal GmbH Neue vanilloid-rezeptor liganden und ihre verwendung zur herstellung von arzneimitteln
CN101687799A (zh) * 2007-04-16 2010-03-31 格吕伦塔尔有限公司 新的香草素受体配体及其在制备药物中的用途
WO2010127856A1 (en) * 2009-05-07 2010-11-11 Grünenthal GmbH Substituted phenyllureas and phenylamides as vanilloid receptor ligands

Non-Patent Citations (2)

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Title
DEVIN M. SWANSON ET AL.: ""Identification and Biological Evaluation of 4-(3-Trifluoromethylpyridin-2-yl)piperazine-1-carboxylic Acid (5-Trifluoromethylpyridin-2-yl)amide, a High Affinity TRPV1 (VR1) Vanilloid Receptor Antagonist"", 《J. MED. CHEM.》 *
戴冬艳等: ""治疗疼痛新途径:瞬时受体电位香草酸亚型1拮抗剂的研究进展"", 《中国药科大学学报》 *

Also Published As

Publication number Publication date
JP6189313B2 (ja) 2017-08-30
MX2014005610A (es) 2014-07-30
EP2776398B1 (en) 2020-09-02
CA2854932A1 (en) 2013-05-16
AU2012334065A1 (en) 2014-05-22
IN2014KN00849A (enExample) 2015-10-02
JP2014532741A (ja) 2014-12-08
AU2012334065B2 (en) 2017-06-08
BR112014011262A2 (pt) 2017-04-25
EP2776398A1 (en) 2014-09-17
HK1201839A1 (en) 2015-09-11
BR112014011262B1 (pt) 2022-02-15
AR088702A1 (es) 2014-06-25
KR101985442B1 (ko) 2019-06-03
ES2823577T3 (es) 2021-05-07
CN103889961A (zh) 2014-06-25
TW201326133A (zh) 2013-07-01
KR20140091043A (ko) 2014-07-18
BR112014011262A8 (pt) 2018-03-06
WO2013068461A1 (en) 2013-05-16

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Application publication date: 20180227