CN1312136C - 用作速激肽受体拮抗剂的三唑衍生物 - Google Patents

用作速激肽受体拮抗剂的三唑衍生物 Download PDF

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Publication number
CN1312136C
CN1312136C CNB038091046A CN03809104A CN1312136C CN 1312136 C CN1312136 C CN 1312136C CN B038091046 A CNB038091046 A CN B038091046A CN 03809104 A CN03809104 A CN 03809104A CN 1312136 C CN1312136 C CN 1312136C
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CN
China
Prior art keywords
trifluoromethyl
phenyl
benzyl
bis
chloro
Prior art date
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Expired - Lifetime
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CNB038091046A
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English (en)
Chinese (zh)
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CN1646502A (zh
Inventor
A·K·阿梅加兹
K·M·加迪尼尔
E·J·赫姆布雷
J·E·洪
L·N·荣黑姆
B·S·米尔
D·M·雷米克
M·A·罗伯逊
K·A·萨文
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Eli Lilly and Co
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Eli Lilly and Co
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Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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    • 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
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • 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
    • 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
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • A61P25/24—Antidepressants
    • 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
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/04—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles
    • C07D249/06—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles with aryl radicals directly attached to ring atoms
    • 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
    • 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
    • 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
    • C07D403/14—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
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms 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
    • C07D417/14—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
    • 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

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Pulmonology (AREA)
  • Hospice & Palliative Care (AREA)
  • Otolaryngology (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CNB038091046A 2002-04-26 2003-04-22 用作速激肽受体拮抗剂的三唑衍生物 Expired - Lifetime CN1312136C (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US37612102P 2002-04-26 2002-04-26
US60/376,121 2002-04-26

Publications (2)

Publication Number Publication Date
CN1646502A CN1646502A (zh) 2005-07-27
CN1312136C true CN1312136C (zh) 2007-04-25

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CNB038091046A Expired - Lifetime CN1312136C (zh) 2002-04-26 2003-04-22 用作速激肽受体拮抗剂的三唑衍生物

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Country Link
US (1) US7320994B2 (enExample)
EP (1) EP1501809B1 (enExample)
JP (1) JP4559087B2 (enExample)
KR (1) KR100755577B1 (enExample)
CN (1) CN1312136C (enExample)
AR (1) AR039329A1 (enExample)
AT (1) ATE384053T1 (enExample)
AU (1) AU2003230829B8 (enExample)
BR (1) BRPI0309534B8 (enExample)
CA (1) CA2483159C (enExample)
CR (1) CR7548A (enExample)
CY (1) CY1107221T1 (enExample)
DE (1) DE60318697T2 (enExample)
DK (1) DK1501809T3 (enExample)
EA (1) EA007720B1 (enExample)
EC (1) ECSP045391A (enExample)
ES (1) ES2298513T3 (enExample)
HR (1) HRP20041008B1 (enExample)
IL (2) IL164675A0 (enExample)
MX (1) MXPA04010622A (enExample)
MY (1) MY141559A (enExample)
NO (1) NO333647B1 (enExample)
NZ (1) NZ535886A (enExample)
PE (1) PE20040600A1 (enExample)
PL (1) PL212090B1 (enExample)
PT (1) PT1501809E (enExample)
TW (1) TWI265807B (enExample)
UA (1) UA79113C2 (enExample)
WO (1) WO2003091226A1 (enExample)
ZA (1) ZA200408670B (enExample)

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GB201609603D0 (en) 2016-06-01 2016-07-13 Kalvista Pharmaceuticals Ltd Polymorphs of N-[(6-cyano-2-fluoro-3-methoxyphenyl)Methyl]-3-(methoxymethyl)-1-({4-[(2-ox opyridin-1-YL)Methyl]phenyl}methyl)pyrazole-4-carboxamide
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CN111093671A (zh) 2017-09-13 2020-05-01 万达制药公司 以托吡坦对特应性皮炎的改进治疗
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DK3716952T3 (da) 2017-11-29 2022-03-14 Kalvista Pharmaceuticals Ltd Doseringsformer omfattende en plasmakallikrein-inhibitor
WO2019162519A1 (en) 2018-02-26 2019-08-29 Ospedale San Raffaele S.R.L. Nk-1 antagonists for use in the treatment of ocular pain
CA3101210A1 (en) * 2018-06-08 2019-12-12 Vanda Pharmaceuticals Inc. Method of treatment with tradipitant
US10821099B2 (en) 2018-09-28 2020-11-03 Vanda Pharmaceuticals Inc. Use of tradipitant in motion sickness
JP7468964B2 (ja) 2018-09-28 2024-04-16 バンダ・ファーマシューティカルズ・インコーポレイテッド 動揺病におけるトラジピタントの使用
US20220096449A1 (en) 2018-12-03 2022-03-31 Vanda Pharmaceuticals Inc. Method of treatment with tradipitant
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CN115052599A (zh) 2020-02-25 2022-09-13 万达制药公司 以川地匹坦对特应性皮炎的改进治疗
US20230134843A1 (en) 2020-03-11 2023-05-04 Ospedale San Raffaele S.R.L. Treatment of stem cell deficiency
US20230145932A1 (en) 2020-03-26 2023-05-11 Vanda Pharmaceuticals Inc. Treatment of lower respiratory tract infection with tradipitant
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CN113563306B (zh) * 2020-04-28 2022-07-01 新发药业有限公司 一种2-(4-苯氧基苯基)-6-(哌啶-4-)基烟酰胺的制备方法
MX2022014901A (es) 2020-06-02 2023-01-18 Nerre Therapeutics Ltd Antagonistas del receptor de neuroquinina (nk)-1 para su uso en el tratamiento de condiciones de fibrosis pulmonar promovidas por lesion mecanica a los pulmones.
CN111662235B (zh) * 2020-06-23 2023-12-22 黄淮学院 一种苯甲酰基哒嗪衍生物及其制备方法
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US20240350469A1 (en) 2021-08-31 2024-10-24 Vanda Pharmaceuticals Inc. Treatment of lower respiratory tract infection with tradipitant
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CY1107221T1 (el) 2012-11-21
EP1501809B1 (en) 2008-01-16
HK1073304A1 (en) 2005-09-30
WO2003091226A1 (en) 2003-11-06
MY141559A (en) 2010-05-14
CR7548A (es) 2006-12-01
BRPI0309534B8 (pt) 2021-05-25
BRPI0309534B1 (pt) 2017-11-07
ATE384053T1 (de) 2008-02-15
NZ535886A (en) 2007-07-27
TW200306824A (en) 2003-12-01
ZA200408670B (en) 2005-10-26
MXPA04010622A (es) 2005-01-25
EA007720B1 (ru) 2006-12-29
US7320994B2 (en) 2008-01-22
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JP4559087B2 (ja) 2010-10-06
IL198122A0 (en) 2009-12-24
UA79113C2 (en) 2007-05-25
ECSP045391A (es) 2005-01-03
IL164675A0 (en) 2005-12-18
AU2003230829A1 (en) 2003-11-10
DK1501809T3 (da) 2008-05-13
PL212090B1 (pl) 2012-08-31
PT1501809E (pt) 2008-03-18
HRP20041008A2 (en) 2004-12-31
ES2298513T3 (es) 2008-05-16
AU2003230829B8 (en) 2008-12-11
EA200401431A1 (ru) 2005-06-30
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AU2003230829B2 (en) 2008-12-04
AR039329A1 (es) 2005-02-16
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US20050239786A1 (en) 2005-10-27
KR100755577B1 (ko) 2007-09-12
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BR0309534A (pt) 2005-02-01
CN1646502A (zh) 2005-07-27
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CA2483159A1 (en) 2003-11-06
HRP20041008B1 (hr) 2012-10-31
PE20040600A1 (es) 2004-09-15
NO20045120L (no) 2004-12-07

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