JP7171567B2 - 一過性受容体電位型チャネル阻害剤としてのオキサジアゾロン類 - Google Patents

一過性受容体電位型チャネル阻害剤としてのオキサジアゾロン類 Download PDF

Info

Publication number
JP7171567B2
JP7171567B2 JP2019527497A JP2019527497A JP7171567B2 JP 7171567 B2 JP7171567 B2 JP 7171567B2 JP 2019527497 A JP2019527497 A JP 2019527497A JP 2019527497 A JP2019527497 A JP 2019527497A JP 7171567 B2 JP7171567 B2 JP 7171567B2
Authority
JP
Japan
Prior art keywords
mmol
methyl
preparation
oxo
stirred
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.)
Active
Application number
JP2019527497A
Other languages
English (en)
Japanese (ja)
Other versions
JP2019535761A (ja
JP2019535761A5 (enExample
Inventor
ボーミエ，フランシス
チェン，ホイフェン
クライドランド，アンドリュー
ドゥリー，マルタン
フウ，バイフア
ラルーシュ－ゴーチエ，ロバン
ルウ，アイジュン
ショア，ダニエル
ヴィルミュール，エリシア
ヴォルグラフ，マシュー
ワード，スチュアート
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.)
F Hoffmann La Roche AG
Original Assignee
F Hoffmann La Roche 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 F Hoffmann La Roche AG filed Critical F Hoffmann La Roche AG
Publication of JP2019535761A publication Critical patent/JP2019535761A/ja
Publication of JP2019535761A5 publication Critical patent/JP2019535761A5/ja
Application granted granted Critical
Publication of JP7171567B2 publication Critical patent/JP7171567B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/28—Oxygen atom
    • C07D473/30—Oxygen atom attached in position 6, e.g. hypoxanthine
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • 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
    • 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
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/14—Antitussive agents
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • 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
    • 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
    • A61P27/16—Otologicals
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Epidemiology (AREA)
  • Neurology (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Dermatology (AREA)
  • Biomedical Technology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
JP2019527497A 2016-11-28 2017-11-27 一過性受容体電位型チャネル阻害剤としてのオキサジアゾロン類 Active JP7171567B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
CN2016107423 2016-11-28
CNPCT/CN2016/107423 2016-11-28
CN201711122317 2017-11-14
CN201711122317.2 2017-11-14
PCT/EP2017/080571 WO2018096159A1 (en) 2016-11-28 2017-11-27 Oxadiazolones as transient receptor potential channel inhibitors

Publications (3)

Publication Number Publication Date
JP2019535761A JP2019535761A (ja) 2019-12-12
JP2019535761A5 JP2019535761A5 (enExample) 2021-01-07
JP7171567B2 true JP7171567B2 (ja) 2022-11-15

Family

ID=60473538

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2019527497A Active JP7171567B2 (ja) 2016-11-28 2017-11-27 一過性受容体電位型チャネル阻害剤としてのオキサジアゾロン類

Country Status (6)

Country Link
US (1) US10913742B2 (enExample)
EP (1) EP3544979B1 (enExample)
JP (1) JP7171567B2 (enExample)
CN (1) CN110225911B (enExample)
TW (1) TW201831477A (enExample)
WO (1) WO2018096159A1 (enExample)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110461838B (zh) 2017-03-07 2022-05-06 豪夫迈·罗氏有限公司 噁二唑瞬时受体电位通道抑制剂
US10710994B2 (en) 2018-03-19 2020-07-14 Genentech, Inc. Oxadiazole transient receptor potential channel inhibitors
GB201901757D0 (en) 2019-02-08 2019-03-27 Syngenta Crop Protection Ag Herbicidal compounds
US11884652B2 (en) * 2020-06-29 2024-01-30 Boehringer Ingelheim International Gmbh Tetrazole derivatives as TRPA1 inhibitors
US11891403B2 (en) * 2020-06-29 2024-02-06 Boehringer Ingelheim International Gmbh Tetrazole derivatives as TRPA1 inhibitors
FR3114235A1 (fr) 2020-09-18 2022-03-25 Université Grenoble Alpes Inhibition du canal trpa1 astrocytaire comme nouvelle cible therapeutique neuroprotectrice dans les phases prodromales de la maladie d’alzheimer
CN112794860B (zh) * 2021-03-24 2021-06-29 上海肇钰医药科技有限公司 噁唑嘧啶酮酰胺类化合物或其可药用盐，制备方法及用途
TW202309015A (zh) * 2021-04-14 2023-03-01 德商百靈佳殷格翰國際股份有限公司 作為trpa1抑制劑之尿嘧啶衍生物
TW202309035A (zh) * 2021-04-14 2023-03-01 德商百靈佳殷格翰國際股份有限公司 作為TRPA1抑制劑之咪唑并[4,5-d]噠嗪酮基衍生物
IT202100015098A1 (it) 2021-06-09 2022-12-09 Flonext S R L Composto antagonista del canale trpa1 per uso in patologie degenerative della retina
CN118206482B (zh) * 2024-03-05 2025-04-25 山东京博生物科技有限公司 一种4-三氟甲基烟酰胺的合成方法

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2010522723A (ja) 2007-03-29 2010-07-08 ノバルティス アーゲー 増殖性疾患の処置のための３−イミダゾリル−インドール
WO2011114184A1 (en) 2010-03-15 2011-09-22 Glenmark Pharmaceuticals S.A. Amides of heterocyclic compounds as trpa1 inhibitors
WO2017060488A1 (en) 2015-10-09 2017-04-13 Almirall, S.A. New trpa1 antagonists

Family Cites Families (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3773919A (en) 1969-10-23 1973-11-20 Du Pont Polylactide-drug mixtures
CH583213A5 (enExample) * 1973-05-21 1976-12-31 Ciba Geigy Ag
US4485045A (en) 1981-07-06 1984-11-27 Research Corporation Synthetic phosphatidyl cholines useful in forming liposomes
EP0102324A3 (de) 1982-07-29 1984-11-07 Ciba-Geigy Ag Lipide und Tenside in wässriger Phase
US4544545A (en) 1983-06-20 1985-10-01 Trustees University Of Massachusetts Liposomes containing modified cholesterol for organ targeting
HUT35524A (en) 1983-08-02 1985-07-29 Hoechst Ag Process for preparing pharmaceutical compositions containing regulatory /regulative/ peptides providing for the retarded release of the active substance
US4500653A (en) * 1983-09-14 1985-02-19 Mobay Chemical Corporation Blowing agents for thermoplastic compositions
US5004697A (en) 1987-08-17 1991-04-02 Univ. Of Ca Cationized antibodies for delivery through the blood-brain barrier
US5112596A (en) 1990-04-23 1992-05-12 Alkermes, Inc. Method for increasing blood-brain barrier permeability by administering a bradykinin agonist of blood-brain barrier permeability
US5268164A (en) 1990-04-23 1993-12-07 Alkermes, Inc. Increasing blood-brain barrier permeability with permeabilizer peptides
WO1994002178A1 (en) 1992-07-27 1994-02-03 The Government Of The United States Of America As Represented By The Secretary Of The Department Of Health And Human Services Targeting of liposomes to the blood-brain barrier
US6514221B2 (en) 2000-07-27 2003-02-04 Brigham And Women's Hospital, Inc. Blood-brain barrier opening
US20020065259A1 (en) 2000-08-30 2002-05-30 Schatzberg Alan F. Glucocorticoid blocking agents for increasing blood-brain barrier permeability
US7034036B2 (en) 2000-10-30 2006-04-25 Pain Therapeutics, Inc. Inhibitors of ABC drug transporters at the blood-brain barrier
DE10121982B4 (de) 2001-05-05 2008-01-24 Lts Lohmann Therapie-Systeme Ag Nanopartikel aus Protein mit gekoppeltem Apolipoprotein E zur Überwindung der Blut-Hirn-Schranke und Verfahren zu ihrer Herstellung
EP1554572B1 (en) 2001-07-25 2009-10-14 Raptor Pharmaceutical Inc. Compositions and methods for modulating blood-brain barrier transport
US20030162695A1 (en) 2002-02-27 2003-08-28 Schatzberg Alan F. Glucocorticoid blocking agents for increasing blood-brain barrier permeability
KR101186210B1 (ko) 2002-12-03 2012-10-08 블랜체트 록펠러 뉴로사이언시즈 인스티튜트 혈뇌장벽을 통과하는 물질 수송용 인공 저밀도 지단백질 운반체
EP1663239A4 (en) 2003-09-10 2008-07-23 Cedars Sinai Medical Center KALIUM CHANNEL-MEDIATED FEEDING OF MEDICINES BY THE BLOOD BRAIN BARRIER
WO2017064068A1 (en) 2015-10-14 2017-04-20 Almirall, S.A. New trpa1 antagonists

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2010522723A (ja) 2007-03-29 2010-07-08 ノバルティス アーゲー 増殖性疾患の処置のための３−イミダゾリル−インドール
WO2011114184A1 (en) 2010-03-15 2011-09-22 Glenmark Pharmaceuticals S.A. Amides of heterocyclic compounds as trpa1 inhibitors
WO2017060488A1 (en) 2015-10-09 2017-04-13 Almirall, S.A. New trpa1 antagonists

Non-Patent Citations (8)

* Cited by examiner, † Cited by third party
Title
CAS Registry No. 887037-04-9，File REGISTRY [online], STN International，Entered STN，2006年06月07日，3-[2-(4-Methoxyphenyl)ethyl]-5-(5-quinolinyl)-1,3,4-oxadiazol-2(3H)-one
CAS Registry No.1381342-13-7，File REGISTRY [online], STN International，Entered STN，2012年07月04日，3-(2-Pyridinylmethyl)-5-(5-quinolinyl)-1,3,4-oxadiazol-2(3H)-one
MONGE, A.，J. Heterocyclic Chem.，1984年，21(2)，397 - 400
MUSSER, John H.，J.Med.Chem.，1984年，27，121-125
PATEL, Syham Sunder，Org.Biomol.Chem.，2016年，14(24)，5683 - 5689，http://dx.doi.org/10.1039/C5OB02667A
PubChem CID: 3437423，Database PubChem [ONLINE]，2005年09月08日，https://pubchem.ncbi.nlm.nih.gov/compound/3437423，7-[[4-[(2-METHOXYPHENYL)METHYL]-5-OXO-1,3,4-OXADIAZOL-2-YL]METHYL]-1,3-DIMETHYLPURINE-2,6-DIONE
SCHENKEL, Laurie B.，J.Med.Chem.，2016年，59，2794-2809
SUGIMOTO, Osamu，Chem.Commun.，2014年，50(55)，7314 - 7317，http://dx.doi.org/10.1039/C4CC01971G

Also Published As

Publication number Publication date
WO2018096159A1 (en) 2018-05-31
EP3544979A1 (en) 2019-10-02
TW201831477A (zh) 2018-09-01
CN110225911A (zh) 2019-09-10
JP2019535761A (ja) 2019-12-12
CN110225911B (zh) 2022-04-05
US10913742B2 (en) 2021-02-09
US20190284189A1 (en) 2019-09-19
EP3544979B1 (en) 2021-08-04

Similar Documents

Publication Publication Date Title
JP7171567B2 (ja) 一過性受容体電位型チャネル阻害剤としてのオキサジアゾロン類
US12202824B2 (en) Oxadiazole transient receptor potential channel inhibitors
US10711004B2 (en) Oxadiazole transient receptor potential channel inhibitors
US10766878B2 (en) Sulfonylcycloalkyl carboxamide compounds
CA2798831A1 (en) Morpholine compounds as mineralocorticoid receptor antagonists
EP3487853A1 (en) Bicyclic proline compounds
EP3497093A1 (en) Sulfonyl pyridyl trp inhibitors
RU2818244C2 (ru) Ингибиторы каналов с транзиторным потенциалом на основе оксадиазолов
HK40009776B (zh) 恶二唑酮瞬时受体电位通道抑制剂
HK40009776A (en) Oxadiazolones as transient receptor potential channel inhibitors

Legal Events

Date Code Title Description
A529 Written submission of copy of amendment under article 34 pct

Free format text: JAPANESE INTERMEDIATE CODE: A529

Effective date: 20190522

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20201120

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20201120

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20211007

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20211026

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20220118

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20220510

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20220713

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20221004

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20221102

R150 Certificate of patent or registration of utility model

Ref document number: 7171567

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150