JP2020510061A - ピラゾロクロロフェニル化合物、組成物及びその使用方法 - Google Patents
ピラゾロクロロフェニル化合物、組成物及びその使用方法 Download PDFInfo
- Publication number
- JP2020510061A JP2020510061A JP2019550583A JP2019550583A JP2020510061A JP 2020510061 A JP2020510061 A JP 2020510061A JP 2019550583 A JP2019550583 A JP 2019550583A JP 2019550583 A JP2019550583 A JP 2019550583A JP 2020510061 A JP2020510061 A JP 2020510061A
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- compound
- group
- pharmaceutically acceptable
- membered
- 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.)
- Ceased
Links
- 0 CN(C)C(CN1CCN(C*)CC1)=O Chemical compound CN(C)C(CN1CCN(C*)CC1)=O 0.000 description 12
- NMILGIZTAZXMTM-UHFFFAOYSA-N CCCN1CCOCC1 Chemical compound CCCN1CCOCC1 NMILGIZTAZXMTM-UHFFFAOYSA-N 0.000 description 2
- YNAVUWVOSKDBBP-UHFFFAOYSA-O C1[NH2+]CCOC1 Chemical compound C1[NH2+]CCOC1 YNAVUWVOSKDBBP-UHFFFAOYSA-O 0.000 description 1
- ADZPDQCVDKYSRC-UHFFFAOYSA-N CC1(CNN)CC1 Chemical compound CC1(CNN)CC1 ADZPDQCVDKYSRC-UHFFFAOYSA-N 0.000 description 1
- NEJYYNCKEGEHOY-UHFFFAOYSA-N CC1C=NCC2NC=NC12 Chemical compound CC1C=NCC2NC=NC12 NEJYYNCKEGEHOY-UHFFFAOYSA-N 0.000 description 1
- AUPZGPPSZBJFBW-UHFFFAOYSA-N CCC(C1)C1[O](C)(C)CN Chemical compound CCC(C1)C1[O](C)(C)CN AUPZGPPSZBJFBW-UHFFFAOYSA-N 0.000 description 1
- BZAIDSKABHRTHH-UHFFFAOYSA-N CCN1CCN(CC(N(C)C)=O)CC1 Chemical compound CCN1CCN(CC(N(C)C)=O)CC1 BZAIDSKABHRTHH-UHFFFAOYSA-N 0.000 description 1
- AEOMLJVHGODKEW-UHFFFAOYSA-N CCc(cc(cc1)Cl)c1OC(F)F Chemical compound CCc(cc(cc1)Cl)c1OC(F)F AEOMLJVHGODKEW-UHFFFAOYSA-N 0.000 description 1
- ATINWPMQAWKACZ-UHFFFAOYSA-N CN(C1COC1)C(CC1)CCN1C(C[n](cc1NC(c2cnc3[n]2nccc3)=O)nc1-c(cc(cc1)Cl)c1OC(F)F)=O Chemical compound CN(C1COC1)C(CC1)CCN1C(C[n](cc1NC(c2cnc3[n]2nccc3)=O)nc1-c(cc(cc1)Cl)c1OC(F)F)=O ATINWPMQAWKACZ-UHFFFAOYSA-N 0.000 description 1
- SJRJJKPEHAURKC-UHFFFAOYSA-N CN1CCOCC1 Chemical compound CN1CCOCC1 SJRJJKPEHAURKC-UHFFFAOYSA-N 0.000 description 1
- KHPZORNIMRLKQF-UHFFFAOYSA-N CNCC1(CC1)C1N=C1 Chemical compound CNCC1(CC1)C1N=C1 KHPZORNIMRLKQF-UHFFFAOYSA-N 0.000 description 1
- LSROIKUOAAGJRN-UHFFFAOYSA-N C[N](C)(C)c1cncc2c1nc[s]2 Chemical compound C[N](C)(C)c1cncc2c1nc[s]2 LSROIKUOAAGJRN-UHFFFAOYSA-N 0.000 description 1
- BECYPEHQFUPGLR-UHFFFAOYSA-N Cc1cnc2[nH]ccc2n1 Chemical compound Cc1cnc2[nH]ccc2n1 BECYPEHQFUPGLR-UHFFFAOYSA-N 0.000 description 1
- SAKYJTGICSUFFG-UHFFFAOYSA-N Ic1c2ncccc2n[s]1 Chemical compound Ic1c2ncccc2n[s]1 SAKYJTGICSUFFG-UHFFFAOYSA-N 0.000 description 1
- DWTIXFHDZUJGOB-UHFFFAOYSA-N Ic1c[o]c2c1nccc2 Chemical compound Ic1c[o]c2c1nccc2 DWTIXFHDZUJGOB-UHFFFAOYSA-N 0.000 description 1
- DMYLRZUXZGLCPE-UHFFFAOYSA-N Ic1cncc2c1[nH]nc2 Chemical compound Ic1cncc2c1[nH]nc2 DMYLRZUXZGLCPE-UHFFFAOYSA-N 0.000 description 1
- MXAVOGVTZLDXRR-UHFFFAOYSA-N O=C(c1c[o]c2c1nccc2)Nc1c[nH]nc1-c(cc(cc1)Cl)c1OC(F)F Chemical compound O=C(c1c[o]c2c1nccc2)Nc1c[nH]nc1-c(cc(cc1)Cl)c1OC(F)F MXAVOGVTZLDXRR-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- 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
-
- 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
-
- 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
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
- C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
- C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
-
- 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)
- Pulmonology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2017076598 | 2017-03-14 | ||
| CNPCT/CN2017/076598 | 2017-03-14 | ||
| PCT/EP2018/056129 WO2018166993A2 (en) | 2017-03-14 | 2018-03-13 | Pyrazolochlorophenyl compounds, compositions and methods of use thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2020510061A true JP2020510061A (ja) | 2020-04-02 |
| JP2020510061A5 JP2020510061A5 (enExample) | 2021-04-22 |
Family
ID=61655767
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019550583A Ceased JP2020510061A (ja) | 2017-03-14 | 2018-03-13 | ピラゾロクロロフェニル化合物、組成物及びその使用方法 |
Country Status (5)
| Country | Link |
|---|---|
| US (2) | US20200002346A1 (enExample) |
| EP (1) | EP3596072B1 (enExample) |
| JP (1) | JP2020510061A (enExample) |
| CN (1) | CN110494434B (enExample) |
| WO (1) | WO2018166993A2 (enExample) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20200010390A (ko) | 2017-05-22 | 2020-01-30 | 에프. 호프만-라 로슈 아게 | 치료 화합물 및 조성물, 및 이의 사용 방법 |
| JP7657740B2 (ja) | 2019-06-18 | 2025-04-07 | エフ・ホフマン-ラ・ロシュ・アクチェンゲゼルシャフト | Jakキナーゼのピラゾロピリミジンスルホン阻害剤およびその使用 |
| TW202115069A (zh) | 2019-06-18 | 2021-04-16 | 瑞士商赫孚孟拉羅股份公司 | Jak激酶之經四唑取代之吡唑并嘧啶抑制劑及其用途 |
| WO2022256358A1 (en) * | 2021-06-03 | 2022-12-08 | Genentech, Inc. | Process for preparing medicaments |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2006070202A1 (en) * | 2004-12-30 | 2006-07-06 | Astex Therapeutics Limited | Pyrazole derivatives having kinase modulating activity |
| JP2007516194A (ja) * | 2003-07-03 | 2007-06-21 | アステックス、セラピューティックス、リミテッド | 医薬化合物 |
| JP2012532112A (ja) * | 2009-07-02 | 2012-12-13 | ジェネンテック, インコーポレイテッド | ピラゾロピリミジンjak阻害剤化合物及び方法 |
| WO2015177326A1 (en) * | 2014-05-23 | 2015-11-26 | F. Hoffmann-La Roche Ag | 5-chloro-2-difluoromethoxyphenyl pyrazolopyrimidine compounds which are jak inhibitors |
| JP2016535772A (ja) * | 2013-11-08 | 2016-11-17 | 武田薬品工業株式会社 | 自己免疫疾患治療のためのピラゾール |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU650953B2 (en) | 1991-03-21 | 1994-07-07 | Novartis Ag | Inhaler |
| US5543523A (en) | 1994-11-15 | 1996-08-06 | Regents Of The University Of Minnesota | Method and intermediates for the synthesis of korupensamines |
| WO1997002289A1 (en) | 1995-07-06 | 1997-01-23 | Zeneca Limited | Peptide inhibitors of fibronectine |
| US6248713B1 (en) | 1995-07-11 | 2001-06-19 | Biogen, Inc. | Cell adhesion inhibitors |
| YU25500A (sh) | 1999-05-11 | 2003-08-29 | Pfizer Products Inc. | Postupak za sintezu analoga nukleozida |
| GB0028383D0 (en) | 2000-11-21 | 2001-01-03 | Novartis Ag | Organic compounds |
| EP1241176A1 (en) | 2001-03-16 | 2002-09-18 | Pfizer Products Inc. | Purine derivatives for the treatment of ischemia |
| JP4486817B2 (ja) | 2001-12-20 | 2010-06-23 | バイエル・シェーリング・ファルマ・アクチェンゲゼルシャフト | 1,4−ジヒドロ−1,4−ジフェニルピリジン誘導体 |
| SE0302487D0 (sv) | 2003-09-18 | 2003-09-18 | Astrazeneca Ab | Novel compounds |
| GB0502258D0 (en) | 2005-02-03 | 2005-03-09 | Argenta Discovery Ltd | Compounds and their use |
| EP1968579A1 (en) * | 2005-12-30 | 2008-09-17 | Astex Therapeutics Limited | Pharmaceutical compounds |
| WO2008001101A2 (en) * | 2006-06-29 | 2008-01-03 | Astex Therapeutics Limited | Pharmaceutical combinations |
| JP5523829B2 (ja) * | 2006-06-29 | 2014-06-18 | アステックス、セラピューティックス、リミテッド | 複合薬剤 |
| US20100048557A1 (en) | 2008-06-20 | 2010-02-25 | Bing-Yan Zhu | Triazolopyridine JAK Inhibitor Compounds and Methods |
| JP5769199B2 (ja) * | 2008-10-31 | 2015-08-26 | ジェネンテック, インコーポレイテッド | ピラゾロピリミジンjak阻害剤化合物と方法 |
| US8575336B2 (en) | 2011-07-27 | 2013-11-05 | Pfizer Limited | Indazoles |
| EP3416967B1 (en) * | 2016-02-18 | 2022-02-09 | F. Hoffmann-La Roche AG | Therapeutic compounds, compositions and methods of use thereof |
-
2018
- 2018-03-13 WO PCT/EP2018/056129 patent/WO2018166993A2/en not_active Ceased
- 2018-03-13 EP EP18711294.1A patent/EP3596072B1/en active Active
- 2018-03-13 JP JP2019550583A patent/JP2020510061A/ja not_active Ceased
- 2018-03-13 CN CN201880017772.2A patent/CN110494434B/zh not_active Expired - Fee Related
-
2019
- 2019-09-05 US US16/561,447 patent/US20200002346A1/en not_active Abandoned
-
2021
- 2021-02-12 US US17/174,733 patent/US11649241B2/en active Active
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2007516194A (ja) * | 2003-07-03 | 2007-06-21 | アステックス、セラピューティックス、リミテッド | 医薬化合物 |
| WO2006070202A1 (en) * | 2004-12-30 | 2006-07-06 | Astex Therapeutics Limited | Pyrazole derivatives having kinase modulating activity |
| JP2012532112A (ja) * | 2009-07-02 | 2012-12-13 | ジェネンテック, インコーポレイテッド | ピラゾロピリミジンjak阻害剤化合物及び方法 |
| JP2016535772A (ja) * | 2013-11-08 | 2016-11-17 | 武田薬品工業株式会社 | 自己免疫疾患治療のためのピラゾール |
| WO2015177326A1 (en) * | 2014-05-23 | 2015-11-26 | F. Hoffmann-La Roche Ag | 5-chloro-2-difluoromethoxyphenyl pyrazolopyrimidine compounds which are jak inhibitors |
Non-Patent Citations (4)
| Title |
|---|
| "RN 1348439-69-9, 1348366-33-5, 1348342-66-4, 1348042-57-8, 1347970-24-4, 1347873-72-6 REGISTRY", DATABASE REGISTRY [ONLINE] RETRIEVED FROM STN, JPN7022000927, 4 December 2011 (2011-12-04), ISSN: 0004965067 * |
| "RN 1349237-47-3, 1348949-82-5 REGISTRY", DATABASE REGISTRY [ONLINE] RETRIEVED FROM STN, JPN7022000928, 5 December 2011 (2011-12-05), ISSN: 0004965066 * |
| "RN 1825504-02-6 REGISTRY", DATABASE REGISTRY [ONLINE] RETRIEVED FROM STN, JPN7022000929, 9 December 2015 (2015-12-09), ISSN: 0004965065 * |
| "RN 1935725-26-0 REGISTRY", DATABASE REGISTRY [ONLINE] RETRIEVED FROM STN, JPN7022000930, 20 June 2016 (2016-06-20), ISSN: 0004965064 * |
Also Published As
| Publication number | Publication date |
|---|---|
| WO2018166993A2 (en) | 2018-09-20 |
| US20200002346A1 (en) | 2020-01-02 |
| WO2018166993A3 (en) | 2019-02-07 |
| CN110494434B (zh) | 2022-05-24 |
| US20210179626A1 (en) | 2021-06-17 |
| US11649241B2 (en) | 2023-05-16 |
| EP3596072B1 (en) | 2022-06-22 |
| CN110494434A (zh) | 2019-11-22 |
| EP3596072A2 (en) | 2020-01-22 |
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