JP2021530470A - カテプシンc阻害剤 - Google Patents
カテプシンc阻害剤 Download PDFInfo
- Publication number
- JP2021530470A JP2021530470A JP2021500105A JP2021500105A JP2021530470A JP 2021530470 A JP2021530470 A JP 2021530470A JP 2021500105 A JP2021500105 A JP 2021500105A JP 2021500105 A JP2021500105 A JP 2021500105A JP 2021530470 A JP2021530470 A JP 2021530470A
- Authority
- JP
- Japan
- Prior art keywords
- compound
- phenyl
- substituted
- cathepsin
- amino
- 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.)
- Pending
Links
- NVVMUQZCIADBFK-UHFFFAOYSA-N Cc(ccc(Oc(nc(cc1)Nc(c(OC)c2)ccc2N2CCN(C)CC2)c1N(CCC1)CC1O)c1)c1NC(C=C)=O Chemical compound Cc(ccc(Oc(nc(cc1)Nc(c(OC)c2)ccc2N2CCN(C)CC2)c1N(CCC1)CC1O)c1)c1NC(C=C)=O NVVMUQZCIADBFK-UHFFFAOYSA-N 0.000 description 2
- LYEVWGIIXUNTKM-UHFFFAOYSA-N CN(CC1)CCN1c(cc1OC)ccc1Nc(cc1)nc(Oc2cc(N)ccc2)c1C#C Chemical compound CN(CC1)CCN1c(cc1OC)ccc1Nc(cc1)nc(Oc2cc(N)ccc2)c1C#C LYEVWGIIXUNTKM-UHFFFAOYSA-N 0.000 description 1
- KOYFMYZXEWYTIQ-UHFFFAOYSA-N CN(CC1)CCN1c(cc1OC)ccc1Nc(cc1)nc(Oc2cccc([N+]([O-])=O)c2)c1Cl Chemical compound CN(CC1)CCN1c(cc1OC)ccc1Nc(cc1)nc(Oc2cccc([N+]([O-])=O)c2)c1Cl KOYFMYZXEWYTIQ-UHFFFAOYSA-N 0.000 description 1
- BUXDVRKYYXZOPJ-UHFFFAOYSA-N Cc(c(NC(C=C)=O)c1)ccc1Oc(nc(cc1)Nc(nc2)ccc2N(CC2)CCC2N(C)C)c1N1CCCCC1 Chemical compound Cc(c(NC(C=C)=O)c1)ccc1Oc(nc(cc1)Nc(nc2)ccc2N(CC2)CCC2N(C)C)c1N1CCCCC1 BUXDVRKYYXZOPJ-UHFFFAOYSA-N 0.000 description 1
- PONPXMDPXUKJAO-UHFFFAOYSA-N Cc(ccc(Oc(nc(cc1)Nc(c(OC)c2)ccc2N2CCN(C)CC2)c1N(CC1)CC1O)c1)c1NC(C=C)=O Chemical compound Cc(ccc(Oc(nc(cc1)Nc(c(OC)c2)ccc2N2CCN(C)CC2)c1N(CC1)CC1O)c1)c1NC(C=C)=O PONPXMDPXUKJAO-UHFFFAOYSA-N 0.000 description 1
- BQOPZUJZKFPSSY-UHFFFAOYSA-N Cc(ccc(Oc(nc(cc1)Nc(c(OC)c2)ccc2N2CCNCC2)c1N1CCCCC1)c1)c1NC(C=C)=O Chemical compound Cc(ccc(Oc(nc(cc1)Nc(c(OC)c2)ccc2N2CCNCC2)c1N1CCCCC1)c1)c1NC(C=C)=O BQOPZUJZKFPSSY-UHFFFAOYSA-N 0.000 description 1
- PTEDRHAOUDENOU-UHFFFAOYSA-N Cc(ccc(Oc(nc(cc1)Nc2ccc(N3CCN(C)CC3)nc2OC)c1N1CCCCC1)c1)c1NC(C=C)=O Chemical compound Cc(ccc(Oc(nc(cc1)Nc2ccc(N3CCN(C)CC3)nc2OC)c1N1CCCCC1)c1)c1NC(C=C)=O PTEDRHAOUDENOU-UHFFFAOYSA-N 0.000 description 1
- ZJSUTKAHANAQQG-UHFFFAOYSA-N [O-][N+](c1cccc(Nc(nc(cc2)Cl)c2Cl)c1)=O Chemical compound [O-][N+](c1cccc(Nc(nc(cc2)Cl)c2Cl)c1)=O ZJSUTKAHANAQQG-UHFFFAOYSA-N 0.000 description 1
Images
Classifications
-
- 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
-
- 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
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
- C07D213/72—Nitrogen atoms
- C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D213/84—Nitriles
- C07D213/85—Nitriles in position 3
-
- 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
- C07D401/02—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
- C07D401/12—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 linked by a chain containing hetero atoms as chain links
-
- 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
- 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
- C07D405/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- 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
- C07D471/08—Bridged systems
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Immunology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Transplantation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyridine Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2018093886 | 2018-06-30 | ||
| CNPCT/CN2018/093886 | 2018-06-30 | ||
| PCT/CN2019/092488 WO2020001392A1 (en) | 2018-06-30 | 2019-06-24 | Cathepsin c inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2021530470A true JP2021530470A (ja) | 2021-11-11 |
| JPWO2020001392A5 JPWO2020001392A5 (https=) | 2022-07-01 |
| JP2021530470A5 JP2021530470A5 (https=) | 2022-07-01 |
Family
ID=68986057
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021500105A Pending JP2021530470A (ja) | 2018-06-30 | 2019-06-24 | カテプシンc阻害剤 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US20210114983A1 (https=) |
| EP (1) | EP3814324A4 (https=) |
| JP (1) | JP2021530470A (https=) |
| CN (1) | CN112601742A (https=) |
| WO (1) | WO2020001392A1 (https=) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2023243601A1 (ja) * | 2022-06-13 | 2023-12-21 | モジュラス株式会社 | アザシクロアルキルカルボニル環状アミン化合物 |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US12030875B2 (en) | 2018-09-07 | 2024-07-09 | PIC Therapeutics, Inc. | EIF4E inhibitors and uses thereof |
| AU2021230289A1 (en) | 2020-03-03 | 2022-09-29 | PIC Therapeutics, Inc. | eIF4E inhibitors and uses thereof |
| CN112920124B (zh) * | 2021-01-29 | 2024-03-01 | 安徽医科大学 | 一种嘧啶-2,4-二胺类化合物及其制备方法与应用 |
| US12157732B2 (en) | 2021-08-25 | 2024-12-03 | PIC Therapeutics, Inc. | eIF4E inhibitors and uses thereof |
| JP2024534127A (ja) | 2021-08-25 | 2024-09-18 | ピク セラピューティクス, インコーポレイテッド | eIF4E阻害剤及びその使用 |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2012112733A1 (en) * | 2011-02-16 | 2012-08-23 | Glaxosmithkline Llc | Cathepsin c inhibitors |
| JP2012526113A (ja) * | 2009-05-05 | 2012-10-25 | ダナ ファーバー キャンサー インスティテュート インコーポレイテッド | Egfr阻害剤及び疾患の治療方法 |
| CN103664878A (zh) * | 2012-09-12 | 2014-03-26 | 山东亨利医药科技有限责任公司 | 杂芳环及其衍生物类酪氨酸激酶抑制剂 |
| US20170112833A1 (en) * | 2014-04-18 | 2017-04-27 | Xuanzhu Pharma Co., Ltd. | Tyrosine Kinase Inhibitor And Uses Thereof |
| JP2018515597A (ja) * | 2015-04-07 | 2018-06-14 | イーエルエイ ファーマ リミテッドEla Pharma Ltd | カテプシンcおよび/またはcela1および/またはcela3aおよび/またはそれらに構造的に関連する酵素を特異的に標的とする細胞および/または組織壊死の処置および/または防止のための組成物 |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3019491A4 (en) * | 2013-07-09 | 2016-12-21 | Dana Farber Cancer Inst Inc | KINASEHEMMER FOR THE TREATMENT OF DISEASES |
| BR112016008632A8 (pt) * | 2013-10-21 | 2020-03-17 | Merck Patent Gmbh | compostos de heteroarila como inibidores de btk, seus usos, e composição farmacêutica |
| CN108137544B (zh) * | 2015-12-10 | 2022-01-04 | 深圳市塔吉瑞生物医药有限公司 | 用于抑制蛋白酪氨酸激酶活性的氨基嘧啶类化合物 |
-
2019
- 2019-06-24 JP JP2021500105A patent/JP2021530470A/ja active Pending
- 2019-06-24 EP EP19826742.9A patent/EP3814324A4/en not_active Withdrawn
- 2019-06-24 WO PCT/CN2019/092488 patent/WO2020001392A1/en not_active Ceased
- 2019-06-24 CN CN201980055883.7A patent/CN112601742A/zh active Pending
-
2020
- 2020-12-30 US US17/137,458 patent/US20210114983A1/en not_active Abandoned
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2012526113A (ja) * | 2009-05-05 | 2012-10-25 | ダナ ファーバー キャンサー インスティテュート インコーポレイテッド | Egfr阻害剤及び疾患の治療方法 |
| WO2012112733A1 (en) * | 2011-02-16 | 2012-08-23 | Glaxosmithkline Llc | Cathepsin c inhibitors |
| CN103664878A (zh) * | 2012-09-12 | 2014-03-26 | 山东亨利医药科技有限责任公司 | 杂芳环及其衍生物类酪氨酸激酶抑制剂 |
| US20170112833A1 (en) * | 2014-04-18 | 2017-04-27 | Xuanzhu Pharma Co., Ltd. | Tyrosine Kinase Inhibitor And Uses Thereof |
| JP2018515597A (ja) * | 2015-04-07 | 2018-06-14 | イーエルエイ ファーマ リミテッドEla Pharma Ltd | カテプシンcおよび/またはcela1および/またはcela3aおよび/またはそれらに構造的に関連する酵素を特異的に標的とする細胞および/または組織壊死の処置および/または防止のための組成物 |
Non-Patent Citations (1)
| Title |
|---|
| CELL CHEMICAL BIOLOGY, vol. 24, JPN6023031064, 2017, pages 1388 - 1400, ISSN: 0005275235 * |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2023243601A1 (ja) * | 2022-06-13 | 2023-12-21 | モジュラス株式会社 | アザシクロアルキルカルボニル環状アミン化合物 |
| US12522593B2 (en) | 2022-06-13 | 2026-01-13 | Alivexis, Inc. | Azacycloalkyl carbonyl cyclic amine compound |
Also Published As
| Publication number | Publication date |
|---|---|
| CN112601742A (zh) | 2021-04-02 |
| WO2020001392A1 (en) | 2020-01-02 |
| EP3814324A1 (en) | 2021-05-05 |
| EP3814324A4 (en) | 2021-08-25 |
| US20210114983A1 (en) | 2021-04-22 |
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