CN113272297B - 作为h4拮抗剂化合物的吡唑衍生物 - Google Patents
作为h4拮抗剂化合物的吡唑衍生物 Download PDFInfo
- Publication number
- CN113272297B CN113272297B CN201980084053.7A CN201980084053A CN113272297B CN 113272297 B CN113272297 B CN 113272297B CN 201980084053 A CN201980084053 A CN 201980084053A CN 113272297 B CN113272297 B CN 113272297B
- Authority
- CN
- China
- Prior art keywords
- mmol
- methyl
- compound
- acid
- pyrazol
- 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.)
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Classifications
-
- 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
-
- 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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further 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
- 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
- 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
- A61P17/04—Antipruritics
-
- 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
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
- C07D405/14—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 three or more hetero rings
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pulmonology (AREA)
- Rheumatology (AREA)
- Dermatology (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB1817047.2A GB201817047D0 (en) | 2018-10-19 | 2018-10-19 | H4 antagonist compounds |
| GB1817047.2 | 2018-10-19 | ||
| PCT/GB2019/052997 WO2020079457A1 (en) | 2018-10-19 | 2019-10-21 | Pyrazole derivatives as h4 antagonist compounds |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN113272297A CN113272297A (zh) | 2021-08-17 |
| CN113272297B true CN113272297B (zh) | 2024-03-19 |
Family
ID=64453795
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201980084053.7A Active CN113272297B (zh) | 2018-10-19 | 2019-10-21 | 作为h4拮抗剂化合物的吡唑衍生物 |
Country Status (13)
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB202005858D0 (en) * | 2020-04-22 | 2020-06-03 | Heptares Therapeutics Ltd | H4 Antagonist compounds |
| GB202019667D0 (en) * | 2020-12-14 | 2021-01-27 | Heptares Therapeutics Ltd | H4 antagonist comnpounds |
| KR102655210B1 (ko) * | 2021-03-26 | 2024-04-08 | 주식회사 스탠다임 | 아데노신 a2a 수용체 길항제 및 이의 용도 |
| WO2022232259A1 (en) * | 2021-04-28 | 2022-11-03 | Cornell University | Soluble adenylyl cyclase (sac) inhibitors and uses thereof |
| EP4421067A4 (en) * | 2021-10-19 | 2026-01-14 | Unimatec Co Ltd | PYRAZOLE COMPOUND CONTAINING FLUORIDE AND ITS PRODUCTION PROCESS |
| KR102621694B1 (ko) * | 2022-09-15 | 2024-01-08 | 주식회사 스탠다임 | 아데노신 a2a 수용체 길항제 및 이의 용도 |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1103551A1 (en) * | 1998-07-24 | 2001-05-30 | Daiichi Pharmaceutical Co., Ltd. | Pyrazole derivatives and salts thereof |
| WO2005054239A1 (en) * | 2003-12-05 | 2005-06-16 | Bayer Healthcare Ag | 2-aminopyrimidine derivatives |
| CN101341134A (zh) * | 2005-12-20 | 2009-01-07 | 辉瑞股份有限公司 | 嘧啶衍生物 |
| WO2010059658A1 (en) * | 2008-11-20 | 2010-05-27 | Glaxosmithkline Llc | Chemical compounds |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2000169475A (ja) | 1998-07-24 | 2000-06-20 | Dai Ichi Seiyaku Co Ltd | ピラゾ―ル誘導体およびその塩 |
| EP2066645A2 (en) | 2006-09-12 | 2009-06-10 | UCB Pharma S.A. | 2 amino-pyrimidine derivatives as h4 receptor antagonists, processes for preparing them and their use in pharmaceutical compositions |
| US7985745B2 (en) | 2006-10-02 | 2011-07-26 | Abbott Laboratories | Method for pain treatment |
| CL2008000467A1 (es) | 2007-02-14 | 2008-08-22 | Janssen Pharmaceutica Nv | Compuestos derivados de 2-aminopirimidina, moduladores del receptor histamina h4; su procedimiento de preparacion; composicion farmaceutica que comprende a dichos compuestos; y su uso para tratar un trastorno inflamatorio seleccionado de alegia, asma |
| WO2009068512A1 (en) | 2007-11-30 | 2009-06-04 | Palau Pharma, S. A. | 2 -amino-pyrimidine derivatives as histamine h4 antagonists |
| PE20091524A1 (es) | 2007-12-19 | 2009-09-25 | Palau Pharma Sa | Derivados de 2-aminopirimidina |
| RU2489430C2 (ru) | 2007-12-21 | 2013-08-10 | Палау Фарма, С.А. | Производные 4-аминопиримидина |
| TW201035078A (en) | 2009-03-20 | 2010-10-01 | Incyte Corp | Substituted heterocyclic compounds |
| WO2011059839A1 (en) | 2009-10-29 | 2011-05-19 | Sirtris Pharmaceuticals, Inc. | Bicyclic pyridines and analogs as sirtuin modulators |
| JP5781537B2 (ja) | 2009-12-23 | 2015-09-24 | メディシス ファーマシューティカル コーポレイション | ヒスタミンｈ４受容体アンタゴニストとしてのアミノアルキルピリミジン誘導体 |
| AR093512A1 (es) | 2012-11-16 | 2015-06-10 | Merck Patent Gmbh | Derivados heterociclicos como moduladores de la actividad de cinasas |
| JP2019525929A (ja) | 2016-07-28 | 2019-09-12 | メイヨ・ファウンデーション・フォー・メディカル・エデュケーション・アンド・リサーチ | Ｐａｒｋｉｎ酵素機能の小分子活性化因子 |
-
2018
- 2018-10-19 GB GBGB1817047.2A patent/GB201817047D0/en not_active Ceased
-
2019
- 2019-10-21 WO PCT/GB2019/052997 patent/WO2020079457A1/en not_active Ceased
- 2019-10-21 MX MX2021004280A patent/MX2021004280A/es unknown
- 2019-10-21 ES ES19794235T patent/ES3058587T3/es active Active
- 2019-10-21 EP EP19794235.2A patent/EP3867248B1/en active Active
- 2019-10-21 JP JP2021521390A patent/JP7532353B2/ja active Active
- 2019-10-21 CA CA3116628A patent/CA3116628A1/en active Pending
- 2019-10-21 US US17/285,776 patent/US12234227B2/en active Active
- 2019-10-21 BR BR112021007372-8A patent/BR112021007372A2/pt unknown
- 2019-10-21 AU AU2019360428A patent/AU2019360428B2/en active Active
- 2019-10-21 KR KR1020217014805A patent/KR102873380B1/ko active Active
- 2019-10-21 CN CN201980084053.7A patent/CN113272297B/zh active Active
- 2019-10-21 SG SG11202103133QA patent/SG11202103133QA/en unknown
-
2024
- 2024-09-05 US US18/826,098 patent/US20250115587A1/en active Pending
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1103551A1 (en) * | 1998-07-24 | 2001-05-30 | Daiichi Pharmaceutical Co., Ltd. | Pyrazole derivatives and salts thereof |
| WO2005054239A1 (en) * | 2003-12-05 | 2005-06-16 | Bayer Healthcare Ag | 2-aminopyrimidine derivatives |
| CN101341134A (zh) * | 2005-12-20 | 2009-01-07 | 辉瑞股份有限公司 | 嘧啶衍生物 |
| WO2010059658A1 (en) * | 2008-11-20 | 2010-05-27 | Glaxosmithkline Llc | Chemical compounds |
Non-Patent Citations (2)
| Title |
|---|
| Structure-Activity Studies on a Series of a 2-Aminopyrimidine-Containing Histamine H4 Receptor Ligands;Robert J. Altenbach,et al;《Journal of Medicinal Chemistry》;第51卷(第20期);第6571-6580页 * |
| Structure-Based Design of Potent and Selective 3-Phosphoinositide-Dependent Kinase-1 (PDK1) Inhibitors;Jesus R. Medina,et al;《Journal of Medicinal Chemistry》;第54卷;第1871-1895页 * |
Also Published As
| Publication number | Publication date |
|---|---|
| JP2022507013A (ja) | 2022-01-18 |
| EP3867248A1 (en) | 2021-08-25 |
| US20210300906A1 (en) | 2021-09-30 |
| WO2020079457A1 (en) | 2020-04-23 |
| KR20210079318A (ko) | 2021-06-29 |
| CA3116628A1 (en) | 2020-04-23 |
| BR112021007372A2 (pt) | 2021-07-20 |
| KR102873380B1 (ko) | 2025-10-23 |
| GB201817047D0 (en) | 2018-12-05 |
| SG11202103133QA (en) | 2021-05-28 |
| US12234227B2 (en) | 2025-02-25 |
| AU2019360428A1 (en) | 2021-04-29 |
| MX2021004280A (es) | 2021-05-31 |
| ES3058587T3 (en) | 2026-03-11 |
| AU2019360428B2 (en) | 2024-05-09 |
| CN113272297A (zh) | 2021-08-17 |
| EP3867248C0 (en) | 2025-12-10 |
| US20250115587A1 (en) | 2025-04-10 |
| JP7532353B2 (ja) | 2024-08-13 |
| EP3867248B1 (en) | 2025-12-10 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PB01 | Publication | ||
| PB01 | Publication | ||
| SE01 | Entry into force of request for substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| GR01 | Patent grant | ||
| GR01 | Patent grant | ||
| CP03 | Change of name, title or address | ||
| CP03 | Change of name, title or address |
Address after: Cambridge, County of Cambridge, UK Patentee after: Nexla Pharmaceuticals UK Ltd. Country or region after: Britain Address before: Cambridge, County of Cambridge, UK Patentee before: Heptares Therapeutics Ltd. Country or region before: Britain |