CN114981251A - 一种二苯并呋喃类衍生物组织蛋白酶k抑制剂及其制备方法和医药用途 - Google Patents
一种二苯并呋喃类衍生物组织蛋白酶k抑制剂及其制备方法和医药用途 Download PDFInfo
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- 229940079488 strontium ranelate Drugs 0.000 description 1
- KVJIIORUFXGTFN-UHFFFAOYSA-L strontium;5-[bis(carboxymethyl)amino]-3-(carboxymethyl)-4-cyanothiophene-2-carboxylate Chemical compound [Sr+2].OC(=O)CN(CC(O)=O)C=1SC(C([O-])=O)=C(CC(O)=O)C=1C#N.OC(=O)CN(CC(O)=O)C=1SC(C([O-])=O)=C(CC(O)=O)C=1C#N KVJIIORUFXGTFN-UHFFFAOYSA-L 0.000 description 1
- 150000003456 sulfonamides Chemical class 0.000 description 1
- 239000011593 sulfur Substances 0.000 description 1
- 125000004434 sulfur atom Chemical group 0.000 description 1
- 239000000375 suspending agent Substances 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- FCMLWBBLOASUSO-UHFFFAOYSA-N tert-butyl 3-oxopiperazine-1-carboxylate Chemical compound CC(C)(C)OC(=O)N1CCNC(=O)C1 FCMLWBBLOASUSO-UHFFFAOYSA-N 0.000 description 1
- NKFZWJFQHSGCNX-NSHDSACASA-N tert-butyl n-[(2s)-1-[(1-cyanocyclopropyl)amino]-4-methyl-1-oxopentan-2-yl]carbamate Chemical compound CC(C)(C)OC(=O)N[C@@H](CC(C)C)C(=O)NC1(C#N)CC1 NKFZWJFQHSGCNX-NSHDSACASA-N 0.000 description 1
- 150000005621 tetraalkylammonium salts Chemical class 0.000 description 1
- CZDYPVPMEAXLPK-UHFFFAOYSA-N tetramethylsilane Chemical group C[Si](C)(C)C CZDYPVPMEAXLPK-UHFFFAOYSA-N 0.000 description 1
- 229940124597 therapeutic agent Drugs 0.000 description 1
- 230000008354 tissue degradation Effects 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
- 230000002588 toxic effect Effects 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 description 1
- WRECIMRULFAWHA-UHFFFAOYSA-N trimethyl borate Chemical compound COB(OC)OC WRECIMRULFAWHA-UHFFFAOYSA-N 0.000 description 1
- 229910052721 tungsten Inorganic materials 0.000 description 1
- 230000036269 ulceration Effects 0.000 description 1
- 210000002700 urine Anatomy 0.000 description 1
- 235000013311 vegetables Nutrition 0.000 description 1
- 235000019166 vitamin D Nutrition 0.000 description 1
- 239000011710 vitamin D Substances 0.000 description 1
- 150000003710 vitamin D derivatives Chemical class 0.000 description 1
- 229940046008 vitamin d Drugs 0.000 description 1
Classifications
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- 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
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
-
- 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
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
- A61K31/343—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
-
- 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
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
- C07D307/77—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
- C07D307/91—Dibenzofurans; Hydrogenated dibenzofurans
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Physical Education & Sports Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
提供了一系列的组织蛋白酶K的抑制剂，尤其提供了一种二苯并呋喃衍生物组织蛋白酶K的抑制剂，属于化学药物技术领域。还涉及包含这些化合物的药物组合物以及使用该化合物治疗骨关节炎等疾病的药物中的用途。
Description
PCT国内申请，说明书已公开。
Claims (15)
- PCT国内申请，权利要求书已公开。
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN202010069378 | 2020-01-21 | ||
| CN2020100693782 | 2020-01-21 | ||
| PCT/CN2021/072803 WO2021147882A1 (zh) | 2020-01-21 | 2021-01-20 | 一种二苯并呋喃类衍生物组织蛋白酶k抑制剂及其制备方法和医药用途 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN114981251A true CN114981251A (zh) | 2022-08-30 |
| CN114981251B CN114981251B (zh) | 2023-11-21 |
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| CN202180009972.5A Active CN114981251B (zh) | 2020-01-21 | 2021-01-20 | 一种二苯并呋喃类衍生物组织蛋白酶k抑制剂及其制备方法和医药用途 |
Country Status (2)
| Country | Link |
|---|---|
| CN (1) | CN114981251B (zh) |
| WO (1) | WO2021147882A1 (zh) |
Citations (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1998008802A1 (en) * | 1996-08-28 | 1998-03-05 | Smithkline Beecham Corporation | Inhibitors of cysteine protease |
| WO1998009934A1 (en) * | 1996-09-04 | 1998-03-12 | Warner-Lambert Company | Matrix metalloproteinase inhibitors and their therapeutic uses |
| CN1310716A (zh) * | 1998-07-30 | 2001-08-29 | 沃尼尔·朗伯公司 | 作为基质金属蛋白酶抑制剂的三环磺胺化合物及其衍生物 |
| US6294674B1 (en) * | 1996-09-04 | 2001-09-25 | Warner-Lambert Company | Dibenzofuran sulfonamide matrix metalloproteinase inhibitors |
| US20030229226A1 (en) * | 2000-04-06 | 2003-12-11 | Osamu Okamoto | Cathepsin cysteine protease inhibitors |
| US20070015797A1 (en) * | 1999-09-22 | 2007-01-18 | Cheng Peter T | Substituted acid derivatives useful as antidiabetic and antiobesity agents and method |
| CN102417480A (zh) * | 2006-06-01 | 2012-04-18 | 塞诺菲-安万特股份有限公司 | 作为蛋白酶抑制剂的螺环腈类 |
| CN105884752A (zh) * | 2015-02-13 | 2016-08-24 | 山东轩竹医药科技有限公司 | 并环类回旋酶和拓扑异构酶iv抑制剂 |
| CN106866502A (zh) * | 2015-12-10 | 2017-06-20 | 广东东阳光药业有限公司 | 组织蛋白酶k抑制剂及其用途 |
| US20180230138A1 (en) * | 2015-08-29 | 2018-08-16 | Sunshine Lake Pharma Co., Ltd. | Cathepsin k inhibitors and application thereof |
| WO2019218956A1 (zh) * | 2018-05-16 | 2019-11-21 | 深圳信立泰药业股份有限公司 | 作为用于治疗血小板聚集的蛋白酶激活受体4(par4)抑制剂的化合物 |
-
2021
- 2021-01-20 CN CN202180009972.5A patent/CN114981251B/zh active Active
- 2021-01-20 WO PCT/CN2021/072803 patent/WO2021147882A1/zh active Application Filing
Patent Citations (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1998008802A1 (en) * | 1996-08-28 | 1998-03-05 | Smithkline Beecham Corporation | Inhibitors of cysteine protease |
| WO1998009934A1 (en) * | 1996-09-04 | 1998-03-12 | Warner-Lambert Company | Matrix metalloproteinase inhibitors and their therapeutic uses |
| US6294674B1 (en) * | 1996-09-04 | 2001-09-25 | Warner-Lambert Company | Dibenzofuran sulfonamide matrix metalloproteinase inhibitors |
| CN1310716A (zh) * | 1998-07-30 | 2001-08-29 | 沃尼尔·朗伯公司 | 作为基质金属蛋白酶抑制剂的三环磺胺化合物及其衍生物 |
| US20070015797A1 (en) * | 1999-09-22 | 2007-01-18 | Cheng Peter T | Substituted acid derivatives useful as antidiabetic and antiobesity agents and method |
| US20030229226A1 (en) * | 2000-04-06 | 2003-12-11 | Osamu Okamoto | Cathepsin cysteine protease inhibitors |
| CN102417480A (zh) * | 2006-06-01 | 2012-04-18 | 塞诺菲-安万特股份有限公司 | 作为蛋白酶抑制剂的螺环腈类 |
| CN105884752A (zh) * | 2015-02-13 | 2016-08-24 | 山东轩竹医药科技有限公司 | 并环类回旋酶和拓扑异构酶iv抑制剂 |
| US20180230138A1 (en) * | 2015-08-29 | 2018-08-16 | Sunshine Lake Pharma Co., Ltd. | Cathepsin k inhibitors and application thereof |
| CN106866502A (zh) * | 2015-12-10 | 2017-06-20 | 广东东阳光药业有限公司 | 组织蛋白酶k抑制剂及其用途 |
| WO2019218956A1 (zh) * | 2018-05-16 | 2019-11-21 | 深圳信立泰药业股份有限公司 | 作为用于治疗血小板聚集的蛋白酶激活受体4(par4)抑制剂的化合物 |
Non-Patent Citations (4)
| Title |
|---|
| 任玉杰，等: "2-咪唑烷酮衍生物的合成研究进展", 上海应用技术学院学报(自然科学版), vol. 12, no. 06, pages 112 - 119 * |
| 朱康乐，等: "蛋白质精氨酸甲基转移酶5抑制剂的设计、合成及活性评价", 药学学报, vol. 11, no. 08, pages 112 - 118 * |
| 赵成英，等: "2010～2013之海洋微生物新天然产物", 有机化学, vol. 25, no. 06, pages 15 - 18 * |
| 马晓东，等: "新型咪唑酮并吡啶类化合物的合成和体外抗肿瘤活性", 中国新药杂志, vol. 01, no. 20, pages 566 - 572 * |
Also Published As
| Publication number | Publication date |
|---|---|
| WO2021147882A1 (zh) | 2021-07-29 |
| CN114981251B (zh) | 2023-11-21 |
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