CN112028825B - 酪氨酸激酶抑制剂及包含该酪氨酸激酶抑制剂的药物组合物 - Google Patents
酪氨酸激酶抑制剂及包含该酪氨酸激酶抑制剂的药物组合物 Download PDFInfo
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- CN112028825B CN112028825B CN202011033493.0A CN202011033493A CN112028825B CN 112028825 B CN112028825 B CN 112028825B CN 202011033493 A CN202011033493 A CN 202011033493A CN 112028825 B CN112028825 B CN 112028825B
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms 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
- C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
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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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
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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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- 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
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- 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
- C07D401/10—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 carbon chain containing aromatic rings
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- 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
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- 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
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- 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
- C07D405/12—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 linked by a chain containing hetero atoms as chain links
-
- 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
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
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- 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
- 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
- C07D491/056—Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
-
- 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
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
- C07F9/576—Six-membered rings
- C07F9/60—Quinoline or hydrogenated quinoline ring systems
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Quinoline Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
- Pyridine Compounds (AREA)
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510161674 | 2015-04-07 | ||
| CN2015101616744 | 2015-04-07 | ||
| CN201680019729.0A CN107683279B (zh) | 2015-04-07 | 2016-04-07 | 酪氨酸激酶抑制剂及包含该酪氨酸激酶抑制剂的药物组合物 |
| PCT/CN2016/078703 WO2016161952A1 (zh) | 2015-04-07 | 2016-04-07 | 酪氨酸激酶抑制剂及包含该酪氨酸激酶抑制剂的药物组合物 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201680019729.0A Division CN107683279B (zh) | 2015-04-07 | 2016-04-07 | 酪氨酸激酶抑制剂及包含该酪氨酸激酶抑制剂的药物组合物 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN112028825A CN112028825A (zh) | 2020-12-04 |
| CN112028825B true CN112028825B (zh) | 2025-03-14 |
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Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201680019729.0A Active CN107683279B (zh) | 2015-04-07 | 2016-04-07 | 酪氨酸激酶抑制剂及包含该酪氨酸激酶抑制剂的药物组合物 |
| CN202011033493.0A Active CN112028825B (zh) | 2015-04-07 | 2016-04-07 | 酪氨酸激酶抑制剂及包含该酪氨酸激酶抑制剂的药物组合物 |
| CN201610211659.0A Active CN106046007B (zh) | 2015-04-07 | 2016-04-07 | 酪氨酸激酶抑制剂及包含该酪氨酸激酶抑制剂的药物组合物 |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201680019729.0A Active CN107683279B (zh) | 2015-04-07 | 2016-04-07 | 酪氨酸激酶抑制剂及包含该酪氨酸激酶抑制剂的药物组合物 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201610211659.0A Active CN106046007B (zh) | 2015-04-07 | 2016-04-07 | 酪氨酸激酶抑制剂及包含该酪氨酸激酶抑制剂的药物组合物 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US10654808B2 (enExample) |
| EP (1) | EP3293177B1 (enExample) |
| JP (2) | JP6617155B6 (enExample) |
| CN (3) | CN107683279B (enExample) |
| WO (1) | WO2016161952A1 (enExample) |
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| AU2016378154B2 (en) * | 2015-12-25 | 2020-08-13 | Otsuka Pharmaceutical Factory, Inc. | Phenylimidazole compound |
| CN110023288B (zh) * | 2016-09-30 | 2022-10-28 | 广东众生睿创生物科技有限公司 | 酪氨酸激酶抑制剂的晶型、盐型以及制备方法 |
| CN110049969A (zh) * | 2017-02-07 | 2019-07-23 | 恩瑞生物医药科技(上海)有限公司 | 喹啉类化合物、其制备方法及其医药用途 |
| CN107115344B (zh) * | 2017-03-23 | 2019-06-14 | 广东众生睿创生物科技有限公司 | 酪氨酸激酶抑制剂在制备用于预防和/或治疗纤维化疾病的药物中的用途 |
| KR102327054B1 (ko) * | 2017-08-29 | 2021-11-17 | 기초과학연구원 | 퀴놀린 유도체 및 alk와 변이된 alk의 저해제로서의 용도 |
| CR20200140A (es) * | 2017-08-31 | 2020-05-15 | Abbvie Inc | Inhibidores de la ectonucleótido pirofosfatasa-fosfodiesterasa 1 (enpp-1) y usos de los mismos |
| WO2019062637A1 (zh) * | 2017-09-28 | 2019-04-04 | 南京明德新药研发股份有限公司 | 喹啉衍生物及其作为酪氨酸激酶抑制剂的应用 |
| CN108623521B (zh) * | 2018-03-22 | 2020-09-04 | 盐城师范学院 | 一种乐伐替尼的制备方法 |
| CN110483482A (zh) * | 2018-05-15 | 2019-11-22 | 北京诺诚健华医药科技有限公司 | 吲哚啉-1-甲酰胺类化合物、其制备方法及其在医药学上的应用 |
| CN110590839B (zh) * | 2018-06-13 | 2022-04-05 | 四川海思科制药有限公司 | 一种乐伐替尼衍生物及制备方法和用途 |
| CN110862397A (zh) * | 2018-08-27 | 2020-03-06 | 北京赛特明强医药科技有限公司 | 二噁烷并喹唑啉与二噁烷并喹啉类化合物及其制备方法与应用 |
| US12415816B2 (en) | 2018-11-07 | 2025-09-16 | Dana-Farber Cancer Institute, Inc. | Benzothiazole derivatives and 7-aza-benzothiazole derivatives as janus kinase 2 inhibitors and uses thereof |
| CN109485620A (zh) * | 2018-12-26 | 2019-03-19 | 安徽工大化工科技有限公司 | 一种2-甲氧基-6-甲氧基苯并噻唑的制备方法 |
| CA3128044A1 (en) * | 2019-02-01 | 2020-08-06 | The Board Of Trustees Of The Leland Stanford Junior University | Enpp1 inhibitors and methods of modulating immune response |
| KR20210151818A (ko) * | 2019-04-12 | 2021-12-14 | 내셔날 헬스 리서치 인스티튜트 | 치료 용도를 위한 키나제 억제제로서의 헤테로사이클릭 화합물 |
| CN111892536B (zh) * | 2019-05-05 | 2022-06-28 | 北京福元医药股份有限公司 | 取代的喹啉甲酰胺类化合物及其用途 |
| CA3141424C (en) * | 2019-06-14 | 2023-11-07 | Zhengxia CHEN | Fused ring compound as fgfr and vegfr dual inhibitor |
| PE20221034A1 (es) * | 2019-08-08 | 2022-06-17 | B C I Pharma | Derivados de quinolina como inhibidores de proteina quinasa |
| CN113321654B (zh) * | 2020-02-28 | 2022-05-03 | 上海济煜医药科技有限公司 | 作为激酶抑制剂的稠合吡啶酮类化合物 |
| EP4146639A1 (en) | 2020-05-06 | 2023-03-15 | Ajax Therapeutics, Inc. | 6-heteroaryloxy benzimidazoles and azabenzimidazoles as jak2 inhibitors |
| TW202241889A (zh) | 2020-12-23 | 2022-11-01 | 美商雅捷可斯治療公司 | 作為jak2抑制劑之6-雜芳基氧基苯并咪唑及氮雜苯并咪唑 |
| CN113582924A (zh) * | 2021-09-09 | 2021-11-02 | 四川国康药业有限公司 | 一种多靶点酪氨酸激酶抑制剂及其制备方法和用途 |
| WO2023086320A1 (en) | 2021-11-09 | 2023-05-19 | Ajax Therapeutics, Inc. | Forms and compositions of inhibitors of jak2 |
| JP7782035B2 (ja) | 2021-11-09 | 2025-12-08 | エイジャックス セラピューティクス, インコーポレイテッド | Jak2阻害剤としての6-ヘテロアリールオキシベンゾイミダゾール及びアザベンゾイミダゾール |
| CN114213404B (zh) * | 2021-12-27 | 2024-08-06 | 武汉九州钰民医药科技有限公司 | Vegfr抑制剂替沃扎尼的合成工艺 |
| CN118843617A (zh) * | 2022-03-29 | 2024-10-25 | 广东众生睿创生物科技有限公司 | 一种喹啉衍生物的晶型及其制备方法 |
| CN115215799B (zh) * | 2022-08-12 | 2024-05-31 | 上海爱博医药科技有限公司 | 脲类多靶点酪氨酸激酶抑制剂及其多种医药应用 |
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| US9334239B2 (en) * | 2012-12-21 | 2016-05-10 | Eisai R&D Management Co., Ltd. | Amorphous form of quinoline derivative, and method for producing same |
| EA201691850A1 (ru) * | 2014-03-17 | 2016-12-30 | Экселиксис, Инк. | Дозирование составов, содержащих кабозантиниб |
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2016
- 2016-04-07 US US15/562,825 patent/US10654808B2/en active Active
- 2016-04-07 EP EP16776127.9A patent/EP3293177B1/en active Active
- 2016-04-07 CN CN201680019729.0A patent/CN107683279B/zh active Active
- 2016-04-07 CN CN202011033493.0A patent/CN112028825B/zh active Active
- 2016-04-07 CN CN201610211659.0A patent/CN106046007B/zh active Active
- 2016-04-07 JP JP2017553109A patent/JP6617155B6/ja active Active
- 2016-04-07 WO PCT/CN2016/078703 patent/WO2016161952A1/zh not_active Ceased
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2019
- 2019-11-11 JP JP2019203698A patent/JP6928774B2/ja active Active
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| Publication number | Priority date | Publication date | Assignee | Title |
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| WO2000050405A1 (en) * | 1999-02-24 | 2000-08-31 | Astrazeneca Ab | Quinoline derivatives as tyrosine kinase inhibitors |
| CN1478078A (zh) * | 2000-10-20 | 2004-02-25 | ������������ʽ���� | 含氮芳环衍生物 |
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| CAS-RN:1348964-95-3.《REGISTRY》.2011, * |
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|---|---|
| EP3293177A1 (en) | 2018-03-14 |
| JP6928774B2 (ja) | 2021-09-01 |
| JP6617155B2 (ja) | 2019-12-11 |
| US20190119217A1 (en) | 2019-04-25 |
| JP6617155B6 (ja) | 2020-01-22 |
| EP3293177B1 (en) | 2024-11-27 |
| JP2020037576A (ja) | 2020-03-12 |
| JP2018513150A (ja) | 2018-05-24 |
| CN106046007A (zh) | 2016-10-26 |
| CN112028825A (zh) | 2020-12-04 |
| CN107683279A (zh) | 2018-02-09 |
| US10654808B2 (en) | 2020-05-19 |
| CN106046007B (zh) | 2019-02-05 |
| CN107683279B (zh) | 2020-11-03 |
| WO2016161952A1 (zh) | 2016-10-13 |
| EP3293177A4 (en) | 2018-12-12 |
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