TWI789446B - 作為jak激酶抑制劑之嘧啶化合物 - Google Patents
作為jak激酶抑制劑之嘧啶化合物 Download PDFInfo
- Publication number
- TWI789446B TWI789446B TW107137865A TW107137865A TWI789446B TW I789446 B TWI789446 B TW I789446B TW 107137865 A TW107137865 A TW 107137865A TW 107137865 A TW107137865 A TW 107137865A TW I789446 B TWI789446 B TW I789446B
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- TW
- Taiwan
- Prior art keywords
- compound
- pharmaceutically acceptable
- acceptable salt
- crystalline form
- inflammatory
- Prior art date
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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
- A61K31/495—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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0014—Skin, i.e. galenical aspects of topical compositions
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/06—Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
-
- 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
-
- 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
- A61P17/14—Drugs for dermatological disorders for baldness or alopecia
-
- 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]
-
- 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
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- 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
- C07D403/02—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 two hetero rings
- C07D403/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
- C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
- C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
- C07D451/14—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing 9-azabicyclo [3.3.1] nonane ring systems, e.g. granatane, 2-aza-adamantane; Cyclic acetals thereof
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Immunology (AREA)
- Dermatology (AREA)
- Transplantation (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicinal Preparation (AREA)
- Dental Preparations (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762577852P | 2017-10-27 | 2017-10-27 | |
| US62/577,852 | 2017-10-27 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| TW201930304A TW201930304A (zh) | 2019-08-01 |
| TWI789446B true TWI789446B (zh) | 2023-01-11 |
Family
ID=64277858
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TW107137865A TWI789446B (zh) | 2017-10-27 | 2018-10-26 | 作為jak激酶抑制劑之嘧啶化合物 |
Country Status (38)
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SG11202001706RA (en) * | 2017-10-27 | 2020-03-30 | Theravance Biopharma R&D Ip Llc | Pyrimidine compound as jak kinase inhibitor |
| WO2020108613A1 (zh) * | 2018-11-30 | 2020-06-04 | 江苏豪森药业集团有限公司 | 杂芳类衍生物调节剂、其制备方法和应用 |
| PL3958969T3 (pl) | 2019-04-24 | 2024-05-20 | Theravance Biopharma R&D Ip, Llc | Estrowe i węglanowe związki pirymidynowe jako inhibitory kinaz |
| TW202106681A (zh) * | 2019-04-24 | 2021-02-16 | 美商施萬生物製藥研發Ｉｐ有限責任公司 | 用於治療皮膚疾病之嘧啶jak抑制劑 |
| WO2022027041A1 (en) | 2020-07-28 | 2022-02-03 | Arcutis Biotherapeutics, Inc. | Topical formulation containing jak inhibitor and laureth-4 |
| CA3190539A1 (en) * | 2020-08-26 | 2022-03-03 | William Greenlee | Modulators of myc family proto-oncogene protein |
| WO2022076771A1 (en) * | 2020-10-08 | 2022-04-14 | Icahn School Of Medicine At Mount Sinai | Compositions for treatment alopecia areata, biomarkers for treatment success, and methods of use thereof |
| TW202311256A (zh) * | 2021-06-18 | 2023-03-16 | 美商基利科學股份有限公司 | 用於治療ｆｘｒ誘發之搔癢之ｉｌ－３１調節劑 |
| EP4423086A1 (en) | 2021-10-25 | 2024-09-04 | Kymera Therapeutics, Inc. | Tyk2 degraders and uses thereof |
| CA3240662A1 (en) | 2021-12-15 | 2023-06-22 | Herbert R. Brinkman | Stable formulations of shr0302 |
| CN114246938A (zh) * | 2022-01-25 | 2022-03-29 | 中山大学中山眼科中心 | Il-4在制备用于治疗视网膜变性疾病药物中的应用 |
| CN115487301B (zh) * | 2022-11-08 | 2023-07-07 | 四川大学华西医院 | Il-13抑制剂在制备延缓或治疗视网膜色素变性的药物中的用途 |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2015094803A1 (en) * | 2013-12-16 | 2015-06-25 | Calitor Sciences, Llc | Substituted heteroaryl compounds and methods of use |
| US20160052930A1 (en) * | 2014-08-21 | 2016-02-25 | Pfizer Inc. | Aminopyrimidinyl compounds |
| WO2016191524A1 (en) * | 2015-05-28 | 2016-12-01 | Theravance Biopharma R&D Ip, Llc | Naphthyridine compounds as jak kinase inhibitors |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4919934A (en) | 1989-03-02 | 1990-04-24 | Richardson-Vicks Inc. | Cosmetic sticks |
| US6660731B2 (en) | 2000-09-15 | 2003-12-09 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| WO2002022605A1 (en) | 2000-09-15 | 2002-03-21 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| US6989385B2 (en) | 2000-12-21 | 2006-01-24 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| JP2008525422A (ja) * | 2004-12-23 | 2008-07-17 | ファイザー・プロダクツ・インク | 抗癌剤として有用な複素芳香族誘導体 |
| US20070179125A1 (en) | 2005-11-16 | 2007-08-02 | Damien Fraysse | Aminopyrimidines useful as kinase inhibitors |
| TW200817391A (en) | 2006-06-30 | 2008-04-16 | Astrazeneca Ab | Novel compounds |
| EP2043651A2 (en) | 2006-07-05 | 2009-04-08 | Exelixis, Inc. | Methods of using igf1r and abl kinase modulators |
| CN104011050A (zh) | 2011-12-22 | 2014-08-27 | 霍夫曼-拉罗奇有限公司 | 作为丝氨酸/苏氨酸激酶抑制剂的2,4-二氨基-嘧啶衍生物 |
| JP2017535520A (ja) * | 2014-09-30 | 2017-11-30 | ハンミ・ファイン・ケミカル・カンパニー・リミテッドＨａｎｍｉ Ｆｉｎｅ Ｃｈｅｍｉｃａｌ Ｃｏ．， Ｌｔｄ． | 高純度の（ｒ）−９−［２−（ホスホノメトキシ）プロピル］アデニンの製造方法 |
| JP2018527362A (ja) * | 2015-09-11 | 2018-09-20 | サンシャイン・レイク・ファーマ・カンパニー・リミテッドＳｕｎｓｈｉｎｅ Ｌａｋｅ Ｐｈａｒｍａ Ｃｏ．，Ｌｔｄ． | 置換されたヘテロアリール化合物および使用方法 |
| CA3020506A1 (en) | 2016-04-28 | 2017-11-02 | Theravance Biopharma R&D Ip, Llc | Pyrimidine compounds as jak kinase inhibitors |
| SG11202001706RA (en) | 2017-10-27 | 2020-03-30 | Theravance Biopharma R&D Ip Llc | Pyrimidine compound as jak kinase inhibitor |
| PL3958969T3 (pl) | 2019-04-24 | 2024-05-20 | Theravance Biopharma R&D Ip, Llc | Estrowe i węglanowe związki pirymidynowe jako inhibitory kinaz |
| TW202106681A (zh) | 2019-04-24 | 2021-02-16 | 美商施萬生物製藥研發Ｉｐ有限責任公司 | 用於治療皮膚疾病之嘧啶jak抑制劑 |
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2018
- 2018-10-26 SG SG11202001706RA patent/SG11202001706RA/en unknown
- 2018-10-26 AU AU2018354370A patent/AU2018354370B2/en active Active
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- 2018-10-26 ES ES18801171T patent/ES2932526T3/es active Active
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- 2018-10-26 CN CN201880068081.5A patent/CN111247142B/zh active Active
- 2018-10-26 CU CU2020000053A patent/CU24671B1/es unknown
- 2018-10-26 UA UAA202003146A patent/UA125130C2/uk unknown
- 2018-10-26 SI SI201830770T patent/SI3672965T1/sl unknown
- 2018-10-26 MA MA49956A patent/MA49956B1/fr unknown
- 2018-10-26 PT PT188011712T patent/PT3672965T/pt unknown
- 2018-10-26 PE PE2020000414A patent/PE20201495A1/es unknown
- 2018-10-26 MD MDE20200681T patent/MD3672965T2/ro not_active IP Right Cessation
- 2018-10-26 LT LTEPPCT/US2018/057682T patent/LT3672965T/lt unknown
- 2018-10-26 CA CA3074034A patent/CA3074034A1/en active Pending
- 2018-10-26 GE GEAP202115340A patent/GEAP202115340A/en unknown
- 2018-10-26 TW TW107137865A patent/TWI789446B/zh active
- 2018-10-26 MX MX2020004255A patent/MX2020004255A/es unknown
- 2018-10-26 BR BR112020008015-2A patent/BR112020008015A2/pt unknown
- 2018-10-26 PL PL18801171.2T patent/PL3672965T3/pl unknown
- 2018-10-26 GE GEAP201815340A patent/GEP20227344B/en unknown
- 2018-10-26 HR HRP20221221TT patent/HRP20221221T1/hr unknown
- 2018-10-26 JP JP2020523324A patent/JP7218364B2/ja active Active
- 2018-10-26 RS RS20220903A patent/RS63608B1/sr unknown
- 2018-10-26 IL IL274037A patent/IL274037B2/en unknown
- 2018-10-26 HU HUE18801171A patent/HUE060401T2/hu unknown
- 2018-10-26 EA EA202091016A patent/EA202091016A1/ru unknown
- 2018-10-26 KR KR1020207012597A patent/KR102613503B1/ko active Active
- 2018-10-26 WO PCT/US2018/057682 patent/WO2019084383A1/en not_active Ceased
- 2018-10-26 US US16/171,693 patent/US10308646B2/en active Active
- 2018-10-26 DK DK18801171.2T patent/DK3672965T3/da active
- 2018-10-26 EP EP18801171.2A patent/EP3672965B1/en active Active
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2019
- 2019-04-22 US US16/390,175 patent/US10562894B2/en active Active
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2020
- 2020-01-08 US US16/737,067 patent/US10774080B2/en active Active
- 2020-03-13 PH PH12020500528A patent/PH12020500528A1/en unknown
- 2020-03-16 ZA ZA2020/01641A patent/ZA202001641B/en unknown
- 2020-04-23 CL CL2020001090A patent/CL2020001090A1/es unknown
- 2020-04-24 NI NI202000032A patent/NI202000032A/es unknown
- 2020-04-27 EC ECSENADI202023795A patent/ECSP20023795A/es unknown
- 2020-05-06 DO DO2020000083A patent/DOP2020000083A/es unknown
- 2020-08-12 US US16/991,268 patent/US10988470B2/en active Active
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2021
- 2021-03-30 US US17/301,243 patent/US11420965B2/en active Active
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2022
- 2022-06-30 US US17/855,539 patent/US11814377B2/en active Active
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2023
- 2023-10-03 US US18/480,442 patent/US12172994B2/en active Active
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2015094803A1 (en) * | 2013-12-16 | 2015-06-25 | Calitor Sciences, Llc | Substituted heteroaryl compounds and methods of use |
| US20160052930A1 (en) * | 2014-08-21 | 2016-02-25 | Pfizer Inc. | Aminopyrimidinyl compounds |
| WO2016191524A1 (en) * | 2015-05-28 | 2016-12-01 | Theravance Biopharma R&D Ip, Llc | Naphthyridine compounds as jak kinase inhibitors |
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