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
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- 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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- pharmaceutically acceptable
- acceptable salt
- crystalline form
- inflammatory
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- 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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- A61K9/0014—Skin, i.e. galenical aspects of topical compositions
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- A61K9/06—Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
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- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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- 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
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- 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
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- 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
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- 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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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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| US201762577852P | 2017-10-27 | 2017-10-27 | |
| US62/577,852 | 2017-10-27 |
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| TW201930304A TW201930304A (zh) | 2019-08-01 |
| TWI789446B true TWI789446B (zh) | 2023-01-11 |
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| AU2018354370B2 (en) | 2017-10-27 | 2023-04-27 | Theravance Biopharma R&D Ip, Llc | Pyrimidine compound as JAK kinase inhibitor |
| MX2021006283A (es) * | 2018-11-30 | 2021-10-22 | Jiangsu Hansoh Pharmaceutical Group Co Ltd | Derivados heteroaromáticos para uso como regulador, método de preparación de los mismos y uso de los mismos. |
| AR118768A1 (es) | 2019-04-24 | 2021-10-27 | Theravance Biopharma R&D Ip Llc | Derivados de pirimidina como inhibidores de las cinasas jak |
| HRP20241053T1 (hr) * | 2019-04-24 | 2024-11-08 | Theravance Biopharma R&D Ip, Llc | Pirimidinski inhibitori jak, namijenjeni liječenju kožnih bolesti |
| KR102891680B1 (ko) * | 2020-07-28 | 2025-11-27 | 아큐티스 바이오테라퓨틱스, 인크. | Jak 저해제 및 라우레스-4를 함유하는 국소 제형 |
| BR112023003517A2 (pt) * | 2020-08-26 | 2023-05-09 | Nalo Therapeutics | Moduladores da proteína proto-oncogênica da família myc |
| 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 |
| US20250051338A1 (en) | 2021-10-25 | 2025-02-13 | Kymera Therapeutics, Inc. | Tyk2 degraders and uses thereof |
| MX2024007437A (es) | 2021-12-15 | 2024-09-04 | Arcutis Biotherapeutics Inc | Formulaciones estables de 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)
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| 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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| 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 |
| ATE346064T1 (de) | 2000-09-15 | 2006-12-15 | Vertex Pharma | Pyrazolverbindungen als protein-kinasehemmer |
| ATE354573T1 (de) | 2000-12-21 | 2007-03-15 | Vertex Pharma | ßPYRAZOLVERBINDUNGEN, DIE SICH ALS PROTEINKINASEINHIBITOREN EIGNENß |
| CA2588220A1 (en) | 2004-12-23 | 2006-06-29 | Pfizer Products Inc. | Heteroaromatic derivatives useful as anticancer agents |
| CA2629781A1 (en) | 2005-11-16 | 2007-05-24 | Vertex Pharmaceuticals Incorporated | Aminopyrimidines useful as kinase inhibitors |
| UY30444A1 (es) | 2006-06-30 | 2008-01-31 | Astrazeneca Ab | Derivados de pirimidina, procesos para su preparacinn, composiciones farmaccuticos y usos de los mismos. |
| CA2656290A1 (en) | 2006-07-05 | 2008-01-10 | Exelixis, Inc. | Methods of using igf1r and abl kinase modulators |
| WO2013092940A1 (en) | 2011-12-22 | 2013-06-27 | F. Hoffmann-La Roche Ag | 2, 4-diamine-pyrimidine derivative as serine/threonine kinase inhibitors |
| CN106687467A (zh) * | 2014-09-30 | 2017-05-17 | 韩美精密化学株式会社 | 高纯度（r）‑9‑[2‑（磷酰甲氧基）丙基]腺嘌呤的制备方法 |
| US9938257B2 (en) | 2015-09-11 | 2018-04-10 | Calitor Sciences, Llc | Substituted heteroaryl compounds and methods of use |
| AU2017258186B2 (en) | 2016-04-28 | 2020-09-17 | Theravance Biopharma R&D Ip, Llc | Pyrimidine compounds as JAK kinase inhibitors |
| AU2018354370B2 (en) * | 2017-10-27 | 2023-04-27 | Theravance Biopharma R&D Ip, Llc | Pyrimidine compound as JAK kinase inhibitor |
| AR118768A1 (es) | 2019-04-24 | 2021-10-27 | Theravance Biopharma R&D Ip Llc | Derivados de pirimidina como inhibidores de las cinasas jak |
| HRP20241053T1 (hr) | 2019-04-24 | 2024-11-08 | Theravance Biopharma R&D Ip, Llc | Pirimidinski inhibitori jak, namijenjeni liječenju kožnih bolesti |
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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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