TWI729530B - 吡咯并〔2,3-d〕嘧啶甲苯磺酸鹽類、其晶形以及其製造方法及中間體 - Google Patents

吡咯并〔2,3-d〕嘧啶甲苯磺酸鹽類、其晶形以及其製造方法及中間體 Download PDF

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TWI729530B
TWI729530B TW108137470A TW108137470A TWI729530B TW I729530 B TWI729530 B TW I729530B TW 108137470 A TW108137470 A TW 108137470A TW 108137470 A TW108137470 A TW 108137470A TW I729530 B TWI729530 B TW I729530B
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disease
cancer
pyrrolo
amino
methylpiperidin
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TW108137470A
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TW202033525A (zh
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道格拉斯 克里契爾
大衛 丹尼爾斯
布萊恩 桑瑪斯
勇 陶
凱文 吉拉爾
格列高利 高肯
彼得 羅斯
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美商輝瑞股份有限公司
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/14Drugs for dermatological disorders for baldness or alopecia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (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)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
TW108137470A 2018-10-22 2019-10-17 吡咯并〔2,3-d〕嘧啶甲苯磺酸鹽類、其晶形以及其製造方法及中間體 TWI729530B (zh)

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US201862748628P 2018-10-22 2018-10-22
US62/748,628 2018-10-22

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TW202033525A TW202033525A (zh) 2020-09-16
TWI729530B true TWI729530B (zh) 2021-06-01

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EP (1) EP3870584A1 (enExample)
JP (1) JP6944496B2 (enExample)
KR (1) KR102629132B1 (enExample)
CN (1) CN112888691B (enExample)
AR (1) AR116797A1 (enExample)
AU (1) AU2019363840B2 (enExample)
BR (1) BR112021007568A2 (enExample)
CA (1) CA3059000A1 (enExample)
IL (1) IL282446B2 (enExample)
MX (1) MX2021003241A (enExample)
SG (1) SG11202103667QA (enExample)
TW (1) TWI729530B (enExample)
WO (1) WO2020084435A1 (enExample)
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CA3152021A1 (en) 2019-08-26 2021-03-04 Chemwerth, Inc. Substituted (7h-pyrrolo[2,3-d]pyrimidin-4-yl)amino compounds useful as jak1 inhibitors
CN113121539A (zh) * 2019-12-31 2021-07-16 江苏艾立康医药科技有限公司 一种pf06651600的制备方法
CN115023221B (zh) * 2019-12-31 2024-05-28 辉瑞英国研发有限公司 1-((2s,5r)-5-((7h-吡咯并[2,3-d]嘧啶-4-基)氨基)-2-甲基哌啶-1-基)丙-2-烯-1-酮的稳定立即释放片剂和胶囊制剂
CN111620880B (zh) * 2020-06-15 2022-06-10 江苏艾立康医药科技有限公司 Pf-06651600 dl-酒石酸盐,晶型及其制备方法
CN111732591B (zh) * 2020-06-15 2022-06-10 江苏艾立康医药科技有限公司 Pf-06651600 l-酒石酸盐,晶型及其制备方法
CN114835715B (zh) * 2020-06-15 2024-04-05 江苏艾立康医药科技有限公司 Pf-06651600马来酸盐及其制备方法
WO2022012587A1 (zh) * 2020-07-14 2022-01-20 苏州晶云药物科技股份有限公司 丙烯酮类化合物的丙二酸盐晶型及其制备方法
KR102473645B1 (ko) * 2020-08-28 2022-12-05 (주)부흥산업사 (2S,5R)-벤질 5-(t-부톡시카르보닐아미노)-2-메틸피페리딘-1-카르복실레이트의 제조방법
CN112877379B (zh) * 2021-01-18 2023-09-01 华南理工大学 一种化学酶法合成n-[(3r,6r)-6-甲基哌啶-3-基]氨基甲酸叔丁酯的方法
WO2025144783A1 (en) * 2023-12-28 2025-07-03 Aclaris Therapeutics, Inc. Methods of synthesizing substituted pyrrolopyrimidine compounds
WO2025146702A1 (en) * 2024-01-03 2025-07-10 Msn Laboratories Private Limited, R&D Center Solid state forms of 1-{(2s,5r)-2-methyl-5-[(7h-pyrrolo[2,3-d]pyrimidin-4-yl)amino] piperidine-1-yl}prop-2-en-1-one 4-methylbenzene-1-sulfonic acid
WO2025244944A1 (en) * 2024-05-20 2025-11-27 Opna Bio SA Crystal forms of an agent
WO2025257773A1 (en) 2024-06-11 2025-12-18 Assia Chemical Industries Ltd. Processes for the preparation of ritlecitinib and intermediates thereof
CN119060059B (zh) * 2024-08-21 2025-10-28 武汉九州钰民医药科技有限公司 一种甲苯磺酸利特昔替尼的制备工艺

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW201524977A (zh) * 2013-12-05 2015-07-01 Pfizer 吡咯并[2,3-d]嘧啶基、吡咯并[2,3-b]吡基及吡咯并[2,3-d]吡啶基丙烯醯胺

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT1087970E (pt) 1998-06-19 2004-06-30 Pfizer Prod Inc Compostos pirrolo¬2,3-d|pirimidina
MA41350A (fr) * 2015-01-14 2017-11-21 Janssen Pharmaceutica Nv Synthèse d'un inhibiteur de la tyrosine kinase de bruton
CN105859721B (zh) * 2015-01-22 2018-04-17 浙江京新药业股份有限公司 一种伊布鲁替尼的制备方法

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW201524977A (zh) * 2013-12-05 2015-07-01 Pfizer 吡咯并[2,3-d]嘧啶基、吡咯并[2,3-b]吡基及吡咯并[2,3-d]吡啶基丙烯醯胺

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IL282446B1 (en) 2024-02-01
JP6944496B2 (ja) 2021-10-06
IL282446A (en) 2021-06-30
BR112021007568A2 (pt) 2021-07-27
CN112888691A (zh) 2021-06-01
EP3870584A1 (en) 2021-09-01
MX2021003241A (es) 2021-05-12
WO2020084435A1 (en) 2020-04-30
TW202033525A (zh) 2020-09-16
US20210387989A1 (en) 2021-12-16
US12116368B2 (en) 2024-10-15
IL282446B2 (en) 2024-06-01
JP2020066629A (ja) 2020-04-30
ZA202101735B (en) 2022-07-27
KR102629132B1 (ko) 2024-01-29
CN112888691B (zh) 2023-10-31
SG11202103667QA (en) 2021-05-28
AR116797A1 (es) 2021-06-16
AU2019363840A1 (en) 2021-04-01
KR20210080468A (ko) 2021-06-30
CA3059000A1 (en) 2020-04-22
AU2019363840B2 (en) 2021-12-09

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