CN112888691B - 吡咯并[2,3-d]嘧啶甲苯磺酸盐、其结晶形式以及有关的制备方法和中间体 - Google Patents

吡咯并[2,3-d]嘧啶甲苯磺酸盐、其结晶形式以及有关的制备方法和中间体 Download PDF

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CN112888691B
CN112888691B CN201980069164.0A CN201980069164A CN112888691B CN 112888691 B CN112888691 B CN 112888691B CN 201980069164 A CN201980069164 A CN 201980069164A CN 112888691 B CN112888691 B CN 112888691B
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disease
cancer
disorder
crystalline form
autoimmune
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CN112888691A (zh
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D·J·克瑞彻
D·S·B·丹尼尔斯
B·M·萨马斯
Y·陶
K·P·吉拉德
G·S·戈肯
P·R·罗斯
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Pfizer Corp SRL
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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)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Immunology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CN201980069164.0A 2018-10-22 2019-10-21 吡咯并[2,3-d]嘧啶甲苯磺酸盐、其结晶形式以及有关的制备方法和中间体 Active CN112888691B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862748628P 2018-10-22 2018-10-22
US62/748628 2018-10-22
PCT/IB2019/058940 WO2020084435A1 (en) 2018-10-22 2019-10-21 Pyrrolo[2,3-d]pyrimidine tosylate salt, crystalline form thereof and manufacturing process and intermediates thereto

Publications (2)

Publication Number Publication Date
CN112888691A CN112888691A (zh) 2021-06-01
CN112888691B true CN112888691B (zh) 2023-10-31

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Country Status (15)

Country Link
US (1) US12116368B2 (enExample)
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)
ZA (1) ZA202101735B (enExample)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114761011B (zh) 2019-08-26 2024-06-14 肯沃斯公司 用作jak1抑制剂的取代的(7h-吡咯并[2,3-d]嘧啶-4-基)氨基化合物
AU2020417043A1 (en) * 2019-12-31 2022-06-09 Pfizer Inc. Stable immediate release tablet and capsule formulations of 1-((2S,5R)-5-((7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one
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
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
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 (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105859721A (zh) * 2015-01-22 2016-08-17 浙江京新药业股份有限公司 一种伊布鲁替尼的制备方法
EP3318565A1 (en) * 2013-12-05 2018-05-09 Pfizer Inc Pyrrolo[2,3-d]pyrimidinyl, pyrrolo[2,3-b]pyrazinyl and pyrrolo[2,3-d]pyridinyl acrylamides

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RS50087B (sr) 1998-06-19 2009-01-22 Pfizer Products Inc., Pirolo (2,3-d) pirimidin jedinjenja
MA41350A (fr) * 2015-01-14 2017-11-21 Janssen Pharmaceutica Nv Synthèse d'un inhibiteur de la tyrosine kinase de bruton

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3318565A1 (en) * 2013-12-05 2018-05-09 Pfizer Inc Pyrrolo[2,3-d]pyrimidinyl, pyrrolo[2,3-b]pyrazinyl and pyrrolo[2,3-d]pyridinyl acrylamides
CN105859721A (zh) * 2015-01-22 2016-08-17 浙江京新药业股份有限公司 一种伊布鲁替尼的制备方法

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Atli Thorarensen等.Design of a Janus Kinase 3 (JAK3) Specific Inhibitor 1‑((2S,5R)‑5- ((7H‑Pyrrolo[2,3‑d]pyrimidin-4-yl)amino)-2-methylpiperidin-1- yl)prop-2-en-1-one (PF-06651600) Allowing for the Interrogation of JAK3 Signaling in Humans.《J. Med. Chem.》.2017,第第60卷卷第1971−1993页. *

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Publication number Publication date
AU2019363840B2 (en) 2021-12-09
CN112888691A (zh) 2021-06-01
BR112021007568A2 (pt) 2021-07-27
KR20210080468A (ko) 2021-06-30
ZA202101735B (en) 2022-07-27
MX2021003241A (es) 2021-05-12
JP6944496B2 (ja) 2021-10-06
KR102629132B1 (ko) 2024-01-29
EP3870584A1 (en) 2021-09-01
IL282446B2 (en) 2024-06-01
IL282446A (en) 2021-06-30
TWI729530B (zh) 2021-06-01
US12116368B2 (en) 2024-10-15
WO2020084435A1 (en) 2020-04-30
AR116797A1 (es) 2021-06-16
CA3059000A1 (en) 2020-04-22
AU2019363840A1 (en) 2021-04-01
JP2020066629A (ja) 2020-04-30
IL282446B1 (en) 2024-02-01
TW202033525A (zh) 2020-09-16
SG11202103667QA (en) 2021-05-28
US20210387989A1 (en) 2021-12-16

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