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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Publication number
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
autoimmune
crystalline form
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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 Inc
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Pfizer Inc
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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
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • 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
    • A61P17/06—Antipsoriatics
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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]
    • 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)
  • 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)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (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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CN201980069164.0A Active CN112888691B (zh) 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

Country Status (15)

Country Link
US (1) US12116368B2 (https=)
EP (1) EP3870584A1 (https=)
JP (1) JP6944496B2 (https=)
KR (1) KR102629132B1 (https=)
CN (1) CN112888691B (https=)
AR (1) AR116797A1 (https=)
AU (1) AU2019363840B2 (https=)
BR (1) BR112021007568A2 (https=)
CA (1) CA3059000C (https=)
IL (1) IL282446B2 (https=)
MX (1) MX2021003241A (https=)
SG (1) SG11202103667QA (https=)
TW (1) TWI729530B (https=)
WO (1) WO2020084435A1 (https=)
ZA (1) ZA202101735B (https=)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2020338043B2 (en) 2019-08-26 2025-12-18 Chemwerth, Inc. Substituted (7H-pyrrolo[2,3-D]pyrimidin-4-yl)amino compounds useful as JAK1 inhibitors
KR20220123271A (ko) * 2019-12-31 2022-09-06 화이자 알앤디 유케이 리미티드 1-((2S,5R)-5-((7H-피롤로[2,3-d]피리미딘-4-일)아미노)-2-메틸피페리딘-1-일)프로프-2-엔-1-온의 안정한 즉시 방출형 정제 및 캡슐 제형
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
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
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
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
WO2025219875A1 (en) * 2024-04-17 2025-10-23 Alembic Pharmaceuticals Limited Solid forms of ritlecitinib or its salts
CN118420493B (zh) * 2024-04-24 2026-04-14 山东福长药业有限公司 一种2,5-二取代氨基己酸酯的制备方法及使用其制备利特昔替尼的方法
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 (2)

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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

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BR9911365A (pt) 1998-06-19 2001-03-13 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

Patent Citations (2)

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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
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;Atli Thorarensen等;《J. Med. Chem.》;第第60卷卷;第1971−1993页 *

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CA3059000A1 (en) 2020-04-22
US20210387989A1 (en) 2021-12-16
SG11202103667QA (en) 2021-05-28
TWI729530B (zh) 2021-06-01
EP3870584A1 (en) 2021-09-01
AR116797A1 (es) 2021-06-16
AU2019363840A1 (en) 2021-04-01
ZA202101735B (en) 2022-07-27
JP6944496B2 (ja) 2021-10-06
KR20210080468A (ko) 2021-06-30
US12116368B2 (en) 2024-10-15
BR112021007568A2 (pt) 2021-07-27
KR102629132B1 (ko) 2024-01-29
TW202033525A (zh) 2020-09-16
CN112888691A (zh) 2021-06-01
MX2021003241A (es) 2021-05-12
IL282446B1 (en) 2024-02-01
JP2020066629A (ja) 2020-04-30
WO2020084435A1 (en) 2020-04-30
IL282446B2 (en) 2024-06-01
IL282446A (en) 2021-06-30
AU2019363840B2 (en) 2021-12-09
CA3059000C (en) 2026-04-14

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