KR102629132B1 - 피롤로[2,3-d]피리미딘 토실레이트 염, 이의 결정질 형태, 이의 제조 방법 및 이에 대한 중간체 - Google Patents

피롤로[2,3-d]피리미딘 토실레이트 염, 이의 결정질 형태, 이의 제조 방법 및 이에 대한 중간체 Download PDF

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KR102629132B1
KR102629132B1 KR1020217015125A KR20217015125A KR102629132B1 KR 102629132 B1 KR102629132 B1 KR 102629132B1 KR 1020217015125 A KR1020217015125 A KR 1020217015125A KR 20217015125 A KR20217015125 A KR 20217015125A KR 102629132 B1 KR102629132 B1 KR 102629132B1
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disease
cancer
autoimmune
pyrrolo
pyrimidin
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KR20210080468A (ko
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더글라스 제임스 크리처
데이비드 시드니 버나드 다니엘스
브라이언 매튜 사마스
용 타오
케빈 폴 지라드
그레고리 스콧 괴켄
피터 로버트 로즈
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화이자 인코포레이티드
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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)
  • 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)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
KR1020217015125A 2018-10-22 2019-10-21 피롤로[2,3-d]피리미딘 토실레이트 염, 이의 결정질 형태, 이의 제조 방법 및 이에 대한 중간체 Active KR102629132B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862748628P 2018-10-22 2018-10-22
US62/748,628 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
KR20210080468A KR20210080468A (ko) 2021-06-30
KR102629132B1 true KR102629132B1 (ko) 2024-01-29

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KR1020217015125A Active KR102629132B1 (ko) 2018-10-22 2019-10-21 피롤로[2,3-d]피리미딘 토실레이트 염, 이의 결정질 형태, 이의 제조 방법 및 이에 대한 중간체

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
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
CA3166050C (en) * 2019-12-31 2024-02-20 Pfizer R&D Uk Limited 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
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
CN111620879B (zh) * 2020-06-15 2022-06-10 江苏艾立康医药科技有限公司 Pf-06651600马来酸盐，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
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

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SK286640B6 (sk) 1998-06-19 2009-03-05 Pfizer Products Inc. Pyrol [2,3-d] pyrimidínová zlúčenina, jej použitie na výrobu liečiva, farmaceutická kompozícia s jej obsahom, použitie jej kombinácie s ďalšími činidlami a súpravy s jej obsahom na výrobu liečiva
SI3077395T1 (en) * 2013-12-05 2018-03-30 Pfizer Inc. Pyrrolo(2,3-d)pyrimidinyl, pyrrolo(2,3-b)pyrazinyl and pyrrolo(2,3-d)pyridinyl acrylamides
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

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US12116368B2 (en) 2024-10-15
CN112888691B (zh) 2023-10-31
SG11202103667QA (en) 2021-05-28
CN112888691A (zh) 2021-06-01
IL282446A (en) 2021-06-30
WO2020084435A1 (en) 2020-04-30
CA3059000A1 (en) 2020-04-22
BR112021007568A2 (pt) 2021-07-27
MX2021003241A (es) 2021-05-12
AU2019363840A1 (en) 2021-04-01
KR20210080468A (ko) 2021-06-30
JP2020066629A (ja) 2020-04-30
ZA202101735B (en) 2022-07-27
AU2019363840B2 (en) 2021-12-09
TWI729530B (zh) 2021-06-01
IL282446B2 (en) 2024-06-01
CA3059000C (en) 2026-04-14
EP3870584A1 (en) 2021-09-01
IL282446B1 (en) 2024-02-01
US20210387989A1 (en) 2021-12-16
AR116797A1 (es) 2021-06-16
JP6944496B2 (ja) 2021-10-06
TW202033525A (zh) 2020-09-16

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