AU2019363840B2 - Pyrrolo(2,3-d)pyrimidine tosylate salt, crystalline form thereof and manufacturing process and intermediates thereto - Google Patents

Pyrrolo(2,3-d)pyrimidine tosylate salt, crystalline form thereof and manufacturing process and intermediates thereto Download PDF

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Publication number
AU2019363840B2
AU2019363840B2 AU2019363840A AU2019363840A AU2019363840B2 AU 2019363840 B2 AU2019363840 B2 AU 2019363840B2 AU 2019363840 A AU2019363840 A AU 2019363840A AU 2019363840 A AU2019363840 A AU 2019363840A AU 2019363840 B2 AU2019363840 B2 AU 2019363840B2
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Prior art keywords
pyrrolo
pyrimidin
prop
amino
methylpiperidin
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AU2019363840A1 (en
Inventor
Douglas James Critcher
David Sydney Bernard Daniels
Kevin Paul Girard
Gregory Scott Goeken
Peter Robert Rose
Brian Matthew Samas
Yong Tao
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Pfizer Corp SRL
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Pfizer Corp Belgium
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)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (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)
  • 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)
AU2019363840A 2018-10-22 2019-10-21 Pyrrolo(2,3-d)pyrimidine tosylate salt, crystalline form thereof and manufacturing process and intermediates thereto Active AU2019363840B2 (en)

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)

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AU2019363840A1 AU2019363840A1 (en) 2021-04-01
AU2019363840B2 true AU2019363840B2 (en) 2021-12-09

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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 (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP4021452B1 (en) * 2019-08-26 2023-12-20 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
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
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
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
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
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 (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1087970B1 (en) 1998-06-19 2004-04-28 Pfizer Products Inc. PYRROLO 2,3-d]PYRIMIDINE COMPOUNDS
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
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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Publication number Publication date
US20210387989A1 (en) 2021-12-16
AR116797A1 (es) 2021-06-16
KR102629132B1 (ko) 2024-01-29
BR112021007568A2 (pt) 2021-07-27
IL282446A (en) 2021-06-30
CN112888691A (zh) 2021-06-01
US12116368B2 (en) 2024-10-15
EP3870584A1 (en) 2021-09-01
AU2019363840A1 (en) 2021-04-01
TW202033525A (zh) 2020-09-16
ZA202101735B (en) 2022-07-27
CA3059000A1 (en) 2020-04-22
IL282446B2 (en) 2024-06-01
KR20210080468A (ko) 2021-06-30
MX2021003241A (es) 2021-05-12
TWI729530B (zh) 2021-06-01
CN112888691B (zh) 2023-10-31
JP2020066629A (ja) 2020-04-30
WO2020084435A1 (en) 2020-04-30
IL282446B1 (en) 2024-02-01
JP6944496B2 (ja) 2021-10-06
SG11202103667QA (en) 2021-05-28

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