ZA200800284B - Pyrrolo [2,3-d] pyrimidine derivatives; their intermediates and synthesis - Google Patents

Pyrrolo [2,3-d] pyrimidine derivatives; their intermediates and synthesis

Info

Publication number: ZA200800284B
Authority: ZA; South Africa
Prior art keywords: pyrrolo; intermediates; synthesis; pyrimidine derivatives; pyrimidine
Prior art date: 2005-07-29

Application number

ZA200800284A

Other languages

English (en)

Inventor

Ruggeri Sally Gut

Makowski Teresa Margaret

Urban Frank John

Hawkins Joel Michael

Rutherford Jennifer Lea

Original Assignee

Pfizer Prod Inc

Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)

2005-07-29

Filing date

2008-01-09

Publication date

2008-12-31

2008-01-09 Application filed by Pfizer Prod Inc filed Critical Pfizer Prod Inc

2008-12-31 Publication of ZA200800284B publication Critical patent/ZA200800284B/xx

Classifications

- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
- 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
- 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
- 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
- A61P25/00—Drugs for disorders of the nervous system
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
- 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]
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D211/56—Nitrogen atoms
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

Health & Medical Sciences (AREA)
Organic Chemistry (AREA)
Chemical & Material Sciences (AREA)
Medicinal Chemistry (AREA)
Chemical Kinetics & Catalysis (AREA)
General Chemical & Material Sciences (AREA)
Veterinary Medicine (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Pharmacology & Pharmacy (AREA)
Life Sciences & Earth Sciences (AREA)
Animal Behavior & Ethology (AREA)
General Health & Medical Sciences (AREA)
Public Health (AREA)
Bioinformatics & Cheminformatics (AREA)
Engineering & Computer Science (AREA)
Immunology (AREA)
Diabetes (AREA)
Biomedical Technology (AREA)
Neurosurgery (AREA)
Pulmonology (AREA)
Neurology (AREA)
Dermatology (AREA)
Rheumatology (AREA)
Hematology (AREA)
Obesity (AREA)
Transplantation (AREA)
Oncology (AREA)
Endocrinology (AREA)
Psychiatry (AREA)
Pain & Pain Management (AREA)
Emergency Medicine (AREA)
Hospice & Palliative Care (AREA)
Orthopedic Medicine & Surgery (AREA)
Physical Education & Sports Medicine (AREA)
Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
Nitrogen Condensed Heterocyclic Rings (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Hydrogenated Pyridines (AREA)

ZA200800284A 2005-07-29 2008-01-09 Pyrrolo [2,3-d] pyrimidine derivatives; their intermediates and synthesis ZA200800284B (en)

Applications Claiming Priority (1)

Application Number	Priority Date	Filing Date	Title
US70401105P	2005-07-29	2005-07-29

Publications (1)

Publication Number	Publication Date
ZA200800284B true ZA200800284B (en)	2008-12-31

Family

ID=36950230

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
ZA200800284A ZA200800284B (en)	2005-07-29	2008-01-09	Pyrrolo [2,3-d] pyrimidine derivatives; their intermediates and synthesis

Country Status (24)

Country	Link
US (2)	US8232394B2 (fr)
EP (1)	EP1913000B1 (fr)
JP (1)	JP4052523B2 (fr)
KR (1)	KR100987870B1 (fr)
CN (1)	CN101233138A (fr)
AR (1)	AR056004A1 (fr)
AT (1)	ATE540952T1 (fr)
AU (1)	AU2006273762A1 (fr)
BR (1)	BRPI0613876A2 (fr)
CA (1)	CA2614907C (fr)
CY (1)	CY1112319T1 (fr)
DK (1)	DK1913000T3 (fr)
ES (1)	ES2377771T3 (fr)
IL (1)	IL188372A0 (fr)
MX (1)	MX2008001334A (fr)
NZ (1)	NZ565363A (fr)
PL (1)	PL1913000T3 (fr)
PT (1)	PT1913000E (fr)
RU (1)	RU2384583C2 (fr)
SG (1)	SG170783A1 (fr)
SI (1)	SI1913000T1 (fr)
TW (1)	TWI319402B (fr)
WO (1)	WO2007012953A2 (fr)
ZA (1)	ZA200800284B (fr)

Families Citing this family (78)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
KR101258316B1 (ko)	2007-07-11	2013-04-30	화이자 인코포레이티드	안구 건조증 치료용 약학 조성물 및 방법
ES2552805T3 (es)	2009-04-20	2015-12-02	Auspex Pharmaceuticals, Llc	Inhibidores piperidínicos de la cinasa Janus 3
BR112012005382A2 (pt) *	2009-09-10	2016-03-29	Hoffmann La Roche	inibidores de jak
CA2776028C (fr)	2009-10-15	2015-12-01	Pfizer Inc.	Composes pyrrolo[2,3-d]pyrimidine
ES2461967T3 (es)	2009-12-18	2014-05-21	Pfizer Inc.	Compuestos de pirrolo[2,3-d]pirimidina
CN102712640A (zh)	2010-01-12	2012-10-03	弗·哈夫曼-拉罗切有限公司	三环杂环化合物、其组合物和应用方法
JP2013518882A (ja)	2010-02-05	2013-05-23	ファイザー・インク	ＪＡＫ阻害剤としてのピロロ［２，３−ｄ］ピリミジン尿素化合物
CN104610264A (zh)	2011-04-08	2015-05-13	辉瑞大药厂	结晶和非结晶形式的托法替尼,以及包含托法替尼和渗透增强剂的药物组合物
US8993756B2 (en)	2011-12-06	2015-03-31	Merck Sharp & Dohme Corp.	Pyrrolopyrimidines as janus kinase inhibitors
EP3170827A1 (fr) *	2011-12-15	2017-05-24	ratiopharm GmbH	Sel de mono-oxalate de tofacitinib
ES2657912T3 (es) *	2012-07-17	2018-03-07	Glaxosmithkline Intellectual Property (No. 2) Limited	Indolcarbonitrilos como moduladores selectivos de los receptores de andrógenos
WO2014016338A1 (fr)	2012-07-25	2014-01-30	Lek Pharmaceuticals D.D.	Nouvelle voie de synthèse pour la préparation de composés 3-amino-pipéridine
CN102875555A (zh) *	2012-09-27	2013-01-16	同济大学	一种JAK抑制剂Tofacitinib的合成方法
CN104955803B (zh) *	2012-11-30	2017-11-28	斯洛文尼亚莱柯制药股份有限公司	通过硝基‑四氢吡啶前体制备3‑氨基‑哌啶化合物
US9481679B2 (en)	2012-12-17	2016-11-01	Sun Pharmaceutical Industries Limited	Process for the preparation of tofacitinib and intermediates thereof
EP2938616A4 (fr) *	2012-12-28	2016-06-15	Glenmark Pharmaceuticals Ltd	Procédé de préparation de tofacitinib et d'intermédiaires
CN103073552B (zh) *	2013-02-05	2015-08-12	华润赛科药业有限责任公司	一种无定型枸橼酸托法替尼的制备方法
MY177476A (en)	2013-02-22	2020-09-16	Pfizer	Pyrrolo [2,3-d]pyrimidine derivatives as inhibitors of janus kinases (jak)
WO2014174073A1 (fr)	2013-04-26	2014-10-30	Sandoz Ag	Formulations de tofacitinib à libération prolongée
CN104447752A (zh) *	2013-09-16	2015-03-25	天津市汉康医药生物技术有限公司	一种托法替尼水合物及其制备方法
CN104447751A (zh) *	2013-09-16	2015-03-25	天津市汉康医药生物技术有限公司	一种托法替尼化合物
CN104292231B (zh) *	2013-09-17	2016-11-30	广东东阳光药业有限公司	一种枸橼酸托法替尼的制备方法
WO2015051738A1 (fr) *	2013-10-08	2015-04-16	Sunshine Lake Pharma Co., Ltd.	Citrate de tofacitinib
CN103819474A (zh) *	2013-11-04	2014-05-28	湖南华腾制药有限公司	一种托法替尼的制备方法
MD4649C1 (ro)	2013-12-05	2020-04-30	Pfizer Inc.	Pirol[2,3-d]pirimidinil, pirol[2,3-b]pirazinil şi pirol[2,3-d]piridinil acrilamide
ES2720066T3 (es)	2013-12-09	2019-07-17	Unichem Lab Ltd	Mejora del proceso de preparación de (3R,4R)-(1-bencil-4-metilpiperidín-3-il)-metilamina
CN104774206A (zh) *	2014-01-14	2015-07-15	江苏柯菲平医药股份有限公司	制备枸橼酸托伐替尼晶型a的新方法
CN103755624B (zh) *	2014-01-20	2018-10-09	上海博氏医药科技有限公司	一种哌啶衍生物的合成方法
CN105085527A (zh) *	2014-05-20	2015-11-25	南京海纳医药科技有限公司	高效合成托法替尼的方法
EP3180344B1 (fr)	2014-08-12	2019-09-18	Pfizer Inc	Dérivés de pyrrolo[2,3-d]pyrimidine utiles pour inhiber la janus kinase
KR101710127B1 (ko)	2014-08-29	2017-02-27	한화제약주식회사	야누스인산화효소 억제제로서의 치환된 N-(피롤리딘-3-일)-7H-피롤로[2,3-d]피리미딘-4-아민
MX2017002775A (es) *	2014-09-15	2017-08-10	Rugen Holdings (Cayman) Ltd	Derivados de pirrolopirimidina como antagonistas del receptor de n-metil-d-aspartato (nmda), subunidad nr2b.
CN104530053A (zh) *	2014-12-08	2015-04-22	合肥远志医药科技开发有限公司	一种药用晶型枸橼酸托法替尼的制备方法
CN104530055A (zh) *	2014-12-23	2015-04-22	南京艾德凯腾生物医药有限责任公司	枸橼酸托法替布的制备方法
CN105837574B (zh) *	2015-02-02	2018-03-02	四川大学	N‑(3‑哌啶基)‑芳香胺衍生物及其制备方法和用途
CN104710346B (zh) *	2015-02-15	2017-04-12	江苏苏利精细化工股份有限公司	一种合成顺式‑1‑苄基‑3‑甲氨基‑4‑甲基‑哌啶的方法
WO2016132341A1 (fr) *	2015-02-20	2016-08-25	Sun Pharmaceutical Industries Limited	Procédé de préparation de citrate de tofacitinib
CN104761556B (zh) *	2015-03-21	2017-06-23	河北国龙制药有限公司	托法替布中间体杂质、托法替布杂质及其合成方法，以及托法替布的质量监控方法
CN104860872A (zh) *	2015-03-27	2015-08-26	天津药物研究院有限公司	一种双-(3r,4r)-1-苄基-n,4-二甲基哌啶-3-胺l-二对甲基苯甲酰酒石酸盐的合成方法
EP3078665A1 (fr)	2015-04-10	2016-10-12	OLON S.p.A.	Procédé efficace pour la préparation de tofacitinib citrate
CN104788461A (zh) *	2015-04-30	2015-07-22	南京臣功制药股份有限公司	一种适合枸橼酸托法替尼工业化的生产方法
WO2016178110A1 (fr)	2015-05-01	2016-11-10	Pfizer Inc.	Pyrrolo [2,3-d] pyrimidinyl, pyrrolo[2,3-b] pyrazinyl, pyrrolo [2,3-b] pyridinyl acrylamides et leur époxydes
CN104987339A (zh) *	2015-07-29	2015-10-21	张燕梅	一种枸橼酸托法替布的合成方法
JP6568324B2 (ja)	2016-02-16	2019-08-28	ゾエティス・サービシーズ・エルエルシー	７Ｈ−ピロロ［２，３−ｄ］ピリミジン化合物の調製方法
CN105732641A (zh) *	2016-03-28	2016-07-06	南通常佑药业科技有限公司	一种JAKs抑制剂药物托法替尼的制备方法
CN105884781B (zh) *	2016-04-18	2018-04-20	山东罗欣药业集团股份有限公司	一种枸橼酸托法替布的制备方法
CN106146517B (zh) *	2016-06-20	2018-08-28	山东大学	一种枸橼酸托法替尼的合成方法
CN106188064A (zh) *	2016-07-07	2016-12-07	国药集团容生制药有限公司	一种N‑甲基‑N‑((3R，4R)‑4‑甲基吡啶‑3‑基)‑7H‑吡咯并[2,3‑d]嘧啶‑4‑胺的制备方法
CN105949204A (zh) *	2016-07-25	2016-09-21	国药集团容生制药有限公司	一种N-((3R，4R)-1-苄基-4-甲基吡啶-3-基)-N-甲基-7H-吡咯并[2,3-d]嘧啶-4-胺的制备方法
EP3421455B1 (fr)	2017-06-29	2019-03-27	F.I.S.- Fabbrica Italiana Sintetici S.p.A.	Procédé amélioré pour la préparation de3-amino-piperidins chiraux, des intermédiaires utiles pour la préparation de tofacitinib
CN109293682A (zh) *	2017-07-25	2019-02-01	重庆医药工业研究院有限责任公司	一种托法替布杂质及其制备方法
CN107698595A (zh) *	2017-09-23	2018-02-16	江苏正大清江制药有限公司	一种枸橼酸托法替布有关物质的制备方法
CN107793418B (zh) *	2017-10-24	2020-08-04	扬子江药业集团有限公司	一种枸橼酸托法替布的工业化生产方法
CN108640923A (zh) *	2018-07-09	2018-10-12	湖南天地恒制药有限公司	一种托法替布关键中间体的制备方法
CN108822112B (zh) *	2018-08-13	2019-12-20	山东罗欣药业集团恒欣药业有限公司	一种托法替尼化合物的制备方法
CN109608468B (zh) *	2018-12-29	2020-09-29	成都倍特药业股份有限公司	一种枸橼酸托法替布杂质及其合成方法和用途
KR102131107B1 (ko) *	2019-01-15	2020-07-07	주식회사 다산제약	3-아미노-피페리딘 화합물의 신규한 제조 방법
CN109503462B (zh) *	2019-01-21	2022-03-25	内蒙古京东药业有限公司	托法替布中间体(3r，4r)-n，4-二甲基-1-苄基-3-哌啶胺的合成方法
CN109761884B (zh) *	2019-01-30	2020-03-31	湖北扬信医药科技有限公司	一种手性胺b的制备方法及其应用
CA3132109A1 (fr)	2019-03-13	2020-09-17	Intas Pharmaceuticals Ltd.	Procede de preparation de tofacitinib et son sel pharmaceutiquement acceptable
CN113993585B (zh)	2019-03-27	2024-10-01	英矽智能科技知识产权有限公司	双环jak抑制剂及其用途
JP7515510B2 (ja) *	2019-04-05	2024-07-12	ユーハン・コーポレイション	（３ｒ，４ｒ）－１－ベンジル－ｎ，４－ジメチルピペリジン－３－アミンまたはその塩の製造方法、およびそれを使用したトファシチニブの製造方法
CN110724146B (zh) *	2019-11-04	2022-03-11	四川大学	一种枸橼酸托法替布的制备方法
CA3192099A1 (fr)	2020-08-18	2022-02-24	Incyte Corporation	Procede et intermediaires pour la preparation d'un inhibiteur de jak
WO2022040172A1 (fr)	2020-08-18	2022-02-24	Incyte Corporation	Procédé et intermédiaires pour la préparation d'un inhibiteur de jak1
CN112159410B (zh) *	2020-09-30	2025-10-17	天地恒一制药股份有限公司	一种高纯度枸橼酸托法替布的制备方法
CN114685510A (zh) *	2020-12-25	2022-07-01	上海科胜药物研发有限公司	一种托法替布中间体及其制备方法
CN114907353A (zh) *	2021-02-09	2022-08-16	明慧医药（杭州）有限公司	一种前药化合物及其制备方法和用途
CN112679508B (zh) *	2021-03-09	2021-08-10	正大天晴药业集团南京顺欣制药有限公司	一种托法替布中间体的制备方法
CN113248509B (zh) *	2021-05-17	2022-10-04	上海中西三维药业有限公司	一种枸橼酸托法替布中间体的制备方法
CN113549075B (zh) *	2021-06-23	2025-09-23	合肥华方医药科技有限公司	一种枸橼酸托法替布非对映异构体杂质的合成方法
JP2024526762A (ja)	2021-07-12	2024-07-19	インサイト・コーポレイション	Ｊａｋ阻害剤を調製するためのプロセス及び中間体
CN113735860A (zh) *	2021-08-26	2021-12-03	安徽鼎旺医药有限公司	一种枸橼酸托法替布的合成方法
CN114685515A (zh) *	2022-03-15	2022-07-01	上海蓝乐鸟实业有限公司	一种托法替尼的制备方法
CN114835714A (zh) *	2022-04-01	2022-08-02	上海蓝乐鸟实业有限公司	一种托法替尼的制备方法
CN117185884A (zh) *	2023-09-08	2023-12-08	四川大学	一种(r)-4-取代六氢嘧啶化合物的合成方法
CN117247388A (zh) *	2023-09-18	2023-12-19	天地恒一制药股份有限公司	托法替布及其中间体的制备方法和系统
CN118290348A (zh) *	2024-03-22	2024-07-05	诚达药业股份有限公司	一种4-氯吡咯并嘧啶类化合物或其衍生物的合成方法

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
JPH0710877A (ja) *	1993-06-24	1995-01-13	Teijin Ltd	４―ヘテロアリサイクリック―ピロロ［２，３―ｄ］ピリミジン
US5679683A (en) *	1994-01-25	1997-10-21	Warner-Lambert Company	Tricyclic compounds capable of inhibiting tyrosine kinases of the epidermal growth factor receptor family
UA72290C2 (uk)	1999-12-10	2005-02-15	Пфайзер Продактс Інк.	СПОЛУКИ ПІРОЛО[2.3-d]ПІРИМІДИНУ, ФАРМАЦЕВТИЧНА КОМПОЗИЦІЯ (ВАРІАНТИ), СПОСІБ ІНГІБУВАННЯ ПРОТЕЇНКІНАЗ АБО JANUS КІНАЗИ 3 (ВАРІАНТИ)
US7301023B2 (en)	2001-05-31	2007-11-27	Pfizer Inc.	Chiral salt resolution
AP2003002929A0 (en)	2001-06-23	2003-12-31	Aventis Pharma Inc	Pyrrolopyrimidines as protein kinase inhibitors
GT200200234A (es)	2001-12-06	2003-06-27		Compuestos cristalinos novedosos
US20040012627A1 (en)	2002-07-17	2004-01-22	Sany Zakharia	Configurable browser for adapting content to diverse display types
JP2006503826A (ja)	2002-09-06	2006-02-02	スミスクライン・ビーチャム・コーポレイション	ピロロ［２，３−ｄ］ピリミジン−４−イルおよびプリン−６−イル尿素化合物
AU2003278529A1 (en)	2002-11-21	2004-06-15	Pfizer Products Inc.	3-amino-piperidine derivatives and processes for their preparation
US7417055B2 (en) *	2003-04-25	2008-08-26	Gilead Sciences, Inc.	Kinase inhibitory phosphonate analogs

2006
- 2006-07-17 CN CNA2006800279013A patent/CN101233138A/zh active Pending
- 2006-07-17 US US11/996,899 patent/US8232394B2/en active Active
- 2006-07-17 DK DK06779900.7T patent/DK1913000T3/da active
- 2006-07-17 MX MX2008001334A patent/MX2008001334A/es active IP Right Grant
- 2006-07-17 PL PL06779900T patent/PL1913000T3/pl unknown
- 2006-07-17 SI SI200631245T patent/SI1913000T1/sl unknown
- 2006-07-17 NZ NZ565363A patent/NZ565363A/en not_active IP Right Cessation
- 2006-07-17 AT AT06779900T patent/ATE540952T1/de active
- 2006-07-17 SG SG201102177-1A patent/SG170783A1/en unknown
- 2006-07-17 KR KR1020087002240A patent/KR100987870B1/ko not_active Expired - Fee Related
- 2006-07-17 BR BRPI0613876-4A patent/BRPI0613876A2/pt not_active IP Right Cessation
- 2006-07-17 WO PCT/IB2006/002048 patent/WO2007012953A2/fr not_active Ceased
- 2006-07-17 CA CA2614907A patent/CA2614907C/fr active Active
- 2006-07-17 PT PT06779900T patent/PT1913000E/pt unknown
- 2006-07-17 RU RU2008103279/04A patent/RU2384583C2/ru not_active IP Right Cessation
- 2006-07-17 EP EP06779900A patent/EP1913000B1/fr active Active
- 2006-07-17 AU AU2006273762A patent/AU2006273762A1/en not_active Abandoned
- 2006-07-17 ES ES06779900T patent/ES2377771T3/es active Active
- 2006-07-27 AR ARP060103254A patent/AR056004A1/es unknown
- 2006-07-28 TW TW095127592A patent/TWI319402B/zh not_active IP Right Cessation
- 2006-07-28 JP JP2006206218A patent/JP4052523B2/ja not_active Expired - Fee Related
2007
- 2007-12-24 IL IL188372A patent/IL188372A0/en unknown
2008
- 2008-01-09 ZA ZA200800284A patent/ZA200800284B/xx unknown
2012
- 2012-02-06 CY CY20121100122T patent/CY1112319T1/el unknown
- 2012-06-20 US US13/528,099 patent/US8309716B2/en active Active

Also Published As

Publication number	Publication date
SI1913000T1 (sl)	2012-02-29
AU2006273762A1 (en)	2007-02-01
ATE540952T1 (de)	2012-01-15
IL188372A0 (en)	2008-04-13
PT1913000E (pt)	2012-02-28
KR100987870B1 (ko)	2010-10-13
WO2007012953A2 (fr)	2007-02-01
WO2007012953A3 (fr)	2007-05-18
EP1913000A2 (fr)	2008-04-23
JP2007039455A (ja)	2007-02-15
RU2384583C2 (ru)	2010-03-20
ES2377771T3 (es)	2012-03-30
CY1112319T1 (el)	2015-12-09
DK1913000T3 (da)	2012-03-12
MX2008001334A (es)	2008-03-24
NZ565363A (en)	2010-03-26
AR056004A1 (es)	2007-09-12
CA2614907A1 (fr)	2007-02-01
CN101233138A (zh)	2008-07-30
JP4052523B2 (ja)	2008-02-27
US20120259115A1 (en)	2012-10-11
PL1913000T3 (pl)	2012-05-31
US8309716B2 (en)	2012-11-13
RU2008103279A (ru)	2009-08-10
BRPI0613876A2 (pt)	2011-02-15
US8232394B2 (en)	2012-07-31
EP1913000B1 (fr)	2012-01-11
SG170783A1 (en)	2011-05-30
CA2614907C (fr)	2012-02-28
TW200745119A (en)	2007-12-16
KR20080031338A (ko)	2008-04-08
TWI319402B (en)	2010-01-11
US20110288297A1 (en)	2011-11-24

Publication	Publication Date	Title
TWI319402B (en)	2010-01-11	Pyrrolo[2,3-d]pyrimidine derivatives; their intermediates and synthesis
ZA201202025B (en)	2022-03-30	INTERMEDIATES USEFUL IN THE PREPARATION OF PYRROLO[2,3-b] PYRIDINE DERIVATIVES
TWI365189B (en)	2012-06-01	Novel pyrrolo[3,2-d]pyrimidin-4-one derivatives
IL182099A0 (en)	2007-07-24	Piperidinylamino-thieno[2,3-d] pyrimidine compounds
HUE041382T2 (hu)	2019-05-28	Pirrolo[2,3-d]pirimidin származékok janus-kináz inhibitorként
IL181386A0 (en)	2007-07-04	Pyrimidine derivatives
EP1599482A4 (fr)	2008-10-01	Derives de pyrazolo 1,5-a pyrimidine
AP2008004486A0 (en)	2008-06-30	Pyrimidine derivatives
GB0415364D0 (en)	2004-08-11	Pyrimidine derivatives
IL194010A (en)	2015-10-29	Pyrzolido [4,3– d] derivatives, pyrimidine containing preparations and their use
IL177259A0 (en)	2006-12-10	Heteroaryl -fused pyrazolo derivatives
IL192236A0 (en)	2008-12-29	Aryl-isoxazol-4-yl-imidazo[1,5-a]pyridine derivatives
IL186939A0 (en)	2008-02-09	Pyrimidine derivatives and their use as
IL185912A0 (en)	2008-01-06	Novel 5-substituted 7-amino-[1,3]thiazolo[4,5-d]pyrimidine derivatives
IL190446A0 (en)	2008-11-03	2-amino-7,8-dihydro-6h-pyrido[4,3-d]
GB0525080D0 (en)	2006-01-18	Pyrimidine derivatives
GB0525083D0 (en)	2006-01-18	Pyrimidine derivatives
IL170680A0 (en)	2009-02-11	8 - SUBSTITUTED - 6,7,8,9 -TETRAHYDROPYRIMIDO [1,2-a] PYRIMIDIN - 4 - ONE DERIVATIVES
ZA200507192B (en)	2007-03-28	Substituted 8-perfluoroalkyl-6,7,8,9-tetrahydropyrimido [1,2-A] pyrimidin-4-one derivatives
GB0415367D0 (en)	2004-08-11	Pyrimidine derivatives
IL198239A0 (en)	2009-12-24	Substituted 8-piperidinyl-2-pyridinyl-pyrimido [1,2-a] pyrimidin -6- one and 8-piperidinyl-2- pyrimidinyl [1,2-a] pyrimidin -6- one derivatives
SI1957492T1 (sl)	2011-02-28	Substituirani biciklični pirimidonski derivati
ZA200803658B (en)	2009-09-30	2-amino-7,8-dihydro-6H-pyrido[4,3-d] pyrimidin-5-ones
IL182147A0 (en)	2007-07-24	Efficient synthesis of 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones
PT2020410E (pt)	2014-03-20	Derivados de pirido[2,3-d]pirimidina, sua preparação, sua aplicação em terapêutica