CN102822177A - 吡咯并[2,3-d]嘧啶脲化合物 - Google Patents

吡咯并[2,3-d]嘧啶脲化合物 Download PDF

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Publication number
CN102822177A
CN102822177A CN2011800171067A CN201180017106A CN102822177A CN 102822177 A CN102822177 A CN 102822177A CN 2011800171067 A CN2011800171067 A CN 2011800171067A CN 201180017106 A CN201180017106 A CN 201180017106A CN 102822177 A CN102822177 A CN 102822177A
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CN
China
Prior art keywords
compound
jak
methyl
disease
compounds
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Pending
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CN2011800171067A
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English (en)
Chinese (zh)
Inventor
T.A.约翰逊
A.芬维克
G.M.凯恩
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Zoetis LLC
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Pfizer Inc
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Publication of CN102822177A publication Critical patent/CN102822177A/zh
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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
    • 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
    • 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
    • A61P17/04—Antipruritics
    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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
    • A61P35/00—Antineoplastic agents
    • 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
    • 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
    • A61P37/08—Antiallergic agents

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Ophthalmology & Optometry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CN2011800171067A 2010-02-05 2011-01-24 吡咯并[2,3-d]嘧啶脲化合物 Pending CN102822177A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US30191510P 2010-02-05 2010-02-05
US61/301,915 2010-02-05
PCT/US2011/022216 WO2011097087A1 (en) 2010-02-05 2011-01-24 Pyrrolo [ 2, 3 - d] pyrimidine urea compounds as jak inhibitors

Publications (1)

Publication Number Publication Date
CN102822177A true CN102822177A (zh) 2012-12-12

Family

ID=43629121

Family Applications (1)

Application Number Title Priority Date Filing Date
CN2011800171067A Pending CN102822177A (zh) 2010-02-05 2011-01-24 吡咯并[2,3-d]嘧啶脲化合物

Country Status (9)

Country Link
US (1) US20120309776A1 (https=)
EP (1) EP2531508A1 (https=)
JP (1) JP2013518882A (https=)
CN (1) CN102822177A (https=)
AU (1) AU2011213198B2 (https=)
BR (1) BR112012019511A2 (https=)
CA (1) CA2788071A1 (https=)
MX (1) MX2012009074A (https=)
WO (1) WO2011097087A1 (https=)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103896946A (zh) * 2012-12-28 2014-07-02 浙江导明医药科技有限公司 用于预防及治疗多种自身免疫疾病的新化合物
CN105732637A (zh) * 2014-12-30 2016-07-06 广东东阳光药业有限公司 杂芳化合物及其在药物中的应用
CN108290918A (zh) * 2015-11-24 2018-07-17 施万生物制药研发Ip有限责任公司 用于治疗胃肠发炎疾病的jak抑制剂化合物的前药

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EP2455382B1 (en) 2005-12-13 2016-10-26 Incyte Holdings Corporation Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as Janus kinase inhibitors
EP2895172B1 (en) 2012-09-12 2019-02-06 Rigel Pharmaceuticals, Inc. Treatment for vitiligo
CN113384546A (zh) 2012-11-15 2021-09-14 因赛特公司 鲁索利替尼的缓释剂型
EP2951590A1 (en) 2013-02-04 2015-12-09 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for assaying jak2 activity in red blood cells and uses thereof
US20140343034A1 (en) * 2013-04-25 2014-11-20 Japan Tobacco Inc. Skin barrier function improving agent
EP3006445B1 (en) * 2013-06-07 2017-11-15 Jiangsu Hengrui Medicine Co. Ltd. Bisulfate of janus kinase (jak) inhibitor and preparation method therefor
SG10201801069QA (en) 2013-08-07 2018-03-28 Incyte Corp Sustained release dosage forms for a jak1 inhibitor
WO2017013270A1 (en) 2015-07-23 2017-01-26 Universite De Strasbourg Use of leptin signaling inhibitor for protecting kidneys from patients having ciliopathy
WO2017143014A1 (en) 2016-02-16 2017-08-24 Brian Kim Jak inhibitors and uses thereof
US10472366B2 (en) 2017-03-08 2019-11-12 Theravance Biopharma R&D Ip, Llc Glucuronide prodrugs of tofacitinib
WO2018167283A1 (en) 2017-03-17 2018-09-20 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for the diagnosis and treatment of pancreatic ductal adenocarcinoma associated neural remodeling
WO2018189335A1 (en) 2017-04-13 2018-10-18 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for the diagnosis and treatment of pancreatic ductal adenocarcinoma
BR112019024509A2 (pt) 2017-05-23 2020-06-23 Theravance Biopharma R&D Ip, Llc Glicuronídeo de pró-fármacos dos inibidores da janus quinase
WO2018217699A1 (en) 2017-05-23 2018-11-29 Theravance Biopharma R&D Ip, Llc Thiocarbamate prodrugs of tofacitinib
WO2020092015A1 (en) 2018-11-02 2020-05-07 University Of Rochester Therapeutic mitigation of epithelial infection
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms

Citations (5)

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CN1141298A (zh) * 1995-06-07 1997-01-29 美国辉瑞有限公司 杂环稠合嘧啶衍生物
WO2002000661A1 (en) * 2000-06-26 2002-01-03 Pfizer Products Inc. PYRROLO[2,3-d]PYRIMIDINE COMPOUNDS AS IMMUNOSUPPRESSIVE AGENTS
CN1443155A (zh) * 2000-06-30 2003-09-17 艾兰制药公司 治疗早老性痴呆的化合物
WO2008029237A2 (en) * 2006-09-05 2008-03-13 Pfizer Products Inc. Combination therapies for rheumatoid arthritis
CN101233138A (zh) * 2005-07-29 2008-07-30 辉瑞产品公司 吡咯并[2，3-d]嘧啶衍生物、其中间体和合成方法

Family Cites Families (6)

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PA8474101A1 (es) 1998-06-19 2000-09-29 Pfizer Prod Inc Compuestos de pirrolo [2,3-d] pirimidina
BR9911365A (pt) 1998-06-19 2001-03-13 Pfizer Prod Inc Compostos pirrolo[2,3-d]pirimidina
EP1382339B1 (en) 1999-12-10 2007-12-05 Pfizer Products Inc. Compositions containing pyrrolo ¬2,3-d pyrimidine derivatives
US7301023B2 (en) 2001-05-31 2007-11-27 Pfizer Inc. Chiral salt resolution
KR100678800B1 (ko) 2002-11-21 2007-02-05 화이자 프로덕츠 인코포레이티드 3-아미노-피페리딘 유도체 및 그의 제조 방법
US7732237B2 (en) 2005-06-27 2010-06-08 The Regents Of The University Of California Quantum dot based optoelectronic device and method of making same

Patent Citations (6)

* Cited by examiner, † Cited by third party
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CN1141298A (zh) * 1995-06-07 1997-01-29 美国辉瑞有限公司 杂环稠合嘧啶衍生物
WO2002000661A1 (en) * 2000-06-26 2002-01-03 Pfizer Products Inc. PYRROLO[2,3-d]PYRIMIDINE COMPOUNDS AS IMMUNOSUPPRESSIVE AGENTS
CN1439010A (zh) * 2000-06-26 2003-08-27 辉瑞产品公司 吡咯并[2,3－d]嘧啶化合物作为免疫抑制剂
CN1443155A (zh) * 2000-06-30 2003-09-17 艾兰制药公司 治疗早老性痴呆的化合物
CN101233138A (zh) * 2005-07-29 2008-07-30 辉瑞产品公司 吡咯并[2，3-d]嘧啶衍生物、其中间体和合成方法
WO2008029237A2 (en) * 2006-09-05 2008-03-13 Pfizer Products Inc. Combination therapies for rheumatoid arthritis

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
SCOTT N. VANDERWEL,等: "Pyrido[2,3-d]pyrimidin-7-ones as Specific Inhibitors of Cyclin-Dependent Kinase 4", 《J. MED. CHEM.》 *

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103896946A (zh) * 2012-12-28 2014-07-02 浙江导明医药科技有限公司 用于预防及治疗多种自身免疫疾病的新化合物
CN103896946B (zh) * 2012-12-28 2018-04-03 浙江导明医药科技有限公司 用于预防及治疗多种自身免疫疾病的新化合物
CN105732637A (zh) * 2014-12-30 2016-07-06 广东东阳光药业有限公司 杂芳化合物及其在药物中的应用
CN105732637B (zh) * 2014-12-30 2020-04-21 广东东阳光药业有限公司 杂芳化合物及其在药物中的应用
CN108290918A (zh) * 2015-11-24 2018-07-17 施万生物制药研发Ip有限责任公司 用于治疗胃肠发炎疾病的jak抑制剂化合物的前药
CN108290918B (zh) * 2015-11-24 2021-06-08 施万生物制药研发Ip有限责任公司 用于治疗胃肠发炎疾病的jak抑制剂化合物的前药

Also Published As

Publication number Publication date
CA2788071A1 (en) 2011-08-11
JP2013518882A (ja) 2013-05-23
BR112012019511A2 (pt) 2016-08-23
MX2012009074A (es) 2012-08-23
EP2531508A1 (en) 2012-12-12
AU2011213198A1 (en) 2012-08-09
AU2011213198B2 (en) 2014-04-24
WO2011097087A1 (en) 2011-08-11
US20120309776A1 (en) 2012-12-06

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Application publication date: 20121212