CN101679440A - 作为jak3抑制剂的吡咯并嘧啶衍生物 - Google Patents

作为jak3抑制剂的吡咯并嘧啶衍生物 Download PDF

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Publication number
CN101679440A
CN101679440A CN200880015843A CN200880015843A CN101679440A CN 101679440 A CN101679440 A CN 101679440A CN 200880015843 A CN200880015843 A CN 200880015843A CN 200880015843 A CN200880015843 A CN 200880015843A CN 101679440 A CN101679440 A CN 101679440A
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J·萨拉斯索拉那
C·阿曼萨罗萨勒斯
R·索利瓦索利瓦
M·方特斯尤斯特尔
M·温德尔埃斯克巴
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Palau Pharma SA
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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
    • 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
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Pulmonology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • Oncology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CN200880015843A 2007-04-02 2008-03-31 作为jak3抑制剂的吡咯并嘧啶衍生物 Pending CN101679440A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP07380088 2007-04-02
EP07380088.0 2007-04-02
PCT/EP2008/053842 WO2008119792A1 (en) 2007-04-02 2008-03-31 Pyrrolopyrimidine derivatives as jak3 inhibitors

Publications (1)

Publication Number Publication Date
CN101679440A true CN101679440A (zh) 2010-03-24

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CN200880015843A Pending CN101679440A (zh) 2007-04-02 2008-03-31 作为jak3抑制剂的吡咯并嘧啶衍生物

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US (1) US20110160185A9 (enExample)
EP (1) EP2142550A1 (enExample)
JP (1) JP2010523522A (enExample)
KR (1) KR20100015353A (enExample)
CN (1) CN101679440A (enExample)
AR (1) AR065901A1 (enExample)
AU (1) AU2008234822A1 (enExample)
BR (1) BRPI0809992A2 (enExample)
CA (1) CA2682646A1 (enExample)
CL (1) CL2008000946A1 (enExample)
IL (1) IL201073A0 (enExample)
MX (1) MX2009010595A (enExample)
PE (1) PE20090996A1 (enExample)
RU (1) RU2009140319A (enExample)
TW (1) TW200904442A (enExample)
WO (1) WO2008119792A1 (enExample)

Cited By (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102985425A (zh) * 2010-07-09 2013-03-20 利奥制药有限公司 作为蛋白酪氨酸激酶抑制剂的新的高哌嗪衍生物及其医药用途
WO2014111037A1 (zh) * 2013-01-18 2014-07-24 上海昀怡健康管理咨询有限公司 五元并六元杂环化合物、其制备方法、药物组合物和应用
CN104876934A (zh) * 2015-05-12 2015-09-02 山东大学 一种含氮杂环苯基哌啶类化合物及其制备方法与应用
WO2015143692A1 (en) * 2014-03-28 2015-10-01 Changzhou Jiekai Pharmatech Co., Ltd. Heterocyclic compounds as axl inhibitors
CN105732636A (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
CN107074867A (zh) * 2014-08-21 2017-08-18 辉瑞公司 作为jak抑制剂的氨基嘧啶基化合物
CN107667108A (zh) * 2015-05-28 2018-02-06 施万生物制药研发Ip有限责任公司 作为jak激酶抑制剂的萘啶化合物
CN110183471A (zh) * 2019-05-21 2019-08-30 江苏大学 一种新型哌嗪类衍生物及制备方法及应用
WO2021000884A1 (zh) * 2019-07-04 2021-01-07 沈阳药科大学 2-氨基嘧啶类化合物及其用途
CN116528869A (zh) * 2020-11-27 2023-08-01 安锐生物医药科技(广州)有限公司 氨基杂芳基激酶抑制剂
CN116783198A (zh) * 2020-12-02 2023-09-19 百极弘烨（广东）医药科技有限公司 螺环jak抑制剂、含其的药物组合物及其应用
WO2024099229A1 (zh) * 2022-11-09 2024-05-16 沈阳药科大学 2-氨基嘧啶类化合物及其用途

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WO2009026107A1 (en) 2007-08-17 2009-02-26 Portola Pharmaceuticals, Inc. Protein kinase inhibitors
US8138339B2 (en) 2008-04-16 2012-03-20 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
US8063058B2 (en) 2008-04-16 2011-11-22 Portola Pharmaceuticals, Inc. Inhibitors of syk and JAK protein kinases
WO2009131687A2 (en) * 2008-04-22 2009-10-29 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
TW201024298A (en) * 2008-09-23 2010-07-01 Palau Pharma Sa (R)-3-(N,N-dimethylamino)pyrrolidine derivatives
CN102232076B (zh) * 2008-12-05 2014-12-31 霍夫曼-拉罗奇有限公司 吡咯并吡嗪基脲激酶抑制剂
HRP20150701T1 (hr) * 2009-06-08 2015-08-28 Takeda Pharmaceutical Company Limited Spojevi dihidropirolonaftiridinona kao inhibitori jak
TWI466885B (zh) * 2009-07-31 2015-01-01 Japan Tobacco Inc 含氮螺環化合物及其醫藥用途
AU2010311378B2 (en) * 2009-10-29 2014-04-24 Vectura Limited N-containing heteroaryl derivatives as JAK3 kinase inhibitors
JP5749341B2 (ja) 2010-08-20 2015-07-15 ハチソン メディファーマ リミテッド ピロロピリミジン化合物およびその使用
WO2012030924A1 (en) * 2010-09-01 2012-03-08 Ambit Biosciences Corporation Azolopyridine and azolopyrimidine compounds and methods of use thereof
WO2012030912A1 (en) * 2010-09-01 2012-03-08 Ambit Biosciences Corporation 7-cyclylquinazoline derivatives and methods of use thereof
JP6039683B2 (ja) 2011-11-23 2016-12-07 ポートラ ファーマシューティカルズ， インコーポレイテッド ピラジンキナーゼ阻害剤
WO2014013014A1 (en) 2012-07-18 2014-01-23 Fundació Privada Centre De Regulació Genòmica (Crg) Jak inhibitors for activation of epidermal stem cell populations
KR101657616B1 (ko) * 2013-05-24 2016-09-19 주식회사유한양행 피리미딘 고리를 포함하는 바이사이클릭 유도체 및 그의 제조방법
CN105315285B (zh) * 2014-07-25 2017-12-08 上海海雁医药科技有限公司 2,4‑二取代7H‑吡咯并[2,3‑d]嘧啶衍生物、其制法与医药上的用途
EP3778605A3 (en) 2015-02-13 2021-03-10 Dana Farber Cancer Institute, Inc. Lrrk2 inhibitors and methods of making and using the same
US10550126B2 (en) 2015-10-16 2020-02-04 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-A]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
US11773106B2 (en) 2015-10-16 2023-10-03 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
SG10201913989QA (en) 2015-10-16 2020-03-30 Abbvie Inc PROCESSES FOR THE PREPARATION OF (3S,4R)-3-ETHYL-4-(3H-IMIDAZO[1,2-a]PYRROLO[2,3-e]-PYRAZIN-8-YL)-N-(2,2,2-TRIFLUOROETHYL)PYRROLIDINE-1-CARBOXAMIDE AND SOLID STATE FORMS THEREOF
US11365198B2 (en) 2015-10-16 2022-06-21 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
US12365689B2 (en) 2015-10-16 2025-07-22 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
JOP20190024A1 (ar) 2016-08-26 2019-02-19 Gilead Sciences Inc مركبات بيروليزين بها استبدال واستخداماتها
WO2018041989A1 (en) 2016-09-02 2018-03-08 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for diagnosing and treating refractory celiac disease type 2
JP7050165B2 (ja) 2018-02-26 2022-04-07 ギリアード サイエンシーズ， インコーポレイテッド Ｈｂｖ複製阻害剤としての置換ピロリジン化合物
CN110526915B (zh) * 2018-05-25 2022-02-01 首药控股(北京)股份有限公司 一种间变性淋巴瘤激酶抑制剂的制备方法
MX2021005334A (es) * 2018-11-05 2021-06-23 Avista Pharma Solutions Inc Compuestos quimicos.
EP3947737A2 (en) 2019-04-02 2022-02-09 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods of predicting and preventing cancer in patients having premalignant lesions
WO2020212395A1 (en) 2019-04-16 2020-10-22 INSERM (Institut National de la Santé et de la Recherche Médicale) Use of jak inhibitors for the treatment of painful conditions involving nav1.7 channels
KR20200133188A (ko) * 2019-05-17 2020-11-26 보로노이바이오 주식회사 헤테로고리 융합 피리미딘 유도체 및 이의 용도
KR102666918B1 (ko) * 2021-04-08 2024-05-20 주식회사 스탠다임 신규한 lrrk2 억제제
US20250283174A1 (en) 2022-05-16 2025-09-11 Institut National de la Santé et de la Recherche Médicale Methods for assessing the exhaustion of hematopoietic stem cells induced by chronic inflammation
JP2025522733A (ja) * 2022-06-29 2025-07-17 アルコン インコーポレイテッド アゼチジニルピリミジンおよびｊａｋ阻害剤としてのその使用

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Cited By (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102985425A (zh) * 2010-07-09 2013-03-20 利奥制药有限公司 作为蛋白酪氨酸激酶抑制剂的新的高哌嗪衍生物及其医药用途
US9745320B2 (en) 2013-01-18 2017-08-29 Guangzhou Maxinovel Pharmaceuticals Co., Ltd. Five-and-six-membered heterocyclic compound, and preparation method, pharmaceutical composition and use thereof
WO2014111037A1 (zh) * 2013-01-18 2014-07-24 上海昀怡健康管理咨询有限公司 五元并六元杂环化合物、其制备方法、药物组合物和应用
CN106458914B (zh) * 2014-03-28 2020-01-14 常州捷凯医药科技有限公司 作为axl抑制剂的杂环化合物
WO2015143692A1 (en) * 2014-03-28 2015-10-01 Changzhou Jiekai Pharmatech Co., Ltd. Heterocyclic compounds as axl inhibitors
CN106458914A (zh) * 2014-03-28 2017-02-22 常州捷凯医药科技有限公司 作为axl抑制剂的杂环化合物
CN107074867B (zh) * 2014-08-21 2019-10-22 辉瑞公司 作为jak抑制剂的氨基嘧啶基化合物
CN107074867A (zh) * 2014-08-21 2017-08-18 辉瑞公司 作为jak抑制剂的氨基嘧啶基化合物
CN105732636B (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
CN105732636A (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
CN104876934A (zh) * 2015-05-12 2015-09-02 山东大学 一种含氮杂环苯基哌啶类化合物及其制备方法与应用
CN107667108B (zh) * 2015-05-28 2020-05-12 施万生物制药研发Ip有限责任公司 作为jak激酶抑制剂的萘啶化合物
CN107667108A (zh) * 2015-05-28 2018-02-06 施万生物制药研发Ip有限责任公司 作为jak激酶抑制剂的萘啶化合物
AU2020202181B2 (en) * 2015-05-28 2021-07-01 Theravance Biopharma R&D Ip, Llc Naphthyridine compounds as jak kinase inhibitors
CN110183471A (zh) * 2019-05-21 2019-08-30 江苏大学 一种新型哌嗪类衍生物及制备方法及应用
CN110183471B (zh) * 2019-05-21 2022-02-15 江苏大学 一种哌嗪类衍生物及制备方法及应用
WO2021000884A1 (zh) * 2019-07-04 2021-01-07 沈阳药科大学 2-氨基嘧啶类化合物及其用途
CN113891881A (zh) * 2019-07-04 2022-01-04 沈阳药科大学 2-氨基嘧啶类化合物及其用途
CN116528869A (zh) * 2020-11-27 2023-08-01 安锐生物医药科技(广州)有限公司 氨基杂芳基激酶抑制剂
CN116783198A (zh) * 2020-12-02 2023-09-19 百极弘烨（广东）医药科技有限公司 螺环jak抑制剂、含其的药物组合物及其应用
WO2024099229A1 (zh) * 2022-11-09 2024-05-16 沈阳药科大学 2-氨基嘧啶类化合物及其用途

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US20110160185A9 (en) 2011-06-30
AU2008234822A1 (en) 2008-10-09
US20100113420A1 (en) 2010-05-06
WO2008119792A1 (en) 2008-10-09
CL2008000946A1 (es) 2008-10-10
CA2682646A1 (en) 2008-10-09
KR20100015353A (ko) 2010-02-12
JP2010523522A (ja) 2010-07-15
PE20090996A1 (es) 2009-07-15
EP2142550A1 (en) 2010-01-13
MX2009010595A (es) 2009-10-22
IL201073A0 (en) 2010-05-17
RU2009140319A (ru) 2011-05-10
AR065901A1 (es) 2009-07-08
TW200904442A (en) 2009-02-01
BRPI0809992A2 (pt) 2014-10-14

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