CN107001378A - 吡咯并嘧啶化合物 - Google Patents

吡咯并嘧啶化合物 Download PDF

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Publication number
CN107001378A
CN107001378A CN201580066687.1A CN201580066687A CN107001378A CN 107001378 A CN107001378 A CN 107001378A CN 201580066687 A CN201580066687 A CN 201580066687A CN 107001378 A CN107001378 A CN 107001378A
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China
Prior art keywords
methyl
compound
alkyl
nhco
pyrimidine
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CN201580066687.1A
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CN107001378B (zh
Inventor
祝力
校登明
胡远东
戴丽光
段小伟
孙颖慧
彭勇
孔凡胜
罗鸿
韩永信
杨玲
王善春
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Capital Pharmaceutical Holdings Beijing Co ltd
Chia Tai Tianqing Pharmaceutical Group Co Ltd
Lianyungang Runzhong Pharmaceutical Co Ltd
Original Assignee
Chia Tai Tianqing Pharmaceutical Group Co Ltd
Lianyungang Runzhong Pharmaceutical Co Ltd
Shouyao Holdings Beijing Co Ltd
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Priority to CN201910594361.6A priority Critical patent/CN111018861B/zh
Publication of CN107001378A publication Critical patent/CN107001378A/zh
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    • 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
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

本申请涉及药物化学领域，具体涉及如式I所示的吡咯并嘧啶化合物、其立体异构体、其药学上可接受的盐。本申请还涉及制备如式I所示的吡咯并嘧啶化合物的方法、药物组合物、以及该化合物在治疗两面神激酶介导的疾病中的用途。

Description

PCT国内申请，说明书已公开。

Claims (21)

  1. PCT国内申请，权利要求书已公开。
CN201580066687.1A 2014-12-16 2015-12-15 吡咯并嘧啶化合物 Active CN107001378B (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201910594361.6A CN111018861B (zh) 2014-12-16 2015-12-15 吡咯并嘧啶化合物

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN2014107844612 2014-12-16
CN201410784461.2A CN105777754B (zh) 2014-12-16 2014-12-16 吡咯并嘧啶化合物
PCT/CN2015/097411 WO2016095805A1 (zh) 2014-12-16 2015-12-15 吡咯并嘧啶化合物

Related Child Applications (1)

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CN201910594361.6A Division CN111018861B (zh) 2014-12-16 2015-12-15 吡咯并嘧啶化合物

Publications (2)

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CN107001378A true CN107001378A (zh) 2017-08-01
CN107001378B CN107001378B (zh) 2019-08-16

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CN201410784461.2A Active CN105777754B (zh) 2014-12-16 2014-12-16 吡咯并嘧啶化合物
CN201580066687.1A Active CN107001378B (zh) 2014-12-16 2015-12-15 吡咯并嘧啶化合物
CN201910594361.6A Active CN111018861B (zh) 2014-12-16 2015-12-15 吡咯并嘧啶化合物

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US (1) US10561657B2 (zh)
EP (1) EP3235819B1 (zh)
JP (2) JP6684803B2 (zh)
KR (1) KR102634308B1 (zh)
CN (3) CN105777754B (zh)
AU (1) AU2015366636B2 (zh)
CA (1) CA2971114C (zh)
DK (1) DK3235819T3 (zh)
ES (1) ES2847051T3 (zh)
HU (1) HUE053463T2 (zh)
RU (1) RU2701206C2 (zh)
WO (1) WO2016095805A1 (zh)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN108368115B (zh) * 2015-12-15 2020-01-03 正大天晴药业集团股份有限公司 吡咯并嘧啶化合物的盐
CN107513067A (zh) * 2016-06-16 2017-12-26 北京赛林泰医药技术有限公司 含有取代环戊基的吡咯并嘧啶化合物
CN107759600A (zh) * 2016-06-16 2018-03-06 正大天晴药业集团股份有限公司 作为jak抑制剂的吡咯并嘧啶化合物的结晶
CN107513069A (zh) * 2016-06-16 2017-12-26 正大天晴药业集团股份有限公司 手性吡咯并嘧啶化合物的制备方法
CN109651424B (zh) * 2017-10-11 2021-01-22 新发药业有限公司 一种7-保护基-4-(1-氢-吡唑-4-基)吡咯[2,3-d]嘧啶的合成方法
CN113149993A (zh) * 2017-12-01 2021-07-23 北京普祺医药科技有限公司 一种吡咯并嘧啶衍生的化合物、药物组合物以及其用途
JP2022515272A (ja) * 2018-12-24 2022-02-17 チア タイ ティエンチン ファーマシューティカル グループ カンパニー リミテッド ピロロピリミジン化合物の治療的使用およびその固形医薬組成物
EP4119562A4 (en) * 2020-03-09 2024-04-24 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. USE OF A PYRROLOPYRIMIDINE COMPOUND FOR THE TREATMENT OF HEMOPHAGOCYTIC SYNDROME
WO2021236139A1 (en) * 2020-05-21 2021-11-25 Concert Pharmaceuticals, Inc. Novel deuterated jak inhibitor and uses thereof
CN114085224A (zh) * 2020-08-25 2022-02-25 北京普祺医药科技有限公司 一种吡咯并嘧啶化合物的制备方法
WO2022268083A1 (zh) * 2021-06-21 2022-12-29 正大天晴药业集团股份有限公司 吡咯并嘧啶化合物及其药物组合物治疗慢性移植物抗宿主病的用途
WO2023179547A1 (zh) * 2022-03-21 2023-09-28 正大天晴药业集团股份有限公司 吡咯并嘧啶化合物治疗中高危骨髓纤维化的用途
WO2024027790A1 (zh) * 2022-08-04 2024-02-08 正大天晴药业集团股份有限公司 吡咯并嘧啶化合物治疗急性移植物抗宿主病的用途

Citations (4)

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CN101448826A (zh) * 2005-12-13 2009-06-03 因塞特公司 作为两面神激酶抑制剂的杂芳基取代的吡咯并[2,3-b]吡咯和吡咯并[2,3-b]嘧啶
CN102026999A (zh) * 2008-03-11 2011-04-20 因塞特公司 作为jak抑制剂的氮杂环丁烷和环丁烷衍生物
US20140343034A1 (en) * 2013-04-25 2014-11-20 Japan Tobacco Inc. Skin barrier function improving agent
CN105218548A (zh) * 2014-06-09 2016-01-06 上海海和药物研究开发有限公司 一种新型杂环化合物及其制备方法和作为激酶抑制剂的用途

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AU2007235487A1 (en) 2006-04-05 2007-10-18 Vertex Pharmaceuticals Incorporated Deazapurines useful as inhibitors of janus kinases
CL2009001884A1 (es) 2008-10-02 2010-05-14 Incyte Holdings Corp Uso de 3-ciclopentil-3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il)propanonitrilo, inhibidor de janus quinasa, y uso de una composición que lo comprende para el tratamiento del ojo seco.
BR112012008267B1 (pt) * 2009-10-09 2022-10-04 Incyte Holdings Corporation Derivados hidroxila, ceto e glucuronida de 3-(4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1- il)-3-ciclopentilpropanonitrila
WO2011130146A1 (en) * 2010-04-14 2011-10-20 Array Biopharma Inc. 5, 7-substituted-imidazo [1, 2-c] pyrimidines as inhibitors of jak kinases
US9089574B2 (en) * 2011-11-30 2015-07-28 Emory University Antiviral JAK inhibitors useful in treating or preventing retroviral and other viral infections
US20130310340A1 (en) 2012-05-16 2013-11-21 Rigel Pharmaceuticals, Inc. Method of treating muscular degradation
CN110229159B (zh) * 2013-12-18 2021-08-24 康塞特医药品有限公司 卢索替尼的氘代衍生物

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101448826A (zh) * 2005-12-13 2009-06-03 因塞特公司 作为两面神激酶抑制剂的杂芳基取代的吡咯并[2,3-b]吡咯和吡咯并[2,3-b]嘧啶
CN102026999A (zh) * 2008-03-11 2011-04-20 因塞特公司 作为jak抑制剂的氮杂环丁烷和环丁烷衍生物
US20140343034A1 (en) * 2013-04-25 2014-11-20 Japan Tobacco Inc. Skin barrier function improving agent
CN105218548A (zh) * 2014-06-09 2016-01-06 上海海和药物研究开发有限公司 一种新型杂环化合物及其制备方法和作为激酶抑制剂的用途

Also Published As

Publication number Publication date
EP3235819A4 (en) 2017-11-01
RU2017122824A (ru) 2019-01-18
CA2971114C (en) 2023-03-21
RU2701206C2 (ru) 2019-09-25
CN105777754B (zh) 2019-07-26
WO2016095805A1 (zh) 2016-06-23
CN107001378B (zh) 2019-08-16
CN105777754A (zh) 2016-07-20
CA2971114A1 (en) 2016-06-23
RU2017122824A3 (zh) 2019-03-28
KR102634308B1 (ko) 2024-02-06
JP2017537950A (ja) 2017-12-21
ES2847051T3 (es) 2021-07-30
US10561657B2 (en) 2020-02-18
DK3235819T3 (da) 2020-12-07
CN111018861B (zh) 2021-11-19
EP3235819B1 (en) 2020-11-18
US20190201403A1 (en) 2019-07-04
HUE053463T2 (hu) 2021-06-28
JP6684803B2 (ja) 2020-04-22
AU2015366636A1 (en) 2017-07-27
AU2015366636B2 (en) 2020-03-12
CN111018861A (zh) 2020-04-17
KR20170095310A (ko) 2017-08-22
JP2020105206A (ja) 2020-07-09
EP3235819A1 (en) 2017-10-25

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Address after: 222062 Yuzhou South Road, Haizhou District, Lianyungang, Jiangsu 369

Applicant after: Chia Tai Tianqing Pharmaceutical Group Co., Ltd.

Applicant after: Capital Pharmaceutical Holdings (Beijing) Co., Ltd.

Applicant after: Lianyungang Runzhong Pharmaceutical Co.,Ltd.

Address before: 222062 Yuzhou South Road, Haizhou District, Lianyungang, Jiangsu 369

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Address after: 222062 No. 369 Yuzhou South Road, Lianyungang City, Jiangsu Province

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Patentee after: Chia Tai Tianqing Pharmaceutical Group Co., Ltd.

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Address before: 222062, No. 369, Yu Nan Road, Haizhou District, Jiangsu, Lianyungang

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Address after: No. 369, Yuzhou South Road, Lianyungang, Jiangsu Province

Patentee after: CHIA TAI TIANQING PHARMACEUTICAL GROUP Co.,Ltd.

Patentee after: Capital Pharmaceutical Holdings (Beijing) Co.,Ltd.

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Patentee before: CHIA TAI TIANQING PHARMACEUTICAL GROUP Co.,Ltd.

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Patentee before: LIANYUNGANG RUNZHONG PHARMACEUTICAL Co.,Ltd.