CN109563097A - 一种7H-吡咯并[2,3-d]嘧啶类化合物的晶型、盐型及其制备方法 - Google Patents

一种7H-吡咯并[2,3-d]嘧啶类化合物的晶型、盐型及其制备方法 Download PDF

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CN109563097A
CN109563097A CN201780045482.4A CN201780045482A CN109563097A CN 109563097 A CN109563097 A CN 109563097A CN 201780045482 A CN201780045482 A CN 201780045482A CN 109563097 A CN109563097 A CN 109563097A
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CN109563097B (zh
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毛魏魏
吴颢
郭强
郑学建
廖勇刚
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WUXI FORTUNE PHARMACEUTICAL CO LTD
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • 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
    • A61K31/275—Nitriles; Isonitriles
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07—Optical isomers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline 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)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Physics & Mathematics (AREA)
  • Condensed Matter Physics & Semiconductors (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • General Physics & Mathematics (AREA)

Abstract

本发明公开了一种7H‑吡咯并[2,3‑d]嘧啶类化合物晶型、盐型及其制备方法，还包括所述晶型和盐型在制备治疗关节炎药物中的应用。

Description

PCT国内申请，说明书已公开。

Claims (20)

  1. PCT国内申请，权利要求书已公开。
CN201780045482.4A 2016-11-23 2017-11-23 一种7H-吡咯并[2,3-d]嘧啶类化合物的晶型、盐型及其制备方法 Active CN109563097B (zh)

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CN201611046683.X 2016-11-23
CN201611046683 2016-11-23
PCT/CN2017/112493 WO2018095345A1 (zh) 2016-11-23 2017-11-23 一种7H-吡咯并[2,3-d]嘧啶类化合物的晶型、盐型及其制备方法

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CN109563097A true CN109563097A (zh) 2019-04-02
CN109563097B CN109563097B (zh) 2021-05-14

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US (1) US10774094B2 (zh)
EP (1) EP3511333B1 (zh)
JP (1) JP6788114B2 (zh)
KR (1) KR102136958B1 (zh)
CN (1) CN109563097B (zh)
AU (1) AU2017366375B2 (zh)
CA (1) CA3033456C (zh)
DK (1) DK3511333T3 (zh)
EA (1) EA039655B1 (zh)
ES (1) ES2882214T3 (zh)
HU (1) HUE055530T2 (zh)
MX (1) MX2019002077A (zh)
PL (1) PL3511333T3 (zh)
PT (1) PT3511333T (zh)
UA (1) UA123709C2 (zh)
WO (1) WO2018095345A1 (zh)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN115867273A (zh) * 2020-09-29 2023-03-28 广州白云山医药集团股份有限公司白云山制药总厂 吡啶并吡唑类化合物的晶型及其制备方法

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111039963B (zh) * 2019-12-31 2021-03-19 卓和药业集团有限公司 Wxfl10203614水溶性类似物及其合成方法
CN113372366B (zh) * 2020-12-04 2022-08-30 广州嘉越医药科技有限公司 一种吡咯并嘧啶类化合物的盐、其晶型及其应用

Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999051599A1 (en) * 1998-04-02 1999-10-14 Neurogen Corporation Aminoalkyl substituted pyrrolo[2,3-b]pyridine and pyrrolo[2,3-d]pyrimidine derivatives: modulators of crf1 receptors
JP2003516405A (ja) * 1999-12-10 2003-05-13 ファイザー・プロダクツ・インク ピロロ［２，３−ｄ］ピリミジン化合物
JP2005511696A (ja) * 2001-12-06 2005-04-28 ファイザー・プロダクツ・インク 新規結晶性化合物
WO2012022045A1 (en) * 2010-08-20 2012-02-23 Hutchison Medipharma Limited Pyrrolopyrimidine compounds and uses thereof
JP2012219099A (ja) * 2011-04-08 2012-11-12 Pfizer Inc 結晶性ピロロ［２，３−ｄ］ピリミジン化合物
WO2015193168A1 (en) * 2014-06-17 2015-12-23 Ucb Biopharma Sprl Fused bicyclic heteroaromatic derivatives as kinase inhibitors
CN105367576A (zh) * 2014-08-15 2016-03-02 正大天晴药业集团股份有限公司 作为tlr7激动剂的吡咯并嘧啶化合物
WO2016054959A1 (zh) * 2014-10-09 2016-04-14 江苏恒瑞医药股份有限公司 一种jak激酶抑制剂的硫酸氢盐的结晶形式及其制备方法
WO2016192563A1 (zh) * 2015-05-29 2016-12-08 南京明德新药研发股份有限公司 Janus激酶抑制剂

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT3077395T (pt) 2013-12-05 2018-01-03 Pfizer Pirrolo[2,3-d]pirimidinilo, pirrolo[2,3-b]pirazinilo e pirrolo[2,3-d]piridinilo acrilamidas
CN104144337B (zh) 2014-08-05 2016-07-06 深圳市华星光电技术有限公司 一种多视点立体显示器的图像显示方法及装置

Patent Citations (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999051599A1 (en) * 1998-04-02 1999-10-14 Neurogen Corporation Aminoalkyl substituted pyrrolo[2,3-b]pyridine and pyrrolo[2,3-d]pyrimidine derivatives: modulators of crf1 receptors
JP2003516405A (ja) * 1999-12-10 2003-05-13 ファイザー・プロダクツ・インク ピロロ［２，３−ｄ］ピリミジン化合物
JP2005511696A (ja) * 2001-12-06 2005-04-28 ファイザー・プロダクツ・インク 新規結晶性化合物
WO2012022045A1 (en) * 2010-08-20 2012-02-23 Hutchison Medipharma Limited Pyrrolopyrimidine compounds and uses thereof
JP2012219099A (ja) * 2011-04-08 2012-11-12 Pfizer Inc 結晶性ピロロ［２，３−ｄ］ピリミジン化合物
WO2015193168A1 (en) * 2014-06-17 2015-12-23 Ucb Biopharma Sprl Fused bicyclic heteroaromatic derivatives as kinase inhibitors
CN105367576A (zh) * 2014-08-15 2016-03-02 正大天晴药业集团股份有限公司 作为tlr7激动剂的吡咯并嘧啶化合物
WO2016054959A1 (zh) * 2014-10-09 2016-04-14 江苏恒瑞医药股份有限公司 一种jak激酶抑制剂的硫酸氢盐的结晶形式及其制备方法
WO2016192563A1 (zh) * 2015-05-29 2016-12-08 南京明德新药研发股份有限公司 Janus激酶抑制剂
CN107531711A (zh) * 2015-05-29 2018-01-02 无锡福祈制药有限公司 Janus激酶抑制剂

Non-Patent Citations (6)

* Cited by examiner, † Cited by third party
Title
G. STEFFEN PAULEKUHN，ET AL.: "Trends in Active Pharmaceutical Ingredient Salt Selection based on Analysis of the Orange Book Database", 《J. MED. CHEM.》 *
HARRY G. BRITTAIN: "《Polymorphism in Pharmaceutical Solids》", 31 December 2009 *
STEPHEN M. BERGE，ET AL.: "Pharmaceutical Salts", 《JOURNAL OF PHARMACEUTICAL SCIENCES》 *
YI LIU，ET AL.: "Synthesis and antitumor activity of a novel series of 6-substituted pyrrolo[2,3-d]pyrimidines as potential nonclassical antifolates targeting both thymidylate and purine nucleotide biosynthesis", 《EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY》 *
杨千姣 等: "治疗类风湿关节炎选择性JAK抑制剂的研究进展", 《中国新药杂志》 *
白光清主编: "《药物晶型专利保护》", 30 April 2016 *

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN115867273A (zh) * 2020-09-29 2023-03-28 广州白云山医药集团股份有限公司白云山制药总厂 吡啶并吡唑类化合物的晶型及其制备方法

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MX2019002077A (es) 2019-05-15
EP3511333A1 (en) 2019-07-17
KR20190037291A (ko) 2019-04-05
DK3511333T3 (da) 2021-08-02
AU2017366375B2 (en) 2020-12-03
EA201990364A1 (ru) 2019-10-31
UA123709C2 (uk) 2021-05-19
US20190218231A1 (en) 2019-07-18
JP2019535771A (ja) 2019-12-12
KR102136958B1 (ko) 2020-08-26
CN109563097B (zh) 2021-05-14
PT3511333T (pt) 2021-08-02
CA3033456A1 (en) 2018-05-31
EA039655B1 (ru) 2022-02-22
JP6788114B2 (ja) 2020-11-18
AU2017366375A1 (en) 2019-04-18
US10774094B2 (en) 2020-09-15
PL3511333T3 (pl) 2021-12-06
ES2882214T3 (es) 2021-12-01
HUE055530T2 (hu) 2021-12-28
EP3511333B1 (en) 2021-05-12
EP3511333A4 (en) 2019-08-28
CA3033456C (en) 2021-03-09
WO2018095345A1 (zh) 2018-05-31

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