CN115667228A - 杂芳类衍生物的盐、晶型及其制备方法 - Google Patents

杂芳类衍生物的盐、晶型及其制备方法 Download PDF

Info

Publication number
CN115667228A
CN115667228A CN202180035951.0A CN202180035951A CN115667228A CN 115667228 A CN115667228 A CN 115667228A CN 202180035951 A CN202180035951 A CN 202180035951A CN 115667228 A CN115667228 A CN 115667228A
Authority
CN
China
Prior art keywords
acid
amino
degrees
methyl
pyrazol
Prior art date
Legal status (The legal status 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 status listed.)
Pending
Application number
CN202180035951.0A
Other languages
English (en)
Inventor
李媛媛
呙临松
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.)
Jiangsu Hansoh Pharmaceutical Group Co Ltd
Shanghai Hansoh Biomedical Co Ltd
Original Assignee
Jiangsu Hansoh Pharmaceutical Group Co Ltd
Shanghai Hansoh Biomedical Co Ltd
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.)
Filing date
Publication date
Application filed by Jiangsu Hansoh Pharmaceutical Group Co Ltd, Shanghai Hansoh Biomedical Co Ltd filed Critical Jiangsu Hansoh Pharmaceutical Group Co Ltd
Publication of CN115667228A publication Critical patent/CN115667228A/zh
Pending legal-status Critical Current

Links

Images

Classifications

    • 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
    • A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
    • 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
    • A61K31/46—8-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
    • 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
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/78—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/14—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing 9-azabicyclo [3.3.1] nonane ring systems, e.g. granatane, 2-aza-adamantane; Cyclic acetals thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (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)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Emergency Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

本发明涉及一种含杂芳类衍生物的盐及晶型。具体涉及一种具有通式(I)化合物盐及晶型、制备方法和含有治疗有效量的该晶型的药物组合物，及其作为JAK激酶抑制剂，在治疗类风湿性关节炎、皮炎、银屑病、炎症性肠病等炎症性疾病及结肠癌、非小细胞肺癌等肿瘤疾病的用途。
Figure DDA0003948282740000011

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。
CN202180035951.0A 2020-05-25 2021-05-25 杂芳类衍生物的盐、晶型及其制备方法 Pending CN115667228A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN202010451845 2020-05-25
CN2020104518458 2020-05-25
PCT/CN2021/095767 WO2021238908A1 (zh) 2020-05-25 2021-05-25 杂芳类衍生物的盐、晶型及其制备方法

Publications (1)

Publication Number Publication Date
CN115667228A true CN115667228A (zh) 2023-01-31

Family

ID=78745577

Family Applications (1)

Application Number Title Priority Date Filing Date
CN202180035951.0A Pending CN115667228A (zh) 2020-05-25 2021-05-25 杂芳类衍生物的盐、晶型及其制备方法

Country Status (3)

Country Link
CN (1) CN115667228A (zh)
TW (1) TW202144366A (zh)
WO (1) WO2021238908A1 (zh)

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102066338A (zh) * 2008-04-22 2011-05-18 波托拉医药品公司 蛋白激酶抑制剂
CN103242341A (zh) * 2013-04-19 2013-08-14 中国科学院广州生物医药与健康研究院 噻吩并2，4取代嘧啶类化合物及其药物组合物与应用
WO2015094803A1 (en) * 2013-12-16 2015-06-25 Calitor Sciences, Llc Substituted heteroaryl compounds and methods of use
CN105367555A (zh) * 2014-08-07 2016-03-02 广东东阳光药业有限公司 取代的杂芳基化合物及其组合物和用途
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

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111511738B (zh) * 2018-11-30 2023-01-20 江苏豪森药业集团有限公司 杂芳类衍生物调节剂、其制备方法和应用

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102066338A (zh) * 2008-04-22 2011-05-18 波托拉医药品公司 蛋白激酶抑制剂
CN103242341A (zh) * 2013-04-19 2013-08-14 中国科学院广州生物医药与健康研究院 噻吩并2，4取代嘧啶类化合物及其药物组合物与应用
WO2015094803A1 (en) * 2013-12-16 2015-06-25 Calitor Sciences, Llc Substituted heteroaryl compounds and methods of use
CN105367555A (zh) * 2014-08-07 2016-03-02 广东东阳光药业有限公司 取代的杂芳基化合物及其组合物和用途
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

Also Published As

Publication number Publication date
WO2021238908A1 (zh) 2021-12-02
TW202144366A (zh) 2021-12-01

Similar Documents

Publication Publication Date Title
CN111511738B (zh) 杂芳类衍生物调节剂、其制备方法和应用
JP7373992B2 (ja) 過剰増殖性疾患の治療のための置換ピラゾール化合物およびそれらの使用方法
US11629148B2 (en) Substituted pyrrolo[3,4-d]imidazoles as JAK inhibitors
EP3092226B1 (en) Indazole compounds as irak4 inhibitors
KR102376354B1 (ko) 6-(5-히드록시-1h-피라졸-1-일)니코틴아미드 유도체 및 ｐｈｄ의 저해제로서의 그의 용도
EP2382207B1 (en) Pi3k/mtor kinase inhibitors
AU2007270814B2 (en) Pyrazole derivatives as cytochrome P450 inhibitors
CN115232154A (zh) 杂环类衍生物抑制剂、其制备方法和应用
CN111601804B (zh) 含氮杂芳类衍生物调节剂、其制备方法和应用
CN104837829A (zh) 抑制剂化合物
AU2020385527B2 (en) Compound used as EGFR kinase inhibitor and use thereof
CN115315423A (zh) 取代芳基类化合物
US20230134869A1 (en) Crystal form of free alkali of nitrogen-containing aromatic derivatives
CA3047137A1 (en) Poly-adp ribose polymerase (parp) inhibitors
CN117177744A (zh) Cdk2抑制剂及其使用方法
CN113493440A (zh) 含氮杂芳类衍生物的盐及其晶型
WO2023081637A1 (en) Fused tetracyclic quinazoline derivatives as inhibitors of erbb2
CN115667228A (zh) 杂芳类衍生物的盐、晶型及其制备方法
CN112574208B (zh) 取代的稠合三环衍生物及其组合物及用途
CN113717194A (zh) 杂芳类衍生物的盐及其制备方法
CN113717202A (zh) 杂芳类衍生物的自由碱晶型及其制备方法
WO2023077259A1 (en) Fused tetracyclic quinazoline derivatives as inhibitors of erbb2
CN111868060A (zh) 二氢吡啶并酞嗪酮衍生物、其制备方法及应用
WO2022152259A1 (zh) Cdk2/4/6抑制剂及其制备方法和应用
CN113493439B (zh) 取代的丙烯酰胺衍生物及其组合物及用途

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 40085921

Country of ref document: HK