CN113226312A - (3s)-3-[2-(6-氨基-2-氟吡啶-3-基)-4-氟-1h-咪唑-5-基]-7-[5-氯-2-(1h-四唑-1-基)苯基]-2,3-二氢吲哚嗪-5(1h)-酮的新型晶体 - Google Patents

(3s)-3-[2-(6-氨基-2-氟吡啶-3-基)-4-氟-1h-咪唑-5-基]-7-[5-氯-2-(1h-四唑-1-基)苯基]-2,3-二氢吲哚嗪-5(1h)-酮的新型晶体 Download PDF

Info

Publication number
CN113226312A
CN113226312A CN201980079268.XA CN201980079268A CN113226312A CN 113226312 A CN113226312 A CN 113226312A CN 201980079268 A CN201980079268 A CN 201980079268A CN 113226312 A CN113226312 A CN 113226312A
Authority
CN
China
Prior art keywords
compound
acid
fluoro
chloro
imidazol
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
CN201980079268.XA
Other languages
English (en)
Chinese (zh)
Inventor
藤户贵之
小野静香
大谷修平
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.)
Ono Pharmaceutical Co Ltd
Original Assignee
Ono Pharmaceutical 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 Ono Pharmaceutical Co Ltd filed Critical Ono Pharmaceutical Co Ltd
Publication of CN113226312A publication Critical patent/CN113226312A/zh
Pending legal-status Critical Current

Links

Images

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/38Cellulose; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0087Galenical forms not covered by A61K9/02 - A61K9/7023
    • A61K9/0095Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Hematology (AREA)
  • Molecular Biology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Dermatology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Inorganic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CN201980079268.XA 2018-11-30 2019-11-29 (3s)-3-[2-(6-氨基-2-氟吡啶-3-基)-4-氟-1h-咪唑-5-基]-7-[5-氯-2-(1h-四唑-1-基)苯基]-2,3-二氢吲哚嗪-5(1h)-酮的新型晶体 Pending CN113226312A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
JP2018224434 2018-11-30
JP2018-224434 2018-11-30
PCT/JP2019/046893 WO2020111268A1 (ja) 2018-11-30 2019-11-29 (3s)-3-[2-(6-アミノ-2-フルオロピリジン-3-イル)-4-フルオロ-1h-イミダゾール-5-イル]-7-[5-クロロ-2-(1h-テトラゾール-1-イル)フェニル]-2,3-ジヒドロインドリジン-5(1h)-オンの新規結晶

Publications (1)

Publication Number Publication Date
CN113226312A true CN113226312A (zh) 2021-08-06

Family

ID=70853323

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201980079268.XA Pending CN113226312A (zh) 2018-11-30 2019-11-29 (3s)-3-[2-(6-氨基-2-氟吡啶-3-基)-4-氟-1h-咪唑-5-基]-7-[5-氯-2-(1h-四唑-1-基)苯基]-2,3-二氢吲哚嗪-5(1h)-酮的新型晶体

Country Status (16)

Country Link
US (1) US20210395250A1 (enExample)
EP (1) EP3888653A4 (enExample)
JP (1) JP7196931B2 (enExample)
KR (1) KR20210097119A (enExample)
CN (1) CN113226312A (enExample)
AU (1) AU2019390094A1 (enExample)
BR (1) BR112021010476A2 (enExample)
CA (1) CA3121447A1 (enExample)
IL (1) IL283481A (enExample)
MX (1) MX2021006147A (enExample)
NZ (1) NZ776666A (enExample)
PH (1) PH12021551219A1 (enExample)
SG (1) SG11202105697SA (enExample)
TW (1) TWI826599B (enExample)
WO (1) WO2020111268A1 (enExample)
ZA (1) ZA202103692B (enExample)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2023179624A1 (zh) * 2022-03-21 2023-09-28 上海济煜医药科技有限公司 三并环类化合物制备方法及其中间体

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20240108639A1 (en) * 2020-12-11 2024-04-04 Board Of Regents, The University Of Texas System Compositions and methods of making cocrystals using dielectric heating with dispersive and distributive mixing
JP2024125436A (ja) * 2021-07-20 2024-09-19 小野薬品工業株式会社 イミダゾール化合物の製造方法

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2015500868A (ja) * 2011-12-21 2015-01-08 小野薬品工業株式会社 第XIa因子阻害剤としての新規ピリジノンおよびピリミジノン誘導体
CN107001363A (zh) * 2014-12-10 2017-08-01 小野药品工业株式会社 二氢吲嗪酮衍生物
JP2017218449A (ja) * 2016-06-06 2017-12-14 小野薬品工業株式会社 ジヒドロインドリジノン誘導体を含有する医薬組成物

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2016093285A (ja) 2014-11-13 2016-05-26 株式会社ユニバーサルエンターテインメント 遊技機

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2015500868A (ja) * 2011-12-21 2015-01-08 小野薬品工業株式会社 第XIa因子阻害剤としての新規ピリジノンおよびピリミジノン誘導体
CN107001363A (zh) * 2014-12-10 2017-08-01 小野药品工业株式会社 二氢吲嗪酮衍生物
JP2017218449A (ja) * 2016-06-06 2017-12-14 小野薬品工業株式会社 ジヒドロインドリジノン誘導体を含有する医薬組成物

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2023179624A1 (zh) * 2022-03-21 2023-09-28 上海济煜医药科技有限公司 三并环类化合物制备方法及其中间体

Also Published As

Publication number Publication date
SG11202105697SA (en) 2021-06-29
ZA202103692B (en) 2023-03-29
PH12021551219A1 (en) 2021-11-08
TWI826599B (zh) 2023-12-21
TW202039485A (zh) 2020-11-01
CA3121447A1 (en) 2020-06-04
KR20210097119A (ko) 2021-08-06
NZ776666A (en) 2024-11-29
JP7196931B2 (ja) 2022-12-27
EP3888653A4 (en) 2022-08-24
MX2021006147A (es) 2021-06-23
BR112021010476A2 (pt) 2021-08-24
WO2020111268A1 (ja) 2020-06-04
EP3888653A1 (en) 2021-10-06
IL283481A (en) 2021-07-29
AU2019390094A1 (en) 2021-06-17
JPWO2020111268A1 (ja) 2021-10-14
US20210395250A1 (en) 2021-12-23

Similar Documents

Publication Publication Date Title
US20230138003A1 (en) Dihydroindolizinone derivative
JP7196931B2 (ja) (3s)-3-[2-(6-アミノ-2-フルオロピリジン-3-イル)-4-フルオロ-1h-イミダゾール-5-イル]-7-[5-クロロ-2-(1h-テトラゾール-1-イル)フェニル]-2,3-ジヒドロインドリジン-5(1h)-オンの新規結晶
JP6992284B2 (ja) ジヒドロインドリジノン誘導体を含有する医薬組成物
HK40056300A (en) Novel crystal of (3s)-3-[2-(6-amino-2-fluoropyridine-3-yl)-4-fluoro-1h-imidazole-5-yl]-7-[5-chloro-2-(1h-tetrazole-1-yl)phenyl]-2,3-dihydroindolizine-5(1h)-one
EP3854783A1 (en) Novel salt of 4-(\{(4s)-1-(4-carbamimidoylbenzoyl)-4-[4-(methylsulfonyl)piperazin-1-yl]-l-prolyl\}amino)benzoic acid, and and novel crystal form of said salt
HK1236193A (en) Dihydroindolizinone derivative
HK1236193B (zh) 二氢吲嗪酮衍生物

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: 40056300

Country of ref document: HK

AD01 Patent right deemed abandoned

Effective date of abandoning: 20241022

AD01 Patent right deemed abandoned