JP7529667B2 - 改善された特性を有するメチル｛４，６－ジアミノ－２－［５－フルオロ－１－（２－フルオロベンジル）－１ｈ－ピラゾロ［３，４－ｂ］ピリジン－３－イル］ピリミジン－５－イル｝カルバメート活性化合物生成物、その製造及び製剤化 - Google Patents

改善された特性を有するメチル｛４，６－ジアミノ－２－［５－フルオロ－１－（２－フルオロベンジル）－１ｈ－ピラゾロ［３，４－ｂ］ピリジン－３－イル］ピリミジン－５－イル｝カルバメート活性化合物生成物、その製造及び製剤化 Download PDF

Info

Publication number
JP7529667B2
JP7529667B2 JP2021534766A JP2021534766A JP7529667B2 JP 7529667 B2 JP7529667 B2 JP 7529667B2 JP 2021534766 A JP2021534766 A JP 2021534766A JP 2021534766 A JP2021534766 A JP 2021534766A JP 7529667 B2 JP7529667 B2 JP 7529667B2
Authority
JP
Japan
Prior art keywords
active compound
wetting agent
formula
water
methyl
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.)
Active
Application number
JP2021534766A
Other languages
English (en)
Japanese (ja)
Other versions
JP2022515376A5 (https=
JP2022515376A (ja
Inventor
ペーター・フェイ
ミヒャル・ゾヴァ
イェルク・ブロッコプ
マルクス・ロンゲリッヒ
グイド・ベッカー
ハイケ・ノイマン
Original Assignee
アドヴェリオ・ファーマ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツング
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 アドヴェリオ・ファーマ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツング filed Critical アドヴェリオ・ファーマ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツング
Publication of JP2022515376A publication Critical patent/JP2022515376A/ja
Publication of JP2022515376A5 publication Critical patent/JP2022515376A5/ja
Application granted granted Critical
Publication of JP7529667B2 publication Critical patent/JP7529667B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicinal Preparation (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2021534766A 2018-12-17 2019-12-16 改善された特性を有するメチル｛４，６－ジアミノ－２－［５－フルオロ－１－（２－フルオロベンジル）－１ｈ－ピラゾロ［３，４－ｂ］ピリジン－３－イル］ピリミジン－５－イル｝カルバメート活性化合物生成物、その製造及び製剤化 Active JP7529667B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP18213115 2018-12-17
EP18213115.1 2018-12-17
PCT/EP2019/085255 WO2020126983A1 (en) 2018-12-17 2019-12-16 Methyl {4,6-diamino-2-[5-fluoro-1-(2-fluorobenzyl)-1h-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}carbamate active compound product having improved properties, production and formulation thereof

Publications (3)

Publication Number Publication Date
JP2022515376A JP2022515376A (ja) 2022-02-18
JP2022515376A5 JP2022515376A5 (https=) 2022-12-26
JP7529667B2 true JP7529667B2 (ja) 2024-08-06

Family

ID=64744472

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2021534766A Active JP7529667B2 (ja) 2018-12-17 2019-12-16 改善された特性を有するメチル｛４，６－ジアミノ－２－［５－フルオロ－１－（２－フルオロベンジル）－１ｈ－ピラゾロ［３，４－ｂ］ピリジン－３－イル］ピリミジン－５－イル｝カルバメート活性化合物生成物、その製造及び製剤化

Country Status (19)

Country Link
US (1) US12172996B2 (https=)
EP (1) EP3898624A1 (https=)
JP (1) JP7529667B2 (https=)
KR (1) KR102872983B1 (https=)
CN (1) CN113207290B (https=)
AR (1) AR116912A1 (https=)
AU (1) AU2019409269B2 (https=)
BR (1) BR112021009122A2 (https=)
CA (1) CA3123360A1 (https=)
CL (1) CL2021001580A1 (https=)
CO (1) CO2021007668A2 (https=)
IL (1) IL283976B2 (https=)
JO (1) JOP20210155B1 (https=)
MX (1) MX2021007090A (https=)
PE (1) PE20211593A1 (https=)
SG (1) SG11202104953VA (https=)
TW (1) TWI830835B (https=)
UA (1) UA129677C2 (https=)
WO (1) WO2020126983A1 (https=)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI830835B (zh) 2018-12-17 2024-02-01 德商亞德維瑞醫藥有限公司 具改善性質之{4,6-二胺基-2-[5-氟-1-(2-氟芐基)-1H-吡唑並[3,4-b]吡啶-3-基]嘧啶-5-基}胺基甲酸甲酯活性化合物產物、其製造及調配物
EP4099987B1 (en) 2020-02-03 2025-03-12 Adverio Pharma GmbH Nanoformulations of methyl {4,6-diamino-2-[5-fluoro-1-(2-fluorobenzyl)-1h-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}carbamate
EP3925953A1 (en) 2020-06-16 2021-12-22 Adverio Pharma GmbH Process for preparing methyl {4,6-diamino-2-[5-fluoro-1-(2-fluorobenzyl)-1h-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}carbamate
WO2025114276A1 (en) 2023-12-01 2025-06-05 Krka, D.D., Novo Mesto Solid oral composition comprising vericiguat

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013076168A1 (de) 2011-11-25 2013-05-30 Bayer Pharma Aktiengesellschaft Verfahren zur herstellung von substituierten 5-fluor-1h-pyrazolopyridinen

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2745813B1 (fr) 1996-03-07 1998-05-07 Rhone Poulenc Chimie Agglomerats spheriques d'acide 10-phenothiazinylpropanoique et leur procede de preparation
DE19834044A1 (de) 1998-07-29 2000-02-03 Bayer Ag Neue substituierte Pyrazolderivate
UY33041A (es) 2009-11-27 2011-06-30 Bayer Schering Pharma Aktienegesellschaft Procedimiento para la preparaciòn de {4,6-diamino-2-[1-(2-fluorobencil)-1h-pirazolo[3,4-b]piridin-3-il]pirimidin-5-il}carbamato de metilo y su purificaciòn para el uso como principio activo farmacèutico
PL2604608T3 (pl) 2009-11-27 2016-02-29 Adverio Pharma Gmbh Sposób wytwarzania {4,6-diamino-2-[1-(2-fluorobenzylo)-1H-pirazolo[3,4-b]pirydyn-3-ylo]pirymidyn-5-ylo}metylokarbaminianu metylu
DE102010021637A1 (de) 2010-05-26 2011-12-01 Bayer Schering Pharma Aktiengesellschaft Substituierte 5-Fluor-1H-Pyrazolopyridine und ihre Verwendung
MX2015010725A (es) * 2013-02-21 2016-05-31 Adverio Pharma Gmbh Formas de metil {4,6-diamino-2-[1-(2-fluorobencil)-1h-pirazolo [3,4-b] piridino-3-il] pirimidino-5-il} metil carbamato.
PL2792682T3 (pl) 2013-04-19 2017-04-28 Zach System Sposób wytwarzania stałej postaci octanu abirateronu
WO2016113415A1 (en) * 2015-01-16 2016-07-21 Sandoz Ag Process for the preparation of riociguat essentially free from genotoxic impurities
WO2017025981A1 (en) * 2015-08-13 2017-02-16 Msn Laboratories Private Limited Process for the preparation of methyl 4,6-diamino-2-[l-(2-fhiorobenzvr)-lh-pyrazolo i3,4-blpvridin-3-vn-5-pyrimidinyl(methvl)carbamate and its polymorphs thereof
TWI830835B (zh) 2018-12-17 2024-02-01 德商亞德維瑞醫藥有限公司 具改善性質之{4,6-二胺基-2-[5-氟-1-(2-氟芐基)-1H-吡唑並[3,4-b]吡啶-3-基]嘧啶-5-基}胺基甲酸甲酯活性化合物產物、其製造及調配物
CN113272286B (zh) 2019-01-22 2024-04-16 阿德弗里奥药品有限责任公司 制备4-(2,2,3,3-四氟丙基)吗啉的方法
EP4099987B1 (en) * 2020-02-03 2025-03-12 Adverio Pharma GmbH Nanoformulations of methyl {4,6-diamino-2-[5-fluoro-1-(2-fluorobenzyl)-1h-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}carbamate
EP3925953A1 (en) * 2020-06-16 2021-12-22 Adverio Pharma GmbH Process for preparing methyl {4,6-diamino-2-[5-fluoro-1-(2-fluorobenzyl)-1h-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}carbamate

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013076168A1 (de) 2011-11-25 2013-05-30 Bayer Pharma Aktiengesellschaft Verfahren zur herstellung von substituierten 5-fluor-1h-pyrazolopyridinen

Also Published As

Publication number Publication date
MX2021007090A (es) 2021-08-11
PE20211593A1 (es) 2021-08-18
CL2021001580A1 (es) 2021-12-03
SG11202104953VA (en) 2021-06-29
JOP20210155B1 (ar) 2025-10-01
AU2019409269A1 (en) 2021-06-03
IL283976B1 (en) 2024-12-01
TW202039488A (zh) 2020-11-01
IL283976B2 (en) 2025-04-01
CN113207290A (zh) 2021-08-03
JOP20210155A1 (ar) 2023-01-30
EP3898624A1 (en) 2021-10-27
KR102872983B1 (ko) 2025-10-17
BR112021009122A2 (pt) 2021-08-10
US20220048907A1 (en) 2022-02-17
UA129677C2 (uk) 2025-07-02
WO2020126983A1 (en) 2020-06-25
IL283976A (en) 2021-07-29
CA3123360A1 (en) 2020-06-25
JP2022515376A (ja) 2022-02-18
AR116912A1 (es) 2021-06-23
AU2019409269B2 (en) 2025-04-03
TWI830835B (zh) 2024-02-01
CO2021007668A2 (es) 2021-07-19
CN113207290B (zh) 2024-04-09
KR20210104703A (ko) 2021-08-25
US12172996B2 (en) 2024-12-24

Similar Documents

Publication Publication Date Title
JP7529667B2 (ja) 改善された特性を有するメチル｛４，６－ジアミノ－２－［５－フルオロ－１－（２－フルオロベンジル）－１ｈ－ピラゾロ［３，４－ｂ］ピリジン－３－イル］ピリミジン－５－イル｝カルバメート活性化合物生成物、その製造及び製剤化
US11911511B2 (en) Anticancer compositions
KR20240096691A (ko) 결정성 의약품의 제조
EA023286B1 (ru) Способ получения полиморфной формы i эторикоксиба
RU2818488C2 (ru) Продукт активного соединения метил { 4,6-диамино-2-[5-фтор-1-(2-фторбензил)-1H-пиразоло[3,4-b]пиридин-3-ил]пиримидин-5-ил} карбамата, имеющий улучшенные свойства, его получение и состав
HK40050973B (zh) 具有改善的特性的活性化合物产品、其制备和制剂
HK40050973A (en) Active compound product having improved properties, production and formulation thereof
JP2026504517A (ja) 改善された溶解性を示す新規バモロロン製剤
WO2023174937A1 (en) Particles comprising non-crystalline odevixibat
US20210332073A1 (en) Process for the preparation of ferric citrate
HK40066972A (en) Anticancer compositions

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20221216

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20221216

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20230925

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20231225

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20240205

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20240402

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20240701

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20240725

R150 Certificate of patent or registration of utility model

Ref document number: 7529667

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150