KR102928815B1 - 혈장 칼리크레인 억제제의 공정-스케일 합성 - Google Patents

혈장 칼리크레인 억제제의 공정-스케일 합성

Info

Publication number
KR102928815B1
KR102928815B1 KR1020227003932A KR20227003932A KR102928815B1 KR 102928815 B1 KR102928815 B1 KR 102928815B1 KR 1020227003932 A KR1020227003932 A KR 1020227003932A KR 20227003932 A KR20227003932 A KR 20227003932A KR 102928815 B1 KR102928815 B1 KR 102928815B1
Authority
KR
South Korea
Prior art keywords
compound
salt
acid
solvent
combining
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
KR1020227003932A
Other languages
English (en)
Korean (ko)
Other versions
KR20220044276A (ko
Inventor
야햐 엘-카탄
얄라가다 에스. 바부
Original Assignee
바이오크리스트파마슈티컬즈,인코포레이티드
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 바이오크리스트파마슈티컬즈,인코포레이티드 filed Critical 바이오크리스트파마슈티컬즈,인코포레이티드
Publication of KR20220044276A publication Critical patent/KR20220044276A/ko
Application granted granted Critical
Publication of KR102928815B1 publication Critical patent/KR102928815B1/ko
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C253/00—Preparation of carboxylic acid nitriles
    • C07C253/30—Preparation of carboxylic acid nitriles by reactions not involving the formation of cyano groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00—Carboxylic acid nitriles
    • C07C255/49—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C255/58—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2602/00—Systems containing two condensed rings
    • C07C2602/02—Systems containing two condensed rings the rings having only two atoms in common

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Physical Or Chemical Processes And Apparatus (AREA)
KR1020227003932A 2019-08-06 2020-08-05 혈장 칼리크레인 억제제의 공정-스케일 합성 Active KR102928815B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962883396P 2019-08-06 2019-08-06
US62/883,396 2019-08-06
PCT/US2020/044921 WO2021026182A1 (en) 2019-08-06 2020-08-05 Process-scale synthesis of a plasma kallikrein inhibitor

Publications (2)

Publication Number Publication Date
KR20220044276A KR20220044276A (ko) 2022-04-07
KR102928815B1 true KR102928815B1 (ko) 2026-02-19

Family

ID=74504082

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020227003932A Active KR102928815B1 (ko) 2019-08-06 2020-08-05 혈장 칼리크레인 억제제의 공정-스케일 합성

Country Status (26)

Country Link
US (1) US12503443B2 (enExample)
EP (1) EP4010320A4 (enExample)
JP (1) JP7626751B2 (enExample)
KR (1) KR102928815B1 (enExample)
CN (1) CN114206839B (enExample)
AR (1) AR119617A1 (enExample)
AU (1) AU2020324422B2 (enExample)
BR (1) BR112022002060A2 (enExample)
CA (1) CA3149176A1 (enExample)
CL (2) CL2022000264A1 (enExample)
CO (1) CO2022002392A2 (enExample)
CR (1) CR20220092A (enExample)
DO (1) DOP2022000027A (enExample)
EC (1) ECSP22016209A (enExample)
GE (2) GEAP202515893A (enExample)
IL (1) IL290113B2 (enExample)
JO (1) JOP20220021A1 (enExample)
MX (1) MX2022001608A (enExample)
PE (1) PE20221009A1 (enExample)
PH (1) PH12022550221A1 (enExample)
PY (1) PY2042865A (enExample)
TN (1) TN2022000028A1 (enExample)
TW (1) TWI881995B (enExample)
UA (1) UA130182C2 (enExample)
UY (1) UY38826A (enExample)
WO (1) WO2021026182A1 (enExample)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
LT3113772T (lt) 2014-03-07 2020-12-28 Biocryst Pharmaceuticals, Inc. Trifluormetilo pakeistieji pirazolai kaip žmogaus plazmos kalikreino inhibitoriai
UY38438A (es) 2018-11-02 2020-05-29 Biocryst Pharm Inc Sales cristalinas de un inhibidor de calicreína plasmática
EP4010320A4 (en) 2019-08-06 2023-08-16 Biocryst Pharmaceuticals, Inc. Process-scale synthesis of a plasma kallikrein inhibitor
CN116375648A (zh) * 2023-03-22 2023-07-04 苏州农平科技发展有限公司 贝罗司他中间体的制备方法

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20020037857A1 (en) 2000-08-11 2002-03-28 Corvas International, Inc. Non-covalent inhibitors of urokinase and blood vessel formation
US20130296245A1 (en) 2010-11-08 2013-11-07 Shanghai Institute Of Pharmaceutical Industry Prolinamiade derivatives as thrombin inhibitor, prepraration method and application thereof

Family Cites Families (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4559157A (en) 1983-04-21 1985-12-17 Creative Products Resource Associates, Ltd. Cosmetic applicator useful for skin moisturizing
LU84979A1 (fr) 1983-08-30 1985-04-24 Oreal Composition cosmetique ou pharmaceutique sous forme aqueuse ou anhydre dont la phase grasse contient un polyether oligomere et polyethers oligomeres nouveaux
LU86084A1 (fr) 1985-09-20 1987-04-02 Faco Sa Apparei de massage electrique
US5102417A (en) 1985-11-07 1992-04-07 Expandable Grafts Partnership Expandable intraluminal graft, and method and apparatus for implanting an expandable intraluminal graft
US4800882A (en) 1987-03-13 1989-01-31 Cook Incorporated Endovascular stent and delivery system
US4820508A (en) 1987-06-23 1989-04-11 Neutrogena Corporation Skin protective composition
US4886062A (en) 1987-10-19 1989-12-12 Medtronic, Inc. Intravascular radially expandable stent and method of implant
US4992478A (en) 1988-04-04 1991-02-12 Warner-Lambert Company Antiinflammatory skin moisturizing composition and method of preparing same
US4938949A (en) 1988-09-12 1990-07-03 University Of New York Treatment of damaged bone marrow and dosage units therefor
WO1990013332A1 (en) 1989-05-11 1990-11-15 Cedars-Sinai Medical Center Stent with sustained drug delivery
WO1991012779A1 (en) 1990-02-28 1991-09-05 Medtronic, Inc. Intralumenal drug eluting prosthesis
US5429634A (en) 1993-09-09 1995-07-04 Pdt Systems Biogenic implant for drug delivery and method
US5419760A (en) 1993-01-08 1995-05-30 Pdt Systems, Inc. Medicament dispensing stent for prevention of restenosis of a blood vessel
US6774278B1 (en) 1995-06-07 2004-08-10 Cook Incorporated Coated implantable medical device
US7038057B2 (en) 2001-08-13 2006-05-02 E.I. Du Pont De Nemours And Company Substituted 1H-dihydropyrazoles, their preparation and use
US6770729B2 (en) 2002-09-30 2004-08-03 Medtronic Minimed, Inc. Polymer compositions containing bioactive agents and methods for their use
KR101687743B1 (ko) 2008-12-18 2016-12-19 바이엘 인텔렉쳐 프로퍼티 게엠베하 살해충제로서의 테트라졸 치환된 안트라닐산 아미드
DK2909181T3 (da) 2012-10-16 2017-11-20 Tolero Pharmaceuticals Inc PKM2-modulatorer og fremgangsmåder til anvendelse deraf
LT3113772T (lt) 2014-03-07 2020-12-28 Biocryst Pharmaceuticals, Inc. Trifluormetilo pakeistieji pirazolai kaip žmogaus plazmos kalikreino inhibitoriai
EP4010320A4 (en) 2019-08-06 2023-08-16 Biocryst Pharmaceuticals, Inc. Process-scale synthesis of a plasma kallikrein inhibitor

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20020037857A1 (en) 2000-08-11 2002-03-28 Corvas International, Inc. Non-covalent inhibitors of urokinase and blood vessel formation
US20130296245A1 (en) 2010-11-08 2013-11-07 Shanghai Institute Of Pharmaceutical Industry Prolinamiade derivatives as thrombin inhibitor, prepraration method and application thereof

Also Published As

Publication number Publication date
AU2020324422B2 (en) 2026-02-26
JP7626751B2 (ja) 2025-02-04
TWI881995B (zh) 2025-05-01
KR20220044276A (ko) 2022-04-07
IL290113B1 (en) 2025-04-01
BR112022002060A2 (pt) 2022-06-07
GEAP202515893A (en) 2025-02-25
CO2022002392A2 (es) 2022-04-08
UA130182C2 (uk) 2025-12-10
AR119617A1 (es) 2021-12-29
WO2021026182A1 (en) 2021-02-11
EP4010320A1 (en) 2022-06-15
IL290113B2 (en) 2025-08-01
CR20220092A (es) 2022-06-03
PE20221009A1 (es) 2022-06-15
PH12022550221A1 (en) 2022-12-19
IL290113A (en) 2022-03-01
PY2042865A (es) 2021-05-05
CL2022000264A1 (es) 2022-10-21
GEP20257777B (en) 2025-07-10
EP4010320A4 (en) 2023-08-16
ECSP22016209A (es) 2022-06-30
CL2023000942A1 (es) 2023-11-24
US12503443B2 (en) 2025-12-23
TW202120481A (zh) 2021-06-01
DOP2022000027A (es) 2022-05-31
JOP20220021A1 (ar) 2023-01-30
CN114206839B (zh) 2025-03-07
TN2022000028A1 (en) 2023-10-09
UY38826A (es) 2021-02-26
US20220289683A1 (en) 2022-09-15
AU2020324422A1 (en) 2022-03-17
CN114206839A (zh) 2022-03-18
CA3149176A1 (en) 2021-02-11
MX2022001608A (es) 2022-03-11
JP2022543419A (ja) 2022-10-12

Similar Documents

Publication Publication Date Title
TWI881995B (zh) 血漿激肽釋放酶抑制劑之工業合成
US12552750B2 (en) Crystalline salts of a plasma kallikrein inhibitor
OA20652A (en) Process-scale synthesis of a plasma kallikrein inhibitor.

Legal Events

Date Code Title Description
PA0105 International application

St.27 status event code: A-0-1-A10-A15-nap-PA0105

PG1501 Laying open of application

St.27 status event code: A-1-1-Q10-Q12-nap-PG1501

A201 Request for examination
E13-X000 Pre-grant limitation requested

St.27 status event code: A-2-3-E10-E13-lim-X000

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

PA0201 Request for examination

St.27 status event code: A-1-2-D10-D11-exm-PA0201

R17-X000 Change to representative recorded

St.27 status event code: A-3-3-R10-R17-oth-X000

D21 Rejection of application intended

Free format text: ST27 STATUS EVENT CODE: A-1-2-D10-D21-EXM-PE0902 (AS PROVIDED BY THE NATIONAL OFFICE)

PE0902 Notice of grounds for rejection

St.27 status event code: A-1-2-D10-D21-exm-PE0902

P11 Amendment of application requested

Free format text: ST27 STATUS EVENT CODE: A-2-2-P10-P11-NAP-X000 (AS PROVIDED BY THE NATIONAL OFFICE)

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13 Application amended

Free format text: ST27 STATUS EVENT CODE: A-2-2-P10-P13-NAP-X000 (AS PROVIDED BY THE NATIONAL OFFICE)

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

D22 Grant of ip right intended

Free format text: ST27 STATUS EVENT CODE: A-1-2-D10-D22-EXM-PE0701 (AS PROVIDED BY THE NATIONAL OFFICE)

PE0701 Decision of registration

St.27 status event code: A-1-2-D10-D22-exm-PE0701

F11 Ip right granted following substantive examination

Free format text: ST27 STATUS EVENT CODE: A-2-4-F10-F11-EXM-PR0701 (AS PROVIDED BY THE NATIONAL OFFICE)

PR0701 Registration of establishment

St.27 status event code: A-2-4-F10-F11-exm-PR0701

PR1002 Payment of registration fee

St.27 status event code: A-2-2-U10-U12-oth-PR1002

Fee payment year number: 1

U12 Designation fee paid

Free format text: ST27 STATUS EVENT CODE: A-2-2-U10-U12-OTH-PR1002 (AS PROVIDED BY THE NATIONAL OFFICE)

Year of fee payment: 1

PG1601 Publication of registration

St.27 status event code: A-4-4-Q10-Q13-nap-PG1601

Q13 Ip right document published

Free format text: ST27 STATUS EVENT CODE: A-4-4-Q10-Q13-NAP-PG1601 (AS PROVIDED BY THE NATIONAL OFFICE)