CN112969458A - 血浆激肽释放酶抑制剂的结晶盐 - Google Patents

血浆激肽释放酶抑制剂的结晶盐 Download PDF

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Publication number
CN112969458A
CN112969458A CN201980072995.3A CN201980072995A CN112969458A CN 112969458 A CN112969458 A CN 112969458A CN 201980072995 A CN201980072995 A CN 201980072995A CN 112969458 A CN112969458 A CN 112969458A
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crystalline salt
salt
xrpd
pattern
compound
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Pending
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CN201980072995.3A
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Chinese (zh)
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Y·埃尔-卡坦
Y·S·巴布
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Biocryst Pharmaceuticals Inc
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Biocryst Pharmaceuticals Inc
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Application filed by Biocryst Pharmaceuticals Inc filed Critical Biocryst Pharmaceuticals Inc
Publication of CN112969458A publication Critical patent/CN112969458A/zh
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    • 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
    • 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
    • C07D231/44—Oxygen and nitrogen or sulfur and nitrogen atoms
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23L—FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF
    • A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
    • A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A61K9/0029—Parenteral nutrition; Parenteral nutrition compositions as drug carriers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10—Antioedematous agents; Diuretics
    • 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
    • A61P9/10—Drugs 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
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
    • A23V2002/00—Food compositions, function of food ingredients or processes for food or foodstuffs
    • 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)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Epidemiology (AREA)
  • Nutrition Science (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Physiology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Food Science & Technology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Polymers & Plastics (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Mycology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
CN201980072995.3A 2018-11-02 2019-11-01 血浆激肽释放酶抑制剂的结晶盐 Pending CN112969458A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862754983P 2018-11-02 2018-11-02
US62/754983 2018-11-02
PCT/US2019/059385 WO2020092898A1 (en) 2018-11-02 2019-11-01 Crystalline salts of a plasma kallikrein inhibitor

Publications (1)

Publication Number Publication Date
CN112969458A true CN112969458A (zh) 2021-06-15

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ID=70457981

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CN201980072995.3A Pending CN112969458A (zh) 2018-11-02 2019-11-01 血浆激肽释放酶抑制剂的结晶盐

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Country Link
US (11) US10662160B1 (https=)
EP (1) EP3873463A4 (https=)
JP (2) JP2022505670A (https=)
KR (1) KR102810837B1 (https=)
CN (1) CN112969458A (https=)
AR (1) AR116951A1 (https=)
AU (1) AU2019374115B8 (https=)
BR (1) BR112021008249A2 (https=)
CA (1) CA3117123A1 (https=)
CL (1) CL2021001094A1 (https=)
CO (1) CO2021007172A2 (https=)
EA (1) EA202191192A1 (https=)
IL (2) IL322896A (https=)
MA (1) MA54087A (https=)
MX (1) MX2021004917A (https=)
PE (1) PE20211280A1 (https=)
PH (1) PH12021550883A1 (https=)
PY (1) PY1991831A (https=)
SG (1) SG11202103804TA (https=)
TW (1) TW202031255A (https=)
UY (1) UY38438A (https=)
WO (1) WO2020092898A1 (https=)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR102736869B1 (ko) 2014-03-07 2024-12-02 바이오크리스트파마슈티컬즈,인코포레이티드 인간 혈장 칼리크레인 저해제
UY38438A (es) 2018-11-02 2020-05-29 Biocryst Pharm Inc Sales cristalinas de un inhibidor de calicreína plasmática
WO2021025969A1 (en) * 2019-08-02 2021-02-11 Teva Pharmaceuticals International Gmbh Solid state forms of berotralstat
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 (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101495468A (zh) * 2006-07-31 2009-07-29 艾克提弗赛特制药股份有限公司 血浆激肽释放酶抑制剂
US20150191421A1 (en) * 2012-07-06 2015-07-09 Kalvista Pharmaceuticals Limited Polymorphs of n-[(r)-1-[(s)-1-(4-aminomethyl-benzylcarbamoyl)-2-phenyl-ethylcarbamoyl]-2-(4-ethoxy-phenyl)-ethyl]-benzamide hydrochloride
CN106257976A (zh) * 2014-03-07 2016-12-28 拜奥克里斯特制药公司 人类血浆激肽释放酶抑制剂

Family Cites Families (8)

* 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
BRPI0519331A2 (pt) 2004-12-15 2009-01-20 Bristol Myers Squibb Co formas cristalina de um inibidor de fator xa
WO2008016883A2 (en) 2006-07-31 2008-02-07 Activesite Pharmaceuticals, Inc. Inhibitors of plasma kallikrein
RU2585683C2 (ru) * 2010-05-19 2016-06-10 Сандоз Аг Очистка позаконазола и промежуточных продуктов для синтеза позаконазола
US9012464B2 (en) 2010-11-25 2015-04-21 Ratiopharm Gmbh Salts and polymorphic forms of Afatinib
DK4019022T3 (en) 2015-10-01 2024-02-19 Biocryst Pharm Inc Human plasma kallikrein inhibitors
UY38438A (es) 2018-11-02 2020-05-29 Biocryst Pharm Inc Sales cristalinas de un inhibidor de calicreína plasmática
CN114206839B (zh) 2019-08-06 2025-03-07 拜奥克里斯特制药公司 血浆激肽释放酶抑制剂的生产规模合成

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101495468A (zh) * 2006-07-31 2009-07-29 艾克提弗赛特制药股份有限公司 血浆激肽释放酶抑制剂
US20150191421A1 (en) * 2012-07-06 2015-07-09 Kalvista Pharmaceuticals Limited Polymorphs of n-[(r)-1-[(s)-1-(4-aminomethyl-benzylcarbamoyl)-2-phenyl-ethylcarbamoyl]-2-(4-ethoxy-phenyl)-ethyl]-benzamide hydrochloride
CN106257976A (zh) * 2014-03-07 2016-12-28 拜奥克里斯特制药公司 人类血浆激肽释放酶抑制剂

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US20250388548A1 (en) 2025-12-25
UY38438A (es) 2020-05-29
US11618733B2 (en) 2023-04-04
AR116951A1 (es) 2021-06-30
PY1991831A (es) 2020-07-03
US20250388546A1 (en) 2025-12-25
US12545646B2 (en) 2026-02-10
US20250376448A1 (en) 2025-12-11
US11117867B2 (en) 2021-09-14
US20250388545A1 (en) 2025-12-25
IL322896A (en) 2025-10-01
MX2021004917A (es) 2021-06-18
JP2022505670A (ja) 2022-01-14
MA54087A (fr) 2022-02-09
US12590069B2 (en) 2026-03-31
TW202031255A (zh) 2020-09-01
WO2020092898A1 (en) 2020-05-07
US12545647B2 (en) 2026-02-10
BR112021008249A2 (pt) 2021-08-03
PH12021550883A1 (en) 2022-02-21
EP3873463A4 (en) 2022-06-22
AU2019374115B8 (en) 2025-08-07
US20240109844A1 (en) 2024-04-04
US12590068B2 (en) 2026-03-31
PE20211280A1 (es) 2021-07-19
AU2019374115B1 (en) 2025-07-17
KR20210087037A (ko) 2021-07-09
IL282454A (en) 2021-06-30
US12552750B2 (en) 2026-02-17
KR102810837B1 (ko) 2025-05-20
CO2021007172A2 (es) 2021-06-10
AU2019374115A1 (en) 2021-06-03
US20250388547A1 (en) 2025-12-25
SG11202103804TA (en) 2021-05-28
CA3117123A1 (en) 2020-05-07
EP3873463A1 (en) 2021-09-08
US20200308118A1 (en) 2020-10-01
US20220204454A1 (en) 2022-06-30
JP2024109860A (ja) 2024-08-14
US20200140389A1 (en) 2020-05-07
US20250376447A1 (en) 2025-12-11
US12344585B2 (en) 2025-07-01
EA202191192A1 (ru) 2021-09-23
US20250388549A1 (en) 2025-12-25
US12545645B2 (en) 2026-02-10
US10662160B1 (en) 2020-05-26
CL2021001094A1 (es) 2021-10-15

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