CN114615984B - 作为klk5/7双重抑制剂的苯并噁嗪酮化合物 - Google Patents

作为klk5/7双重抑制剂的苯并噁嗪酮化合物 Download PDF

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Publication number
CN114615984B
CN114615984B CN202080069819.7A CN202080069819A CN114615984B CN 114615984 B CN114615984 B CN 114615984B CN 202080069819 A CN202080069819 A CN 202080069819A CN 114615984 B CN114615984 B CN 114615984B
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compound
formula
pharmaceutically acceptable
skin
subject
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Chinese (zh)
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CN114615984A (zh
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A·贝茨
R·赞博尼
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Molecular Skin Therapy
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Molecular Skin Therapy
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5365—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61K9/0014—Skin, i.e. galenical aspects of topical compositions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
    • C12Q1/34—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving hydrolase
    • C12Q1/37—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving hydrolase involving peptidase or proteinase

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Dermatology (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Zoology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Wood Science & Technology (AREA)
  • Analytical Chemistry (AREA)
  • Genetics & Genomics (AREA)
  • Immunology (AREA)
  • Microbiology (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Physics & Mathematics (AREA)
  • Biochemistry (AREA)
  • General Engineering & Computer Science (AREA)
  • Biotechnology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Peptides Or Proteins (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CN202080069819.7A 2019-10-01 2020-09-30 作为klk5/7双重抑制剂的苯并噁嗪酮化合物 Active CN114615984B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962909006P 2019-10-01 2019-10-01
US62/909,006 2019-10-01
PCT/US2020/053369 WO2021067335A1 (en) 2019-10-01 2020-09-30 Benzoxazinone compounds as klk5/7 dual inhibitors

Publications (2)

Publication Number Publication Date
CN114615984A CN114615984A (zh) 2022-06-10
CN114615984B true CN114615984B (zh) 2025-02-07

Family

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CN202080069819.7A Active CN114615984B (zh) 2019-10-01 2020-09-30 作为klk5/7双重抑制剂的苯并噁嗪酮化合物

Country Status (12)

Country Link
US (2) US11643420B2 (https=)
EP (1) EP4037687B1 (https=)
JP (1) JP7854389B2 (https=)
KR (1) KR20220091488A (https=)
CN (1) CN114615984B (https=)
AU (1) AU2020359526A1 (https=)
BR (1) BR112022005881A2 (https=)
CA (1) CA3151626A1 (https=)
ES (1) ES3053975T3 (https=)
IL (1) IL291398B2 (https=)
MX (1) MX2022003929A (https=)
WO (1) WO2021067335A1 (https=)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20200040103A1 (en) 2018-03-14 2020-02-06 Genentech, Inc. Anti-klk5 antibodies and methods of use
PH12022550646A1 (en) 2019-09-18 2023-04-03 Genentech Inc Anti-klk7 antibodies, anti-klk5 antibodies, multispecific anti-klk5/klk7 antibodies, and methods of use
ES3053975T3 (en) 2019-10-01 2026-01-28 Molecular Skin Therapeutics Inc Benzoxazinone compounds as klk5/7 dual inhibitors
TW202304890A (zh) * 2021-04-14 2023-02-01 美商百歐克斯製藥公司 Klk5雙環雜芳香族抑制劑

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106132941A (zh) * 2014-01-23 2016-11-16 西可斯拉制药公司 用于治疗皮肤病的苯并恶嗪酮衍生物

Family Cites Families (36)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3536809A (en) 1969-02-17 1970-10-27 Alza Corp Medication method
US3598123A (en) 1969-04-01 1971-08-10 Alza Corp Bandage for administering drugs
US3845770A (en) 1972-06-05 1974-11-05 Alza Corp Osmatic dispensing device for releasing beneficial agent
US3916899A (en) 1973-04-25 1975-11-04 Alza Corp Osmotic dispensing device with maximum and minimum sizes for the passageway
US4008719A (en) 1976-02-02 1977-02-22 Alza Corporation Osmotic system having laminar arrangement for programming delivery of active agent
HU196714B (en) 1984-10-04 1989-01-30 Monsanto Co Process for producing non-aqueous composition comprising somatotropin
IE58110B1 (en) 1984-10-30 1993-07-14 Elan Corp Plc Controlled release powder and process for its preparation
CA1309556C (en) * 1987-06-09 1992-10-27 Masayuki Kokubo 4h-3,1-benzoxazin-4-one compounds and pharmaceutical composition thereoffor the inhibition of serine proteases
US5073543A (en) 1988-07-21 1991-12-17 G. D. Searle & Co. Controlled release formulations of trophic factors in ganglioside-lipsome vehicle
IT1229203B (it) 1989-03-22 1991-07-25 Bioresearch Spa Impiego di acido 5 metiltetraidrofolico, di acido 5 formiltetraidrofolico e dei loro sali farmaceuticamente accettabili per la preparazione di composizioni farmaceutiche in forma a rilascio controllato attive nella terapia dei disturbi mentali organici e composizioni farmaceutiche relative.
PH30995A (en) 1989-07-07 1997-12-23 Novartis Inc Sustained release formulations of water soluble peptides.
US5120548A (en) 1989-11-07 1992-06-09 Merck & Co., Inc. Swelling modulated polymeric drug delivery device
US5733566A (en) 1990-05-15 1998-03-31 Alkermes Controlled Therapeutics Inc. Ii Controlled release of antiparasitic agents in animals
DE4134770A1 (de) 1991-10-22 1993-04-29 Basf Ag Koernige bleichaktivatorzusammensetzung
US5580578A (en) 1992-01-27 1996-12-03 Euro-Celtique, S.A. Controlled release formulations coated with aqueous dispersions of acrylic polymers
TW333456B (en) 1992-12-07 1998-06-11 Takeda Pharm Ind Co Ltd A pharmaceutical composition of sustained-release preparation the invention relates to a pharmaceutical composition of sustained-release preparation which comprises a physiologically active peptide.
US5591767A (en) 1993-01-25 1997-01-07 Pharmetrix Corporation Liquid reservoir transdermal patch for the administration of ketorolac
US6087324A (en) 1993-06-24 2000-07-11 Takeda Chemical Industries, Ltd. Sustained-release preparation
IT1270594B (it) 1994-07-07 1997-05-07 Recordati Chem Pharm Composizione farmaceutica a rilascio controllato di moguisteina in sospensione liquida
AU6242096A (en) 1995-06-27 1997-01-30 Takeda Chemical Industries Ltd. Method of producing sustained-release preparation
TW448055B (en) 1995-09-04 2001-08-01 Takeda Chemical Industries Ltd Method of production of sustained-release preparation
JP2909418B2 (ja) 1995-09-18 1999-06-23 株式会社資生堂 薬物の遅延放出型マイクロスフイア
US5980945A (en) 1996-01-16 1999-11-09 Societe De Conseils De Recherches Et D'applications Scientifique S.A. Sustained release drug formulations
US6264970B1 (en) 1996-06-26 2001-07-24 Takeda Chemical Industries, Ltd. Sustained-release preparation
US6419961B1 (en) 1996-08-29 2002-07-16 Takeda Chemical Industries, Ltd. Sustained release microcapsules of a bioactive substance and a biodegradable polymer
CA2184851A1 (en) 1996-09-05 1998-03-06 Cheng Chung Wu Method of manufacturing a microweavable flatware article made of synthetic material, the article produced thereby and an ink-imprinted film component for use in making the flatware article
CA2217134A1 (en) 1996-10-09 1998-04-09 Sumitomo Pharmaceuticals Co., Ltd. Sustained release formulation
PT839525E (pt) 1996-10-31 2004-10-29 Takeda Chemical Industries Ltd Preparacao de libertacao prolongada
WO1998027980A2 (en) 1996-12-20 1998-07-02 Takeda Chemical Industries, Ltd. Method of producing a sustained-release preparation
US5891474A (en) 1997-01-29 1999-04-06 Poli Industria Chimica, S.P.A. Time-specific controlled release dosage formulations and method of preparing same
US6613358B2 (en) 1998-03-18 2003-09-02 Theodore W. Randolph Sustained-release composition including amorphous polymer
PL343317A1 (en) * 1998-03-31 2001-08-13 Warner Lambert Co Benzoxazinones/benzothiazinones as serine protease inhibitors
KR19990085365A (ko) 1998-05-16 1999-12-06 허영섭 지속적으로 약물 조절방출이 가능한 생분해성 고분자 미립구 및그 제조방법
US6248363B1 (en) 1999-11-23 2001-06-19 Lipocine, Inc. Solid carriers for improved delivery of active ingredients in pharmaceutical compositions
SI1631295T1 (sl) 2003-06-06 2010-06-30 Arexis Ab Uporaba kondenziranih heterocikličnih spojin kotSCCE inhibitorjev za zdravljenje kožnih bolezni
ES3053975T3 (en) 2019-10-01 2026-01-28 Molecular Skin Therapeutics Inc Benzoxazinone compounds as klk5/7 dual inhibitors

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106132941A (zh) * 2014-01-23 2016-11-16 西可斯拉制药公司 用于治疗皮肤病的苯并恶嗪酮衍生物

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Publication number Publication date
BR112022005881A2 (pt) 2022-06-21
CN114615984A (zh) 2022-06-10
TW202126631A (zh) 2021-07-16
JP7854389B2 (ja) 2026-05-01
US12281123B2 (en) 2025-04-22
IL291398B1 (en) 2025-01-01
ES3053975T3 (en) 2026-01-28
JP2022551583A (ja) 2022-12-12
AU2020359526A1 (en) 2022-04-21
IL291398A (en) 2022-05-01
US20210101911A1 (en) 2021-04-08
IL291398B2 (en) 2025-05-01
EP4037687B1 (en) 2025-10-29
MX2022003929A (es) 2022-06-14
WO2021067335A1 (en) 2021-04-08
CA3151626A1 (en) 2021-04-08
EP4037687A4 (en) 2023-09-27
EP4037687A1 (en) 2022-08-10
US20240067658A1 (en) 2024-02-29
US11643420B2 (en) 2023-05-09
KR20220091488A (ko) 2022-06-30

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