TWI918610B - 作為klk5/7雙重抑制劑之苯并酮化合物 - Google Patents
作為klk5/7雙重抑制劑之苯并酮化合物Info
- Publication number
- TWI918610B TWI918610B TW109134275A TW109134275A TWI918610B TW I918610 B TWI918610 B TW I918610B TW 109134275 A TW109134275 A TW 109134275A TW 109134275 A TW109134275 A TW 109134275A TW I918610 B TWI918610 B TW I918610B
- Authority
- TW
- Taiwan
- Prior art keywords
- compound
- approximately
- skin
- pharmaceutically acceptable
- ppm
- Prior art date
Links
Classifications
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Dermatology (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Wood Science & Technology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Zoology (AREA)
- General Engineering & Computer Science (AREA)
- Biotechnology (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Analytical Chemistry (AREA)
- Microbiology (AREA)
- Genetics & Genomics (AREA)
- Physics & Mathematics (AREA)
- Immunology (AREA)
- Biophysics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (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)
- Peptides Or Proteins (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962909006P | 2019-10-01 | 2019-10-01 | |
| US62/909,006 | 2019-10-01 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| TW202126631A TW202126631A (zh) | 2021-07-16 |
| TWI918610B true TWI918610B (zh) | 2026-03-21 |
Family
ID=75274622
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TW109134275A TWI918610B (zh) | 2019-10-01 | 2020-09-30 | 作為klk5/7雙重抑制劑之苯并酮化合物 |
Country Status (13)
| Country | Link |
|---|---|
| US (2) | US11643420B2 (enExample) |
| EP (1) | EP4037687B1 (enExample) |
| JP (1) | JP7854389B2 (enExample) |
| KR (1) | KR102994600B1 (enExample) |
| CN (1) | CN114615984B (enExample) |
| AU (1) | AU2020359526B2 (enExample) |
| BR (1) | BR112022005881A2 (enExample) |
| CA (1) | CA3151626A1 (enExample) |
| ES (1) | ES3053975T3 (enExample) |
| IL (1) | IL291398B2 (enExample) |
| MX (1) | MX2022003929A (enExample) |
| TW (1) | TWI918610B (enExample) |
| WO (1) | WO2021067335A1 (enExample) |
Families Citing this family (4)
| 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 |
| AU2020349509A1 (en) | 2019-09-18 | 2022-03-31 | Genentech, Inc. | Anti-KLK7 antibodies, anti-KLK5 antibodies, multispecific anti-KLK5/KLK7 antibodies, and methods of use |
| MX2022003929A (es) | 2019-10-01 | 2022-06-14 | Molecular Skin Therapeutics Inc | Compuestos de benzoxazinona como inhibidores dobles de klk5/7. |
| 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 |
Family Cites Families (37)
| 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 |
| KR890002631B1 (ko) | 1984-10-04 | 1989-07-21 | 몬산토 캄파니 | 생물학적으로 활성인 소마토트로핀을 지속적으로 유리하는 조성물 |
| 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 |
| DE69632684T2 (de) | 1995-06-27 | 2005-06-09 | Takeda Pharmaceutical Co. Ltd. | Verfahren zur herstellung von zubereitungen mit verzögerter freisetzung |
| 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 |
| ES2221019T3 (es) | 1996-10-31 | 2004-12-16 | Takeda Chemical Industries, Ltd. | Preparacion de liberacion mantenida. |
| EP0946169B1 (en) | 1996-12-20 | 2003-02-26 | 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 |
| HUP0101699A3 (en) | 1998-03-31 | 2002-05-28 | Warner Lambert Co | Benzoxazinones/benzothiazinones as serine protease inhibitors and pharmaceutical compositions containing the same |
| 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 |
| CN101152185B (zh) | 2003-06-06 | 2010-12-08 | 阿里克斯股份公司 | 杂环化合物作为scce抑制剂的用途 |
| DK3097085T3 (da) * | 2014-01-23 | 2020-10-26 | Sixera Pharma Ab | Benzoxazinonderivater til behandling af hudsygdomme |
| MX2022003929A (es) | 2019-10-01 | 2022-06-14 | Molecular Skin Therapeutics Inc | Compuestos de benzoxazinona como inhibidores dobles de klk5/7. |
-
2020
- 2020-09-30 MX MX2022003929A patent/MX2022003929A/es unknown
- 2020-09-30 US US17/037,910 patent/US11643420B2/en active Active
- 2020-09-30 WO PCT/US2020/053369 patent/WO2021067335A1/en not_active Ceased
- 2020-09-30 IL IL291398A patent/IL291398B2/en unknown
- 2020-09-30 JP JP2022520290A patent/JP7854389B2/ja active Active
- 2020-09-30 BR BR112022005881A patent/BR112022005881A2/pt unknown
- 2020-09-30 KR KR1020227014268A patent/KR102994600B1/ko active Active
- 2020-09-30 ES ES20872712T patent/ES3053975T3/es active Active
- 2020-09-30 EP EP20872712.3A patent/EP4037687B1/en active Active
- 2020-09-30 AU AU2020359526A patent/AU2020359526B2/en active Active
- 2020-09-30 TW TW109134275A patent/TWI918610B/zh active
- 2020-09-30 CA CA3151626A patent/CA3151626A1/en active Pending
- 2020-09-30 CN CN202080069819.7A patent/CN114615984B/zh active Active
-
2023
- 2023-04-03 US US18/295,009 patent/US12281123B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| MX2022003929A (es) | 2022-06-14 |
| TW202126631A (zh) | 2021-07-16 |
| AU2020359526B2 (en) | 2026-07-16 |
| IL291398B1 (en) | 2025-01-01 |
| US12281123B2 (en) | 2025-04-22 |
| IL291398A (en) | 2022-05-01 |
| ES3053975T3 (en) | 2026-01-28 |
| US20210101911A1 (en) | 2021-04-08 |
| KR102994600B1 (ko) | 2026-07-22 |
| US11643420B2 (en) | 2023-05-09 |
| US20240067658A1 (en) | 2024-02-29 |
| CN114615984A (zh) | 2022-06-10 |
| CA3151626A1 (en) | 2021-04-08 |
| EP4037687A4 (en) | 2023-09-27 |
| JP7854389B2 (ja) | 2026-05-01 |
| EP4037687A1 (en) | 2022-08-10 |
| AU2020359526A1 (en) | 2022-04-21 |
| KR20220091488A (ko) | 2022-06-30 |
| BR112022005881A2 (pt) | 2022-06-21 |
| WO2021067335A1 (en) | 2021-04-08 |
| JP2022551583A (ja) | 2022-12-12 |
| EP4037687B1 (en) | 2025-10-29 |
| IL291398B2 (en) | 2025-05-01 |
| CN114615984B (zh) | 2025-02-07 |
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