TWI849082B - 蛋白酪胺酸磷酸酶抑制劑及其使用方法 - Google Patents
蛋白酪胺酸磷酸酶抑制劑及其使用方法 Download PDFInfo
- Publication number
- TWI849082B TWI849082B TW109108506A TW109108506A TWI849082B TW I849082 B TWI849082 B TW I849082B TW 109108506 A TW109108506 A TW 109108506A TW 109108506 A TW109108506 A TW 109108506A TW I849082 B TWI849082 B TW I849082B
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- Prior art keywords
- alkyl
- hydroxy
- fluoro
- alkylene
- trione
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
- C07D285/01—Five-membered rings
- C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
- C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
- C07D285/10—1,2,5-Thiadiazoles; Hydrogenated 1,2,5-thiadiazoles
-
- 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
- A61K31/433—Thidiazoles
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
-
- 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
- A61P3/04—Anorexiants; Antiobesity agents
-
- 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
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
- C07D285/01—Five-membered rings
- C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Diabetes (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Epidemiology (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Child & Adolescent Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Enzymes And Modification Thereof (AREA)
- Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962818447P | 2019-03-14 | 2019-03-14 | |
| US62/818,447 | 2019-03-14 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| TW202100515A TW202100515A (zh) | 2021-01-01 |
| TWI849082B true TWI849082B (zh) | 2024-07-21 |
Family
ID=70190226
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TW109108506A TWI849082B (zh) | 2019-03-14 | 2020-03-13 | 蛋白酪胺酸磷酸酶抑制劑及其使用方法 |
| TW113128010A TW202519515A (zh) | 2019-03-14 | 2020-03-13 | 蛋白酪胺酸磷酸酶抑制劑及其使用方法 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TW113128010A TW202519515A (zh) | 2019-03-14 | 2020-03-13 | 蛋白酪胺酸磷酸酶抑制劑及其使用方法 |
Country Status (24)
| Country | Link |
|---|---|
| US (1) | US10851073B2 (enExample) |
| EP (1) | EP3938038A1 (enExample) |
| JP (3) | JP7204005B2 (enExample) |
| KR (2) | KR20230074822A (enExample) |
| CN (2) | CN116332873A (enExample) |
| AR (1) | AR118374A1 (enExample) |
| AU (1) | AU2020234712B2 (enExample) |
| BR (1) | BR112021017430A2 (enExample) |
| CA (1) | CA3131894A1 (enExample) |
| CL (2) | CL2021002382A1 (enExample) |
| CO (1) | CO2021013524A2 (enExample) |
| CR (1) | CR20210516A (enExample) |
| DO (1) | DOP2021000188A (enExample) |
| EC (1) | ECSP21075909A (enExample) |
| IL (2) | IL286373B1 (enExample) |
| MA (1) | MA55301A (enExample) |
| MX (2) | MX2021010544A (enExample) |
| MY (1) | MY209419A (enExample) |
| PE (1) | PE20212154A1 (enExample) |
| PH (1) | PH12021552194A1 (enExample) |
| SG (1) | SG11202109067PA (enExample) |
| TW (2) | TWI849082B (enExample) |
| UY (1) | UY38613A (enExample) |
| WO (1) | WO2020186199A1 (enExample) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3938038A1 (en) * | 2019-03-14 | 2022-01-19 | Calico Life Sciences LLC | Protein tyrosine phosphatase inhibitors and methods of use thereof |
| EP4077291A1 (en) * | 2019-12-18 | 2022-10-26 | Calico Life Sciences LLC | Protein tyrosine phosphatase inhibitors and methods of use thereof |
| AU2021342161A1 (en) * | 2020-09-11 | 2023-05-25 | Abbvie Inc. | Protein tyrosine phosphatase inhibitors and methods of use thereof |
| IL305072A (en) * | 2021-02-12 | 2023-10-01 | Recovery Therapeutics Inc | Compounds, compositions, and methods for modulating fgf activity |
| EP4305030A4 (en) * | 2021-03-11 | 2025-05-21 | Kumquat Biosciences Inc. | HETEROCYCLES AND THEIR USES |
| WO2022261145A1 (en) * | 2021-06-10 | 2022-12-15 | Ness Therapeutics, Inc. | Compounds having 5-(2-fluoro-6-hydroxyphenyl)-1,2,5-thiadiazolidin-3-one 1,1-dioxide as inhibitors of protein kinase phosphatase enzymes |
| EP4430038A1 (en) * | 2021-11-11 | 2024-09-18 | Calico Life Sciences LLC | Protein tyrosine phosphatase inhibitors and methods of use thereof |
| MX2024005656A (es) * | 2021-11-11 | 2024-08-06 | Calico Life Sciences Llc | Inhibidores de proteina tirosina fosfatasa y metodos de uso de estos. |
| CA3243580A1 (en) * | 2022-02-02 | 2023-08-10 | Nerio Therapeutics Inc | TYROSINE PHOSPHATASE PROTEIN INHIBITORS AND THEIR USES |
| JP2025507292A (ja) * | 2022-02-02 | 2025-03-18 | ネリオ セラピューティクス，インク． | プロテインチロシンホスファターゼ阻害剤およびその使用 |
| JP2025505994A (ja) * | 2022-02-02 | 2025-03-05 | ネリオ セラピューティクス，インク． | プロテインチロシンホスファターゼ阻害剤およびその使用 |
| EP4496797A1 (en) * | 2022-03-21 | 2025-01-29 | Gasherbrum Bio, Inc. | 5,8-dihydro-1,7-naphthyridine derivatives as glp-1 agonists for the treatment of diabetes |
| EP4587436A1 (en) * | 2022-09-13 | 2025-07-23 | Kumquat Biosciences Inc. | Benzo-fused n-heterocycles and uses thereof |
| WO2024067802A1 (zh) * | 2022-09-30 | 2024-04-04 | 深圳众格生物科技有限公司 | 蛋白酪氨酸磷酸酶抑制剂及其制备方法和医药用途 |
| WO2024141015A1 (en) * | 2022-12-30 | 2024-07-04 | Insilico Medicine Ip Limited | Protein tyrosine phosphatase inhibitors and uses thereof |
| WO2025011570A1 (zh) * | 2023-07-11 | 2025-01-16 | 深圳众格生物科技有限公司 | 蛋白酪氨酸磷酸酶抑制剂及其组合物、医药用途 |
| TW202519514A (zh) | 2023-07-14 | 2025-05-16 | 天主教魯汶大學 | 新穎化合物(一) |
| WO2025026158A1 (zh) * | 2023-07-28 | 2025-02-06 | 杭州中美华东制药有限公司 | 具有ptpn2抑制作用的化合物及其用途 |
| WO2025030008A1 (en) * | 2023-08-02 | 2025-02-06 | Nerio Therapeutics, Inc. | Protein tyrosine phosphatase inhibitor combinations |
| WO2025055985A1 (zh) * | 2023-09-15 | 2025-03-20 | 深圳众格生物科技有限公司 | 蛋白酪氨酸磷酸酶抑制剂及其组合物、医药用途 |
| CN120004876A (zh) * | 2023-11-16 | 2025-05-16 | 英矽智能科技(上海)有限公司 | 蛋白酪氨酸磷酸酶抑制剂及其应用 |
| CN117343052B (zh) * | 2023-12-04 | 2024-02-06 | 英矽智能科技(上海)有限公司 | 蛋白酪氨酸磷酸酶抑制剂及其应用 |
| WO2025136841A1 (en) * | 2023-12-19 | 2025-06-26 | Merck Sharp & Dohme Llc | Substituted isoquinoline derivatives and methods of use thereof |
| WO2025242216A1 (zh) * | 2024-05-24 | 2025-11-27 | 杭州百新生物医药科技有限公司 | 吲哚啉类化合物及其用途 |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2007067612A1 (en) * | 2005-12-08 | 2007-06-14 | Novartis Ag | 1-orthofluorophenyl substituted 1, 2, 5-thiazolidinedione derivatives as ptp-as inhibitors |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| US4911920A (en) | 1986-07-30 | 1990-03-27 | Alcon Laboratories, Inc. | Sustained release, comfort formulation for glaucoma therapy |
| FR2588189B1 (fr) | 1985-10-03 | 1988-12-02 | Merck Sharp & Dohme | Composition pharmaceutique de type a transition de phase liquide-gel |
| EP0495421B1 (en) | 1991-01-15 | 1996-08-21 | Alcon Laboratories, Inc. | Use of carrageenans in topical ophthalmic compositions |
| US5212162A (en) | 1991-03-27 | 1993-05-18 | Alcon Laboratories, Inc. | Use of combinations gelling polysaccharides and finely divided drug carrier substrates in topical ophthalmic compositions |
| JP4846978B2 (ja) | 2001-10-30 | 2011-12-28 | メルク セローノ ソシエテ アノニム | タンパク質チロシンホスファターゼのオキシンドールヒドラジンモジュレータ |
| UA94724C2 (en) * | 2005-12-08 | 2011-06-10 | Новартис Аг | Thiadiazolidinone derivatives as antidiabetic agents |
| JP2009532379A (ja) | 2006-03-31 | 2009-09-10 | ノバルティス アクチエンゲゼルシャフト | ＰＴＰａｓｅのチアジアゾリジノン阻害剤 |
| US20100160228A1 (en) | 2007-05-23 | 2010-06-24 | Valtion Teknillinen Tutkimuskeskus | Method for inhibiting or stimulating angiogenesis in an individual |
| AR066820A1 (es) | 2007-06-04 | 2009-09-16 | Novartis Ag | Compuestos de tiadiazolidin-3 ona |
| WO2010008852A2 (en) | 2008-06-23 | 2010-01-21 | Taiga Biotechnologies, Inc. | Methods of trea fing λλd methods of diagnosing an immunoproliferative disorder |
| US9217012B2 (en) | 2009-04-08 | 2015-12-22 | Indiana University Research And Technology Corporation | Inhibitors of protein tyrosine phosphatases |
| WO2011057331A1 (en) | 2009-11-11 | 2011-05-19 | Monash University | A method for treating obesity |
| WO2011094806A1 (en) | 2010-02-03 | 2011-08-11 | Monash University | Diagnostic and prognostic assay for breast cancer |
| WO2014068527A1 (en) * | 2012-11-02 | 2014-05-08 | Pfizer Inc. | Bruton's tyrosine kinase inhibitors |
| CN106471004A (zh) | 2014-02-28 | 2017-03-01 | 麦吉尔大学学术发展皇家学院 | 作为用于免疫疗法的apc活化剂的tc‑ptp抑制剂 |
| US20170224731A1 (en) | 2014-06-10 | 2017-08-10 | Monash University | Method of producing leukocytes using ptpn2 inhibition for adoptive cell transfer |
| CN111303159A (zh) * | 2014-10-02 | 2020-06-19 | 豪夫迈·罗氏有限公司 | 用于治疗由布鲁顿酪氨酸激酶(btk)介导的疾病的吡唑甲酰胺化合物 |
| US20180325925A1 (en) | 2015-11-06 | 2018-11-15 | Kyungpook National University Industry-Academic Cooperation Foundation | Composition for prevention or treatment of neuroinflammatory disease, containing protein tyrosine phosphatase inhibitor |
| WO2017078499A2 (ko) | 2015-11-06 | 2017-05-11 | 경북대학교 산학협력단 | 단백질 타이로신 탈인산화효소 억제제를 포함하는 신경염증성 질환의 예방 또는 치료용 조성물 |
| WO2018148378A1 (en) | 2017-02-08 | 2018-08-16 | Dana-Farber Cancer Institute, Inc. | Modulating biomarkers to increase tumor immunity and improve the efficiacy of cancer immunotherapy |
| WO2018227248A1 (en) | 2017-06-13 | 2018-12-20 | Monash University | Methods and compositions for the treatment of obesity |
| CA3073755A1 (en) | 2017-08-24 | 2019-02-28 | The Royal Institution For The Advancement Of Learning/Mcgill Universit | Enhancing cd8+ t cells for adoptive cell therapy by inhibiting ptpn1 (ptp1b) and ptpn2 (tc-ptp) |
| AU2019290197B2 (en) * | 2018-06-21 | 2023-08-24 | Abbvie Inc. | Protein tyrosine phosphatase inhibitors and methods of use thereof |
| EP3938038A1 (en) | 2019-03-14 | 2022-01-19 | Calico Life Sciences LLC | Protein tyrosine phosphatase inhibitors and methods of use thereof |
-
2020
- 2020-03-13 EP EP20717505.0A patent/EP3938038A1/en active Pending
- 2020-03-13 JP JP2021555178A patent/JP7204005B2/ja active Active
- 2020-03-13 CR CR20210516A patent/CR20210516A/es unknown
- 2020-03-13 WO PCT/US2020/022717 patent/WO2020186199A1/en not_active Ceased
- 2020-03-13 KR KR1020237016132A patent/KR20230074822A/ko not_active Ceased
- 2020-03-13 AU AU2020234712A patent/AU2020234712B2/en active Active
- 2020-03-13 PE PE2021001510A patent/PE20212154A1/es unknown
- 2020-03-13 MX MX2021010544A patent/MX2021010544A/es unknown
- 2020-03-13 TW TW109108506A patent/TWI849082B/zh active
- 2020-03-13 CA CA3131894A patent/CA3131894A1/en active Pending
- 2020-03-13 KR KR1020217032888A patent/KR102533599B1/ko active Active
- 2020-03-13 MA MA055301A patent/MA55301A/fr unknown
- 2020-03-13 CN CN202210783687.5A patent/CN116332873A/zh active Pending
- 2020-03-13 SG SG11202109067PA patent/SG11202109067PA/en unknown
- 2020-03-13 MY MYPI2021004954A patent/MY209419A/en unknown
- 2020-03-13 BR BR112021017430A patent/BR112021017430A2/pt unknown
- 2020-03-13 TW TW113128010A patent/TW202519515A/zh unknown
- 2020-03-13 PH PH1/2021/552194A patent/PH12021552194A1/en unknown
- 2020-03-13 MX MX2024010859A patent/MX2024010859A/es unknown
- 2020-03-13 CN CN202080035755.9A patent/CN114025844B/zh active Active
- 2020-03-16 UY UY0001038613A patent/UY38613A/es unknown
- 2020-03-16 AR ARP200100729A patent/AR118374A1/es unknown
- 2020-06-04 US US16/892,786 patent/US10851073B2/en active Active
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2021
- 2021-09-13 IL IL286373A patent/IL286373B1/en unknown
- 2021-09-13 CL CL2021002382A patent/CL2021002382A1/es unknown
- 2021-09-13 DO DO2021000188A patent/DOP2021000188A/es unknown
- 2021-10-11 CO CONC2021/0013524A patent/CO2021013524A2/es unknown
- 2021-10-13 EC ECSENADI202175909A patent/ECSP21075909A/es unknown
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2022
- 2022-12-27 JP JP2022209142A patent/JP7617890B2/ja active Active
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2024
- 2024-06-11 CL CL2024001723A patent/CL2024001723A1/es unknown
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2025
- 2025-01-07 JP JP2025002163A patent/JP2025061064A/ja active Pending
- 2025-10-16 IL IL324019A patent/IL324019A/en unknown
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2007067612A1 (en) * | 2005-12-08 | 2007-06-14 | Novartis Ag | 1-orthofluorophenyl substituted 1, 2, 5-thiazolidinedione derivatives as ptp-as inhibitors |
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