PE20212154A1 - Inhibidores de la proteina tirosina fosfatasa y metodos para usarlos - Google Patents
Inhibidores de la proteina tirosina fosfatasa y metodos para usarlosInfo
- Publication number
- PE20212154A1 PE20212154A1 PE2021001510A PE2021001510A PE20212154A1 PE 20212154 A1 PE20212154 A1 PE 20212154A1 PE 2021001510 A PE2021001510 A PE 2021001510A PE 2021001510 A PE2021001510 A PE 2021001510A PE 20212154 A1 PE20212154 A1 PE 20212154A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- protein tyrosine
- tyrosine phosphatase
- compounds
- cycloalkyl
- Prior art date
Links
Classifications
-
- 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)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Diabetes (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Epidemiology (AREA)
- Child & Adolescent Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
Abstract
Esta referido a compuestos de Formula I, en donde: Z es C(H)(R3 ), un enlace o N(R8 ); R1 es H, halogeno, alquilo, cicloalquilo, O-alquilo; R2 es H, alquilo, alquenilo, alquilo-O-, NH2, entre otras opciones; R2' es H, -NRaRb o -N(Ra )-N(Rb )-C(O)-fenilo; R4 es H, halogeno, alquilo, cicloalquilo, alquileno-hetrociclilo; R5 es H, deuterio, halogeno, alquilo, cicloalquilo, alquileno-heterociclilo; R6 y R7 son H, deuterio. Entre los compuestos preferidos tenemos los siguientes: 5-[1-fluoro-3-hidroxi-7-(3-metilbutoxi)-5,6,7,8-tetrahidronaftalen-2-il]-1?6 ,2,5-tiadiazolidina1,1,3-triona; 5-{7-[(2-ciclopropiletil)amino]-1-fluoro-3-hidroxi-5,6,7,8-tetrahidronaftalen-2-il}-1?6 ,2,5- tiadiazolidina-1,1,3-triona; entre otros. Estos compuestos son inhibidores de la proteina tirosina fosfatasa, por ejemplo, proteina tirosina fosfatasa no receptora tipo 2 (PTPN2) y/o proteina tirosina fosfatasa no receptora tipo 1 (PTPN1), tambien denominada proteina tirosina fosfatasa 1B (PTP1B)). Estos compuestos se emplean en el tratamiento de enfermedades o trastornos como por ejemplo, cancer, diabetes tipo 2, obesidad, una enfermedad metabolica, o cualquier otra enfermedad, trastorno o dolencia que responda favorablemente al tratamiento con un inhibidor de PTPN2 o PTPN1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962818447P | 2019-03-14 | 2019-03-14 | |
| PCT/US2020/022717 WO2020186199A1 (en) | 2019-03-14 | 2020-03-13 | Protein tyrosine phosphatase inhibitors and methods of use thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20212154A1 true PE20212154A1 (es) | 2021-11-09 |
Family
ID=70190226
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2021001510A PE20212154A1 (es) | 2019-03-14 | 2020-03-13 | Inhibidores de la proteina tirosina fosfatasa y metodos para usarlos |
Country Status (22)
| Country | Link |
|---|---|
| US (1) | US10851073B2 (es) |
| EP (1) | EP3938038A1 (es) |
| JP (2) | JP7204005B2 (es) |
| KR (2) | KR20230074822A (es) |
| CN (2) | CN114025844B (es) |
| AR (1) | AR118374A1 (es) |
| AU (1) | AU2020234712A1 (es) |
| BR (1) | BR112021017430A2 (es) |
| CA (1) | CA3131894A1 (es) |
| CL (1) | CL2021002382A1 (es) |
| CO (1) | CO2021013524A2 (es) |
| CR (1) | CR20210516A (es) |
| DO (1) | DOP2021000188A (es) |
| EC (1) | ECSP21075909A (es) |
| IL (1) | IL286373A (es) |
| MA (1) | MA55301A (es) |
| MX (1) | MX2021010544A (es) |
| PE (1) | PE20212154A1 (es) |
| SG (1) | SG11202109067PA (es) |
| TW (1) | TW202100515A (es) |
| UY (1) | UY38613A (es) |
| WO (1) | WO2020186199A1 (es) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2023507774A (ja) * | 2019-12-18 | 2023-02-27 | カリコ ライフ サイエンシーズ エルエルシー | タンパク質チロシンホスファターゼ阻害剤及びそれらの使用方法 |
| MX2023002953A (es) * | 2020-09-11 | 2023-06-01 | Calico Life Sciences Llc | Inhibidores de proteína tirosina fosfatasa y métodos para su uso. |
| IL305072A (en) * | 2021-02-12 | 2023-10-01 | Recovery Therapeutics Inc | Materials, compositions and methods for modulating FGF activity |
| AU2022234402A1 (en) * | 2021-03-11 | 2023-09-28 | Kumquat Biosciences Inc. | Heterocycles and uses thereof |
| EP4351558A1 (en) * | 2021-06-10 | 2024-04-17 | 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 |
| WO2023086498A1 (en) * | 2021-11-11 | 2023-05-19 | Calico Life Sciences Llc | Protein tyrosine phosphatase inhibitors and methods of use thereof |
| WO2023086495A1 (en) * | 2021-11-11 | 2023-05-19 | Calico Life Sciences Llc | Protein tyrosine phosphatase inhibitors and methods of use thereof |
| WO2023150150A1 (en) * | 2022-02-02 | 2023-08-10 | Nerio Therapeutics, Inc. | Protein tyrosine phosphatase inhibitors and uses thereof |
| TW202342437A (zh) * | 2022-02-02 | 2023-11-01 | 美商耐瑞歐醫療公司 | 蛋白酪胺酸磷酸酶抑制劑及其用途 |
| TW202337459A (zh) * | 2022-02-02 | 2023-10-01 | 美商耐瑞歐醫療公司 | 蛋白酪胺酸磷酸酶抑制劑及其用途 |
| WO2023179542A1 (en) * | 2022-03-21 | 2023-09-28 | Gasherbrum Bio , Inc. | 5,8-dihydro-1,7-naphthyridine derivatives as glp-1 agonists for the treatment of diabetes |
| WO2024059041A1 (en) * | 2022-09-13 | 2024-03-21 | 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 |
| 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 |
Family Cites Families (22)
| 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 |
| DE69212850T2 (de) | 1991-01-15 | 1997-03-06 | Alcon Lab Inc | Verwendung von Karrageenan in topischen ophthalmologischen Zusammensetzungen |
| 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 |
| EP1439834A1 (en) | 2001-10-30 | 2004-07-28 | Applied Research Systems ARS Holding N.V. | Oxindole hydrazide modulators of protein tyrosine phosphatases (ptps) |
| UA94724C2 (en) * | 2005-12-08 | 2011-06-10 | Новартис Аг | Thiadiazolidinone derivatives as antidiabetic agents |
| UA94921C2 (en) * | 2005-12-08 | 2011-06-25 | Новартис Аг | 1-orthofluorophenyl substituted 1, 2, 5-thiazolidinedione derivatives as ptp-as inhibitors |
| EP2038267A2 (en) * | 2006-03-31 | 2009-03-25 | Novartis AG | Thiadiazolidinone inhibitors of ptpase |
| WO2008142198A2 (en) | 2007-05-23 | 2008-11-27 | Valtion Teknillinen Tutkimuskeskus | A 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 |
| WO2015127548A1 (en) | 2014-02-28 | 2015-09-03 | The Royal Institution For The Advancement Of Learning / Mcgill University | Tc-ptp inhibitors as apc activators for immunotherapy |
| US20170224731A1 (en) | 2014-06-10 | 2017-08-10 | Monash University | Method of producing leukocytes using ptpn2 inhibition for adoptive cell transfer |
| WO2017078499A2 (ko) | 2015-11-06 | 2017-05-11 | 경북대학교 산학협력단 | 단백질 타이로신 탈인산화효소 억제제를 포함하는 신경염증성 질환의 예방 또는 치료용 조성물 |
| 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 |
| 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 |
| US11597739B2 (en) | 2017-08-24 | 2023-03-07 | The Royal Institution For The Advancement Of Learning/Mcgill University | Enhancing CD8+ T cells for adoptive T cell therapy by inhibiting PTPN1 (PTP1B) and PTPN2 (TC-PTP) |
| WO2019246513A1 (en) * | 2018-06-21 | 2019-12-26 | Calico Life Sciences Llc | Protein tyrosine phosphatase inhibitors and methods of use thereof |
-
2020
- 2020-03-13 KR KR1020237016132A patent/KR20230074822A/ko active Application Filing
- 2020-03-13 CA CA3131894A patent/CA3131894A1/en active Pending
- 2020-03-13 MA MA055301A patent/MA55301A/fr unknown
- 2020-03-13 CN CN202080035755.9A patent/CN114025844B/zh active Active
- 2020-03-13 EP EP20717505.0A patent/EP3938038A1/en active Pending
- 2020-03-13 KR KR1020217032888A patent/KR102533599B1/ko active IP Right Grant
- 2020-03-13 JP JP2021555178A patent/JP7204005B2/ja active Active
- 2020-03-13 AU AU2020234712A patent/AU2020234712A1/en active Pending
- 2020-03-13 WO PCT/US2020/022717 patent/WO2020186199A1/en unknown
- 2020-03-13 TW TW109108506A patent/TW202100515A/zh unknown
- 2020-03-13 PE PE2021001510A patent/PE20212154A1/es unknown
- 2020-03-13 SG SG11202109067PA patent/SG11202109067PA/en unknown
- 2020-03-13 BR BR112021017430A patent/BR112021017430A2/pt unknown
- 2020-03-13 CN CN202210783687.5A patent/CN116332873A/zh active Pending
- 2020-03-13 MX MX2021010544A patent/MX2021010544A/es unknown
- 2020-03-13 CR CR20210516A patent/CR20210516A/es unknown
- 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
-
2021
- 2021-09-13 IL IL286373A patent/IL286373A/en unknown
- 2021-09-13 DO DO2021000188A patent/DOP2021000188A/es unknown
- 2021-09-13 CL CL2021002382A patent/CL2021002382A1/es unknown
- 2021-10-11 CO CONC2021/0013524A patent/CO2021013524A2/es unknown
- 2021-10-13 EC ECSENADI202175909A patent/ECSP21075909A/es unknown
-
2022
- 2022-12-27 JP JP2022209142A patent/JP2023052094A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| CL2021002382A1 (es) | 2022-06-03 |
| WO2020186199A1 (en) | 2020-09-17 |
| MX2021010544A (es) | 2021-10-01 |
| CO2021013524A2 (es) | 2022-02-28 |
| UY38613A (es) | 2020-09-30 |
| IL286373A (en) | 2021-10-31 |
| CN114025844A (zh) | 2022-02-08 |
| AU2020234712A1 (en) | 2021-09-09 |
| US20200299246A1 (en) | 2020-09-24 |
| CA3131894A1 (en) | 2020-09-17 |
| CN114025844B (zh) | 2022-07-26 |
| US10851073B2 (en) | 2020-12-01 |
| TW202100515A (zh) | 2021-01-01 |
| CN116332873A (zh) | 2023-06-27 |
| JP2022522526A (ja) | 2022-04-19 |
| JP7204005B2 (ja) | 2023-01-13 |
| KR102533599B1 (ko) | 2023-05-17 |
| DOP2021000188A (es) | 2022-03-15 |
| KR20210151821A (ko) | 2021-12-14 |
| KR20230074822A (ko) | 2023-05-31 |
| JP2023052094A (ja) | 2023-04-11 |
| SG11202109067PA (en) | 2021-09-29 |
| CR20210516A (es) | 2022-07-19 |
| EP3938038A1 (en) | 2022-01-19 |
| AR118374A1 (es) | 2021-09-29 |
| BR112021017430A2 (pt) | 2022-01-18 |
| ECSP21075909A (es) | 2021-11-30 |
| MA55301A (fr) | 2022-01-19 |
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