PE20240545A1 - Moleculas bifuncionales novedosas para la degradacion de proteinas dirigidas - Google Patents
Moleculas bifuncionales novedosas para la degradacion de proteinas dirigidasInfo
- Publication number
- PE20240545A1 PE20240545A1 PE2023001888A PE2023001888A PE20240545A1 PE 20240545 A1 PE20240545 A1 PE 20240545A1 PE 2023001888 A PE2023001888 A PE 2023001888A PE 2023001888 A PE2023001888 A PE 2023001888A PE 20240545 A1 PE20240545 A1 PE 20240545A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- together form
- membered heterocyclic
- heteroaryl
- aryl
- Prior art date
Links
- 230000001588 bifunctional effect Effects 0.000 title abstract 4
- 230000017854 proteolysis Effects 0.000 title abstract 2
- 125000004051 hexyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 abstract 4
- 125000002373 5 membered heterocyclic group Chemical group 0.000 abstract 3
- 125000004070 6 membered heterocyclic group Chemical group 0.000 abstract 3
- 125000003341 7 membered heterocyclic group Chemical group 0.000 abstract 3
- 125000001072 heteroaryl group Chemical group 0.000 abstract 3
- 102000004169 proteins and genes Human genes 0.000 abstract 3
- 108090000623 proteins and genes Proteins 0.000 abstract 3
- 125000003118 aryl group Chemical group 0.000 abstract 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 2
- 125000002837 carbocyclic group Chemical group 0.000 abstract 1
- 230000000593 degrading effect Effects 0.000 abstract 1
- 239000003937 drug carrier Substances 0.000 abstract 1
- 239000003446 ligand Substances 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 230000008684 selective degradation Effects 0.000 abstract 1
- 125000003107 substituted aryl group Chemical group 0.000 abstract 1
Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
- A61K47/545—Heterocyclic compounds
-
- 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
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
- C07D277/08—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
- C07D277/10—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
-
- 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
- A61K31/425—Thiazoles
- A61K31/426—1,3-Thiazoles
-
- 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
-
- 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
- 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
- C07D417/06—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 only aliphatic carbon atoms
-
- 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
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- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
- G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
- G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
- G01N33/5005—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells
- G01N33/5008—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics
- G01N33/5011—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics for testing antineoplastic activity
-
- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N2500/00—Screening for compounds of potential therapeutic value
- G01N2500/10—Screening for compounds of potential therapeutic value involving cells
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Engineering & Computer Science (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Immunology (AREA)
- Biomedical Technology (AREA)
- Epidemiology (AREA)
- Molecular Biology (AREA)
- Hematology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Urology & Nephrology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Physics & Mathematics (AREA)
- Biotechnology (AREA)
- Microbiology (AREA)
- Toxicology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Analytical Chemistry (AREA)
- Physics & Mathematics (AREA)
- Food Science & Technology (AREA)
- Biochemistry (AREA)
- Cell Biology (AREA)
- Pathology (AREA)
- Peptides Or Proteins (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicinal Preparation (AREA)
Abstract
La presente invencion se refiere a una molecula bifuncional que comprende la formula general: TBL - L - Z en donde TBL es un ligando de union a proteina diana; L es un enlazador; y Z comprende una estructura de acuerdo con la formula (I): en donde R1 es alquilo C1 a C6, bencilo, bencilo sustituido, entre otros; A esta ausente o es CR2R2'; B es arilo, heteroarilo, arilo sustituido y heteroarilo sustituido; R2 y R2' son cada uno independientemente H y alquilo C1 a C6, entre otros; R3 es alquilo C1 a C6, arilo, heteroarilo, entre otros; R4 es H, alquilo C1 a C6, entre otros; o en donde R1 y R4 forman juntos un anillo heterociclico de 5, 6 o 7 miembros; o en donde cuando A es CR2R2': R1 y R2 juntos forman un anillo heterociclico de 5, 6 o 7 miembros; o R2 y R4 juntos forman un anillo heterociclico o carbociclico de 5, 6 o 7 miembros; y L muestra el punto de union del enlazador. Ademas, menciona una composicion farmaceutica que comprende la molecula bifuncional, un portador farmaceuticamente aceptable y otros, asi como un metodo para degradar y/o aumentar la proteolisis de una proteina diana en una celula. Las moleculas bifuncionales son utiles en la degradacion dirigida o selectiva de una proteina.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB2020186.9A GB202020186D0 (en) | 2020-12-18 | 2020-12-18 | Novel bifunctional molecules for targeted protein degradation |
| GBGB2102494.8A GB202102494D0 (en) | 2021-02-22 | 2021-02-22 | Novel bifunctional molecules for targeted protein degredation |
| PCT/GB2021/053332 WO2022129925A1 (en) | 2020-12-18 | 2021-12-16 | Novel bifunctional molecules for targeted protein degradation |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20240545A1 true PE20240545A1 (es) | 2024-03-19 |
Family
ID=79164461
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2023001888A PE20240545A1 (es) | 2020-12-18 | 2021-12-16 | Moleculas bifuncionales novedosas para la degradacion de proteinas dirigidas |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US20240115711A1 (es) |
| EP (1) | EP4263511A1 (es) |
| JP (1) | JP2024505328A (es) |
| KR (1) | KR20230137889A (es) |
| AU (1) | AU2021400059A1 (es) |
| CA (1) | CA3201962A1 (es) |
| CL (1) | CL2023001735A1 (es) |
| CO (1) | CO2023007768A2 (es) |
| IL (1) | IL303717A (es) |
| MX (1) | MX2023007032A (es) |
| PE (1) | PE20240545A1 (es) |
| WO (1) | WO2022129925A1 (es) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2023242598A1 (en) | 2022-06-16 | 2023-12-21 | Amphista Therapeutics Limited | Bifunctional molecules for targeted protein degradation |
| WO2023242597A1 (en) | 2022-06-16 | 2023-12-21 | Amphista Therapeutics Limited | Bifunctional molecules for targeted protein degradation |
| WO2024057021A1 (en) | 2022-09-13 | 2024-03-21 | Amphista Therapeutics Limited | Compounds for targeted protein degradation |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1991012237A1 (fr) * | 1990-02-08 | 1991-08-22 | Eisai Co., Ltd. | Derive de sulfonamide de benzene |
| PE20020354A1 (es) | 2000-09-01 | 2002-06-12 | Novartis Ag | Compuestos de hidroxamato como inhibidores de histona-desacetilasa (hda) |
| US7208157B2 (en) | 2000-09-08 | 2007-04-24 | California Institute Of Technology | Proteolysis targeting chimeric pharmaceutical |
| AU2005229522A1 (en) * | 2004-03-11 | 2005-10-13 | Actelion Pharmaceuticals Ltd. | Indol-1-yl-acetic acid derivatives |
| RU59063U1 (ru) | 2006-05-30 | 2006-12-10 | Государственное образовательное учреждение высшего профессионального образования "Ульяновский государственный технический университет" | Режущий инструмент с многослойным покрытием |
| WO2012078559A2 (en) | 2010-12-07 | 2012-06-14 | Yale University | Small-molecule hydrophobic tagging of fusion proteins and induced degradation of same |
| TW201444836A (zh) | 2013-03-14 | 2014-12-01 | Abbvie Inc | 吡咯并［２，３－ｂ］吡啶ｃｄｋ９激酶抑制劑 |
| WO2014210354A1 (en) | 2013-06-28 | 2014-12-31 | Genentech, Inc. | Azaindazole compounds as inhibitors of t790m containing egfr mutants |
| HUE061599T2 (hu) | 2017-11-15 | 2023-07-28 | Mirati Therapeutics Inc | KRas G12C inhibotorok |
| WO2019238886A1 (en) | 2018-06-13 | 2019-12-19 | University Of Dundee | Bifunctional molecules for targeting usp14 |
| CA3103185A1 (en) | 2018-06-13 | 2019-12-19 | Amphista Therapeutics Ltd | Bifunctional molecules for targeting rpn11 |
| US20210283139A1 (en) | 2018-06-13 | 2021-09-16 | Amphista Therapeutics Ltd | Bifunctional molecules for targeting uchl5 |
-
2021
- 2021-12-16 PE PE2023001888A patent/PE20240545A1/es unknown
- 2021-12-16 AU AU2021400059A patent/AU2021400059A1/en active Pending
- 2021-12-16 MX MX2023007032A patent/MX2023007032A/es unknown
- 2021-12-16 EP EP21834860.5A patent/EP4263511A1/en active Pending
- 2021-12-16 US US18/266,294 patent/US20240115711A1/en active Pending
- 2021-12-16 KR KR1020237023787A patent/KR20230137889A/ko unknown
- 2021-12-16 CA CA3201962A patent/CA3201962A1/en active Pending
- 2021-12-16 IL IL303717A patent/IL303717A/en unknown
- 2021-12-16 JP JP2023535988A patent/JP2024505328A/ja active Pending
- 2021-12-16 WO PCT/GB2021/053332 patent/WO2022129925A1/en active Application Filing
-
2023
- 2023-06-14 CO CONC2023/0007768A patent/CO2023007768A2/es unknown
- 2023-06-14 CL CL2023001735A patent/CL2023001735A1/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| JP2024505328A (ja) | 2024-02-06 |
| MX2023007032A (es) | 2023-07-18 |
| KR20230137889A (ko) | 2023-10-05 |
| CL2023001735A1 (es) | 2024-02-16 |
| AU2021400059A1 (en) | 2023-07-06 |
| CA3201962A1 (en) | 2022-06-23 |
| WO2022129925A1 (en) | 2022-06-23 |
| IL303717A (en) | 2023-08-01 |
| CO2023007768A2 (es) | 2023-09-29 |
| US20240115711A1 (en) | 2024-04-11 |
| EP4263511A1 (en) | 2023-10-25 |
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