PE20240237A1 - Inhibidores heterociclicos de la cinasa rip1 - Google Patents
Inhibidores heterociclicos de la cinasa rip1Info
- Publication number
- PE20240237A1 PE20240237A1 PE2023002567A PE2023002567A PE20240237A1 PE 20240237 A1 PE20240237 A1 PE 20240237A1 PE 2023002567 A PE2023002567 A PE 2023002567A PE 2023002567 A PE2023002567 A PE 2023002567A PE 20240237 A1 PE20240237 A1 PE 20240237A1
- Authority
- PE
- Peru
- Prior art keywords
- independently
- compounds
- methyl
- inhibitors
- linker
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 101001109145 Homo sapiens Receptor-interacting serine/threonine-protein kinase 1 Proteins 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- 102100022501 Receptor-interacting serine/threonine-protein kinase 1 Human genes 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 abstract 1
- QQQCOAJFIZICNV-IBGZPJMESA-N FC1=CC=CC(=N1)CC=1C=NN(C=1)C(=O)N[C@@H]1C(N(C2=C(OC1)C=CC(=C2)C#CC(C)(C)O)C)=O Chemical compound FC1=CC=CC(=N1)CC=1C=NN(C=1)C(=O)N[C@@H]1C(N(C2=C(OC1)C=CC(=C2)C#CC(C)(C)O)C)=O QQQCOAJFIZICNV-IBGZPJMESA-N 0.000 abstract 1
- 101000971351 Homo sapiens KRR1 small subunit processome component homolog Proteins 0.000 abstract 1
- 102100021559 KRR1 small subunit processome component homolog Human genes 0.000 abstract 1
- 150000001204 N-oxides Chemical class 0.000 abstract 1
- 101710138589 Receptor-interacting serine/threonine-protein kinase 1 Proteins 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 150000002391 heterocyclic compounds Chemical class 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 230000004957 immunoregulator effect Effects 0.000 abstract 1
- 230000002757 inflammatory effect Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000003226 pyrazolyl group Chemical group 0.000 abstract 1
- 125000004076 pyridyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
Classifications
-
- 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
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Dermatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Diabetes (AREA)
- Endocrinology (AREA)
- Pulmonology (AREA)
- Pain & Pain Management (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyridine Compounds (AREA)
Abstract
Referido a compuestos heterociclicos de formula (I), o una sal, N-oxido, solvato, tautomero o estereoisomero farmaceuticamente aceptable de este; en donde el anillo B es heteroarilo de 5 o 6 miembros tal como pirazolilo o piridinilo; cada R1 es independientemente halogeno o un grupo enlazador-R6, en donde el enlazador es una union o Ra, siempre que Ra no sea H o D, y R6 es heterociclilo, Rb, -C(Rf)3, o -C(Rf)=C(Rf)2; R2 es Ra, R3 es Ray pueden ser H; cada R4 es independientemente Re; L es un heteroatomo o Ra, siempre que Ra no sea H o D; X es CH2 u O; Z es heteroarilo; m es 1-4; n es 0-2; Ra es independientemente H o D; Rb es independientemente -OH, -SH, -ORc, entre otros. Dichos compuestos son inhibidores de la proteina 1 cinasa que interactua con el receptor (RIP1). Un compuesto seleccionado es (S)-4-((6-fluoropiridin-2-il)metil)-N-(7-(3-hidroxi-3-metilbut-1-in-1-il)-5-metil-4-oxo-2,3,4,5- tetrahidrobenzo[b][1,4]oxazepin-3-il)-1H-pirazol-1-carboxamida. Tambien se refiere a metodos para preparar dichos compuestos y una composicion farmaceutica que los comprende, siendo utiles para tratar o prevenir una enfermedad o asociada a RIP 1, tal como un trastorno inflamatorio o inmunorregulador.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202163159970P | 2021-03-11 | 2021-03-11 | |
| PCT/US2022/019744 WO2022192533A1 (en) | 2021-03-11 | 2022-03-10 | Heterocyclic rip1 kinase inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20240237A1 true PE20240237A1 (es) | 2024-02-16 |
Family
ID=81327717
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2023002567A PE20240237A1 (es) | 2021-03-11 | 2022-03-10 | Inhibidores heterociclicos de la cinasa rip1 |
Country Status (19)
| Country | Link |
|---|---|
| US (1) | US20220296608A1 (es) |
| EP (1) | EP4304713A1 (es) |
| JP (1) | JP2024509466A (es) |
| KR (1) | KR20230144575A (es) |
| CN (1) | CN117083270A (es) |
| AR (1) | AR125587A1 (es) |
| AU (1) | AU2022232927A1 (es) |
| BR (1) | BR112023018167A2 (es) |
| CA (1) | CA3211778A1 (es) |
| CL (1) | CL2023002704A1 (es) |
| CO (1) | CO2023012077A2 (es) |
| CR (1) | CR20230438A (es) |
| DO (1) | DOP2023000186A (es) |
| EC (1) | ECSP23068893A (es) |
| IL (1) | IL305456A (es) |
| MX (1) | MX2023010624A (es) |
| PE (1) | PE20240237A1 (es) |
| TW (1) | TW202300490A (es) |
| WO (1) | WO2022192533A1 (es) |
Family Cites Families (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4921475A (en) | 1983-08-18 | 1990-05-01 | Drug Delivery Systems Inc. | Transdermal drug patch with microtubes |
| US5087240A (en) | 1983-08-18 | 1992-02-11 | Drug Delivery Systems Inc. | Transdermal drug patch with conductive fibers |
| US4738851A (en) | 1985-09-27 | 1988-04-19 | University Of Iowa Research Foundation, Inc. | Controlled release ophthalmic gel formulation |
| US5163899A (en) | 1987-03-20 | 1992-11-17 | Drug Delivery Systems Inc. | Transdermal drug delivery system |
| US5312325A (en) | 1987-05-28 | 1994-05-17 | Drug Delivery Systems Inc | Pulsating transdermal drug delivery system |
| GB8804164D0 (en) | 1988-02-23 | 1988-03-23 | Tucker J M | Bandage for administering physiologically active compound |
| US4882150A (en) | 1988-06-03 | 1989-11-21 | Kaufman Herbert E | Drug delivery system |
| US5008110A (en) | 1988-11-10 | 1991-04-16 | The Procter & Gamble Company | Storage-stable transdermal patch |
| US5088977A (en) | 1988-12-21 | 1992-02-18 | Drug Delivery Systems Inc. | Electrical transdermal drug applicator with counteractor and method of drug delivery |
| US5521222A (en) | 1989-09-28 | 1996-05-28 | Alcon Laboratories, Inc. | Topical ophthalmic pharmaceutical vehicles |
| CA2031376A1 (en) | 1989-12-04 | 1991-06-05 | Bahram Farhadieh | Single layer transdermal drug administration system |
| US5112596A (en) | 1990-04-23 | 1992-05-12 | Alkermes, Inc. | Method for increasing blood-brain barrier permeability by administering a bradykinin agonist of blood-brain barrier permeability |
| US5268164A (en) | 1990-04-23 | 1993-12-07 | Alkermes, Inc. | Increasing blood-brain barrier permeability with permeabilizer peptides |
| US5077033A (en) | 1990-08-07 | 1991-12-31 | Mediventures Inc. | Ophthalmic drug delivery with thermo-irreversible gels of polxoxyalkylene polymer and ionic polysaccharide |
| JP2594486B2 (ja) | 1991-01-15 | 1997-03-26 | アルコン ラボラトリーズ インコーポレイテッド | 局所的眼薬組成物 |
| US5352456A (en) | 1991-10-10 | 1994-10-04 | Cygnus Therapeutic Systems | Device for administering drug transdermally which provides an initial pulse of drug |
| DE69228827T2 (de) | 1991-12-18 | 1999-10-21 | Minnesota Mining And Mfg. Co., Saint Paul | Mehrschichtige sperrstrukturen |
| ATE132381T1 (de) | 1992-01-29 | 1996-01-15 | Voelkl Franz Ski | Ballspielschläger, insbesondere tennisschläger |
| IL114193A (en) | 1994-06-20 | 2000-02-29 | Teva Pharma | Ophthalmic pharmaceutical compositions based on sodium alginate |
| ES2094688B1 (es) | 1994-08-08 | 1997-08-01 | Cusi Lab | Manoemulsion del tipo de aceite en agua, util como vehiculo oftalmico y procedimiento para su preparacion. |
| IT1283911B1 (it) | 1996-02-05 | 1998-05-07 | Farmigea Spa | Soluzioni oftalmiche viscosizzate con polisaccaridi della gomma di tamarindo |
| US5800807A (en) | 1997-01-29 | 1998-09-01 | Bausch & Lomb Incorporated | Ophthalmic compositions including glycerin and propylene glycol |
| US6261547B1 (en) | 1998-04-07 | 2001-07-17 | Alcon Manufacturing, Ltd. | Gelling ophthalmic compositions containing xanthan gum |
| US6197934B1 (en) | 1998-05-22 | 2001-03-06 | Collagenesis, Inc. | Compound delivery using rapidly dissolving collagen film |
| US8922322B2 (en) * | 2012-08-31 | 2014-12-30 | Delta Electronics, Inc. | Combined structure of hollow bobbin and conductive sheet, hollow bobbin, and conductive sheet |
| TWI637951B (zh) * | 2013-02-15 | 2018-10-11 | 英商葛蘭素史克智慧財產發展有限公司 | 作為激酶抑制劑之雜環醯胺類 |
| CN106573006A (zh) * | 2014-08-21 | 2017-04-19 | 葛兰素史密斯克莱知识产权发展有限公司 | 作为药物的rip1激酶抑制剂杂环酰胺 |
| KR102603915B1 (ko) * | 2015-07-02 | 2023-11-21 | 에프. 호프만-라 로슈 아게 | 이환형 락탐 및 이의 사용 방법 |
| MY196648A (en) * | 2016-02-05 | 2023-04-27 | Denali Therapeutics Inc | Inhibitors of Receptor-Interacting Protein Kinase 1 |
| CN111138448B (zh) * | 2018-11-02 | 2022-08-02 | 中国科学院上海药物研究所 | 抑制rip1激酶的杂环酰胺及其用途 |
| WO2020088194A1 (zh) * | 2018-11-02 | 2020-05-07 | 中国科学院上海药物研究所 | 抑制rip1激酶的杂环酰胺及其用途 |
| EP4025568A1 (en) * | 2019-09-06 | 2022-07-13 | Rigel Pharmaceuticals, Inc. | Rip1 inhibitory compounds and methods for making and using the same |
| US11690850B2 (en) * | 2019-11-26 | 2023-07-04 | Board Of Regents, The University Of Texas System | Inhibitors of receptor interacting protein kinase I for the treatment of disease |
-
2022
- 2022-03-02 TW TW111107595A patent/TW202300490A/zh unknown
- 2022-03-02 AR ARP220100461A patent/AR125587A1/es unknown
- 2022-03-10 IL IL305456A patent/IL305456A/en unknown
- 2022-03-10 MX MX2023010624A patent/MX2023010624A/es unknown
- 2022-03-10 AU AU2022232927A patent/AU2022232927A1/en active Pending
- 2022-03-10 JP JP2023555403A patent/JP2024509466A/ja active Pending
- 2022-03-10 PE PE2023002567A patent/PE20240237A1/es unknown
- 2022-03-10 CA CA3211778A patent/CA3211778A1/en active Pending
- 2022-03-10 WO PCT/US2022/019744 patent/WO2022192533A1/en active Application Filing
- 2022-03-10 EP EP22714650.3A patent/EP4304713A1/en active Pending
- 2022-03-10 KR KR1020237030350A patent/KR20230144575A/ko active Search and Examination
- 2022-03-10 CR CR20230438A patent/CR20230438A/es unknown
- 2022-03-10 BR BR112023018167A patent/BR112023018167A2/pt unknown
- 2022-03-10 CN CN202280020689.7A patent/CN117083270A/zh active Pending
- 2022-03-10 US US17/691,596 patent/US20220296608A1/en active Pending
-
2023
- 2023-09-11 DO DO2023000186A patent/DOP2023000186A/es unknown
- 2023-09-11 EC ECSENADI202368893A patent/ECSP23068893A/es unknown
- 2023-09-11 CL CL2023002704A patent/CL2023002704A1/es unknown
- 2023-09-12 CO CONC2023/0012077A patent/CO2023012077A2/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| JP2024509466A (ja) | 2024-03-01 |
| CR20230438A (es) | 2024-01-16 |
| ECSP23068893A (es) | 2023-10-31 |
| KR20230144575A (ko) | 2023-10-16 |
| EP4304713A1 (en) | 2024-01-17 |
| US20220296608A1 (en) | 2022-09-22 |
| CN117083270A (zh) | 2023-11-17 |
| IL305456A (en) | 2023-10-01 |
| MX2023010624A (es) | 2023-11-28 |
| TW202300490A (zh) | 2023-01-01 |
| DOP2023000186A (es) | 2023-11-30 |
| CO2023012077A2 (es) | 2024-01-15 |
| AU2022232927A1 (en) | 2023-08-17 |
| BR112023018167A2 (pt) | 2023-10-31 |
| AR125587A1 (es) | 2023-08-02 |
| WO2022192533A1 (en) | 2022-09-15 |
| CL2023002704A1 (es) | 2024-03-22 |
| CA3211778A1 (en) | 2022-09-15 |
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