PE20170247A1 - Derivados de pirrolidina-2,5-diona, composiciones farmaceuticas y metodos para usar como inhibidores ido1 - Google Patents
Derivados de pirrolidina-2,5-diona, composiciones farmaceuticas y metodos para usar como inhibidores ido1Info
- Publication number
- PE20170247A1 PE20170247A1 PE2016002241A PE2016002241A PE20170247A1 PE 20170247 A1 PE20170247 A1 PE 20170247A1 PE 2016002241 A PE2016002241 A PE 2016002241A PE 2016002241 A PE2016002241 A PE 2016002241A PE 20170247 A1 PE20170247 A1 PE 20170247A1
- Authority
- PE
- Peru
- Prior art keywords
- pyrrolidine
- methods
- pharmaceutical compositions
- ido1 inhibitors
- diona
- Prior art date
Links
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 229940043367 IDO1 inhibitor Drugs 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 2
- 239000000203 mixture Substances 0.000 abstract 2
- KZNICNPSHKQLFF-UHFFFAOYSA-N succinimide Chemical compound O=C1CCC(=O)N1 KZNICNPSHKQLFF-UHFFFAOYSA-N 0.000 abstract 2
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 1
- TXQAZWIBPGKHOX-UHFFFAOYSA-N 1H-indol-3-amine Chemical compound C1=CC=C2C(N)=CNC2=C1 TXQAZWIBPGKHOX-UHFFFAOYSA-N 0.000 abstract 1
- MXKLDYKORJEOPR-UHFFFAOYSA-N 3-(5-fluoro-1h-indol-3-yl)pyrrolidine-2,5-dione Chemical compound C12=CC(F)=CC=C2NC=C1C1CC(=O)NC1=O MXKLDYKORJEOPR-UHFFFAOYSA-N 0.000 abstract 1
- 201000009273 Endometriosis Diseases 0.000 abstract 1
- 102000004190 Enzymes Human genes 0.000 abstract 1
- 108090000790 Enzymes Proteins 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 239000003937 drug carrier Substances 0.000 abstract 1
- 125000001475 halogen functional group Chemical group 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/4015—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
- C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D207/36—Oxygen or sulfur atoms
- C07D207/40—2,5-Pyrrolidine-diones
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
- C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D207/36—Oxygen or sulfur atoms
- C07D207/40—2,5-Pyrrolidine-diones
- C07D207/404—2,5-Pyrrolidine-diones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms, e.g. succinimide
- C07D207/408—Radicals containing only hydrogen and carbon atoms attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/46—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with hetero atoms directly attached to the ring nitrogen atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyrrole Compounds (AREA)
- Steroid Compounds (AREA)
Abstract
Se refiere a una composicion farmaceutica que comprende un compuesto, derivado de pirrolidina-2,5-diona, de formula I´, de formula I´´ o una mezcla de ellos; en donde: X es -NH- o -CQ2=CQ3-; Q2 y Q3 son, independientemente, H o alquilo C1-C6; R1 y R2 son, independientemente, H, halo, ciano, alquilo C1-C6 o alcoxi C1-C6; y al menos un portador farmaceuticamente aceptable. Tambien se refiere a una mezcla racemica de ambos compuestos, siendo seleccionado 3-(5-fluoro-1H-indol-3-il)pirrolidin-2,5-diona, entre otros. Dichos compuestos son inhibidores de la enzima indolamina 2,3-dioxigenasa-1 (IDO1) siendo utiles en el tratamiento o prevencion de cancer y endometriosis
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201461996976P | 2014-05-15 | 2014-05-15 | |
| EP14168534 | 2014-05-15 | ||
| BE2014/0754A BE1021251B1 (fr) | 2014-05-15 | 2014-10-21 | Derives de pyrrolidine-2,5-dione, compositions pharmaceutiques et methodes d'utilisation comme inhibiteurs de ido1 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20170247A1 true PE20170247A1 (es) | 2017-03-29 |
Family
ID=54479389
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2016002241A PE20170247A1 (es) | 2014-05-15 | 2015-05-14 | Derivados de pirrolidina-2,5-diona, composiciones farmaceuticas y metodos para usar como inhibidores ido1 |
Country Status (20)
| Country | Link |
|---|---|
| US (3) | US9603836B2 (es) |
| EP (1) | EP3148531A1 (es) |
| JP (1) | JP6231226B2 (es) |
| KR (1) | KR101873672B1 (es) |
| CN (1) | CN106536480B (es) |
| AP (1) | AP2016009527A0 (es) |
| AU (1) | AU2015260826B2 (es) |
| CA (1) | CA2948842C (es) |
| CU (1) | CU20160162A7 (es) |
| DO (1) | DOP2016000299A (es) |
| EA (1) | EA201650031A1 (es) |
| IL (1) | IL248915A0 (es) |
| MD (1) | MD20160118A2 (es) |
| MX (1) | MX2016015005A (es) |
| PE (1) | PE20170247A1 (es) |
| SG (1) | SG11201608708WA (es) |
| TN (1) | TN2016000501A1 (es) |
| TW (1) | TWI567059B (es) |
| UY (1) | UY36122A (es) |
| WO (1) | WO2015173764A1 (es) |
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| GB201311891D0 (en) | 2013-07-03 | 2013-08-14 | Glaxosmithkline Ip Dev Ltd | Novel compound |
| GB201311888D0 (en) | 2013-07-03 | 2013-08-14 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| US20180228907A1 (en) | 2014-04-14 | 2018-08-16 | Arvinas, Inc. | Cereblon ligands and bifunctional compounds comprising the same |
| MX2016015005A (es) | 2014-05-15 | 2017-09-28 | Iteos Therapeutics | Derivados de pirrolidina-2,5-diona, composiciones farmaceuticas y metodos para usar como inhibidores ido1. |
| BR112017019699A2 (pt) | 2015-03-17 | 2018-09-04 | Pfizer Inc. | derivados substituídos por 3-indol, composições farmacêuticas e métodos para uso |
| WO2016181349A1 (en) | 2015-05-14 | 2016-11-17 | Pfizer Inc. | Combinations comprising a pyrrolidine-2,5-dione ido1 inhibitor and an anti-body |
| IL274151B (en) | 2015-05-21 | 2022-07-01 | Harpoon Therapeutics Inc | Trispecific binding proteins and methods of use |
| EP3334733A1 (en) | 2015-08-10 | 2018-06-20 | Pfizer Inc | 3-indol substituted derivatives, pharmaceutical compositions and methods for use |
| SG11201805621SA (en) | 2016-01-19 | 2018-08-30 | Pfizer | Cancer vaccines |
| EP3426638B1 (en) | 2016-03-09 | 2020-05-06 | Netherlands Translational Research Center B.V. | Inhibitors of indoleamine 2,3-dioxygenase |
| EP3455219A4 (en) | 2016-05-10 | 2019-12-18 | C4 Therapeutics, Inc. | AMINE-RELATED C3-GLUTARIMIDE DEGRONIMERS FOR TARGET PROTEIN REDUCTION |
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| WO2018089301A1 (en) * | 2016-11-08 | 2018-05-17 | The Johns Hopkins University | Pharmaceutical treatments for preventing or treating pancreatic cancer |
| EP3570832A4 (en) | 2017-01-17 | 2020-06-10 | Board Of Regents, The University Of Texas System | COMPOUNDS AS INHIBITORS OF INDOLAMINE-2,3-DIOXYGENASE AND / OR TRYPTOPHANE-DIOXYGENASE |
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| EP3694529B1 (en) | 2017-10-13 | 2024-06-26 | Harpoon Therapeutics, Inc. | Trispecific proteins and methods of use |
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| WO2020018670A1 (en) | 2018-07-17 | 2020-01-23 | Board Of Regents, The University Of Texas System | Compounds useful as inhibitors of indoleamine 2,3-dioxygenase and/or tryptophan dioxygenase |
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| TW202333802A (zh) | 2021-10-11 | 2023-09-01 | 德商拜恩迪克公司 | 用於肺癌之治療性rna(二) |
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2015
- 2015-05-14 MX MX2016015005A patent/MX2016015005A/es unknown
- 2015-05-14 UY UY0001036122A patent/UY36122A/es not_active Application Discontinuation
- 2015-05-14 KR KR1020167031517A patent/KR101873672B1/ko not_active Expired - Fee Related
- 2015-05-14 AU AU2015260826A patent/AU2015260826B2/en not_active Ceased
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- 2015-05-14 CN CN201580024882.8A patent/CN106536480B/zh not_active Expired - Fee Related
- 2015-05-14 US US14/711,911 patent/US9603836B2/en active Active
- 2015-05-14 JP JP2016567533A patent/JP6231226B2/ja not_active Expired - Fee Related
- 2015-05-14 PE PE2016002241A patent/PE20170247A1/es not_active Application Discontinuation
- 2015-05-14 EP EP15731680.3A patent/EP3148531A1/en not_active Withdrawn
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- 2015-05-14 EA EA201650031A patent/EA201650031A1/ru unknown
- 2015-05-14 WO PCT/IB2015/053557 patent/WO2015173764A1/en not_active Ceased
- 2015-05-14 SG SG11201608708WA patent/SG11201608708WA/en unknown
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- 2015-05-14 TN TN2016000501A patent/TN2016000501A1/en unknown
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2016
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2018
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| DOP2016000299A (es) | 2017-03-15 |
| CN106536480B (zh) | 2019-09-03 |
| KR20160146807A (ko) | 2016-12-21 |
| US9949951B2 (en) | 2018-04-24 |
| KR101873672B1 (ko) | 2018-07-02 |
| MX2016015005A (es) | 2017-09-28 |
| AU2015260826A1 (en) | 2016-11-03 |
| SG11201608708WA (en) | 2016-11-29 |
| JP6231226B2 (ja) | 2017-11-15 |
| JP2017515850A (ja) | 2017-06-15 |
| CN106536480A8 (zh) | 2017-06-30 |
| US10398679B2 (en) | 2019-09-03 |
| CA2948842A1 (en) | 2015-11-19 |
| US20150329525A1 (en) | 2015-11-19 |
| AU2015260826B2 (en) | 2019-10-24 |
| TN2016000501A1 (en) | 2018-04-04 |
| US9603836B2 (en) | 2017-03-28 |
| IL248915A0 (en) | 2017-01-31 |
| TW201605794A (zh) | 2016-02-16 |
| WO2015173764A1 (en) | 2015-11-19 |
| MD20160118A2 (ro) | 2017-04-30 |
| EP3148531A1 (en) | 2017-04-05 |
| UY36122A (es) | 2016-01-08 |
| AP2016009527A0 (en) | 2016-10-31 |
| CA2948842C (en) | 2019-09-24 |
| US20180214415A1 (en) | 2018-08-02 |
| CU20160162A7 (es) | 2017-03-03 |
| TWI567059B (zh) | 2017-01-21 |
| CN106536480A (zh) | 2017-03-22 |
| US20170035731A1 (en) | 2017-02-09 |
| EA201650031A1 (ru) | 2017-06-30 |
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