PE20120304A1 - Derivados de 1,3-tiazolidina-2,4-diona con actividad sobre quinasas pim-1 y/o pim-2 y/o pim-3 - Google Patents
Derivados de 1,3-tiazolidina-2,4-diona con actividad sobre quinasas pim-1 y/o pim-2 y/o pim-3Info
- Publication number
- PE20120304A1 PE20120304A1 PE2010001221A PE2010001221A PE20120304A1 PE 20120304 A1 PE20120304 A1 PE 20120304A1 PE 2010001221 A PE2010001221 A PE 2010001221A PE 2010001221 A PE2010001221 A PE 2010001221A PE 20120304 A1 PE20120304 A1 PE 20120304A1
- Authority
- PE
- Peru
- Prior art keywords
- pim
- diona
- alkyl
- thiazolidine
- phenyl
- Prior art date
Links
- 101100297652 Coturnix japonica PIM3 gene Proteins 0.000 title abstract 2
- 101100297651 Mus musculus Pim2 gene Proteins 0.000 title abstract 2
- 101001001642 Xenopus laevis Serine/threonine-protein kinase pim-3 Proteins 0.000 title abstract 2
- 230000000694 effects Effects 0.000 title abstract 2
- 108091000080 Phosphotransferase Proteins 0.000 title 1
- 102000020233 phosphotransferase Human genes 0.000 title 1
- -1 CYCLOPENTHYL Chemical class 0.000 abstract 4
- ROSDSFDQCJNGOL-UHFFFAOYSA-N Dimethylamine Chemical compound CNC ROSDSFDQCJNGOL-UHFFFAOYSA-N 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 3
- WZKSXHQDXQKIQJ-UHFFFAOYSA-N F[C](F)F Chemical class F[C](F)F WZKSXHQDXQKIQJ-UHFFFAOYSA-N 0.000 abstract 2
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical compound [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 abstract 2
- 201000010099 disease Diseases 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- GOJUJUVQIVIZAV-UHFFFAOYSA-N 2-amino-4,6-dichloropyrimidine-5-carbaldehyde Chemical compound NC1=NC(Cl)=C(C=O)C(Cl)=N1 GOJUJUVQIVIZAV-UHFFFAOYSA-N 0.000 abstract 1
- VLRGXXKFHVJQOL-UHFFFAOYSA-N 3-chloropentane-2,4-dione Chemical compound CC(=O)C(Cl)C(C)=O VLRGXXKFHVJQOL-UHFFFAOYSA-N 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 102000001253 Protein Kinase Human genes 0.000 abstract 1
- XIPUIGPNIDKXJU-UHFFFAOYSA-N [CH]1CC1 Chemical class [CH]1CC1 XIPUIGPNIDKXJU-UHFFFAOYSA-N 0.000 abstract 1
- METKIMKYRPQLGS-UHFFFAOYSA-N atenolol Chemical compound CC(C)NCC(O)COC1=CC=C(CC(N)=O)C=C1 METKIMKYRPQLGS-UHFFFAOYSA-N 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 230000009088 enzymatic function Effects 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical group 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- WCYWZMWISLQXQU-UHFFFAOYSA-N methyl Chemical class [CH3] WCYWZMWISLQXQU-UHFFFAOYSA-N 0.000 abstract 1
- 108060006633 protein kinase Proteins 0.000 abstract 1
Classifications
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- 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
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- 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
- A61K31/41—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
- A61K31/427—Thiazoles not condensed 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
-
- 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
-
- 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
-
- 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
- C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three 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
- C07D277/34—Oxygen 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
- C07D417/02—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
- C07D417/02—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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Thiazole And Isothizaole Compounds (AREA)
Abstract
REFERIDA A UN COMPUESTO DERIVADO DE 1,3-TIAZOLIDINA-2,4-DIONA DE FORMULA (I), DONDE R1 ES UN GRUPO CARBOCICLILO TAL COMO CICLOPROPILO, CICLOPENTILO, CICLOHEXILO, ENTRE OTROS, UN GRUPO ARILO TAL COMO FENILO O NAFTILO, O UN GRUPO HETEROCICLILO; R1 PUEDE ESTAR OPCIONALMENTE SUSTITUIDO POR UNO O MAS R2, DONDE R2 ES HALOGENO, ALQUILO C1-C6, ALQUILO C1-C6 HALOGENADO, AMINO, ALQUIL C1-C6 AMINO, (ALQUIL C1-C6)2AMINO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: 5-({2-[(3S)-3-AMINOPIPERIDIN-1-IL]-3-CLORO-5-(TRIFLUOROMETIL) FENIL}METILIDENO-1,3-TIAZOLIDONA-2,4-DIONA, 5-({3-CLORO-2-[(3S)-3-(DIMETILAMINO)PIRROLIDIN-1-IL]-5-(TRIFLUOROMETIL)FENIL}METILIDENO)-1,3-TIAZOLIDINA-2,4-DIONA, N-{4-[3-(DIMETILAMINO)PIRROLIDIN-1-IL]-3-[(Z)-(2,4-DIOXO-1,3-TIAZOLIDIN-5-ILIDENO)METIL]FENIL}ACETAMIDA, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UN PROCEDIMIENTO DE PREPARACION. DICHOS COMPUESTOS SON INHIBIDORES O MODULADORES DE LA ACTIVIDAD O FUNCION ENZIMATICA DE LA PROTEINA QUINASA PIM-1 Y/O PIM-2 Y/O PIM-3 Y SON UTILES EN EL TRATAMIENTO DE ENFERMEDADES MEDIADAS POR DICHAS QUINASAS, PREFERIBLEMENTE, CANCER
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US7763908P | 2008-07-02 | 2008-07-02 | |
| US18327809P | 2009-06-02 | 2009-06-02 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20120304A1 true PE20120304A1 (es) | 2012-04-22 |
Family
ID=41050276
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2010001221A PE20120304A1 (es) | 2008-07-02 | 2009-07-02 | Derivados de 1,3-tiazolidina-2,4-diona con actividad sobre quinasas pim-1 y/o pim-2 y/o pim-3 |
Country Status (27)
| Country | Link |
|---|---|
| US (2) | US8901307B2 (es) |
| EP (1) | EP2310010A2 (es) |
| JP (2) | JP5261575B2 (es) |
| KR (1) | KR20110031367A (es) |
| CN (2) | CN102137666B (es) |
| AR (1) | AR072791A1 (es) |
| AU (1) | AU2009265362B2 (es) |
| BR (1) | BRPI0914599A2 (es) |
| CA (1) | CA2729557A1 (es) |
| CL (1) | CL2010001636A1 (es) |
| CO (1) | CO6341555A2 (es) |
| CR (1) | CR20110016A (es) |
| DO (1) | DOP2010000408A (es) |
| EA (1) | EA018989B1 (es) |
| EC (1) | ECSP10010735A (es) |
| HN (1) | HN2010002786A (es) |
| IL (1) | IL210127A0 (es) |
| MX (1) | MX2010014233A (es) |
| MY (1) | MY155961A (es) |
| NI (1) | NI201100007A (es) |
| NZ (1) | NZ590859A (es) |
| PE (1) | PE20120304A1 (es) |
| SV (1) | SV2011003786A (es) |
| TW (1) | TWI461423B (es) |
| UY (1) | UY31952A (es) |
| WO (1) | WO2010001169A2 (es) |
| ZA (1) | ZA201100844B (es) |
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| SI2426129T1 (sl) | 2005-12-13 | 2017-02-28 | Incyte Holdings Corporation | Heteroarilno substituirani pirolo(2,3-b)piridini in pirolo(2,3-b)pirimidini kot zaviralci janusove kinaze |
| MX342814B (es) | 2007-06-13 | 2016-10-13 | Incyte Holdings Corp | Sales de inhibidor de janus cinasa (r)-3-(4-7h-pirrolo[2,3-d]pirim idin-4-il)-1h-pirazol-1-il)-3-ciclopentilpropanitrilo. |
| UY31952A (es) * | 2008-07-02 | 2010-01-29 | Astrazeneca Ab | 5-metilideno-1,3-tiazolidina-2,4-dionas sustituidas como inhibidores de quinasa pim |
| CN102458581B (zh) | 2009-05-22 | 2016-03-30 | 因塞特控股公司 | 作为JANUS激酶抑制剂的吡唑-4-基-吡咯并[2，3-d]嘧啶和吡咯-3-基-吡咯并[2，3-d]嘧啶的N-(杂)芳基-吡咯烷衍生物 |
| HUE046493T2 (hu) | 2009-05-22 | 2020-03-30 | Incyte Holdings Corp | 3-[4-(7H-Pirrolo[2,3-d]pirimidin-4-il)-lH-pirazol-l-il]oktán- vagy heptán-nitril JAK inhibitorokként |
| WO2011028685A1 (en) | 2009-09-01 | 2011-03-10 | Incyte Corporation | Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors |
| RS57219B1 (sr) | 2010-03-10 | 2018-07-31 | Incyte Holdings Corp | Piperidin-4-il azetidin derivati kao inhibitori jak1 |
| EP3087972A1 (en) | 2010-05-21 | 2016-11-02 | Incyte Holdings Corporation | Topical formulation for a jak inhibitor |
| SG190839A1 (en) | 2010-11-19 | 2013-07-31 | Incyte Corp | Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors |
| ES2536415T3 (es) | 2010-11-19 | 2015-05-25 | Incyte Corporation | Pirrolopiridinas y pirrolopirimidinas sustituidas heterocíclicas como inhibidores de JAK |
| PH12013502612A1 (en) | 2011-06-20 | 2014-04-28 | Incyte Holdings Corp | Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors |
| TW201313721A (zh) | 2011-08-18 | 2013-04-01 | Incyte Corp | 作為ｊａｋ抑制劑之環己基氮雜環丁烷衍生物 |
| UA111854C2 (uk) | 2011-09-07 | 2016-06-24 | Інсайт Холдінгс Корпорейшн | Способи і проміжні сполуки для отримання інгібіторів jak |
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