AR072791A1 - DERIVADOS DE TIAZOLIDIN-2, 4-DIONA, MÉTODOS PARA SU PREPARACIoN, COMPOSICIoN FARMACÉUTICA QUE LOS COMPRENDE Y SU USO EN LA ELABORACIoN DE UN MEDICAMENTO PARA EL TRATAMIENTO DEL CÁNCER. - Google Patents
DERIVADOS DE TIAZOLIDIN-2, 4-DIONA, MÉTODOS PARA SU PREPARACIoN, COMPOSICIoN FARMACÉUTICA QUE LOS COMPRENDE Y SU USO EN LA ELABORACIoN DE UN MEDICAMENTO PARA EL TRATAMIENTO DEL CÁNCER.Info
- Publication number
- AR072791A1 AR072791A1 ARP090102486A ARP090102486A AR072791A1 AR 072791 A1 AR072791 A1 AR 072791A1 AR P090102486 A ARP090102486 A AR P090102486A AR P090102486 A ARP090102486 A AR P090102486A AR 072791 A1 AR072791 A1 AR 072791A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- heterocyclyl
- pim
- carbocyclyl
- aryl
- Prior art date
Links
- 206010028980 Neoplasm Diseases 0.000 title abstract 4
- 201000011510 cancer Diseases 0.000 title abstract 4
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 4
- 238000000034 method Methods 0.000 title abstract 3
- 229940126601 medicinal product Drugs 0.000 title 1
- -1 nitro, cyano, hydroxy, amino, mercapto, formyl Chemical group 0.000 abstract 20
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 7
- 125000000623 heterocyclic group Chemical group 0.000 abstract 5
- 125000003118 aryl group Chemical group 0.000 abstract 4
- 125000004452 carbocyclyl group Chemical group 0.000 abstract 4
- 229910052736 halogen Inorganic materials 0.000 abstract 4
- 150000002367 halogens Chemical group 0.000 abstract 4
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 abstract 3
- GOJUJUVQIVIZAV-UHFFFAOYSA-N 2-amino-4,6-dichloropyrimidine-5-carbaldehyde Chemical group NC1=NC(Cl)=C(C=O)C(Cl)=N1 GOJUJUVQIVIZAV-UHFFFAOYSA-N 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 2
- 125000004738 (C1-C6) alkyl sulfinyl group Chemical group 0.000 abstract 2
- 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 abstract 2
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 abstract 2
- 102000001253 Protein Kinase Human genes 0.000 abstract 2
- 125000004391 aryl sulfonyl group Chemical group 0.000 abstract 2
- 101100297651 Mus musculus Pim2 gene Proteins 0.000 abstract 1
- 101001001642 Xenopus laevis Serine/threonine-protein kinase pim-3 Proteins 0.000 abstract 1
- 238000003745 diagnosis Methods 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 230000002255 enzymatic effect Effects 0.000 abstract 1
- 230000009088 enzymatic function Effects 0.000 abstract 1
- 125000003754 ethoxycarbonyl group Chemical group C(=O)(OCC)* 0.000 abstract 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 abstract 1
- 125000006125 ethylsulfonyl group Chemical group 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 125000001160 methoxycarbonyl group Chemical group [H]C([H])([H])OC(*)=O 0.000 abstract 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 1
- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 abstract 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 108060006633 protein kinase Proteins 0.000 abstract 1
- 108010083755 proto-oncogene proteins pim Proteins 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 208000024891 symptom Diseases 0.000 abstract 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 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
-
- 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)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Hematology (AREA)
- Oncology (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
Estos compuestos actuan como inhibidores o moduladores de la actividad o funcion enzimática de las proteína quinasas Pim-1 y/o Pim-2 y/o Pim-3. Se proveen además métodos para su preparacion composiciones farmacéuticas que comprenden a los compuestos divulgados en la presente y su uso en la prevencion y el tratamiento de condiciones y enfermedades relacionadas con Pim quinasas, preferentemente cáncer. Reivindicacion 1: Un método de tratar o prevenir el cáncer, caracterizado porque comprende. a) proveer una composicion farmacéutica que comprende un compuesto de la formula 1, o sus sales, cuya funcionalidad es inhibir una quinasa Pim, donde R1 se selecciona entre un carbociclilo, arilo, y heterociclilo, donde R1 se sustituye opcionalmente con uno o más R2 iguales o diferentes: R2 se selecciona entre halogeno, alquilo C1-6, alquilo C1-6 halogenado, amino, aIquilamino C1-6, (alquil C1-6)2amino, y heterociclilo, donde R2 se sustituye opcionalmente con uno o más R3 iguales o diferentes; R3 se selecciona entre alquilo C1-6, halogeno, nitro, ciano, hidroxi, amino, mercapto, formilo, carboxi, carbamoilo, alcoxi C1-6, alquiltio C1-6, alquilamino C1-6, (alquil C1-6)2amino, alquilsulfinilo C1-6, alquilsulfonilo C1-6, arilsulfonilo, carbociclilo, arilo, y heterociclilo, donde R3 se sustituye opcionalmente con uno o más R4 iguales o diferentes; R4 se selecciona entre alquilo C1-6, halogeno, nitro, ciano, hidroxi, amino, mercapto, formilo, carboxi, carbamoilo, alcoxi C1-6, alquiltio C1-6, alquilamino C1-6, (alquil C1-6)2amino, alquilsulfinilo C1-6, alquilsulfonilo C1-6, arilsulfonilo, carbociclilo, arilo, y heterociclilo, donde R4 se sustituye opcionalmente con uno o más R5 iguales o diferentes; y R5 se selecciona entre halogeno, nitro, ciano, hidroxi, trifluorometoxi, trifluorometilo, amino, formilo, carboxi, carbamoilo, mercapto, sulfamoilo, metilo, etilo, metoxi, etoxi, acetilo, acetoxi, metilamino, etilamino, dimetilamino, dietilamino, N-metil-N-etilamino, acetilamino, N-metilcarbamoilo, N-etilcarbamoilo, N,N-dimetilcarbamoilo. N,N-dietilcarbamoilo, N-metil-N-etilcarbamoilo, metiltio, etiltio, metilsulfinilo, etilsulfinilo, mesilo, etilsulfonilo, metoxicarbonilo, etoxicarbonilo, N-metilsulfamoilo, N-etilsulfamoilo, N,N-dimetilsulfamoilo, N,N-dietilsulfamoilo, N-metil-N-etilsulfamoilo, carbociclilo, arilo, y heterociclilo; y b) administrar dicha composicion farmacéutica a un sujeto con diagnostico, síntomas , o en riesgo de contraer cáncer.
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 |
|---|---|
| AR072791A1 true AR072791A1 (es) | 2010-09-22 |
Family
ID=41050276
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP090102486A AR072791A1 (es) | 2008-07-02 | 2009-07-02 | DERIVADOS DE TIAZOLIDIN-2, 4-DIONA, MÉTODOS PARA SU PREPARACIoN, COMPOSICIoN FARMACÉUTICA QUE LOS COMPRENDE Y SU USO EN LA ELABORACIoN DE UN MEDICAMENTO PARA EL TRATAMIENTO DEL CÁNCER. |
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) |
Families Citing this family (62)
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|---|---|---|---|---|
| DK3184526T3 (en) | 2005-12-13 | 2019-01-14 | Incyte Holdings Corp | PYRROLO [2,3-D] PYRIMIDINE DERIVATIVES AS A JANUS-KINASE INHIBITOR |
| DK2740731T3 (en) | 2007-06-13 | 2016-04-11 | Incyte Holdings Corp | CRYSTALLINE SALTS OF JANUSKINASEINHIBITOREN (R) -3- (4- (7H-pyrrolo [2,3-d] pyrimidin-4-yl) -1H-pyrazol-1-yl) -3-CYCLOPENTYLPROPANNITRIL |
| TWI461423B (zh) * | 2008-07-02 | 2014-11-21 | Astrazeneca Ab | 用於治療Pim激酶相關病狀及疾病之噻唑啶二酮化合物 |
| MY156727A (en) | 2009-05-22 | 2016-03-15 | Incyte Corp | N-(hetero)aryl-pyrrolidine derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines and pyrrol-3-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors |
| AU2010249443B2 (en) | 2009-05-22 | 2015-08-13 | Incyte Holdings Corporation | 3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]octane- or heptane-nitrile as JAK inhibitors |
| TW201113285A (en) | 2009-09-01 | 2011-04-16 | Incyte Corp | Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors |
| AU2011224484A1 (en) | 2010-03-10 | 2012-09-27 | Incyte Holdings Corporation | Piperidin-4-yl azetidine derivatives as JAK1 inhibitors |
| MY161078A (en) | 2010-05-21 | 2017-04-14 | Incyte Holdings Corp | Topical formulation for a jak inhibitor |
| WO2012068440A1 (en) | 2010-11-19 | 2012-05-24 | Incyte Corporation | Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as jak inhibitors |
| EP2640723A1 (en) | 2010-11-19 | 2013-09-25 | Incyte Corporation | Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors |
| KR20140040819A (ko) | 2011-06-20 | 2014-04-03 | 인사이트 코포레이션 | Ｊａｋ 저해제로서의 아제티디닐 페닐, 피리딜 또는 피라지닐 카르복스아미드 유도체 |
| 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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| WO2013173720A1 (en) | 2012-05-18 | 2013-11-21 | Incyte Corporation | Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors |
| JO3407B1 (ar) | 2012-05-31 | 2019-10-20 | Eisai R&D Man Co Ltd | مركبات رباعي هيدرو بيرازولو بيريميدين |
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| ME03780B (me) | 2013-01-15 | 2021-04-20 | Incyte Holdings Corp | Jedinjenja tiazolkarboksamida i piridinkarboksamida korisna kao inhibitori pim kinaze |
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| JP6769982B2 (ja) | 2015-03-06 | 2020-10-14 | ビヨンドスプリング ファーマシューティカルズ，インコーポレイテッド | Ｒａｓ変異と関連するがんの治療方法 |
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