AR054078A1 - Procedimiento para la preparacion de dihidropteridinonas - Google Patents
Procedimiento para la preparacion de dihidropteridinonasInfo
- Publication number
- AR054078A1 AR054078A1 ARP050103384A ARP050103384A AR054078A1 AR 054078 A1 AR054078 A1 AR 054078A1 AR P050103384 A ARP050103384 A AR P050103384A AR P050103384 A ARP050103384 A AR P050103384A AR 054078 A1 AR054078 A1 AR 054078A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- group
- aryl
- radical selected
- hydrogen
- Prior art date
Links
- 238000000034 method Methods 0.000 title abstract 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 5
- 229910052739 hydrogen Inorganic materials 0.000 abstract 5
- 239000001257 hydrogen Substances 0.000 abstract 5
- 125000005842 heteroatom Chemical group 0.000 abstract 4
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 3
- 125000006652 (C3-C12) cycloalkyl group Chemical group 0.000 abstract 3
- 125000005915 C6-C14 aryl group Chemical group 0.000 abstract 3
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000004400 (C1-C12) alkyl group Chemical group 0.000 abstract 1
- 125000004769 (C1-C4) alkylsulfonyl group Chemical group 0.000 abstract 1
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 abstract 1
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 abstract 1
- 125000006374 C2-C10 alkenyl group Chemical group 0.000 abstract 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 1
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 1
- 125000005974 C6-C14 arylcarbonyl group Chemical group 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000003302 alkenyloxy group Chemical group 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 1
- 125000004448 alkyl carbonyl group Chemical group 0.000 abstract 1
- 125000004390 alkyl sulfonyl group Chemical group 0.000 abstract 1
- 125000000304 alkynyl group Chemical group 0.000 abstract 1
- 125000005133 alkynyloxy group Chemical group 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 125000004391 aryl sulfonyl group Chemical group 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 125000004366 heterocycloalkenyl group Chemical group 0.000 abstract 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 125000002757 morpholinyl group Chemical group 0.000 abstract 1
- 150000002829 nitrogen Chemical group 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 125000004193 piperazinyl group Chemical group 0.000 abstract 1
- -1 piperazinylcarbonyl Chemical group 0.000 abstract 1
- 125000003386 piperidinyl group Chemical group 0.000 abstract 1
- 125000005592 polycycloalkyl group Polymers 0.000 abstract 1
- 125000004309 pyranyl group Chemical group O1C(C=CC=C1)* 0.000 abstract 1
- 125000004076 pyridyl group Chemical group 0.000 abstract 1
- 125000000714 pyrimidinyl group Chemical group 0.000 abstract 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 abstract 1
- 229920006395 saturated elastomer Polymers 0.000 abstract 1
- 125000004568 thiomorpholinyl group Chemical group 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
- C07C235/42—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton
- C07C235/44—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring
- C07C235/54—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring
-
- 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
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
- C07D295/12—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
- C07D295/135—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D475/00—Heterocyclic compounds containing pteridine ring systems
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Hydrogenated Pyridines (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
La se refiere a un procedimiento para la preparacion de dihidropteridinonas. Reivindicacion 1: Procedimiento para la preparacion de dihidropteridinonas de la formula general (1), en la que significan: R1, R2 iguales o distintos, hidrogeno o alquilo C1-6 eventualmente sustituido; o R1 y R2 juntos un puente alquilo de 2 a 5 miembros, que puede contener 1 a 2 heteroátomos; R3 hidrogeno o un radical seleccionado del grupo compuesto por alquilo C1-12, alquenilo C2-12, alquinilo C2-12 y arilo C6-14 eventualmente sustituidos; o un radical seleccionado del grupo compuesto por cicloalquilo C3-12, cicloalquilo C3-12, policicloalquilo C7-12, policicloalquenilo C7-12, espirocicloalquilo C5-12, heterocicloalquilo C3-12 eventualmente sustituidos y/o en puente, que contiene 1 a 2 heteroátomos y heterocicloalquenilo C3-12 que contiene 1 a 2 heteroátomos; o R1 y R3 o R2 y R3 juntos un puente de alquilo C3-4 saturado o insaturado, que eventualmente puede contener 1 heteroátomo; R4 es un radical seleccionado del grupo compuesto por hidrogeno, -CN, hidroxi, -NR6R7 y halogeno; o un radical seleccionado del grupo compuesto por alquilo C1-6, alquenilo C2-6, alquinilo C2-6, alquiloxi C1-5, alqueniloxi C2-5, alquiniloxi C2-5, alquiltio C1-6, alquilsulfoxo C1-6 y alquilsulfonilo C1-6 eventualmente sustituidos; L es un ligador seleccionado del grupo compuesto por alquilo C2-10, alquenilo C2-10, arilo C6-14, -alquilC2-4-ariloC6-14, -arilC6-14-alquiloC1-4 eventualmente sustituidos, cicloalquilo C3-12 eventualmente en puente y heteroarilo que eventualmente contiene 1 o 2 átomos de nitrogeno; n es 0 o 1; m es 1 o 2; R5 es un radical seleccionado del grupo compuesto por morfolinilo, piperidinilo, piperazinilo, piperazinilcarbonilo, pirrolidinilo, tropenilo, R8-dicetometilpiperazinilo, sulfoxomorfolinilo, sulfonilmofolinilo, tiomorfolinilo, -NR8R9 y azacicloheptilo eventualmente sustituidos; R6, R7 iguales o distintos, hidrogeno o alquilo C1-4; y R8, R9 sustituyentes no sustituidos de nitrogeno en R5, iguales o distintos, ya sea hidrogeno o un radical seleccionado del grupo compuesto por alquilo C1-6, -alquilC1-4-cicloalquiloC3-10, cicloalquilo C3-10, arilo C6-14, -alquilC1-4-ariloC6-14, piranilo, piridinilo, pirimidinilo, alquiloxicarbonilo C1-4, arilcarbonilo C6-14, alquilcarbonilo C1-4, arilmetiloxicarbonilo C6-14, arilsulfonilo C6-14, alquilsulfonilo C1-4 y arilC6-14-alquilsulfoniloC1-4; caracterizado porque se hace reaccionar un compuesto de la formula (2), en la que: R1 a R3 presentan el significado indicado y A es un grupo lábil; con un compuesto de la formula (3), en la que R4, R5, L y M, n pueden representar el significado indicado.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP04019365 | 2004-08-14 | ||
| EP05001611 | 2005-01-27 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR054078A1 true AR054078A1 (es) | 2007-06-06 |
Family
ID=35907775
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP050103384A AR054078A1 (es) | 2004-08-14 | 2005-08-12 | Procedimiento para la preparacion de dihidropteridinonas |
Country Status (30)
| Country | Link |
|---|---|
| US (3) | US7759485B2 (es) |
| EP (1) | EP1778668B1 (es) |
| JP (2) | JP5094391B2 (es) |
| KR (1) | KR101214394B1 (es) |
| CN (1) | CN101023070B (es) |
| AR (1) | AR054078A1 (es) |
| AU (1) | AU2005274338B2 (es) |
| BR (1) | BRPI0514361A8 (es) |
| CA (1) | CA2576290C (es) |
| CL (1) | CL2010000204A1 (es) |
| CY (1) | CY1114564T1 (es) |
| DK (1) | DK1778668T3 (es) |
| EA (1) | EA013820B1 (es) |
| EC (1) | ECSP077248A (es) |
| ES (1) | ES2429873T3 (es) |
| HR (1) | HRP20130890T1 (es) |
| IL (1) | IL181303A (es) |
| ME (1) | ME01599B (es) |
| MX (1) | MX2007001852A (es) |
| MY (2) | MY150538A (es) |
| NO (1) | NO20070753L (es) |
| NZ (1) | NZ553650A (es) |
| PE (2) | PE20060644A1 (es) |
| PL (1) | PL1778668T3 (es) |
| PT (1) | PT1778668E (es) |
| RS (1) | RS52917B (es) |
| SI (1) | SI1778668T1 (es) |
| TW (1) | TWI355383B (es) |
| UY (1) | UY29061A1 (es) |
| WO (1) | WO2006018220A2 (es) |
Families Citing this family (47)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6861422B2 (en) * | 2003-02-26 | 2005-03-01 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Dihydropteridinones, processes for preparing them and their use as pharmaceutical compositions |
| DE102004029784A1 (de) * | 2004-06-21 | 2006-01-05 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue 2-Benzylaminodihydropteridinone, Verfahren zur deren Herstellung und deren Verwendung als Arzneimittel |
| DE102004033670A1 (de) * | 2004-07-09 | 2006-02-02 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Pyridodihydropyrazinone, Verfahren zu Ihrer Herstellung und Ihre Verwendung als Arzneimittel |
| US20060035903A1 (en) * | 2004-08-14 | 2006-02-16 | Boehringer Ingelheim International Gmbh | Storage stable perfusion solution for dihydropteridinones |
| US20060074088A1 (en) * | 2004-08-14 | 2006-04-06 | Boehringer Ingelheim International Gmbh | Dihydropteridinones for the treatment of cancer diseases |
| US20060058311A1 (en) | 2004-08-14 | 2006-03-16 | Boehringer Ingelheim International Gmbh | Combinations for the treatment of diseases involving cell proliferation |
| US7759485B2 (en) | 2004-08-14 | 2010-07-20 | Boehringer Ingelheim International Gmbh | Process for the manufacture of dihydropteridinones |
| US7728134B2 (en) * | 2004-08-14 | 2010-06-01 | Boehringer Ingelheim International Gmbh | Hydrates and polymorphs of 4[[(7R)-8-cyclopentyl-7-ethyl-5,6,7,8-tetrahydro-5-methyl-6-oxo-2-pteridinyl]amino]-3-methoxy-N-(1-methyl-4-piperidinyl)-benzamide, process for their manufacture and their use as medicament |
| EP1630163A1 (de) * | 2004-08-25 | 2006-03-01 | Boehringer Ingelheim Pharma GmbH & Co.KG | Dihydropteridinonderivative, Verfahren zu deren Herstellung und deren Verwendung als Arzneimittel |
| EP1632493A1 (de) * | 2004-08-25 | 2006-03-08 | Boehringer Ingelheim Pharma GmbH & Co.KG | Dihydropteridinonderivative, Verfahren zu deren Herstellung und deren Verwendung als Arzneimittel |
| DE102004058337A1 (de) * | 2004-12-02 | 2006-06-14 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Verfahren zur Herstellung von annelierten Piperazin-2-on Derivaten |
| US7439358B2 (en) | 2006-02-08 | 2008-10-21 | Boehringer Ingelheim International Gmbh | Specific salt, anhydrous and crystalline form of a dihydropteridione derivative |
| TW200808325A (en) | 2006-07-06 | 2008-02-16 | Astrazeneca Ab | Novel compounds |
| WO2008009909A1 (en) * | 2006-07-17 | 2008-01-24 | Astrazeneca Ab | Pteridimones as modulators of polo-like kinase |
| US8883790B2 (en) | 2006-10-12 | 2014-11-11 | Astex Therapeutics Limited | Pharmaceutical combinations |
| US8916552B2 (en) | 2006-10-12 | 2014-12-23 | Astex Therapeutics Limited | Pharmaceutical combinations |
| CA2695406A1 (en) * | 2007-08-03 | 2009-02-12 | Boehringer Ingelheim International Gmbh | Crystalline form of a dihydropteridione derivative |
| EP2100894A1 (en) | 2008-03-12 | 2009-09-16 | 4Sc Ag | Pyridopyrimidines used as Plk1 (polo-like kinase) inhibitors |
| CN102020643A (zh) | 2009-09-22 | 2011-04-20 | 上海恒瑞医药有限公司 | 二氢喋啶酮类衍生物、其制备方法及其在医药上的应用 |
| EP2569434B1 (en) | 2010-05-14 | 2019-09-04 | Dana-Farber Cancer Institute, Inc. | Compositions and methods for treating leukemia and related disorders |
| US9301962B2 (en) | 2010-05-14 | 2016-04-05 | Baylor College Of Medicine | Male contraceptive compositions and methods of use |
| AU2011252808B2 (en) | 2010-05-14 | 2015-05-14 | Dana-Farber Cancer Institute, Inc. | Compositions and methods for treating neoplasia, inflammatory disease and other disorders |
| US8546566B2 (en) * | 2010-10-12 | 2013-10-01 | Boehringer Ingelheim International Gmbh | Process for manufacturing dihydropteridinones and intermediates thereof |
| US9358233B2 (en) | 2010-11-29 | 2016-06-07 | Boehringer Ingelheim International Gmbh | Method for treating acute myeloid leukemia |
| ES2533042T3 (es) | 2011-02-25 | 2015-04-07 | Takeda Pharmaceutical Company Limited | Oxazinopteridinas y oxazinopteridinonas N-sustituidas |
| US9370535B2 (en) | 2011-05-17 | 2016-06-21 | Boehringer Ingelheim International Gmbh | Method for treatment of advanced solid tumors |
| UY34893A (es) | 2012-07-10 | 2014-02-28 | Takeda Pharmaceutical | Derivados de azaindol |
| WO2014159392A1 (en) | 2013-03-14 | 2014-10-02 | Dana-Farber Cancer Institute, Inc. | Bromodomain binding reagents and uses thereof |
| US9975896B2 (en) | 2013-07-25 | 2018-05-22 | Dana-Farber Cancer Institute, Inc. | Inhibitors of transcription factors and uses thereof |
| US20150031699A1 (en) | 2013-07-26 | 2015-01-29 | Boehringer Ingelheim International Gmbh | Treatment of myelodysplastic syndrome |
| EP3066101B1 (en) | 2013-11-08 | 2020-07-29 | Dana-Farber Cancer Institute, Inc. | Combination therapy for cancer using bromodomain and extra-terminal (bet) protein inhibitors |
| UY35945A (es) | 2014-01-09 | 2015-08-31 | Takeda Pharmaceutical | Derivados de azaindol |
| MX2016009975A (es) * | 2014-01-31 | 2016-10-31 | Dana Farber Cancer Inst Inc | Derivados de dihidropteridinona y sus usos. |
| HK1225383A1 (zh) | 2014-01-31 | 2017-09-08 | 达纳-法伯癌症研究所股份有限公司 | 二氮杂环庚烷衍生物及其用途 |
| CN106029653A (zh) | 2014-01-31 | 2016-10-12 | 达纳-法伯癌症研究所股份有限公司 | 二氨基嘧啶苯砜衍生物及其用途 |
| WO2015117087A1 (en) | 2014-01-31 | 2015-08-06 | Dana-Farber Cancer Institute, Inc. | Uses of diazepane derivatives |
| CN106456653A (zh) | 2014-02-28 | 2017-02-22 | 腾沙治疗公司 | 高胰岛素血症相关病症的治疗 |
| CN104003989B (zh) * | 2014-05-26 | 2015-11-11 | 苏州明锐医药科技有限公司 | 伏拉塞替及其中间体的制备方法 |
| MX2017001757A (es) * | 2014-08-08 | 2017-05-30 | Dana Farber Cancer Inst Inc | Derivados de dihidropteridinona y sus usos. |
| BR112017002369A2 (pt) | 2014-08-08 | 2017-12-05 | Dana Farber Cancer Inst Inc | derivados de diazepana e usos dos mesmos |
| US9867831B2 (en) | 2014-10-01 | 2018-01-16 | Boehringer Ingelheim International Gmbh | Combination treatment of acute myeloid leukemia and myelodysplastic syndrome |
| EP3212654B1 (en) | 2014-10-27 | 2020-04-08 | Tensha Therapeutics, Inc. | Bromodomain inhibitors |
| CN105646398B (zh) * | 2014-12-05 | 2018-09-07 | 上海医药工业研究院 | N-((1r,4r)-4-(4-(环丙基甲基)哌嗪-1-基)环己基)乙酰胺的制备方法 |
| EP3307728A4 (en) | 2015-06-12 | 2019-07-17 | Dana Farber Cancer Institute, Inc. | COMBINATION THERAPY OF TRANSCRIPTION INHIBITORS AND CHINESE INHIBITORS |
| PE20181086A1 (es) | 2015-09-11 | 2018-07-05 | Dana Farber Cancer Inst Inc | Acetamida tienotrizolodiazepinas y usos de las mismas |
| RU2750164C2 (ru) | 2015-09-11 | 2021-06-22 | Дана-Фарбер Кэнсер Инститьют, Инк. | Цианотиенотриазолодиазепины и пути их применения |
| MX2018006499A (es) | 2015-11-25 | 2018-08-01 | Dana Farber Cancer Inst Inc | Inhibidores de bromodominio bivalentes y usos de los mismos. |
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