AR049540A1 - Derivados de quinazolindiona como inhibidores del parp; metodos para su preparacion; composiciones farmaceuticas que los contienen como ingrediente activo y su uso en medicamentos para el tratamiento o prevencion del cancer. - Google Patents
Derivados de quinazolindiona como inhibidores del parp; metodos para su preparacion; composiciones farmaceuticas que los contienen como ingrediente activo y su uso en medicamentos para el tratamiento o prevencion del cancer.Info
- Publication number
- AR049540A1 AR049540A1 ARP050102689A ARP050102689A AR049540A1 AR 049540 A1 AR049540 A1 AR 049540A1 AR P050102689 A ARP050102689 A AR P050102689A AR P050102689 A ARP050102689 A AR P050102689A AR 049540 A1 AR049540 A1 AR 049540A1
- Authority
- AR
- Argentina
- Prior art keywords
- formula
- quinazolindione
- alkanediyl
- piperidinyl
- compound
- Prior art date
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- 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
- C07D401/02—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 two hetero rings
- C07D401/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
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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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- A61P13/12—Drugs for disorders of the urinary system of the kidneys
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
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- 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
- A61P37/02—Immunomodulators
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- 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
- C07D401/02—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 two hetero rings
- C07D401/06—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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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- 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
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- 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
- C07D403/12—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 linked by a chain containing hetero atoms as chain links
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- 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
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Abstract
Derivados de quinazolindiona como inhibidores de PARP así como también composiciones farmacéuticas que los contengan y su uso en medicamentos para la profilaxis o el tratamiento del cáncer. Reivindicacion 1: Un compuesto de la formula (1), las formas N-oxidos, las sales de adicion farmacéuticamente aceptables y las formas estereoquímicamente isoméricas de las mismas, donde cada X es independientemente >N-, o >CH-; y cuando X es >CH- entonces Y es >N-; cada Y es independientemente >N-, o >CH-; excepto cuando X es >CH- entonces Y es >N-; L1 es un enlace directo o un radical bivalente seleccionado de alcanodiilo C1-6; L2 es un enlace directo o un radical bivalente seleccionado de carbonilo, alcanodiilo C1-6, -(hidroxi)alcanodiilo C1- 6, -C(O)-alcanodiilo C1-6 o alcanodiilo C1-6-C(O)-; R1 es H o hidroxi; y Z es H o un radical seleccionado del grupo de formulas (2) donde R2 se selecciona independientemente de H, halo o alquilo C1-6 con la condicion de que 1-[1-[(2S)-2-[(2R)-3,4- dihidro-2H-1-benzopiran-2-il]-2-hidroxietil]-4-piperidinil]-2,4-(1H,3H)-quinazolindiona, 1-[2-[4-(4-fluorbenzoil)-1-piperidinil]etil]-2,4-(1H,3H)-quinazolindiona, 1-[3-[4-(4-fluorbenzoil)-1-piperidinil]propil]-2,4-(1H,3H)-quinazolindiona, 3-[2-[4-(4- clorobenzoil)-1-piperidinil]etil]-2,4-(1H,3H)-quinazolindiona y 3-[2-[4-[(4-fluorfenil)hidroximetil]-1-piperidinil]etil]-2,4-(1H,3H)-quinazolindiona no están incluidos. Reivindicacion 13: Un proceso para la preparacion de un compuesto como se reivindico en la reivindicacion 1, caracterizado por a) la reaccion de un producto intermedio de la formula (3) con un producto intermedio de la formula (4), donde W es un grupo saliente apropiado, con la formacion de un compuesto de la formula (5), donde X es >N-, en un solvente inerte de reaccion y con el agregado de una base adecuada, o b) la reaccion de un producto intermedio de la formula (6) con un producto intermedio de la formula (7), donde W es un grupo saliente apropiado, con la formacion de un compuesto de la formula (8), donde Y es >N-, en un solvente inerte de reaccion y con el agregado de una base apropiada.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP04076885 | 2004-06-30 |
Publications (1)
Publication Number | Publication Date |
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AR049540A1 true AR049540A1 (es) | 2006-08-09 |
Family
ID=34979083
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP050102689A AR049540A1 (es) | 2004-06-30 | 2005-06-29 | Derivados de quinazolindiona como inhibidores del parp; metodos para su preparacion; composiciones farmaceuticas que los contienen como ingrediente activo y su uso en medicamentos para el tratamiento o prevencion del cancer. |
Country Status (21)
Country | Link |
---|---|
US (4) | US8080557B2 (es) |
EP (1) | EP1763523B1 (es) |
JP (1) | JP5100376B2 (es) |
CN (1) | CN1980913B (es) |
AR (1) | AR049540A1 (es) |
AU (1) | AU2005259190B2 (es) |
BR (1) | BRPI0512938A (es) |
CA (1) | CA2569827C (es) |
EA (1) | EA011552B1 (es) |
EG (1) | EG25942A (es) |
ES (1) | ES2415771T3 (es) |
HK (1) | HK1105957A1 (es) |
IL (1) | IL180409A0 (es) |
MX (1) | MXPA06014541A (es) |
NO (2) | NO20070529L (es) |
NZ (1) | NZ551801A (es) |
SG (1) | SG154432A1 (es) |
TW (1) | TWI359142B (es) |
UA (1) | UA88012C2 (es) |
WO (1) | WO2006003148A1 (es) |
ZA (1) | ZA200610771B (es) |
Families Citing this family (38)
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CA2546002C (en) | 2003-11-20 | 2012-09-18 | Janssen Pharmaceutica N.V. | 7-phenylalkyl substituted 2-quinolinones and 2-quinoxalinones as poly(adp-ribose) polymerase inhibitors |
CA2546300C (en) | 2003-11-20 | 2012-10-02 | Janssen Pharmaceutica N.V. | 6-alkenyl and 6-phenylalkyl substituted 2-quinolinones and 2-quinoxalinones as poly(adp-ribose) polymerase inhibitors |
JP4806353B2 (ja) * | 2003-12-05 | 2011-11-02 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | ポリ(adp−リボース)ポリメラーゼインヒビターとしての6−置換2−キノリノンおよび2−キノキサリノン |
MXPA06014543A (es) | 2004-06-30 | 2007-03-23 | Janssen Pharmaceutica Nv | Derivados de quinazolinona como inhibidores de la poli(adp-ribosa)polimerasa-i. |
ES2563954T3 (es) | 2004-06-30 | 2016-03-16 | Janssen Pharmaceutica Nv | Derivados de ftalazina como inhibidores de PARP |
CN1980913B (zh) | 2004-06-30 | 2011-12-14 | 詹森药业有限公司 | 作为parp抑制剂的喹唑啉二酮衍生物 |
MY150958A (en) * | 2005-06-16 | 2014-03-31 | Astrazeneca Ab | Compounds for the treatment of multi-drug resistant bacterial infections |
SG164368A1 (en) | 2005-07-18 | 2010-09-29 | Bipar Sciences Inc | Treatment of cancer |
CA2662517A1 (en) | 2006-09-05 | 2008-03-13 | Jerome Moore | Treatment of cancer |
WO2008030891A2 (en) | 2006-09-05 | 2008-03-13 | Bipar Sciences, Inc. | Inhibition of fatty acid synthesis by parp inhibitors and methods of treatment thereof |
WO2008107478A1 (en) | 2007-03-08 | 2008-09-12 | Janssen Pharmaceutica Nv | Quinolinone derivatives as parp and tank inhibitors |
JP5525447B2 (ja) | 2007-10-26 | 2014-06-18 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | Parp阻害剤としてのキノリノン誘導体 |
US7732491B2 (en) | 2007-11-12 | 2010-06-08 | Bipar Sciences, Inc. | Treatment of breast cancer with a PARP inhibitor alone or in combination with anti-tumor agents |
JP5464609B2 (ja) * | 2008-03-27 | 2014-04-09 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | チューブリン重合阻害剤としてのキナゾリノン誘導体 |
WO2009118382A1 (en) | 2008-03-27 | 2009-10-01 | Janssen Pharmaceutica Nv | Tetrahydrophenanthridinones and tetrahydrocyclopentaquinolinones as parp and tubulin polymerization inhibitors |
WO2010081778A1 (en) | 2009-01-17 | 2010-07-22 | Universität Zürich | Blockers of parp for the prevention and treatment of helicobacter pylori induced gastric cancer |
FR2943673B1 (fr) * | 2009-03-27 | 2013-03-29 | Sanofi Aventis | Applications therapeutiques de derives de quinazolinedione |
WO2011058367A2 (en) | 2009-11-13 | 2011-05-19 | Astrazeneca Ab | Diagnostic test for predicting responsiveness to treatment with poly(adp-ribose) polymerase (parp) inhibitor |
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CN103130723B (zh) | 2011-11-30 | 2015-01-14 | 成都地奥制药集团有限公司 | 一种多聚(adp-核糖)聚合酶抑制剂 |
EP2858995A1 (en) * | 2012-06-07 | 2015-04-15 | F. Hoffmann-La Roche AG | Pyrrolopyrimidone and pyrrolopyridone inhibitors of tankyrase |
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EP3325623B3 (en) | 2015-07-23 | 2021-01-20 | Institut Curie | Use of a combination of dbait molecule and parp inhibitors to treat cancer |
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EP3438096B1 (en) * | 2016-04-01 | 2020-12-02 | Impact Therapeutics, Inc | Manufacturing process for 1-(arylmethyl) quinazoline-2,4 (1h, 3h)-dione |
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- 2005-06-28 EP EP05771970A patent/EP1763523B1/en active Active
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- 2005-06-28 WO PCT/EP2005/053031 patent/WO2006003148A1/en active Application Filing
- 2005-06-28 SG SG200904449-6A patent/SG154432A1/en unknown
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- 2005-06-28 MX MXPA06014541A patent/MXPA06014541A/es active IP Right Grant
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