ES2282410T3 - Derivados de isoquinolinona como inhibidores de parp. - Google Patents
Derivados de isoquinolinona como inhibidores de parp. Download PDFInfo
- Publication number
- ES2282410T3 ES2282410T3 ES02724438T ES02724438T ES2282410T3 ES 2282410 T3 ES2282410 T3 ES 2282410T3 ES 02724438 T ES02724438 T ES 02724438T ES 02724438 T ES02724438 T ES 02724438T ES 2282410 T3 ES2282410 T3 ES 2282410T3
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- VDBNYAPERZTOOF-UHFFFAOYSA-N isoquinolin-1(2H)-one Chemical class C1=CC=C2C(=O)NC=CC2=C1 VDBNYAPERZTOOF-UHFFFAOYSA-N 0.000 title abstract description 6
- 239000012661 PARP inhibitor Substances 0.000 title description 6
- 229940121906 Poly ADP ribose polymerase inhibitor Drugs 0.000 title description 6
- 150000001875 compounds Chemical class 0.000 claims abstract description 102
- 229920000776 Poly(Adenosine diphosphate-ribose) polymerase Polymers 0.000 claims abstract description 30
- 230000005764 inhibitory process Effects 0.000 claims abstract description 14
- 239000003814 drug Substances 0.000 claims abstract description 12
- 238000011282 treatment Methods 0.000 claims abstract description 11
- 201000010099 disease Diseases 0.000 claims abstract description 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract description 4
- 150000003839 salts Chemical class 0.000 claims description 18
- 239000012453 solvate Substances 0.000 claims description 14
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 11
- 239000002671 adjuvant Substances 0.000 claims description 7
- 238000002360 preparation method Methods 0.000 claims description 6
- 239000003085 diluting agent Substances 0.000 claims description 5
- 239000008194 pharmaceutical composition Substances 0.000 claims description 5
- 230000005865 ionizing radiation Effects 0.000 claims description 4
- 239000003795 chemical substances by application Substances 0.000 claims description 3
- 230000000973 chemotherapeutic effect Effects 0.000 claims description 2
- 125000001207 fluorophenyl group Chemical group 0.000 claims description 2
- 238000011275 oncology therapy Methods 0.000 claims description 2
- 102000012338 Poly(ADP-ribose) Polymerases Human genes 0.000 abstract description 2
- 108010061844 Poly(ADP-ribose) Polymerases Proteins 0.000 abstract description 2
- -1 oxygen radicals Chemical class 0.000 description 51
- 239000000203 mixture Substances 0.000 description 41
- 125000003118 aryl group Chemical group 0.000 description 40
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 33
- 125000000623 heterocyclic group Chemical group 0.000 description 29
- 101710179684 Poly [ADP-ribose] polymerase Proteins 0.000 description 27
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- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 22
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- 229910052757 nitrogen Inorganic materials 0.000 description 14
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 13
- 125000004429 atom Chemical group 0.000 description 13
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- 125000006701 (C1-C7) alkyl group Chemical group 0.000 description 8
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- ZWEHNKRNPOVVGH-UHFFFAOYSA-N 2-Butanone Chemical compound CCC(C)=O ZWEHNKRNPOVVGH-UHFFFAOYSA-N 0.000 description 6
- QGNQEODJYRGEJX-UHFFFAOYSA-N 4h-isoquinoline-1,3-dione Chemical compound C1=CC=C2C(=O)NC(=O)CC2=C1 QGNQEODJYRGEJX-UHFFFAOYSA-N 0.000 description 6
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- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 description 6
- KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical compound C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 description 6
- 239000004480 active ingredient Substances 0.000 description 6
- 229910052796 boron Inorganic materials 0.000 description 6
- 125000004122 cyclic group Chemical group 0.000 description 6
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- 239000003381 stabilizer Substances 0.000 description 6
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 description 5
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- 150000008163 sugars Chemical class 0.000 description 1
- 125000000475 sulfinyl group Chemical group [*:2]S([*:1])=O 0.000 description 1
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- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 description 1
- 125000002088 tosyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1C([H])([H])[H])S(*)(=O)=O 0.000 description 1
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Classifications
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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
- C07D401/12—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 chain containing hetero atoms as chain links
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/472—Non-condensed isoquinolines, e.g. papaverine
- A61K31/4725—Non-condensed isoquinolines, e.g. papaverine 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
- C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems 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 carbon atoms of the nitrogen-containing ring
- C07D217/24—Oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—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
- C07D405/02—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 two hetero rings
- C07D405/06—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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—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
- C07D405/02—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 two hetero rings
- C07D405/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms 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
- C07D417/02—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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Other In-Based Heterocyclic Compounds (AREA)
Applications Claiming Priority (4)
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|---|---|---|---|
| US28963101P | 2001-05-08 | 2001-05-08 | |
| US289631P | 2001-05-08 | ||
| US34527402P | 2002-01-03 | 2002-01-03 | |
| US345274P | 2002-01-03 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2282410T3 true ES2282410T3 (es) | 2007-10-16 |
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| Application Number | Title | Priority Date | Filing Date |
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| ES02724438T Expired - Lifetime ES2282410T3 (es) | 2001-05-08 | 2002-04-30 | Derivados de isoquinolinona como inhibidores de parp. |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US6664269B2 (enExample) |
| EP (1) | EP1397350B1 (enExample) |
| JP (1) | JP2004528376A (enExample) |
| AT (1) | ATE355278T1 (enExample) |
| CA (1) | CA2444531A1 (enExample) |
| DE (1) | DE60218458T2 (enExample) |
| ES (1) | ES2282410T3 (enExample) |
| WO (1) | WO2002090334A1 (enExample) |
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| US7151102B2 (en) | 2000-10-30 | 2006-12-19 | Kudos Pharmaceuticals Limited | Phthalazinone derivatives |
| JP4500161B2 (ja) | 2002-04-30 | 2010-07-14 | クドス ファーマシューティカルズ リミテッド | フタラジノン誘導体 |
| KR100735781B1 (ko) | 2002-10-01 | 2007-07-06 | 미쯔비시 웰 파마 가부시키가이샤 | 이소퀴놀린 화합물 및 그의 의약 용도 |
| US7501412B2 (en) | 2002-11-22 | 2009-03-10 | Mitsubishi Tanabe Pharma Corporation | Isoquinoline compounds and medicinal use thereof |
| EP1633724B1 (en) * | 2003-03-12 | 2011-05-04 | Kudos Pharmaceuticals Limited | Phthalazinone derivatives |
| GB0305681D0 (en) | 2003-03-12 | 2003-04-16 | Kudos Pharm Ltd | Phthalazinone derivatives |
| US7449464B2 (en) | 2003-03-12 | 2008-11-11 | Kudos Pharmaceuticals Limited | Phthalazinone derivatives |
| GB0317466D0 (en) | 2003-07-25 | 2003-08-27 | Univ Sheffield | Use |
| CN1905864B (zh) * | 2003-12-01 | 2011-04-06 | 库多斯药物有限公司 | 用于治疗癌症的dna损伤修复抑制剂 |
| EP1684736B1 (en) * | 2003-12-01 | 2011-08-24 | Kudos Pharmaceuticals Limited | Dna damage repair inhibitors for treatment of cancer |
| DE102004028973A1 (de) * | 2004-06-16 | 2006-01-05 | Sanofi-Aventis Deutschland Gmbh | Substituierte Tetrahydro-2H-isochinolin-1-on-Derivate, Verfahren zu ihrer Herstellung und ihre Verwendung als Medikament |
| MX2007002318A (es) * | 2004-08-26 | 2007-04-17 | Kudos Pharm Ltd | Derivados de ftalazinona substituidos con 4-heteroarilmetilo. |
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| EP1831225A2 (en) | 2004-11-19 | 2007-09-12 | The Regents of the University of California | Anti-inflammatory pyrazolopyrimidines |
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-
2002
- 2002-04-30 ES ES02724438T patent/ES2282410T3/es not_active Expired - Lifetime
- 2002-04-30 CA CA002444531A patent/CA2444531A1/en not_active Abandoned
- 2002-04-30 WO PCT/GB2002/001967 patent/WO2002090334A1/en not_active Ceased
- 2002-04-30 AT AT02724438T patent/ATE355278T1/de not_active IP Right Cessation
- 2002-04-30 US US10/135,247 patent/US6664269B2/en not_active Expired - Fee Related
- 2002-04-30 EP EP02724438A patent/EP1397350B1/en not_active Expired - Lifetime
- 2002-04-30 JP JP2002587414A patent/JP2004528376A/ja not_active Ceased
- 2002-04-30 DE DE60218458T patent/DE60218458T2/de not_active Expired - Fee Related
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| Publication number | Publication date |
|---|---|
| US6664269B2 (en) | 2003-12-16 |
| DE60218458T2 (de) | 2007-11-15 |
| EP1397350B1 (en) | 2007-02-28 |
| EP1397350A1 (en) | 2004-03-17 |
| DE60218458D1 (de) | 2007-04-12 |
| US20030008896A1 (en) | 2003-01-09 |
| WO2002090334A1 (en) | 2002-11-14 |
| ATE355278T1 (de) | 2006-03-15 |
| CA2444531A1 (en) | 2002-11-14 |
| JP2004528376A (ja) | 2004-09-16 |
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