SI2797921T1 - Condensed tetra- or pentacyclic dihydrodiazepinocarbazolones as PARP inhibitors - Google Patents
Condensed tetra- or pentacyclic dihydrodiazepinocarbazolones as PARP inhibitors Download PDFInfo
- Publication number
- SI2797921T1 SI2797921T1 SI201131351T SI201131351T SI2797921T1 SI 2797921 T1 SI2797921 T1 SI 2797921T1 SI 201131351 T SI201131351 T SI 201131351T SI 201131351 T SI201131351 T SI 201131351T SI 2797921 T1 SI2797921 T1 SI 2797921T1
- Authority
- SI
- Slovenia
- Prior art keywords
- heteroaryl
- alkyl
- heterocyclyl
- cycloalkyl
- aryl
- Prior art date
Links
- 239000012661 PARP inhibitor Substances 0.000 title claims 2
- 229940121906 Poly ADP ribose polymerase inhibitor Drugs 0.000 title claims 2
- 150000003839 salts Chemical class 0.000 claims abstract 9
- 125000000217 alkyl group Chemical group 0.000 claims 38
- 125000001072 heteroaryl group Chemical group 0.000 claims 38
- 125000000753 cycloalkyl group Chemical group 0.000 claims 37
- 125000000623 heterocyclic group Chemical group 0.000 claims 37
- 125000003118 aryl group Chemical group 0.000 claims 36
- 125000003342 alkenyl group Chemical group 0.000 claims 35
- 125000000304 alkynyl group Chemical group 0.000 claims 34
- 229910052739 hydrogen Inorganic materials 0.000 claims 19
- 239000001257 hydrogen Substances 0.000 claims 19
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 18
- 125000001424 substituent group Chemical group 0.000 claims 18
- 150000001875 compounds Chemical class 0.000 claims 16
- 229910052736 halogen Inorganic materials 0.000 claims 10
- 150000002367 halogens Chemical class 0.000 claims 10
- 125000004429 atom Chemical group 0.000 claims 9
- 229920006395 saturated elastomer Polymers 0.000 claims 7
- 125000001188 haloalkyl group Chemical group 0.000 claims 6
- 125000005842 heteroatom Chemical group 0.000 claims 6
- 125000003710 aryl alkyl group Chemical group 0.000 claims 5
- 101100134929 Gallus gallus COR9 gene Chemical group 0.000 claims 3
- JCXJVPUVTGWSNB-UHFFFAOYSA-N Nitrogen dioxide Chemical compound O=[N]=O JCXJVPUVTGWSNB-UHFFFAOYSA-N 0.000 claims 3
- 102000012338 Poly(ADP-ribose) Polymerases Human genes 0.000 claims 2
- 108010061844 Poly(ADP-ribose) Polymerases Proteins 0.000 claims 2
- 229920000776 Poly(Adenosine diphosphate-ribose) polymerase Polymers 0.000 claims 2
- 230000005764 inhibitory process Effects 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 239000000203 mixture Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/06—Peri-condensed systems
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
- A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
- A61K31/5517—1,4-Benzodiazepines, e.g. diazepam or clozapine condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
-
- 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
- C07D471/12—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 three hetero rings
- C07D471/16—Peri-condensed systems
-
- 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
- C07D471/22—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 systems contains four or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
- C07D487/14—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Rheumatology (AREA)
- Engineering & Computer Science (AREA)
- Pain & Pain Management (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PCT/CN2011/085148 WO2013097225A1 (en) | 2011-12-31 | 2011-12-31 | Fused tetra or penta-cyclic dihydrodiazepinocarbazolones as parp inhibitors |
| EP11878508.8A EP2797921B1 (en) | 2011-12-31 | 2011-12-31 | Fused tetra or penta-cyclic dihydrodiazepinocarbazolones as parp inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| SI2797921T1 true SI2797921T1 (en) | 2018-01-31 |
Family
ID=48696280
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SI201131351T SI2797921T1 (en) | 2011-12-31 | 2011-12-31 | Condensed tetra- or pentacyclic dihydrodiazepinocarbazolones as PARP inhibitors |
Country Status (29)
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2011384858B2 (en) | 2011-12-31 | 2016-05-05 | Beigene, Ltd. | Fused tetra or penta-cyclic dihydrodiazepinocarbazolones as PARP inhibitors |
| CA2865511A1 (en) | 2012-03-07 | 2013-09-12 | Institute Of Cancer Research: Royal Cancer Hospital (The) | 3-aryl-5-substituted-isoquinolin-1-one compounds and their therapeutic use |
| US9611223B2 (en) | 2013-09-11 | 2017-04-04 | Institute Of Cancer Research: Royal Cancer Hospital (The) | 3-aryl-5-substituted-isoquinolin-1-one compounds and their therapeutic use |
| NZ739876A (en) * | 2015-08-25 | 2022-09-30 | Beigene Ltd | Process for preparing parp inhibitor, crystalline forms, and uses thereof |
| EP3442971B1 (en) | 2016-04-01 | 2024-09-25 | Recurium IP Holdings, LLC | Estrogen receptor modulators |
| CN110087730B (zh) * | 2016-09-27 | 2023-03-28 | 百济神州(苏州)生物科技有限公司 | 使用包含parp抑制剂的组合产品治疗癌症 |
| CN115433187B (zh) * | 2017-02-28 | 2023-10-27 | 百济神州(苏州)生物科技有限公司 | 稠合的四环或五环二氢二氮杂䓬并咔唑酮的盐的结晶形式组合物及其用途 |
| CN106883232B (zh) * | 2017-03-31 | 2019-01-22 | 苏州康润医药有限公司 | 一种氮杂非那烯-3-酮的衍生物及其制备方法与应用 |
| TW201908317A (zh) * | 2017-07-17 | 2019-03-01 | 開曼群島商百濟神州有限公司 | 使用parp抑制劑、替莫唑胺及/或放射療法的組合治療癌症 |
| TW202002985A (zh) * | 2018-06-01 | 2020-01-16 | 英屬開曼群島商百濟神州有限公司 | 在胃癌治療中的parp抑制劑維持療法 |
| CN111171031B (zh) * | 2019-05-10 | 2021-04-09 | 百济神州(苏州)生物科技有限公司 | 一种含parp抑制剂倍半水合物产物的制备方法 |
| CN113402502B (zh) * | 2019-05-16 | 2022-10-14 | 百济神州(苏州)生物科技有限公司 | 一种parp抑制剂中间体制备的物料组合体系 |
| AU2020282478A1 (en) * | 2019-05-31 | 2021-09-16 | Beigene, Ltd. | PARP inhibitor pellet preparation and preparation process therefor |
| AU2020326691A1 (en) | 2019-08-06 | 2022-03-03 | Recurium Ip Holdings, Llc | Estrogen receptor modulators for treating mutants |
| WO2021046014A1 (en) | 2019-09-03 | 2021-03-11 | Teva Czech Industries S.R.O | Solid state forms of pamiparib and process for preparation thereof |
| TW202508595A (zh) | 2023-05-04 | 2025-03-01 | 美商銳新醫藥公司 | 用於ｒａｓ相關疾病或病症之組合療法 |
| US20250049810A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| US20250154171A1 (en) | 2023-10-12 | 2025-05-15 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
Family Cites Families (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SE445326B (sv) | 1983-04-05 | 1986-06-16 | Malmstroem Anders E H | Sett och anordning for forhindrande av veggturbulens |
| US6799298B2 (en) | 1998-03-11 | 2004-09-28 | Overture Services, Inc. | Technique for locating an item of interest within a stored representation of data |
| SI20691B (sl) | 1999-01-11 | 2008-10-31 | Agouron Pharma | Triciklični inhibitorji poli(ADP-riboza) polimeraz |
| DE60142921D1 (de) | 2000-12-01 | 2010-10-07 | Eisai Inc | Azaphenanthridone-derivate und deren verwendung als parp-inhibitoren |
| US6423705B1 (en) | 2001-01-25 | 2002-07-23 | Pfizer Inc. | Combination therapy |
| US6906096B2 (en) | 2002-06-28 | 2005-06-14 | Irm Llc | 4,7-Disubstituted indoles and methods of making |
| PL378372A1 (pl) * | 2003-01-09 | 2006-04-03 | Pfizer Inc. | Tricykliczne związki jako inhibitory kinaz białkowych do wzmacniania skuteczności środków przeciwnowotworowych i radioterapii |
| MXPA05012812A (es) | 2003-05-28 | 2006-02-28 | Guilford Pharm Inc | Compuestos, metodos y composiciones farmaceuticas para inhibir poli(adenosina-5'-difosfo-ribosa)polimerasa(parp). |
| CA2648369A1 (en) | 2006-04-04 | 2007-10-11 | Pfizer Products Inc. | Polymorphic forms of (2r,z)-2-amino-2-cyclohexyl-n-(5-(1-methyl-1h-pyrazol-4?l)-1-oxo-2,6-dihydro-1h-[1,2]diazepino[4,5,6-cd]indol-8-yl)acetamide |
| BRPI0709731A2 (pt) | 2006-04-04 | 2011-07-26 | Pfizer Prod Inc | terapia de combinaÇço de (2r,z)-2-amino-2-cicloexil-n-(5-(1-metil-1h-pirazol-4-il)-1- oxo-2,6-diidro-1h-[1,2]diazepino[4,5,6-cd]indol-8-il)acet amida |
| WO2009063244A1 (en) | 2007-11-15 | 2009-05-22 | Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. | Pyridazinone derivatives as parp inhibitors |
| CA2732797C (en) | 2008-08-06 | 2017-01-03 | Biomarin Pharmaceutical Inc. | Dihydropyridophthalazinone inhibitors of poly(adp-ribose)polymerase (parp) |
| WO2011130661A1 (en) | 2010-04-16 | 2011-10-20 | Biomarin Pharmaceutical Inc. | Methods of using dihydropyridophthalazinone inhibitors of poly (adp-ribose)polymerase (parp) |
| AU2011384858B2 (en) | 2011-12-31 | 2016-05-05 | Beigene, Ltd. | Fused tetra or penta-cyclic dihydrodiazepinocarbazolones as PARP inhibitors |
| CA2924172C (en) | 2013-09-13 | 2020-06-30 | Beigene, Ltd. | Anti-pd1 antibodies and their use as therapeutics and diagnostics |
| CN110156892B (zh) | 2014-07-03 | 2023-05-16 | 百济神州有限公司 | 抗pd-l1抗体及其作为治疗剂及诊断剂的用途 |
| US9637488B2 (en) | 2015-01-29 | 2017-05-02 | Fuqiang Ruan | Heterocyclic compounds as inhibitors of class I PI3KS |
| NZ739876A (en) | 2015-08-25 | 2022-09-30 | Beigene Ltd | Process for preparing parp inhibitor, crystalline forms, and uses thereof |
| CN110087730B (zh) | 2016-09-27 | 2023-03-28 | 百济神州(苏州)生物科技有限公司 | 使用包含parp抑制剂的组合产品治疗癌症 |
| CN115433187B (zh) | 2017-02-28 | 2023-10-27 | 百济神州(苏州)生物科技有限公司 | 稠合的四环或五环二氢二氮杂䓬并咔唑酮的盐的结晶形式组合物及其用途 |
| TW201908317A (zh) | 2017-07-17 | 2019-03-01 | 開曼群島商百濟神州有限公司 | 使用parp抑制劑、替莫唑胺及/或放射療法的組合治療癌症 |
-
2011
- 2011-12-31 AU AU2011384858A patent/AU2011384858B2/en not_active Ceased
- 2011-12-31 JP JP2014549295A patent/JP6034877B2/ja not_active Expired - Fee Related
- 2011-12-31 RS RS20171228A patent/RS56616B1/sr unknown
- 2011-12-31 KR KR1020147018104A patent/KR101716012B1/ko active Active
- 2011-12-31 NZ NZ624063A patent/NZ624063A/en not_active IP Right Cessation
- 2011-12-31 HU HUE11878508A patent/HUE035153T2/en unknown
- 2011-12-31 PL PL11878508T patent/PL2797921T3/pl unknown
- 2011-12-31 EA EA201491303A patent/EA027533B1/ru not_active IP Right Cessation
- 2011-12-31 IN IN6169DEN2014 patent/IN2014DN06169A/en unknown
- 2011-12-31 ES ES11878508.8T patent/ES2645814T3/es active Active
- 2011-12-31 SI SI201131351T patent/SI2797921T1/en unknown
- 2011-12-31 DK DK11878508.8T patent/DK2797921T3/en active
- 2011-12-31 BR BR112014012628A patent/BR112014012628B8/pt active IP Right Grant
- 2011-12-31 SG SG11201401726VA patent/SG11201401726VA/en unknown
- 2011-12-31 NO NO11878508A patent/NO2797921T3/no unknown
- 2011-12-31 US US14/369,374 patent/US9260440B2/en active Active
- 2011-12-31 EP EP17183473.2A patent/EP3315500B1/en active Active
- 2011-12-31 CN CN201610603192.4A patent/CN106220635B/zh active Active
- 2011-12-31 PT PT118785088T patent/PT2797921T/pt unknown
- 2011-12-31 EP EP11878508.8A patent/EP2797921B1/en active Active
- 2011-12-31 SM SM20170543T patent/SMT201700543T1/it unknown
- 2011-12-31 CA CA2856309A patent/CA2856309C/en active Active
- 2011-12-31 WO PCT/CN2011/085148 patent/WO2013097225A1/en not_active Application Discontinuation
- 2011-12-31 CN CN201180072418.8A patent/CN103703004B/zh active Active
- 2011-12-31 LT LTEP11878508.8T patent/LT2797921T/lt unknown
- 2011-12-31 HR HRP20171883TT patent/HRP20171883T1/hr unknown
- 2011-12-31 ME MEP-2017-278A patent/ME02855B/me unknown
- 2011-12-31 MX MX2014007840A patent/MX353578B/es active IP Right Grant
-
2014
- 2014-06-25 IL IL233365A patent/IL233365A/en active IP Right Grant
- 2014-07-28 ZA ZA2014/05560A patent/ZA201405560B/en unknown
-
2016
- 2016-01-05 US US14/988,484 patent/US9617273B2/en not_active Expired - Fee Related
-
2017
- 2017-04-05 US US15/479,958 patent/US10112952B2/en active Active
- 2017-11-16 CY CY20171101198T patent/CY1119804T1/el unknown
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2018
- 2018-09-19 US US16/135,512 patent/US10501467B2/en active Active
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