RU2009147819A - Комбинация ингибиторов снк и parp для лечения злокачественных новообразований - Google Patents
Комбинация ингибиторов снк и parp для лечения злокачественных новообразований Download PDFInfo
- Publication number
- RU2009147819A RU2009147819A RU2009147819/15A RU2009147819A RU2009147819A RU 2009147819 A RU2009147819 A RU 2009147819A RU 2009147819/15 A RU2009147819/15 A RU 2009147819/15A RU 2009147819 A RU2009147819 A RU 2009147819A RU 2009147819 A RU2009147819 A RU 2009147819A
- Authority
- RU
- Russia
- Prior art keywords
- alkyl
- cancer
- heterocyclyl
- aryl
- substituted
- Prior art date
Links
- 239000012661 PARP inhibitor Substances 0.000 title claims abstract 3
- 229940121906 Poly ADP ribose polymerase inhibitor Drugs 0.000 title claims abstract 3
- 206010028980 Neoplasm Diseases 0.000 title claims 21
- 201000011510 cancer Diseases 0.000 title claims 21
- 125000000623 heterocyclic group Chemical group 0.000 claims abstract 30
- 125000003118 aryl group Chemical group 0.000 claims abstract 26
- 125000000753 cycloalkyl group Chemical group 0.000 claims abstract 16
- 229910052757 nitrogen Inorganic materials 0.000 claims abstract 15
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims abstract 12
- 125000004093 cyano group Chemical group *C#N 0.000 claims abstract 10
- 125000004433 nitrogen atom Chemical group N* 0.000 claims abstract 9
- PXQLVRUNWNTZOS-UHFFFAOYSA-N sulfanyl Chemical class [SH] PXQLVRUNWNTZOS-UHFFFAOYSA-N 0.000 claims abstract 9
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims abstract 8
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims abstract 8
- 125000004432 carbon atom Chemical group C* 0.000 claims abstract 8
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims abstract 7
- 150000003839 salts Chemical class 0.000 claims abstract 7
- -1 isociano Chemical group 0.000 claims abstract 6
- 125000000392 cycloalkenyl group Chemical group 0.000 claims abstract 5
- 150000001875 compounds Chemical class 0.000 claims abstract 4
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims abstract 3
- 229940043355 kinase inhibitor Drugs 0.000 claims abstract 3
- 239000003757 phosphotransferase inhibitor Substances 0.000 claims abstract 3
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims abstract 2
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 claims abstract 2
- 229910052760 oxygen Inorganic materials 0.000 claims abstract 2
- 229910052717 sulfur Inorganic materials 0.000 claims abstract 2
- 125000001544 thienyl group Chemical group 0.000 claims abstract 2
- 125000000217 alkyl group Chemical group 0.000 claims 99
- 229930194542 Keto Natural products 0.000 claims 7
- 229910052799 carbon Inorganic materials 0.000 claims 7
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 7
- 229910052736 halogen Inorganic materials 0.000 claims 7
- 150000002367 halogens Chemical class 0.000 claims 7
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 7
- 125000000468 ketone group Chemical group 0.000 claims 7
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 7
- 208000026310 Breast neoplasm Diseases 0.000 claims 6
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 6
- 206010041067 Small cell lung cancer Diseases 0.000 claims 6
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 6
- 150000001721 carbon Chemical group 0.000 claims 6
- 208000020816 lung neoplasm Diseases 0.000 claims 6
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 6
- 208000000587 small cell lung carcinoma Diseases 0.000 claims 6
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 6
- 206010006187 Breast cancer Diseases 0.000 claims 5
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 5
- 206010060862 Prostate cancer Diseases 0.000 claims 5
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 5
- 206010038389 Renal cancer Diseases 0.000 claims 5
- 201000010982 kidney cancer Diseases 0.000 claims 5
- 201000005202 lung cancer Diseases 0.000 claims 5
- 238000000034 method Methods 0.000 claims 5
- 201000002510 thyroid cancer Diseases 0.000 claims 5
- 125000003545 alkoxy group Chemical group 0.000 claims 4
- PEUGKEHLRUVPAN-YFKPBYRVSA-N (3s)-piperidin-3-amine Chemical compound N[C@H]1CCCNC1 PEUGKEHLRUVPAN-YFKPBYRVSA-N 0.000 claims 3
- 206010005003 Bladder cancer Diseases 0.000 claims 3
- 208000003174 Brain Neoplasms Diseases 0.000 claims 3
- 206010008342 Cervix carcinoma Diseases 0.000 claims 3
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 3
- 208000006168 Ewing Sarcoma Diseases 0.000 claims 3
- 208000007766 Kaposi sarcoma Diseases 0.000 claims 3
- 206010029260 Neuroblastoma Diseases 0.000 claims 3
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 3
- 206010033128 Ovarian cancer Diseases 0.000 claims 3
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 3
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 3
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 3
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 3
- 201000000170 Thyroid lymphoma Diseases 0.000 claims 3
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 3
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 3
- 210000000481 breast Anatomy 0.000 claims 3
- 201000010881 cervical cancer Diseases 0.000 claims 3
- 201000004101 esophageal cancer Diseases 0.000 claims 3
- 206010017758 gastric cancer Diseases 0.000 claims 3
- 201000010536 head and neck cancer Diseases 0.000 claims 3
- 208000014829 head and neck neoplasm Diseases 0.000 claims 3
- 229910052739 hydrogen Inorganic materials 0.000 claims 3
- 208000032839 leukemia Diseases 0.000 claims 3
- 210000004072 lung Anatomy 0.000 claims 3
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 3
- 201000001441 melanoma Diseases 0.000 claims 3
- 230000001394 metastastic effect Effects 0.000 claims 3
- 206010061289 metastatic neoplasm Diseases 0.000 claims 3
- 201000000050 myeloid neoplasm Diseases 0.000 claims 3
- 230000000683 nonmetastatic effect Effects 0.000 claims 3
- 201000002528 pancreatic cancer Diseases 0.000 claims 3
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 3
- 201000011549 stomach cancer Diseases 0.000 claims 3
- 210000001685 thyroid gland Anatomy 0.000 claims 3
- 201000005112 urinary bladder cancer Diseases 0.000 claims 3
- 210000001072 colon Anatomy 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 210000003494 hepatocyte Anatomy 0.000 claims 2
- 125000002462 isocyano group Chemical group *[N+]#[C-] 0.000 claims 2
- 210000003734 kidney Anatomy 0.000 claims 2
- YHONVYJMVUMQAJ-UHFFFAOYSA-N 2-(carbamoylamino)-n-(1-ethylpiperidin-3-yl)-5-methylthiophene-3-carboxamide Chemical compound C1N(CC)CCCC1NC(=O)C1=C(NC(N)=O)SC(C)=C1 YHONVYJMVUMQAJ-UHFFFAOYSA-N 0.000 claims 1
- FPSWBSQHEQBJSL-UHFFFAOYSA-N 4-(carbamoylamino)-2-morpholin-4-yl-1,3-thiazole-5-carboxylic acid Chemical compound S1C(C(O)=O)=C(NC(=O)N)N=C1N1CCOCC1 FPSWBSQHEQBJSL-UHFFFAOYSA-N 0.000 claims 1
- RTJBIQCMDFNUBB-UHFFFAOYSA-N 5-(carbamoylamino)-2-methyl-1,3-oxazole-4-carboxylic acid Chemical compound CC1=NC(C(O)=O)=C(NC(N)=O)O1 RTJBIQCMDFNUBB-UHFFFAOYSA-N 0.000 claims 1
- 229940121977 Checkpoint kinase inhibitor Drugs 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- 101710179684 Poly [ADP-ribose] polymerase Proteins 0.000 claims 1
- 102100023712 Poly [ADP-ribose] polymerase 1 Human genes 0.000 claims 1
- 229920000776 Poly(Adenosine diphosphate-ribose) polymerase Polymers 0.000 claims 1
- 208000015634 Rectal Neoplasms Diseases 0.000 claims 1
- QNKJYHQPXXAMHX-VIFPVBQESA-N [3-[(3s)-3-aminoazepane-1-carbonyl]-5-ethylthiophen-2-yl]urea Chemical compound S1C(CC)=CC(C(=O)N2C[C@@H](N)CCCC2)=C1NC(N)=O QNKJYHQPXXAMHX-VIFPVBQESA-N 0.000 claims 1
- CJCKGXRROSPGDG-NSHDSACASA-N [3-[(3s)-3-aminoazepane-1-carbonyl]-5-pyridin-2-ylthiophen-2-yl]urea Chemical compound C1[C@@H](N)CCCCN1C(=O)C1=C(NC(N)=O)SC(C=2N=CC=CC=2)=C1 CJCKGXRROSPGDG-NSHDSACASA-N 0.000 claims 1
- 125000002252 acyl group Chemical group 0.000 claims 1
- 125000003368 amide group Chemical group 0.000 claims 1
- 125000006367 bivalent amino carbonyl group Chemical group [H]N([*:1])C([*:2])=O 0.000 claims 1
- 125000004452 carbocyclyl group Chemical group 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 150000002148 esters Chemical class 0.000 claims 1
- 125000001475 halogen functional group Chemical group 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- 150000002431 hydrogen Chemical class 0.000 claims 1
- 210000005229 liver cell Anatomy 0.000 claims 1
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 210000002307 prostate Anatomy 0.000 claims 1
- 206010038038 rectal cancer Diseases 0.000 claims 1
- 201000001275 rectum cancer Diseases 0.000 claims 1
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 1
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 3
- 101100294115 Caenorhabditis elegans nhr-4 gene Proteins 0.000 abstract 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 1
Classifications
-
- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4535—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
-
- 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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/502—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US94020307P | 2007-05-25 | 2007-05-25 | |
| US60/940,203 | 2007-05-25 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| RU2009147819A true RU2009147819A (ru) | 2011-06-27 |
Family
ID=39672970
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2009147819/15A RU2009147819A (ru) | 2007-05-25 | 2008-05-23 | Комбинация ингибиторов снк и parp для лечения злокачественных новообразований |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US20100249112A1 (https=) |
| EP (1) | EP2167086A1 (https=) |
| JP (1) | JP2010527981A (https=) |
| KR (1) | KR20100020981A (https=) |
| CN (1) | CN101743003A (https=) |
| AU (1) | AU2008256562A1 (https=) |
| BR (1) | BRPI0811059A2 (https=) |
| CA (1) | CA2687786A1 (https=) |
| MX (1) | MX2009012705A (https=) |
| RU (1) | RU2009147819A (https=) |
| WO (1) | WO2008146035A1 (https=) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2010081778A1 (en) * | 2009-01-17 | 2010-07-22 | Universität Zürich | Blockers of parp for the prevention and treatment of helicobacter pylori induced gastric cancer |
| JP2013532683A (ja) | 2010-07-27 | 2013-08-19 | カディラ ヘルスケア リミティド | ポリ（ａｄｐリボース）ポリメラーゼ−１阻害剤としての、置換４−（４−フルオロ−３−（ピペラジン−１−カルボニル）ベンジル）フタラジン−１（２ｈ）−オン誘導体 |
| CN108478577A (zh) | 2012-04-05 | 2018-09-04 | 沃泰克斯药物股份有限公司 | 可用作atr激酶抑制剂的化合物及其组合疗法 |
| HUE030613T2 (en) | 2012-12-31 | 2017-05-29 | Cadila Healthcare Ltd | Substituted phthalazin-1 (2H) -one derivatives as selective inhibitors of poly (ADP-ribose) polymerase-1 |
| AU2016296905B2 (en) | 2015-07-23 | 2018-07-05 | Centre National De La Recherche Scientifique | Use of a combination of Dbait molecule and parp inhibitors to treat cancer |
| AU2016331955B2 (en) | 2015-09-30 | 2022-07-21 | Vertex Pharmaceuticals Incorporated | Method for treating cancer using a combination of DNA damaging agents and ATR inhibitors |
| WO2018162439A1 (en) | 2017-03-08 | 2018-09-13 | Onxeo | New predictive biomarker for the sensitivity to a treatment of cancer with a dbait molecule |
| JP7273791B2 (ja) | 2017-04-10 | 2023-05-15 | シエラ オンコロジー， インコーポレイテッド | 腫瘍成長を阻害するＣＨＫ１（ＳＲＡ７３７）／ＰＡＲＰｉ組み合わせ方法 |
| EP3461480A1 (en) | 2017-09-27 | 2019-04-03 | Onxeo | Combination of a dna damage response cell cycle checkpoint inhibitors and belinostat for treating cancer |
| CA3092779A1 (en) | 2018-03-13 | 2019-09-19 | Onxeo | A dbait molecule against acquired resistance in the treatment of cancer |
| WO2019194738A1 (en) | 2018-04-05 | 2019-10-10 | Noviga Research Ab | Novel combinations of a tubulin polymerization inhibitor and a poly (adp-ribose) polymerase (parp) inhibitor for use in the treatment of cancer |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| TW202204348A (zh) | 2020-04-07 | 2022-02-01 | 美商西爾拉癌症醫學公司 | Ｃｈｋ１抑制劑之合成方法 |
| WO2022000946A1 (zh) * | 2020-06-29 | 2022-01-06 | 中国药科大学 | 含有酞嗪-1(2h)-酮结构的parp抑制剂、其制法及医药用途 |
| CN112375070B (zh) * | 2020-06-29 | 2023-03-28 | 中国药科大学 | 含有酞嗪-1(2h)-酮结构的parp抑制剂、其制法及医药用途 |
| CN121398822A (zh) | 2023-06-21 | 2026-01-23 | 四方生物科学有限公司 | 用于在治疗hr功能正常的癌症的方法中的用途的包含脱氧胞苷衍生物和parp抑制剂的组合 |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PL1633724T3 (pl) * | 2003-03-12 | 2011-10-31 | Kudos Pharm Ltd | Pochodne ftalazynonu |
| PL2305221T3 (pl) * | 2003-12-01 | 2015-11-30 | Kudos Pharm Ltd | Inhibitory naprawy uszkodzeń DNA w leczeniu raka |
| ATE501138T1 (de) * | 2004-01-05 | 2011-03-15 | Astrazeneca Ab | Thiophenderivate als chk-1-inhibitoren |
| US20060204981A1 (en) * | 2005-01-07 | 2006-09-14 | Chiang Li | Compositions for modulation of PARP and methods for screening for same |
| WO2008020180A2 (en) * | 2006-08-17 | 2008-02-21 | Kudos Pharmaceuticals Limited | Methods of increasing the sensitivity of cancer cells to dna damage |
-
2008
- 2008-05-23 US US12/601,328 patent/US20100249112A1/en not_active Abandoned
- 2008-05-23 EP EP08750767A patent/EP2167086A1/en not_active Withdrawn
- 2008-05-23 WO PCT/GB2008/050372 patent/WO2008146035A1/en not_active Ceased
- 2008-05-23 RU RU2009147819/15A patent/RU2009147819A/ru not_active Application Discontinuation
- 2008-05-23 CA CA2687786A patent/CA2687786A1/en not_active Abandoned
- 2008-05-23 KR KR1020097026995A patent/KR20100020981A/ko not_active Withdrawn
- 2008-05-23 CN CN200880024432A patent/CN101743003A/zh active Pending
- 2008-05-23 AU AU2008256562A patent/AU2008256562A1/en not_active Abandoned
- 2008-05-23 JP JP2010508909A patent/JP2010527981A/ja active Pending
- 2008-05-23 BR BRPI0811059A patent/BRPI0811059A2/pt not_active IP Right Cessation
- 2008-05-23 MX MX2009012705A patent/MX2009012705A/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| WO2008146035A1 (en) | 2008-12-04 |
| BRPI0811059A2 (pt) | 2017-05-09 |
| CN101743003A (zh) | 2010-06-16 |
| CA2687786A1 (en) | 2008-12-04 |
| AU2008256562A1 (en) | 2008-12-04 |
| US20100249112A1 (en) | 2010-09-30 |
| EP2167086A1 (en) | 2010-03-31 |
| KR20100020981A (ko) | 2010-02-23 |
| JP2010527981A (ja) | 2010-08-19 |
| MX2009012705A (es) | 2009-12-08 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA92 | Acknowledgement of application withdrawn (lack of supplementary materials submitted) |
Effective date: 20120926 |