JP2011506402A5 - - Google Patents
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- Publication number
- JP2011506402A5 JP2011506402A5 JP2010537460A JP2010537460A JP2011506402A5 JP 2011506402 A5 JP2011506402 A5 JP 2011506402A5 JP 2010537460 A JP2010537460 A JP 2010537460A JP 2010537460 A JP2010537460 A JP 2010537460A JP 2011506402 A5 JP2011506402 A5 JP 2011506402A5
- Authority
- JP
- Japan
- Prior art keywords
- cancer
- substituted
- alkyl
- group
- agent
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 206010028980 Neoplasm Diseases 0.000 claims 30
- 239000003795 chemical substances by application Substances 0.000 claims 23
- 150000001875 compounds Chemical class 0.000 claims 18
- 125000000217 alkyl group Chemical group 0.000 claims 15
- 125000001072 heteroaryl group Chemical group 0.000 claims 15
- 125000000623 heterocyclic group Chemical group 0.000 claims 15
- -1 carboxyl ester Chemical class 0.000 claims 12
- 239000003814 drug Substances 0.000 claims 11
- 229940079593 drug Drugs 0.000 claims 11
- 239000001257 hydrogen Substances 0.000 claims 11
- 229910052739 hydrogen Inorganic materials 0.000 claims 11
- 150000003839 salts Chemical class 0.000 claims 11
- 125000001475 halogen functional group Chemical group 0.000 claims 10
- 206010006187 Breast cancer Diseases 0.000 claims 9
- 208000026310 Breast neoplasm Diseases 0.000 claims 9
- 125000003118 aryl group Chemical group 0.000 claims 9
- 201000010099 disease Diseases 0.000 claims 9
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 9
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 9
- 230000002062 proliferating effect Effects 0.000 claims 9
- 125000003107 substituted aryl group Chemical group 0.000 claims 9
- 125000002947 alkylene group Chemical group 0.000 claims 8
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 8
- 125000000547 substituted alkyl group Chemical group 0.000 claims 7
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 6
- 208000017604 Hodgkin disease Diseases 0.000 claims 6
- 208000021519 Hodgkin lymphoma Diseases 0.000 claims 6
- 208000010747 Hodgkins lymphoma Diseases 0.000 claims 6
- 208000034578 Multiple myelomas Diseases 0.000 claims 6
- 201000003793 Myelodysplastic syndrome Diseases 0.000 claims 6
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 6
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 6
- 206010060862 Prostate cancer Diseases 0.000 claims 6
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 6
- 206010041067 Small cell lung cancer Diseases 0.000 claims 6
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 6
- 201000011510 cancer Diseases 0.000 claims 6
- 125000000753 cycloalkyl group Chemical group 0.000 claims 6
- 206010017758 gastric cancer Diseases 0.000 claims 6
- 201000005787 hematologic cancer Diseases 0.000 claims 6
- 230000002489 hematologic effect Effects 0.000 claims 6
- 208000024200 hematopoietic and lymphoid system neoplasm Diseases 0.000 claims 6
- 208000000587 small cell lung carcinoma Diseases 0.000 claims 6
- 201000011549 stomach cancer Diseases 0.000 claims 6
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 5
- 125000002252 acyl group Chemical group 0.000 claims 5
- 208000032839 leukemia Diseases 0.000 claims 5
- 125000003545 alkoxy group Chemical group 0.000 claims 4
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 4
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 4
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 3
- 102100033350 ATP-dependent translocase ABCB1 Human genes 0.000 claims 3
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 3
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims 3
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims 3
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 3
- 206010005003 Bladder cancer Diseases 0.000 claims 3
- 206010055113 Breast cancer metastatic Diseases 0.000 claims 3
- 206010008342 Cervix carcinoma Diseases 0.000 claims 3
- 206010009944 Colon cancer Diseases 0.000 claims 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 3
- 208000028018 Lymphocytic leukaemia Diseases 0.000 claims 3
- 241000124008 Mammalia Species 0.000 claims 3
- 108010047230 Member 1 Subfamily B ATP Binding Cassette Transporter Proteins 0.000 claims 3
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 3
- 208000001894 Nasopharyngeal Neoplasms Diseases 0.000 claims 3
- 206010061306 Nasopharyngeal cancer 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
- 206010033701 Papillary thyroid cancer Diseases 0.000 claims 3
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims 3
- 208000006265 Renal cell carcinoma Diseases 0.000 claims 3
- 206010039491 Sarcoma Diseases 0.000 claims 3
- 208000000453 Skin Neoplasms Diseases 0.000 claims 3
- 208000000102 Squamous Cell Carcinoma of Head and Neck Diseases 0.000 claims 3
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 3
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 3
- 201000010881 cervical cancer Diseases 0.000 claims 3
- 208000029742 colonic neoplasm Diseases 0.000 claims 3
- 201000000459 head and neck squamous cell carcinoma Diseases 0.000 claims 3
- 201000007270 liver cancer Diseases 0.000 claims 3
- 208000014018 liver neoplasm Diseases 0.000 claims 3
- 201000005202 lung cancer Diseases 0.000 claims 3
- 208000020816 lung neoplasm Diseases 0.000 claims 3
- 208000003747 lymphoid leukemia Diseases 0.000 claims 3
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 3
- 239000000203 mixture Substances 0.000 claims 3
- 208000025113 myeloid leukemia Diseases 0.000 claims 3
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 3
- 201000002528 pancreatic cancer Diseases 0.000 claims 3
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 3
- 208000015347 renal cell adenocarcinoma Diseases 0.000 claims 3
- 201000000849 skin cancer Diseases 0.000 claims 3
- 206010041823 squamous cell carcinoma Diseases 0.000 claims 3
- 125000005415 substituted alkoxy group Chemical group 0.000 claims 3
- 208000030045 thyroid gland papillary carcinoma Diseases 0.000 claims 3
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 3
- 201000005112 urinary bladder cancer Diseases 0.000 claims 3
- 239000004480 active ingredient Substances 0.000 claims 2
- 125000004442 acylamino group Chemical group 0.000 claims 2
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 125000000304 alkynyl group Chemical group 0.000 claims 2
- 125000000266 alpha-aminoacyl group Chemical group 0.000 claims 2
- 125000004104 aryloxy group Chemical group 0.000 claims 2
- 230000001886 ciliary effect Effects 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 125000005844 heterocyclyloxy group Chemical group 0.000 claims 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 1
- 125000002853 C1-C4 hydroxyalkyl group Chemical group 0.000 claims 1
- 125000003277 amino group Chemical group 0.000 claims 1
- 125000005002 aryl methyl group Chemical group 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 125000004216 fluoromethyl group Chemical group [H]C([H])(F)* 0.000 claims 1
- 201000009277 hairy cell leukemia Diseases 0.000 claims 1
- 239000004615 ingredient Substances 0.000 claims 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 1
- 125000004043 oxo group Chemical group O=* 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 125000005017 substituted alkenyl group Chemical group 0.000 claims 1
- 125000004426 substituted alkynyl group Chemical group 0.000 claims 1
- 238000006467 substitution reaction Methods 0.000 claims 1
- 0 Cc1ccc(*)cc1-c1c[n](Cc2ccccc2)c(C(*)(*)N(C)C(*O*)=O)n1 Chemical compound Cc1ccc(*)cc1-c1c[n](Cc2ccccc2)c(C(*)(*)N(C)C(*O*)=O)n1 0.000 description 2
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US1396607P | 2007-12-14 | 2007-12-14 | |
| US61/013,966 | 2007-12-14 | ||
| PCT/EP2008/067412 WO2009077448A1 (en) | 2007-12-14 | 2008-12-12 | Kinesin inhibitors as cancer therapeutics |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2011506402A JP2011506402A (ja) | 2011-03-03 |
| JP2011506402A5 true JP2011506402A5 (Direct) | 2012-02-02 |
| JP5501976B2 JP5501976B2 (ja) | 2014-05-28 |
Family
ID=40328566
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010537460A Expired - Fee Related JP5501976B2 (ja) | 2007-12-14 | 2008-12-12 | 癌治療薬としてのキネシン阻害剤 |
Country Status (30)
| Country | Link |
|---|---|
| US (2) | US8252832B2 (Direct) |
| EP (1) | EP2229170B1 (Direct) |
| JP (1) | JP5501976B2 (Direct) |
| KR (1) | KR20100098394A (Direct) |
| CN (1) | CN101939005B (Direct) |
| AR (1) | AR069676A1 (Direct) |
| AU (1) | AU2008337570B2 (Direct) |
| BR (1) | BRPI0821248A2 (Direct) |
| CA (1) | CA2708822A1 (Direct) |
| CL (1) | CL2008003707A1 (Direct) |
| CO (1) | CO6290651A2 (Direct) |
| CR (1) | CR11412A (Direct) |
| DO (1) | DOP2010000175A (Direct) |
| EA (1) | EA018014B1 (Direct) |
| EC (1) | ECSP10010248A (Direct) |
| ES (1) | ES2459442T3 (Direct) |
| GE (1) | GEP20125647B (Direct) |
| GT (1) | GT201000172A (Direct) |
| IL (1) | IL205831A0 (Direct) |
| MA (1) | MA31872B1 (Direct) |
| MY (1) | MY150214A (Direct) |
| NI (1) | NI201000091A (Direct) |
| NZ (1) | NZ585142A (Direct) |
| PA (1) | PA8807801A1 (Direct) |
| PE (1) | PE20091451A1 (Direct) |
| SM (1) | SMP201000095B (Direct) |
| TN (1) | TN2010000204A1 (Direct) |
| TW (1) | TW200930704A (Direct) |
| UY (1) | UY31532A1 (Direct) |
| WO (1) | WO2009077448A1 (Direct) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8765817B1 (en) | 2008-12-03 | 2014-07-01 | Arrowhead Center, Inc. | Selective inhibitors of EG5 motors and methods of use |
| US8349899B1 (en) | 2008-12-03 | 2013-01-08 | Arrowhead Center, Inc. | Selective inhibitors of EG5 motors and methods of use |
| WO2011128388A2 (en) * | 2010-04-15 | 2011-10-20 | Novartis Ag | Oxazole and thiazole compounds as ksp inhibitors |
| US9498540B2 (en) | 2013-03-15 | 2016-11-22 | Novartis Ag | Cell proliferation inhibitors and conjugates thereof |
| JP2016516035A (ja) * | 2013-03-15 | 2016-06-02 | ノバルティス アーゲー | 細胞増殖阻害剤およびそれらのコンジュゲート |
| US10786578B2 (en) | 2014-08-05 | 2020-09-29 | Novartis Ag | CKIT antibody drug conjugates |
| EP4406606A3 (de) | 2015-06-22 | 2024-10-09 | Bayer Pharma Aktiengesellschaft | Binder-wirkstoff-konjugate (adcs) und binder-prodrug-konjugate (apdcs) mit enzymatisch spaltbaren g |
| CN105418527A (zh) * | 2015-12-28 | 2016-03-23 | 青岛友诚高新技术有限公司 | 一种具有抗乳腺导管癌活性的化合物及其制备方法、用途 |
| CN105646361B (zh) * | 2016-02-17 | 2017-12-01 | 吉首大学 | 一种2,4,5‑三芳基咪唑型化合物及其制法和用途 |
| JP7066714B2 (ja) | 2016-12-21 | 2022-05-13 | バイエル・ファルマ・アクティエンゲゼルシャフト | 酵素的に切断可能な基を有する抗体薬物コンジュゲート（ａｄｃ） |
| CN106668863B (zh) * | 2017-02-21 | 2019-04-23 | 南方医科大学 | 靶向ktn1治疗皮肤鳞状细胞癌的药物 |
| GB201706162D0 (en) * | 2017-04-19 | 2017-05-31 | Nat Univ Singapore | Compounds |
| CN111954532A (zh) * | 2018-04-13 | 2020-11-17 | 上海交通大学医学院附属瑞金医院 | 杂芳基酰胺类化合物的抗肿瘤多药耐药性、治疗癌症的用途和蛋白质-药物分子复合物 |
| CN109646679A (zh) * | 2019-01-28 | 2019-04-19 | 中国科学院长春应用化学研究所 | 铁离子螯合剂及其可药用盐的用途 |
| CN111529526B (zh) * | 2020-04-14 | 2021-04-23 | 广州领晟医疗科技有限公司 | 一种化合物在制备治疗急性胰腺炎的药物中的用途 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2006002236A1 (en) * | 2004-06-18 | 2006-01-05 | Novartis Vaccines And Diagnostics Inc. | N- (1- (1-benzyl -4-phenyl-1h-imidazol-2-yl) -2,2-dymethylpropyl) benzamide derivatives and related compounds as kinesin spindle protein (ksp) inhibitors for the treatment of cancer |
| US7271271B2 (en) | 2004-06-28 | 2007-09-18 | Amgen Sf, Llc | Imidazolo-related compounds, compositions and methods for their use |
| MY147188A (en) | 2005-08-09 | 2012-11-14 | Novartis Ag | Substituted imidazole compounds as ksp inhibitors |
| JP2010515687A (ja) | 2007-01-05 | 2010-05-13 | ノバルティス アーゲー | キネシンスピンドルタンパク質阻害剤（ｅｇ−５）としてのイミダゾール誘導体 |
-
2008
- 2008-11-25 US US12/313,923 patent/US8252832B2/en not_active Expired - Fee Related
- 2008-12-12 AU AU2008337570A patent/AU2008337570B2/en not_active Ceased
- 2008-12-12 PA PA20088807801A patent/PA8807801A1/es unknown
- 2008-12-12 WO PCT/EP2008/067412 patent/WO2009077448A1/en not_active Ceased
- 2008-12-12 EP EP08863009.0A patent/EP2229170B1/en active Active
- 2008-12-12 MY MYPI2010002030A patent/MY150214A/en unknown
- 2008-12-12 JP JP2010537460A patent/JP5501976B2/ja not_active Expired - Fee Related
- 2008-12-12 BR BRPI0821248-1A patent/BRPI0821248A2/pt not_active IP Right Cessation
- 2008-12-12 GE GEAP200811846A patent/GEP20125647B/en unknown
- 2008-12-12 CN CN200880120667.8A patent/CN101939005B/zh not_active Expired - Fee Related
- 2008-12-12 EA EA201000900A patent/EA018014B1/ru not_active IP Right Cessation
- 2008-12-12 ES ES08863009.0T patent/ES2459442T3/es active Active
- 2008-12-12 CA CA2708822A patent/CA2708822A1/en not_active Abandoned
- 2008-12-12 KR KR1020107012912A patent/KR20100098394A/ko not_active Withdrawn
- 2008-12-12 CL CL2008003707A patent/CL2008003707A1/es unknown
- 2008-12-12 TW TW097148535A patent/TW200930704A/zh unknown
- 2008-12-12 PE PE2008002064A patent/PE20091451A1/es not_active Application Discontinuation
- 2008-12-12 NZ NZ585142A patent/NZ585142A/en not_active IP Right Cessation
- 2008-12-12 AR ARP080105410A patent/AR069676A1/es not_active Application Discontinuation
- 2008-12-15 UY UY31532A patent/UY31532A1/es not_active Application Discontinuation
-
2010
- 2010-05-05 CR CR11412A patent/CR11412A/es not_active Application Discontinuation
- 2010-05-07 TN TN2010000204A patent/TN2010000204A1/fr unknown
- 2010-05-17 IL IL205831A patent/IL205831A0/en unknown
- 2010-05-31 MA MA32879A patent/MA31872B1/fr unknown
- 2010-06-02 NI NI201000091A patent/NI201000091A/es unknown
- 2010-06-10 CO CO10070369A patent/CO6290651A2/es not_active Application Discontinuation
- 2010-06-11 DO DO2010000175A patent/DOP2010000175A/es unknown
- 2010-06-14 EC EC2010010248A patent/ECSP10010248A/es unknown
- 2010-06-14 GT GT201000172A patent/GT201000172A/es unknown
- 2010-07-13 SM SM201000095T patent/SMP201000095B/it unknown
-
2012
- 2012-07-11 US US13/546,713 patent/US8664256B2/en not_active Expired - Fee Related
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