JP2014532768A5 - - Google Patents
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- Publication number
- JP2014532768A5 JP2014532768A5 JP2014541274A JP2014541274A JP2014532768A5 JP 2014532768 A5 JP2014532768 A5 JP 2014532768A5 JP 2014541274 A JP2014541274 A JP 2014541274A JP 2014541274 A JP2014541274 A JP 2014541274A JP 2014532768 A5 JP2014532768 A5 JP 2014532768A5
- Authority
- JP
- Japan
- Prior art keywords
- agent
- alkyl
- administration
- aryl
- combination
- 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
- 125000000217 alkyl group Chemical group 0.000 claims description 113
- 239000003795 chemical substances by application Substances 0.000 claims description 77
- 125000000623 heterocyclic group Chemical group 0.000 claims description 20
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 10
- 229940079593 drug Drugs 0.000 claims description 8
- 239000003814 drug Substances 0.000 claims description 8
- 230000001613 neoplastic effect Effects 0.000 claims description 6
- MLDQJTXFUGDVEO-UHFFFAOYSA-N BAY-43-9006 Chemical compound C1=NC(C(=O)NC)=CC(OC=2C=CC(NC(=O)NC=3C=C(C(Cl)=CC=3)C(F)(F)F)=CC=2)=C1 MLDQJTXFUGDVEO-UHFFFAOYSA-N 0.000 claims description 5
- 239000005511 L01XE05 - Sorafenib Substances 0.000 claims description 5
- 229960003787 sorafenib Drugs 0.000 claims description 5
- 208000006265 Renal cell carcinoma Diseases 0.000 claims description 3
- 229940124302 mTOR inhibitor Drugs 0.000 claims description 3
- 239000003628 mammalian target of rapamycin inhibitor Substances 0.000 claims description 3
- 150000003839 salts Chemical class 0.000 claims description 3
- XXJWYDDUDKYVKI-UHFFFAOYSA-N 4-[(4-fluoro-2-methyl-1H-indol-5-yl)oxy]-6-methoxy-7-[3-(1-pyrrolidinyl)propoxy]quinazoline Chemical compound COC1=CC2=C(OC=3C(=C4C=C(C)NC4=CC=3)F)N=CN=C2C=C1OCCCN1CCCC1 XXJWYDDUDKYVKI-UHFFFAOYSA-N 0.000 claims description 2
- 206010006187 Breast cancer Diseases 0.000 claims description 2
- 208000026310 Breast neoplasm Diseases 0.000 claims description 2
- 206010014733 Endometrial cancer Diseases 0.000 claims description 2
- 206010014759 Endometrial neoplasm Diseases 0.000 claims description 2
- 239000002147 L01XE04 - Sunitinib Substances 0.000 claims description 2
- 239000003798 L01XE11 - Pazopanib Substances 0.000 claims description 2
- 239000002118 L01XE12 - Vandetanib Substances 0.000 claims description 2
- 239000002138 L01XE21 - Regorafenib Substances 0.000 claims description 2
- 206010033128 Ovarian cancer Diseases 0.000 claims description 2
- 206010061535 Ovarian neoplasm Diseases 0.000 claims description 2
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 2
- 206010060862 Prostate cancer Diseases 0.000 claims description 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 2
- 206010039491 Sarcoma Diseases 0.000 claims description 2
- 208000000102 Squamous Cell Carcinoma of Head and Neck Diseases 0.000 claims description 2
- 229960003005 axitinib Drugs 0.000 claims description 2
- RITAVMQDGBJQJZ-FMIVXFBMSA-N axitinib Chemical group CNC(=O)C1=CC=CC=C1SC1=CC=C(C(\C=C\C=2N=CC=CC=2)=NN2)C2=C1 RITAVMQDGBJQJZ-FMIVXFBMSA-N 0.000 claims description 2
- 229960002412 cediranib Drugs 0.000 claims description 2
- 201000000459 head and neck squamous cell carcinoma Diseases 0.000 claims description 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 2
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 2
- 201000002120 neuroendocrine carcinoma Diseases 0.000 claims description 2
- 201000002528 pancreatic cancer Diseases 0.000 claims description 2
- 208000008443 pancreatic carcinoma Diseases 0.000 claims description 2
- 229960000639 pazopanib Drugs 0.000 claims description 2
- CUIHSIWYWATEQL-UHFFFAOYSA-N pazopanib Chemical compound C1=CC2=C(C)N(C)N=C2C=C1N(C)C(N=1)=CC=NC=1NC1=CC=C(C)C(S(N)(=O)=O)=C1 CUIHSIWYWATEQL-UHFFFAOYSA-N 0.000 claims description 2
- 229960004836 regorafenib Drugs 0.000 claims description 2
- FNHKPVJBJVTLMP-UHFFFAOYSA-N regorafenib Chemical compound C1=NC(C(=O)NC)=CC(OC=2C=C(F)C(NC(=O)NC=3C=C(C(Cl)=CC=3)C(F)(F)F)=CC=2)=C1 FNHKPVJBJVTLMP-UHFFFAOYSA-N 0.000 claims description 2
- 208000015347 renal cell adenocarcinoma Diseases 0.000 claims description 2
- 229950003647 semaxanib Drugs 0.000 claims description 2
- WUWDLXZGHZSWQZ-WQLSENKSSA-N semaxanib Chemical compound N1C(C)=CC(C)=C1\C=C/1C2=CC=CC=C2NC\1=O WUWDLXZGHZSWQZ-WQLSENKSSA-N 0.000 claims description 2
- 229960001796 sunitinib Drugs 0.000 claims description 2
- WINHZLLDWRZWRT-ATVHPVEESA-N sunitinib Chemical compound CCN(CC)CCNC(=O)C1=C(C)NC(\C=C/2C3=CC(F)=CC=C3NC\2=O)=C1C WINHZLLDWRZWRT-ATVHPVEESA-N 0.000 claims description 2
- 229960000241 vandetanib Drugs 0.000 claims description 2
- UHTHHESEBZOYNR-UHFFFAOYSA-N vandetanib Chemical compound COC1=CC(C(/N=CN2)=N/C=3C(=CC(Br)=CC=3)F)=C2C=C1OCC1CCN(C)CC1 UHTHHESEBZOYNR-UHFFFAOYSA-N 0.000 claims description 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 239000013066 combination product Substances 0.000 claims 1
- 229940127555 combination product Drugs 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- -1 substituted Chemical class 0.000 claims 1
- RWRIWBAIICGTTQ-UHFFFAOYSA-N difluoromethane Chemical compound FCF RWRIWBAIICGTTQ-UHFFFAOYSA-N 0.000 description 114
- 125000000304 alkynyl group Chemical group 0.000 description 49
- 238000000034 method Methods 0.000 description 40
- 125000003118 aryl group Chemical group 0.000 description 38
- 125000005843 halogen group Chemical group 0.000 description 24
- 125000001072 heteroaryl group Chemical group 0.000 description 23
- 125000004093 cyano group Chemical group *C#N 0.000 description 18
- 125000004404 heteroalkyl group Chemical group 0.000 description 18
- 125000006374 C2-C10 alkenyl group Chemical group 0.000 description 15
- 125000000753 cycloalkyl group Chemical group 0.000 description 14
- 229910052739 hydrogen Inorganic materials 0.000 description 13
- 125000002877 alkyl aryl group Chemical group 0.000 description 12
- 229910052757 nitrogen Inorganic materials 0.000 description 12
- 239000001257 hydrogen Substances 0.000 description 11
- 125000003342 alkenyl group Chemical group 0.000 description 8
- 150000002431 hydrogen Chemical class 0.000 description 8
- 208000035475 disorder Diseases 0.000 description 7
- 229910052736 halogen Inorganic materials 0.000 description 7
- 150000002367 halogens Chemical class 0.000 description 7
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 description 5
- 125000003545 alkoxy group Chemical group 0.000 description 5
- 231100000419 toxicity Toxicity 0.000 description 5
- 230000001988 toxicity Effects 0.000 description 5
- 125000005024 alkenyl aryl group Chemical group 0.000 description 4
- 125000005025 alkynylaryl group Chemical group 0.000 description 4
- 229940034982 antineoplastic agent Drugs 0.000 description 4
- 239000002246 antineoplastic agent Substances 0.000 description 4
- 125000003710 aryl alkyl group Chemical group 0.000 description 4
- 125000000392 cycloalkenyl group Chemical group 0.000 description 4
- 125000004446 heteroarylalkyl group Chemical group 0.000 description 4
- 125000000592 heterocycloalkyl group Chemical group 0.000 description 4
- 125000002950 monocyclic group Chemical group 0.000 description 4
- 125000004433 nitrogen atom Chemical group N* 0.000 description 4
- 229920006395 saturated elastomer Polymers 0.000 description 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 3
- 102000009308 Mechanistic Target of Rapamycin Complex 2 Human genes 0.000 description 3
- 108010034057 Mechanistic Target of Rapamycin Complex 2 Proteins 0.000 description 3
- 125000005213 alkyl heteroaryl group Chemical group 0.000 description 3
- 230000037396 body weight Effects 0.000 description 3
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 description 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 description 3
- 125000001424 substituent group Chemical group 0.000 description 3
- 230000002195 synergetic effect Effects 0.000 description 3
- 102000008135 Mechanistic Target of Rapamycin Complex 1 Human genes 0.000 description 2
- 108010035196 Mechanistic Target of Rapamycin Complex 1 Proteins 0.000 description 2
- 0 NC1NCNC(**2)C1C2c1ccc2[o]c(N)nc2c1 Chemical compound NC1NCNC(**2)C1C2c1ccc2[o]c(N)nc2c1 0.000 description 2
- 206010059516 Skin toxicity Diseases 0.000 description 2
- 150000001875 compounds Chemical class 0.000 description 2
- 125000004122 cyclic group Chemical group 0.000 description 2
- 125000005842 heteroatom Chemical group 0.000 description 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 2
- 238000000338 in vitro Methods 0.000 description 2
- 239000003112 inhibitor Substances 0.000 description 2
- 238000000021 kinase assay Methods 0.000 description 2
- 125000004043 oxo group Chemical group O=* 0.000 description 2
- 230000002062 proliferating effect Effects 0.000 description 2
- QFJCIRLUMZQUOT-HPLJOQBZSA-N sirolimus Chemical compound C1C[C@@H](O)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 QFJCIRLUMZQUOT-HPLJOQBZSA-N 0.000 description 2
- 231100000438 skin toxicity Toxicity 0.000 description 2
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 description 1
- 208000004998 Abdominal Pain Diseases 0.000 description 1
- 201000004384 Alopecia Diseases 0.000 description 1
- 206010012735 Diarrhoea Diseases 0.000 description 1
- 208000010201 Exanthema Diseases 0.000 description 1
- 206010061218 Inflammation Diseases 0.000 description 1
- 101150097381 Mtor gene Proteins 0.000 description 1
- 206010028813 Nausea Diseases 0.000 description 1
- 206010040844 Skin exfoliation Diseases 0.000 description 1
- 206010040914 Skin reaction Diseases 0.000 description 1
- 239000004037 angiogenesis inhibitor Substances 0.000 description 1
- 208000022531 anorexia Diseases 0.000 description 1
- 239000002260 anti-inflammatory agent Substances 0.000 description 1
- 229940121363 anti-inflammatory agent Drugs 0.000 description 1
- 230000001028 anti-proliverative effect Effects 0.000 description 1
- 239000003472 antidiabetic agent Substances 0.000 description 1
- 229940125708 antidiabetic agent Drugs 0.000 description 1
- 125000002619 bicyclic group Chemical group 0.000 description 1
- 206010061428 decreased appetite Diseases 0.000 description 1
- 230000035618 desquamation Effects 0.000 description 1
- 206010012601 diabetes mellitus Diseases 0.000 description 1
- 201000005884 exanthem Diseases 0.000 description 1
- 208000024963 hair loss Diseases 0.000 description 1
- 230000003676 hair loss Effects 0.000 description 1
- 230000004054 inflammatory process Effects 0.000 description 1
- 239000002502 liposome Substances 0.000 description 1
- 230000008693 nausea Effects 0.000 description 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 description 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 description 1
- ZAHRKKWIAAJSAO-UHFFFAOYSA-N rapamycin Natural products COCC(O)C(=C/C(C)C(=O)CC(OC(=O)C1CCCCN1C(=O)C(=O)C2(O)OC(CC(OC)C(=CC=CC=CC(C)CC(C)C(=O)C)C)CCC2C)C(C)CC3CCC(O)C(C3)OC)C ZAHRKKWIAAJSAO-UHFFFAOYSA-N 0.000 description 1
- 206010037844 rash Diseases 0.000 description 1
- 229940124617 receptor tyrosine kinase inhibitor Drugs 0.000 description 1
- 229960002930 sirolimus Drugs 0.000 description 1
- 231100000430 skin reaction Toxicity 0.000 description 1
- 230000035483 skin reaction Effects 0.000 description 1
- 238000011269 treatment regimen Methods 0.000 description 1
- 230000004580 weight loss Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161557326P | 2011-11-08 | 2011-11-08 | |
| US61/557,326 | 2011-11-08 | ||
| PCT/US2012/064239 WO2013070976A1 (en) | 2011-11-08 | 2012-11-08 | Treatment regimens using multiple pharmaceutical agents |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014532768A JP2014532768A (ja) | 2014-12-08 |
| JP2014532768A5 true JP2014532768A5 (enExample) | 2015-12-24 |
| JP6114296B2 JP6114296B2 (ja) | 2017-04-12 |
Family
ID=48290566
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014541274A Expired - Fee Related JP6114296B2 (ja) | 2011-11-08 | 2012-11-08 | 複数の医薬品を使用した治療レジメン |
Country Status (7)
| Country | Link |
|---|---|
| US (3) | US20140377285A1 (enExample) |
| EP (1) | EP2776441A4 (enExample) |
| JP (1) | JP6114296B2 (enExample) |
| CN (3) | CN104080786A (enExample) |
| CA (1) | CA2854926A1 (enExample) |
| HK (1) | HK1201828A1 (enExample) |
| WO (1) | WO2013070976A1 (enExample) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2793893A4 (en) * | 2011-11-23 | 2015-07-08 | Intellikine Llc | IMPROVED TREATMENT REGIMES USING MTOR INHIBITORS |
| CN104250250A (zh) * | 2013-06-25 | 2014-12-31 | 苏州科捷生物医药有限公司 | 4-芳香胺基嘧啶类化合物及其抗肿瘤用途 |
| WO2015069217A1 (en) * | 2013-11-05 | 2015-05-14 | Baylor College Of Medicine | Src kinase inhibition as treatment for lympangioleiomyomatosis and tuberous sclerosis |
| WO2015073274A1 (en) * | 2013-11-13 | 2015-05-21 | Albert Einstein College Of Medicine Of Yeshiva University | Wnt/beta-catenin inhibitor-eluting endovascular stent |
| US10118890B2 (en) | 2014-10-10 | 2018-11-06 | The Research Foundation For The State University Of New York | Trifluoromethoxylation of arenes via intramolecular trifluoromethoxy group migration |
| ES2803581T3 (es) * | 2014-10-29 | 2021-01-28 | Walter & Eliza Hall Inst Medical Res | Inhibidores de Mcl-1 para su uso en el tratamiento de enfermedades provocadas por neovascularización patológica |
| CA2971687C (en) | 2014-12-30 | 2024-05-28 | University Of Iowa Research Foundation | Methods and compositions for treating brain diseases |
| CA3037469C (en) * | 2015-09-24 | 2024-04-16 | Drexel University | Treatment of dermal disorders comprising a mtorc1 inhibitor |
| DK3417294T3 (da) * | 2016-02-15 | 2022-02-21 | Astrazeneca Ab | Fremgangsmåder, som omfatter fast intermitterende dosering af cediranib |
| US11103159B2 (en) * | 2016-03-04 | 2021-08-31 | United States Of America As Represented By The Secretary Of The Air Force | Exhaled breath hypoxia biomarkers |
| TWI753892B (zh) | 2016-03-28 | 2022-02-01 | 美商英塞特公司 | 作為ｔａｍ抑制劑之吡咯并三嗪化合物 |
| CN115650985B (zh) | 2016-04-15 | 2024-08-02 | 癌症研究科技有限公司 | 作为ret激酶抑制剂的杂环化合物 |
| WO2017178845A1 (en) | 2016-04-15 | 2017-10-19 | Cancer Research Technology Limited | Heterocyclic compounds as ret kinase inhibitors |
| CN107513068A (zh) * | 2016-06-16 | 2017-12-26 | 中国科学院上海药物研究所 | 一种具有fgfr抑制活性的新型化合物及其制备和应用 |
| GB201705971D0 (en) | 2017-04-13 | 2017-05-31 | Cancer Res Tech Ltd | Inhibitor compounds |
| US11253594B2 (en) * | 2017-07-07 | 2022-02-22 | University Of Pittsburgh-Of The Commonwealth System Of Higher Education | Drug combinations for protecting against neuronal cell death |
| CN109298169B (zh) * | 2018-09-21 | 2022-04-15 | 中国农业科学院兰州畜牧与兽药研究所 | 抗奶牛子宫内膜炎药物的筛选方法、细胞模型及用途 |
| CN111454268B (zh) * | 2019-01-18 | 2023-09-08 | 明慧医药（上海）有限公司 | 作为布鲁顿酪氨酸激酶抑制剂的环状分子 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0600618D0 (en) * | 2006-01-12 | 2006-02-22 | Novartis Ag | Organic compounds |
| EP1880723A1 (en) * | 2006-07-14 | 2008-01-23 | Novartis AG | Combination of mTOR inhibitor and antifolate compound |
| JP2010503696A (ja) * | 2006-09-13 | 2010-02-04 | ヌベロ， インコーポレイテッド | 癌を処置するための方法 |
| US20110195966A1 (en) * | 2008-10-31 | 2011-08-11 | Novartis Ag | Combination of a phosphatidylinositol-3-kinase (pi3k) inhibitor and a mtor inhibitor |
| US8476431B2 (en) * | 2008-11-03 | 2013-07-02 | Itellikine LLC | Benzoxazole kinase inhibitors and methods of use |
| JP2013502421A (ja) * | 2009-08-21 | 2013-01-24 | マウント シナイ スクール オブ メディシン オブ ニューヨーク ユニバーシティー | 癌治療のためのｃｄ４４融合タンパク質の使用方法 |
| AU2010322105B2 (en) * | 2009-11-17 | 2014-05-08 | Novartis Ag | Combination |
| SG2014009492A (en) * | 2011-08-11 | 2014-09-26 | Intellikine Llc | Kinase inhibitor polymorphs |
| KR102229478B1 (ko) * | 2012-11-01 | 2021-03-18 | 인피니티 파마슈티칼스, 인코포레이티드 | Pi3 키나아제 동형단백질 조절인자를 사용하는 암의 치료 |
-
2012
- 2012-11-08 CA CA2854926A patent/CA2854926A1/en not_active Abandoned
- 2012-11-08 CN CN201280066443.XA patent/CN104080786A/zh active Pending
- 2012-11-08 CN CN201710256289.7A patent/CN106924741A/zh active Pending
- 2012-11-08 CN CN201710256328.3A patent/CN106994126A/zh active Pending
- 2012-11-08 US US14/357,134 patent/US20140377285A1/en not_active Abandoned
- 2012-11-08 JP JP2014541274A patent/JP6114296B2/ja not_active Expired - Fee Related
- 2012-11-08 WO PCT/US2012/064239 patent/WO2013070976A1/en not_active Ceased
- 2012-11-08 HK HK15102295.1A patent/HK1201828A1/xx unknown
- 2012-11-08 EP EP12847122.4A patent/EP2776441A4/en not_active Withdrawn
-
2016
- 2016-04-15 US US15/099,731 patent/US20160287597A1/en not_active Abandoned
-
2017
- 2017-02-07 US US15/426,271 patent/US20170209448A1/en not_active Abandoned
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