JP2016512831A5 - - Google Patents
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- JP2016512831A5 JP2016512831A5 JP2016501574A JP2016501574A JP2016512831A5 JP 2016512831 A5 JP2016512831 A5 JP 2016512831A5 JP 2016501574 A JP2016501574 A JP 2016501574A JP 2016501574 A JP2016501574 A JP 2016501574A JP 2016512831 A5 JP2016512831 A5 JP 2016512831A5
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- JP
- Japan
- Prior art keywords
- acceptable salt
- pharmaceutically acceptable
- same
- compound
- compound according
- 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.)
- Pending
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- 150000001875 compounds Chemical class 0.000 claims description 30
- 150000003839 salts Chemical class 0.000 claims description 17
- 201000010099 disease Diseases 0.000 claims description 12
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 12
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 10
- 239000003814 drug Substances 0.000 claims description 10
- 229910052739 hydrogen Inorganic materials 0.000 claims description 10
- 239000001257 hydrogen Substances 0.000 claims description 10
- 229940124597 therapeutic agent Drugs 0.000 claims description 10
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims description 9
- 229910052805 deuterium Inorganic materials 0.000 claims description 9
- 206010028980 Neoplasm Diseases 0.000 claims description 7
- 239000008194 pharmaceutical composition Substances 0.000 claims description 6
- 206010006187 Breast cancer Diseases 0.000 claims description 4
- 208000026310 Breast neoplasm Diseases 0.000 claims description 4
- 206010009944 Colon cancer Diseases 0.000 claims description 4
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims description 4
- 208000025205 Mantle-Cell Lymphoma Diseases 0.000 claims description 4
- 208000034578 Multiple myelomas Diseases 0.000 claims description 4
- 206010035226 Plasma cell myeloma Diseases 0.000 claims description 4
- 125000000217 alkyl group Chemical group 0.000 claims description 4
- 125000003118 aryl group Chemical group 0.000 claims description 4
- GXJABQQUPOEUTA-RDJZCZTQSA-N bortezomib Chemical compound C([C@@H](C(=O)N[C@@H](CC(C)C)B(O)O)NC(=O)C=1N=CC=NC=1)C1=CC=CC=C1 GXJABQQUPOEUTA-RDJZCZTQSA-N 0.000 claims description 4
- 229960001467 bortezomib Drugs 0.000 claims description 4
- 201000011510 cancer Diseases 0.000 claims description 4
- 125000002947 alkylene group Chemical group 0.000 claims description 3
- 230000000155 isotopic effect Effects 0.000 claims description 3
- 206010000830 Acute leukaemia Diseases 0.000 claims description 2
- 208000023275 Autoimmune disease Diseases 0.000 claims description 2
- 206010020751 Hypersensitivity Diseases 0.000 claims description 2
- 206010033128 Ovarian cancer Diseases 0.000 claims description 2
- 206010061535 Ovarian neoplasm Diseases 0.000 claims description 2
- 229930012538 Paclitaxel Natural products 0.000 claims description 2
- 208000026935 allergic disease Diseases 0.000 claims description 2
- 230000007815 allergy Effects 0.000 claims description 2
- 229960002932 anastrozole Drugs 0.000 claims description 2
- YBBLVLTVTVSKRW-UHFFFAOYSA-N anastrozole Chemical compound N#CC(C)(C)C1=CC(C(C)(C#N)C)=CC(CN2N=CN=C2)=C1 YBBLVLTVTVSKRW-UHFFFAOYSA-N 0.000 claims description 2
- UREBDLICKHMUKA-CXSFZGCWSA-N dexamethasone Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@@H](C)[C@@](C(=O)CO)(O)[C@@]1(C)C[C@@H]2O UREBDLICKHMUKA-CXSFZGCWSA-N 0.000 claims description 2
- 229960003957 dexamethasone Drugs 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 208000005017 glioblastoma Diseases 0.000 claims description 2
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims description 2
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims description 2
- 229960003881 letrozole Drugs 0.000 claims description 2
- HPJKCIUCZWXJDR-UHFFFAOYSA-N letrozole Chemical compound C1=CC(C#N)=CC=C1C(N1N=CN=C1)C1=CC=C(C#N)C=C1 HPJKCIUCZWXJDR-UHFFFAOYSA-N 0.000 claims description 2
- 206010024627 liposarcoma Diseases 0.000 claims description 2
- DWAFYCQODLXJNR-BNTLRKBRSA-L oxaliplatin Chemical compound O1C(=O)C(=O)O[Pt]11N[C@@H]2CCCC[C@H]2N1 DWAFYCQODLXJNR-BNTLRKBRSA-L 0.000 claims description 2
- 229960001756 oxaliplatin Drugs 0.000 claims description 2
- 229960001592 paclitaxel Drugs 0.000 claims description 2
- RCINICONZNJXQF-MZXODVADSA-N taxol Chemical compound O([C@@H]1[C@@]2(C[C@@H](C(C)=C(C2(C)C)[C@H](C([C@]2(C)[C@@H](O)C[C@H]3OC[C@]3([C@H]21)OC(C)=O)=O)OC(=O)C)OC(=O)[C@H](O)[C@@H](NC(=O)C=1C=CC=CC=1)C=1C=CC=CC=1)O)C(=O)C1=CC=CC=C1 RCINICONZNJXQF-MZXODVADSA-N 0.000 claims description 2
- 238000010348 incorporation Methods 0.000 claims 2
- UFHFLCQGNIYNRP-VVKOMZTBSA-N Dideuterium Chemical compound [2H][2H] UFHFLCQGNIYNRP-VVKOMZTBSA-N 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 0 *C(*)(C(*)(*)C1(*)*)C(*)(*)C1(*)N(c(nc(Nc(cc1)ncc1N(C(*)(*)C(*)(*)N(*)C1(*)*)C1(*)*=C)nc1)c1C(*)=C1C(*)=O)C1=O Chemical compound *C(*)(C(*)(*)C1(*)*)C(*)(*)C1(*)N(c(nc(Nc(cc1)ncc1N(C(*)(*)C(*)(*)N(*)C1(*)*)C1(*)*=C)nc1)c1C(*)=C1C(*)=O)C1=O 0.000 description 1
- 101100005789 Caenorhabditis elegans cdk-4 gene Proteins 0.000 description 1
- 201000003793 Myelodysplastic syndrome Diseases 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 239000000203 mixture Substances 0.000 description 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 description 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361787540P | 2013-03-15 | 2013-03-15 | |
| US61/787,540 | 2013-03-15 | ||
| PCT/US2014/024564 WO2014150925A2 (en) | 2013-03-15 | 2014-03-12 | Deuterated palbociclib |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2016512831A JP2016512831A (ja) | 2016-05-09 |
| JP2016512831A5 true JP2016512831A5 (OSRAM) | 2017-10-12 |
Family
ID=51581623
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016501574A Pending JP2016512831A (ja) | 2013-03-15 | 2014-03-12 | 重水素化されたパルボシクリブ |
Country Status (8)
| Country | Link |
|---|---|
| US (3) | US20160024084A1 (OSRAM) |
| EP (2) | EP2970209B1 (OSRAM) |
| JP (1) | JP2016512831A (OSRAM) |
| AU (1) | AU2014235462C1 (OSRAM) |
| CA (1) | CA2904054A1 (OSRAM) |
| EA (2) | EA032094B1 (OSRAM) |
| MX (1) | MX2015012741A (OSRAM) |
| WO (1) | WO2014150925A2 (OSRAM) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2015296322B2 (en) | 2014-07-26 | 2019-09-19 | Sunshine Lake Pharma Co., Ltd. | 2-amino-pyrido[2,3-d]pyrimidin-7(8h)-one derivatives as CDK inhibitors and uses thereof |
| CN105111201B (zh) * | 2014-10-16 | 2017-01-11 | 上海页岩科技有限公司 | 5-甲基-2-(吡啶-2-基氨基)-8H-吡啶并[2,3-d]嘧啶-7-酮化合物 |
| WO2016092442A1 (en) * | 2014-12-08 | 2016-06-16 | Sun Pharmaceutical Industries Limited | Processes for the preparation of crystalline forms of palbociclib acetate |
| CN104892604B (zh) * | 2015-06-19 | 2016-08-24 | 北京康立生医药技术开发有限公司 | 一种cdk4抑制剂的合成方法 |
| CN105153149B (zh) * | 2015-07-29 | 2017-09-19 | 江苏中邦制药有限公司 | 一种选择性激酶抑制剂Palbociclib的制备方法 |
| EP3386981B1 (en) * | 2015-12-13 | 2021-10-13 | Hangzhou Innogate Pharma Co., Ltd. | Heterocycles useful as anti-cancer agents |
| CN106986871B (zh) * | 2017-03-29 | 2019-02-26 | 浙江同源康医药股份有限公司 | 一种氘代Palbociclib的晶型及其制备方法和应用 |
| CN106967064B (zh) * | 2017-03-29 | 2018-03-23 | 郑州泰基鸿诺医药股份有限公司 | 氘代Palbociclib的衍生物、制备方法及其应用 |
| SG11202100429TA (en) | 2018-07-27 | 2021-02-25 | California Inst Of Techn | Cdk inhibitors and uses thereof |
| WO2020114519A1 (zh) * | 2018-12-07 | 2020-06-11 | 杭州英创医药科技有限公司 | 作为cdk-hdac双通路抑制剂的杂环化合物 |
| WO2021113595A1 (en) * | 2019-12-06 | 2021-06-10 | Beta Pharma, Inc. | Phosphorus derivatives as kras inhibitors |
| LV15575A (lv) | 2019-12-20 | 2021-06-20 | Latvijas Organiskās Sintēzes Institūts | Selenofēnhromēnu deiterēti analogi, to iegūšana un izmantošana |
Family Cites Families (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5304121A (en) | 1990-12-28 | 1994-04-19 | Boston Scientific Corporation | Drug delivery system making use of a hydrogel polymer coating |
| US5994341A (en) | 1993-07-19 | 1999-11-30 | Angiogenesis Technologies, Inc. | Anti-angiogenic Compositions and methods for the treatment of arthritis |
| US6099562A (en) | 1996-06-13 | 2000-08-08 | Schneider (Usa) Inc. | Drug coating with topcoat |
| TW354293B (en) | 1995-06-06 | 1999-03-11 | Bristol Myers Squibb Co | Prodrugs of paclitaxel derivatives |
| GB9925962D0 (en) | 1999-11-02 | 1999-12-29 | Novartis Ag | Organic compounds |
| CN1255185C (zh) | 2001-05-03 | 2006-05-10 | 弗·哈夫曼-拉罗切有限公司 | 无定形甲磺酸奈非那韦的药物剂型 |
| CA2446904A1 (en) | 2001-05-24 | 2003-04-03 | Alexza Molecular Delivery Corporation | Delivery of drug esters through an inhalation route |
| JP4291696B2 (ja) * | 2002-01-22 | 2009-07-08 | ワーナー−ランバート カンパニー リミテッド ライアビリティー カンパニー | ２−（ピリジン−２−イルアミノ）−ピリド［２，３−ｄ］ピリミジン−７−オン |
| JP4053073B2 (ja) * | 2003-07-11 | 2008-02-27 | ワーナー−ランバート カンパニー リミテッド ライアビリティー カンパニー | 選択的ｃｄｋ４阻害剤のイセチオン酸塩 |
| WO2006039237A1 (en) | 2004-09-29 | 2006-04-13 | Cordis Corporation | Pharmaceutical dosage forms of stable amorphous rapamycin like compounds |
| CN102516176A (zh) | 2005-10-28 | 2012-06-27 | 雅培制药有限公司 | 抑制trpv1受体的吲唑衍生物 |
| AU2007297286A1 (en) * | 2006-09-08 | 2008-03-20 | Pfizer Products Inc. | Synthesis of 2-(pyridin-2-ylamino)-pyrido[2,3-d]pyrimidin-7-ones |
| JP2010513317A (ja) | 2006-12-14 | 2010-04-30 | パナシー ファーマシューティカルズ インコーポレーティッド | サイクリン依存性キナーゼの阻害による神経保護方法 |
| US20090030005A1 (en) | 2007-07-19 | 2009-01-29 | Amgen Inc. | Combinations for the treatment of cancer |
| US9259399B2 (en) | 2007-11-07 | 2016-02-16 | Cornell University | Targeting CDK4 and CDK6 in cancer therapy |
| EP2242493B1 (en) * | 2008-01-22 | 2013-06-05 | Concert Pharmaceuticals Inc. | Derivatives of gefitinib |
| CA2738925A1 (en) | 2008-10-01 | 2010-04-08 | The University Of North Carolina At Chapel Hill | Hematopoietic protection against chemotherapeutic compounds using selective cyclin-dependent kinase 4/6 inhibitors |
| JP2012504645A (ja) | 2008-10-01 | 2012-02-23 | ザ ユニバーシティ オブ ノース カロライナ アット チャペル ヒル | 健康な細胞に対する電離放射線の影響を低下させる又は防止するための医薬組成物 |
| EP3718560A3 (en) | 2009-05-13 | 2020-12-09 | The University of North Carolina at Chapel Hill | Cyclin dependent kinase inhibitors and methods of use |
| UY33226A (es) * | 2010-02-19 | 2011-09-30 | Novartis Ag | Compuestos de pirrolopirimidina deuterada como inhibidores de la cdk4/6 |
| US20130035336A1 (en) | 2010-04-13 | 2013-02-07 | Novartis Ag | Combination comprising a cyclin dependent kinase 4 or cyclin dependent kinase (cdk4/6) inhibitor for treating cancer |
| CN101967142B (zh) * | 2010-05-17 | 2012-05-30 | 苏州波锐生物医药科技有限公司 | 噻唑酰胺类化合物及其在治疗恶性肿瘤中的药物用途 |
| US9808461B2 (en) | 2010-11-17 | 2017-11-07 | The University Of North Carolina At Chapel Hill | Protection of renal tissues from ischemia through inhibition of the proliferative kinases CDK4 and CDK6 |
-
2014
- 2014-03-12 JP JP2016501574A patent/JP2016512831A/ja active Pending
- 2014-03-12 WO PCT/US2014/024564 patent/WO2014150925A2/en not_active Ceased
- 2014-03-12 EP EP14769343.6A patent/EP2970209B1/en active Active
- 2014-03-12 MX MX2015012741A patent/MX2015012741A/es unknown
- 2014-03-12 EA EA201591628A patent/EA032094B1/ru not_active IP Right Cessation
- 2014-03-12 EA EA201892726A patent/EA201892726A1/ru unknown
- 2014-03-12 AU AU2014235462A patent/AU2014235462C1/en not_active Ceased
- 2014-03-12 CA CA2904054A patent/CA2904054A1/en not_active Abandoned
- 2014-03-12 US US14/775,854 patent/US20160024084A1/en not_active Abandoned
- 2014-03-12 EP EP18205631.7A patent/EP3492470A1/en not_active Withdrawn
-
2017
- 2017-06-29 US US15/636,976 patent/US20180051022A1/en not_active Abandoned
-
2018
- 2018-11-13 US US16/189,304 patent/US20190225605A1/en not_active Abandoned
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