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 (enExample) | 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 (enExample) |
| EP (2) | EP3492470A1 (enExample) |
| JP (1) | JP2016512831A (enExample) |
| AU (1) | AU2014235462C1 (enExample) |
| CA (1) | CA2904054A1 (enExample) |
| EA (2) | EA032094B1 (enExample) |
| MX (1) | MX2015012741A (enExample) |
| WO (1) | WO2014150925A2 (enExample) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2016015597A1 (en) | 2014-07-26 | 2016-02-04 | Sunshine Lake Pharma Co., Ltd. | Compounds as cdk small-molecule 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 |
| WO2017101763A1 (en) | 2015-12-13 | 2017-06-22 | Hangzhou Innogate Pharma Co., Ltd. | Heterocycles useful as anti-cancer agents |
| 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 |
| 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 |
| WO2020023917A1 (en) | 2018-07-27 | 2020-01-30 | California Institute Of Technology | Cdk inhibitors and uses thereof |
| US12358911B2 (en) | 2018-12-07 | 2025-07-15 | Hangzhou Innogate Pharma Co., Ltd. | Heterocyclic comipound as CDK-HDAC dual pathway inhibitor |
| 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 |
| CZ20033211A3 (cs) | 2001-05-03 | 2004-09-15 | F. Hoffmann-La Roche Ag | Farmaceutická léková forma amorfního nelfinavir mesylátu |
| CA2446904A1 (en) | 2001-05-24 | 2003-04-03 | Alexza Pharmaceuticals, Inc. | Delivery of drug esters through an inhalation route |
| NZ534069A (en) | 2002-01-22 | 2007-03-30 | Warner Lambert Co | 2-(Pyridin-2-ylamino)-pyrido[2,3-d]pyrimidin-7-ones to be used to treat neurodegenerative disorders, viruses and cancer |
| DE602004017474D1 (de) * | 2003-07-11 | 2008-12-11 | Warner Lambert Co | Isethionat salz eines selektiven cdk4 inhibitors |
| WO2006039237A1 (en) | 2004-09-29 | 2006-04-13 | Cordis Corporation | Pharmaceutical dosage forms of stable amorphous rapamycin like compounds |
| AU2006306146A1 (en) | 2005-10-28 | 2007-05-03 | Abbott Laboratories | Indazole derivatives that inhibit TRPV1 receptor |
| KR20090052385A (ko) * | 2006-09-08 | 2009-05-25 | 화이자 프로덕츠 인크. | 2-（피리딘-2-일아미노）-피리도［2,3-ｄ］피리미딘-7-온의합성 |
| CA2672898A1 (en) | 2006-12-14 | 2008-06-26 | Panacea Pharmaceuticals, Inc. | Methods of neuroprotection by cyclin-dependent kinase inhibition |
| WO2009014642A1 (en) | 2007-07-19 | 2009-01-29 | Amgen Inc. | Combination of a de novo purine biosynthesis inhibitor and a cyclin dependent kinase inhibitor for the treatment of cancer |
| US9259399B2 (en) | 2007-11-07 | 2016-02-16 | Cornell University | Targeting CDK4 and CDK6 in cancer therapy |
| US7855204B2 (en) * | 2008-01-22 | 2010-12-21 | Concert Pharmaceuticals Inc. | Derivatives of gefitinib |
| WO2010039997A2 (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 |
| AU2009310352A1 (en) | 2008-10-01 | 2010-05-06 | The University Of North Carolina At Chapel Hill | Hematopoietic protection against ionizing radiation using selective cyclin-dependent kinase 4/6 inhibitors |
| EP3025724B1 (en) | 2009-05-13 | 2018-07-11 | 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 |
| WO2012068381A2 (en) | 2010-11-17 | 2012-05-24 | The University Of North Carolina At Chapel Hill | Protection of renal tissues from schema through inhibition of the proliferative kisses cdk4 and cdk6 |
-
2014
- 2014-03-12 JP JP2016501574A patent/JP2016512831A/ja active Pending
- 2014-03-12 AU AU2014235462A patent/AU2014235462C1/en not_active Ceased
- 2014-03-12 EA EA201591628A patent/EA032094B1/ru not_active IP Right Cessation
- 2014-03-12 EP EP18205631.7A patent/EP3492470A1/en not_active Withdrawn
- 2014-03-12 WO PCT/US2014/024564 patent/WO2014150925A2/en not_active Ceased
- 2014-03-12 EA EA201892726A patent/EA201892726A1/ru unknown
- 2014-03-12 CA CA2904054A patent/CA2904054A1/en not_active Abandoned
- 2014-03-12 MX MX2015012741A patent/MX2015012741A/es unknown
- 2014-03-12 US US14/775,854 patent/US20160024084A1/en not_active Abandoned
- 2014-03-12 EP EP14769343.6A patent/EP2970209B1/en active Active
-
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